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Zaleplon | CAS No: 151319-34-5 | GMP-certified suppliers
A medication that provides short-term treatment of adult insomnia by promoting rapid sleep initiation through central nervous system depressant effects.
Therapeutic categories
Primary indications
- For the treatment of short-term treatment of insomnia in adults
Product Snapshot
- Zaleplon is formulated as oral capsules, including gelatin-coated variants
- It is primarily indicated for the short-term treatment of insomnia in adults
- The product has regulatory approval in the US, EU, and Canada
Clinical Overview
Pharmacologically, zaleplon modulates the gamma-aminobutyric acid (GABA) neurotransmitter system by interacting with the GABA_A receptor complex, specifically binding to the benzodiazepine omega-1 (BZ1) receptor subtype located on the alpha subunit of the GABA_A receptor chloride ion channel. This selective binding enhances GABAergic inhibitory neurotransmission, resulting in sedative and hypnotic effects. Although structurally distinct from benzodiazepines, barbiturates, and other hypnotics, zaleplon shares some pharmacodynamic features with benzodiazepines, including anxiolytic, muscle relaxant, and anticonvulsant properties observed in animal models.
Zaleplon’s mechanism involves subunit-specific modulation of the GABA_BZD receptor macromolecular complex, potentiating chloride ion channel opening which facilitates neuronal hyperpolarization and CNS depression. It also enhances binding of t-butyl-bicyclophosphorothionate (TBPS), supporting its central nervous system inhibitory action.
Following oral administration, zaleplon is rapidly absorbed and extensively metabolized primarily by hepatic cytochrome P450 enzymes, notably CYP3A4, resulting in inactive metabolites. It is predominantly excreted renally. The rapid onset and short elimination half-life contribute to its clinical use for sleep initiation rather than maintenance.
Safety considerations include its classification as a Schedule IV controlled substance in the United States due to potential for dependence and abuse. Common adverse effects include dizziness and headache. Caution is advised regarding concomitant use with other CNS depressants and in populations with hepatic impairment.
Zaleplon is marketed globally under various proprietary names and is utilized mainly for short-term insomnia management. For API procurement, ensuring compliance with cGMP standards and confirming batch consistency in purity and potency are critical given its clinical indication and controlled substance status. Additionally, sourcing should prioritize suppliers with validated processes for minimizing impurities and adherence to regulatory requirements pertinent to sedative-hypnotic agents.
Identification & chemistry
| Generic name | Zaleplon |
|---|---|
| Molecule type | Small molecule |
| CAS | 151319-34-5 |
| UNII | S62U433RMH |
| DrugBank ID | DB00962 |
Pharmacology
| Summary | Zaleplon is a nonbenzodiazepine hypnotic that modulates the gamma-aminobutyric acid (GABA) receptor complex to exert sedative effects. It selectively targets the omega-1 (BZ1) receptor site on the GABA-A receptor alpha-1 subunit, enhancing GABAergic inhibitory neurotransmission. This mechanism facilitates its therapeutic use in the short-term management of insomnia. |
|---|---|
| Mechanism of action | Zaleplon exerts its action through subunit modulation of the GABA<sub>B</sub>Z receptor chloride channel macromolecular complex. Zaleplon also binds selectively to the brain omega-1 receptor located on the alpha subunit of the GABA-A/chloride ion channel receptor complex and potentiates t-butyl-bicyclophosphorothionate (TBPS) binding. |
| Pharmacodynamics | Zaleplon is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class and is indicated for the short-term treatment of insomnia. While Zaleplon is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABA<sub>B</sub>Z) receptor complex. Subunit modulation of the GABA<sub>B</sub>Z receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Zaleplon also binds selectively to the CNS GABA<sub>A</sub>-receptor chloride ionophore complex at benzodiazepine(BZ) omega-1 (BZ1, ο1) receptors. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Gamma-aminobutyric acid receptor subunit alpha-1 | Humans | potentiator |
ADME / PK
| Absorption | Absorption Zaleplon is rapidly and almost completely absorbed following oral administration. |
|---|---|
| Half-life | Approximately 1 hour |
| Protein binding | Approximately 60% (in vitro plasma protein binding). |
| Metabolism | Zaleplon is primarily metabolized by aldehyde oxidase. |
| Route of elimination | Zaleplon is metabolized primarily by the liver and undergoes significant presystemic metabolism. After oral administration, zaleplon is extensively metabolized, with less than 1% of the dose excreted unchanged in urine. Renal excretion of unchanged zaleplon accounts for less than 1% of the administered dose. |
| Volume of distribution | * 1.4 L/kg |
| Clearance | * 1 L/h/kg |
Formulation & handling
- Zaleplon is a small molecule intended for oral administration in capsule form.
- Due to its low water solubility and moderate logP, formulation strategies should consider enhancing bioavailability.
- Avoid co-administration with high-fat meals and alcohol to prevent reduced efficacy and increased CNS depression risk.
Regulatory status
| Lifecycle | The API is approaching patent expiry in key markets including the US, EU, and Canada, resulting in increased generic competition and greater market maturity across these regions. Product availability and regulatory approvals are well established in these markets. |
|---|
| Markets | US, EU, Canada |
|---|
Supply Chain
| Supply chain summary | Zaleplon is produced by multiple manufacturers, including original research companies and several generic pharmaceutical firms, indicating an established supply base with diverse manufacturing roles. The branded product, Sonata, has a global presence in markets such as the US, EU, and Canada. Patent expirations have led to existing generic competition, reflected in the broad range of generic manufacturers and packagers operating in these regions. |
|---|
Safety
| Toxicity | Side effects include abdominal pain, amnesia, dizziness, drowsiness, eye pain, headache, memory loss, menstrual pain, nausea, sleepiness, tingling, weakness |
|---|
- May cause central nervous system effects including dizziness, drowsiness, and headache
- Handle with appropriate exposure controls
- Reported adverse reactions include gastrointestinal symptoms such as nausea and abdominal pain
Zaleplon is a type of Benzodiazepine agonists
Benzodiazepine agonists are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that possess specific pharmacological properties similar to benzodiazepine drugs. These compounds are widely used in the medical field for their anxiolytic (anti-anxiety), sedative, hypnotic, muscle relaxant, and anticonvulsant effects. Benzodiazepine agonists work by binding to specific receptors in the central nervous system (CNS), known as benzodiazepine receptors. This interaction enhances the activity of gamma-aminobutyric acid (GABA), a neurotransmitter that inhibits neuronal activity, leading to a calming effect on the CNS.
These APIs find applications in various medical conditions, including anxiety disorders, insomnia, seizures, muscle spasms, and alcohol withdrawal symptoms. Some commonly prescribed benzodiazepine agonists include diazepam, lorazepam, alprazolam, and clonazepam.
Due to their widespread usage, benzodiazepine agonists undergo rigorous quality control and testing to ensure purity, potency, and safety. They are manufactured under strict pharmaceutical guidelines and regulations to meet the standards set by regulatory authorities.
It's important to note that benzodiazepine agonists should be used with caution due to the potential for dependence and abuse. They are typically prescribed for short-term use to minimize these risks.
In summary, benzodiazepine agonists are a class of pharmaceutical APIs that mimic the effects of benzodiazepine drugs, providing therapeutic benefits for anxiety, insomnia, seizures, and muscle spasms. They are crucial tools in medical treatment but require careful monitoring and responsible use to mitigate potential risks.
Zaleplon (Benzodiazepine agonists), classified under Anti-anxiety
The Anti-anxiety category in the pharmaceutical API (Active Pharmaceutical Ingredient) market refers to a group of substances specifically developed to alleviate symptoms associated with anxiety disorders. Anxiety disorders are mental health conditions characterized by excessive worry, fear, and unease that can significantly impact daily life.
Pharmaceutical APIs within the Anti-anxiety category work by modulating the activity of neurotransmitters in the brain, particularly gamma-aminobutyric acid (GABA). GABA is an inhibitory neurotransmitter that helps regulate the excitability of neurons. By enhancing GABA's inhibitory effects, these APIs promote a calming effect, reducing anxiety symptoms.
Common Anti-anxiety APIs include benzodiazepines, such as alprazolam, diazepam, and lorazepam. These substances act as central nervous system depressants, inducing sedation and relaxation. Other APIs in this category include selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), and certain antihistamines.
Pharmaceutical companies develop and manufacture Anti-anxiety APIs to meet the growing demand for effective anxiety treatment options. These APIs are typically used as the active ingredient in the production of various anti-anxiety medications, such as tablets, capsules, or liquid formulations.
The market for Anti-anxiety APIs is influenced by factors such as increasing awareness about mental health, rising prevalence of anxiety disorders, and the growing demand for personalized treatment options. Regulatory compliance, quality control, and safety are crucial considerations in the development and production of these APIs to ensure efficacy and minimize potential side effects.
Overall, Anti-anxiety APIs play a vital role in the pharmaceutical industry by providing effective solutions for individuals struggling with anxiety disorders, enhancing their quality of life, and promoting overall well-being.
Zaleplon API manufacturers & distributors
Compare qualified Zaleplon API suppliers worldwide. We currently have 4 companies offering Zaleplon API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| Centaur Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 40 products |
| Cipla | Producer | India | India | CoA, USDMF | 164 products |
| Gedeon Richter | Producer | Hungary | Hungary | CoA, GMP | 48 products |
| Medichem | Producer | Spain | Malta | CoA, GMP | 39 products |
When sending a request, specify which Zaleplon 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.).
Use the list above to find high-quality Zaleplon API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
