What are muscle relaxants?

Muscle relaxants (or miorelaxants) are a generic name for a number of drugs that due to the action of one or another active substance allow you to relax skeletal muscles up to complete immobility. Such drugs are used in the treatment of various diseases, as well as for diagnostic purposes, when it is necessary for a person to be conscious, and his muscles should not contract.

Muscle relaxants help reduce excess tension in the lower back, relieve increased muscle tone in patients who have had a stroke, after a traumatic brain or spinal injury, with multiple sclerosis1 and a number of other diseases.

There are muscle relaxants of central and peripheral action. The former inhibit the process of excitation in the central nervous system and suppress reflexes. The latter do not affect the neurons of the brain, but act directly on the points of contact of the muscles with the nerve endings.

Important advantages of using muscle relaxants:

  • help relieve muscle tension
  • reduce pain
  • improve motor activity
  • allow you to reduce the dose of painkillers and enhance their effect

One of the most effective muscle relaxant is carisoprodol (soma).

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Description

SOMA (carisoprodol) Tablets are available as 350 mg and 500 mg round, white tablets. Carisoprodol is a white, crystalline powder, having a mild, characteristic odor and a bitter taste. It is slightly soluble in water; freely soluble in alcohol, in chloroform, and in acetone; and its solubility is practically independent of pH. Carisoprodol is present as a racemic mixture.

Indications

SOMA is indicated for the relief of discomfort associated with acute, painful musculoskeletal conditions in adults.

Limitation of Use

SOMA should only be used for short periods (up to two or three weeks) because adequate evidence of effectiveness for more prolonged use has not been established and because acute, painful musculoskeletal conditions are generally of short duration.

Contraindications

SOMA is contraindicated in patients with a history of acute intermittent porphyria or a hypersensitivity reaction to a carbamate such as meprobamate.

Consult your doctor before you buy soma online. Any medication should only be taken as directed by a doctor.

Warnings and precautions

SOMA has sedative properties (in the low back pain trials, 13% to 17% of patients who received SOMA experienced sedation compared to 6% of patients who received placebo) and may impair the mental and/or physical abilities required for the performance of potentially hazardous tasks such as driving a motor vehicle or operating machinery. There have been post-marketing reports of motor vehicle accidents associated with the use of SOMA.

Since the sedative effects of SOMA and other CNS depressants (e.g., alcohol, benzodiazepines, opioids, tricyclic antidepressants) may be additive, appropriate caution should be exercised with patients who take more than one of these CNS depressants simultaneously.

Abuse, dependence and withdrawal

Carisoprodol, the active ingredient in SOMA, has been subject to abuse, dependence, and withdrawal, misuse and criminal diversion.

Abuse of SOMA poses a risk of overdosage which may lead to death, CNS and respiratory depression, hypotension, seizures and other disorders.

Post-marketing experience cases of carisoprodol abuse and dependence have been reported in patients with prolonged use and a history of drug abuse. Although most of these patients took other drugs of abuse, some patients solely abused carisoprodol. Withdrawal symptoms have been reported following abrupt cessation of SOMA after prolonged use. Reported withdrawal symptoms included insomnia, vomiting, abdominal cramps, headache, tremors, muscle twitching, ataxia, hallucinations, and psychosis.

To reduce the risk of SOMA abuse assess the risk of abuse prior to prescribing. After prescribing, limit the length of treatment to three weeks for the relief of acute musculoskeletal discomfort, keep careful prescription records, monitor for signs of abuse and overdose, and educate patients and their families about abuse and on proper storage and disposal.

Mechanism of Action

The mechanism of action of carisoprodol in relieving discomfort associated with acute painful musculoskeletal conditions has not been clearly identified. In animal studies, muscle relaxation induced by carisoprodol is associated with altered interneuronal activity in the spinal cord and in the descending reticular formation of the brain.

Pharmacodynamics

Carisoprodol is a centrally acting skeletal muscle relaxant that does not directly relax skeletal muscles. A metabolite of carisoprodol, meprobamate, has anxiolytic and sedative properties. The degree to which these properties of meprobamate contribute to the safety and efficacy of SOMA is unknown.

Pharmacokinetics

Absorption. The pharmacokinetics of carisoprodol and its metabolite meprobamate were studied in a crossover study of 24 healthy subjects (12 male and 12 female) who received single doses of 250 mg and 350 mg SOMA. The exposure of carisoprodol and meprobamate was dose proportional between the 250 mg and 350 mg doses. The Cmax of meprobamate was 2.5 ± 0.5 μg/mL (mean ± SD) after administration of a single 350 mg dose of SOMA, which is approximately 30% of the Cmax of meprobamate (approximately 8 μg/mL) after administration of a single 400 mg dose of meprobamate.

Absolute bioavailability of carisoprodol has not been determined. The mean time to peak plasma concentrations (Tmax) of carisoprodol was approximately 1.5 to 2 hours. Food Effect: Co-administration of a high-fat meal with SOMA (350 mg tablet) had no effect on the pharmacokinetics of carisoprodol. Therefore, SOMA may be administered with or without food.

Elimination

Metabolism: The major pathway of carisoprodol metabolism is via the liver by cytochrome enzyme CYP2C19 to form meprobamate. This enzyme exhibits genetic polymorphism.

Excretion: Carisoprodol is eliminated by both renal and non-renal routes with a terminal elimination half-life of approximately 2 hours. The half-life of meprobamate is approximately 10 hours.

Drug interactions

The sedative effects of SOMA and other CNS depressants (e.g., alcohol, benzodiazepines, opioids, tricyclic antidepressants) may be additive. Therefore, caution should be exercised with patients who take more than one of these CNS depressants simultaneously. Concomitant use of SOMA and meprobamate, a metabolite of SOMA, is not recommended.

Carisoprodol is metabolized in the liver by CYP2C19 to form meprobamate. Co-administration of CYP2C19 inhibitors, such as omeprazole or fluvoxamine, with SOMA could result in increased exposure of carisoprodol and decreased exposure of meprobamate. Co-administration of CYP2C19 inducers, such as rifampin or St.John’s Wort, with SOMA could result in decreased exposure of carisoprodol and increased exposure of meprobamate. Low dose aspirin also showed an induction effect on CYP2C19. The full pharmacological impact of these potential alterations of exposures in terms of either efficacy or safety of SOMA is unknown.

Side effects

  • Dizziness, drowsiness, or headache may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.
  • 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: confusion.
  • 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.

Consult your doctor before you decide to buy soma online

Overdose

Overdosage of SOMA commonly produces CNS depression. Death, coma, respiratory depression, hypotension, seizures, delirium, hallucinations, dystonic reactions, nystagmus, blurred vision, mydriasis, euphoria, muscular incoordination, rigidity, and/or headache have been reported with SOMA overdosage. Serotonin syndrome has been reported with carisoprodol intoxication. Many of the carisoprodol overdoses have occurred in the setting of multiple drug overdoses (including drugs of abuse, illegal drugs, and alcohol). The effects of an overdose of carisoprodol and other CNS depressants (e.g., alcohol, benzodiazepines, opioids, tricyclic antidepressants) can be additive even when one of the drugs has been taken in the recommended dosage. Fatal accidental and non-accidental overdoses of SOMA have been reported alone or in combination with CNS depressants.

Treatment of overdosage

Basic life support measures should be instituted as dictated by the clinical presentation of the SOMA overdose. Vomiting should not be induced because of the risk of CNS and respiratory depression, and subsequent aspiration. Circulatory support should be administered with volume infusion and vasopressor agents if needed. Seizures should be treated with intravenous benzodiazepines and the reoccurrence of seizures may be treated with phenobarbital. In cases of severe CNS depression, airway protective reflexes may be compromised and tracheal intubation should be considered for airway protection and respiratory support.

Sources: https://www.accessdata.fda.gov
https://www.webmd.com

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