Benzonatate side effects 200 mg: Benzonatate: Uses, Side Effects, Dosage, Warnings

29.08.197025.07.2021 by alexxlab

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What to Know About Benzonatate

Benzonatate is a prescription non-narcotic antitussive used to relieve a cough. It works by relaxing the cough reflex in your airways. It can be used to treat a new-onset cough from viruses like the flu or the common cold.

Benzonatate comes in a capsule and a liquid-filled capsule. Common brand names include Tessalon and Zonatuss. Generic benzonatate is also available.

Mallika Wiriyathitipirn / EyeEm / Getty Images

Uses

Benzonatate is used to temporarily relieve a cough, but cannot cure a respiratory illness. Your doctor may prescribe it for a limited amount of time. Benzonatate is not meant to be used for a chronic cough from asthma or smoking.

Benzonatate works by relaxing the cough reflex in your lungs and airways. This is especially helpful for a cough that keeps you up at night.

Before Taking

Before this drug is prescribed for a cough, your doctor will determine if the possible benefits outweigh the risks. Your doctor will probably ask if your cough is productive, which means that when you cough into a tissue, mucus or phlegm comes out.

Benzonatate makes you cough less and should not be used for a cough that produces a large amount of mucus or phlegm. That is because reducing your cough could cause mucus to build up in your lungs, putting you at risk for serious respiratory illnesses and trouble breathing.

Talk to your doctor about all medications, supplements, and vitamins that you currently take. While some drugs pose minor interaction risks, others may outright contraindicate use or prompt careful consideration as to whether the pros of treatment outweigh the cons in your case.

Precautions and Contraindications

Benzonatate should not be used in children under 10 years old. If this medication is being prescribed for your child, ask your doctor about safer options.

Your doctor will ask what medications and supplements you are currently taking. Benzonatate can interact with a long list of medications, including psychiatric medications. A small number of patients have reported confusion and visual hallucinations while taking Benzonatate with their other prescribed drugs.

Benzonatate should not be used in patients with allergies to Novocaine or tetracaine, because those are included in the capsule.

If you are pregnant, breastfeeding, or have surgery coming up, your doctor may look into an alternate option to help control your cough.

Other Cough Suppressants

In addition to benzonatate, the most common prescription antitussives include:

Over-the-counter cough suppressants are also available, including:

Dosage

Benzonatate comes in liquid-filled capsules and can be taken up to three times per day. The capsules should always be swallowed whole and never crushed, chewed, or dissolved. If you do this, you will lose feeling in your mouth and throat, and it may cause you to choke or have a severe allergic reaction.

According to the manufacturer, dosing should be as follows. Your doctor will most likely start you at a dose of a 100 milligram (mg) capsule up to three times per day as needed for a cough. Your doctor may increase your dose to a 200 mg capsule up to three times per day as needed, for a total of 600 mg per day.

All listed dosages are according to the drug manufacturer. Check your prescription and talk to your doctor to make sure you are taking the right dose for you.

How to Take and Store

Because benzonatate capsules contain Novocaine, they should never be cut open or chewed. Novocaine is the numbing agent you have probably had at the dentist. It can quickly numb your mouth, and this could put you at risk for choking or trouble breathing.

If you notice a numbing sensation in your mouth or throat after taking benzonatate, let your doctor know right away and don’t attempt to eat or drink anything until feeling in your throat returns to normal.

Benzonatate can be taken with food or on an empty stomach. If you miss a dose, skip the missed dose and wait until your next scheduled time. Never double up on dosages.

The capsules should be kept in a cool, dry room, avoiding humid rooms like the bathroom.

Benzonatate can be deadly in children under 10 years old, so it is critical that you keep the prescription bottle sealed and on a high shelf out of their reach. Keep the bottle out of sight, as children may be curious about the liquid-filled capsules.

The best way to dispose of extra medication once you no longer need it is with a prescription take-back program at your local pharmacy or health department. Avoid placing unused capsules in the garbage or flushing them down the toilet.

Side Effects

Common

Most side effects of Benzonatate are mild and uncommon. Possible side effects include:

Constipation
Dizziness
Drowsiness
Headache
Nausea
Stuffy nose
Stomach upset

This drug may make you drowsy or dizzy. It is best to avoid alcohol or marijuana while taking benzonatate.

Severe

Severe side effects are possible from hypersensitivity reactions, drug interactions, or a damaged capsule. Call your doctor right away if you experience any of the following side effects:

Confusion
Hallucination
Itchy rash or hives
Numbness in the mouth, throat, or chest
Tightening of the throat
Trouble breathing or swallowing

Overdose Warning

A benzonatate overdose can happen quickly. Symptoms can appear within 15 minutes, and death has been reported within an hour. Symptoms of an overdose may include:

Restlessness
Tremors
Seizures
Loss of consciousness

If you or your child experience any of these overdose symptoms, call 911 immediately.

Warnings and Interactions

Benzonatate should be used with caution in patients who:

Are pregnant or breastfeeding
Have a chronic cough
Have a productive cough
Have a history of hallucinations
Are current smokers

Warnings

Benzonatate can be taken up to three times per day as needed for a cough. Do not take your next dose if your cough is controlled. If after taking Benzonatate for seven days you still experience a cough, talk with your doctor.

This medication should be used to treat an acute cough for a limited amount of time. If your cough is not improving after one week, your doctor may need to examine you again.

If you develop a fever, rash, or new-onset headache while taking benzonatate, stop the medication and call your doctor. This could be a sign that you have other medical conditions that need to be addressed.

Benzonatate can cause overdose and death in children under 10 years old with only one or two doses. Keep the medication out of reach of children and never give your child a capsule of Benzonatate.

Benzonatate (benzonatate) dose, indications, adverse effects, interactions… from PDR.net

CLASSES

Non-Opioid Antitussives

DESCRIPTION

Oral nonnarcotic antitussive agent; chemically related to the ester-type local anesthetics; effective in suppressing cough particularly in cases of chronic cough resistant to opiate agonists; off-label use includes topical application to the oropharynx to obliterate the gag reflex prior to intubation or endoscopy.

COMMON BRAND NAMES

Tessalon Perles, Zonatuss

HOW SUPPLIED

Benzonatate/Tessalon Perles/Zonatuss Oral Cap: 100mg, 150mg, 200mg

DOSAGE & INDICATIONS

For the symptomatic treatment of cough.

Oral dosage

Adults, Adolescents and Children 10 years and older

100 mg, 150 mg, or 200 mg PO 3 times daily is the normal dosage. Maximum dosage is 600 mg/day PO.

For the treatment of intractable singultus (hiccups)† unresponsive to standard therapies.

Oral dosage

Adults, Adolescents and Children 10 years and older

Anecdotal reports suggest a dosage of 100 mg PO as a single dose. May repeat in 4 hours if needed. Dose of 100 mg PO may be given up to every 4 hours; do not exceed 600 mg/day PO.

For topical anesthesia† of the oropharyngeal region prior to awake endotracheal intubation† or prior to endoscopy†.
NOTE: This route should only be used by health care professionals trained in anesthesia and intubation. Specialized references should be consulted for specific procedures and administration techniques. Resuscitative equipment and drugs used in the management of adverse reactions should be immediately available.

Oropharyngeal topical dosage†

Adults

A dose of 200 mg applied topically to the oropharyngeal area, followed by 4% lidocaine translaryngeally has been used. This route should only be used by those trained in anesthesia and intubation. In 1 study, a shorter time period was required to obtain the loss of gag reflex in the benzonatate-treated group (i.e., roughly 1 minute) vs. the 5 to 6 minutes required in those patients receiving superior laryngeal nerve block with 1% lidocaine.

†Indicates off-label use

MAXIMUM DOSAGE

Adults

600 mg/day PO.

Geriatric

600 mg/day PO.

Adolescents

600 mg/day PO.

Children

10 years and older: 600 mg/day PO.
9 years and younger: Safety and efficacy have not been established.

Infants

Safety and efficacy have not been established.

Neonates

Safety and efficacy have not been established.

DOSING CONSIDERATIONS

Hepatic Impairment

Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

Renal Impairment

Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

ADMINISTRATION

Oral Administration

Oral Solid Formulations

Swallow whole. Do not break, chew, or dissolve in the mouth as this could cause temporary anesthesia of the mouth and throat and could cause choking.

STORAGE

Generic:
– Protect from light
– Store at controlled room temperature (between 68 and 77 degrees F)
Tessalon Perles:
– Avoid excessive humidity
– Do not freeze
– Protect from light
– Protect from moisture
– Store at controlled room temperature (between 68 and 77 degrees F)
Zonatuss :
– Protect from light
– Store at controlled room temperature (between 68 and 77 degrees F)

CONTRAINDICATIONS / PRECAUTIONS

Ester local anesthetic hypersensitivity, paraben hypersensitivity

Benzonatate is chemically related to tetracaine and other ester-type local anesthetics. Use of benzonatate is contraindicated in those patients with ester local anesthetic hypersensitivity or a previous history of reaction to benzonatate. The benzonatate formulation also contains methyl- and propylparaben; these may be a problem for patients with paraben hypersensitivity. Severe hypersensitivity reactions have been reported with benzonatate use. In some cases local anesthesia resulting from the sucking or chewing of the capsule has been responsible for bronchospasm or laryngospasm. Patients should always swallow benzonatate capsules whole, do not chew or dissolve in the mouth.

Children, infants, neonates, potential for overdose or poisoning

Children 10 years of age or older may receive benzonatate with careful administration instructions to avoid chewing or dissolving the dose in the mouth. Safe and effective use of benzonatate has not been established in neonates, infants, or children under the age of 10 years. Accidental ingestion of benzonatate liquid capsules poses a significant potential for overdose or poisoning to pediatric patients younger than 10 years of age due in part to the candy-like appearance. Signs and symptoms of overdose have been reported within 15 to 20 minutes, and death has been reported within one hour of ingestion. Advise patients to store this medication out of reach of children in a child-resistant container and to seek medical help immediately if accidental ingestion is suspected. The Adverse Event Reporting System database of the FDA includes 7 cases of accidental pediatric exposure reported between 1982 and May 2010, including 5 deaths in children less than 2 years of age. Overdose has occurred in children under 2 years after accidental ingestion of one or two benzonatate capsules. In addition, the benzonatate dosage form could represent a choking hazard to young children.

Driving or operating machinery

Benzonatate is occasionally associated with CNS sedation, mental confusion, visual hallucinations or other bizarre behaviors. Patients should be advised to use caution with driving or operating machinery or performing other activities requiring mental alertness until they know how this medication affects them. Concomitant medications could increase the risk of these types of adverse reactions.

Labor, obstetric delivery, pregnancy

Benzonatate is classified as FDA pregnancy risk category C. Animal studies to evaluate carcinogenic and mutagenic potential and effect on gestation and fertility have not been performed. Due to a lack of available data on the safety of benzonatate during pregnancy, the drug should be administered to a pregnant woman only if clearly needed. The effects of benzonatate during labor and obstetric delivery are unknown. However, benzonatate is chemically related to anesthetic agents such as procaine and similar effects could be observed if enough absorption takes place. Local anesthetics rapidly cross the placenta and can cause varying degrees of maternal, fetal, and neonatal toxicity when used for paracervical or pudendal block anesthesia during labor and delivery. The use of some local anesthetics during labor and delivery may be followed by diminished muscle strength and tone for the first day or two of life in the newborn. The long-term significance of these observations is unknown.

Breast-feeding

According to the manufacturer, it is not known if benzonatate is excreted in human milk, and caution is recommended if the drug is used during breast-feeding. The effects of benzonatate on a nursing infant are unknown, and the American Academy of Pediatrics (AAP) has not issued any specific recommendations relating to benzonatate and breast-feeding. Because no breast-feeding information is available, an alternate anti-tussive may be preferred, especially while nursing a newborn or premature infant. Despite the lack of published data, some experts consider dextromethorphan to be compatible with breast-feeding when usual adult doses are taken by the mother. Dextromethorphan products containing alcohol should be avoided. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.

Para-aminobenzoic acid, PABA hypersensitivity

Cautious use of benzonatate may be warranted for patients with para-aminobenzoic acid, PABA hypersensitivity. Benzonatate is chemically related to anesthetic agents of the para-aminobenzoic acid class such as procaine and tetracaine. Benzonatate has been associated with adverse CNS effects possibly related to a prior sensitivity to related agents or to an interaction with concomitant medication.

Dysphagia, geriatric

Geriatric patients taking benzonatate should be able to swallow the capsules as directed, as inadvertant release of capsule contents in the mouth can produce a temporary local anesthesia of the oral mucosa and choking or other serious side effects could occur. The medication is advised to be avoided if dysphagia is present. The federal Omnibus Budget Reconciliation Act (OBRA) regulates medication use in residents (e.g., geriatric adults) of long-term care facilities. According to the OBRA guidelines, cough medications should be used only for a limited duration (less than 14 days) unless there is documented evidence of enduring symptoms that cannot otherwise be alleviated and for which a cause cannot be identified and corrected.

ADVERSE REACTIONS

Severe

laryngospasm / Rapid / Incidence not known
anaphylactoid reactions / Rapid / Incidence not known
bronchospasm / Rapid / Incidence not known

Moderate

constipation / Delayed / Incidence not known
dysphagia / Delayed / Incidence not known
hypotension / Rapid / Incidence not known
confusion / Early / Incidence not known
hallucinations / Early / Incidence not known

Mild

nausea / Early / Incidence not known
rash / Early / Incidence not known
pruritus / Rapid / Incidence not known
drowsiness / Early / Incidence not known
dizziness / Early / Incidence not known
headache / Early / Incidence not known
ocular irritation / Rapid / Incidence not known
chills / Rapid / Incidence not known
nasal congestion / Early / Incidence not known

DRUG INTERACTIONS

Acetaminophen; Butalbital; Caffeine; Codeine: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Acetaminophen; Codeine: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Acetaminophen; Hydrocodone: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Acetaminophen; Oxycodone: (Moderate) Coadministration of oxycodone and benzonatate may result in additive CNS depression.
Acetaminophen; Propoxyphene: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Alfentanil: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Aliskiren; Amlodipine: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Amide local anesthetics: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Amlodipine: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Amlodipine; Atorvastatin: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Amlodipine; Benazepril: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Amlodipine; Celecoxib: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Amlodipine; Olmesartan: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Amlodipine; Telmisartan: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Amlodipine; Valsartan: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Amlodipine; Valsartan; Hydrochlorothiazide, HCTZ: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Articaine; Epinephrine: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Aspirin, ASA; Butalbital; Caffeine; Codeine: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Aspirin, ASA; Carisoprodol; Codeine: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Aspirin, ASA; Oxycodone: (Moderate) Coadministration of oxycodone and benzonatate may result in additive CNS depression.
Atropine; Difenoxin: (Moderate) Concurrent administration of diphenoxylate/difenoxin with benzonatate can potentiate the CNS-depressant effects of diphenoxylate/difenoxin. Use caution during coadministration.
Atropine; Diphenoxylate: (Moderate) Concurrent administration of diphenoxylate/difenoxin with benzonatate can potentiate the CNS-depressant effects of diphenoxylate/difenoxin. Use caution during coadministration.
Belladonna; Opium: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Brompheniramine; Guaifenesin; Hydrocodone: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Brompheniramine; Hydrocodone; Pseudoephedrine: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Bupivacaine Liposomal: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Bupivacaine: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Bupivacaine; Lidocaine: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Bupivacaine; Meloxicam: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Calcium-channel blockers: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Carbinoxamine; Hydrocodone; Phenylephrine: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Carbinoxamine; Hydrocodone; Pseudoephedrine: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Chloroprocaine: (Major) Caution is advised if chloroprocaine is used concurrently with other local anesthetics. The toxic effects of the drugs are additive.
Chlorpheniramine; Codeine: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Chlorpheniramine; Hydrocodone: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Chlorpheniramine; Hydrocodone; Phenylephrine: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Chlorpheniramine; Hydrocodone; Pseudoephedrine: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Chlorthalidone; Clonidine: (Moderate) Epidural clonidine may prolong the duration of action of local anesthetics, including both sensory and motor blockade.
Clevidipine: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Clonidine: (Moderate) Epidural clonidine may prolong the duration of action of local anesthetics, including both sensory and motor blockade.
Cocaine: (Moderate) The actions of benzonatate could be additive to those of other local anesthetics.
Codeine: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Codeine; Guaifenesin: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Codeine; Phenylephrine; Promethazine: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Codeine; Promethazine: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Diltiazem: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Diphenhydramine; Hydrocodone; Phenylephrine: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Enalapril; Felodipine: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Felodipine: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Guaifenesin; Hydrocodone: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Guaifenesin; Hydrocodone; Pseudoephedrine: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Homatropine; Hydrocodone: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Hydrocodone: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Hydrocodone; Ibuprofen: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Hydrocodone; Phenylephrine: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Hydrocodone; Potassium Guaiacolsulfonate: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Hydrocodone; Pseudoephedrine: (Moderate) The vagal effects and respiratory depression induced by hydrocodone may be increased by the use of benzonatate.
Hydromorphone: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Ibuprofen; Oxycodone: (Moderate) Coadministration of oxycodone and benzonatate may result in additive CNS depression.
Isradipine: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Levamlodipine: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Levobupivacaine: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Levorphanol: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Lidocaine: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Lidocaine; Prilocaine: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Magnesium Salts: (Moderate) Because of the CNS-depressant effects of magnesium sulfate, additive central-depressant effects can occur following concurrent administration with local anesthetics.
Meperidine: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Meperidine; Promethazine: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Mepivacaine: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Mepivacaine; Levonordefrin: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Monoamine oxidase inhibitors: (Major) It may be advisable to avoid the use of benzonatate, which is structurally similar to para-amino-benzoic acid class local anesthetic agents, in patients receiving a monoamine oxidase inhibitor (MAOI). Consider alternatives to benzonatate. Patients receiving an MAOI concurrently with local anesthetics may have an increased risk of hypotension or CNS-related effects. If coadministration is medically necessary, observe the patient for additive effects such as low blood pressure, sedation, dizziness, mental confusion, or other side effects. Isolated instances of bizarre behavior, including mental confusion and visual hallucinations, have also been reported in patients taking benzonatate in combination with other prescribed drugs.
Nicardipine: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Nifedipine: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Nimodipine: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Nisoldipine: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Oxycodone: (Moderate) Coadministration of oxycodone and benzonatate may result in additive CNS depression.
Oxymorphone: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Perindopril; Amlodipine: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Prilocaine: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Prilocaine; Epinephrine: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Procaine: (Major) Caution is advised if procaine is used concurrently with other local anesthetics. The toxic effects of local anesthetics are additive.
Procarbazine: (Moderate) These drugs should be prescribed with caution. It may be advisable to avoid the use of benzonatate, which is structurally similar to local anesthetic agents, in patients receiving MAOIs. Consider alternatives to benzonatate. Procarbazine is a drug with monoamine oxidase inhibitor (MAOI) activity. Use of a drug with MAOI activity with local anesthetics may increase the risk of hypotension or CNS-related effects. If co-use is medically necessary, observe the patient for additive effects such as low blood pressure, sedation, dizziness, mental confusion, or other side effects.
Propofol: (Minor) Propofol potentiates CNS depression and may enhance the sedative, respiratory depressive, and hypotensive effects of local anesthetics. A reduced dose of propofol may be needed for induction if it is used in conjunction with other medications that cause CNS depression.
Propoxyphene: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Remifentanil: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Ropivacaine: (Major) Caution is advised if amide local anesthetics are used concurrently with benzonatate. The toxic effects of local anesthetics are additive.
Saquinavir: (Major) The FDA recommends that saquinavir boosted with ritonavir should not be used in combination with other drugs that may prolong the QT interval. Benzonatate has a low, but possible risk for QT prolongation and torsades de pointes.
Sodium Sulfate; Magnesium Sulfate; Potassium Chloride: (Moderate) Because of the CNS-depressant effects of magnesium sulfate, additive central-depressant effects can occur following concurrent administration with local anesthetics.
Sufentanil: (Moderate) The vagal effects and respiratory depression induced by opiate agonists may be increased by the use of benzonatate.
Tetracaine: (Major) The actions of benzonatate could be additive to those of other local anesthetics. Benzonatate is structurally related to tetracaine, which would explain additive pharmacodynamic effects.
Trandolapril; Verapamil: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.
Vancomycin: (Moderate) The concurrent administration of vancomycin and anesthetics has been associated with erythema, histamine-like flushing, and anaphylactoid reactions.
Verapamil: (Moderate) Local anesthetics may cause additive hypotension in combination with antihypertensive agents.

PREGNANCY AND LACTATION

Pregnancy

MECHANISM OF ACTION

Benzonatate acts peripherally by anesthetizing the stretch receptors of vagal afferent fibers located in the alveoli of the lungs, the bronchi, and the pleura. The drug may also act centrally by inhibiting the transmission of the cough reflex at the level of the medulla where the vagal afferent impulse is transmitted to the motor nerves. In patients with asthma, intravenously administered benzonatate increased minute ventilation, rate and depth of respiration. However, overall lung volume and expiratory flow rate were not altered. At recommended oral dosages, benzonatate has no inhibitory effect on the respiratory center; however, in overdosage, the pharmacology of benzonatate resembles that of other ester-type local anesthetics. Clinical effects include initial CNS stimulation, which is followed by CNS depression and respiratory compromise.

When applied locally, as in the oropharynx prior to intubation or endoscopy, benzonatate acts like other local anesthetics. The drug blocks the generation and conduction of nerve impulses at the level of the cell membrane. Local anesthetics bind directly within the intracellular portion of voltage-gated sodium channels. This decreases the rate of membrane depolarization, thereby increasing the threshold for electrical excitability. The blockade affects all nerve fibers in the following sequence: autonomic, sensory, and motor, with effects diminishing in reverse order. Loss of nerve function clinically is as follows: pain, temperature, touch, proprioception, and skeletal muscle tone. Direct nerve membrane penetration is necessary for effective anesthesia, which is achieved by applying benzonatate around the nerve trunks or ganglia supplying the area to be anesthetized. Benzonatate provides anesthesia in roughly 1—2 minutes after direct topical application to the oropharynx, noticeable clinically as the loss of the gag reflex.

PHARMACOKINETICS

Benzonatate is usually administered orally. The onset of action is 15 to 20 minutes, and antitussive effects last for approximately 3—8 hours. It is assumed that benzonatate, like other ester-type local anesthetics, is hydrolyzed to para-aminobenzoic acid (PABA) by plasma esterases. However, the absorption, distribution, metabolism and excretion of benzonatate are not well characterized.

Benzonatate Toxicity: Nothing to Cough At | Journal of Analytical Toxicology

Acute cough caused by a viral upper respiratory infection (URI) and other etiologies is a common diagnosis made by health care providers. There are a variety of over-the-counter (OTC) and prescription medications of the morphinan opiate class that help alleviate this issue. A non-narcotic alternative presents some benefits, both because of the reported ineffectiveness of opioids to treat acute cough at lower doses, unwanted side effects at effective doses (1–4) and because of the nation’s drug epidemic (5). Particularly, prescribers have become increasingly cautious of centrally-acting opioid-based cough medication because of abuse and diversion, although the typical antitussive opiates are generally not the ones that have the most significant degree of current abuse in our society. Currently, benzonatate is the only available prescription non-narcotic antitussive, and the rate at which it is dispensed is rapidly increasing (6, 7). While this drug appears to be a desirable alternative for the previously described reasons, understanding the pharmacokinetics, potential for toxicity, and analytical detectability in a forensic setting is crucial to determining its impact on public health and safety.

Benzonatate (Tessalon^® Perles) was approved in 1958 as a peripherally-acting antitussive for its ability to inhibit cough before its mechanism of action was completely understood. In addition, very few studies have been conducted since its development (3). Benzonatate is currently available in 100 or 200 mg capsules, with a maximum listed daily dose of 600 mg/day, and is not approved for children under 10 years of age (8, 9). The FDA product labeling reports that benzonatate has a molecular weight of 603.7 g/mol with a side chain of nine ethoxy units. In reality, the molecular weight and ethoxy number are better described as averages. Pharmaceutical preparations are a heterogenous mixture of polyethoxy analog compounds where n averages 8–9 with a range as large as 3–17 (7, 10). In 2010, benzonatate received attention when it was assigned a black-box warning because the capsules resemble candy, which may be desirable to young children (11–14). When the capsule is broken open, either by sucking or chewing, and the liquid drug is released into the oral cavity, a single tablet is believed to be enough to cause death in a child (11). McLawhorn et al. describe fatalities in 20 of the 31 overdose cases reported to the FDA Adverse Event Reporting System (AERS), recognizing a rapid onset of symptoms (within 1 h) and a relatively low margin for safety (6).

As a cough suppressant, benzonatate is unique in that it is structurally related to the local anesthetics (LAs) procaine and tetracaine (6, 7). Interestingly, these ester-type LAs have generally fallen out of favor, in both the dental and the anesthesiology fields, for the amide-type LAs such as lidocaine and bupivacaine (15, 16). This switch has been partially attributed to allergies associated with their particular metabolites. Unusual reactions to p-aminobenzoic acid (PABA)-derived ester-based LAs have been associated with these underlying allergies; however, the incidence of true IgE-mediated reactions is unknown and presumed to be rare (15–18). Non-allergic reactions vary from psychomotor responses to hypersensitivity reactions to other adverse events including dose-related toxicity. Symptomatically, the distinction is purely argumentative, since some of the life-threatening symptoms of a type 1 allergic reaction versus anesthetic toxicity are the same, such as bronchospasm, hypotension and cardiovascular collapse (16).

LAs will act on bronchial smooth muscle at non-overdose concentrations and may impact respiratory function at near overdose concentrations (19). Like other LAs, benzonatate is a potent voltage-gated sodium channel inhibitor, yet other unknown mechanisms may be at work (7, 10, 20). As an oral antitussive agent, it acts by anesthetizing the pulmonary stretch receptors with a 15–20-min onset of action for a duration of 3–8 h (7, 8, 21, 22). Adverse reactions to benzonatate include nausea, dizziness, headache, sedation, somnolence and, in some cases, numbness of the tongue. Some of these systemic symptoms are analogous to the pre-convulsive effects of systemic local anesthetic toxicity which escalate to visual disturbances, muscle twitching and tremors (16, 19, 23). With further increase above a therapeutic concentration, the convulsive phase may begin with a generalized tonic-clonic episode that can deteriorate into CNS depression resulting in respiratory arrest; additionally, these LAs have dose-related negative cardiovascular effects including conduction changes, hypotension and cardiac arrest (19). Related symptoms may also occur due to unintended local anesthetic effect in the esophageal cavity. When a therapeutic dose, administered as a single capsule, is chewed or crushed, there is potential for bronchospasm, laryngospasm, seizures and cardiovascular collapse which mimics the systemic toxicity seen at high doses (6, 15, 19, 20).

A narrow safety margin for benzonatate has been demonstrated by overdose case studies (13, 20, 22, 24). In several of the published over-ingestion cases, as well as those observed in our office, only a small handful of pills was enough to cause seizures, a cardiac event and death. Interestingly, the product insert directs one to not double up a missed dose of benzonatate and only take a maximum of 200 mg at a time. Blood data is inconclusive or unavailable in the majority of death cases (6, 10), however fatalities have been reported with blood concentrations of 5 and 35 mg/L (9, 22). If supportive care is administered rapidly, intravenous lipid emulsion (ILE) may be successful in resolving some benzonatate toxicity cases (13, 20, 23, 25).

Benzonatate is analytically problematic and will be underestimated in forensic laboratory reports because of the chemical and pharmacological make-up of this prescription product. Details obtained through investigation by the medical examiner helped to support the possibility of benzonatate over-ingestion in some of our in-house cases. Benzonatate is rapidly hydrolyzed by plasma butyrylcholinesterase (BChE) to the major metabolite 4-(butylamino)benzoic acid (BABA) along with the corresponding polyethylene glycol monomethyl ethers (Figure 1) (7, 9, 21). The series of polyethoxy metabolites (e.g., n = 9 identified by the NIST mass spectral database as 2-[2-[2-[2-[2-[2-[2-[2-(2-Methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy] ethanol) and BABA (identified by comparison to a USP standard) are detectable in our acidic/neutral screen described in previous publications (26) and a phthalate peak of unknown origin appears in our basic drug extraction (27). Once the metabolic peak pattern became recognizable, the North Carolina Office of the Chief Medical Examiner (N.C. OCME) discovered three benzonatate-related cases over the past year and a total of six potential cases since 2012. It is possible that past benzonatate-related cases were not identified based on our previous lack of knowledge.

Figure 1.

Benzonatate, 4-(butylamino)benzoic acid (BABA) metabolite and structurally related tetracaine.

Figure 1.

Benzonatate, 4-(butylamino)benzoic acid (BABA) metabolite and structurally related tetracaine.

Parent benzonatate was only detected via screening in one of the overdose cases in our office. It appeared as a late-eluting compound after trazodone in the base screen and was quantitated by a reference laboratory using traditional HPLC methodology. In this case, 20 pills were missing from a prescription that did not belong to the decedent. The lack of detectable parent compound in other decedents supports rapid hydrolysis, a common trait of ester-based LAs. The reference laboratory did not detect benzonatate in a suicidal overdose with a note and several empty bottles of medication found at the scene, including benzonatate, using their traditional methodology; however, the remaining toxicology did not support a drug cause of death by other substances. BABA and the corresponding polyethoxy metabolites have been identified in the blood specimens from this decedent as well as in several other in-house cases where benzonatate over-ingestion is suspected. Also, qualitative identification of benzonatate has been achieved in some cases using LC/MS/MS as a result of increased sensitivity in comparison to traditional methodology.

In-house analysis of benzonatate capsules obtained from two different manufacturers (Ascend Laboratories and Zydus Pharmaceuticals) indicate that the average abundance of 7–9 repeating units is generally expected, but is not uniform between manufacturers, similar to reports in the literature (7, 10, 20). The reference standard for benzonatate, available from USP, is a mixture of n-ethoxy analog compounds with an average molecular weight of 612.23 g/mol (28). Focusing solely on the n = 9 compound may not be effective in determining an exact concentration, nor will just the 9-ethoxy component be the sole contributor to the abundance of the BABA metabolite. Evans et al. have demonstrated the inability of the BABA metabolite to block voltage-gated sodium currents at 100 µM, and other mechanisms may be at work; however, this metabolite will be the best candidate for detection of benzonatate exposure (7, 21). Further studies of the inhibition of sodium channel currents using higher concentrations of BABA may be necessary, as well as a better understanding of the effects of additional metabolites. Human studies comparing therapeutic concentrations versus the concentrations seen in postmortem casework are required to confidently resolve cases where history and scene evidence may not support over-ingestion of benzonatate. The pseudocholinesterase deficient portion of the population may be prone to increased sensitivities of this cough medication (16) because of diminished ability to hydrolyze the parent compound and thus potential prolongation of increased benzonatate activity. Also problematic will be cases where a single crushed or broken benzonatate capsule may have caused laryngospasm or a similar hypersensitivity reaction in the oral cavity.

Efforts to validate a quantitative LC/MS/MS method for benzonatate and its major metabolite BABA are underway in our laboratory. Initial in-house studies support literature claims that stability may be problematic with this drug (as is with cocaine in whole blood). Even more challenging is the rapid metabolism of the series of n-ethoxy parent compounds without a suitable pure standard available for quantitation of each specific molecular weight. Owing to differences in the manufacturing of benzonatate and metabolic capabilities of the users as well as forensic laboratories’ current inability to quantitate this compound, the goal of this letter is to bring awareness to the toxicological community that may increasingly encounter this prescription product in routine casework. Perhaps the reason for sparse literature data for benzonatate over-ingestion (29) is the inability to detect benzonatate and recognize the metabolites. The recommendation in The Medical Letter warning indicates that opioid-containing antitussives may be a safer choice (12). Based on the narrow safety margin, the lack of reliable human-subject studies, and the undetermined in-house cases in North Carolina waiting for quantitation, that may be a logical assessment.

References

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Benzonatate (Tessalon Perles) Prescribed Online. Request Benzonatate Prescription or Tessalon Capsules

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Benzonatate (Tessalon Perles) – An Overview

Benzonatate, marketed under the brand name Tessalon, is a nonnarcotic oral antitussive agent that is indicated for the symptomatic relief of cough. Push Health can connect people in need of a benzonatate prescription or Tessalon Perles with an online medical provider who can prescribe benzonatate capsules, including benzonatate 100 mg medication, when appropriate to do so.

What Is Benzonatate Used For?

What is benzonatate used for? Benzonatate is a medication used in preventing or relieving a cough. Tessalon works to reduce the cough reflex and is thought to do so anesthetizing specific receptors found in the respiratory passages and lungs. Benzonatate is sometimes prescribed along with azithromycin (Zithromax) as found in a Z-pak in helping people who are coughing and receiving treatment for a pneumonia or chronic bronchitis. Tessalon has peripheral effects only and is not thought to inhibit the respiratory center itself.

Request Benzonatate Prescription »

Benzonatate – Capsules Cost

The cost of benzonatate prescription medication is a relatively affordable medication at roughly forty cents per pill at many pharmacies. Some insurance plans may also cover the cost of benzonatate 100 mg capsules and benzonatate 200 mg capsules. Benzonatate coupons may also be available online or through the manufacturer. At this time, benzonatate requires a prescription from a medical provider and, as a result, benzonatate OTC is not available.

Benzonatate – Dosage

Benzonatate medication is often prescribed in the branded from, Tessalon. Tessalon Perles contain benzonatate 100 mg while Tessalon capsules contain benzonatate 200 mg. Once administered, Tessalon (benzonatate) begins to work within 15 minutes and the effects can last up to eight hours. Frequently, the dosage of Tessalon used is benzonatate 100 mg or benzonatate 200 mg up to three times per day as needed for cough. Benzonatate capsules need to be swallowed whole and not be broken, chewed, crushed, cut or dissolved.

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Can I Buy Benzonatate Online?

Benzonatate and the branded version, Tessalon Perles and Tessalon capsules, are prescription medications in the US. As a result, it is not possible to just buy benzonatate online or get benzonatate OTC without a valid prescription. Push Health can connect people who might need a benzonatate prescription with an online medication provider who can prescribe benzonatate medication when appropriate to do so.

Benzonatate – Side Effects

Benzonatate prescription medication can cause side effects when used. Side effects to benzonatate include, but are not limited to, confusion, bronchospasm, nausea, constipation, and a rash. Anyone with a hypersensitivity or allergy to benzonatate or related compounds should avoid using the medication. Benzonatate medication and alcohol should not be used together. Questions regarding the side effects of benzonatate prescription medication should be directed to one’s medical provider and pharmacist.

More Benzonatate Information

Last updated June 14, 2021. Given the evolving nature of medicine and science, this information might not be accurate and should not be construed as medical advice or diagnosis / treatment recommendations. Please consult a licensed medical provider if you have additional questions.

Benzonatate Coupons, Discounts & Prices 2021

Generic Name: benzonatate (ben ZOE na tate)
Brand Names: Tessalon Perles, Tessalon, Zonatuss

What is benzonatate?

Benzonatate is a non-narcotic cough medicine.

Benzonatate works by numbing the throat and lungs, making the cough reflex less active.

Benzonatate is used to relieve coughing.

Important Information

You should not use this medication if you are allergic to benzonatate or topical numbing medicines such as tetracaine or procaine (found in some insect bite and sunburn creams).

Never suck or chew on a benzonatate capsule. Swallow the pill whole. Sucking or chewing the capsule may cause your mouth and throat to feel numb or cause other serious side effects.

Serious side effects of benzonatate include choking feeling, chest pain or numbness, feeling like you might pass out, confusion, or hallucinations. Some of these side effects may result from chewing or sucking on a capsule.

Do not give this medication to a child younger than 10 years old without medical advice. An overdose of benzonatate can be fatal to a child.

Before Taking Benzonatate

You should not use this medicine if you are allergic to benzonatate or topical numbing medicines such as tetracaine or procaine (found in some insect bite and sunburn creams).

Tell your doctor if you are pregnant or breastfeeding.

Benzonatate is not approved for use by anyone younger than 10 years old. An overdose can be fatal, especially to a young child who has accidentally swallowed the medicine.

How should I take benzonatate?

Take benzonatate exactly as prescribed by your doctor. Follow all directions on your prescription label and read all medication guides or instruction sheets.

Always ask a doctor before giving a cough medicine to a child. Death can occur from the misuse of cough and cold medicines in very young children.

Take each dose with a full glass of water.

Never suck or chew on a benzonatate capsule. Swallow the pill whole. Sucking or chewing the capsule may cause serious side effects.

Store at room temperature away from moisture, heat, and light.

What happens if I miss a dose of Benzonatate?

Skip the missed dose and use your next dose at the regular time. Do not use two doses at one time.

What happens if I overdose of Benzonatate?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. An overdose of benzonatate can be fatal, especially to a child. Accidental death has occurred in children under 10 years old.

Overdose symptoms may include tremors, feeling restless, seizure (convulsions), slow heart rate, weak pulse, fainting, and slow breathing (breathing may stop).

What should I avoid while taking benzonatate?

Avoid eating or drinking anything while you feel numbness or tingling in your mouth or throat.

Benzonatate side effects

Stop taking benzonatate and get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

severe drowsiness or dizziness;
confusion, hallucinations.
ongoing numbness or tingling in your mouth, throat, or face;
numbness in your chest;
a choking feeling;
chills; or
burning in your eyes.

Some of these side effects may result from chewing or sucking on a benzonatate capsule.

Common benzonatate side effects may include:

headache, dizziness;
nausea, upset stomach;
constipation;
itching, rash; or
stuffy nose.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Benzonatate dosing information

Usual Adult Dose for Cough:

100 mg to 200 mg orally three times a day as needed for cough

Comments: This drug should be swallowed whole.

Use: Symptomatic relief of cough

Usual Pediatric Dose for Cough:

Children older than 10 years:
100 mg to 200 mg orally three times a day as needed for cough

Comments: This drug should be swallowed whole.

Use: Symptomatic relief of cough

What other drugs will affect benzonatate?

Using benzonatate with other drugs that make you drowsy can worsen this effect. Ask your doctor before using opioid medication, a sleeping pill, a muscle relaxer, or medicine for anxiety or seizures.

Other drugs may interact with benzonatate, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell your doctor about all your current medicines and any medicine you start or stop using.

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use benzonatate only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Editorial References and Review

Medically reviewed by USARx EDITORIAL TEAM Last updated on 1/27/2021.

Source: Drugs.com Benzonatate (www.drugs.com/benzonatate.html).

benzonatate and high blood pressure

If coadministration is medically necessary, observe the patient for additive effects such as low blood pressureâ¦ Benzonatate starts to work within 15 to 20 minutes and its effects last â¦ Benzonatate is the generic name of the brand-name drug Tessalon (the gelcaps are called Tessalon Perles). Consider alternatives to benzonatate. Tessalon was initially authorized by the Food and Drug Administration (FDA) in 1958 and is made by Pfizer. The medication is a non-narcotic, prescription cough medicine. Will you have Systolic Hypertension with Methylprednisolone? If you continue to use this site we will assume that you are happy with it. It is available in generic and brand versions. It is not known whether benzonatate crosses into breast milk. Melatonin can also increase the sedative effect of â¦ You must not take dosages in between scheduled times, nor take two doses of the medication at the very same time. * Approximation only. Pseudoephedrine can also increase the heart rate or cause heart palpitations. If you miss a dosage of benzonatate, do not take it up until the next dose is arranged, and then only take the normal dosage amount. If you have any of these typical side effects and they are not going away, call your medical professional: Call for emergency situation medical assistance immediately if you experience any of the following symptoms: Presently, there are no known medications that engage with benzonatate. If you use this eHealthMe study on publication, please acknowledge it with a citation: study title, URL, accessed date. We use cookies to ensure that we give you the best experience on our website. High blood pressure has been reported by people with high blood pressure, rheumatoid arthritis, multiple sclerosis, osteoporosis, pain. Start now, it’s free and anonymous. Benzonatate is chemically similar to medications that are called “ester-type local anesthetics.” These consist of the pain relievers procaine, tetracaine, and lidocaine, which numb the skin, muscles, or gums before medical and dental treatments. High blood pressure is found among people who take Benzonatate, especially for people who are female, 60+ old, have been taking the drug for 100 mm Hg) during the first 3 days after the infarct [see Warnings and Precautions (5.4)]. It is the stretching of these sensors with breathing that causes the cough. Benzonatate has active ingredients of benzonatate. High intake comes from a tree called the âsilent killer. Benzonatate is unrelated to codeine and other narcotics that are frequently used to suppress coughs. 1. The above could cause drop in blood pressure, please double check it with you doc/pharmacist. Pins and needles or tingling in the face, tongue, mouth, or throat. The phase IV clinical study is created by eHealthMe based on reports of 10,019 people who have side effects when taking Benzonatate from the FDA, and is updated regularly. If your medical professional prescribed the 200 mg dose and you have difficulty swallowing large pills, try taking 2 of the 100 mg pills instead one of the 200 mg ones. SingleCare, a leading online service for a prescription, oral, and vision discounts have partnered with many significant pharmacies around the nation to assist you to save up to 80 percent off prescription costs. it damages the myelin sheath): 21 people, 6.07%, Idiopathic Pulmonary Fibrosis (chronic lung disease): 20 people, 5.78%, Cataplexy (loss of muscle tone accompanied by full conscious awareness): 17 people, 4.91%, Renal Cell Carcinoma (a kidney cancer): 17 people, 4.91%, High Blood Cholesterol: 16 people, 4.62%, Osteoporosis (bones weak and more likely to break): 14 people, 4.05%, Multiple Myeloma (cancer of the plasma cells): 14 people, 4.05%, Rheumatoid Arthritis (a chronic progressive disease causing inflammation in the joints): 13 people, 3.76%, Primary Pulmonary Hypertension (primary high blood pressure that affects the arteries in the lungs and the right side of your heart): 10 people, 2.89%, Insomnia (sleeplessness): 10 people, 2.89%, Metastases To Bone (cancer spreads to bone): 9 people, 2.60%, Chronic Obstructive Pulmonary Disease (a progressive disease that makes it hard to breathe): 9 people, 2.60%, Muscle Spasms (muscle contraction): 7 people, 2.02%, Pulmonary Hypertension (increase in blood pressure in the lung artery): 7 people, 2.02%, Anaemia (lack of blood): 7 people, 2.02%, Chronic Lymphocytic Leukaemia (cancer in which the bone marrow makes too many lymphocytes (a type of white blood cell)): 6 people, 1.73%, Restless Leg Syndrome (a powerful urge to move your legs): 6 people, 1.73%, Cardiac Failure Congestive: 6 people, 1.73%, Lung Cancer – Non-Small Cell (lung cancer): 6 people, 1.73%, Cushing’s Syndrome (obesity, a rounded face, increased fat): 5 people, 1.45%, Immunodeficiency Common Variable: 5 people, 1.45%, Arthritis (form of joint disorder that involves inflammation of one or more joints): 5 people, 1.45%, Plasmacytoma (neoplasm of plasma cells (usually in bone marrow)): 5 people, 1.45%, Relapsing-Remitting Multiple Sclerosis (reoccurrence of an inflammatory disease in which the insulating covers of nerve cells in the brain and spinal cord are damaged): 5 people, 1.45%, Multiple Sclerosis Relapse (reoccurrence of a nervous system disease that affects your brain and spinal cord. Some people have had deadly allergies to benzonatate, triggering the muscles in their throats to spasm and restrict, making it difficult to breathe, or producing an unexpected and dangerous drop in blood pressure. 0. Benzonatate oral capsule is a prescription drug thatâs available as a brand-name drug called Tessalon.Itâs also available as a generic drug. 10,019 people reported to have side effects when taking Benzonatate. Generic drugs usually cost less. benzonatate does not have any direct effect (or at least it has not been reported) on blood pressure or any heart condition. Will you have Blood Immunoglobulin A Increased with drugs of ingredients of amoxicillin; clavulanate potassium? Intentional and unexpected overdoses of benzonatate can kill adults or children quickly. Benzonatate is a medication taken orally to suppress coughs. Patients receiving an MAOI concurrently with local anesthetics may have an increased risk of hypotension or CNS-related effects. 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Benzonatate FDA Warnings & Precautions | Healthgrades

Severe hypersensitivity reactions (including bronchospasm, laryngospasm and cardiovascular collapse) have been reported which are possibly related to local anesthesia from sucking or chewing the capsule instead of swallowing it. Severe reactions have required intervention with vasopressor agents and supportive measures.

Isolated instances of bizarre behavior, including mental confusion and visual hallucinations, have also been reported in patients taking benzonatate capsules in combination with other prescribed drugs.

accidental ingestion & death in children

Keep benzonatate capsules out of reach of children. Accidental ingestion of benzonatate capsules resulting in death has been reported in children below age 10. Signs and symptoms of overdose have been reported within 15 to 20 minutes and death has been reported within one hour of ingestion. If accidental ingestion occurs, seek medical attention immediately (see OVERDOSAGE).

Benzonatate is chemically related to anesthetic agents of the para-amino-benzoic acid class (e.g. procaine; tetracaine) and has been associated with adverse CNS effects possibly related to a prior sensitivity to related agents or interaction with concomitant medication.

Swallow benzonatate capsules whole. Do not break, chew, dissolve, cut, or crush benzonatate capsules.Release of benzonatate from the capsule in the mouth can produce a temporary local anesthesia of the oral mucosa and choking could occur. If numbness or tingling of the tongue, mouth, throat, or face occurs, refrain from oral ingestion of food or liquids until the numbness has resolved. If the symptoms worsen or persist, seek medical attention.

Keep benzonatate capsules out of reach of children. Accidental ingestion resulting in death has been reported in children. Signs and symptoms of overdose have been reported within 15 to 20 minutes and death has been reported within one hour of ingestion. Signs and symptoms may include restlessness, tremors, convulsions, coma and cardiac arrest. If accidental ingestion occurs, seek medical attention immediately.

Overdosage resulting in death may occur in adults.

Do not exceed a single dose of 200 mg and a total daily dosage of 600 mg. If you miss a dose of benzonatate capsules, skip that dose and take the next dose at the next scheduled time. Do not take 2 doses of benzonatate capsules at one time.

Pregnancy Category C. Animal reproduction studies have not been conducted with benzonatate capsules. It is also not known whether benzonatate capsules can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Benzonatate capsules should be given to a pregnant woman only if clearly needed.

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk caution should be exercised when benzonatate capsules are administered to a nursing woman.

carcinogenesis, mutagenesis, impairment of fertility

Carcinogenicity, mutagenicity, and reproduction studies have not been conducted with benzonatate capsules.

Safety and effectiveness in children below the age of 10 have not been established. Accidental ingestion resulting in death has been reported in children below age 10. Keep out of reach of children.

Benzonatate: Pediatric Medication | Memorial Sloan Kettering Cancer Center

This document, provided by Lexicomp ^®, contains all the information you need to know about the drug, including the indications, route of administration, side effects and when you should contact your healthcare provider.

Trade names: USA

Tessalon Perles

What is this drug used for?

Used to relieve coughs.

What do I need to tell my doctor BEFORE my child takes this drug?

If your child is allergic to this drug, any of its ingredients, other drugs, foods, or substances. Tell your doctor about the allergy and how your child has it.

Combination of this drug with certain medications and medical conditions may be adverse.

Talk to your doctor or pharmacist about all medications your child is taking (prescription and over-the-counter, natural products, and vitamins) and any health concerns.You need to make sure it is safe to take this drug if your child is ill and in combination with other drugs that he or she is already taking. You should not start, stop, or change the dosage of any drug your child is taking without talking to your doctor.

What do I need to know or do while my child is taking this drug?

Tell all health care providers for your child that your child is taking this drug.These are your child’s doctors, nurses, pharmacists and dentists.
Have your child avoid tasks or activities that require attention until you see how this drug is working for your child. This includes cycling, playing sports, or using items such as scissors, lawn mowers, electric scooters, toy cars, or motorized vehicles.
Keep out of the reach of children.Cases of unintentional overdose and death have been reported among children under the age of 10 who took the drug by accident. Overdose may manifest as anxiety, tremors, seizures, loss of consciousness, or the development of myocardial infarction. If this drug is accidentally taken by a child, seek medical attention immediately.

If your daughter is pregnant or breastfeeding:

Consult a doctor if your daughter is pregnant, pregnant, or breastfeeding.The benefits and risks for your daughter and her child will need to be discussed.

What side effects should I report to my child’s healthcare provider right away?

WARNING / CAUTION Although rare, this drug can cause very serious and sometimes deadly side effects in some people. Call your child’s doctor right away or get medical attention if your child has any of the following signs or symptoms that could be associated with a very bad side effect:

Signs of an allergic reaction such as rash, hives, itching, reddened and swollen skin with blistering or scaling, possibly associated with fever, wheezing or wheezing, tightness in the chest or throat, difficulty breathing, swallowing or speaking, unusual hoarseness, swelling in the mouth, face, lips, tongue, or throat.
Changes in the behavior of the child.
Confusion of consciousness.
Hallucinations (a person sees or hears something that is not in reality).
Cases of numbness or tingling in the mouth, tongue, pharynx and face have been reported upon breaking, crushing, chewing, dissolving in the mouth or dissolving the drug. Choking and very severe allergic reactions also occurred. If the child feels numb or tingling, do not allow him to eat or drink until these symptoms are resolved.If your child develops an allergic reaction, or if the numbness or tingling sensation persists or gets worse, contact your child’s healthcare provider right away.

What are some other side effects of this drug?

Any drug can have side effects. However, many people have little or no side effects. Call your child’s doctor or get medical help if any of these or other side effects bothers your child or does not go away:

Constipation.
Dizziness or headache.
Sleepiness.
stuffy nose.
Nausea.

This list of potential side effects is not exhaustive. If you have any questions about side effects, talk to your child’s doctor. Talk to your child’s doctor about side effects.

You can report side effects to the National Health Office.

What is the best way to give this drug?

Give this drug to your child as directed by the doctor.Read all the information provided to you. Follow all instructions strictly.

Make sure the child swallows the drug whole. Do not allow your child to chew, crush, grind, or dissolve the drug in the mouth.
Tell your child not to suckle this drug.
Try to have your child drink lots of non-caffeinated liquids every day, unless directed by a doctor to drink less liquids.

What if my child misses a dose of a drug?

If your child is taking the drug regularly, give the missed dose as soon as you remember.
If it is time for your child to take the next dose, do not take the missed dose and then return to your child’s normal schedule.
Do not give a double dose at the same time or additional doses.
In most cases, this drug is used as needed. Do not give your child the drug more often than the doctor tells you to.

How do I store and / or discard this drug?

Store at room temperature, protected from light.Store in a dry place. Do not store in the bathroom.
Store all medicines in a safe place. Keep all medicines out of the reach of children and pets.
Dispose of unused or expired drugs. Do not empty into toilet or drain unless directed to do so. If you have any questions about the disposal of your medicinal products, consult your pharmacist. Your area may have drug recycling programs.

General information on medicinal products

If your child’s symptoms or health problems do not improve, or if they get worse, see your child’s doctor.
Do not share your child’s medication with others or give anyone else’s medication to your child.
Some medicines may come with other patient information sheets. If you have questions about this drug, talk with your child’s doctor, nurse, pharmacist, or other healthcare professional.
If you think an overdose has occurred, call a Poison Control Center immediately or seek medical attention. Be prepared to tell or show which drug you took, how much and when it happened.

Use of information by the consumer and limitation of liability

This information should not be used to make decisions about taking this or any other drug. Only the attending physician has the necessary knowledge and experience to make decisions about which drugs are suitable for a particular patient.This information does not guarantee that the drug is safe, effective, or approved for the treatment of any disease or specific patient. Here are only brief general information about this drug. It does NOT contain all available information on the possible use of the drug with instructions for use, warnings, precautions, information about interactions, side effects and risks that may be associated with this drug. This information should not be construed as a guide to treatment and does not replace the information provided to you by your healthcare professional.Please consult your doctor for complete information on the possible risks and benefits of taking this drug. Use of this information is governed by the Lexicomp End User License Agreement available at https://www.wolterskluwer.com/en/solutions/lexicomp/about/eula.

Copyright

90,000 🏥 Sodium benzonate | Side effects, dosage, uses and more 2021

Basic data for benzonatate

Benzonatate Tumor Capsule is available for both generic drug and brand name drug. Brand: Thessalon.
Benzonatate comes in capsule and pearl (smaller capsule) form that you take by mouth. This medicine must be swallowed whole. You must not break, chew, cut, or crush this medication.
This medication is used to relieve coughs. It starts working about 15-20 minutes after you swallow it. Its effect lasts 3-8 hours.

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Important warnings

Allergic reactions: This drug must be swallowed whole.People who chew or suck the capsule are at increased risk of allergic reactions. This can cause spasms of your bronchi (the main passage to your throat and airways) and vocal cords. It can also cause negative effects on your heart and blood vessels.
Psychiatric problems: This drug may cause confusion and visual hallucinations (seeing what is not there). This serious side effect only occurs in people who have also taken other medications.
Overdose in children: Accidental ingestion of this drug can be fatal (cause death) in children under 10 years of age. Overdose symptoms may appear 15-20 minutes after the capsule is swallowed, and death may occur in about an hour. If your child swallows this medication, see a doctor or get medical help right away.

About

What is benzonate?

Benzonatate Vinegar Capsule is a prescription drug available as a brand name drug called Tessalon .It is also available as a generic drug. The drugs usually cost less. In some cases, they may not be available in every strength or form as a branded version.

Benzonatate is also supplied as oral perle (smaller capsule).

Why is it used

Benzonate is used to relieve coughs. It starts working about 15-20 minutes after you swallow it. Its effect lasts 3-8 hours.

Benzonate can be used as part of combination therapy.This means that you may need to take it with other medicines.

How it works

Benzonate belongs to a class of drugs called antitussives. A drug class is a group of drugs that work in a similar way. These drugs are often used to treat these conditions.

Benzonatate works by numbing receptors in your airways that make you cough. This makes you cough less after taking the drug.

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Side effects

Benzonatate

side effects

Benzonatate tumor capsule may cause drowsiness and other side effects.

More common side effects

More common benzonatate capsule side effects:

drowsiness
dizziness
headaches
constipation
nausea
upset stomach
Breakouts
nasal congestion

If these effects are mild, they may subside within days or weeks.If they are more severe or persist, talk to your doctor or pharmacist.

Serious side effects

Call your doctor at once if you have a serious side effect. Call 911 if your symptoms feel life threatening or if you think you have a medical emergency. Serious side effects and their symptoms may include the following:

Allergic reactions. Symptoms may include:
- breathing problems
- swelling or tightness in your throat
- heart and blood vessel problems such as very low blood pressure.This may make you dizzy or weak.
Confusion
Hallucinations (seeing or hearing something that is not there)
Chest Feeling
Burning your eyes

Disclaimer: Our goal is to provide you with the most current and current information. However, since drugs affect each person differently, we cannot guarantee that this information includes all possible side effects.This information does not replace medical advice. Always discuss possible side effects with a healthcare provider who knows your medical history.

Interaction

Benzonate can interact with other drugs

Interaction occurs when a substance changes the way the drug works. This can be harmful or interfere with the work of the drug. To help prevent interactions, your doctor must carefully manage all of your medications.Be sure to tell your doctor about any medications, vitamins, or herbs you are taking.

To find out how Benzonatate Capsule might interact with something else you are taking, talk to your doctor or pharmacist.

Disclaimer: Our goal is to provide you with the most current and up-to-date information. However, because drugs interact differently in each person, we cannot guarantee that this information includes all possible interactions.This information does not replace medical advice. Always talk with your healthcare provider about possible interactions with all prescription drugs, vitamins, herbs and dietary supplements, and over-the-counter medications you are taking.

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Other warnings

Benzonatate Warnings

This drug comes with several warnings.

Numbness

Call your doctor if you have numbness in your tongue, mouth, throat, or face that does not go away or get worse.

You should not eat or drink if you have numbness in your tongue, mouth, throat, or face after taking this drug. Once the numbness disappears, you can eat and drink.

Allergies

Benzonate may cause a severe allergic reaction. Your risk may be higher if you chew or suck on the capsule rather than swallowing it whole. Symptoms may include:

breathing problems
swelling or tightness in your throat
heart and blood vessel problems such as very low blood pressure.This may make you dizzy or weak.

If you have an allergic reaction, call your doctor or local poison control center right away. If your symptoms are severe, call 911 or go to the nearest emergency room. Do not take this drug again if you have ever had an allergic reaction to it. Recurrence can be fatal (cause of death).

Warnings for specific groups

For pregnant women: Benzonatate is a category C pregnancy drug.This means two things:

Animal studies have shown adverse effects on the fetus when the mother takes the drug.
There have not been enough human studies to be sure how this drug might affect the fetus.

Talk to your doctor if you are pregnant or planning to become pregnant. This medication should only be used if the potential benefit justifies the potential risk to the fetus.

Call your doctor right away if you become pregnant while taking this drug.

Women who are breastfeeding: Benzonate can pass into breast milk and may cause side effects in a breastfeeding baby. Talk to your doctor if you are breastfeeding. You may need to decide whether to stop breastfeeding or stop taking this drug.

For children: This drug has not been studied and should not be used in children under 10 years of age.Accidental swallowing of this drug can be fatal (cause death) in children under 10 years of age. Keep this medication out of the reach of young children.

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Dosage

How to take benzonatate

This dosage information is for benzonatate oral capsule. All possible doses and dosage forms cannot be included here. Your dose, dosage form, and how often you take the drug will depend on:

your age
condition that is being treated
how bad is your condition
other medical conditions you have
How do you react to the first dose

Forms and strengths

General: Benzonate

Form: Oral Capsule
Strengths: 100 mg, 150 mg, 200 mg

Make: Tessalon

Form: Oral Capsule
Strengths: 200 mg

Cough relief dose

Adult dose (ages 18 and over)

Take 100-200 mg three times daily as needed for your cough.The maximum dose is 600 mg per day.

Child dosage (ages 11-17)

Take 100-200 mg three times daily as needed for your cough. The maximum dose is 600 mg per day.

Child dosage (age 0-10 years)

This drug has not been studied and should not be used in children under 10 years of age.

Disclaimer: Our goal is to provide you with the most current and up-to-date information.However, since medications affect each person differently, we cannot guarantee that this list includes all possible doses. This information does not replace medical advice. Always talk to your doctor or pharmacist about the dosages that are right for you.

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Accept as specified

Take as directed

Benzonatate capsule is usually used for short term treatment. It’s risky if you don’t take it as prescribed.

If you do not take it at all: Your cough will continue.

If you take too much: You may have dangerous levels of the drug in your body. Your risk may be higher if you chew or suck on this medication rather than swallow it whole. Symptoms may appear 15-20 minutes after taking too much. Overdose symptoms include:

suffocation
breathing problems
feeling anxious
shiver
attacks
brain swelling
stopping your heart
coma (unconscious for a long time)
death

If you think you have taken too much of this drug, call your doctor or local poison control center.If your symptoms are severe, call 911 or go to the nearest emergency room right away.

How to tell if a drug is working: You shouldn’t cough that much. This medication starts working about 15 to 20 minutes after you swallow it. Its effect lasts 3-8 hours.

Important considerations

Important considerations for the use of benzonatate

Keep these considerations in mind if your doctor prescribes benzonatate oral capsule for you.

General

You can take benzonate with or without food.
You must swallow this drug whole. Do not break, chew, cut, or crush this drug.
Not every pharmacy stocks this drug. When filling out a prescription, be sure to call ahead to make sure your pharmacy carries it.

Storage

Store benzonatate at room temperature between 59 ° F and 86 ° F (15 ° C and 30 ° C).Keep it as close to 77 ° F (25 ° C) as possible.
Keep this medication away from light.
Do not store this medication in humid or damp areas such as bathrooms.

Inserts

Prescription for this reusable drug. You will not need to enter a new prescription for this medication. Your doctor will write down the number of refills authorized for your prescription.

Travel

When traveling with your medicine:

Always carry your medicine with you.When flying, never put it in a checked bag. Keep it in your carry bag.
Don’t worry about the X-ray machines at the airport. They cannot damage your medications.
You may need to show airport staff the pharmacy label for your medications. Always carry the original prescription-labeled box with you.
Do not put this medication in your car’s glove box or leave it in your car. Be sure to avoid this when the weather is very high or very cold.

Clinical monitoring

You and your doctor must monitor certain health problems. This can help you stay safe while you are taking this drug. These issues include:

Cough. Call your doctor if your cough does not improve.

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Alternatives

Are there alternatives?

There are other medicines available to treat your condition.Some may be better for you than others. Talk with your doctor about other drug options that might work for you.

Disclaimer: Healthline has made every effort to ensure that all information is factually correct, comprehensive and current. However, this article should not be used as a substitute for the knowledge and experience of a licensed healthcare professional. You should always check with your doctor or other healthcare professional before taking any medication.The drug information contained herein is subject to change and is not intended to cover all potential uses, directions, precautions, warnings, drug interactions, allergic reactions, or side effects. The absence of warnings or other information for a given drug does not mean that the drug or drug combination is safe, effective, or appropriate for all patients or for all specific purposes.

Hydromorphone

“Dihydromorphinone” is redirected here.Not to be confused with dihydromorphine, another opioid.

Opioid medication used to relieve pain

41 Administration intravenously, subcutaneously

Elimination

9 0498

Hydromorphone
Clinical data


Trade names	Dilaudin, Palladon5 Others 9049 Dilaudin, Palladon5 others 9049 Dihydromorphinone
AHFS / Drugs.com	Monograph
MedlinePlus	a682013
License data

		8	US : N (not yet classified) ^[1]
Dependency Duty	High ^[2]
Routes
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability	, Intra: 30–354% IV / IM: 100%
Protein binding	20%
Metabolism	Liver
Onset of action	15 to 30 min ^[4]
	2-3 hours ^[5]
Duration of action	4 to 5 hours ^[4]
Excretion	Kidney
Identifiers		00 4 , 5-α-epoxy-3-hydroxy-17-methylmorphinan-6-one
CAS number
PubChem CID
IUPHAR / BPS
DrugBank
ChemSpider
UNII
Kerr
CHEBI
CHEMBL
CompTox Control Panel ( EPA )
ECHA InfoCard	100.006.713
Chemical and physical data
Formula	C ₁₇ HOUR ₁₉ NO ₃
Molar mass	285.343 g (JSmol)
Water solubility	HCl salt: 333 mg / ml (20 ° C)
O = C4 [C @@ H] 5Oc1c2c (ccc1O) C [C @ H ] 3N (CC [C @] 25 [C @ H] 3CC4) C
InChI = 1S / C17h29NO3 / c1-18-7-6-17-10-3-5-13 ( 20) 16 (17) 21-15-12 (19) 4-2-9 (14 (15) 17) 8-11 (10) 18 / h 2,4,10-11,16,19H, 3,5- 8h3,1h4 / t10-, 11 +, 16-, 17- / m0 / s1 ^Y Key: WVLOADHCBXTIJK-YNHQPCIGSA-N ^Y
(check)

, also known as dihydromorphinone 9003 8, and marketed under the brand name Dilaudid , among others, this opioid is used to treat moderate to severe pain.^[4] As a general rule, long-term use is only recommended for pain due to cancer. ^[6] It can be taken orally or injected into a vein, muscle, or under the skin. ^[4] The effect usually begins within half an hour and lasts up to five hours. ^[4]

Common side effects include dizziness, drowsiness, nausea, itching, and constipation. ^[4] Serious side effects may include: overuse, low blood pressure, seizures, respiratory depression, and serotonin syndrome.^[4] Rapid dose reduction can lead to opioid syndrome. ^[4] Generally use during pregnancy or breastfeeding is not recommended. ^[7] Hydromorphone is believed to work by activating opioid receptors, predominantly in the brain and spinal cord. ^[4] Hydromorphone 2 mg orally is equivalent to approximately 10 mg. morphine by mouth. ^[6]

Hydromorphone was patented in 1923. ^[8] It is available as a generic drug.^[4] In the United Kingdom, this costs the NHS around £ 0.32 per 2 mg tablet as of 2019. ^[6] In the US, the wholesale value of this amount is about US $ 0.07. ^[9] In 2017, it was the 205th most commonly prescribed drug in the United States, with over two million prescriptions issued. ^[10] ^[11] Hydromorphone is made from morphine. ^[12]

Medical use

Hydromorphone is used to treat moderate to severe pain.^[4] It can be taken orally or injected into a vein, muscle, or under the skin. ^[4] The effect usually begins within half an hour and lasts up to five hours. ^[4] As a general rule, long-term use is only recommended for pain due to cancer. ^[6] A 2016 Cochrane review found little difference in the benefits of hydromorphone and other opioids for cancer pain. ^[13]

Side effects

The side effects of hydromorphone are similar to those of other potent opioid analgesics such as morphine and heroin.The main hazards of hydromorphone include dose-dependent respiratory depression, urinary retention, bronchospasm, and sometimes circulatory depression. ^[14] Common side effects include lightheadedness, dizziness, sedation, itching, constipation, nausea, vomiting, headache, sweat, and hallucinations. ^[14] These symptoms are common in outpatients and those without severe pain.

The simultaneous use of hydromorphone with other opioids, muscle relaxants, tranquilizers, sedatives and general anesthetics can cause a significant increase in respiratory depression, progressing to coma or death.Taking benzodiazepines (such as diazepam) in combination with hydromorphone may increase side effects such as dizziness and poor concentration. ^[15] If concomitant use of these drugs is required, dose adjustments may be made. ^[16]

A particular problem that can arise with hydromorphone is accidental administration instead of morphine due to confusion of similar names, either during prescription or dispensing.This has led to several deaths and calls for the distribution of hydromorphone in packaging that is different from that of morphine to avoid confusion. ^[17] ^[18]

People with an opioid tolerance rarely have massive overdoses, but when they do, they can cause circulatory collapse. Overdose symptoms include respiratory depression, drowsiness leading to coma and sometimes death, skeletal muscle sagging, low heart rate, and low blood pressure.In the hospital, supportive care such as assisted ventilation to provide oxygen and bowel decontamination using activated charcoal via a nasogastric tube is provided to persons with a hydromorphone overdose. Opioid antagonists such as naloxone can also be administered concurrently with oxygen supplementation. Naloxone works by reversing the action of hydromorphone and is only given when there is significant respiratory and circulatory depression. ^[16]

Sugar cravings associated with hydromorphone use are the result of a drop in glucose after short-term hyperglycemia after injection, or a less profound drop in blood sugar levels over several hours, as with morphine, heroin, codeine, and other opiates …

Hormonal imbalance

Like other opioids, hydromorphone (especially with heavy chronic use) often causes temporary hypogonadism or hormonal imbalance. ^[19]

Neurotoxicity

With prolonged use, high dosages, and / or renal dysfunction, hydromorphone has been associated with neuroexcitatory symptoms such as tremor, myoclonus, anxiety, and cognitive dysfunction. ^[20] ^[21] ^[22] This toxicity is less than that of other classes of opioids, such as the pethidine class of synthetics in particular.

Withdrawal

Hydromorphone users may experience painful symptoms if the drug is stopped. ^[23] Some people cannot tolerate their symptoms, which leads to constant drug use. ^[23] Opioid withdrawal symptoms are difficult to decipher because there are differences between drug seeking behavior and the true effects of withdrawal. ^[24] Symptoms associated with hydromorphone withdrawal include: ^[23] ^[24] ^[25]

Abdominal pain
Anxiety or panic attacks
Depression
Goose bumps
Inability to enjoy daily activities
Muscle and joint pain
Nausea
Runny nose and excessive lacrimation
Sweating
Vomiting

In clinical settings, excessive tear production, yawning and dilated pupils are useful indicators in the diagnosis of opioid withdrawal …^[26] Hydromorphone – fast-acting pain reliever; however, some formulations can last up to several hours. Patients who stop taking this drug abruptly may experience withdrawal symptoms. ^[25] ^[27] which can start a few hours after the last dose of hydromorphone and last up to several weeks. ^[23] Withdrawal symptoms in people who stop taking opioids can be controlled with opioids or non-opioid supplements.^[28] Methadone is an opioid commonly used for this type of therapy. However, the therapy should be selected individually for each individual person. ^[29] Methadone is also used to detoxify people with opioid dependence, such as heroin or drugs similar to morphine. ^[29] It can be administered orally or intramuscularly. There is controversy regarding the use of opioids for people experiencing withdrawal symptoms, as these agents can also cause relapse in patients when they stop therapy.^[23] Clonidine is a non-opioid supplement that can be used in situations where opioid use is undesirable, such as in patients with high blood pressure. ^[30]

Interactions

CNS depressants may enhance the depressive effects of hydromorphone, such as other opioids, anesthetics, sedatives, hypnotics, barbiturates, benzodiazepines, phenothiazines, chloral hydrate, dimensionhydrinate, and glutethimide. The inhibitory effect of hydromorphone can also be enhanced by monoamine oxidase inhibitors (MAO inhibitors), first generation antihistamines (brompheniramine, promethazine, diphenhydramine, chlorphenamine), beta blockers, and alcohol.When combination therapy is contemplated, the dose of one or both agents should be reduced. ^[20]

Pharmacology

Hydromorphone on opioid receptors ^[31]
Affinity ( K _I )			Ratio
MOR	90 DOR950948 K KOR
0.47 nM	18.5 nM	24.9 nM	1:39:53

Hydromorphone is a semisynthetic μ-opioid agonist.As hydrogenated morphine ketone, it has pharmacological properties typical of opioid analgesics. Hydromorphone and related opioids have major effects on the central nervous system and gastrointestinal tract. These include pain relief, drowsiness, confusion, mood swings, euphoria or dysphoria, respiratory depression, suppressed cough, decreased gastrointestinal motility, nausea, vomiting, increased cerebrospinal fluid pressure, increased biliary pressure, and increased pinpoint pupillary constriction.^[27]

Formulations

Hydromorphone is available as parenteral, rectal, subcutaneous and oral formulations and can also be administered via epidural or intrathecal injection. ^[35] Hydromorphone was also administered by nebulization for the treatment of dyspnea, but it is not used as a method of pain relief due to its low bioavailability. ^[36] Transdermal delivery systems capable of causing local cutaneous analgesia are also contemplated.^[37]

Concentrated aqueous solutions of hydromorphone hydrochloride have a noticeably different refractive index from pure water, isotonic 9 ‰ (0.9%) saline, etc., especially when stored in transparent ampoules and vials, can acquire lung transparent amber discoloration upon exposure to light; It is reported that this does not affect the effectiveness of the solution, but 14-dihydromorphinones such as hydromorphone, oxymorphone, and relatives come with instructions for protection from light.^[38] The ampoule of the solution in which the precipitate has formed should be discarded. ^[38]

Battery-operated intrathecal drug delivery systems are implanted for chronic pain when other options such as surgery and conventional pharmacotherapy have been ruled out, provided the patient is considered eligible for any contraindications, physiological or psychological. ^[39]

An extended release version of Hydromorphone (once a day) is available in the United States.^[40] An earlier extended-release version of hydromorphone, Palladone, was available before being voluntarily withdrawn from the market after the FDA warned in July 2005 of a high potential for overdose when taken with alcohol. As of March 2010, it is still available in the UK under the Palladone SR brand, Nepal under the Opidol brand and in most other European countries. ^[41]

Pharmacokinetics

Chemical modification of the morphine molecule to hydromorphone results in higher lipid solubility and greater ability to cross the blood-brain barrier for faster and more complete penetration into the central nervous system.Per milligram, hydromorphone is believed to be five times stronger than morphine; although conversion rates can vary from 4 to 8 times, in typical clinical use it is five times. ^[42] ^[43] The development of tolerance can also vary from person to person.

Patients with impaired renal function should be careful when dosing hydromorphone. In people with renal impairment, the half-life of hydromorphone can increase to 40 hours.The typical half-life of intravenous hydromorphone is 2.3 hours. ^[44] Peak plasma levels usually occur between 30 and 60 minutes after oral administration. ^[45]

The onset of action of intravenous hydromorphone is less than 5 minutes and within 30 minutes after oral administration (immediate release). ^[36]

Metabolism

While other opioids in this class such as codeine or oxycodone are metabolized by CYP450 enzymes, hydromorphone is not.^[46] Hydromorphone is extensively metabolized in the liver to hydromorphone-3-glucuronide, which has no analgesic effect. As with the morphine metabolite, morphine-3-glucuronide, elevated hydromorphone-3-glucuronide levels can cause excitatory neurotoxic effects such as agitation, myoclonus, and hyperalgesia. Patients with impaired renal function and elderly patients have a higher risk of metabolite accumulation. ^[47] ^[48]

Chemistry

According to the formula C ₁₇ HOUR ₁₉ NO ₃ and with a molecular weight of 285.343, both identical to morphine, hydromorphone can be considered as the structural isomer of morphine and its hydrogenated ketone.^[49]

Hydromorphone is obtained from morphine either by direct rearrangement (by heating under reflux an alcoholic or acidic aqueous solution of morphine in the presence of a platinum or palladium catalyst), or reduction to dihydromorphine (usually through catalytic hydrogenation), followed by oxidation with benzophenone in the presence of potassium tert-butoxide or aluminum tert-butoxide (Oppenauer oxidation). The 6-ketone group can be replaced with a methylene group through the Wittig reaction to produce 6-methylenedihydrodeoxymorphine, which is 80 times stronger than morphine.^[50]

Conversion of morphine to hydromorphone increases its activity and therefore makes hydromorphone about eight times more potent by weight than morphine, all other things being equal. ^{[ citation needed ]} Lipid solubility is also altered, resulting in a faster onset of hydromorphone action and a change in the overall absorption, distribution, metabolism and excretion profile and side effect profile (generally less nausea and itching) compared to morphine …… Semisynthetic opiates, of which hydromorphone and its codeine analogue hydrocodone are among the best known and oldest, include a wide variety of drugs of varying strengths and differences, both subtle and harsh, allowing for many different treatment options.

Hydromorphone is more soluble in water than morphine; therefore, hydromorphone solutions can be prepared to deliver the drug in a smaller volume of water. The hydrochloride salt is soluble in three parts of water, while a gram of morphine hydrochloride is dissolved in 16 ml of water; For all common purposes, pure hospital powder can be used to produce solutions of virtually arbitrary concentration.When the powder appears on the street, this very small amount of powder required per dose means that an overdose is likely for those who mistake it for heroin or other powdered drugs, especially those that have been diluted before use. ^[51]

Endogenous production

Hydromorphone is produced from morphine by catalytic hydrogenation and is also produced in trace amounts during the metabolism of morphine by humans and other mammals.It sometimes appears in very small quantities in opium latex assays, apparently forming in plants in an unknown percentage of cases under poorly understood conditions. ^{[ citation needed ]}

Bacteria

Several bacteria have been shown to convert morphine into closely related drugs, including hydromorphone and dihydromorphine. The bacterium Pseudomonas putida serotype M10 produces a natural NADH-dependent morphinone reductase that can work with unsaturated bonds 7,8, as a result of which, when these bacteria live in an aqueous solution containing morphine, significant amounts of hydromorphone are formed, since it is an intermediate metabolite in this process; the same goes for the conversion of codeine to hydrocodone.^[52]

As a result, various concentrations of hydromorphone, dihydromorphine, hydromorphinol, and oxymorphone were obtained during the experiments. Three pathways have been discovered: from morphine to hydromorphone with dihydromorphine as the penultimate step, from morphine to hydromorphone with morphinone as the penultimate step, and from morphine to hydromorphinol to hydromorphone.

History

Hydromorphone was patented in 1923. ^[8] It was introduced to the mass market in 1926 under the trade name Dilaudid , ^[53] indicating its origin and degree of similarity to morphine (via laudanum).

Society and culture

Names

Hydromorphone is known worldwide under the trademarks Hydal, Dimorphone, Exalgo, Sophidone LP, Dilaudid, Hydrostat, Hydromorfan, Hydromorphan, Hymorphan, Laudicon, Opidol, Palladone, Hydromorph Contin and others. An extended-release version of hydromorphone, called Palladone, was available for a short time in the United States before being voluntarily withdrawn from the market after the FDA warned in July 2005 of a high potential for overdose when taken with alcohol.^[54] As of March 2010, it is still available in Nepal under the brand name Opidol, in the United Kingdom under the brand name Palladone SR and in most other European countries.

Also, since May 2009, a once-daily version of hydromorphone with an extended release period has been released under the Jurnista trademark in Australia. ^[55]

Legal status

In the United States, the main drug control agency, the Drug Enforcement Administration, reports an increase in the annual cumulative quota of hydromorphone production from 766 kilograms (1689 lb) in 1998 to 3300 kilograms (7300 lb ) in 2006, as well as an increase in the number of recipes.at this time 289%, from about 470,000 to 1,830,000. The production quota for 2013 was 5,968 kilograms (13,157 lb). ^[56]

Like all opioids used for pain relief, hydromorphone is potentially addictive and listed in Appendix II of the United States Controlled Substances Act 1970 and at similar levels under the drug laws of virtually all other countries and included in the Single Convention on Narcotic Drugs.DEA ACSCN for hydromorphone – 9150.

Hydromorphone is listed by German Betäubungsmittelgesetz as Betäubungsmittel in the most limited list of drugs; similarly, it is controlled in Austria (Suchtgift) under SMG and Swiss BetmG. The Drug Abuse Act 1971 (United Kingdom) and comparable laws from France, Canada, Australia, Italy, Czech Republic, Croatia, Slovenia, Sweden, Poland, Spain, Greece, Russia and other countries control it in the same way as the rules of virtually all others. countries.

Use in Executions

In 2009, Ohio approved the use of an intramuscular injection of 500 mg hydromorphone and a supratherapeutic dose of midazolam as a back-up for execution when a suitable intravenous vein cannot be found. ^[57]

Hydromorphone and midazolam were injected intravenously to execute double assassin Joseph Wood in Arizona on July 24, 2014. Wood was heavily sedated ( surgical anesthesia ) for four minutes from initiation, but it took almost two hours to progress to stage 4 (cessation of breathing) and death.^a ^b ^c ^d ^e ^{9004 W}

00 975 hours ⁱ ^j ^k ^l ^{m monograph …}

“Execution in Arizona takes two hours.” BBC News . 2014 Jul 24 Retrieved Jul 24 2014
external link
MOR
DOR
KOR
0 NOP 905 908 908 905 908 905 908 908 908 908 908 908 908 905 908 908 908 908 905 Others: Kyotorfin (meth-enkephalin releasing / decomposition stabilizer)
What is benzonatate?
Benzonatate is an antitussive agent, also known as cough medicine, that is prescribed for patients who are struggling with diseases such as colds or pneumonia.This drug is extremely dangerous for children under the age of 10 and should not be left within reach. Unless otherwise directed by your healthcare professional, liquid-filled benzonatate capsules are taken once every four to six hours as needed, but no more than three times a day. One of the advantages of this medication is that it is not an opioid and therefore less likely to be used in illegal ways than drugs containing drugs such as dextromethorphan.Benzonatate can cause minor side effects like headaches and dangerous side effects like difficulty breathing.
Whether this medication is prescribed depends on the type of cough. If the cough is dry and unproductive, benzonatate may be prescribed to suppress it. On the other hand, if the patient is coughing up phlegm or mucus, medication may be prescribed to thin the phlegm to relieve the cough. When a doctor can treat the real cause of a cough, such as an infection or asthma, it is usually treated instead of or in combination with the cough.
Children can easily overdose this drug; in fact, children under the age of two can fatally overdose with just a couple of capsules. Some side effects of overdose are convulsions, tremors, and cardiac arrest, which can occur within 30 minutes of consumption.
Benzonatate can cause certain effects that are not necessarily dangerous, but they can all be bad if they last too long. For example, gastrointestinal problems, stomach discomfort and constipation are fairly common side effects of the drug.In addition, nasal congestion, burning eyes, and headaches also occur regularly with benzonatate. Finally, this medication causes dizziness and drowsiness.
In addition to the signs of an overdose such as coma, tremors and anxiety, there are several symptoms that can be very dangerous if they do occur. Skin problems such as rashes, itching, and the presence of hives can be dangerous, and it is generally advised to see a healthcare professional if someone taking benzonatate experiences these symptoms.