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	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
Bone density decreased	32.84	18.65	17	4158	14595	63470252
Malnutrition	29.30	18.65	16	4159	15282	63469565
Mood swings	29.30	18.65	17	4158	18231	63466616
Hallucination, tactile	28.15	18.65	6	4169	303	63484544
Vascular device infection	27.10	18.65	12	4163	7300	63477547
Disturbance in social behaviour	26.67	18.65	10	4165	3983	63480864
Crying	25.44	18.65	17	4158	23326	63461521
Mood altered	24.37	18.65	14	4161	14729	63470118
Cardiogenic shock	24.35	18.65	15	4160	17917	63466930
Sleep apnoea syndrome	24.27	18.65	18	4157	29115	63455732
Mental status changes	23.41	18.65	20	4155	39579	63445268
Hallucination	23.28	18.65	23	4152	54794	63430053
Delirium	22.95	18.65	22	4153	50519	63434328
Psychomotor hyperactivity	22.80	18.65	12	4163	10651	63474196
Joint destruction	22.34	18.65	10	4165	6242	63478605
Oesophageal spasm	21.51	18.65	8	4167	3115	63481732
Mydriasis	21.51	18.65	12	4163	11944	63472903
Personality change	21.29	18.65	10	4165	6963	63477884
Cystic fibrosis	21.09	18.65	8	4167	3288	63481559
Sinus tachycardia	20.23	18.65	15	4160	24253	63460594
Oesophageal pain	20.19	18.65	8	4167	3693	63481154
Infusion site bruising	19.92	18.65	8	4167	3824	63481023
Intentional overdose	19.17	18.65	24	4151	74128	63410719
Hypoperfusion	18.88	18.65	6	4169	1461	63483386
Irritability	18.72	18.65	16	4159	31678	63453169

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
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
Anti-saccharomyces cerevisiae antibody	26.60	21.50	4	3172	17	34953738
Pneumonia aspiration	25.93	21.50	25	3151	41878	34911877
Obsessive-compulsive symptom	24.96	21.50	5	3171	133	34953622
Intentional overdose	23.23	21.50	24	3152	43650	34910105
Weight gain poor	23.03	21.50	7	3169	1065	34952690
Hospitalisation	22.88	21.50	27	3149	56875	34896880

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	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
Butterfly rash	37.44	16.46	11	6399	1685	79736293
Apallic syndrome	33.84	16.46	9	6401	959	79737019
Malnutrition	32.33	16.46	21	6389	22481	79715497
Pulmonary function test decreased	30.41	16.46	14	6396	7623	79730355
Juvenile idiopathic arthritis	29.73	16.46	12	6398	4751	79733227
Agitation	29.22	16.46	38	6372	99677	79638301
Anti-saccharomyces cerevisiae antibody	27.09	16.46	4	6406	17	79737961
Suicide attempt	26.50	16.46	33	6377	82899	79655079
Cystic fibrosis respiratory infection suppression	24.79	16.46	6	6404	438	79737540
Obsessive-compulsive disorder	24.02	16.46	11	6399	5916	79732062
Gastric hypomotility	23.92	16.46	5	6405	187	79737791
Rhinorrhoea	23.87	16.46	30	6380	76044	79661934
Obsessive-compulsive symptom	23.82	16.46	5	6405	191	79737787
Nasal congestion	23.72	16.46	30	6380	76522	79661456
Mental status changes	23.60	16.46	28	6382	66931	79671047
Pneumonia aspiration	23.59	16.46	28	6382	66939	79671039
Hallucination, tactile	22.90	16.46	6	6404	603	79737375
Electrocardiogram QT prolonged	22.76	16.46	32	6378	90354	79647624
Crying	22.56	16.46	17	6393	23026	79714952
Clonus	22.52	16.46	11	6399	6829	79731149
Immobile	22.31	16.46	11	6399	6962	79731016
Hyperthermia	21.51	16.46	15	6395	18022	79719956
Sleep apnoea syndrome	21.36	16.46	20	6390	36458	79701520
Joint destruction	20.93	16.46	10	6400	5915	79732063
Mood swings	20.20	16.46	15	6395	19865	79718113
Disturbance in social behaviour	19.44	16.46	9	6401	4961	79733017
Respiratory failure	19.33	16.46	44	6366	180867	79557111
Oesophageal spasm	19.17	16.46	8	6402	3448	79734530
Aggression	19.10	16.46	22	6388	50936	79687042
Delirium	18.46	16.46	28	6382	84599	79653379
Atypical mycobacterial lower respiratory tract infection	18.40	16.46	4	6406	181	79737797
Psychomotor hyperactivity	17.77	16.46	13	6397	16836	79721142
Oesophageal pain	17.52	16.46	8	6402	4271	79733707
Mydriasis	17.23	16.46	13	6397	17630	79720348
Mood altered	17.10	16.46	13	6397	17834	79720144
Meningioma benign	16.59	16.46	4	6406	287	79737691

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
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 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
5-hydroxytryptamine receptor 2A	GPCR		5HT2A_RAT		Ki	8.80		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 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	42708-156	TABLET	4 mg	ORAL	ANDA	12 sections
Cyproheptadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	42708-177	TABLET	4 mg	ORAL	ANDA	20 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	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