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- Barbiturates
- Amobarbital
Amobarbital API Manufacturers & Suppliers
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Amobarbital | CAS No: 57-43-2 | GMP-certified suppliers
A medication that provides hypnotic, sedative, and anticonvulsant effects for central nervous system depression and seizure management in pharmaceutical formulations.
Therapeutic categories
Product Snapshot
- Amobarbital is available as injectable lyophilized powder and oral capsules
- It is primarily used in therapeutic settings requiring central nervous system depressant effects
- The product is approved for use in the US and Canada, with some formulations classified as illicit
Clinical Overview
The primary mechanism of action of amobarbital involves potentiation of gamma-aminobutyric acid type A (GABAA) receptor activity. Unlike GABA itself or benzodiazepines, amobarbital binds at distinct alpha or beta subunits of the GABAA receptor. This binding enhances the receptor's chloride channel function, resulting in decreased neuronal excitability through reduced input resistance and modulation of tonic and burst firing patterns. Additionally, amobarbital exerts inhibitory effects on AMPA-type glutamate receptors, which mediate excitatory neurotransmission. It also interacts with neuronal nicotinic acetylcholine receptors, contributing to its central nervous system (CNS) depressant effects.
Pharmacokinetic parameters including absorption, distribution, metabolism, and elimination are not specified here, but as with other barbiturates, hepatic metabolism—likely involving cytochrome P450 enzymes such as CYP3A4—is a significant pathway. Amobarbital can induce cytochrome P450 activity, which may affect the metabolism of concomitantly administered drugs.
Safety considerations with amobarbital focus on dose-dependent CNS depression, which can lead to sedation, respiratory depression, and coma in overdose. The risk of physical dependence and tolerance with prolonged use is high. Adverse effects largely result from CNS depressant activity. Careful monitoring and adherence to dosing guidelines are essential when handling this agent.
Amobarbital has been used clinically in some regions but is also subject to illicit use owing to its pharmacological effects. It is categorized among central nervous system depressants, hypnotics, anticonvulsants, and GABA modulators.
When sourcing amobarbital active pharmaceutical ingredient (API), quality control must ensure compliance with pharmacopeial standards, focusing on purity, absence of contaminants, and consistent pharmacological activity. Given its capacity to induce CYP enzymes, potential drug–drug interactions should also be considered during formulation and development. Regulatory status varies by country, requiring careful verification to ensure adherence to local legal and safety requirements.
Identification & chemistry
| Generic name | Amobarbital |
|---|---|
| Molecule type | Small molecule |
| CAS | 57-43-2 |
| UNII | GWH6IJ239E |
| DrugBank ID | DB01351 |
Pharmacology
| Summary | Amobarbital acts primarily as a positive allosteric modulator of GABAA receptors by binding to distinct sites on alpha and beta subunits, enhancing inhibitory neurotransmission through increased chloride channel conductance. Additionally, it inhibits excitatory signaling by antagonizing AMPA-type glutamate receptors and interacts with neuronal nicotinic acetylcholine receptors. These combined actions contribute to its central nervous system depressant effects. |
|---|---|
| Mechanism of action | Amobarbital (like all barbiturates) works by binding to the GABAA receptor at either the alpha or the beta sub unit. These are binding sites that are distinct from GABA itself and also distinct from the benzodiazepine binding site. Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. This GABAA receptor binding decreases input resistance, depresses burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increases both the amplitude and decay time of inhibitory postsynaptic currents. In addition to this GABA-ergic effect, barbiturates also block the AMPA receptor, a subtype of glutamate receptor. Glutamate is the principal excitatory neurotransmitter in the mammalian CNS. Amobarbital also appears to bind neuronal nicotinic acetylcholine receptors. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Gamma-aminobutyric acid receptor subunit alpha-1 | Humans | potentiator |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Humans | potentiator |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Humans | potentiator |
Formulation & handling
- Amobarbital is available for both oral and parenteral (intramuscular, intravenous) administration, with formulations including capsules and lyophilized injection powder.
- This small molecule compound has moderate water solubility and lipid partition coefficient, supporting its use in aqueous injectable and oral dosage forms.
- For oral dosing, administer on an empty stomach to enhance absorption; avoid concurrent alcohol use due to potential CNS depressant interaction.
Regulatory status
| Lifecycle | The API is currently under patent protection in the US, with exclusivity expected to expire in the near future, while in Canada, the patent has already expired, allowing for generic competition. Market activity reflects increasing generic availability and established therapeutic use in both regions. |
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| Markets | US, Canada |
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Supply Chain
| Supply chain summary | The supply landscape for Amobarbital involves multiple packagers operating primarily in the US and Canadian markets. Originator companies have established branded products such as Amytal Sodium across these regions. Patent expirations are not explicitly stated, but the presence of several generic packagers suggests existing generic competition. |
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Amobarbital 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.
