Carisoprodol

Source: Wikipedia, the free encyclopedia.

Carisoprodol
Clinical data
Pronunciation/kərˌaɪsʌˈproʊdɒl/
kahr-EYE-suh-PROH-dol
Trade namesSoma, others[1]
AHFS/Drugs.comMonograph
MedlinePlusa682578
License data
By mouth[3]
Drug classMuscle relaxant[3]
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding60%
MetabolismLiver (CYP2C19-mediated)
MetabolitesMeprobamate
Onset of actionRapid (30 minutes[6][failed verification])
Elimination half-life2.5 hours [12 hours[nb 1]]
ExcretionKidney
Identifiers
  • (RS)-2-{[(aminocarbonyl)oxy]methyl}-2-methylpentyl isopropylcarbamate
JSmol)
SMILES
  • O=C(N)OCC(C)(CCC)COC(=O)NC(C)C
  • InChI=1S/C12H24N2O4/c1-5-6-12(4,7-17-10(13)15)8-18-11(16)14-9(2)3/h9H,5-8H2,1-4H3,(H2,13,15)(H,14,16) checkY
  • Key:OFZCIYFFPZCNJE-UHFFFAOYSA-N checkY
  (verify)


Carisoprodol, sold under the brand name Soma among others, is an oral medication used for

musculoskeletal pain.[7] Effects generally begin within half an hour and last for up to six hours.[7]

Common side effects include headache, dizziness, and sleepiness.

sulfa allergy certain formulations may result in problems.[7] Safety during pregnancy and breastfeeding is not clear.[7][8] How it works is not clear.[7] Some of its effects are believed to occur following metabolic conversion into meprobamate, carisoprodol's main active metabolite.[7]

Carisoprodol was approved for medical use in the United States in 1959.

generic medication.[7] In 2019, it was the 343rd most commonly prescribed medication in the United States, with more than 800 thousand prescriptions.[10] In the United States, it is a Schedule IV controlled substance.[7]

Medical uses

Somadril Comp. – combination muscle relaxant medication containing carisoprodol, paracetamol (acetaminophen), and caffeine

Carisoprodol is meant to be used along with rest,

sprains and muscle injuries.[11] It comes in tablet format and is taken by the mouth three times a day and before bed.[11]

Side effects

The usual dose of 350 mg is unlikely to engender prominent side effects other than

skin rash.[11]

There are 368 drugs known to interact with carisoprodol including 28 major drug interactions.[13] The interaction of carisoprodol with essentially all opioids, and other centrally acting analgesics, but especially codeine, those of the codeine-derived subgroup of the semisynthetic class (ethylmorphine, dihydrocodeine, hydrocodone, oxycodone, nicocodeine, benzylmorphine, the various acetylated codeine derivatives including 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 especially where skeletal muscle injury and/or 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. In recreational drug users, deaths have resulted from combining doses of hydrocodone and carisoprodol. Another danger of misuse of carisoprodol and opiates is the potential to asphyxiate while unconscious.[citation needed]

Meprobamate and other muscle-relaxing drugs often were subjects of misuse in the 1950s and 60s.[14][15] Overdose cases were reported as early as 1957, and have been reported on several occasions since then.[16][17][18][19][20][21][22]

Carisoprodol is metabolized by the liver and excreted by the kidneys, so this drug must be used with caution with patients that have impaired hepatic or

renal function.[23] Because of potential for more severe side effects, this drug is on the list to avoid for elderly people.[24]

Withdrawal

Carisoprodol, meprobamate, and related drugs such as tybamate, have the potential to produce physical dependence of the barbiturate type following periods of prolonged use. Withdrawal of the drug after extensive use may require hospitalization in medically compromised patients. In severe cases the withdrawal can mimic the symptoms of alcohol withdrawal including the potentially lethal status epilepticus.

Psychological dependence has also been linked to carisoprodol use[25] although this is much less severe than with meprobamate itself (presumably due to the slower onset of effects). Psychological dependence is more common in those who use carisoprodol non-medically and those who have a history of substance use (particularly sedatives or alcohol). It may reach clinical significance before physiological tolerance and dependence have occurred and (as with benzodiazepines) has been demonstrated to persist to varying degrees of severity for months or years after discontinuation.

Discontinuation of carisoprodol, as with all GABA-ergics, can result in cognitive changes which persist for weeks, months, or rarely even years including greatly increased anxiety and depression,

phobias, reduced IQ, short term and long-term memory loss, and dozens of other sequelae.[26]
The effects, severity, and duration appear to be slightly dose-dependent but are mainly determined by the patients pattern of use (taken as prescribed, taken in bulk doses, mixed with other drugs, a combination of the above, etc.), genetic predisposition to substance use, and a history of substance use all increase the patients risk of persistent discontinuation syndrome symptoms.

Treatment for physical withdrawal generally involves switching the patient to a long-acting benzodiazepine such as diazepam or clonazepam then slowly titrating them off the replacement drug completely at a rate which is both reasonably comfortable for the patient but rapid enough for the managing physician to consider the rate of progress acceptable (overly rapid dose reduction greatly increases the risk of patient non-compliance such as the use of illicitly obtained alternative sedatives and/or alcohol). Psychotherapy and cognitive behavioral therapy have demonstrated moderate success in reducing the rebound anxiety which results upon carisoprodol discontinuation but only when combined with regular and active attendance to a substance use support group.[27]

Carisoprodol withdrawal can be life-threatening (especially in high dose users and those who attempt to quit "cold turkey"). Medical supervision is recommended, with gradual reduction of dose of carisoprodol or a substituted medication, typical of other depressant drugs.

Non-medical use

Combining a muscle relaxant like carisoprodol with opioids and benzodiazepines is referred to as "The Holy Trinity" as it has been reported to increase the power of the "high".[28]

Recreational users of carisoprodol usually seek its potentially heavy sedating, relaxant, and anxiolytic effects.[29] Also, because of its potentiating effects on narcotics, it is often used in conjunction with many opioid drugs. Also it is not detected on standard drug testing screens. On 26 March 2010 the DEA issued a Notice of Hearing on proposed rule making in respect to the placement of carisoprodol in schedule IV of the Controlled Substances Act.[30] The DEA ended up classifying it under schedule IV.[31] Carisoprodol is sometimes mixed with date rape drugs.[32]

Overdose

As with other GABAergic drugs, combination with other drugs that depress the respiratory system, such as alcohol, sedatives and opioids possess a significant risk to the user in the form of overdose.

respiratory depression (and subsequent pulmonary aspiration), coma, and death.[34]

Carisoprodol is not detected on all toxicology tests which may delay diagnosis of overdose. Overdose symptoms in combination with opiates are similar but are distinguished by the presentation of normal or

pressors as indicated and, in rare cases, bemegride. Total amnesia of the experience is not uncommon following recovery.[citation needed
]

In 2014 actress Skye McCole Bartusiak died of an overdose due to the combined effects of carisoprodol, hydrocodone and difluoroethane.[35]

In 1999 actress Dana Plato died after taking carisoprodol (Soma) along with a few doses of a hydrocodone / acetaminophen painkiller (Lortab), in an overdose that was ruled a suicide.[36]

Pharmacology

Pharmacodynamics

Carisoprodol, has a chemical structure similar to

glutamate
, a neurotransmitter, and dimethylglycine.

Carisoprodol's structural similarity to meprobamate indicates GABAergic activity, including GABAA agonism, similar to the mechanism of benzodiazepines.[37] This will allow for further muscle relaxation and anxiety reduction. Therefore, carisoprodol, at low to moderate dosages, may be clinically indicated for absent seizures, yet exacerbate

tonic-clonic seizures.[medical citation needed
]

Pharmacokinetics

Carisoprodol has a rapid, 30-minute onset of action, with the aforementioned effects lasting about two to six hours. It is metabolized in the liver via the

cytochrome P450 oxidase isozyme CYP2C19, excreted by the kidneys and has about an eight-hour half-life. In patients with low levels of CYP2C19 (poor metabolizers), standard doses can lead to increased concentrations of carisoprodol (up-to a four-fold increase).[38] A considerable proportion of carisoprodol is metabolized to meprobamate
, which is a known addictive substance; this could account for the addictive potential of carisoprodol (meprobamate levels reach higher peak plasma levels than carisoprodol itself following administration).

It is slightly

soluble in water and freely soluble in ethanol, chloroform and acetone. The drug's solubility is practically independent of pH
.

History

In June 1959, several American pharmacologists convened at

Wallace Laboratories and was named carisoprodol.[39]

Building on meprobamate's pharmacological effects, carisoprodol was intended to have better muscle relaxing properties, less potential for addiction, and a lower risk of overdose. Carisoprodol's effect profile did indeed turn out to differ significantly with respect to meprobamate, with carisoprodol possessing stronger muscle relaxant and analgesic effects.[40]

Norway

Reports from Norway have shown carisoprodol has addictive potential[41] as a prodrug of meprobamate and/or potentiator of hydrocodone, oxycodone, codeine, and similar drugs. In May 2008 it was taken off the market in Norway.[42]

European Union

In the EU, the European Medicines Agency issued a release recommending member states suspend marketing authorization for this product in the treatment of acute (not chronic) back pain.[43]

As of November 2007, carisoprodol has been taken off the market in Sweden due to problems with dependence and side effects. The agency overseeing pharmaceuticals considered other drugs used with the same indications as carisoprodol to have the same or better effects without the risks of the drug.[44]

United States

In December 2011, the Drug Enforcement Administration (DEA) issued the final ruling placing carisoprodol on Schedule IV of the Controlled Substances Act (CSA). The placement of carisoprodol on Schedule IV was effective in January 2012.[45]

Canada

Federally, carisoprodol is a prescription drug (Schedule I, sub-schedule F1).[46] Provincial regulations vary.[47] It is no longer readily available.[medical citation needed]

Indonesia

  • In September 2013, carisoprodol was taken off the market due to problems with diversion, dependence and side effects.
  • In September 2017, one child died and 50 had seizures when PCC, which stands for "Paracetamol Caffeine Carisoprodol" was mixed (probably illicit) into children's drinks in elementary and junior high schools in Kendari.[48]

Notes

  1. ^ At least 25% of the carisoprodol in the body is transformed by the liver into meprobamate, its main active metabolite, which in turn has a half-life of 10 hours.[6]

References

  1. ^ "Carisoprodol". drugs.com. Retrieved 16 April 2017.
  2. ^ "Drug Scheduling". U.S. Drug Enforcement Administration (DEA). Retrieved 24 March 2024.
  3. ^ a b c "Soma- carisoprodol tablet". DailyMed. 15 May 2023. Retrieved 20 May 2024.
  4. ^ "Soma Product information". Health Canada. 14 March 2003. Retrieved 20 May 2024.
  5. ^ "Notice of consultation: Removing carisoprodol from the Prescription Drug List (PDL)". Health Canada. 18 February 2025. Retrieved 20 February 2025.
  6. ^
    ISBN 978-607-625-072-3
    . Retrieved 13 June 2021.
  7. ^ a b c d e f g h i j k "Carisoprodol Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 8 April 2019.
  8. ^ "DailyMed - carisoprodol tablet". dailymed.nlm.nih.gov. Retrieved 8 April 2019.
  9. ^ "Carisoprodol". European Medicines Agency. 15 November 2007. Retrieved 8 April 2019.
  10. ^ "Carisoprodol - Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.
  11. ^ a b c "Carisoprodol". MedlinePlus. National Library of Medicine. Retrieved 6 May 2019.
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  13. ^ "Carisoprodol Drug Interactions". Drugs.com. Drugs.com. Retrieved 4 June 2024.
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  23. ^ "CARISOPRODOL". TOXNET. National Library of Medicine. Retrieved 6 May 2019.
  24. ^ NCQA's HEDIS Measure: Use of High Risk Medications in the Elderly Archived 1 February 2010 at the Wayback Machine
  25. ^ "What is Carisoprodol used for?". Pain o Soma medicines. 19 March 2021. Retrieved 29 April 2021.
  26. PMID 15033227
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  27. ^ Susan D (1 April 2025). "Buying Soma Online Without a Prescription? A 2025 Safety Guide". Pharma Care. Retrieved 3 April 2025.
  28. S2CID 25909460
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  29. ^ "DEA Drugs & Chemicals of Concern "Carisoprodol"". Archived from the original on 17 April 2011. Retrieved 29 April 2011.
  30. ^ "Schedules of Controlled Substances: Placement of Carisoprodol Into Schedule IV; Announcement of Hearing". Archived from the original on 15 July 2011. Retrieved 19 April 2010.
  31. ^ "Carisoprodol" (PDF). Drug Enforcement Administration, Diversion Control Division, Drug & Chemical Evaluation Section. U.S. Department of Justice. December 2019.
  32. PMID 19547737
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  33. ISBN 978-0-444-53716-4
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  34. ^ "What Does a Soma Overdose Look Like?". Project Know. Retrieved 22 October 2023.
  35. ^ Duke A (22 July 2014). "'Patriot' actress Skye McCole Bartusiak dead at 21". CNN Entertainment. Retrieved 24 February 2019.
  36. ^ "Death of 'Diff'rent Strokes' Actress Ruled A Suicide". Chicago Tribune. 21 May 1999. Archived from the original on 24 March 2019. Retrieved 3 June 2024.
  37. PMID 31971718
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  38. PMID 28520382
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  39. ISBN 978-0-7837-3656-3.[page needed
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  40. S2CID 11909344
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  42. ^ "Somadril trekkes fra markedet" [Somadril is withdrawn from the market]. Norwegian Medicines Agency (in Norwegian). 20 April 2008. Archived from the original on 16 July 2011. Retrieved 12 March 2010.
  43. ^ "Carisprodol press release" (PDF). EMEA. Archived from the original (PDF) on 18 July 2009. Retrieved 12 May 2008.
  44. ^ "Marknadsföringen av Somadril och Somadril comp rekommenderas upphöra tillfälligt" [Marketing of Somadril and Somadril is recommended to cease temporarily] (in Swedish). 16 November 2007. Archived from the original on 23 July 2014. Retrieved 9 May 2009.
  45. ^ US Department of Justice (2011). "Schedules of Controlled Substances: Placement of Carisoprodol into Schedule IV" (PDF). Federal Register. 76 (238): 77330–77360. Retrieved 1 February 2012.
  46. ^ "NAPRA – Search National Drug Schedule". National Association of Pharmacy Regulatory Authorities. 2009. Archived from the original (ASP) on 1 February 2014. Retrieved 7 January 2014.
  47. ^ For British Columbia, see library.bcpharmacists.org/D-Legislation_Standards Archived 17 December 2013 at the Wayback Machine
  48. ^ "One Schoolchild Dies, More Than 50 Suffer Seizures After Consuming Pills in Southeast Sulawesi". Jakarta Globe. 14 September 2017.

Further reading
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