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Carisoprodol | CAS No: 78-44-4 | GMP-certified suppliers
A medication that provides short-term relief of discomfort from acute, painful musculoskeletal conditions through centrally mediated muscle relaxation.
Therapeutic categories
Primary indications
- 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
Product Snapshot
- Carisoprodol is an oral small molecule available in multiple tablet and capsule formulations
- It is primarily used for the relief of discomfort associated with acute, painful musculoskeletal conditions
- Carisoprodol is approved for use in the US and Canada
Clinical Overview
Pharmacodynamically, carisoprodol exerts its effects through central nervous system mechanisms rather than direct action on skeletal muscle. It alleviates muscle spasm-related pain by modulating interneuronal activity in the spinal cord and descending reticular formation in the brain. The precise mechanism responsible for its muscle relaxant properties has not been fully elucidated. Carisoprodol is metabolized in the liver to meprobamate, a compound with documented anxiolytic and sedative effects, contributing to the overall pharmacological profile.
Carisoprodol is classified within the carbamate ester chemical family, and functions as a substrate of cytochrome P450 enzymes, including CYP2C19. Its metabolism is characterized by hepatic biotransformation, with considerations for drug interactions involving CYP450 pathways.
Safety considerations include psychomotor impairment and central nervous system depression. Due to reports of abuse and dependence, several U.S. states have classified carisoprodol as a Schedule IV controlled substance since 2012, although its overall abuse potential is regarded as low. The abuse liability is linked to modulation of GABAA receptor subunits, which can produce anxiolytic effects.
When sourcing carisoprodol API, manufacturers should ensure compliance with regulatory standards for controlled substances and consistency in purity and impurity profiles. Characterization of the carbamate ester structure and control of potential contaminants are critical for quality assurance, especially given the compound’s CNS activity and regulatory status.
Identification & chemistry
| Generic name | Carisoprodol |
|---|---|
| Molecule type | Small molecule |
| CAS | 78-44-4 |
| UNII | 21925K482H |
| DrugBank ID | DB00395 |
Pharmacology
| Summary | Carisoprodol is a centrally acting skeletal muscle relaxant indicated for the relief of discomfort associated with acute musculoskeletal conditions. Its pharmacologic effects are linked to modulation of GABAA receptor subunits, altering inhibitory neurotransmission in the central nervous system. The muscle relaxation observed is associated with changes in spinal cord and brain interneuronal activity, while its metabolite meprobamate contributes anxiolytic and sedative properties. |
|---|---|
| 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.[A176062, A176068] 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 [A176101, F4093]. 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.[A176062, A176095] |
Targets
| Target | Organism | Actions |
|---|---|---|
| Gamma-aminobutyric acid receptor subunit alpha-1 | Humans | activator, modulator |
| Gamma-aminobutyric acid receptor subunit beta-2 | Humans | modulator |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Humans |
ADME / PK
| 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. |
|---|---|
| Half-life | The terminal half-life is approximately 2 hours. |
| Protein binding | Approximately 60% . |
| 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. |
| Route of 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 . |
Formulation & handling
- Carisoprodol is a small molecule administered exclusively via oral routes in tablet or capsule forms.
- The absorption of Carisoprodol is not affected by food intake, allowing flexible dosing with or without meals.
- Handle as a solid with moderate aqueous solubility and consider avoiding concomitant use with alcohol due to interaction potential.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is currently marketed in the US and Canada, with patent protections expiring in the near term, indicating transition toward increased generic competition and market maturity. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Carisoprodol is manufactured by multiple companies, including both originator and generic pharmaceutical firms, indicating a competitive supply landscape. Its branded products are primarily present in the US and Canadian markets. Given the wide range of manufacturers and no recent mention of patent-protected exclusivity, generic competition is established and ongoing. |
|---|
Safety
| 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. The majority of dependence and withdrawal cases, as well as abuse, have occurred in patients with a history of addiction or who have used this drug in combination with other drugs having abuse potential. However, multiple post-marketing adverse event reports have been made of carisodopril-associated abuse when used without other drugs possessing abuse potential. Withdrawal symptoms have been observed and reported following sudden abrupt cessation after long-term carisodoprol use. To reduce the chance of carisodopril dependence, withdrawal, or abuse, carisodopril should be used with caution in addiction-prone patients and in patients taking other CNS depressants including alcohol. This drug should not be taken for longer than 2 to 3 weeks for symptomatic relief of acute musculoskeletal discomfort. **Use in pregnancy** This drug has been classified as Pregnancy Category C. There are no clinical trial data on the use of carisoprodol during human pregnancy. Animal studies show that carisoprodol crosses the placenta and leads to adverse effects on fetal growth and postnatal survival. In postmarketing reports, the main metabolite, _meprobamate_, has not demonstrated a consistent association between maternal use and an increased risk for specific congenital malformations. **Use in nursing** Limited data in humans demonstrate that this is found excreted in breast milk and may reach concentrations in breast milk of 2-4 times the maternal plasma concentrations. It is therefore advisable to exercise caution when this drug is used during breastfeeding. |
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- Carisoprodol exhibits acute toxicity, with intravenous LD50 values ranging from 124 mg/kg in rabbits to 450 mg/kg in rats, indicating potential for serious toxic effects at high exposure levels
- Overdose may result in central nervous system depression, respiratory failure, seizures, and death, with additive toxicity observed when combined with alcohol or other CNS depressants
- Prolonged exposure has been associated with dependence, withdrawal symptoms, and abuse potential, particularly in patients with a history of addiction or concomitant CNS depressant use
Carisoprodol is a type of Muscle relaxants
Muscle relaxants are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) commonly used to alleviate muscle spasms and promote muscle relaxation. These medications act on the central nervous system (CNS) or directly on muscle fibers to reduce muscle tone and tension.
Muscle relaxants can be classified into two main groups: spasmolytics and neuromuscular blockers. Spasmolytics primarily target the CNS to inhibit the transmission of nerve signals, thus reducing muscle spasms. They are often prescribed for conditions such as back pain, muscle strains, and spasms caused by neurological disorders.
Neuromuscular blockers, on the other hand, act at the neuromuscular junction to prevent the transmission of nerve impulses, resulting in temporary paralysis of skeletal muscles. These medications are primarily used during surgical procedures to induce muscle relaxation and facilitate intubation.
Commonly prescribed muscle relaxants include benzodiazepines, such as diazepam and lorazepam, which have sedative properties and can provide relief from muscle spasms. Another class of muscle relaxants is the centrally acting skeletal muscle relaxants, including carisoprodol and cyclobenzaprine, which work by affecting neurotransmitters in the CNS.
It is important to note that muscle relaxants can cause side effects such as drowsiness, dizziness, and impaired coordination. They should only be used under the guidance of a healthcare professional, and the dosage and duration of treatment should be strictly followed to avoid dependence or other complications.
In conclusion, muscle relaxants are pharmaceutical APIs used to alleviate muscle spasms and promote muscle relaxation. They are available in different forms and can target the CNS or directly act on muscle fibers. It is crucial to consult a healthcare professional for proper diagnosis, prescription, and monitoring when using muscle relaxants.
Carisoprodol (Muscle relaxants), classified under Skeletal muscle relaxants
Skeletal muscle relaxants are a category of pharmaceutical active pharmaceutical ingredients (APIs) that are commonly used in the treatment of musculoskeletal conditions characterized by muscle spasms, stiffness, or tension. These medications work by targeting the central nervous system to reduce muscle activity and promote relaxation.
Skeletal muscle relaxants act on various receptors in the central nervous system, such as gamma-aminobutyric acid (GABA) receptors, to inhibit the transmission of nerve impulses and decrease muscle tone. This results in a reduction in muscle spasms, pain relief, and improved mobility.
There are different classes of skeletal muscle relaxants, including benzodiazepines, antispasmodics, and centrally acting muscle relaxants. Benzodiazepines, such as diazepam and lorazepam, exert their muscle relaxant effects by enhancing the activity of GABA receptors. Antispasmodics like cyclobenzaprine work by inhibiting the release of certain neurotransmitters involved in muscle contractions. Centrally acting muscle relaxants, such as baclofen and tizanidine, directly target the spinal cord to reduce muscle hyperactivity.
Skeletal muscle relaxants are commonly prescribed for conditions like muscle spasms, back pain, fibromyalgia, and multiple sclerosis. However, they are typically used for short-term treatment due to their potential side effects, including drowsiness, dizziness, and sedation.
It is important to note that skeletal muscle relaxants should only be used under the supervision and prescription of a qualified healthcare professional. Proper dosage and duration of treatment should be determined based on the patient's condition and medical history to ensure safe and effective use of these medications.
Carisoprodol API manufacturers & distributors
Compare qualified Carisoprodol API suppliers worldwide. We currently have 7 companies offering Carisoprodol API, with manufacturing taking place in 1 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Aquatic Remedies Pvt Ltd | Producer | India | India | CoA | 35 products |
| Fleming Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 8 products |
| Harman Finochem | Producer | India | India | CoA, FDA, GMP, USDMF, WC | 34 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Tresinde Biotech | Producer | India | India | CoA, GMP | 50 products |
| Verdant Life Sciences | Producer | India | India | CoA, WC | 5 products |
When sending a request, specify which Carisoprodol API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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