How is metaxalone prescribed for muscle injuries. What are the common side effects of metaxalone. How should metaxalone be taken and stored properly. What precautions should be considered when using metaxalone.

Understanding Metaxalone: A Comprehensive Guide to This Muscle Relaxant

Metaxalone, pronounced as (me tax’ a lone), is a muscle relaxant medication used to alleviate pain and discomfort associated with various muscle injuries. This drug plays a crucial role in managing muscle-related conditions when combined with other therapeutic approaches.

Primary Uses of Metaxalone

Metaxalone is primarily prescribed for:

• Relaxing muscles
• Relieving pain and discomfort
• Treating strains and sprains
• Managing various muscle injuries

It’s important to note that metaxalone is typically used in conjunction with other treatment modalities, including rest and physical therapy, to achieve optimal results.

Proper Administration and Dosage of Metaxalone

How should metaxalone be taken? Metaxalone is available as an oral tablet and is usually prescribed to be taken three to four times daily. The exact dosage and frequency may vary based on individual needs and the prescribing physician’s recommendations.

To ensure proper use:

1. Follow the directions on your prescription label carefully
2. Consult your doctor or pharmacist if any part of the instructions is unclear
3. Take metaxalone exactly as directed, without altering the dosage or frequency

Missed Dose Protocol

If you forget to take a dose, what should you do? Take the missed dose as soon as you remember. However, if it’s almost time for your next scheduled dose, skip the missed one and continue with your regular dosing schedule. It’s crucial not to double up on doses to compensate for a missed one.

Potential Side Effects and Adverse Reactions to Metaxalone

Like all medications, metaxalone can cause side effects. It’s essential to be aware of both common and severe side effects to ensure safe usage.

Common Side Effects

Some frequently reported side effects include:

• Drowsiness
• Dizziness
• Headache
• Nervousness

These side effects are generally mild and may subside as your body adjusts to the medication. However, if they persist or worsen, it’s advisable to consult your healthcare provider.

Severe Side Effects

While rare, some users may experience more serious side effects that require immediate medical attention:

• Agitation or hallucinations
• Rapid heart rate or high body temperature
• Muscle twitching or loss of muscle control
• Severe gastrointestinal symptoms (nausea, vomiting, diarrhea)
• Severe skin rash
• Difficulty breathing
• Yellowing of skin or eyes (jaundice)
• Unusual bruising or bleeding
• Extreme fatigue or weakness
• Seizures

If you experience any of these severe side effects, it’s crucial to seek medical help immediately.

Essential Precautions and Considerations for Metaxalone Use

Before starting metaxalone treatment, it’s vital to inform your healthcare provider about certain factors that may affect your ability to use this medication safely.

Medical History and Current Conditions

Disclose if you have or have had:

• Kidney disease
• Liver disease
• Seizures
• Blood disorders

Pregnancy and Breastfeeding

Are you pregnant, planning to become pregnant, or breastfeeding? It’s crucial to discuss these circumstances with your doctor, as metaxalone may pose risks to fetal development or nursing infants.

Age Considerations

For individuals aged 65 or older, the use of metaxalone requires careful consideration. Older adults may be more susceptible to side effects, and alternative medications might be preferable for treating muscle-related conditions in this age group.

Interactions with Other Substances

How does metaxalone interact with other substances? It’s essential to be aware of potential interactions with:

• Other prescription medications
• Over-the-counter drugs
• Vitamins and nutritional supplements
• Herbal products
• Alcohol

Alcohol can enhance the drowsiness caused by metaxalone, potentially increasing the risk of accidents or injuries. Always consult your healthcare provider about potential interactions before starting metaxalone treatment.

Safe Storage and Disposal of Metaxalone

Proper storage and disposal of metaxalone are crucial for maintaining its effectiveness and preventing accidental ingestion by others, especially children and pets.

Storage Guidelines

To store metaxalone safely:

• Keep it in its original container
• Ensure the container is tightly closed
• Store at room temperature
• Avoid exposure to excess heat and moisture
• Keep out of reach and sight of children

Proper Disposal Methods

How should unused or expired metaxalone be disposed of? The best approach is to participate in a medicine take-back program. If this option is unavailable:

1. Do not flush the medication down the toilet
2. Contact your local garbage or recycling department for guidance
3. Follow the FDA’s Safe Disposal of Medicines guidelines

Recognizing and Responding to Metaxalone Overdose

While rare, metaxalone overdose can occur and requires immediate medical attention. Understanding the signs and knowing how to respond can be life-saving.

Overdose Symptoms

Potential signs of metaxalone overdose may include:

• Severe drowsiness
• Confusion or disorientation
• Difficulty breathing
• Loss of consciousness
• Seizures

Emergency Response

If you suspect a metaxalone overdose:

1. Call the poison control helpline at 1-800-222-1222 immediately
2. If the person has collapsed, had a seizure, is having trouble breathing, or can’t be awakened, call emergency services right away
3. Provide as much information as possible about the person’s condition and the amount of medication taken

Metaxalone in Special Populations: Considerations and Adaptations

The use of metaxalone may require special considerations for certain groups of people. Understanding these nuances can help ensure safe and effective treatment.

Elderly Patients

Why is caution necessary when prescribing metaxalone to older adults? Elderly patients may be more sensitive to the effects of metaxalone and at higher risk for side effects. Doctors may consider:

• Starting with lower doses
• Monitoring more closely for adverse reactions
• Evaluating potential drug interactions with other medications commonly used by older adults

Patients with Liver or Kidney Impairment

For individuals with liver or kidney disease, metaxalone dosage may need to be adjusted. These organs play a crucial role in metabolizing and eliminating the drug from the body. Regular monitoring of liver and kidney function may be necessary during treatment.

Pregnant and Breastfeeding Women

The safety of metaxalone during pregnancy and breastfeeding is not well-established. Healthcare providers will carefully weigh the potential benefits against the risks when considering prescribing metaxalone to pregnant or nursing women. Alternative treatments may be explored in these cases.

Metaxalone vs. Other Muscle Relaxants: A Comparative Analysis

Understanding how metaxalone compares to other muscle relaxants can help patients and healthcare providers make informed decisions about treatment options.

Mechanism of Action

How does metaxalone work compared to other muscle relaxants? While the exact mechanism is not fully understood, metaxalone is believed to work centrally in the brain and spinal cord to produce its muscle-relaxing effects. This differs from some other muscle relaxants that may work directly on the muscles or through other pathways.

Efficacy and Side Effect Profile

Comparative studies have shown that metaxalone may have:

• Similar efficacy to other commonly prescribed muscle relaxants
• A potentially more favorable side effect profile, with less sedation reported by some patients
• Fewer interactions with other medications, making it a good choice for patients on multiple drugs

Duration of Action

Metaxalone’s effects typically last for 4-6 hours, which is comparable to many other muscle relaxants. This duration allows for flexible dosing schedules to meet individual patient needs.

Integrating Metaxalone into a Comprehensive Treatment Plan

While metaxalone can be an effective tool for managing muscle pain and spasms, it’s most beneficial when used as part of a comprehensive treatment approach.

Complementary Therapies

What other treatments can enhance the effectiveness of metaxalone? Consider incorporating:

• Physical therapy to improve strength and flexibility
• Heat or cold therapy for pain relief
• Gentle stretching exercises
• Massage or acupuncture
• Stress reduction techniques like meditation or yoga

Lifestyle Modifications

Certain lifestyle changes can support recovery and prevent future muscle injuries:

1. Maintaining good posture
2. Using ergonomic equipment at work and home
3. Engaging in regular, low-impact exercise
4. Getting adequate sleep and rest
5. Staying hydrated and eating a balanced diet

Monitoring and Follow-up

Regular check-ins with your healthcare provider are crucial when taking metaxalone. These appointments allow for:

• Assessing the medication’s effectiveness
• Adjusting dosage if necessary
• Monitoring for side effects
• Evaluating progress and determining when to discontinue use

Long-term Considerations and Alternatives to Metaxalone

While metaxalone can be effective for short-term relief, it’s important to consider long-term management strategies for chronic muscle conditions.

Duration of Use

How long should metaxalone be used? Typically, metaxalone is prescribed for short-term use, usually no more than 2-3 weeks. Prolonged use may lead to:

• Decreased effectiveness over time
• Increased risk of side effects
• Potential for dependence in some individuals

Alternative Treatments

For long-term management of muscle pain or spasms, consider exploring:

1. Non-pharmacological approaches like regular exercise and physical therapy
2. Alternative muscle relaxants with different mechanisms of action
3. Topical treatments for localized pain
4. Mind-body techniques like biofeedback or cognitive behavioral therapy
5. Interventional procedures for severe or persistent cases

Gradual Discontinuation

When stopping metaxalone, especially after prolonged use, it’s important to do so gradually under medical supervision. This can help prevent potential withdrawal symptoms and ensure a smooth transition to alternative management strategies.

Metaxalone: MedlinePlus Drug Information

pronounced as (me tax’ a lone)

To use the sharing features on this page, please enable JavaScript.

Metaxalone, a muscle relaxant, is used with rest, physical therapy, and other measures to relax muscles and relieve pain and discomfort caused by strains, sprains, and other muscle injuries.

Metaxalone comes as a tablet to take by mouth. It usually is taken three or four times a day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take metaxalone exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.

Before taking metaxalone,

• tell your doctor and pharmacist if you are allergic to metaxalone, any other medications, or any of the ingredients in metaxalone tablets. Ask your pharmacist for a list of the ingredients.
• tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take while taking metaxolone. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
• tell your doctor if you have or have ever had kidney disease, liver disease, seizures, or a blood disorder.
• tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while taking metaxalone, call your doctor immediately.
• talk to your doctor about the risks and benefits of taking metaxalone if you are 65 years of age or older. Older adults should not usually take metaxalone because it is not as safe or effective as other medications that can be used to treat the same condition.
• you should know that this drug may make you drowsy. Do not drive a car or operate machinery until you know how metaxalone affects you.
• remember that alcohol can add to the drowsiness caused by this drug.

Take the missed dose as soon as you remember it. However, if it is almost time for your next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

Metaxalone may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

• drowsiness
• dizziness
• headache
• nervousness

If you experience any of the following symptoms, call your doctor immediately:

• agitation, hallucinations, coma
• fast heart rate, high body temperature
• muscle twitching, loss of muscle control
• nausea, vomiting, diarrhea
• severe skin rash
• difficulty breathing
• yellowing of the skin or eyes
• unusual bruising or bleeding
• unusual tiredness or weakness
• seizures

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s (FDA) MedWatch Adverse Event Reporting program online (http://www. fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature, away from excess heat and moisture (not in the bathroom).

It is important to keep all medication out of sight and reach of children as many containers (such as weekly pill minders and those for eye drops, creams, patches, and inhalers) are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location – one that is up and away and out of their sight and reach. http://www.upandaway.org

Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of Medicines website (http://goo.gl/c4Rm4p) for more information if you do not have access to a take-back program.

In case of overdose, call the poison control helpline at 1-800-222-1222. Information is also available online at https://www.poisonhelp.org/help. If the victim has collapsed, had a seizure, has trouble breathing, or can’t be awakened, immediately call emergency services at 911.

• Skelaxin^®

Last Revised – 07/15/2022

Browse Drugs and Medicines

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

See also How to Use section.

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.

Some products that may interact with this drug include: diet pills/appetite suppressants (such as diethylpropion), drugs for attention deficit disorder (such as atomoxetine, methylphenidate), apraclonidine, bupropion, buspirone, carbamazepine, cyclobenzaprine, deutetrabenazine, a certain combination product (dextromethorphan/quinidine), levodopa, maprotiline, methyldopa, metoclopramide, certain opioid pain relievers (such as fentanyl, meperidine, methadone, tapentadol), certain drugs for Parkinson’s disease (such as entacapone, tolcapone), certain supplements (such as tryptophan, tyramine), tetrabenazine, tricyclic antidepressants (such as amitriptyline, doxepin), valbenazine.

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 mirtazapine, SSRIs such as fluoxetine/paroxetine, SNRIs such as duloxetine/venlafaxine), tramadol, certain “triptans” used to treat migraine headaches (such as rizatriptan, sumatriptan, zolmitriptan), among others. The risk of serotonin syndrome/toxicity may be more likely when you start or increase the dose of these drugs.

Some products can interact with metaxalone if you take them together, or even if you take them weeks before or after taking metaxalone. Tell your doctor or pharmacist if you take anything in the list of products that may interact with this drug, or any of the products that increase serotonin, within 2 weeks before or after taking metaxalone. Also tell them if you have taken fluoxetine within 5 weeks before starting metaxalone. Ask your doctor how much time to wait between starting or stopping any of these drugs and starting metaxalone.

Taking other MAO inhibitors with this medication may cause a serious (possibly fatal) drug interaction. Do not take any other MAO inhibitors (isocarboxazid, linezolid, 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.

Before using metaxalone, report the use of drugs that may increase the risk of extremely high blood pressure (hypertensive crisis) when combined with metaxalone, including herbal products (such as ephedra/ma huang), nasal decongestants (such as phenylephrine, pseudoephedrine), and stimulants (such as amphetamines, ephedrine, epinephrine, phenylalanine). Metaxalone should not be used with any of these medications. Talk to your doctor or pharmacist for more details.

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

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.

This medication may interfere with certain lab tests (such as certain urine glucose tests), possibly causing false test results. Make sure lab personnel and all your doctors know you use this drug.

Does Metaxalone interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Cheap analogs of expensive antibiotics: analogs of expensive drugs

Antibiotics are one of the most expensive groups of drugs. And if the cost of “old” antibiotics is more or less acceptable, then new broad-spectrum antibiotics are incredibly expensive, which is not surprising, because the development of one new antibiotic costs approximately 1 billion US dollars.

If you think about this topic, you can understand that there are not so many new antibiotics, because not only do development and clinical studies take decades, but also the cost of the project is equal to the cost of space flight. In this regard, very few pharmaceutical companies in the US and Europe can conduct such expensive research.

For example, Linezolid (trade name Zyvox) is the latest antibiotic to enter the market and is patented by Pfizer. At the same time, it was synthesized back in 1990, and only in 2000 was it first put into practice.

And what about other pharmaceutical companies, including domestic ones, who cannot afford such expenses? The answer is simple – they produce generics, that is, analogues of long-known antibiotics, with the same active ingredient as the original drug, but under a different trade name. The cost of such drugs is often lower than the cost of the original drug, but there are also opposite cases.

When prescribing antibiotic therapy, doctors can prescribe both the original drug – an expensive antibiotic (occurs less often), and its analogue – a cheap antibiotic (in most cases). The reason for this is the work of medical representatives of pharmaceutical companies and distributors. So if the doctor prescribed you an expensive antibiotic, do not rush to buy it at the expense of the budget. Most likely, he has a cheaper analogue, which a pharmacist in a pharmacy can also advise you if you ask him about it. However, it is worth remembering that from January 1, 2023 in Ukraine, you can buy an antibiotic only with an electronic prescription, which is pre-written to you by a doctor. The Doc.ua service also provides an opportunity to get an electronic prescription for antibiotics in just a few clicks. You can also buy all the necessary prescription drugs at the Doc.ua Pharmacy.

In this article we have provided a list of analogues of the most famous and widely used antibiotics.

Antibiotics for colds list Ukraine

Antibiotics of the penicillin group

Flemoxin Solutab , cases of bronchitis, sinusitis, pneumonia, peptic ulcer, cystitis and other

The average cost of Flemoxin Solutab and Ospamox is 80-150 UAH. Its analogue is Amoxil (amoxicillin analogues, amoxiclav analogues). The average cost is 50-70 UAH (inexpensive antibiotics for colds).

Antibiotics of the group of inhibitor-protected aminopenicillins

Flemoclav Solutab , Augmentin (amoxicillin and clavulanic acid).

This antibiotic is used to treat mild and uncomplicated cases of bronchitis, sinusitis, pneumonia, peptic ulcer, cystitis, etc. caused by b-lactamase producing bacteria.

The average cost of Flemoclav Solutab is 100-150 UAH, Augmentin is 130-190 UAH.

Flemoclav Solutab analogues, Augmentin analogues ( cheap broad-spectrum antibiotics):

Bactoclav is the cheapest antibiotic, the average price is 60 – 70 UAH.

Amoxil K, Medoklav, Abiklav, Amoksiklav 2x, Betaklav, are also inexpensive antibiotics for colds.

Antibiotics of the cephalosporin group

Emsef , Diacef , Denicef ​​ (ceftriaxone analogues in tablets) – Lorakson, Medakson (ceftriaxone analogue in tablets), Ceftriaxone-Darnitsa, Ceftriaxone-KMP, Ceftriaxone-Lekhim.

Antibiotics treat diseases such as sepsis, meningitis, disseminated Lyme borreliosis (early and late stages of the disease), infections of the abdominal cavity, etc. 27 (cefuroxime) – Aksetin, Aksef , Auroxetil.

Antibiotics treat urinary tract infections – cystitis, pyelonephritis, urethritis; skin and soft tissues – furunculosis, pyoderma, impetigo, etc.

Quadrocef , Roxipim , Abipim , Denipim 900 26, Exipim , Septipim (cefepime) – Cefepim-Lekhim, Cefepim Abryl, Cefepim Aurobindo.

Antibiotics treat respiratory diseases (pneumonia and bronchitis), urinary tract infections, and skin and soft tissue infections.

Eurosidim , Ceftazidime-Vista (ceftazidime) – Ceftazidime Yuria-pharm, Ceftum, Zacef, Ceftazidime-BHFZ.

These antibiotics are used to treat meningitis, sepsis and other illnesses.

Sorcef , Cefinac , Suprax Solutab (cefixime) – Lopraks, Opticef, Cefix.

Antibiotics treat diseases such as pharyngitis, tonsillitis, sinusitis, acute and chronic bronchitis, otitis media, and urinary tract infections.

Macrolide antibiotics

Sumamed , Azax , Azitrox , Aztec , Hemomycin , 9002 6 Zybax (azithromycin analogues are expensive, sumamed analogues) – Azibiot, Azipol, Zitrox, Ormax, Azimed (the best analogue sumamed) Azicin, Zoxy, Azithromycin-Astrapharm, Azithromycin-Health, Azithromycin-BHFZ, Azithromycin-Red Star, Ziomycin (azithromycin analogues of the drug).

These name antibiotics are used to treat pharyngitis, tonsillitis, sinusitis, otitis media, as well as acute bronchitis, pneumonia. 9Ora dro (clarithromycin analogs) – Aziklar, Clarithromycin-Health, Clarithromycin-Astrapharm, Clarithromycin-Darnitsa, Clarithromycin-Arterium, Clubax.

Antibiotics treat diseases such as infections of the upper respiratory tract and ENT organs: tonsillopharyngitis, otitis media, acute sinusitis, as well as infections of the lower respiratory tract: acute bronchitis, exacerbation of chronic bronchitis and others.

Antibiotics of the tetracycline group

Unidox Solutab (doxycycline) – its inexpensive antibiotics – analogues: Doxycycline-Teva, Doxycycline-Darnitsa, Doxycycline-BHFZ (inexpensive antibiotic).

Antibiotics are used to treat pharyngitis, bronchitis, tracheitis, bronchopneumonia, as well as otitis media, tonsillitis, sinusitis and others.

Antibacterial drugs of the fluoroquinolone group

Ofloxin (ofloxacin) – Ofloxacin-Darnitsa, Ofloxacin-Lekhim (inexpensive antibiotic).

Antibiotics treat infectious and inflammatory diseases of bones and joints, abdominal cavity, diseases of the kidneys (pyelonephritis) and urinary tract (cystitis, urethritis.

Abiflox , Levaksela, Lebel , Levoksimed, Levomak , Tigeron (levofloxacin) – Levokilz, Levofloxacin-Lekhim, Levofloxacin-Health, Floxium, Leflok.

Antibiotics are used to treat acute sinusitis, exacerbations of chronic bronchitis, community-acquired pneumonia, complicated urinary tract infections.

Avelox , Moxicum, Timoksi, Moxifloxacin-Sandoz (moxifloxacin) – Moxifloxacin-Lekhim, Moflaxa, Moxifloxacin-Pharmex, Atovax.

Antibiotics are used to treat acute sinusitis, exacerbation of chronic bronchitis, community-acquired pneumonia.

Cifran , Tsiprinol , Tsiprolet analogues , Flaprox, 900 26 Ciprobel (ciprofloxacin analogues are expensive) – Ciprofloxacin-Euro, Ciprofloxacin-Lekhim, Ciprofloxacin-Astrapharm, Citeral.

An antibiotic is used to treat sepsis and peritonitis and to prevent and treat infections in immunosuppressed patients.

Nitroimidazole antibacterials

Strong antibiotics in tablets

Trichopolum , Efloran (metronidazole) – Metrogyl, Metressa, Metronidazole-Health, Metronidazole-Darnitsa, Metronidazole-Infusion, Metronid Zol-Yuria Pharm, Metronidazole Lubnypharm.

Antibiotics treat protozoal infections: extraintestinal amoebiasis, including amoebic liver abscess, intestinal amoebiasis (amebic dysentery), trichomoniasis, giardiasis, balantidiasis, cutaneous leishmaniasis, trichomonas vaginitis, trichomonas urethritis, and others.

Ornigil , Ornizol, Ornimac (ornidazole) – Ornidazol-Darnitsa, Ornidazol-Novofarm, Ornidazol-Infusion.

Antibiotics are used to treat trichomoniasis, amoebiasis, giardiasis, and a mild antibiotic is used to prevent postoperative complications.

Antibiotic analogues table

Help DOC.ua: You can sign up for a consultation with a general practitioner on the website.

Medakson – instructions and analogues of the drug

Instructions for use

Contents of instructions

Composition

active substance: 1 bottle contains ceftriaxone sodium in terms of ceftriaxone 1 g.

Dosage form

Powder for solution for injection.

Pharmacotherapeutic group

Antibacterial agents for systemic use. Cephalosporins. Ceftriaxone. ATC code J01D D04.

Indications

Treatment of infections susceptible to ceftriaxone:

Preoperative prophylaxis of infections in gastrointestinal, biliary, urinary and gynecological surgery, but only in cases of potential or known contamination.

When prescribing the drug, it is necessary to follow official recommendations for antibiotic therapy and recommendations for the prevention of antibiotic resistance.

Contraindications

Hypersensitivity to cephalosporins, penicillins or other β-lactam antibiotics in history, to lidocaine or other amide local anesthetic drugs (when administered – to lidocaine).

Hyperbilirubinemia in neonates and premature infants. Ceftriaxone can displace bilirubin from its association with serum albumin, which may lead to the risk of developing bilirubin-induced encephalopathy.

The use of the drug is contraindicated in preterm infants under 41 weeks of gestational age (gestational age + age after birth) and in newborns ≤ 28 days of age (see section “Children”).

Never use ceftriaxone with calcium-containing solutions (Ringer’s solution). Calcium-containing solutions should not be administered within 48 hours after the last administration of ceftriaxone.

Dosage and administration

Adults and children over 12 years of age: Usually, 1-2 g of Medaxone should be given once a day (every 24 hours). In severe infections or infections with only moderate sensitivity to ceftriaxone, the daily dose may be increased up to 4 g.

Children

Neonates (under 2 weeks): 20-50 mg/kg body weight once a day. Given the underdevelopment of the enzyme system, the daily dose should not exceed 50 mg/kg of body weight. When determining the dose of full-term and premature babies, there are no differences.

Medaxone is contraindicated in neonates ≤ 28 days of age in case of need (or expected need) for treatment with intravenous solutions containing calcium, including intravenous infusions containing calcium, such as parenteral nutrition, due to the risk of precipitation of ceftriaxone calcium salts.

Children aged 15 days to 12 years 20-80 mg/kg body weight once a day. Children weighing more than 50 kg are prescribed doses as for adults.

Intravenous doses of 50 mg/kg or higher should be given by infusion over at least 30 minutes.

Do not exceed 80 mg/kg body weight due to increased risk of biliary precipitation.

Elderly patients

Elderly patients do not need dose adjustment.

Duration of treatment

The duration of treatment depends on the course of the disease. Patients should continue taking Medaxone for at least 48-72 hours after the temperature has returned to normal and tests show the absence of pathogens.

Combination therapy

Studies have shown that synergism exists between ceftriaxone and aminoglycosides for many Gram-negative bacteria. Although the increased effectiveness of such combinations cannot always be foreseen, it should be considered in the presence of severe, life-threatening infections caused by Pseudomonas aeroginosa. Due to the physical incompatibility of ceftriaxone and aminoglycosides, they should be administered separately at the recommended doses.

Dosing in special cases

Meningitis

For bacterial meningitis in children aged 15 days to 12 years, treatment begins with a dose of 100 mg / kg (but not more than 4 g) 1 time per day. Once the pathogen has been identified, its sensitive dose can be reduced accordingly. The best results were achieved with this duration of treatment:

Lyme borreliosis

Adults and children – 50 mg / kg (highest daily dose – 2 g) 1 time per day for 14 days.

Gonorrhea

For the treatment of gonorrhea (caused by penicillinase-producing or non-penicillinase-producing strains), a single dose of 250 mg intramuscularly is recommended.

Prevention of infections in surgery

For the prevention of postoperative infections in surgery, it is recommended, depending on the degree of infection risk, to administer a single dose of 1-2 g of Medaxone 30-90 minutes before the start of the operation. In operations on the colon and rectum, the simultaneous (but separate) administration of the drug and one of the 5-nitroimidazoles, such as ornidazole, has proven itself well.

Renal and hepatic insufficiency

In patients with impaired renal function, there is no need to reduce the dose if liver function remains normal. Only in case of renal insufficiency in the pre-terminal stage (creatinine clearance less than 10 ml / min), the daily dose should not exceed 2 g. .

Patients on hemodialysis do not need additional administration of the drug after dialysis. Serum concentrations of ceftriaxone should, however, be monitored for possible dose adjustments, as the elimination rate may decrease in such patients. The daily dose of Medaxone in patients on hemodialysis should not exceed 2 g.

Prepare solutions immediately before their use.

Freshly prepared solutions retain their physical and chemical stability for 6 hours at room temperature (or 24 hours at 2-8°C). Depending on the concentration and duration of storage, the color of the solutions may vary from pale yellow to amber. This property of the active substance does not affect the efficacy or tolerability of the drug.

Injection

For intramuscular injection dissolve 1 g in 3.5 ml of 1% lidocaine solution; injection to do deep into the gluteal muscle. It is recommended to enter no more than 1 g in one buttock. If a dose greater than 1 g is indicated, it should be divided and administered as several injections.

Solution containing lidocaine must not be administered intravenously.

Intravenous injection

For intravenous injection, dissolve 1 g in 10 ml of sterile water for injection; enter intravenously slowly (2-4 minutes).

Injection

Infusion must last at least 30 minutes. To prepare an infusion solution, dissolve 2 g of Medaxone in 40 ml of one of the following infusion solutions free of calcium ions: 0.9% sodium chloride, 0.45% sodium chloride + 2.5% glucose, 5% glucose, 10% glucose , 6% dextran in glucose solution 5%, 6-10% hydroxyethyl starch, water for injection. Due to possible incompatibilities, solutions containing ceftriaxone should not be mixed with solutions containing other antibiotics, both when preparing and when administered.

Do not use diluents containing calcium, such as Ringer’s solution or Hartmann’s solution, to dissolve the drug in vials or to dilute the reconstituted solution for intravenous administration due to the possibility of precipitation of ceftriaxone calcium salts. The occurrence of precipitation of calcium salts of ceftriaxone can also occur when Medaxone is mixed with solutions containing calcium in the same infusion system for intravenous administration. Medaxone must not be administered simultaneously with solutions containing calcium, including long-term infusions containing calcium, such as parenteral nutrition (see “Interaction with other medicinal products and other types of interactions”).

Adverse reactions

Infections: genital tract mycosis, secondary fungal infections and infections caused by resistant microorganisms.

From the blood and lymphatic system: eosinophilia, neutropenia, leukopenia, granulocytopenia, anemia, including hemolytic anemia, thrombocytopenia, increased prothrombin time, coagulation disorders. Very rarely, cases of agranulocytosis (<500/mm3) have been observed, predominantly after a total dose of 20 g or more. During long-term treatment, the blood picture should be regularly monitored. A slight prolongation of prothrombin time has been reported.

From the digestive tract: diarrhea, nausea, vomiting, stomatitis, glossitis; pancreatitis, possibly due to obstruction of the bile ducts. Most of these patients had risk factors for biliary congestion, such as a history of treatment, severe illness, and total parenteral nutrition, and a role for ceftriaxone-induced biliary tract precipitates in the development of pancreatitis cannot be ruled out; pseudomembranous enterocolitis has been reported.

From the digestive system: precipitates of ceftriaxone calcium salt in the gallbladder with corresponding symptoms in children, reverse cholelithiasis in children. The specified phenomena were seldom observed at children; often – an increase in the level of liver enzymes in the blood serum (AST, ALT, alkaline phosphatase).

From the side of the skin and subcutaneous tissue: skin rash, allergic dermatitis, itching, urticaria, edema, exanthema; exudative erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome).

From the urinary system: oliguria, hematuria, glucosuria; formation of kidney stones, mainly in children aged 3 years and older who received large daily doses of the drug (≥ 80 mg / kg per day), or cumulative doses of more than 10 g, and who had additional risk factors (restricted fluid intake, bed rest). The formation of calculi in the kidneys may be asymptomatic or manifest clinically, may cause renal failure, which disappears after discontinuation of treatment with ceftriaxone.

General disorders: headache and dizziness, fever, chills, anaphylactic or anaphylactoid reactions. In isolated cases, inflammatory reactions of the vein wall are observed. They can be avoided by applying a slow injection (2-4 minutes).

Local reactions: when administered intravenously – phlebitis, pain along the vein; with intramuscular injection – pain at the injection site. Injection without lidocaine is painful.

Interaction with calcium

Medaxone must not be given simultaneously or mixed with calcium-containing solutions, even when using separate infusion systems. Described a small number of deaths due to the formation of precipitates of calcium salts of ceftriaxone in the lungs and kidneys of newborns. In some cases, venous accesses and administration of ceftriaxone and calcium-containing solutions were different.

Laboratory findings

Rarely, patients treated with ceftriaxone may experience false positive Coombs results. Like other antibiotics, ceftriaxone can cause false positive galactosemia. False-positive results can also be obtained when determining glucose in the urine, therefore, during treatment with the drug, glucosuria, if necessary, should be determined only by the enzyme method.

Overdose

In case of overdose, the manifestations of adverse reactions may increase.

Hemodialysis or peritoneal dialysis will not reduce drug levels. There is no specific antidote. Treatment of overdose is symptomatic.

Use during pregnancy or lactation

Ceftriaxone crosses the placental barrier. The safety of ceftriaxone in women during pregnancy has not been studied.

In small concentrations, ceftriaxone passes into breast milk, therefore, when ceftriaxone is prescribed, breastfeeding should be stopped.

Children

The drug is used for children according to the dosage indicated in the section “Method of administration and doses”.

The drug is contraindicated in premature infants up to 41 weeks of gestation (gestational age + age after birth).

In full-term newborns (up to 28 days of life) with jaundice or hypoalbumineria, acidosis, the level of binding of bilirubin to blood proteins is reduced, the risk of bilirubin encephalopathy.

The drug is contraindicated in neonates ≤ 28 days of age for use when necessary (or expected to be needed) for treatment with intravenous solutions containing calcium, including intravenous infusions containing calcium, such as parenteral nutrition, due to the risk of precipitation of calcium salts of ceftriaxone (see . section “Method of administration and doses”).

In newborns and premature infants, cases of precipitates in the lungs and kidneys, resulting in death, have been described with the simultaneous administration of ceftriaxone and calcium preparations. In some of these cases, the same infusion systems were used for administration of ceftriaxone and solutions containing calcium, and precipitation was observed in some infusion systems for administration.

Application considerations

When prescribing ceftriaxone, official recommendations on antibiotic therapy and, in particular, recommendations on the prevention of antibiotic resistance should be followed.

As with other cephalosporins, fatal anaphylactic reactions have been reported with ceftriaxone, even if there is no relevant reference in the detailed history. If allergic reactions occur, Medaxon should be immediately canceled and appropriate treatment prescribed.

Ceftriaxone should be used with caution in patients with a tendency to allergic diathesis.

Ceftriaxone may increase prothrombin time. In this regard, if vitamin K deficiency is suspected, it is necessary to determine the prothrombin time.

With the use of almost all antibacterial drugs, including ceftriaxone, diarrhea associated with Clostridium difficile, from mild severity to fatal colitis, may occur. Antibacterial drugs alter the normal flora of the large intestine, leading to an overgrowth of Clostridium difficile. Clostridium difficile produces toxins A and B, which contribute to the development of diarrhea associated with Clostridium difficile. Excessive toxin-producing strains of Clostridium difficile cause increased morbidity and mortality because these infections may be resistant to antimicrobials and require colectomy. Clostridium difficile-associated diarrhea should be excluded in all patients during antibiotic use. A detailed medical history should be taken, as Clostridium difficile-associated diarrhea may occur up to 2 months after the end of antibiotic use.

If diarrhea associated with Clostridium difficile is suspected or confirmed, antibiotic therapy that does not affect Clostridium difficile should be discontinued. Appropriate amounts of fluids and electrolytes, protein supplements, antibiotic therapy to which Clostridium difficile is susceptible, and surgical examination should be given as clinically indicated.

During long-term use of ceftriaxone, it may be difficult to control non-susceptible organisms. In this regard, careful monitoring of patients is necessary. If superinfection occurs, appropriate measures must be taken.

After the use of ceftriaxone, usually at doses higher than the standard recommended doses, shadows that are mistaken for stones may be observed on ultrasound of the gallbladder. These are precipitates of the calcium salt of ceftriaxone, which disappear after completion or discontinuation of ceftriaxone therapy. Such changes are rarely accompanied by any symptoms. But even in such cases, only conservative treatment is recommended. If these phenomena are accompanied by clinical symptoms, then the decision to cancel the drug is made by the doctor.

Patients treated with ceftriaxone have experienced isolated cases of pancreatitis, possibly due to obstruction of the biliary tract. Most of these patients had risk factors for biliary congestion, such as a history of treatment, severe disease, and total parenteral nutrition. At the same time, the role of precipitates in the development of pancreatitis, formed under the action of ceftriaxone in the biliary tract, cannot be ruled out.

Ceftriaxone may displace bilirubin from its association with serum albumin. In this regard, the use of ceftriaxone in newborns with hyperbilirubinemia is contraindicated (see Section “Contraindications”).

Caution should be exercised when administering ceftriaxone to patients with renal insufficiency who are simultaneously receiving aminoglycosides and diuretics.

Ceftriaxone should not be mixed or administered simultaneously with calcium-containing solutions, even when the drugs are administered through different infusion lines. In newborns and premature babies, there are cases of precipitates in the lungs and kidneys that caused a fatal outcome with the simultaneous administration of ceftriaxone and calcium preparations. In this regard, calcium-containing solutions for intravenous administration should not be used in newborns and patients of other age groups for at least 48 hours after the last dose of ceftriaxone (see Section “Contraindications”).

Cases of intravascular precipitation following concomitant use of ceftriaxone with intravenous calcium-containing solutions have also been reported in patients of other age groups.

Immune-mediated hemolytic anemia has been observed in patients receiving cephalosporins, including ceftriaxone. Cases of severe hemolytic anemia, including fatal cases, have been reported in adult and pediatric patients. With the development of anemia with the use of ceftriaxone, it is necessary to exclude anemia caused by ceftriaxone and stop the drug until the etiology of anemia is established.

During long-term treatment, the blood picture should be monitored regularly.

In rare cases, patients treated with ceftriaxone may experience false-positive Coombs test results. Like other antibiotics, ceftriaxone can cause false positive galactosemia. False positive results can also be obtained when determining glucose in the urine, therefore, during treatment with ceftriaxone, glucosuria, if necessary, should be determined only by the enzyme method.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms

There is no data on the effect of ceftriaxone on the reaction rate, but due to the possibility of dizziness, the drug may affect the ability to drive vehicles or work with complex mechanisms.

Interaction with other medicinal products and other types of interactions

Under no circumstances should the drug be used with calcium-containing solutions (Ringer’s solution).

Calcium-containing solutions should not be administered within 48 hours of the last administration of ceftriaxone.

In neonates and premature infants, cases of precipitates in the lungs and kidneys, resulting in death, have been described with the simultaneous administration of ceftriaxone and calcium preparations.

Co-administration of high doses of ceftriaxone and potent diuretics such as furosemide has not shown renal dysfunction. There is no indication that ceftriaxone increases the nephrotoxicity of aminoglycosides. After taking alcohol immediately after taking ceftriaxone, no effects similar to those of disulfiram (teturam) were observed.

Ceftriaxone does not contain an N-methylthiotetrazole group that could cause ethanol intolerance and the bleeding associated with some other cephalosporins. Probenecid does not affect the excretion of ceftriaxone.

Antagonism between ceftriaxone and chloramphenicol has been found in vitro.

Calcium-containing diluents, such as Ringer’s solution or Hartmann’s solution, should not be used to dissolve ceftriaxone in vials or to dilute the reconstituted solution for intravenous administration due to the possibility of precipitation of ceftriaxone calcium salts. Precipitation of ceftriaxone calcium salts can also occur when ceftriaxone is mixed with solutions containing calcium in the same intravenous infusion set. Ceftriaxone should not be co-administered with solutions containing calcium, including long-term infusions containing calcium, such as parenteral nutrition. In vitro studies have shown that infants have an increased risk of precipitated calcium salts of ceftriaxone.

Ceftriaxone has been reported to be incompatible with amzacrine, vancomycin, fluconazole and aminoglycosides.

Bacteriostatic agents may interfere with the bactericidal action of cephalosporins.

Ceftriaxone may reduce the effectiveness of hormonal oral contraceptives. In this regard, it is recommended to use additional (non-hormonal) methods of contraception during treatment and for 1 month after its completion.

There are no reports of interactions between ceftriaxone and oral products containing calcium, and interactions between ceftriaxone by intramuscular injection and products containing calcium (intravenous or oral), because this information is indicated in the instructions for medical use.

Pharmacological properties

Pharmacodynamics.

Ceftriaxone is a long-acting parenteral cephalosporin antibiotic of the third generation.

The bactericidal activity of ceftriaxone is due to the inhibition of cell wall synthesis. Ceftriaxone is active in vitro against most Gram-negative and Gram-positive microorganisms. Ceftriaxone is characterized by very high resistance to most b-lactamases (both penicillinases and cephalosporinases) of gram-positive and gram-negative bacteria. Ceftriaxone is active against these microorganisms in vitro and in clinical infections:

Gramprene aerobes:

Staphylococcus aureus (including penicillinase form), coagulazoid staphylococci, Streptococcus pyogenes (β-hemolytic, group A), Streptococcus AGALACEE (β-g. Litical, group B), Streptococcus Viridans, Streptococcus Pneumoniae.

Methicillin-resistant Staphylococcus spp., as well as most strains of Enterococcus (eg Enterococcus faecalis, Enterococcus faecium and Listeria monocytogenes) show resistance to cephalosporins, including ceftriaxone;

Gram-negative aerobes:

Acinetobacter lwoffi, Acinetobacter anitratus (mainly A. baumanii)*, Aeromonas spp., Alcaligenes faecalis, Alcaligenes spp., Alkagenous bacteria, Borrelia burgdorferi, Capnocytophaga spp. , Citrobacter diversus (including C. amalonaticus), Citrobacter spp. *, Escherichia coli, Enterobacter aerogenes *, Enterobacter cloacae *, Enterobacter spp (others) *, Haemophilus ducreyi, Haemophilus influenzae, Haemophilus parainfluenzae, Hafnia alvei, Klebsiella oxytoca, Klebsiella pneumoniae **, Moraxella catarrhalis (formerly Branhamella catarrhalis), Mor axella osloensis, Moraxella spp. (Others), Morganella morganii, Neisseria gonorrhoea, Neisseria meningitidis, Pasteurella multocida, Plesiomonas shigelloides, Proteus mirabilis, Proteus penneri *, Proteus vulgaris *, Pseudomonas fluorescens *, Pseudomonas spp. (Others) *, Providentia rettgeri * Providentia spp. (Others), Salmonella typhi, Salmonella spp. (Nontyphoids), Serratia marcescens *, Serratia spp. (Others) *, Shigella spp., Vibrio spp., Yersinia enterocolitica, Yersinia spp. (Other).

* Some isolates of these species are resistant to ceftriaxone mainly due to the formation of

chromosomally encoded β-lactamases;

** Some isolates of these species are resistant to ceftriaxone due to the production of a number of plasmid-mediated β-lactamases.

Many of the strains of the above microorganisms, which have multiple resistance to antibiotics such as aminopenicillins and ureidopenicillins, first and second generation cephalosporins, aminoglycosides, are sensitive to ceftriaxone.

Treponema pallidum is sensitive to ceftriaxone in vitro. Clinical studies show that ceftriaxone is effective for the treatment of primary and secondary syphilis, except for clinical strains of P. aeruginosa that are resistant to ceftriaxone;

anaerobes:

Bacteroides spp. (Bile sensitive) *, Clostridium spp. (Except C. difficile), Fusobacterium nucleatum, Fusobacterium spp. (Others), Gaffkia anaerobica (formerly Peptococcus), Peptostreptococcus spp.

* Some isolates of these species are resistant to ceftriaxone due to the formation of β-lactamases.

Many of the b-lactamase producing strains of Bacteroides spp. (particularly B. fragilis) are resistant to ceftriaxone. Resistant Clostridium difficile.

Pharmacokinetics.

The pharmacokinetics of ceftriaxone is non-linear. All major pharmacokinetic parameters based on total drug concentrations, with the exception of the half-life, are dose dependent.

Absorption

The maximum plasma concentration after a single injection of 1 g of the drug is 81 mg / l and is reached 2-3 hours after administration. The area under the plasma concentration curve after intravenous administration is equal to that after administration. This means that the bioavailability of ceftriaxone after intramuscular administration is 100%.

Distribution

The volume of distribution of ceftriaxone is 7-12 liters. After administration at a dose of 1-2 g, ceftriaxone penetrates well into tissues and body fluids. For more than 24 hours, its concentrations far exceed the minimum inhibitory concentrations for most infectious agents in more than 60 tissues and fluids (including the lungs, heart, biliary tract, liver, tonsils, middle ear and nasal mucosa, bones, and spinal cord, pleural and synovial fluids, in the secretion of the prostate).

After administration, ceftriaxone rapidly penetrates into the cerebrospinal fluid, where bactericidal concentrations against susceptible microorganisms persist for 24 hours.

Protein binding

Ceftriaxone binds reversibly to albumin, and the degree of binding decreases with increasing concentration, for example, it decreases from 95% at a plasma concentration of less than 100 mg / l to 85% at a concentration of 300 mg / l. Due to the low concentration of albumin in tissue fluid, the proportion of free ceftriaxone in it is higher than in blood plasma.

Penetration into certain tissues

Ceftriaxone penetrates through inflamed meninges in children, incl. newborns. 24 hours after the administration of ceftriaxone at a dose of 50-100 mg/kg body weight (newborns and infants, respectively), ceftriaxone concentrations in the cerebrospinal fluid exceed 1.4 mg/l. The maximum concentration in the cerebrospinal fluid is reached approximately 4 hours after administration and averages 18 mg/l. With bacterial meningitis, the average concentration of ceftriaxone in the cerebrospinal fluid is 17% of the concentration in blood plasma, with aseptic meningitis – 4%. In adult patients with meningitis, after a dose of 50 mg / kg body weight, ceftriaxone concentrations in the cerebrospinal fluid are achieved after 2-24 hours, which are many times higher than the minimum inhibitory concentrations for the most common pathogens of meningitis.