Cyproheptadine
Cyproheptadine (cyproheptadine) is a small molecule pharmaceutical. Cyproheptadine was first approved as Periactin on 1982-01-01. It is used to treat allergic rhinitis perennial, blepharospasm, cluster headache, dyskinesias, and nelson syndrome amongst others in the USA. The pharmaceutical is active against histamine H1 receptor. In addition, it is known to target alpha-1A adrenergic receptor, alpha-1B adrenergic receptor, 5-hydroxytryptamine receptor 7, 5-hydroxytryptamine receptor 6, and alpha-1D adrenergic receptor.
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Commercial
Therapeutic Areas
Trade Name
FDA
EMA
Cyproheptadine (discontinued: Cyproheptadine, Periactin)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Cyproheptadine hydrochloride
Tradename | Company | Number | Date | Products |
|---|---|---|---|---|
| PERIACTIN | Merck & Co | N-012649 DISCN | 1982-01-01 | 1 products, RLD |
| PERIACTIN | Merck & Co | N-013220 DISCN | 1982-01-01 | 1 products, RLD |
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FDA
EMA
Brand Name | Status | Last Update |
|---|---|---|
| cyproheptadine | ANDA | 2023-10-05 |
| cyproheptadine hydrochloride | ANDA | 2025-08-06 |
| cyproheptadine hydrochloride solution | ANDA | 2024-06-15 |
Indications
FDA
EMA
Agency Specific
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EMA
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Patent Expiration
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Clinical
Clinical Trials
97 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Allergic rhinitis | D065631 | — | J30.9 | — | — | 2 | 2 | 1 | 5 |
| Rhinitis | D012220 | EFO_0008521 | J31 | — | — | 2 | 2 | 1 | 5 |
| Allergic rhinitis perennial | D012221 | EFO_1001417 | J30.89 | — | — | — | 2 | 1 | 3 |
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Allergic rhinitis seasonal | D006255 | EFO_0003956 | J30 | — | — | 2 | — | 1 | 3 |
Indications Phases 2
No data
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Rheumatoid arthritis | D001172 | EFO_0000685 | M06.9 | 1 | — | — | — | — | 1 |
| Arthritis | D001168 | EFO_0005856 | M05-M14 | 1 | — | — | — | — | 1 |
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Cyproheptadine |
| INN | cyproheptadine |
| Description | Cyproheptadine is the product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia. It has a role as a H1-receptor antagonist, a serotonergic antagonist, an antipruritic drug, an anti-allergic agent and a gastrointestinal drug. It is a member of piperidines and a tertiary amine. |
| Classification | Small molecule |
| Drug class | — |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | CN1CCC(=C2c3ccccc3C=Cc3ccccc32)CC1 |
Identifiers
| PDB | — |
| CAS-ID | 129-03-3 |
| RxCUI | — |
| ChEMBL ID | CHEMBL516 |
| ChEBI ID | 4046 |
| PubChem CID | 2913 |
| DrugBank | DB00434 |
| UNII ID | 2YHB6175DO (ChemIDplus, GSRS) |
Target
Agency Approved
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Alternate
ADRA1D
ADRA1D
SETD7
SETD7
Organism
Homo sapiens
Gene name
ADRA1D
Gene synonyms
ADRA1A
NCBI Gene ID
Protein name
alpha-1D adrenergic receptor
Protein synonyms
adrenergic, alpha -1D-, receptor, adrenergic, alpha-1A-, receptor, Alpha-1A adrenergic receptor, Alpha-1D adrenoceptor, Alpha-1D adrenoreceptor, Alpha-adrenergic receptor 1a
Uniprot ID
Mouse ortholog
Adra1d (11550)
alpha-1D adrenergic receptor (P97714)
Variants
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Financial
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Estimated US medical usage
Cyproheptadine
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Trends
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Safety
Black-box Warning
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Adverse Events
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966 adverse events reported
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