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Cyproheptadine | CAS No: 129-03-3 | GMP-certified suppliers
A medication that relieves diverse allergic symptoms and pruritus while supporting appetite stimulation and, in some markets, offering additional benefit for vascular headache management.
Therapeutic categories
Primary indications
- In the US, prescription cyproheptadine is indicated for the treatment of various allergic symptomatologies - including dermatographia, rhinitis, conjunctivitis, and urticaria - as well as adjunctive therapy in the management of anaphylaxis following treatment with epinephrine
- In Canada, cyproheptadine is available over-the-counter and is indicated for the treatment of pruritus and for appetite stimulation
- In Australia, cyproheptadine is additionally indicated for the treatment vascular headaches
Product Snapshot
- Cyproheptadine is an oral small‑molecule formulation available mainly as tablets, capsules, and syrups
- It is used for allergic symptom control, pruritus management, appetite stimulation, and certain vascular headache indications
- It is approved in the US and Canada for these uses
Clinical Overview
Pharmacologically, cyproheptadine is a competitive antagonist at histamine H1 and serotonin receptors, countering mediator-induced effects such as bronchoconstriction and vasodepression. Its anti-serotonergic activity is thought to contribute to both mitigation of anaphylaxis-related processes and appetite stimulation via actions within the hypothalamic appetite center.
Following oral administration, cyproheptadine is systemically absorbed, but detailed absorption kinetics, distribution characteristics, and elimination parameters are not fully defined in public domain references. It undergoes hepatic metabolism and involves UGT1A3 and UGT1A4 pathways. Cyproheptadine is classified as an OCT1 inhibitor and may interact with other centrally acting or anticholinergic agents.
Safety considerations include sedation, anticholinergic effects, and the potential to lower seizure threshold or contribute to QTc prolongation. Photosensitivity reactions have been reported. Caution is advised in populations sensitive to central nervous system depressants or in those with underlying cardiovascular or seizure disorders. Use in serotonin syndrome is off‑label and requires specialist oversight.
Cyproheptadine is marketed in various regions in tablet and syrup formulations; product branding varies by market. For API procurement, suppliers should provide validated impurity profiles, confirmation of stereochemical identity, and evidence of GMP-compliant manufacturing, with attention to photostability and contaminant controls relevant to dibenzocycloheptene derivatives.
Identification & chemistry
| Generic name | Cyproheptadine |
|---|---|
| Molecule type | Small molecule |
| CAS | 129-03-3 |
| UNII | 2YHB6175DO |
| DrugBank ID | DB00434 |
Pharmacology
| Summary | Cyproheptadine is a first‑generation antagonist of histamine H1 and multiple serotonin (5‑HT2 and 5‑HT7) receptors, with additional antimuscarinic activity. By competitively blocking histamine- and serotonin-mediated signaling, it reduces allergic responses and counteracts several serotonin-driven physiological effects. Antagonism of central serotonin pathways in the hypothalamus is associated with its appetite‑stimulating properties. |
|---|---|
| Mechanism of action | Cyproheptadine appears to exert its antihistamine and antiserotonin effects by competing with free histamine and serotonin for binding at their respective receptors.Antagonism of serotonin on the appetite center of the hypothalamus may account for cyproheptadine's ability to stimulate the appetite. |
| Pharmacodynamics | Cyproheptadine has been observed to antagonize several pharmacodynamic effects of serotonin in laboratory animals, including bronchoconstriction and vasodepression, and has demonstrated similar efficacy in antagonizing histamine-mediated effects.The reason for its efficacy in preventing anaphylactic shock has not been elucidated, but appears to be related to its anti-serotonergic effects. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Histamine H1 receptor | Humans | antagonist |
| 5-hydroxytryptamine receptor 2A | Humans | antagonist |
| 5-hydroxytryptamine receptor 2C | Humans | antagonist |
ADME / PK
| Absorption | A single study examining the difference in absorption of orally administered versus sublingually administered cyproheptadine in five healthy males demonstrated a mean C<sub>max</sub> of 30.0 mcg/L and 4.0 mcg/L, respectively, and a mean AUC of 209 mcg.h/L and 25 mcg.h/L, respectively.The T<sub>max</sub> of orally and sublingually administered cyproheptadine was 4 hours and 9.6 hours, respectively. |
|---|---|
| Metabolism | The principal metabolite found in human urine has been identified as a quaternary ammonium glucuronide conjugate of cyproheptadine. |
| Route of elimination | Approximately 2-20% of the radioactivity from an orally administered radio-labeled dose of cyproheptadine is excreted in the feces, of which approximately 34% is unchanged parent drug (less than 5.7% of the total dose).At least 40% of radioactivity is recovered in the urine. |
Formulation & handling
- Low aqueous solubility and high lipophilicity support conventional oral solid and liquid formulations but may require solubilizers or wetting agents for uniform dispersion.
- As a small‑molecule solid, it offers good chemical stability, with standard protection from moisture and light typically sufficient during handling and storage.
- Oral use is well established; sedative effects can be potentiated by alcohol, but no specific food‑related absorption issues are noted for formulation design.
Regulatory status
| Lifecycle | Patent protections in the US and Canada have lapsed or are nearing expiry, indicating a transition toward a mature competitive landscape. As generics expand in both markets, the API is positioned in a late‑lifecycle phase with stable but largely saturated demand. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Cyproheptadine was originally developed by a single originator company, with today’s supply dominated by numerous generic manufacturers and repackagers that handle distribution across the US and Canada. Branded products have limited global visibility, with current availability concentrated in North American markets. Patent expiry occurred long ago, and the large number of active generic suppliers indicates an established and mature competitive landscape. |
|---|
Safety
| Toxicity | Overdosage with cyproheptadine is likely to result in significant sedation - although paradoxical stimulation has been noted in pediatric patients - and anticholinergic adverse effects such as dry mouth and flushing.Most patients appear to recover without incident, as a review of cyproheptadine overdose cases in Hong Kong found the majority of patients had no or mild symptoms following intentional overdose. In the event of overdosage with cyproheptadine, prescribing information recommends the induction of vomiting (if it has not occurred spontaneously) using syrup of ipecac.Gastric lavage and activated charcoal may also be considered. Vasopressors may be used to treat hypotension and intravenous physostigmine salicylate may be considered for the treatment of significant CNS symptoms depending on the clinical picture. |
|---|
- High-dose exposure is associated with pronounced CNS depression or, less commonly in pediatric contexts, paradoxical CNS stimulation, alongside anticholinergic effects such as mucosal dryness and flushing
- Toxicity reports indicate generally mild clinical courses, but significant sedation and autonomic effects remain key concerns for bulk‑handling scenarios
- Compounds with strong anticholinergic and sedative profiles may require controls to limit inhalation or accidental ingestion during processing
Cyproheptadine is a type of Antihistamines
Antihistamines are a vital subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) widely used in the treatment of allergies and allergic reactions. These compounds work by blocking the action of histamines, which are responsible for triggering allergic symptoms such as itching, sneezing, runny nose, and watery eyes.
Antihistamines can be classified into two main categories: first-generation and second-generation antihistamines. First-generation antihistamines, such as diphenhydramine and chlorpheniramine, have been in use for several decades. They are effective in relieving allergy symptoms but are associated with drowsiness and other side effects due to their ability to cross the blood-brain barrier.
On the other hand, second-generation antihistamines, including cetirizine, loratadine, and fexofenadine, offer similar allergy relief with fewer sedative effects. These newer antihistamines are preferred for their improved safety profiles, making them suitable for use during the day without causing significant drowsiness.
Antihistamines are available in various forms, including tablets, capsules, syrups, and topical creams. They are extensively used to manage conditions such as hay fever, hives, allergic rhinitis, and insect bites. Moreover, antihistamines may also be combined with decongestants or other medications to provide relief from nasal congestion and sinus symptoms.
As pharmaceutical APIs, antihistamines are produced through meticulous synthesis and manufacturing processes, adhering to strict quality standards. These APIs serve as the active components in various branded and generic pharmaceutical formulations, making them crucial in the pharmaceutical industry's production of allergy medications.
In conclusion, antihistamines are a significant subcategory of pharmaceutical APIs widely used for alleviating allergy symptoms. Their classification into first- and second-generation antihistamines offers options based on efficacy and sedative effects. By blocking histamines, antihistamines provide relief from common allergic reactions, making them essential in the development of effective allergy medications.
Cyproheptadine (Antihistamines), classified under Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
Cyproheptadine API manufacturers & distributors
Compare qualified Cyproheptadine API suppliers worldwide. We currently have 7 companies offering Cyproheptadine 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 |
|---|---|---|---|---|---|
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| Aquatic Remedies Pvt Ltd | Producer | India | India | CoA | 35 products |
| Fleming Labs. | Producer | India | India | CoA, GMP, WC | 8 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Vamsi Labs | Producer | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS, USDMF, WHO-GMP | 29 products |
| Vasudha Pharma Chem Ltd. | Producer | India | India | CoA, GMP, MSDS, USDMF, WC | 37 products |
When sending a request, specify which Cyproheptadine 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 Cyproheptadine 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.
Frequently asked questions about Cyproheptadine API
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