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4 mg muscle relaxer. Tizanidine: Complete Dosage Guide, Max Dose, and Adjustments for Muscle Relaxation

What is the recommended dosage for tizanidine. How should the dose be adjusted for renal impairment. What is the maximum daily dose of tizanidine. How does food affect tizanidine absorption. What precautions should be taken when using tizanidine.

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Understanding Tizanidine: A Powerful Muscle Relaxant

Tizanidine, commonly known by its brand name Zanaflex, is a short-acting muscle relaxant used to manage spasticity associated with conditions like multiple sclerosis and spinal cord injuries. It works by blocking nerve impulses that send pain sensations to the brain, thereby temporarily relaxing muscles and reducing muscle spasms.

How Does Tizanidine Work?

Tizanidine acts as a central alpha-2 adrenergic agonist, which means it stimulates certain receptors in the central nervous system. This action results in a reduction of muscle tone and spasticity, providing relief for patients suffering from various neuromuscular disorders.

Tizanidine Dosage Guidelines for Adults

The appropriate dosage of tizanidine can vary depending on individual patient factors and the severity of muscle spasms. Here are the general guidelines for adult dosing:

  • Initial dose: 2 mg orally every 6 to 8 hours as needed
  • Peak effects occur in approximately 1 to 2 hours
  • Effects last for 3 to 6 hours
  • Treatment can be repeated up to a maximum of 3 doses in 24 hours
  • Dose can be gradually increased by 2 to 4 mg at intervals of 1 to 4 days

Maximum Dosage Limits

To ensure patient safety, there are strict limits on the maximum dosage of tizanidine:

  • Maximum single dose: 16 mg
  • Maximum daily dose: 36 mg in 24 hours

Dosage Adjustments for Special Populations

Certain patient groups may require dosage adjustments to ensure safe and effective use of tizanidine.

Renal Impairment Dosing

For patients with severe renal impairment (creatinine clearance less than 25 mL/min):

  • Individualize therapy with lower doses during dose titration
  • If higher doses are required, increase individual doses rather than dosing frequency
  • Closely monitor for toxicity

Liver Impairment Considerations

Tizanidine is not recommended for patients with liver impairment. The drug is primarily metabolized in the liver, and impaired hepatic function can lead to increased drug concentrations and potential toxicity.

The Impact of Food on Tizanidine Absorption

The absorption of tizanidine can be significantly affected by food intake. Clinically significant differences in absorption are expected between capsules and tablets when taken with or without food. These differences could result in changes in efficacy and tolerability.

Consistent Administration Regimen

Once a decision is made regarding formulation (capsule or tablet) and whether to take it with or without food, this regimen should not be altered. Consistency in administration helps maintain predictable drug levels and effects.

Precautions and Monitoring During Tizanidine Therapy

To ensure safe and effective use of tizanidine, several precautions and monitoring strategies should be implemented:

  • Obtain baseline aminotransferase levels and monitor at 1 month after reaching maximum dose
  • Consider obtaining baseline renal function in elderly patients
  • Monitor for hypotension, especially in at-risk patients and those on antihypertensive therapy
  • Watch for sedation in patients receiving concomitant CNS depressant agents

Special Considerations for Elderly Patients

Tizanidine should be used with caution in elderly patients, especially those with renal impairment. Lower initial doses and slower titration may be necessary to minimize adverse effects.

Discontinuation and Withdrawal of Tizanidine

Abrupt discontinuation of tizanidine, especially after prolonged use, can lead to withdrawal symptoms and rebound effects. To minimize these risks, a gradual dose reduction is recommended:

  • Decrease dose by 2 to 4 mg per day
  • This is particularly important for patients who have been receiving doses of 20 to 36 mg per day for periods of 9 weeks or more

Potential Withdrawal Symptoms

Patients should be monitored for signs of withdrawal, which may include:

  • Rebound hypertension
  • Tachycardia
  • Hypertonia (increased muscle tone)

Patient Education and Counseling Points

Proper patient education is crucial for the safe and effective use of tizanidine. Healthcare providers should discuss the following points with patients:

  • Consistency in taking the medication with or without food
  • The importance of not altering the dosing regimen without consulting a healthcare provider
  • Potential interactions with other medications
  • The need to avoid abrupt discontinuation of the drug
  • Awareness of potential hypotension and the need for caution when changing positions
  • The sedative effects of tizanidine, especially when combined with other CNS depressants or alcohol

Reporting Side Effects

Patients should be encouraged to report any unusual or severe side effects to their healthcare provider promptly. This can help in early detection and management of potential complications.

Tizanidine Interactions and Contraindications

Tizanidine can interact with various medications, potentially leading to increased side effects or reduced efficacy. Some notable interactions include:

  • CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin) – can significantly increase tizanidine blood levels
  • Alpha-2 adrenergic agonists (e.g., clonidine) – may enhance hypotensive effects
  • CNS depressants (e.g., alcohol, benzodiazepines) – can increase sedation

Contraindications

Tizanidine is contraindicated in patients with:

  • Known hypersensitivity to tizanidine or its components
  • Concomitant use of fluvoxamine or other potent CYP1A2 inhibitors
  • Severe hepatic impairment

Healthcare providers should carefully review a patient’s medication list and medical history before prescribing tizanidine to avoid potential drug interactions and contraindications.

Monitoring Efficacy and Adjusting Treatment

The effectiveness of tizanidine treatment should be regularly assessed to ensure optimal patient outcomes. Factors to consider include:

  • Reduction in muscle tone and spasticity
  • Improvement in activities of daily living
  • Patient-reported pain and discomfort levels
  • Occurrence and severity of side effects

Treatment Adjustments

Based on the patient’s response and tolerability, the tizanidine regimen may need to be adjusted. This could involve:

  • Dose titration (increasing or decreasing the dose)
  • Changing the dosing frequency
  • Exploring combination therapy with other muscle relaxants or pain medications
  • Considering alternative treatments if tizanidine is ineffective or poorly tolerated

Regular follow-up appointments and open communication between the patient and healthcare provider are essential for optimizing tizanidine therapy and managing any potential issues that may arise during treatment.

Tizanidine Dosage Guide + Max Dose, Adjustments

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Medically reviewed by Drugs.com. Last updated on Feb 27, 2023.

Applies to the following strengths: 4 mg; 2 mg; 6 mg

Usual Adult Dose for:

  • Muscle Spasm
Additional dosage information:
  • Renal Dose Adjustments
  • Liver Dose Adjustments
  • Dose Adjustments
  • Precautions
  • Dialysis
  • Other Comments

Usual Adult Dose for Muscle Spasm

Initial dose: 2 mg orally every 6 to 8 hours as needed

  • Peak effects occur in approximately 1 to 2 hours and last for 3 to 6 hours; treatment can be repeated as needed to a maximum of 3 doses in 24 hours; gradually increase dose by 2 to 4 mg at intervals of 1 to 4 days until satisfactory reduction of muscle tone is achieved.

Maximum single dose: 16 mg
Maximum daily dose: 36 mg in 24 hours

Comments:

  • Clinically significant differences in absorption are expected between capsules and tablets when taken with or without food; these differences could result in changes in efficacy and tolerability.
  • Once a formulation is decided on and a decision is made to take with or without food, this regimen should not be altered.

Use: Management of spasticity.

Renal Dose Adjustments

Severe renal impairment (CrCl less than 25 mL/min): Individualize therapy with lower doses during dose titration; if higher doses are required, individual doses should be increased rather increasing the dosing frequency; closely monitor for toxicity

Liver Dose Adjustments

Not recommended

Dose Adjustments

Use with caution in elderly patients, especially those with renal impairment.

Drug withdrawal:

  • Decrease by 2 to 4 mg per day, especially in patients who have been receiving doses of 20 to 36 mg per day for periods of 9 weeks or more.

Precautions

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

Dialysis

Data not available

Other Comments

Administration advice:

  • May take orally with or without food; however, once a formulation is decided on and a decision is made to take with or without food, this regimen should not be altered.

General:

  • Because this drug has a relatively short duration of effect, dosing should occur at times when relief of spasticity is most important, such as before activities of daily living.
  • Considerable variation in response has been observed and therefore careful titration is necessary in order to not exceed the dose producing the desired effect.
  • Gradual dose reduction is advised on discontinuation so as to minimize risk of withdrawal and rebound hypertension, tachycardia, and hypertonia.

Monitoring:

  • Obtain aminotransferase levels at baseline, 1 month after maximum dose is achieved, and as clinically indicated (e.g. if hepatic injury is suspected).
  • Consider obtaining baseline renal function in elderly patients.
  • Monitor for hypotension in at-risk patients and those receiving concomitant antihypertensive therapy.
  • Monitor for sedation in patients receiving concomitant CNS depressant agents.

Patient advice:

  • Patients may take this drug with or without food, but once the decision is made to take with or without food it should be taken this way consistently.
  • Patients should check with their healthcare provider before starting or stopping any medications as this drug is known to interact with other medications.
  • Patients should be advised not to abruptly stop taking this medication without first talking with their healthcare provider.
  • Patients should be advised that this drug may cause hypotension and they should be careful when changing positions form lying to standing.
  • Patients should be advised this drug may cause significant somnolence, especially if taken with other CNS depressants or alcohol; they should refrain from activities requiring mental alertness until the effects of the drug are known.

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Zanaflex

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Medical Disclaimer

Zanaflex: Uses, Dosage & Side Effects

Generic name: tizanidine [ tye-ZAN-i-deen ]
Drug class: Skeletal muscle relaxants

Medically reviewed by Kaci Durbin, MD. Last updated on Mar 29, 2023.

What is Zanaflex?

Zanaflex is a short-acting muscle relaxer. It works by blocking nerve impulses (pain sensations) that are sent to your brain.

Zanaflex is used to treat spasticity associated with diseases like multiple sclerosis and spinal cord injuries by temporarily relaxing muscle tone.

Zanaflex may also be used for purposes not listed in this medication guide.

Warnings

Zanaflex is a short-acting medication that should be taken only for daily activities that require relief from muscle spasticity.

You should not take tizanidine if you are also taking fluvoxamine (Luvox) or ciprofloxacin (Cipro).

Do not use Zanaflex at a time when you need muscle tone for safe balance and movement during certain activities. In some situations, it may endanger your physical safety to be in a state of reduced muscle tone.

Switching between Zanaflex tablets and capsules, or changing the way you take it with regard to eating, can cause an increase in side effects or a decrease in therapeutic effect. Follow your doctor’s instructions carefully. After making any changes in how you take Zanaflex, contact your doctor if you notice any change in how well the medicine works or if it causes increased side effects.

Do not take more than three doses (36 mg) of tizanidine in a 24-hour period. Too much of tizanidine can damage your liver. Cold or allergy medicine, narcotic pain medicine, sleeping pills, other muscle relaxers, and medicine for seizures, depression or anxiety can add to sleepiness caused by tizanidine. Tell your doctor if you need to use any of these other medicines together with Zanaflex.

Avoid drinking alcohol. It can increase some of the side effects of tizanidine.

Before taking this medicine

You should not use Zanaflex if you are allergic to tizanidine, or if:

To make sure Zanaflex is safe for you, tell your doctor if you have ever had:

It is not known whether Zanaflex will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.

It may not be safe to breastfeed while using tizanidine. Ask your doctor about any risk.

How should I take Zanaflex?

Take Zanaflex exactly as it was prescribed for you. Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not use this medicine in larger or smaller amounts or for longer than recommended.

Zanaflex is usually taken up to 3 times in one day. Allow 6 to 8 hours to pass between doses. Do not take more than three doses (36 mg) in a 24-hour period. Too much of this medicine can damage your liver.

You may take Zanaflex with or without food, but take it the same way each time. Switching between taking tizanidine with food and taking it without food can make the medicine less effective or cause increased side effects.

Switching between Zanaflex tablets and capsules may cause changes in side effects or how well the medicine works.

If you make any changes in how you take Zanaflex, tell your doctor if you notice any change in side effects or in how well the medicine works.

Zanaflex is a short-acting medication, and its effects will be most noticeable between 1 and 3 hours after you take it. You should take this medicine only for daily activities that require relief from muscle spasms.

You will need frequent blood tests to check your liver function.

If you stop using Zanaflex suddenly after long-term use, you may have withdrawal symptoms such as dizziness, fast heartbeats, tremors, and anxiety. Ask your doctor how to safely stop using this medicine.

Store at room temperature away from moisture and heat.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include weakness, drowsiness, confusion, slow heart rate, shallow breathing, feeling light-headed, or fainting.

What to avoid

Do not use Zanaflex at a time when you need muscle tone for safe balance and movement during certain activities. In some situations, it may be dangerous for you to have reduced muscle tone.

Drinking alcohol with this medicine can cause side effects.

Avoid driving or hazardous activity until you know how Zanaflex will affect you. Your reactions could be impaired. Avoid getting up too fast from a sitting or lying position, or you may feel dizzy.

Zanaflex side effects

Get emergency medical help if you have signs of an allergic reaction to Zanaflex: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

  • a light-headed feeling, like you might pass out;

  • weak or shallow breathing;

  • confusion, hallucinations; or

  • yellowing of the eyes or skin.

  • pain or burning when you urinate.

Common Zanaflex side effects may include:

  • drowsiness, dizziness, weakness;

  • dry mouth;

  • feeling nervous;

  • blurred vision;

  • flu-like symptoms;

  • abnormal liver function tests;

  • runny nose, sore throat;

  • urination problems, painful urination;

  • vomiting, constipation; or

  • uncontrolled muscle movements.

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

Dosing information

Usual Adult Dose for Muscle Spasm:

-Initial dose: 2 mg orally every 6 to 8 hours as needed
-The dose of Zanaflex can be increased by your doctor if needed
-The medication effects peak in about 1 to 2 hours and last for 3 to 6 hours
-Do not take more than 16mg of Zanaflex at one time. Do not take more than 36mg in 24 hours.

Comments:
-The capsules and tablets are absorbed differently by the body. Do not switch from one to the other without talking to your doctor.
-Zanaflex should be taken with food every time or without food every time. Do not switch back and forth.

What other drugs will affect Zanaflex?

Taking Zanaflex with other drugs that make you sleepy or slow your breathing can cause dangerous side effects or death. Ask your doctor before using opioid medication, a sleeping pill, a muscle relaxer, or medicine for anxiety or seizures.

Tell your doctor about all your other medicines, especially:

  • acyclovir;

  • ticlopidine;

  • zileuton;

  • birth control pills;

  • an antibiotic, including ciprofloxacin, levofloxacin, moxifloxacin, ofloxacin, or others;

  • blood pressure medicine such as clonidine, guanfacine, methyldopa;

  • heart rhythm medicine including amiodarone, mexiletine, propafenone, verapamil; or

  • stomach acid medicine such as cimetidine, famotidine.

This list is not complete. Other drugs may interact with tizanidine, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

Popular FAQ

The maximum effect of tizanidine occurs about 1 hour to 2 hours after taking a dose. It wears off in about 3 to 6 hours after taking it. Tizanidine is typically given no more than 3 times a day.

Tizanidine is not listed as a controlled substance by the U.S. Drug Enforcement Administration (DEA). Abuse potential has not been evaluated in human studies.

Tizanidine can cause sleepiness, but it has not been approved by the U.S. Food and Drug Administration (FDA) to treat sleep disorders. Tizanidine is a skeletal muscle relaxant. It is approved by the FDA to help relieve muscle spasms.

Tizanidine is known to cause low blood pressure. In some cases, it may cause low blood pressure that is so low that you could faint or pass out. The chances of fainting can be lowered if your doctor raises the dose of tizanidine very slowly. You may also have to be careful when you move from a sitting position to a standing position. In clinical trials, the most common side effects of tizanidine were dry mouth, sleepiness, dizziness and asthenia (defined as weakness, fatigue and/or tiredness).

Tizanidine normally starts working 1 to 2 hours after taking it. It wears off about 3 hours to 6 hours after taking it. Tizanidine can be taken up to 3 times a day to help relieve muscle spasms.

Tizanidine may be addictive, but it has not been evaluated in human studies. Withdrawal symptoms have been reported after abruptly stopping tizanidine, but abuse of other medications concomitantly was suspected in these cases. Dosing should be tapered off to avoid possible withdrawal symptoms.

Tizanidine is not known to cause weight gain. In clinical trials, the most common side effects of tizanidine were dry mouth, sleepiness, dizziness and asthenia (defined as weakness, fatigue and/or tiredness).

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

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

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Copyright 1996-2023 Cerner Multum, Inc. Version: 4.01.

Modern Muscle Relaxants in Anesthesiology. Classification. Clinical application. Side effects. Muscle relaxant antagonists.

Muscle relaxants ( muscle relaxants ) is a group of drugs used in anesthesiology and resuscitation to provide myoplegia. The point of application of the action of muscle relaxants is the synaptic region, in which neuromuscular transmission takes place. Modern muscle relaxants include: nimbex, esmeron, trakrium, mivacron, arduan and listenone. Below you will find the classification of muscle relaxants, clinical use and side effects, as well as muscle relaxant antagonists. The history of the use of muscle relaxants in world practice is here.
Classification of drugs used in anesthesiology (inhalation and intravenous anesthetics, benzodiazepines, vasopressors and cardiotonic drugs) here.

The modern classification of muscle relaxants is based on the mechanism of action and the duration of the clinical effect. Miorel long acting axants (more than 50 min) : arduan

  1. Intermediate-acting muscle relaxants (20-50 min) : esmeron, nimbex, trakrium
  1. Short acting muscle relaxants (15-20 min): mivacron
  1. Ultra short acting muscle relaxants (less than 10 minutes) : listenone

Classification of muscle relaxants according to the mechanism of action (a variant of interruption of the reflex arc in the neuromuscular synapse):

  1. Depolarizing muscle relaxants (prolong the depolarization phase from a few milliseconds to 5-6 minutes or more): listenone
  2. Non-depolarizing muscle relaxants (prevent depolarization phase): Nimbex, Esmeron, Trakrium, Mivacron, Arduan

Clinical use of muscle relaxants in anesthesiology

Clinical use of muscle relaxants largely depends on the skill of the anesthetist. Currently, in general surgery, muscle relaxants of medium and short duration of action are preferred, due to their high controllability and predictability of the clinical effect. Clinical use of arduan (long-acting muscle relaxant) every year decreases .

For tracheal intubation in the Mallampati I, II, III test, all of the above muscle relaxants are used in a planned clinical situation. However, if technically difficult tracheal intubation is predicted (Mallampati IV test), it is preferable to use an ultrashort-acting muscle relaxant (listenone). The combination of esmeron and its selective antagonist brydan can replace listenone.

Nimbex

Nimbex 6 muscle relaxant medium duration action. After an initial dose 0.1–0.15 mg/kg myoplegia occurs within 2–5 minutes tracheal intubation can be performed within 2–3 minutes . The duration of the clinical effect is maintained 45–55 min . To maintain myoplegia, fractional administration of Nimbex 0.02–0.05 mg/kg or infusion 1–2 mcg/kg/min are recommended. Repeated bolus doses of Nimbex provide clinically effective myoplegia within 20-30 minutes.
It is important to note that the main part of the nimbex (about 80%) undergoes spontaneous biodegradation by a non-enzymatic self-destruction mechanism ( Hofmann elimination ), and 20% of the unchanged muscle relaxant is excreted in the urine.

Administration of Nimbex in the range of recommended doses is characterized by no effect on the circulatory system and release of histamine, which allows its use in patients with high anesthetic risk.

Esmeron

Esmeron non-depolarizing muscle relaxant medium duration . After the introduction of a standard induction dose 0.6 mg/kg comfortable conditions for tracheal intubation occur after 1 minute, the duration of action is 30-40 minutes . In outpatient operations of short duration in doses of 0.3–0.45 mg/kg rocuronium bromide provides the onset of myoplegia within 2 minutes, and the clinical duration is on average 14 and 20 minutes , respectively. Increasing the induction dose to 0.9–1 mg/kg allows 45–60 s 0006 . The use of this methodological technique is advisable only in cases where the expected duration of surgery is exceeds 40 minutes . After prescribing the initial dose of esmeron, further maintenance of myoplegia is possible by discrete administration of the drug at a dose of 0.15-0.3 mg/kg every 15-20 minutes, depending on the type, duration of anesthesia and surgery. Infusion tactics the use of esmeron at a rate of 5–12 µg/kg/min is justified in long-term surgical interventions.

Esmeron has the fastest time of onset of any non-depolarizing muscle relaxant currently available. The maximum effect of a dose of 0.25-0.5 mg / kg in the muscles of the larynx develops after 1.5 minutes.

Trakrium

Trakrium depolarizing muscle relaxant intermediate duration . For tracheal intubation the recommended dose is 0.5-0.6 mg/kg . Myoplegia occurs after 2-2. 5 minutes , while the duration of the clinical effect does not exceed 30-35 min . Further maintenance of myoplegia is possible with the help of divided injections of the drug at a dose of 0.1–0.2 mg/kg every 15–30 min or as an infusion at a rate of 5–9 mcg/kg/min . The duration of recovery does not depend on the duration of infusion or the frequency of administration of Trakrium . The depth and duration of myoplegia may increase with respiratory and metabolic acidosis, hypothermia. The opposite effect is observed in respiratory and metabolic alkalosis. The pharmacokinetic profile of Trakrium is almost does not change in violation of liver and kidney function , so there is no need to adjust the dose of the drug in this category of patients. Trakrium practically has no direct effect on the cardiovascular system . Changes in hemodynamic parameters when using this muscle relaxant are due to its histaminogenic properties. In addition, the histamine-liberating effect of Trakrium can cause bronchospasm .

It is very important that the elimination of trakrium is carried out in two ways: 45% spontaneous Hofmann biodegradation , part of the drug is metabolized by lung esterases. Renal excretion in patients without hepatorenal pathology can reach 40%.

mivacron

mivacron 06 short acting muscle relaxant . The recommended doses of for tracheal intubation in adult patients are 0.15–0.25 mg/kg . The clinical effect develops within 2-3 minutes and lasts 15-20 minutes. Maintenance of myoplegia during anesthesia is carried out in fractional doses 0. 05–0.1 mg/kg every 15 minutes or by infusion at a dose of 90 004 3–15 µg/kg/min . The time to achieve the maximum effect depends on the dose and age of the patient and is: in adults, 2-5 minutes with the introduction of 0.1-0.25 mg / kg, and in patients with hepatic and renal insufficiency 2-2.5 minutes after administration of 0.15 mg/kg, in patients over 68 years old – 5 minutes after administration of 0.1 mg/kg. The clinical duration of action of mivacron is 2 times less than that of trakrium. The recovery time of neuromuscular conduction is two times less than that of any medium-acting muscle relaxant (Nimbex, Esmeron, Trakrium), does not depend on the dose or duration of intravenous infusion. Repeated administration of maintenance doses does not lead to the development of tachyphylaxis. Side effects of mivacron such as hypotension, tachycardia, erythema, urticaria and bronchospasm are due to its histaminogenic properties.

Arduan

Arduan .

After an initial dose of arduan 0.07-0.1 mg/kg tracheal intubation can be performed in 3-4 minutes. For further maintain muscle relaxation it is recommended to use doses of 25-30% of the initial dose (0.01-0.015 mg/kg), which allows to continue the action of arduan up to 30-40 minutes .
At present, arduan is used less and less in anesthesiology practice due to the complex predictability of the clinical effect and, as a result, the frequent need for decurarization at the stage of the patient’s awakening.

Listenone

Listenone (suxamethonium chloride; lysthenon; suxamethonium chloride) – depolarizing ultrashort-acting muscle relaxant After injection listenone at a dose of 1–1. 5 mg/kg comfortable conditions for tracheal intubation are created within 1 minute and continue 9000 4 4–6 min .

Listenone is rarely used in elective anesthesiology

5

, given the large number of side effects , such as hyperkalemia, hypersalivation, increased intragastric pressure, anaphylactic reactions, postoperative myalgia, malignant hyperthermia, etc. However, listenone remains indispensable emergency anesthesiology and resuscitation.

Side effects of muscle relaxants

Muscle relaxants play a prominent role in the frequency of adverse reactions during general anesthesia. The UK Medicines Safety Committee reported that 10% drug adverse reactions and 7% of deaths are due to muscle relaxants . The frequency of anaphylactic and anaphylactoid reactions developing during anesthesia is estimated from 1:1000 to 1:25000 anesthesia, with mortality 5% . Based on a retrospective study in France in the 2000s it was concluded that the most common causes of anaphylaxis are muscle relaxants (58%) 9000 5 , latex (16%) and antibiotics (15%).
Recently, there has been much interest in the possibility of using sugammadex in addition to the standards for the treatment of anaphylaxis caused by Esmeron. This was prompted by the hypothesis that cyclohectrin-sugammadex encapsulates rocuronium and therefore interferes with the interaction of rocuronium allergen groups with IgE, mast cells, and basophils. Molecular models and experiments in vivo , however, did not confirm this theory. Sagammadex itself exhibits anaphylaxis and is not currently recommended in the treatment of anaphylaxis due to rocuronium .

Muscle relaxant antagonists in anesthesiology

Muscle relaxant antagonists prozerin and Bridan, who are differ from each other by the mechanism of action.
P roserin cholinesterase inhibitor (anticholinesterase drug) ah and restoration of neuromuscular conduction.
Bridan is a modified gamma-cyclodestrin that selectively binds to aminosteroid muscle relaxant molecules, forming a stable inactive sugammadex + muscle relaxant complex. As a result, the concentration of the muscle relaxant in the blood decreases, and then in the neuromuscular synapse, and there is a rapid restoration of neuromuscular conduction. Unlike anticholinesterase drugs, sugammadex does not affect cholinergic activity.

The use of muscle relaxant antagonists in anesthesiology is limited by strict clinical indications.

To restore muscle tone after the use of depolarizing muscle relaxants anticholinesterase drugs are contraindicated because these drugs inhibit the activity of pseudocholinesterase, the main enzyme responsible for the hydrolysis of suxamethonium.

When performing decurarization after the appointment of non-depolarizing muscle relaxants , it should be remembered that only timely administration of anticholinesterase drugs allows to achieve rapid recovery of spontaneous respiration and muscle tone and minimize the likelihood of recurarization.

Proserin

Proserin ( Proserinum; neostigmine methylsulfate; neostigmine methylsulfate ) – cholinesterase inhibitor . Used in anesthesiology for decurarization after the use of non-depolarizing muscle relaxants.
The usual dose of proserin is 0.03–0.07 mg/kg depending on the severity of residual myoplegia. Excretion of proserin is carried out mainly by the kidneys in unchanged form, a small part is metabolized in the liver. Half-life is 30-45 minutes . Prozerin is contraindicated for use after the appointment of depolarizing muscle relaxants. In case of residual myoplegia after the use of drugs with a depolarizing mechanism of action , it is necessary to continue sedation and mechanical ventilation until the patient’s muscle tone and spontaneous breathing are fully restored.

Bridane

Bridane ( Bridion; sugammadex; sugammadex ) – selective esmeron antagonist . If it is necessary to urgently restore neuromuscular conduction against the background of total myoplegia, sugammadex is prescribed at a dose of 16 mg/kg . This results in a complete regression of block within 1.5 minutes . In situations where recurarization occurs, following the administration of sugammadex at doses of 2 or 4 mg/kg the repeated recommended dose of this drug is 4 mg/kg.

The combination of Esmeron and Bridan can replace Listenone for rapid sequential induction of anesthesia and completely eliminate residual muscle relaxation in the awakening ward. Sugammadex is the first drug that selectively binds a muscle relaxant (su from the word sugar (sugar) and gammadex – from the structure of the gammacyclodextrin molecule (gamma-cyclodextrin).

Sufficiently high cost of sugamadex somewhat limits its wide application in domestic anesthesiology.

Source

  1. Likhvantsev V.V. A practical guide to anesthesiology. M.: OOO “Medical Information Agency”, 2011.
  2. Miller R. Anesthesia by Ronald Miller. Publishing house “Chelovek”, 2015.
  3. Mertes PM, Laxenaire MC, Alla F: Anaphylactic and anaphylactoid reactions occurring during anesthesia in France in 1999-2000. Anesthesiology 99:536-545, 2003.
  4. Jones P, Turkstra T. Mitigation of rocuronium-induced anaphylaxis by sugammadex: the great unknown. Anaesthesia 2010; 65:89–90.
  5. Clarke RC, Sadleir PH, Platt PR. The role of sugammadex in the development and modification of an allergic response to rocuronium: evidence from a cutaneous model. Anaesthesia 2012; 67:266–73.
  6. Tsur A, Kalansky A. Hypersensitivity associated with sugammadex administration: a systematic review. Anaesthesia 2014; 69: 1251–7.
  7. Sadleir PH, Russell T, Clarke RC, Maycock E, Platt PR. Intraoperative anaphylaxis to sugammadex and a protocol for intradermal skin testing. Anaesthesia and Intensive Care 2014; 42:93–6.
  8. Platt P, Clarke R, Johnson G, Sadleir P. Efficacy of sugammadex in rocuronium-induced or antibiotic-induced anaphylaxis. A Case Control Study Anaesthesia 2015; 70:1264–7.
  9. Patton K, Borshoff DC. Adverse drug reactions. Anaesthesia.2018;73:76–84.

MIORELAXANTS – ATC classification | Compendium – drug guide

ATX classification

M AGENTS AFFECTING THE LOCUMENT

  • M03A MIORELAXANTS WITH PERIPHERAL ACTION
  • M03B MIORELAXANTS WITH CENTRAL ACTION
  • No. 25 9No. 10 0002 Prices in pharmacies

    Atracurium-Novo

    injection solution 10 mg /ml vial 2.5 ml, No. 5

    Novofarm-Biosintez

    Prices in pharmacies

    Atracurium-Novo

    injection solution 10 mg/ml vial 5 ml, No. 5

    Novofarm-Biosintez 90 030

    Prices in pharmacies

    Baclofen

    tablets 10 mg, no. 50

    Polpharma

    Pharmacy prices

    Baclofen

    tablets 25 mg, no. 50

    Polpharma 9 0030

    Prices in pharmacies

    Botox ®

    powder for solution for injections 100 units-allergan bottle, No. 1

    Allergan Pharmaceuticals Ireland

    2 Prices in pharmacies

    Dysport ®

    Powder for injection 300 units, No. 1

    9

    Prices in pharmacies ax

    Ditilin-Biolek

    injection solution 20 mg/ml 5 ml ampoule, No. 10

    Biolek

    Prices in pharmacies

    Ditilin-Darnitsa

    injection solution 20 mg/ml 5 ml ampoule blisters, pack, No. 10

    Gift

    Prices in pharmacies

    Dorsum

    solution for injection 500 mg/5 ml ampoule 5 ml, No. 10

    injection 2 mg/ml ampoule 2 ml , № 5

    Microchem

    Prices in pharmacies

    Xeomin

    powder for solution for injection 50 IU vial, № 1

    Merz & Co.

    Prices in pharmacies

    Xeomin

    powder for solution for injection 100 U vial, No. 1

    Merz & Co.

    Prices in pharmacies

    Prices in pharmacies

    Mydocalm tablets

    film-coated tablets 50 mg, № 30

    Gedeon Richter

    Prices in pharmacies

    Mydocalm tablets

    film-coated tablets 150 mg, № 30

    Gedeon Richter

    Prices in pharmacies

    Midostad

    coated tablets 50 mg blister, № 30

    Technologist

    Prices in pharmacies

    Midostad

    film-coated tablets 150 mg blister № 30

    Technologist

    Prices in pharmacies

    Myorix

    extended-release capsules, hard 15 mg blister, no. 14

    Acino

    Prices in pharmacies

    Miorix

    capsules of prolonged action, solid 30 mg blister, № 14

    Acino

    Prices in pharmacies

    Muskomed capsules

    hard capsules 4 mg blister, № 20

    World Medicine

    Prices in pharmacies

    World Medicine

    Prices in pharmacies

    Muskomed solution injection

    injection 4 mg/2 ml ampoule 2 ml blisters, No.