Sunday, January 20, 2008

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Side effects

Carisoprodol seems to be more effective as a muscle relaxant than meprobamate but it also has the side effects of the latter drug (trade name Miltown®) which is a related non-barbiturate and non-benzodiazepine sedative-hypnotic which has been largely replaced by Carisoprodol. Both carisoprodol and meprobamate can produce a glutethimide-like euphoria in certain dose ranges; a euphoriant dose of either drug will also rapidly produce somnolence and the patient can be in a deep sleep shortly after euphoria, anxiolysis, ataxia and other side effects manifest. However, the usual dose of 350 mg is unlikely to engender prominent side effects. At higher doses, in some patients, and/or early in therapy, carisoprodol can have the full spectrum of sedative-hypnotic side effects (and often to an extent to which the patient may not be fully aware) and can dangerously impair the patient's ability to operate an automobile, motorcycle, and other machinery of various types; slurred speech is also a side effect which manifests rather rapidly. The intensity of the side effects of carisoprodol tends to lessen and/or become very predictable as therapy continues, as is the case with many other drugs.

The interaction of carisoprodol with opioids, esentially all opioids and other centrally-acting analgesics, but especially those of the codeine-derived subgroup of the semi-synthetic class (codeine, ethylmorphine, dihydrocodeine, hydrocodone, oxycodone, nicocodeine, benzylmorphine, the various acetylated codeine derivatives including thebacon and acetyldihydrocodeine, dihydroisocodeine, nicodicodeine and others) which allows the use of a smaller dose of the opioid to have a given effect, is useful in general and espcially where injury and/or muscle spasm is a large part of the problem. The potentiation effect is also useful in other pain situations and is also especially useful with opioids of the open-chain class such as methadone, levomethadone, ketobemidone, phenadoxone and others.

The use of methadone with carisoprodol and an NSAID such as diclofenac where indicated is a treatment for chronic low back pain which is gaining in popularity in the United States and other countries. After significant somonolence in some patients in the first few days of this protocol for pain control, patients are able to regain overall function very well in a lot of cases and the interaction of carisoprodol and methadone with the NMDA system in the CNS may be part of the excellent pain relief and attenuation of some opioid side effects usually obtained by using this protocol. In European countries, ketobemidone is a good and even superior replacement for the methadone.

The potentiation effect is also something noted by recreational drugs users, and is accompanied by an economy of scale increase of the euphoria and deaths have resulted from carelessly combining overdoses of hydrocodone and carisoprodol.

Meprobamate and other muscle relaxing drugs often were subjects of misuse and abuse in the 1950s and 1960s.[5][6] Overdose cases were reported as early as 1957 and have been reported on several occasions since then.[7][8][9][10][11][12][13]

[edit] Pharmacokinetics

Carisoprodol has a rapid, 30 minute onset of action, with the aforementioned effects lasting for approximately 2–6 hours. It is metabolized in the liver via the cytochrome P450 oxidase isozyme CYP2C19, excreted by the kidneys and has an approximate 8 hour half-life. A considerable proportion of carisoprodol is metabolized to meprobamate, which is a known drug of abuse and dependence; this could account for the abuse potential of carisoprodol.

[edit] Notes

  1. ^ Bramness JG, Furu K, Engeland A, Skurtveit S. (2007). "Carisoprodol use and abuse in Norway. A pharmacoepidemiological study". Br J Clin Pharmacol (2): 210-218.
  2. ^ Miller JG, ed. The pharmacology and clinical usefulness of carisoprodol. Detroit:Wayne State University; 1959.
  3. ^ Berger F, Kletzkin M, Ludwig B, Margolin S. The history, chemistry, and pharmacology of carisoprodol. Annals of the New York Academy of Sciences. 1959;86:90-107
  4. ^ Brave New Soma - TIME. Retrieved on 2007-08-20.
  5. ^ Kamin I, Shaskan D. (1959). "Death due to massive overdose of meprobamate". Am J Psychiatry 115 (12): 1123-1124.
  6. ^ Hollister LE (1983). "The pre-benzodiazepine era". J Psychoactive Drugs 15 (1-2): 9-13.
  7. ^ Gaillard Y, Billault F, Pepin G (1997). "Meprobamate overdosage: a continuing problem. Sensitive GC-MS quantitation after solid phase extraction in 19 fatal cases". Forensic Sci.Int 86 (3): 173-180.
  8. ^ Allen MD, Greenblatt DJ, Noel BJ (1977). "Meprobamate overdosage: a continuing problem". Clin Toxicol 11 (5): 501-515.
  9. ^ Kintz P, Tracqui A, Mangin P, Lugnier AA (1988). "Fatal meprobamate self-poisoning". Am J Forensic Med Pathol 9 (2): 139-140.
  10. ^ Eeckhout E, Huyghens L, Loef B, Maes V, Sennesael J (1988). "Meprobamate poisoning, hypotension and the Swan-Ganz catheter". Intensive Care Med 14 (4): 437-438.
  11. ^ Lhoste F, Lemaire F, Rapin M (1977). "Treatment of hypotension in meprobamate poisoning". N Engl J Med 296 (17): 1004.
  12. ^ Bedson H (1959). "Coma due to meprobamate intoxication. Report of a case confirmed by chemical analysis". Lancet 273 (1): 288-290.
  13. ^ Blumberg A, Rosett H, Dobrow A (1959). "Severe hypotension reactions following meprobamate overdosage". Ann Intern Med 51: 607-612.

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Drug Name

Soma (Carisoprodol)

Drug Uses

Soma is a muscle relaxant used to relieve the pain and stiffness of muscle spasms and discomfort due to strain and sprain.

How Taken

The usual adult dosage of soma is one 350 mg tablet, three times daily and at bedtime. Usage in patients under age 12 is not recommended. It is recommended that you take Soma with food, or with milk, to minimize the likelihood that you will suffer an upset stomach as a result of taking the medication.

Drug Class and Mechanism

Soma is a muscle relaxant. It acts by blocking electrical communication among nerves in the reticular formation of the brain and in the spinal cord.

Missed Dose

If you miss a Soma dose, take it as soon as remembered if it is within an hour or so. If you do not remember until later, skip the missed dose and resume your usual dosing schedule. Do not 'double-up' the Soma dose to catch up.

Storage

Store at controlled room temperature 15 - 30 degrees C (59 degrees F). Dispense in a tight container.

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