Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/1836
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CARISOPRODOL (Tablet)
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The usual adult dosage of carisoprodol tablets, USP is one 350 mg tablet, three times daily and at bedtime. Usage in patients under age 12 is not recommended.
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| dailymed-instance:descripti... |
Carisoprodol is available as 350 mg round, white tablets. Chemically, carisoprodol is N-isopropyl-2-methyl-2-propyl-1,3-propanediol dicarbamate. Carisoprodol is a white, crystalline powder, having a mild, characteristic odor and a bitter taste. It is very slightly soluble in water; freely soluble in alcohol, in chloroform, and in acetone; its solubility is practically independent of pH. Carisoprodol is present as a racemic mixture. The molecular formula is CHNO, with a molecular weight of 260.33. The structural formula is: Inactive Ingredients: Cornstarch, lactose, magnesium stearate, povidone, sodium lauryl sulfate, sodium starch glycolate, stearic acid.
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Carisoprodol is a centrally acting skeletal muscle relaxant that does not directly relax tense skeletal muscles in man. The mode of action of carisoprodol in relieving acute muscle spasm of local origin has not been clearly identified, but may be related to its sedative properties. In animals, carisoprodol has been shown to produce muscle relaxation by blocking interneuronal activity and depressing transmission of polysynaptic neurons in the spinal cord and in the descending reticular formation of the brain. The onset of action is rapid and lasts four to six hours. Carisoprodol is metabolized in the liver and is excreted by the kidneys. One of the products of metabolism, meprobamate, is active as an anxiolytic. The degree to which it contributes to the efficacy of carisoprodol is unknown. Carisoprodol is dialyzable by peritoneal and hemodialysis.<br/>Absorption, Distribution, Metabolism, Excretion: Following a single oral dose of carisoprodol, the time to maximum concentration (T) was 1.98��1.16 hours and the terminal elimination half-life was 2.44��0.93 hours. By normalizing to a single 350 mg carisoprodol tablet, the mean peak plasma concentration (C) was 2.29��- 0.68 ug/mL, the area under the plasma level time curve (AUC) was 10.33��3.87 ug/mL* hour, and the oral clearance (Cl/F) was 39.52��16.83 L/hour. The mean Cof metabolite, meprobamate, was 2.08��0.48 ug/mL, a subtherapeutic concentration when compared to a plasma concentration of a single oral meprobamate 400 mg tablet which would yield a meprobamate concentration of approximately 8.0 ug/mL.<br/>Pharmacokinetics:<br/>Absorption: The pharmacokinetics of carisoprodol was determined in a small in vivo biostudy of 5 men and 5 women. When the dose was normalized to 350 mg, the mean peak plasma concentration (C) achieved was 2.29��0.68 ug/mL. Women tended to reach peak plasma concentrations earlier than men (1.45 vs. 2.5 hours) and had a faster apparent oral clearance (0.772 vs. 0.38 L/hour/kg). The clinical significance of these findings is unknown and they may in part be due to the small number of subjects present in the trial.<br/>Metabolism: Carisoprodol is metabolized in the liver via cytochrome P450 enzyme, CYP2C19. This enzyme exhibits genetic polymorphism. For example, 15-20% of Asian populations may be expected to be poor metabolizers. For Caucasians and Blacks, the prevalence of poor metabolizers is 3-5%. Following a single 350 mg dose of carisoprodol, the corresponding normalized peak concentration of meprobamate, which is a metabolite of carisoprodol, was 2.08��0.48 ug/mL. These levels are approximately��of those seen following a single 400 mg dose of meprobamate.<br/>Elimination: Carisoprodol is eliminated by both renal and non-renal routes with a terminal elimination half-life of 2.44��0.93 hours. It is dialyzable by peritoneal and hemodialysis.<br/>Special Populations: The pharmacokinetic profile of carisoprodol in patients with renal impairment or hepatic impairment has not been evaluated. Because carisoprodol is metabolized by the liver and excreted by the kidneys, possible increased exposure of carisoprodol is expected if hepatic and/or renal function is impaired. The drug should be used with caution in patients with impaired hepatic or renal function. The pharmacokinetic profile of carisoprodol in elderly patients has not been evaluated.
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Carisoprodol is contraindicated in patients with acute intermittent porphyria, and in patients who are allergic to or who have had idiosyncratic reactions to carisoprodol or meprobamate related compounds.
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Carisoprodol tablets USP, 350 mg white, round, debossed MP 58 Bottles of 20 NDC 53489-110-60Bottles of 30 NDC 53489-110-07Bottles of 60 NDC 53489-110-06Bottles of 100 NDC 53489-110-01Bottles of 500 NDC 53489-110-05Bottles of 1000 NDC 53489-110-10 Store at 20��to 25��C (68��to 77��F). [See USP Controlled Room Temperature] DISPENSE IN TIGHT, LIGHT-RESISTANT CONTAINER.
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Seizure Disorders: There have been rare reports of seizures in postmarketing surveillance in temporal association with carisoprodol. These events have involved patients with and without previous medical histories of seizures and have occurred during therapeutic use, with overdose and during withdrawal from prolonged use. The role of carisoprodol in the causality of these seizures has not been established. Carisoprodol is metabolized in the liver and excreted by the kidney; to avoid its excess accumulation, caution should be exercised in administration to patients with compromised liver or kidney function.
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Overdosage of carisoprodol produces CNS depression, and in severe cases coma. Shock, respiratory depression, seizures and death have also been reported rarely. The following signs and symptoms may be associated with carisoprodol overdosage: horizontal and vertical nystagmus, blurred vision, mydriasis, mild tachycardia and hypotension, respiratory depression, euphoria, CNS stimulation, muscular incoordination, and/or rigidity, confusion, headache, hallucinations, and dystonic reactions. The effects of an overdosage of carisoprodol and alcohol or other CNS depressants or psychotropic agents can be additive even when one of the drugs has been taken in the usual recommended dosage. Fatal accidental and non-accidental overdoses have been reported alone or in combination with alcohol or psychotropic drugs.<br/>Treatment of Overdosage: Basic life support measures should be instituted as dictated by the clinical presentation. Induced emesis is not recommended due to the risk of CNS and respiratory depression. Gastric lavage should be considered soon after ingestion (usually within 1 hour). In cases of severe CNS depression, airway protective reflexes may be compromised. In such cases, tracheal intubation should be considered for airway protection and respiratory support. Circulatory support should be administered with volume infusion and pressor agents as indicated. Seizures should be treated with a benzodiazepine IV and may be followed with phenobarbital if seizures recur. Carisoprodol is metabolized in the liver and excreted by the kidney. The following types of treatment have been used successfully with the related drug meprobamate: activated charcoal (oral or via nasogastric tube), forced diuresis, peritoneal dialysis, and hemodialysis (carisoprodol is dialyzable). Careful monitoring of urinary output is necessary and caution should be taken to avoid overhydration. Observe for possible relapse due to incomplete gastric emptying and delayed absorption. Carisoprodol can be measured in biological fluids by gas chromatography (Douglas, J. F. et al.: J Pharm Sci 58: 145, 1969). For more information on the management of overdose or unintentional ingestion, contact a Poison Control Center.
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carisoprodol
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CARISOPRODOL (Tablet)
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Cardiovascular���Tachycardia, postural hypotension, and facial flushing. Central Nervous System���Drowsiness and other CNS effects may require dosage reduction. Also observed: dizziness, vertigo, ataxia, tremor, agitation, irritability, headache, depressive reactions, syncope, seizures, and insomnia. (See also Idiosyncratic Reactions under "Warnings.") Gastrointestinal���Nausea, vomiting, hiccup, and epigastric distress. Hematologic���Leukopenia, in which other drugs or viral infection may have been responsible, and pancytopenia, attributed to phenylbutazone, have been reported. No serious blood dyscrasias have been attributed to carisoprodol.
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CARISOPRODOL
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