Carisoprodol

Carisoprodol is a centrally-acting skeletal pH.

Carisoprodol is marketed in the United States under the brand name Soma, and in the United Kingdom and other countries under the brand names Sanoma and Carisoma. Carisoprodol is especially useful against various types of pain (whether or not related to muscle spasm) because of its analgesic-sparing (potentiating) effect on opioid analgesics. Carisoprodol is available by itself or mixed with aspirin and in one preparation (Soma Compound With Codeine®) along with codeine and caffeine as well.

As of November 2007 Carisoprodol has been taken off the market in Sweden due to problems with dependence, abuse and side effects. The agency overseeing pharmaceuticals has considered other drugs used with the same indications as carisoprodol to have the same or better effects without the risks of the drug[1].

History

On June 1, 1959 several American pharmacologists convened at Wayne State University in Detroit, Michigan to discuss a new drug. The drug, originally thought to have antiseptic properties, was found to have central muscle relaxing properties.^[2] It had been developed by Dr. Frank M. Berger at Wallace laboratories and had been named carisoprodol (trade name Soma).

Carisoprodol was developed on the basis of molecule with new pharmacological properties.

The brand name Soma is shared with the Soma/Haoma of ancient India, a drug mentioned in ancient Sanskrit writings which various classical and modern researchers have theorised could be anything from epheda to mushrooms of the genus Amanita with hallucinogenic and psychedelic properties related to the coca or other drugs ported from the Western Hemisphere by an as yet unkown pre-Viking, pre-Columbian contact. Soma is also the name of the fictional drug featured in Aldous Huxley's Brave New World.^[4]

Chemistry

It is a carbamic acid stereoisomers.

Effects

• Analgesia
• Relief from hypertonia

Side effects

Carisoprodol seems to be more effective as a muscle relaxant than 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 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]}

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 meprobamate, which is a known drug of abuse and dependence; this could account for the abuse potential of carisoprodol.

Notes

References

• APhA Drug Information Handbook