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- Barbiturates
- Butabarbital
Butabarbital API Manufacturers & Suppliers
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Butabarbital | CAS No: 125-40-6 | GMP-certified suppliers
A medication that provides short-term sedative and hypnotic effects for managing severe insomnia and pre-operative anxiety, with careful regulatory compliance required for controlled substance handling.
Therapeutic categories
Primary indications
- Butabarbital is indicated for use as a sedative or hypnotic
- Butabarbital should not be used to treat insomnia for longer than 2 weeks
Product Snapshot
- Butabarbital is available as an oral tablet and solution formulation
- It is primarily used as a sedative or hypnotic agent
- Butabarbital is approved for use in the US and Canada
Clinical Overview
Pharmacodynamically, butabarbital exerts its effects by potentiating gamma-aminobutyric acid type A (GABA-A) receptors, enhancing inhibitory neurotransmission through increased chloride ion influx, which leads to neuronal hyperpolarization and reduced excitability. Additionally, butabarbital inhibits neuronal acetylcholine receptors and kainate subtype glutamate receptors, further contributing to its sedative effects. The duration of action is approximately 6 to 8 hours, which is shorter than some other barbiturates, correlating with its relatively rapid onset.
Butabarbital’s pharmacokinetic profile includes metabolism primarily through hepatic pathways and renal excretion as a significant elimination route. The therapeutic index is broad; however, individual dose requirements can vary considerably, necessitating careful dose titration and patient monitoring.
Safety considerations include risks of respiratory depression, central nervous system depression, and potential for abuse and dependence, comparable to other barbiturates such as secobarbital. Complex behaviors, increased fall risk, and paradoxical reactions may occur, warranting patient counseling and caution in vulnerable populations. Its high abuse potential and availability of safer alternatives, such as benzodiazepines, have led to decreased clinical use in recent years.
Butabarbital is available under brand names such as Butisol but remains a controlled substance due to its abuse potential. When sourcing butabarbital API, ensuring compliance with regulatory standards for purity, stability, and controlled substance handling is critical. Verification of good manufacturing practice (GMP) certification and rigorous quality control testing are essential to support safe pharmaceutical formulation and regulatory approval pathways.
Identification & chemistry
| Generic name | Butabarbital |
|---|---|
| Molecule type | Small molecule |
| CAS | 125-40-6 |
| UNII | P0078O25A9 |
| DrugBank ID | DB00237 |
Pharmacology
| Summary | Butabarbital is an intermediate-acting barbiturate that produces sedation by potentiating GABA-A receptor activity, leading to increased chloride influx and neuronal hyperpolarization. It concurrently inhibits neuronal acetylcholine and kainate subtype glutamate receptors, contributing to decreased neuronal excitability. These combined pharmacodynamic effects underlie its therapeutic use as a sedative or hypnotic agent. |
|---|---|
| Mechanism of action | Barbiturates like butabarbital potentiate GABA-A receptors and inhibit receptors for neuronal acetylcholine, and kainate. GABA-A receptors are predominantly on the post-synaptic membrane, and upon activation, open chloride channels to hyperpolarize the neuron and decreased firing rate. Potentiation of GABAergic neurons produces sedation. Inhibition of neuronal acetylcholine receptors and glutamate receptors of the kainate subtype desensitize their respective neurons, producing sedation. |
| Pharmacodynamics | Butabarbital potentiates GABAergic neurons while inhibiting neuronal acetylcholine and glutamate receptors to produce sedation. Butabarbital is an intermediate acting barbiturate with a duration of action of approximately 6-8 hours. The therapeutic index is quite wide as doses vary considerably from patient to patient. Patients should be counselled regarding the risk of worsening insomnia, drowsiness, falls, and complex behaviour while not fully awake. |
Targets
| Target | Organism | Actions |
|---|---|---|
| GABA(A) Receptor | Humans | positive allosteric modulator |
| Neuronal Acetylcholine (nACh) Receptor Subunits | Humans | inhibitor |
| Glutamate receptor 1 | Humans | antagonist |
ADME / PK
| Half-life | Butabarbital has a half life of 100 hours but its duration of action is only 6-8 hours. |
|---|---|
| Protein binding | Data regarding the protein binding of butbarbital is not readily available. However, barbiturates generally bind to serum albumin. |
| Metabolism | Data regarding the metabolism of butabarbital in humans are not readily available. In dogs, butabarbital undergoes metabolism to a final glucuronide metabolite. |
| Route of elimination | Barbiturates such as butabarbital are predominantly eliminated in the urine. In dogs, 3-5% of the dose is eliminated in the urine as the unchanged parent compound. |
Formulation & handling
- Butabarbital is a small molecule barbituric acid derivative intended for oral administration in both solution and tablet forms.
- It exhibits moderate water solubility and a LogP of 1.45, supporting formulation as conventional oral solid and liquid dosage forms.
- Avoid coadministration with alcohol due to potential for enhanced central nervous system depression; no specific food sensitivities reported.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient's patent protection has expired in the US and Canada, allowing for generic competition and indicating a mature market phase. Products containing this API are widely available across both markets. |
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| Markets | US, Canada |
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Supply Chain
| Supply chain summary | Butabarbital has multiple originator and generic manufacturers involved in its production, including established pharmaceutical companies with global operations. The product is primarily marketed in the US and Canadian markets, with branded formulations such as Butisol Sodium available. Patent expiries have allowed for existing generic competition, reflected by the presence of numerous manufacturers and generic equivalents. |
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Safety
| Toxicity | Patients experiencing an overdose may present with unsteady gait, slurred speech, nystagmus, confusion, poor judgement, irritability, and insomnia. Acute overdoses may present as CNS depression, respiratory depression, oligouria, tachycardia, hypotension, low body temperature, coma, and shock. An extreme overdose can lead to a flat EEG, resembling death, that is reversible provided there is no hypoxic brain damage. Overdose can be treated with symptomatic and supportive treatment. |
|---|
- Handle with care to prevent accidental overdose due to CNS and respiratory depressant effects
- Avoid exposure scenarios that may lead to systemic toxicity manifesting as hypotension, tachycardia, or shock
- Use appropriate protective measures to minimize risks of central nervous system adverse effects including confusion and impaired coordination
Butabarbital 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.
