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Trazodone for people. Trazodone: Leveraging the Power of a Versatile Antidepressant

What is trazodone used for. How does trazodone work. What are the side effects of trazodone. Dosage and administration of trazodone. Warnings and precautions when taking trazodone.

Содержание

Unlocking the Therapeutic Potential of Trazodone

Trazodone, a widely prescribed antidepressant medication, has been hailed as a versatile and effective solution for managing a variety of mental health conditions. From treating depression to addressing sleep-related issues, this medication has proven to be a valuable tool in the arsenal of healthcare professionals.

Understanding the Mechanism of Action

Trazodone works by restoring the balance of a crucial neurotransmitter in the brain known as serotonin. Serotonin plays a crucial role in regulating mood, appetite, and sleep patterns. By modulating the availability of serotonin, trazodone can help alleviate the symptoms of depression, improve sleep quality, and enhance overall well-being.

Navigating the Dosage and Administration

Trazodone is typically taken orally, either once or twice daily, with or without food. The dosage is tailored to the individual’s needs, with healthcare providers starting at a low dose and gradually increasing it as necessary. It is important to follow the prescribed dosage instructions carefully to ensure optimal therapeutic benefits and minimize the risk of side effects.

Addressing Potential Side Effects

Like any medication, trazodone may cause a range of side effects, including nausea, dizziness, drowsiness, and dry mouth. While these side effects are generally mild and manageable, it is crucial to report any persistent or concerning symptoms to your healthcare provider. Strategies such as staying hydrated, adjusting the timing of medication, and using sugarless candies or gum can help alleviate some of the side effects.

Warnings and Precautions

Antidepressant medications, including trazodone, carry a small risk of worsening depression or triggering suicidal thoughts, especially in younger individuals. It is essential to closely monitor for any changes in mood, behavior, or mental state, and to promptly report any concerning symptoms to your healthcare provider.

Trazodone’s Versatility in Mental Health Management

While initially developed as an antidepressant, trazodone has been found to be effective in treating a range of other mental health conditions, such as anxiety, insomnia, and even certain types of chronic pain. This versatility makes trazodone a valuable option for healthcare providers when developing comprehensive treatment plans for their patients.

Optimizing Trazodone Therapy

To ensure the most successful outcome, it is crucial to work closely with your healthcare provider when taking trazodone. Regular follow-up appointments, open communication about any changes in symptoms or side effects, and adherence to the prescribed treatment plan are essential for maximizing the benefits of this medication.

What are the common side effects of trazodone?

The most common side effects of trazodone include nausea, vomiting, diarrhea, drowsiness, dizziness, tiredness, blurred vision, changes in weight, headache, muscle aches, dry mouth, bad taste in the mouth, stuffy nose, constipation, and changes in sexual interest or ability. If any of these side effects persist or worsen, it is important to inform your healthcare provider.

How long does it take for trazodone to start working?

It may take 2 to 4 weeks before you notice the full effects of trazodone. It is important to continue taking the medication as prescribed, even if you feel better, as stopping the medication abruptly can lead to withdrawal symptoms such as anxiety, agitation, and trouble sleeping.

What should I do if I experience worsening depression or suicidal thoughts while taking trazodone?

If you experience worsening depression, unusual behavior changes, or suicidal thoughts while taking trazodone, it is crucial to immediately inform your healthcare provider. They may need to adjust your medication or dosage, or refer you for additional support and monitoring to ensure your safety and well-being.

Can trazodone be used to treat conditions other than depression?

Yes, trazodone has been found to be effective in treating a variety of mental health conditions beyond depression, such as anxiety, insomnia, and certain types of chronic pain. Healthcare providers may prescribe trazodone off-label for these conditions based on their clinical expertise and the patient’s individual needs.

How important is it to follow the prescribed dosage instructions for trazodone?

It is extremely important to follow the prescribed dosage instructions for trazodone. Do not increase your dose or take the medication more often than prescribed, as this can increase the risk of serious side effects. It is also crucial to not stop taking trazodone without consulting your healthcare provider, as sudden discontinuation can lead to withdrawal symptoms.

What should I do if I experience dizziness or lightheadedness while taking trazodone?

To reduce the risk of dizziness and lightheadedness, it is recommended to get up slowly when rising from a sitting or lying position. If you experience persistent or severe dizziness, be sure to inform your healthcare provider, as they may need to adjust your dosage or explore alternative treatment options.

Trazodone Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Warnings:

Antidepressant medications are used to treat a variety of conditions, including depression and other mental/mood disorders. These medications can help prevent suicidal thoughts/attempts and provide other important benefits. However, studies have shown that a small number of people (especially people younger than 25) who take antidepressants for any condition may experience worsening depression, other mental/mood symptoms, or suicidal thoughts/attempts. It is very important to talk with the doctor about the risks and benefits of antidepressant medication (especially for people younger than 25), even if treatment is not for a mental/mood condition.

Tell the doctor right away if you notice worsening depression/other psychiatric conditions, unusual behavior changes (including possible suicidal thoughts/attempts), or other mental/mood changes (including new/worsening anxiety, panic attacks, trouble sleeping, irritability, hostile/angry feelings, impulsive actions, severe restlessness, very rapid speech). Be especially watchful for these symptoms when a new antidepressant is started or when the dose is changed.

Warnings:

Antidepressant medications are used to treat a variety of conditions, including depression and other mental/mood disorders. These medications can help prevent suicidal thoughts/attempts and provide other important benefits. However, studies have shown that a small number of people (especially people younger than 25) who take antidepressants for any condition may experience worsening depression, other mental/mood symptoms, or suicidal thoughts/attempts. It is very important to talk with the doctor about the risks and benefits of antidepressant medication (especially for people younger than 25), even if treatment is not for a mental/mood condition.

Tell the doctor right away if you notice worsening depression/other psychiatric conditions, unusual behavior changes (including possible suicidal thoughts/attempts), or other mental/mood changes (including new/worsening anxiety, panic attacks, trouble sleeping, irritability, hostile/angry feelings, impulsive actions, severe restlessness, very rapid speech). Be especially watchful for these symptoms when a new antidepressant is started or when the dose is changed.

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Uses

This medication is used to treat depression. It may help to improve your mood, appetite, and energy level as well as decrease anxiety and insomnia related to depression. Trazodone works by helping to restore the balance of a certain natural chemical (serotonin) in the brain.

How to use Trazodone HCL

Read the Medication Guide provided by your pharmacist before you start using trazodone and each time you get a refill. If you have any questions, consult your doctor or pharmacist.

Take this medication by mouth after a meal or snack as directed by your doctor, usually once or twice daily. If drowsiness is a problem and you are taking 1 dose daily, take it at bedtime. If you are taking 2 doses each day, it may help to take 1 of the doses at bedtime. Follow your doctor’s directions carefully.

Dosage is based on your medical condition and response to treatment. To reduce your risk of side effects, your doctor may start you at a low dose and gradually increase your dose.

Take this medication exactly as prescribed. Do not increase your dose or take this medication more often than prescribed. Your condition will not improve any faster, and the risk of serious side effects may be increased.

Keep taking this medication as prescribed even if you feel well. To help you remember, take it at the same time(s) each day. Do not stop taking this medication without consulting your doctor. Anxiety, agitation, and trouble sleeping can occur if the drug is suddenly stopped.

It may take 2 to 4 weeks before you notice the full effects of this medication. Tell your doctor if your condition lasts or gets worse.

Side Effects

See also the Warning section.

Nausea, vomiting, diarrhea, drowsiness, dizziness, tiredness, blurred vision, changes in weight, headache, muscle ache/pain, dry mouth, bad taste in the mouth, stuffy nose, constipation, or change in sexual interest/ability may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

To relieve dry mouth, suck on (sugarless) hard candy or ice chips, chew (sugarless) gum, drink water, or use a saliva substitute.

To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.

Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor right away if you have any serious side effects, including: shaking (tremors), nightmares, ringing in the ears, problems urinating, blood in urine, signs of infection (such as such as sore throat that doesn’t go away, fever), shortness of breath, stomach/abdominal pain.

Get medical help right away if you have any very serious side effects, including: chest/jaw/left arm pain, fainting, fast/irregular heartbeat, seizures, eye pain/swelling/redness, widened pupils, vision changes (such as seeing rainbows around lights at night).

This medication may increase serotonin and rarely cause a very serious condition called serotonin syndrome/toxicity. The risk increases if you are also taking other drugs that increase serotonin, so tell your doctor or pharmacist of all the drugs you take (see Drug Interactions section). Get medical help right away if you develop some of the following symptoms: fast heartbeat, hallucinations, loss of coordination, severe dizziness, severe nausea/vomiting/diarrhea, twitching muscles, unexplained fever, unusual agitation/restlessness.

Rarely, males may have a painful or prolonged erection lasting 4 or more hours. If this occurs, stop using this drug and get medical help right away, or permanent problems could occur.

A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US – Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.

In Canada – Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Precautions

Before taking trazodone, tell your doctor or pharmacist if you are allergic to it; or to nefazodone; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: personal or family history of bipolar disorder, personal or family history of suicide attempts, heart disease (such as irregular heartbeat, heart attack), liver disease, kidney disease, blood pressure problems, personal or family history of glaucoma (angle-closure type).

This drug may make you dizzy or drowsy or blur your vision. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness or clear vision until you can do it safely. Limit alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).

Trazodone may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.

The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using trazodone, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).

Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/”water pills”) or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using trazodone safely.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Older adults may be more sensitive to the side effects of this drug, especially drowsiness, dizziness, and QT prolongation (see above).

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

Since untreated mental/mood problems (such as depression) can be a serious condition, do not stop taking this medication unless directed by your doctor. If you are planning pregnancy, become pregnant, or think you may be pregnant, immediately discuss with your doctor the benefits and risks of using this medication during pregnancy.

This medication passes into breast milk. Consult your doctor before breast-feeding.

Interactions

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor’s approval.

A product that may interact with this drug is: digoxin.

Taking MAO inhibitors with this medication may cause a serious (possibly fatal) drug interaction. Avoid taking MAO inhibitors (isocarboxazid, linezolid, metaxalone, methylene blue, moclobemide, phenelzine, procarbazine, rasagiline, safinamide, selegiline, tranylcypromine) during treatment with this medication. Most MAO inhibitors should also not be taken for two weeks before and after treatment with this medication. Ask your doctor when to start or stop taking this medication.

Other medications can affect the removal of trazodone from your body, which may affect how trazodone works. Examples include azole antifungals (such as itraconazole, ketoconazole), HIV protease inhibitors (such as indinavir), macrolide antibiotics (such as erythromycin), ritonavir, drugs used to treat seizures (such as phenytoin), among others.

The risk of serotonin syndrome/toxicity increases if you are also taking other drugs that increase serotonin. Examples include street drugs such as MDMA/”ecstasy,” St. John’s wort, certain antidepressants (including SSRIs such as fluoxetine/paroxetine, SNRIs such as duloxetine/venlafaxine), among others. The risk of serotonin syndrome/toxicity may be more likely when you start or increase the dose of these drugs.

Tell your doctor or pharmacist if you are taking other products that cause drowsiness including alcohol, marijuana (cannabis), antihistamines (such as cetirizine, diphenhydramine), drugs for sleep or anxiety (such as alprazolam, diazepam, zolpidem), muscle relaxants, and opioid pain relievers (such as codeine).

Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.

Does Trazodone HCL interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose

If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: painful/prolonged erection, slow/rapid/irregular heartbeat, unusual drowsiness, unusual dizziness, vomiting, trouble breathing, seizures.

Do not share this medication with others.

Lab and/or medical tests should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.

If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

Images

trazodone 100 mg tablet

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This medicine is a white, round, scored, tablet imprinted with “8 06”.

trazodone 100 mg tablet

Color: whiteShape: roundImprint: 13 31

This medicine is a white, round, scored, tablet imprinted with “8 06”.

trazodone 50 mg tablet

Color: whiteShape: roundImprint: 13 30

This medicine is a white, round, scored, tablet imprinted with “8 06”.

trazodone 100 mg tablet

Color: whiteShape: roundImprint: MP 114

This medicine is a white, round, scored, tablet imprinted with “8 06”.

trazodone 150 mg tablet

Color: whiteShape: ovalImprint: PLIVA 441 50 50 50

This medicine is a white, round, scored, tablet imprinted with “8 06”.

trazodone 150 mg tablet

Color: whiteShape: ovalImprint: IT 150 50 50 50

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Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.

CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.

Antidepressant, Sleeping Pill, or Both?

Although trazodone was designed to treat depression and anxiety disorders, the medication is now widely prescribed as a nighttime sleep aid

What is trazodone?

Trazodone was developed in Italy in the 1960s as an antidepressant medication. Due to negative side effects associated with the drug early on—including dizziness, fainting, irregular heartbeat (and in rare cases, priapism in men)—the antidepressant wasn’t widely favored in the medical community. Eventually, however, internists and clinicians recognized potential benefits of the drug, particularly when administered at low doses. In 1981, trazodone (the generic name of the pharmaceutical) was approved by the U.S. Food and Drug Administration (FDA) under the brand name Desyrel for use in treating major depressive disorder. Today, the medication is prescribed under the brand name Oleptro to treat sleep disorders such as insomnia as well as anxiety disorder and unipolar depression.

Does trazodone cause sleepiness?

For many patients, the drug has a sedative effect, inducing a relaxed, sleepy feeling. In prescribing the drug for sleep disorders, physicians typically recommend taking a low dose at bedtime in order to limit the effects of drowsiness. Still, some people report lingering effects, including sluggishness and feeling zapped of energy, particularly upon waking.

How does trazodone help to alleviate depression?

Trazodone increases natural neurotransmitters in the central nervous system, essentially restoring depleted chemicals in the brain. One of these important neurotransmitters—serotonin—regulates our internal clock for resting and being awake, as well as mood, appetite, digestion, memory, sexual function and desire. Many experts believe depression involves an imbalance among the brain’s neurotransmitters (acetylcholine, norepinephrine, dopamine and serotonin.) While the cause of depression is not fully understood, trazodone affects the brain’s neurotransmitters by inhibiting the uptake of serotonin by nerves and stimulating other nerves.

How quickly does the drug take effect?

Patients who take the drug for a sleep disorder can experience the sedative effects within 30 minutes, depending on the type used. Patients who take the drug as an antidepressant may not notice symptom relief for one to two weeks, and it may take up to four weeks to experience the full benefits.

Is it safe to take trazodone to treat depression?

Like all medications, trazodone can cause side effects in some people. Ask your physician to discuss all potential side effects as well as drug interactions and potential withdrawal symptoms associated with the medication.

Do all antidepressant drugs work the same way?

While all antidepressant medications are designed to affect brain chemistry, various pharmaceutical formulations of the drugs have different targets and paths. The most commonly prescribed antidepressants are reuptake inhibitors. Reuptake, as described by WebMD, is “the process in which neurotransmitters are naturally reabsorbed back into nerve cells in the brain after they are released to send messages between nerve cells. ” A reuptake inhibitor, then, keeps levels of neurotransmitters in the gap between nerves, potentially strengthening circuits in the brain that regulate mood. There are three different types: selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), and norepinephrine and dopamine reuptake inhibitors (NDRIs). Common SSRIs are Prozac, Zoloft, Paxil, Lexapro, Celexa and Luvox; common SNRIs include Cymbalta and Effexor; and NDRIs are found in only one drug: Wellbutrin.

Because trazodone doesn’t fall under any of these categories, it’s often referred to as an “atypical antidepressant.”

Is it safe to take trazodone for insomnia?

Although trazodone was designed to treat depression and anxiety disorders, the medication is now widely prescribed as a nighttime sleep aid for patients who suffer from acute insomnia.

How is trazodone different from other “sleeping pill” drugs?

Trazodone differs from Ambien, Sonata, Lunesta and other “sleeping pill” medications in a few ways:

  • Both Ambien and Lunesta are classified by the FDA as controlled substances because they have the potential for misuse and abuse, including dependence or addiction
  • Because trazodone is not a controlled substance, physicians aren’t limited in how many pills they can prescribe
  • It’s an inexpensive generic drug covered by most insurance companies
  • It’s not considered to be an addictive substance when used as prescribed

Trazodone should not be taken by pregnant women or women who are breastfeeding.

What risks are associated with taking trazodone to treat depression?

There are heightened risks for patients under age 24, particularly with regard to mental health. According to Medline Plus, the following side effects and symptoms can occur among patients under age 24: “new or worsening depression; thinking about harming or killing yourself, or planning or trying to do so; extreme worry; agitation; panic attacks; difficulty falling asleep or staying asleep; aggressive behavior; irritability; acting without thinking; severe restlessness; and frenzied abnormal excitement.” If any of these symptoms or side effects are experienced, it’s crucial to consult a physician or medical professional immediately.

It’s also imperative that patients know what to avoid while taking SSRIs, SNRIs or other antidepressants. Whether a person has a cold, is having trouble sleeping or is searching for allergy relief, they should talk to their doctor before self-treating with an over-the-counter medication. According to Psychiatry Advisor, one patient who was taking melatonin for insomnia while also prescribed an SSRI woke up with a “headache, dizziness and feeling like his face was on fire”—signs of elevated blood pressure that could have been severe had he taken higher doses. Taking an antidepressant medication in combination with supplements, such as St. John’s wort or aspirin, can increase the likelihood of upper gastrointestinal bleeding. To avoid adverse drug reactions, experts advise making a list of all medications, supplements and other OTC drugs, and sharing it with your physician prior to taking trazodone.

Is it safe to use trazodone with alcohol or other drugs?

Absolutely not. Since both alcohol and trazodone affect the central nervous system, the consequences of mixing the two can be deadly. And mixing the medication with drugs of abuse can result in the onset of serotonin syndrome, a potentially lethal adverse drug reaction. While the potential for trazodone abuse is fairly low, any amount over 600 mg. in 24 hours is an overdose.

What happens if you take too much trazodone? Can it cause serotonin syndrome?

Serotonin syndrome occurs when, according to Mayo Clinic, “high levels of serotonin accumulate in the body.” This is a drug-to-drug interaction involving the over-stimulation of central and peripheral receptors. According to the journal U.S. Pharmacist, “Serotonin syndrome (SS) is caused most often when certain antidepressant agents are taken concurrently with other drugs that modulate synaptic serotonin levels. When patients take two or more antidepressants from different pharmacologic classes, drug-drug interactions may occur; these interactions may lead to potentially severe serotonin toxicity, or serotonin syndrome.” Clinical symptoms of serotonin syndrome can develop within two hours—or up to 24 hours—after taking an increased dose or adding another serotonergic drug.

Signs and symptoms of serotonin syndrome:

  • Tremors
  • Muscle aches
  • Sweating
  • Anxiety
  • Confusion
  • Tachycardia
  • Delirium
  • Hallucinations
  • Seizures
  • Renal failure
  • Death

What are the side effects of trazodone?

Trazodone usage can cause a decrease in sodium levels in the body, a disruption of the nervous system or serotonin syndrome. The most common side effects include:

  • Drowsiness (including feeling groggy the next day)
  • Dizziness (including an increased risk of fainting/falling)
  • Dry mouth
  • Constipation
  • Headache
  • Fatigue
  • Tingling or numbness in hands, arms or legs
  • Blurred vision
  • Disorientation
  • Vertigo
  • Nasal congestion
  • Shaking
  • Anxiety
  • Muscle aches
  • Prolonged and painful erections lasting longer than six hours (priapism) 
  • Abnormally low blood pressure
  • Heart rhythm disorders 
  • Increased risk of suicidal thoughts and behavior in children and adolescents (even when taken at approved doses for depression)
  • Acting on dangerous impulses
  • Insomnia (at high doses)
  • Weight gain or loss

The drug can stay in a person’s system for 42 hours after the final dose. Higher doses can produce more severe side effects.

Can you become addicted to trazodone?

While the drug is considered non-addictive and non-habit-forming, it should only be taken as prescribed and under a physician’s care in order to avoid misuse. This is especially important for individuals who have a history of substance abuse or other drug addiction. Warning signs of drug misuse include using the sleep aid/antidepressant without a prescription, using the medication at higher doses than prescribed, or snorting or crushing the tablets to speed up the intended effects.

Can you fail a drug test while taking trazodone?

Even though the antidepressant/sleep aid is not classified as a narcotic, it can cause false positives on drug tests. According to the National Center for Biotechnology Information, “The trazodone metabolite meta-Chlorophenylpiperazine [m-CPP] can cause false-positive urine amphetamine immunoassay results.…Further, we found that patients taking trazodone can produce urine with sufficient m-CPP to result in false-positive Amphetamines II results.”

What are trazodone’s withdrawal symptoms?

Although technically a non-addictive substance, regular use of the medication can result in mild physical dependence. For this reason, trazodone withdrawal is a concern. Rather than discontinuing use “cold-turkey,” physicians typically recommend a gradual tapering. This approach is considered a better protocol to avoid potential discomfort associated with trazadone withdrawal syndrome, also known as discontinuation syndrome.

Symptoms of trazodone withdrawal include:

  • Agitation
  • Confusion
  • Rapid mood swings
  • Muscle pain
  • Weakness
  • Dizziness
  • Stomach pain
  • Sweating
  • Insomnia
  • Fatigue

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Trazodone – description of the substance, pharmacology, use, contraindications, formula

Contents

  • Structural formula

  • Russian name

  • English name

  • Latin name

  • chemical name

  • Gross formula

  • Pharmacological group of the substance Trazodone

  • Nosological classification

  • CAS code

  • pharmachologic effect

  • Characteristic

  • Pharmacology

  • The use of the substance Trazodone

  • Contraindications

  • Application restrictions

  • Use during pregnancy and lactation

  • Side effects of Trazodone

  • Interaction

  • Overdose

  • Dosage and administration

  • Precautionary measures

  • Trade names with the active ingredient Trazodone

Structural formula

Russian name

Trazodone

English name

Trazodone

Latin name

Trazodonum ( genus Trazodoni)

Chemical name

-one (as hydrochloride)

Gross formula

C 19 H 22 ClN 5 O

Pharmacological group of the substance Trazodone

Antidepressants

Nosological classification

List of ICD-10 codes

CAS code

19794-93-5

Pharmacological action

Pharmacological action

antidepressant .

Characteristic

Thiazolopyridine derivative; according to its chemical structure, it does not belong to tricyclic, tetracyclic or other groups of antidepressants. Trazodone hydrochloride is a white, odorless, crystalline powder that is readily soluble in water. Molecular weight 408.33.

Pharmacology

The mechanism of action is not fully understood. Preclinical studies have shown that trazodone selectively inhibits the reuptake of serotonin by brain synaptosomes and acts as a 5-HT 2A/2C serotonin receptor antagonist. Does not inhibit MAO, does not stimulate the central nervous system. It is an antagonist of alpha 1 -adrenergic receptors.

Relieves mental (affective tension, fear, insomnia) and somatic (palpitations, headache, myalgia, frequent urination, increased sweating) manifestations of anxiety. Increases the depth and duration of sleep in depressed patients, restores the physiological structure of sleep.

Well absorbed from the gastrointestinal tract. Taking trazodone during or immediately after a meal slows down the rate of absorption, reduces max “> C max of trazodone in the blood and increases max”> T max (T max is 0.5-2 hours). Plasma protein binding 89-95%. Passes through histohematic barriers, including the BBB. It is metabolized in the liver, mainly with the participation of the CYP3A4 isoenzyme of cytochrome P450, the active metabolite is m-chlorophenylpiperazine. 1/2″>T 1/2 biphasic: early phase 3-6 hours, late 5-9h; in some patients cumulation is possible. Excreted in bile (20%) and urine (75%, including 70% as inactive metabolites) within 98 hours after ingestion.

Trazodone has been shown to be effective in bulimia, kleptomania, diabetic neuropathy pain and other types of chronic pain, phobias, incl. agoraphobia, panic attacks, acute withdrawal syndrome in alcoholism and for the prevention of migraine.

The use of the substance Trazodone

Depressive states of various etiologies (endogenous, psychotic, neurotic, somatogenic, etc. ) with severe anxiety, tension.

Contraindications

Hypersensitivity, alcohol intoxication and intoxication with sleeping pills, age up to 6 years.

Restrictions on use

Myocardial infarction (early recovery period), AV blockade, arterial hypertension (dose adjustment of antihypertensive drugs may be required), ventricular arrhythmia, history of priapism, liver and / or kidney failure, age up to 18 years.

Use during pregnancy and lactation

Not to be used by pregnant women. Animal studies have shown that trazodone at doses 30 to 50 times the MRHD causes congenital malformations and increases the rate of fetal resorption.

FDA Fetal Category C.

Stop breastfeeding during treatment. Trazodone and its metabolites are found in the milk of lactating rats. It is not known whether trazodone is secreted into human breast milk.

Side effects of the substance Trazodone

From the nervous system and sensory organs: fatigue, weakness, headache, dizziness, insomnia, drowsiness, agitation, psychosis, hypomania, hallucinations, tremor, muscle twitching, grand mal seizures (grand mal) , aphasia, ataxia, akathisia, dyskinesia, paresthesia, confusion, syncope, blurred vision, diplopia.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): arterial hypotension, incl. orthostatic; atrial fibrillation, arrhythmias (including tachycardia and bradycardia, ectopic ventricular rhythms), congestive heart failure, leukocytosis or leukopenia, neutropenia (usually minor), hemolytic anemia, methemoglobinemia.

From the digestive tract: increased appetite, dryness and unpleasant taste in the mouth, hypersalivation, caries, diseases of the periodontal tissues, oral candidiasis, nausea, vomiting, flatulence, diarrhea, constipation, cholestasis, increased levels of bilirubin and amylase in plasma blood, jaundice.

From the genitourinary system: urinary retention, increased urination, hematuria, premature menstruation, hirsutism, increased libido, priapism, impotence, retrograde ejaculation.

Allergic reactions: skin rash, urticaria.

Other: myalgia, chest pain, alopecia, psoriasis, edema.

Interaction

Unlike typical antidepressants, it does not reduce the depriming effects of reserpine, weakens the central effect of amphetamine and the peripheral effect of norepinephrine. Potentiates the effect of drugs that depress the central nervous system (including barbiturates, tricyclic antidepressants, antihistamines, clonidine, alcohol), anticholinergics and muscle relaxants. When taken simultaneously with antihypertensive drugs, the risk of orthostatic hypotension increases. Weakens the effect of psychostimulants. Increases the plasma concentration of digoxin and phenytoin. It should not be used simultaneously with MAO inhibitors.

Overdose

Symptoms: nausea, vomiting, drowsiness, dizziness, lowering blood pressure, impaired coordination, priapism, epileptiform seizures, ECG changes, respiratory arrest, worsening of adverse reactions.

Treatment: gastric lavage, forced diuresis, activated charcoal, maintenance of vital functions, symptomatic therapy. There is no specific antidote.

Route of administration and doses

Inside . Adults: the initial dose is 100 mg, once at bedtime, if necessary, the dose is increased by 50 mg / day every 3-4 days until a therapeutic effect is achieved. The maximum daily dose on an outpatient basis is 450 mg, in stationary conditions – 600 mg. For elderly and debilitated patients, the initial dose is up to 100 mg / day, if necessary, can be increased to 300 mg / day. Children 6–18 years: 1.5–2 mg/kg/day, if necessary, increase the dose to 6 mg/kg/day.

Precautions

During treatment, a complete blood count should be performed regularly (for the timely detection of leuko- and neutropenia), ECG monitoring is desirable in patients with cardiovascular diseases. Careful monitoring of patients with suicidal tendencies is required, especially in the first weeks of treatment. Treatment is immediately stopped with the development of priapism, severe neutro- and leukopenia; in other cases, drug withdrawal should be carried out gradually. Alcohol should be avoided during the treatment period.

Use with caution during work for drivers of vehicles and people whose activities are associated with increased concentration of attention.

Brand names with the active ingredient Trazodone

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Lek. form
All lek. sustained-release tablet forms controlled-release tablets sustained-release tablets

Dosage
All dosages 150 mg 75 mg

Manufacturer
Aziende Kimike Riunite Angelini Francesco A.K.R.A.F. S.p.A.

Description of TRAZODONE indications, dosages, contraindications of the active substance TRAZODONE

Rec.INN
WHO registered


drug interaction

Included in preparations:
list

Pharmacological action

Antidepressant, thiazolopyridine derivative. It also has a thymoleptic, anxiolytic, sedative and muscle relaxant effect. It has a high affinity for some subtypes of serotonin receptors, inhibits the reuptake of serotonin; little effect on neuronal uptake of norepinephrine and dopamine.

Does not have an anticholinergic effect, does not inhibit MAO, does not change body weight. Eliminates both mental (affective tension, irritability, fear, insomnia) and somatic manifestations of anxiety (palpitations, headache, myalgia, frequent urination, increased sweating). Increases the depth and duration of sleep in depressed patients, restores its physiological structure.

Reduces craving for ethanol. It is effective in withdrawal symptoms in patients with drug dependence on anxiolytic benzodiazepine derivatives, eliminates anxiety and depression and sleep disorders (during remission, benzodiazepines can be completely replaced by trazodone). Not addictive. Promotes the restoration of libido and potency.

The therapeutic effect in 50% of patients is observed after 3-7 days, in 25% after 2-4 weeks.

Pharmacokinetics

After oral administration, absorption from the gastrointestinal tract is high. The time to reach C max in plasma is 1-2 hours. Taking trazodone during or immediately after meals increases absorption, reduces C max and increases the time it takes to reach it.

Penetrates through histohematic barriers, including the BBB. Penetrates into tissues and fluids (bile, saliva, breast milk). Plasma protein binding – 89-95%.

Metabolized in the liver by hydroxylation. The isoenzymes CYP3A4, CYP3A5 and CYP3A7 are involved in the metabolism of the drug.

T 1/2 in the α-phase 3-6 hours, in the β-phase – 5-9 hours Excreted by the kidneys – 75% as inactive metabolites within 98 hours after administration; 20% – with bile.

Indications of the active substance
TRAZODONE

Various forms of depression (endogenous, psychotic, neurotic, somatogenic) incl. with severe anxiety, including at least 4 of the following signs: sleep disturbance, appetite disturbance, psychomotor agitation or lethargy, decreased interest in the environment, decreased sexual activity, guilt, increased fatigue, slow thinking, decreased ability to concentrate, suicidal attempts / thoughts ; bulimia, kleptomania, anxiety, phobias. Benzodiazepine drug dependence; acute alcohol withdrawal syndrome. Decreased libido, impotence. Prevention of migraine attacks.

Open list of ICD-10 codes

F10.3 Withdrawal state
F13 Mental and behavioral disorders due to the use of hypnotics or sedatives
F31 Bipolar affective disorder
F32 Depressive episode
F33 Recurrent depressive disorder
F40 Phobic anxiety disorders (including agoraphobia, social phobias)
F41. 1 Generalized anxiety disorder
F41.2 Mixed anxiety and depressive disorder
F41.9 Anxiety disorder, unspecified
F50.2 Bulimia nervosa
F52.0 Lack or loss of sexual desire
F52.2 Lack of genital response (psychogenic impotence)
F63.2 Pathological desire to steal [kleptomania]
G43 Migraine

Dosing regimen

The initial daily dose is 150-200 mg (in 3 divided doses). In mild forms of depression, the average maintenance dose is 150 mg / day; in moderate and severe forms – 300 mg / day. If necessary, the dose can be increased to 600 mg / day. The main part of the daily dose is recommended to be taken at bedtime.

Side effects

From the side of the central nervous system and peripheral nervous system: drowsiness, fatigue, dizziness, insomnia, headache, agitation, myalgia, impaired coordination of movements, paresthesia, disorientation, obscuration of consciousness, tremor.

From the side of the cardiovascular system: arrhythmia, conduction disturbance, bradycardia, ventricular fibrillation, decreased blood pressure, orthostatic hypotension, fainting.

From the digestive system: nausea, vomiting, diarrhea, dryness and bitterness in the mouth.

On the part of the organ of vision: blurred vision, eye irritation.

From the hematopoietic system: leukopenia, neutropenia (usually minor).

Other: nasal congestion, priapism followed by impotence, allergic reactions.

Contraindications

Ventricular arrhythmia, tachycardia, myocardial infarction (early recovery period), history of priapism, pregnancy, lactation, hypersensitivity to trazodone.

Use during pregnancy and lactation

Use during pregnancy and lactation is contraindicated.

Use in hepatic impairment

Use with caution in hepatic impairment.

Use in impaired renal function

Use with caution in renal insufficiency.

Use in children

Use with caution in children and adolescents under 18 years of age.

Special instructions

Use with caution in heart disease, arterial hypotension, arterial hypertension, renal and / or liver failure, in children and adolescents under the age of 18 years.

Do not use concomitantly with MAO inhibitors.

Drug Interactions

A case of torsades de pointes arrhythmia has been described with concomitant use of trazodone with amiodarone.

A case has been described of a moderate decrease in the anticoagulant effect of warfarin when co-administered with trazodone.

With simultaneous use, an increase in the concentration of digoxin in the blood plasma and the development of symptoms of intoxication are possible.

When used simultaneously with carbamazepine, a case of increased plasma concentrations of carbamazepine has been described.

When used simultaneously with lithium salts, tremor, reversible symptoms of neurotoxic action are possible.

When taking pseudoephedrine against the background of trazodone therapy, a case of anxiety, panic, blackout, depersonalization was described.

With simultaneous use with thioridazine, an increase in the concentration of trazodone in the blood plasma is possible; with tryptophan – a case of development of anorexia, psychosis, hypomania is described; with phenytoin – a case of increased side effects of phenytoin is described; with fluoxetine – possibly increased side effects; with chlorpromazine, trifluoperazine – the development of arterial hypotension is possible.

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