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	200.09	18.77	54	3375	8103	56280535
Torus fracture	111.73	18.77	17	3412	127	56288511
Growth retardation	70.39	18.77	16	3413	1179	56287459
Serotonin syndrome	62.36	18.77	31	3398	26459	56262179
Immobile	50.12	18.77	17	3412	5485	56283153
Apallic syndrome	39.92	18.77	9	3420	639	56287999
Butterfly rash	37.02	18.77	10	3419	1496	56287142
Bone density decreased	36.26	18.77	17	3412	12743	56275895
Hospitalisation	34.97	18.77	32	3397	74968	56213670
Juvenile idiopathic arthritis	32.95	18.77	12	3417	4761	56283877
Malnutrition	31.79	18.77	16	3413	13992	56274646
Hallucination, tactile	29.42	18.77	6	3423	264	56288374
Cystic fibrosis	28.87	18.77	10	3419	3434	56285204
Cardiogenic shock	26.73	18.77	15	3414	16310	56272328
Intentional overdose	25.93	18.77	26	3403	68091	56220547
Delirium	25.59	18.77	21	3408	42496	56246142
Joint destruction	25.13	18.77	10	3419	5045	56283593
Psychomotor hyperactivity	24.60	18.77	12	3417	9808	56278830
Mental status changes	23.57	18.77	19	3410	37482	56251156
Mydriasis	23.24	18.77	12	3417	11059	56277579
Sinus tachycardia	22.32	18.77	15	3414	22429	56266209
Atrial tachycardia	20.70	18.77	7	3422	2234	56286404
Agitation	20.61	18.77	21	3408	56015	56232623
Hypoperfusion	19.65	18.77	6	3423	1384	56287254
Intestinal ischaemia	18.94	18.77	9	3420	6946	56281692
Abnormal behaviour	18.86	18.77	13	3416	20259	56268379

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	250.06	21.17	84	2667	18689	31675904
Infective pulmonary exacerbation of cystic fibrosis	161.94	21.17	47	2704	6437	31688156
Cystic fibrosis	43.53	21.17	13	2738	1953	31692640
Nasal polyps	38.96	21.17	12	2739	2001	31692592
Symptom masked	37.62	21.17	9	2742	579	31694014
Chronic sinusitis	35.80	21.17	11	2740	1818	31692775
Cystic fibrosis respiratory infection suppression	33.81	21.17	7	2744	231	31694362
Clonus	32.34	21.17	11	2740	2508	31692085
Intentional overdose	27.18	21.17	25	2726	41364	31653229
Obsessive-compulsive symptom	25.08	21.17	5	2746	136	31694457
Pneumonia aspiration	24.67	21.17	23	2728	38703	31655890
Hospitalisation	21.53	21.17	24	2727	49783	31644810
Rhinorrhoea	21.44	21.17	17	2734	22995	31671598

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	299.83	17.71	85	5376	12073	70910910
Serotonin syndrome	292.62	17.71	113	5348	42001	70880982
Torus fracture	70.09	17.71	11	5450	79	70922904
Cystic fibrosis	62.48	17.71	20	5441	4261	70918722
Intentional overdose	53.98	17.71	51	5410	98384	70824599
Growth retardation	46.99	17.71	13	5448	1679	70921304
Hospitalisation	41.89	17.71	41	5420	82527	70840456
Symptom masked	41.24	17.71	11	5450	1238	70921745
Apallic syndrome	35.05	17.71	9	5452	874	70922109
Nasal polyps	34.44	17.71	13	5448	4503	70918480
Pulmonary function test decreased	32.55	17.71	14	5447	6787	70916196
Butterfly rash	30.75	17.71	9	5452	1421	70921562
Malnutrition	30.04	17.71	19	5442	20298	70902685
Suicide attempt	28.78	17.71	33	5428	79477	70843506
Juvenile idiopathic arthritis	27.95	17.71	12	5449	5788	70917195
Electrocardiogram QT prolonged	25.84	17.71	32	5429	83485	70839498
Obsessive-compulsive disorder	25.52	17.71	11	5450	5359	70917624
Cystic fibrosis respiratory infection suppression	25.17	17.71	6	5455	429	70922554
Gastric hypomotility	24.27	17.71	5	5456	182	70922801
Mental status changes	24.21	17.71	27	5434	63074	70859909
Hallucination, tactile	24.00	17.71	6	5455	523	70922460
Clonus	23.88	17.71	11	5450	6257	70916726
Obsessive-compulsive symptom	23.69	17.71	5	5456	205	70922778
Chronic sinusitis	23.64	17.71	12	5449	8439	70914544
Joint destruction	23.61	17.71	10	5451	4668	70918315
Immobile	23.51	17.71	11	5450	6483	70916500
Hyperthermia	23.18	17.71	15	5446	16656	70906327
Pneumonia aspiration	22.79	17.71	26	5435	62263	70860720
Atypical mycobacterial lower respiratory tract infection	21.62	17.71	4	5457	82	70922901
Delirium	20.57	17.71	27	5434	74587	70848396
Aggression	19.05	17.71	21	5440	48425	70874558
Mydriasis	18.77	17.71	13	5448	16140	70906843
Respiratory failure	18.04	17.71	40	5421	168695	70754288

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(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
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	6.93		WOMBAT-PK
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
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	6.62		CHEMBL
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

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	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	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	50090-6129	TABLET	4 mg	ORAL	ANDA	18 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50268-189	TABLET	4 mg	ORAL	ANDA	23 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	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