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    Carisoprodol molecular structure

    Carisoprodol Stats & Data

    Soma Rela Myolax Vanadom Carisoma
    NPS DataHub
    MW260.33
    FormulaC12H24N2O4
    CAS78-44-4
    IUPAC2-[(carbamoyloxy)methyl]-2-methylpentyl isopropylcarbamate
    SMILESCCCC(C)(COC(N)=O)COC(=O)NC(C)C
    InChIKeyOFZCIYFFPZCNJE-UHFFFAOYSA-N
    Chemical Class medicine
    Psychoactive Class Depressant
    Half-Life ~2 hours (carisoprodol); ~10 hours (meprobamate)

    Pharmacology

    DrugBank
    Protein binding Approximately 60% . State Solid

    Description

    Originally approved by the FDA in 1959 , carisoprodol is a centrally acting muscle relaxant used in painful musculoskeletal conditions in conjunction with physical therapy and other medications . This drug is available by itself in an oral tablet or combined with aspirin, or in a fixed-dose combination with both aspirin and codeine FDA label, F4060, F4069. In January 2012, this drug was classified as a Schedule IV substance under the controlled substances act in several US states due to alarming rates of abuse despite having a low potential for abuse in addition to a low risk of dependence .

    Mechanism of Action

    The mechanism of action of carisoprodol in relieving discomfort associated with acute painful musculoskeletal conditions has not been confirmed. In studies using animal models, the muscle relaxation that is induced by carisoprodol is associated with a change in the interneuronal activity of the spinal cord and of the descending reticular formation, located in the brain . The abuse potential of this drug is attributed to its ability to alter GABAA function . This drug has been shown to modulate a variety of GABAA receptor subunits . GABAA receptor modulation can lead to anxiolysis due to inhibitory effects on neurotransmission .

    Pharmacodynamics

    Carisoprodol is a centrally acting skeletal muscle relaxant that does not act directly on skeletal muscle but acts directly on the central nervous system (CNS). This drug relieves the painful effects of muscle spasm . A metabolite of carisoprodol, _meprobamate_, possesses both anxiolytic and sedative properties . Clinical studies have shown that this drug causes impairment of psychomotor performance in neuropsychological tests .

    Metabolism

    The main pathway of carisoprodol is liver metabolism is by the cytochrome enzyme CYP2C19 to form meprobamate. This enzyme exhibits genetic polymorphism, which may affect the metabolism of this drug .

    Absorption

    The absolute bioavailability of carisoprodol has not yet been established. The mean time to peak plasma concentrations (Tmax) of this drug was about 1.5-2 hours in clinical studies . Co-administration of a fatty meal with carisoprodol (350 mg tablet) had no impact on carisoprodol pharmacokinetics .

    Toxicity

    **LD50 values** The LD50 values of carisoprodol for rats are 450 mg/kg for intravenous (IV) and intraperitoneal injection, and 1,320 mg/kg for gavage dosing. In mice, the LD50 values are 165 mg/kg for intravenous injection, 980 mg/kg for intraperitoneal injection, and 2,340 mg/kg for gavage dosing. The LD50 value for rabbits given carisoprodol by intravenous injection is 124 mg/kg . **Overdose** An overdose of carisoprodol leads to CNS depression, and in severe cases, induction of a coma. Shock, depression of respiratory function, seizures and death have also been reported in rare cases. Several symptoms may be associated with carisoprodol overdose, such as 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. Alcohol or other CNS depressants or psychotropic agents can exert additive effects on carisoprodol even when one of the agents has been ingested at the normal, therapeutic dose. Fatal accidental and non-accidental overdoses have both been reported with carisoprodol ingestion alone or ingestion of carisoprodol in combination with alcohol or psychotropic drugs . **A note on dependence and withdrawal** In the postmarketing reports after carisoprodol use, cases of dependence, withdrawal, and abuse have been reported with long-term use.

    Indication

    Carisoprodol is indicated for the relief of discomfort related to acute, painful musculoskeletal conditions . **Important limitations of use** : • Should only be used for acute treatment periods up to two or three weeks • Adequate evidence of effectiveness for more prolonged use has not been established • Not recommended in pediatric patients less than 16 years of age

    Half-life

    The terminal half-life is approximately 2 hours .

    Elimination

    Carisoprodol is eliminated by the kidneys as well as other routes. The half-life of meprobamate is approximately 10 hours .

    Volume of Distribution

    0.93 to 1.3 L/kg, according to 4 different clinical studies .

    Clearance

    Following an oral dose of carisoprodol, the oral clearance (Cl/F) was 39.52 ± 16.83 L/hour .

    Receptor Profile

    Receptor Actions

    Agonists
    GABA-A receptor agonist (at high concentration)
    Inhibitors
    Adenosine reuptake inhibitor
    Modulators
    GABA-A receptor positive allosteric modulator
    Other
    Prodrug (metabolizes to meprobamate)

    Receptor Binding

    activator modulator
    Gamma-aminobutyric acid receptor subunit beta-2 modulator
    Gamma-aminobutyric acid receptor subunit gamma-2 modulator
    Gamma-aminobutyric acid receptor subunit alpha-5 modulator
    Gamma-aminobutyric acid receptor subunit alpha-3 modulator

    History & Culture

    1956–1959

    Frank M. Berger at Wallace Laboratories (later Carter-Wallace) synthesized carisoprodol in 1956. Berger had also been part of the team responsible for creating meprobamate, which had become a widely used pharmaceutical during the 1950s. The development of carisoprodol arose from ongoing efforts to create and test various meprobamate derivatives. The critical structural modification involved substituting one hydrogen atom with an isopropyl group on one of the carbamyl nitrogens, intended to produce a compound with distinct pharmacological properties. In June 1959, several American pharmacologists convened at Wayne State University in Detroit, Michigan to discuss the newly discovered structural analogue. Building upon meprobamate's established pharmacological effects, carisoprodol was designed to provide improved muscle relaxing properties while offering reduced addiction potential and a lower risk of overdose. The FDA approved the drug later that year. Early publications described it as exhibiting properties similar to both mephenesin and meprobamate, though its effect profile differed significantly from its parent compound, demonstrating stronger muscle relaxant and analgesic effects.

    1960–1978

    During the 1960s, animal research indicated that carisoprodol produced clear EEG changes without causing significant sedation at low doses. In this respect, researchers likened its profile to atropine. The prevailing discussion about the substance during this period suggested it possessed low abuse potential and minimal risk of physical dependence. This perception began to shift in 1978 when a report appeared demonstrating the drug's abuse potential, ultimately contributing to growing concern about its effects and marking the beginning of a reevaluation of its safety profile.

    1990–2008

    Following additional reports documenting physical dependence and recreational use during the 1990s, concerns about carisoprodol increased considerably. Research from this period revealed that only a small percentage of physicians understood carisoprodol's status as a prodrug of meprobamate, with most believing it carried a lower abuse risk than its metabolite. The DEA recommended federal scheduling in 1996, though the FDA opposed this action at the time due to insufficient evidence. Carisoprodol was designated as a "drug of concern" instead. By 1998, it ranked eighteenth out of 123 drugs involved in emergency department visits in the United States. Reports increasingly documented the drug being used to potentiate the effects of opioids, and sometimes benzodiazepines, cocaine, and alcohol. The practice of combining carisoprodol with opioids and benzodiazepines became colloquially known as "The Holy Trinity" due to the reported intensification of euphoric effects. The dangers of such combinations were illustrated by actress Dana Plato's death in 1999, which occurred after taking carisoprodol along with a hydrocodone and acetaminophen painkiller. In 2014, actress Skye McCole Bartusiak died from an overdose involving the combined effects of carisoprodol, hydrocodone, and difluoroethane. Even without federal scheduling, individual states began implementing their own controls. SAMHSA reported a doubling of nonmedical use between 2004 and 2008. The National Forensic Laboratory Information System listed carisoprodol among the top 25 most abused drugs in the United States in 2008, during which year approximately 10.5 million prescriptions were dispensed. The availability of carisoprodol through online sellers significantly contributed to this rise in nonmedical use.

    2007–2013

    Multiple countries began removing carisoprodol from the market or implementing stricter controls during this period. Sweden withdrew the drug from the market in November 2007 due to problems with dependence and adverse effects. Evidence from Norway demonstrating its addictive potential both as a prodrug of meprobamate and as a potentiator of opioids led to its removal from the Norwegian market in May 2008. The European Medicines Agency recommended member states suspend marketing authorization the same year. In January 2012, carisoprodol became a Schedule IV controlled substance in the United States following documented increases in misuse and adverse events. The scheduling decision noted that the drug possesses barbiturate-like effects in vitro, exhibits discriminative stimulus effects similar to other Schedule IV drugs such as barbital, meprobamate, and chlordiazepoxide, and that excessive use produces toxicity and withdrawal symptoms comparable to other controlled depressants. Indonesia removed carisoprodol from the market in September 2013 due to concerns about diversion, dependence, and adverse effects. Despite its removal, a tragic incident occurred in Kendari, Indonesia in September 2017 when pills containing a combination of paracetamol, caffeine, and carisoprodol were mixed into children's drinks at elementary and junior high schools, resulting in one death and 50 children suffering seizures.

    Tolerance & Pharmacokinetics

    drugs.wiki
    Half-Life
    ~2 hours (carisoprodol); ~10 hours (meprobamate)
    Addiction Potential
    Moderate to high. Carisoprodol has a risk of dependence and abuse, especially with prolonged use or at high doses. Its metabolite, meprobamate, is also habit-forming.

    Cross-Tolerances

    Meprobamate
    70% ●○○
    Other sedative‑hypnotics (e.g., benzodiazepines, barbiturates)
    30% ●○○

    Experience Report Analysis

    Erowid BlueLight
    57 Reports
    1995–2023 Date Range
    8 With Age Data
    20 Effects Detected

    Demographics

    Gender Distribution

    Age Distribution

    Reports Over Time

    Effect Analysis

    Erowid + Bluelight

    Effects aggregated from 72 experience reports (57 Erowid + 15 Bluelight)

    72 Reports
    60 Effects Detected
    25 Positive
    17 Adverse
    18 Neutral

    Effect Sentiment Distribution

    Confidence Distribution

    Positive Effects 25

    Sedation 36.1% 91%
    Euphoria 32.0% 88%
    Awe 20.0% 80%
    Contentment 20.0% 83%
    Mystical Quality 20.0% 85%
    Muscle Relaxation 20.0% 83%
    Stimulation 19.3% 70%
    Body High 15.2% 82%
    Anxiety Suppression 13.9% 80%
    Nostalgia 13.3% 80%
    Revelatory Insight 13.3% 85%
    Oneness 13.3% 80%
    Numbness 13.3% 88%
    Music Enhancement 12.3% 70%
    Focus Enhancement 12.3% 70%
    Introspection 11.1% 84%
    Empathy 10.5% 70%
    Tactile Enhancement 8.4% 80%
    Pain Relief 7.0% 90%
    Bliss 6.7% 90%

    Adverse Effects 17

    Ataxia 33.3% 85%
    Body Load 26.7% 76%
    Confusion 16.6% 82%
    Memory Suppression 14.0% 70%
    Vomiting 13.3% 92%
    Tremor 13.3% 82%
    Double Vision 13.3% 90%
    Nausea 12.5% 88%
    Motor Impairment 11.1% 90%
    Seizure 8.8% 70%
    Cold Flashes 6.7% 90%
    Focus Suppression 6.7% 75%
    Muscle Tension 6.7% 70%
    Unconsciousness 6.7% 95%
    Hypersomnia 6.7% 85%
    Emotional Release 6.7% 80%
    Communication Suppression 6.7% 80%

    Dose-Response Correlation

    How effect frequency changes across dose levels

    View data table
    Effect Strong (n=14) Heavy (n=17)
    Sedation 42.9% 41.2%
    Euphoria 42.9% 41.2%
    Stimulation 0% 41.2%
    Hospital 14.3% 35.3%
    Focus Enhancement 14.3% 23.5%
    Confusion 0% 23.5%
    Motor Impairment 0% 23.5%
    Anxiety Suppression 21.4% 17.6%
    Body High 21.4% 17.6%
    Nausea 14.3% 17.6%
    Memory Suppression 0% 17.6%
    Music Enhancement 0% 17.6%
    Visual Distortions 14.3% 11.8%
    Empathy 14.3% 11.8%
    Introspection 14.3% 0%

    Dose–Effect Mapping

    Experience Reports

    How reported effects shift across dose tiers, based on 57 experience reports.

    Limited tier coverage — most reports fall within the Strong / Heavy range. Effects at other dose levels may not be represented.

    Oral dose range: 700.0–1400.0 mg (median 700.0 mg)
    Effect Strong (n=14) Heavy (n=17)
    sedation
    43%
    41%
    euphoria
    43%
    41%
    stimulation
    41%
    hospital
    14%
    35%
    focus enhancement
    14%
    24%
    confusion
    24%
    motor impairment
    24%
    anxiety suppression
    21%
    18%
    body high
    21%
    18%
    nausea
    14%
    18%
    memory suppression
    18%
    music enhancement
    18%
    visual distortions
    14%
    12%
    empathy
    14%
    12%
    introspection
    14%
    auditory effects
    14%
    12%
    dissociation
    12%
    tactile enhancement
    12%
    color enhancement
    12%
    pain relief
    12%

    Risk Escalation

    Sentiment Analysis

    Average frequency of positive vs adverse effects across dose tiers

    Strong n=14
    5 positive 21.4% 2 adverse 17.9%
    Heavy n=17
    9 positive 20.9% 5 adverse 20.0%
    View effect breakdown

    Adverse Effects

    Effect Strong (n=14) Heavy (n=17) Change
    Confusion
    24%
    0%
    Motor Impairment
    24%
    0%
    Anxiety Suppression
    21%
    18%
    -17%
    Nausea
    14%
    18%
    +23%
    Memory Suppression
    18%
    0%

    Positive Effects

    Effect Strong (n=14) Heavy (n=17) Change
    Euphoria
    43%
    41%
    -3%
    Stimulation
    41%
    0%
    Focus Enhancement
    14%
    24%
    +64%
    Body High
    21%
    18%
    -17%
    Music Enhancement
    18%
    0%
    Empathy
    14%
    12%
    -17%
    Introspection
    14%
    0%
    Tactile Enhancement
    12%
    0%
    Color Enhancement
    12%
    0%
    Pain Relief
    12%
    0%

    Dosage Distribution

    Dose distribution from experience reports

    Median: 700.0 mg IQR: 700.0–1400.0 mg n=38

    Real-World Dose Distribution

    62K Doses

    From 91 individual dose entries

    Oral (n=67)

    Median: 700.0mg 25th: 600.0mg 75th: 1050.0mg 90th: 1400.0mg
    mg/kg median: 10.631 mg/kg 75th: 15.432

    Common Combinations

    Most co-occurring substances in experience reports

    Form / Preparation

    Most common forms and preparations reported

    Body-Weight Dosing

    Dose relative to body weight from reports with weight data

    Median: 12.181 mg/kg IQR: 9.079–18.519 mg/kg n=38

    Redose Patterns

    Redosing behavior across 46 reports

    19.6% Redosed
    1.2 Avg Doses
    10m Median Interval

    Legal Status

    Country Status Notes
    Australia No longer registered Removed from the Australian Register of Therapeutic Goods. Access is still possible through the Special Access Scheme for individual patient needs.
    Canada Schedule V Controlled Substance As of April 14, 2025, carisoprodol was removed from the Prescription Drug List and reclassified as a Schedule V Controlled Substance. No pharmaceutical forms are currently marketed in Canada.
    European Union Marketing authorization withdrawn The European Medicines Agency recommended member states suspend marketing authorization in 2008 due to concerns about dependence and insufficient benefit-risk profile for acute back pain treatment.
    Finland No longer available Carisoprodol is no longer available in Finland, including as a prescription medication. Previously marketed as Somadril.
    Germany Prescription only (Anlage 1 AMVV) Classified as a prescription medicine under Anlage 1 of the Arzneimittelverschreibungsverordnung (AMVV). Available only with a valid medical prescription.
    Indonesia Withdrawn from market Taken off the market in September 2013 due to concerns about diversion, dependence, and adverse effects.
    Mexico Available without prescription Sold over-the-counter, though typically in lower doses than those available in the United States. Commonly advertised in border cities.
    Norway Withdrawn from market Removed from the market in May 2008 following reports demonstrating addictive potential as a prodrug of meprobamate and as a potentiator of opioid medications including hydrocodone, oxycodone, and codeine.
    Spain Over-the-counter (unconfirmed) Reports indicate carisoprodol may be available without prescription, though this has not been officially confirmed.
    Sweden Withdrawn from market Taken off the market in November 2007 due to problems with dependence and side effects. The Swedish pharmaceutical regulatory agency determined that alternative medications offered comparable or better efficacy without the associated risks.
    Thailand Over-the-counter (unconfirmed) As of 2005, reported to be available without prescription in combination formulations with phenylbutazone or paracetamol. Status may have changed since then.
    United States Schedule IV Placed on Schedule IV of the Controlled Substances Act by DEA ruling in December 2011, effective January 2012. Classification followed rising rates of abuse and diversion. Requires a valid prescription for legal possession; unauthorized possession or distribution is a federal offense.

    Harm Reduction

    drugs.wiki

    Carisoprodol is a centrally acting muscle relaxant with sedative and anxiolytic properties, commonly prescribed for short‑term treatment of acute musculoskeletal pain. It is metabolized by CYP2C19 to meprobamate, a longer‑acting sedative‑anxiolytic; this can prolong impairment, especially with redosing or in poor CYP2C19 metabolizers, who can have markedly higher carisoprodol exposure and lower meprobamate exposure at the same dose. Because the parent half‑life (~2 h) is shorter than meprobamate (~10 h), stacking doses within a session increases cumulative CNS depression. Even at therapeutic doses, drowsiness and psychomotor impairment are common and have been linked to motor vehicle accidents; avoid driving or hazardous tasks until fully baseline. Polydrug use with CNS depressants (alcohol, opioids, benzodiazepines, barbiturates, GHB, Z‑drugs, gabapentinoids) can cause synergistic respiratory depression, coma, and death; numerous fatalities involve such combinations. Rare cases of serotonin syndrome have been reported; exercise caution if combining with serotonergic agents (SSRIs/SNRIs, tramadol, MAOIs). Label guidance limits use to 2–3 weeks and single doses of 250–350 mg up to 3–4 times daily; exceeding labeled single or daily doses substantially increases risk. The EU suspended carisoprodol marketing due to an unfavorable risk–benefit profile and abuse concerns; outside regulated supply chains, counterfeit or mis‑sold tablets are possible—some “pharmaceuticals” in illicit markets contain unexpected potent sedatives/opioids—so use drug checking where available and verify imprint/strength. Oral use is the intended route; community harm‑reduction forums report insufflation as unpleasant, irritant, and not more effective. Withdrawal after chronic/high‑dose use (often due to meprobamate accumulation) can be severe (anxiety, tremor, insomnia, hallucinations, seizures) and warrants medical supervision—do not abruptly stop after sustained heavy use. Avoid use in acute intermittent porphyria and in older adults (Beers criteria) when possible; use extra caution in hepatic or renal impairment. Combination products exist (e.g., with aspirin ± codeine); verify ingredients to avoid inadvertent opioid or NSAID exposure. Naloxone will not reverse carisoprodol/meprobamate effects, though it may reverse co‑ingested opioids; always prioritize airway and call emergency services in suspected overdose.

    References

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