All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Drug dosage:

Dose	Unit	Route
12	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	3.64 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	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

Approvals:

Date	Agency	Company	Orphan
Oct. 17, 1961	FDA

FDA Adverse Event Reporting System (Female)

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	196.53	20.26	53	3061	7856	50594154
Torus fracture	105.06	20.26	16	3098	119	50601891
Growth retardation	71.88	20.26	16	3098	1062	50600948
Immobile	51.38	20.26	17	3097	5037	50596973
Apallic syndrome	40.04	20.26	9	3105	624	50601386
Bone density decreased	35.22	20.26	16	3098	11059	50590951
Juvenile idiopathic arthritis	34.61	20.26	11	3103	2868	50599142
Serotonin syndrome	33.11	20.26	20	3094	24693	50577317
Malnutrition	32.55	20.26	16	3098	13173	50588837
Hospitalisation	31.45	20.26	29	3085	67908	50534102
Hallucination, tactile	30.48	20.26	6	3108	218	50601792
Joint destruction	27.51	20.26	10	3104	3906	50598104
Delirium	27.40	20.26	21	3093	38171	50563839
Cardiogenic shock	27.23	20.26	15	3099	15584	50586426
Intentional overdose	23.86	20.26	24	3090	62480	50539530
Mydriasis	23.59	20.26	12	3102	10615	50591395
Psychomotor hyperactivity	22.11	20.26	11	3103	9290	50592720
Mental status changes	21.85	20.26	18	3096	36254	50565756
Atrial tachycardia	20.98	20.26	7	3107	2125	50599885
Sinus tachycardia	20.46	20.26	14	3100	21340	50580670

FDA Adverse Event Reporting System (Male)

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
Serotonin syndrome	158.32	22.27	58	2380	17454	29554635
Infective pulmonary exacerbation of cystic fibrosis	157.17	22.27	45	2393	6191	29565898
Cystic fibrosis	43.12	22.27	12	2426	1480	29570609
Symptom masked	38.63	22.27	9	2429	544	29571545
Cystic fibrosis respiratory infection suppression	28.84	22.27	6	2432	214	29571875
Nasal polyps	28.27	22.27	9	2429	1760	29570329
Intentional overdose	27.80	22.27	24	2414	38504	29533585
Obsessive-compulsive symptom	27.26	22.27	5	2433	91	29571998
Pneumonia aspiration	24.73	22.27	22	2416	36715	29535374
Chronic sinusitis	24.46	22.27	8	2430	1703	29570386

FDA Adverse Event Reporting System (Geriatric)

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	293.46	17.51	83	4876	11713	64482060
Serotonin syndrome	172.69	17.51	76	4883	39206	64454567
Torus fracture	63.71	17.51	10	4949	72	64493701
Intentional overdose	52.08	17.51	48	4911	89896	64403877
Cystic fibrosis	49.96	17.51	16	4943	3418	64490355
Growth retardation	48.04	17.51	13	4946	1548	64492225
Symptom masked	41.66	17.51	11	4948	1193	64492580
Hospitalisation	41.34	17.51	39	4920	75168	64418605
Apallic syndrome	35.31	17.51	9	4950	850	64492923
Pulmonary function test decreased	33.26	17.51	14	4945	6447	64487326
Suicide attempt	31.91	17.51	33	4926	70974	64422799
Malnutrition	31.12	17.51	19	4940	19106	64474667
Juvenile idiopathic arthritis	29.00	17.51	11	4948	3868	64489905
Electrocardiogram QT prolonged	27.17	17.51	32	4927	79416	64414357
Obsessive-compulsive disorder	26.68	17.51	11	4948	4807	64488966
Nasal polyps	26.08	17.51	10	4949	3619	64490154
Joint destruction	26.06	17.51	10	4949	3626	64490147
Obsessive-compulsive symptom	25.58	17.51	5	4954	139	64493634
Hallucination, tactile	24.55	17.51	6	4953	477	64493296
Immobile	24.33	17.51	11	4948	6004	64487769
Pneumonia aspiration	23.88	17.51	26	4933	59245	64434528
Atypical mycobacterial lower respiratory tract infection	22.94	17.51	4	4955	58	64493715
Delirium	22.23	17.51	27	4932	69167	64424606
Cystic fibrosis respiratory infection suppression	20.35	17.51	5	4954	406	64493367
Mydriasis	19.41	17.51	13	4946	15299	64478474
Mental status changes	18.25	17.51	23	4936	61139	64432634
Chronic sinusitis	17.80	17.51	9	4950	6283	64487490
Psychomotor hyperactivity	17.68	17.51	12	4947	14439	64479334

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018490	Serotonin Agents
MeSH PA	D012702	Serotonin Antagonists

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

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
SSRI induced sexual dysfunction	off-label use	425528008
Ocular hypertension	contraindication	4210003	DOID:9282
Peptic ulcer	contraindication	13200003	DOID:750
Hyperthyroidism	contraindication	34486009	DOID:7998
Hypertensive disorder	contraindication	38341003	DOID:10763
Chronic idiopathic constipation	contraindication	82934008
Bladder outflow obstruction	contraindication	236645006
Benign prostatic hyperplasia	contraindication	266569009
Retention of urine	contraindication	267064002
Angle-closure glaucoma	contraindication	392291006	DOID:13550

🐶 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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	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
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	8.81		WOMBAT-PK
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	8.65		WOMBAT-PK
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	6.80		WOMBAT-PK
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	6.90		WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	7.40		WOMBAT-PK
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	7.77		DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	8.10		WOMBAT-PK
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	6.71		DRUG MATRIX
Histamine H4 receptor	GPCR	Q9H3N8	HRH4_HUMAN		Ki	8.19		WOMBAT-PK
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	8		WOMBAT-PK
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	8		WOMBAT-PK
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	8		WOMBAT-PK
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	8.66		DRUG MATRIX
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	8.56		DRUG MATRIX
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN		Ki	5.89		PDSP
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	6.73		DRUG MATRIX
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	6.90		WOMBAT-PK
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	7.60		WOMBAT-PK
Calmodulin	Cytosolic other	P0DP23 P0DP24 P0DP25	CALM1_HUMAN CALM2_HUMAN CALM3_HUMAN					WOMBAT-PK
Sodium channel alpha subunits; brain (Types I, II, III)	Ion channel	P35498 Q99250 Q9NY46	SCN1A_HUMAN SCN2A_HUMAN SCN3A_HUMAN		IC50	6		CHEMBL
Histone-lysine N-methyltransferase SETD7	Enzyme	Q8WTS6	SETD7_HUMAN		IC50	4.70		CHEMBL
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	7.36		DRUG MATRIX
5-hydroxytryptamine receptor 1B	GPCR		5HT1B_RAT		Ki	5.90		DRUG MATRIX
Histamine H1 receptor	GPCR		HRH1_CAVPO		Kd	9		CHEMBL
D(2) dopamine receptor	GPCR		DRD2_RAT		IC50	6.85		CHEMBL
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		IC50	6.91		CHEMBL
5-hydroxytryptamine receptor 2A	GPCR		5HT2A_RAT		Ki	8.80		CHEMBL
5-hydroxytryptamine receptor 7	GPCR		5HT7R_RAT		Ki	7.30		CHEMBL
Sodium-dependent noradrenaline transporter	Transporter		SC6A2_MOUSE		Ki	6.54		CHEMBL
5-hydroxytryptamine receptor 2C	GPCR		5HT2C_MOUSE		Ki	7.96		CHEMBL
D(2) dopamine receptor	GPCR		DRD2_MOUSE		Ki	6.95		CHEMBL
Sodium-dependent serotonin transporter	Transporter		SC6A4_MOUSE		Ki	5.39		CHEMBL
5-hydroxytryptamine receptor 6	GPCR		5HT6R_RAT	ANTAGONIST	Ki	6.90		IUPHAR
Muscarinic acetylcholine receptor	GPCR		ACM1_RAT ACM3_RAT ACM4_RAT ACM5_RAT ACM2_RAT		Ki	8.40		CHEMBL
Dopamine receptor	GPCR		DRD1_RAT DRD3_RAT DRD5_RAT DRD4_RAT DRD2_RAT		Ki	7.20		CHEMBL
Serotonin 2 (5-HT2) receptor	GPCR		5HT2C_RAT 5HT2A_RAT 5HT2B_RAT		IC50	8.51		CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	6.62		CHEMBL

External reference:

ID	Source
4019701	VUID
N0000147793	NUI
D02234	KEGG_DRUG
41354-29-4	SECONDARY_CAS_RN
104592	RXNORM
4017931	VANDF
4019701	VANDF
C0010620	UMLSCUI
CHEBI:4046	CHEBI
C7H	PDB_CHEM_ID
CHEMBL516	ChEMBL_ID
CHEMBL1716	ChEMBL_ID
DB00434	DRUGBANK_ID
D003533	MESH_DESCRIPTOR_UI
2913	PUBCHEM_CID
277	IUPHAR_LIGAND_ID
872	INN_ID
2YHB6175DO	UNII
2249	MMSL
331	MMSL
4522	MMSL
d00790	MMSL
001537	NDDF
004617	NDDF
15352003	SNOMEDCT_US
26462003	SNOMEDCT_US
372683000	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1757	TABLET	4 mg	ORAL	ANDA	21 sections
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	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	16571-805	TABLET	4 mg	ORAL	ANDA	13 sections
cyproheptadine hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	23155-703	TABLET	4 mg	ORAL	ANDA	17 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	24689-816	TABLET	4 mg	ORAL	ANDA	3 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	27808-099	SYRUP	2 mg	ORAL	ANDA	19 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	39328-044	SOLUTION	2 mg	ORAL	ANDA	19 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	39328-544	SOLUTION	2 mg	ORAL	ANDA	21 sections
CYPROHEPTADINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	42291-225	TABLET	4 mg	ORAL	ANDA	11 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-4724	TABLET	4 mg	ORAL	ANDA	21 sections
Cyproheptadine Hydrochloride	Human Prescription Drug Label	1	50090-5491	TABLET	4 mg	ORAL	ANDA	20 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50268-189	TABLET	4 mg	ORAL	ANDA	23 sections
CYPROHEPTADINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	50488-5002	TABLET	4 mg	ORAL	ANDA	19 sections
CYPROHEPTADINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	50742-190	TABLET	4 mg	ORAL	ANDA	21 sections
CYPROHEPTADINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	51407-272	TABLET	4 mg	ORAL	ANDA	21 sections
CYPROHEPTADINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	51991-838	TABLET	4 mg	ORAL	ANDA	22 sections
CYPROHEPTADINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	51991-838	TABLET	4 mg	ORAL	ANDA	22 sections
Cyproheptadine Hydrochloride	Human Prescription Drug Label	1	52817-210	TABLET	4 mg	ORAL	ANDA	20 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	53808-0829	TABLET	4 mg	ORAL	ANDA	21 sections
CYPROHEPTADINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	53808-0950	TABLET	4 mg	ORAL	ANDA	19 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	53808-1030	TABLET	4 mg	ORAL	ANDA	21 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	54868-1332	TABLET	4 mg	ORAL	ANDA	11 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	54868-4338	SYRUP	2 mg	ORAL	ANDA	18 sections
CYPROHEPTADINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	55700-700	TABLET	4 mg	ORAL	ANDA	18 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	62033-0346	TABLET	4 mg	ORAL	Export only	10 sections