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cyproheptadine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
histamine-H1 receptor antagonists, tricyclic compounds	765	129-03-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: periactin cyproheptadine cyproheptadine hydrochloride cycloheptadine periactinol cyproheptadine HCl	A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc. Molecular weight: 287.41 Formula: C21H21N CLOGP: 5.16 LIPINSKI: 1 HAC: 1 HDO: 0 TPSA: 3.24 ALOGS: -4.33 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

periactin
cyproheptadine
cyproheptadine hydrochloride
cycloheptadine
periactinol
cyproheptadine HCl

A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.

Molecular weight: 287.41
Formula: C21H21N
CLOGP: 5.16
LIPINSKI: 1
HAC: 1
HDO: 0
TPSA: 3.24
ALOGS: -4.33
ROTB: 0

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
12	mg	O

ADMET properties:

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Property	Value	Reference
S (Water solubility)	3.64 mg/mL	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.74 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Oct. 17, 1961	FDA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Infective pulmonary exacerbation of cystic fibrosis	205.49	18.65	57	4118	8760	63476087
Torus fracture	108.53	18.65	17	4158	144	63484703
Growth retardation	72.57	18.65	17	4158	1324	63483523
Immobile	47.56	18.65	17	4158	5926	63478921
Butterfly rash	43.74	18.65	12	4163	1761	63483086
Serotonin syndrome	38.99	18.65	24	4151	28658	63456189
Apallic syndrome	38.27	18.65	9	4166	712	63484135
Juvenile idiopathic arthritis	36.29	18.65	12	4163	3314	63481533
Agitation	34.99	18.65	30	4145	59727	63425120
Hospitalisation	33.05	18.65	34	4141	85047	63399800

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Infective pulmonary exacerbation of cystic fibrosis	183.99	21.50	53	3123	6748	34947007
Serotonin syndrome	159.45	21.50	62	3114	19871	34933884
Nasal polyps	74.33	21.50	21	3155	2482	34951273
Chronic sinusitis	71.68	21.50	20	3156	2259	34951496
Nasal congestion	46.80	21.50	28	3148	23029	34930726
Cystic fibrosis	45.13	21.50	13	3163	1645	34952110
Rhinorrhoea	44.03	21.50	28	3148	25640	34928115
Symptom masked	36.49	21.50	9	3167	628	34953127
Cystic fibrosis respiratory infection suppression	33.29	21.50	7	3169	238	34953517
Clonus	30.90	21.50	11	3165	2739	34951016

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Infective pulmonary exacerbation of cystic fibrosis	313.72	16.46	90	6320	12761	79725217
Serotonin syndrome	184.27	16.46	84	6326	44943	79693035
Torus fracture	68.34	16.46	11	6399	90	79737888
Nasal polyps	58.28	16.46	22	6388	7305	79730673
Cystic fibrosis	51.31	16.46	17	6393	3863	79734115
Growth retardation	44.65	16.46	13	6397	1930	79736048
Intentional overdose	43.64	16.46	48	6362	105912	79632066
Chronic sinusitis	43.05	16.46	21	6389	13005	79724973
Symptom masked	39.61	16.46	11	6399	1379	79736599
Hospitalisation	39.34	16.46	43	6367	94193	79643785

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	R06AX02	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:50857	anti-allergic drugs
CHEBI has role	CHEBI:55324	gastrointestinal drugs
CHEBI has role	CHEBI:59683	antipruritic drugs
MeSH PA	D018926	Anti-Allergic Agents
MeSH PA	D000982	Antipruritics
MeSH PA	D003879	Dermatologic Agents
MeSH PA	D005765	Gastrointestinal Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Dermatographic urticaria	indication	7632005	DOID:743
Allergic rhinitis	indication	61582004
Nasal discharge	indication	64531003
Nasal congestion	indication	68235000
Sneezing	indication	76067001
Urticaria	indication	126485001
Itching of skin	indication	418363000
Allergic conjunctivitis	indication	473460002	DOID:11204
Serotonin syndrome	off-label use	371089000
Muscle spasticity of spinal origin	off-label use	416830008

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.8	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	10.22	WOMBAT-PK	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	6.93	WOMBAT-PK
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	6.95	WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.98	DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		Ki	4.86	DRUG MATRIX
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN				WOMBAT-PK
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.39	CHEMBL
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	6.54	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	7.23	WOMBAT-PK
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	8.42	WOMBAT-PK

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External reference:

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ID	Source
C7H	PDB_CHEM_ID
001537	NDDF
004617	NDDF
104592	RXNORM
15352003	SNOMEDCT_US
2249	MMSL
26462003	SNOMEDCT_US
277	IUPHAR_LIGAND_ID
2913	PUBCHEM_CID
2YHB6175DO	UNII

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
CYPROHEPTADINE	HUMAN PRESCRIPTION DRUG LABEL	1	0121-0788	SYRUP	2 mg	ORAL	ANDA	21 sections
CYPROHEPTADINE	HUMAN PRESCRIPTION DRUG LABEL	1	0121-4788	SYRUP	2 mg	ORAL	ANDA	21 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1757	TABLET	4 mg	ORAL	ANDA	21 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1757	TABLET	4 mg	ORAL	ANDA	21 sections
CYPROHEPTADINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	0463-6080	TABLET	4 mg	ORAL	ANDA	11 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1949	SOLUTION	2 mg	ORAL	ANDA	19 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0527-1949	SOLUTION	2 mg	ORAL	ANDA	19 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	10135-638	TABLET	4 mg	ORAL	ANDA	21 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	10135-638	TABLET	4 mg	ORAL	ANDA	21 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	16571-805	TABLET	4 mg	ORAL	ANDA	13 sections

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