We regularly hear about the uses and benefits of carisoprodol . Here are all the details about this drug.
Index
Carisoprodol – What is it
Carisoprodol, marketed under the brand name Soma among others, is a prescription drug that has been marketed since 1959. It is a centrally acting skeletal muscle relaxant of the carbamate class and produces all the effects associated with barbiturates. It is a prodrug and is structurally and pharmacologically related to meprobamate. The main metabolic pathway for carisoprodol involves its conversion to meprobamate.
Carisoprodol – Usos
Medical uses
- Analgesia
- Ansiolisis
- Muscle relaxation (and hypertonia relief)
- Erectile hyperfunction
- Drowsiness
Carisoprodol – Side Effects
The usual 350 mg dose is unlikely to produce prominent side effects other than drowsiness, and mild to significant euphoria or dysphoria, but the euphoria is generally short-lived. The drug is well tolerated and without adverse effects in most patients for whom it is indicated. In some patients, however, and / or at the beginning of therapy, carisoprodol can have the full spectrum of sedative side effects and can affect the patient’s ability to operate firearms, motor vehicles and other machinery of various kinds, especially when They are taken with drugs that contain alcohol, in which case an alternative drug would be considered. The intensity of carisoprodol side effects tends to decrease as therapy continues,
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 derivatives of codeine 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 potentiating effect is also useful in other pain situations and is also especially useful with opiates of the open chain class, such as methadone, levomethadone, ketobemidone, phenaxone and others. In recreational drug users, deaths have resulted from the careless combination of hydrocodone and carisoprodol overdoses. Another danger of carisoprodol and opioid misuse is the potential for aspiration while unconscious.
Carisoprodol – Withdrawal
Carisoprodol, meprobamate, and related drugs, such as tybamate, have the potential to produce barbiturate-type physical dependence after periods of prolonged use. Withdrawal of the drug after extensive use may require hospitalization in medically compromised patients. In severe cases, withdrawal can mimic the symptoms of alcohol withdrawal, including life-threatening status epilepticus.
Psychological dependence has also been linked to the use of carisoprodol, although this is much less serious than with meprobamate itself (presumably due to the slower onset of effects). Psychological dependence is more common in those who abuse carisoprodol and those who have a history of drug abuse (particularly sedatives or alcohol). It can reach clinical significance before tolerance and physiological dependence have occurred and (as with benzodiazepines) it has been shown to persist in varying degrees of severity for months to years after discontinuation.
Carisoprodol – Withdrawal
Discontinuation of carisoprodol, as with all GABA-ergics, can lead to persistent cognitive changes that persist for weeks, months, or rarely even years, including severe anxiety and depression, social withdrawal, triggering agitation / aggression. hair loss, chronic insomnia, new or aggravated (often illogical) phobias, lowered IQ, short- and long-term memory loss, and dozens of other sequelae.
The effects, severity, and duration appear to be slightly dose dependent, but are primarily determined by the patient’s use pattern (taken as prescribed, taken in bulk, mixed with other drugs, a combination of the above, etc. ), genetic predisposition to drug abuse, and a history of substance abuse increase patients’ risk of symptoms of persistent discontinuation syndrome.
Psychotherapy and cognitive behavior therapy have shown moderate success in reducing rebound anxiety. Carisoprodol withdrawal can be life-threatening. Medical supervision is recommended, with a gradual reduction in the dose of carisoprodol or a substitute medication, typical of other depressant drugs.
Carisoprodol – Recreational Use and Abuse
Recreational carisoprodol users are generally looking for potentially strong sedative, relaxing, and anxiolytic effects. Furthermore, due to its potentiating effects on narcotics, it is often abused in conjunction with many opioid drugs. Also, it is not detected on standard drug test screens. On March 26, 2010, the DEA issued a Notice of Hearing on the proposed rulemaking regarding the placement of carisoprodol in Schedule IV of the Controlled Substances Act. Carisoprodol is sometimes mixed with date rape drugs.
Carisoprodol produces the same enzyme-inducing effects as barbiturates and can be used to potentiate pro-drug opiates, most commonly codeine and hydrocodone, by increasing the amount of prodrug converted to active metabolites (morphine and hydromorphone, respectively). This mechanism, along with the combined euphoria, sedation, and anxiolytic effects of the two drugs, makes the practice incredibly dangerous, and unintentional overdoses are not uncommon. The combination of hydrocodone and carisoprodol is mentioned in some harm reduction forums as a “Las Vegas cocktail.” Many overdoses have resulted from recreational users combining these drugs to combine their individual effects without being aware of the enzyme-induced potentiation.
Carisoprodol – Overdose
As with other GABAergic medications, the combination with other GABAergic medications, including alcohol, as well as sedatives in general, presents a significant risk to the user in the form of an overdose. Overdose symptoms are similar to those of other GABAergics, including excessive sedation and lack of response to stimuli, severe ataxia, amnesia, confusion, agitation, intoxication, and inappropriate (potentially violent) behavior. Severe overdoses can present with respiratory depression (and subsequent pulmonary aspiration), coma, and death.
Carisoprodol is not detected in all toxicology tests that can delay the diagnosis of overdose. Symptoms of overdose in combination with opiates are similar. Carisoprodol (as with its metabolite meprobamate) is particularly dangerous in combination with alcohol.
Carisoprodol – Pharmacokinetics
After 30 minutes it already works, with the aforementioned effects lasting approximately two to six hours. It is metabolized in the liver via the cytochrome P450 oxidase isoenzyme CYP2C19, is excreted by the kidneys, and has a half-life of approximately eight hours. A considerable proportion of carisoprodol is metabolized to meprobamate, which is a known drug of abuse and dependence; this could explain the potential for abuse of carisoprodol (meprobamate levels reach higher peak plasma levels than carisoprodol itself after administration). Meprobamate is believed to play a significant role in the long half-life effects of carisoprodol and meprobamates on bioaccumulation after prolonged periods of carisoprodol administration.
Dr. Samantha Robson ( CRN: 0510146-5) is a nutritionist and website content reviewer related to her area of expertise. With a postgraduate degree in Nutrition from The University of Arizona, she is a specialist in Sports Nutrition from Oxford University and is also a member of the International Society of Sports Nutrition.