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- Methylphenobarbital
Methylphenobarbital API Manufacturers & Suppliers
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Methylphenobarbital | CAS No: 115-38-8 | GMP-certified suppliers
A medication that provides relief from anxiety and tension and serves as an anticonvulsant for managing epilepsy in central nervous system disorders.
Therapeutic categories
Primary indications
- For the relief of anxiety, tension, and apprehension, also used as an anticonvulsant for the treatment of epilepsy
Product Snapshot
- Methylphenobarbital is formulated as an oral tablet small molecule API
- It is primarily indicated for the management of anxiety, tension, and used as an anticonvulsant in epilepsy treatment
- The product is FDA approved for the US pharmaceutical market
Clinical Overview
Clinically, methylphenobarbital has been used for the relief of anxiety, tension, and apprehension, as well as for the management of epilepsy. It is also utilized in combination formulations with agents such as acetaminophen, aspirin, and caffeine for the treatment of tension headaches, migraines, and associated pain, where its sedative and muscle relaxant properties contribute to symptom control.
Pharmacodynamically, methylphenobarbital exerts CNS depressant effects by modulating gamma-aminobutyric acid type A (GABA_A) receptors. It binds to a specific site associated with a chloride ionophore on the receptor complex, enhancing the duration of chloride channel opening. This results in potentiation of the inhibitory neurotransmitter GABA’s effect, particularly in the thalamus, leading to decreased neuronal excitability. Barbiturates produce a spectrum of CNS effects ranging from mild sedation to anesthesia at sufficiently high doses.
Pharmacokinetic data indicate that methylphenobarbital undergoes biotransformation primarily to phenobarbital, which contributes significantly to its anticonvulsant activity. It is a substrate and inducer of multiple cytochrome P450 enzymes, including CYP2B6, CYP2C19, and members of the CYP3A family, which has implications for drug–drug interactions.
Safety and toxicity profiles align with those of barbiturates; risks include CNS depression, respiratory depression, dependence, and withdrawal phenomena. There is limited evidence supporting any clinical advantage of methylphenobarbital over phenobarbital, which remains the more commonly used agent.
For API procurement, quality considerations include verification of identity and purity to meet pharmacopeial standards. Due to its metabolism and enzyme induction potential, consistency in impurity profile and assay is critical. Suppliers should provide detailed analytical documentation, including data on residual solvents and possible degradation products, to ensure compliance with regulatory requirements globally.
Identification & chemistry
| Generic name | Methylphenobarbital |
|---|---|
| Molecule type | Small molecule |
| CAS | 115-38-8 |
| UNII | 5NC67NU76B |
| DrugBank ID | DB00849 |
Pharmacology
| Summary | Methylphenobarbital acts as a central nervous system depressant primarily by binding to a distinct site on the GABA A receptor chloride ion channel, prolonging channel opening and enhancing GABAergic inhibitory neurotransmission. This mechanism produces sedative, anxiolytic, and anticonvulsant effects, targeting multiple GABA A receptor subunits and other neuronal receptors. It is utilized therapeutically for anxiety relief and seizure control. |
|---|---|
| Mechanism of action | Methylphenobarbital binds at a distinct binding site associated with a Cl<sup>-</sup> ionopore at the GABA<sub>A</sub> receptor, increasing the duration of time for which the Cl<sup>-</sup> ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. |
| Pharmacodynamics | Methylphenobarbital, a barbiturate, is used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain. Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. In sufficiently high therapeutic doses, barbiturates induce anesthesia. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Gamma-aminobutyric acid receptor subunit alpha-2 | Humans | potentiator |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Humans | potentiator |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Humans | potentiator |
ADME / PK
| Absorption | Approximately 50% of an oral dose of mephobarbital is absorbed from the gastrointestinal tract. |
|---|---|
| Half-life | 34 (range 11-67) hours |
| Protein binding | 70-76% |
| Metabolism | Hepatic, primarily by the hepatic microsomal enzyme system. About 75% of a single oral dose of mephobarbital is metabolized to phenobarbital in 24 hours. |
Formulation & handling
- Methylphenobarbital is a small molecule barbiturate intended for oral administration in tablet form. Its moderate water solubility and LogP indicate potential for reasonable oral bioavailability but may require consideration during formulation for consistent dissolution. Stability considerations are typical for solid oral dosage forms; protect from moisture to maintain integrity.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is currently marketed in the US with patent protection set to expire in , after which generic competition is expected to increase, indicating a mature market phase. |
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| Markets | US |
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Supply Chain
| Supply chain summary | Methylphenobarbital is supplied in the US market with multiple brand names derived from a limited number of originator companies involved in manufacturing and packaging. The presence of several packagers suggests established branded distribution channels predominantly in the US, with no indication of a broader global branded presence. Patent expirations have likely allowed for existing generic competition within the market. |
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Methylphenobarbital is a type of Barbiturates
Barbiturates are a category of pharmaceutical active pharmaceutical ingredients (APIs) that have sedative, hypnotic, and anticonvulsant properties. They belong to the class of drugs called depressants, which slow down the central nervous system (CNS) activity. Barbiturates have been widely used in the medical field for their ability to induce sleep, reduce anxiety, and control seizures.
The mechanism of action of barbiturates involves enhancing the effects of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) in the brain. GABA inhibits the transmission of signals between nerve cells, leading to relaxation and sedation. Barbiturates bind to specific GABA receptors, increasing the inhibitory effects of GABA and resulting in a calming effect on the CNS.
In the past, barbiturates were commonly prescribed for insomnia, anxiety disorders, and epilepsy. However, their use has decreased significantly due to the emergence of safer and more effective alternatives with fewer side effects. Nonetheless, barbiturates are still utilized in certain medical situations, such as anesthesia induction, emergency seizure control, and in some cases of refractory epilepsy.
Despite their therapeutic benefits, barbiturates carry potential risks and side effects. They can cause drowsiness, impaired coordination, and dependence when used for extended periods. Overdose of barbiturates can be life-threatening, leading to respiratory depression and coma.
In conclusion, barbiturates are a class of API widely known for their sedative, hypnotic, and anticonvulsant properties. While their use has diminished over time, they remain important in specific medical contexts. Proper caution and medical supervision are crucial when using barbiturates to ensure safety and efficacy.
