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- Secobarbital
Secobarbital API Manufacturers & Suppliers
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Secobarbital | CAS No: 76-73-3 | GMP-certified suppliers
A medication that provides short-term relief of intractable insomnia in barbiturate‑habituated patients and supports controlled sedation needs for selected short procedures.
Therapeutic categories
AdjuvantsAdjuvants, AnesthesiaAnticholinergic AgentsAnticonvulsantsBarbituratesBarbiturates, Plain
Generic name
Secobarbital
Molecule type
small molecule
CAS number
76-73-3
DrugBank ID
DB00418
Approval status
Approved drug, Vet_approved drug
ATC code
N05CB01
Primary indications
- For the Short-term treatment of intractable insomnia for patients habituated to barbiturates
Product Snapshot
- Oral small‑molecule barbiturate supplied as capsules
- Used for short‑term management of intractable insomnia in barbiturate‑habituated patients
- Approved in the US and Canada for human use, with additional veterinary approval
Clinical Overview
Secobarbital (CAS 76-73-3) is a barbituric acid derivative used as a short‑term hypnotic in patients with intractable insomnia who are already habituated to barbiturates. It has also been used for induction of anesthesia prior to other general anesthetic agents and for brief procedures involving minimal painful stimuli. Secobarbital is marketed in some regions under the names Seconal and Tuinal and is also known as quinalbarbitone in the United Kingdom.
Pharmacologically, secobarbital is a central nervous system depressant with sedative, hypnotic, and anticonvulsant properties, although it provides little analgesia. Use in the presence of pain may lead to paradoxical excitation. The compound belongs to the barbiturate class, characterized by substituted barbituric acid structures.
Its mechanism of action involves binding to a site on the GABAA receptor complex that is associated with the chloride ion channel. This interaction increases the duration of channel opening, thereby prolonging inhibitory neurotransmission in the thalamus and enhancing the effect of endogenous GABA. The result is dose‑dependent CNS depression ranging from sedation to hypnosis and anesthesia.
Absorption and distribution parameters are not uniformly reported, but like other barbiturates, secobarbital is expected to exhibit significant plasma protein binding and hepatic metabolism. It is known to induce multiple cytochrome P450 isoenzymes, including CYP1A2, CYP2C19, CYP2C8, CYP2C9, and CYP3A4, which may contribute to drug interactions. Renal excretion of metabolites is a primary elimination pathway.
Safety considerations include respiratory depression, impaired psychomotor performance, and risk of dependence. Tolerance and withdrawal phenomena are well documented for barbiturates. Caution is required in patients with hepatic impairment, respiratory disease, or concomitant CNS depressant use. Overdose can produce profound CNS and cardiovascular depression.
For API procurement, sourcing should focus on manufacturers with demonstrated control of barbiturate handling, validated impurity profiles, and compliance with relevant pharmacopoeial specifications to ensure consistent quality and regulatory suitability.
Pharmacologically, secobarbital is a central nervous system depressant with sedative, hypnotic, and anticonvulsant properties, although it provides little analgesia. Use in the presence of pain may lead to paradoxical excitation. The compound belongs to the barbiturate class, characterized by substituted barbituric acid structures.
Its mechanism of action involves binding to a site on the GABAA receptor complex that is associated with the chloride ion channel. This interaction increases the duration of channel opening, thereby prolonging inhibitory neurotransmission in the thalamus and enhancing the effect of endogenous GABA. The result is dose‑dependent CNS depression ranging from sedation to hypnosis and anesthesia.
Absorption and distribution parameters are not uniformly reported, but like other barbiturates, secobarbital is expected to exhibit significant plasma protein binding and hepatic metabolism. It is known to induce multiple cytochrome P450 isoenzymes, including CYP1A2, CYP2C19, CYP2C8, CYP2C9, and CYP3A4, which may contribute to drug interactions. Renal excretion of metabolites is a primary elimination pathway.
Safety considerations include respiratory depression, impaired psychomotor performance, and risk of dependence. Tolerance and withdrawal phenomena are well documented for barbiturates. Caution is required in patients with hepatic impairment, respiratory disease, or concomitant CNS depressant use. Overdose can produce profound CNS and cardiovascular depression.
For API procurement, sourcing should focus on manufacturers with demonstrated control of barbiturate handling, validated impurity profiles, and compliance with relevant pharmacopoeial specifications to ensure consistent quality and regulatory suitability.
Identification & chemistry
| Generic name | Secobarbital |
|---|---|
| Molecule type | Small molecule |
| CAS | 76-73-3 |
| UNII | 1P7H87IN75 |
| DrugBank ID | DB00418 |
Pharmacology
| Summary | Secobarbital is a barbiturate that enhances GABAergic inhibition by binding to a site on the GABA‑A receptor complex and increasing the duration of chloride channel opening. Its pharmacologic effect produces CNS depression relevant to short‑term use in patients with barbiturate‑habituated insomnia. Secondary interactions with nicotinic acetylcholine and glutamate receptor families contribute to its broader depressant and excitatory‑modulating profile. |
|---|---|
| Mechanism of action | Secobarbital 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 | Secobarbital, a barbiturate, is used for the induction of anesthesia prior to the use of other general anesthetic agents and for induction of anesthesia for short surgical, diagnostic, or therapeutic procedures associated with minimal painful stimuli. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation. |
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
| Route of elimination | Barbiturates are metabolized primarily by the hepatic microsomal enzyme system, and the metabolic products are excreted in the urine and, less commonly, in the feces. |
|---|
Formulation & handling
- Solid small‑molecule barbiturate suitable for oral capsule formulation, with moderate lipophilicity and low aqueous solubility requiring standard dissolution‑enhancing approaches if higher loads are needed.
- Absorption can be influenced by gastric contents, so formulations may need to account for altered uptake under fed versus fasted conditions.
- Light and moisture sensitivity typical of barbiturates should be considered during handling and storage to maintain solid‑state stability.
Regulatory status
| Lifecycle | Patent protections in the US and Canada have lapsed or are nearing completion, indicating a mature stage of market availability. Product presence in both markets suggests stable, established utilization typical of a post‑patent‑expiry lifecycle. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Secobarbital is an established barbiturate with numerous historical manufacturers and packagers, indicating a mature supply base rather than reliance on a single originator. Branded products such as Seconal and regional variants like Novo‑secobarb have been marketed in the US and Canada, but patent expiry long ago means these brands coexist with extensive generic production. The breadth of manufacturers suggests ongoing or longstanding generic competition in both markets. |
|---|
Safety
| Toxicity | Symptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, staggering, and in severe cases coma and death. |
|---|
High Level Warnings:
- Overdose is characterized by profound CNS depression, including impaired coordination, slowed cognition and speech, and progression to deep sedation or coma
- Severe toxicity may involve respiratory depression with shallow breathing and loss of motor control, posing risk of fatal outcomes
- Handling should account for its barbiturate-related depressant profile, with controls to prevent accidental exposure or high-dose accumulation
Secobarbital 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.
Frequently asked questions about Secobarbital API
Sourcing
What matters most when sourcing GMP-grade Secobarbital?
The key factors are compliance with US and Canadian GMP and controlled‑substance regulations, including verification of the supplier’s manufacturing and handling authorizations. Source only from manufacturers with documented GMP status and a traceable quality and audit history. Given the mature, multi‑manufacturer supply base, ensure batch documentation and change‑control practices are consistent across suppliers.
Which documents are typically required when sourcing Secobarbital API?
Request the core API documentation set: GMP (1 company), CoA (1 company). Confirm versions and validity dates match the destination market to avoid delays in qualification.
Which manufacturers are known to produce Secobarbital API?
Known or reported manufacturers for Secobarbital: . Evaluate their GMP history, scale, and regional coverage before requesting dossiers or allocating demand.
How can I request quotes for Secobarbital API from GMP suppliers?
Submit quote requests through the supplier listings with your specs and required documents (specifications, target volume, delivery timeline, and destination). Providing consistent details upfront speeds comparable offers and clarifies technical feasibility.
Is a GMP audit report available for Secobarbital manufacturers?
Audit reports may be requested for Secobarbital: 1 GMP audit report available. Confirm the scope and recency of any audit before relying on it for qualification decisions.
How many suppliers offer Secobarbital API on Pharmaoffer?
Reported supplier count for Secobarbital: 1 verified suppliers. Filter listings by certifications, regions, and delivery options to match your qualification plan.
Which countries are known to manufacture Secobarbital API?
Production countries reported for Secobarbital: Germany (1 producer). Knowing the manufacturing geography helps anticipate logistics lead times and import compliance needs.
Which certifications do suppliers of Secobarbital usually hold?
Common certifications for Secobarbital suppliers: GMP (1 company), CoA (1 company). Always verify issuing authorities and expiry dates when reviewing audit packages.
Technical
What is Secobarbital (CAS 76-73-3) used for?
Secobarbital is used as a short‑term hypnotic for severe or intractable insomnia in patients already accustomed to barbiturates. It is also employed for induction of anesthesia or for brief procedures requiring minimal analgesia.
Which therapeutic class does Secobarbital fall into?
Secobarbital belongs to the following therapeutic categories: Adjuvants, Adjuvants, Anesthesia, Anticholinergic Agents, Anticonvulsants, Barbiturates. This positioning helps teams compare alternative APIs, anticipate pharmacology expectations, and align early research priorities.
What conditions is Secobarbital mainly prescribed for?
The primary indications for Secobarbital: For the Short-term treatment of intractable insomnia for patients habituated to barbiturates. These use cases frame the target patient populations and help prioritize formulation and safety evaluations.
How does Secobarbital work?
Secobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
What should someone know about the safety or toxicity profile of Secobarbital?
Secobarbital produces dose‑dependent central nervous system depression, with risks that include impaired coordination, slowed cognition, and respiratory depression. Severe overdose can progress to deep sedation or coma with shallow breathing and loss of motor control, which may be fatal. Dependence, tolerance, and withdrawal are known concerns, and caution is required in individuals with hepatic or respiratory impairment or when combined with other CNS depressants. Handling should account for its barbiturate depressant profile to avoid accidental exposure or high‑dose accumulation.
What are important formulation and handling considerations for Secobarbital as an API?
Secobarbital’s low aqueous solubility and moderate lipophilicity may require dissolution‑enhancing strategies, such as suitable excipients or particle‑size optimization, especially at higher loadings in oral capsules. Absorption can vary with gastric contents, so formulations should consider fed–fasted differences. The API is sensitive to light and moisture, requiring protected handling and storage to maintain solid‑state stability. Metabolic clearance through hepatic microsomal enzymes does not directly affect formulation but underscores the need for consistent dose delivery.
Is Secobarbital a small molecule?
Secobarbital is classified as a small molecule. That classification shapes process design, impurity profiling, and analytical control strategies.
Are there special stability concerns for oral Secobarbital?
Oral Secobarbital is sensitive to light and moisture, so protection from these conditions is important to maintain solid‑state stability. Its low aqueous solubility can affect dissolution, and formulations may require standard approaches to ensure consistent release. Uptake can vary with gastric contents, so maintaining appropriate storage and administration conditions helps preserve expected performance.
Regulatory
Where is Secobarbital approved or in use globally?
Secobarbital is reported as approved in the following major regions: Canada, US. Understanding geographic coverage informs regulatory filings, supply planning, and risk assessments before escalating procurement.
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Secobarbital procurement?
Pharmaoffer's Smart Sourcing Service coordinates compliant suppliers, documentation, and competitive quotes for Secobarbital. It centralizes outreach, follow-ups, and document validation to shorten procurement timelines.
Is Secobarbital included in the PRO Data Insights coverage?
PRO Data Insights coverage for Secobarbital: . Use the dataset to benchmark suppliers and monitor regulatory activity where available.
Where can I access the API market report for Secobarbital?
Market report availability for Secobarbital: Report Available. The report highlights demand trends, pricing drivers, and supplier landscape insights for procurement planning.
