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

Stem definition	Drug id	CAS RN
serotonin (5-HT1) receptor agonists, sumatriptan derivatives	2869	139264-17-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: zolmitriptan zipton zominat zomigoro 311C90	an antimigraine compound; a serotonin (5HT)-1D receptor agonist Molecular weight: 287.36 Formula: C16H21N3O2 CLOGP: 1.29 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 57.36 ALOGS: -3.18 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

zolmitriptan
zipton
zominat
zomigoro
311C90

an antimigraine compound; a serotonin (5HT)-1D receptor agonist

Molecular weight: 287.36
Formula: C16H21N3O2
CLOGP: 1.29
LIPINSKI: 0
HAC: 5
HDO: 2
TPSA: 57.36
ALOGS: -3.18
ROTB: 5

Status: OFP

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

Drug dosage:

Dose	Unit	Route
2.50	mg	N
2.50	mg	O

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	8 %	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	6.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	45 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	3.60 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	20 mg/mL	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	1.80 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.75 %	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.50 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Nov. 25, 1997	FDA	IPR

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
Migraine	158.42	15.67	127	9216	103219	63376460
Medication overuse headache	108.13	15.67	25	9318	807	63478872
Skin candida	68.43	15.67	20	9323	1635	63478044
Mastoiditis	58.33	15.67	16	9327	1039	63478640
Vascular malformation	52.49	15.67	12	9331	368	63479311
Paranasal cyst	51.67	15.67	12	9331	395	63479284
Headache	48.11	15.67	202	9141	633039	62846640
Antibody test positive	43.50	15.67	16	9327	2691	63476988
Monocyte count abnormal	42.41	15.67	9	9334	194	63479485
Infrequent bowel movements	37.85	15.67	12	9331	1290	63478389

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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
Paraesthesia	41.21	31.63	25	1027	64147	34891732
Therapy partial responder	40.69	31.63	14	1038	9602	34946277
Craniosynostosis	37.95	31.63	7	1045	373	34955506
Medication overuse headache	37.50	31.63	6	1046	136	34955743
Migraine	35.88	31.63	15	1037	17463	34938416

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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
Migraine	177.62	17.18	113	8488	87380	79648407
Medication overuse headache	130.38	17.18	28	8573	884	79734903
Skin candida	65.52	17.18	19	8582	2068	79733719
Headache	62.78	17.18	183	8418	653589	79082198
Mastoiditis	55.66	17.18	16	8585	1688	79734099
Vascular malformation	55.65	17.18	12	8589	386	79735401
Paranasal cyst	54.05	17.18	12	8589	443	79735344
Therapy partial responder	49.60	17.18	28	8573	17369	79718418
Reversible cerebral vasoconstriction syndrome	38.82	17.18	14	8587	3043	79732744
Burns third degree	37.84	17.18	9	8592	452	79735335

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N02CC03	NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Selective serotonin (5HT1) agonists
CHEBI has role	CHEBI:35472	anti-inflammatory drugs
CHEBI has role	CHEBI:35941	serotonin agonists
FDA EPC	N0000175765	Serotonin-1b and Serotonin-1d Receptor Agonist
FDA MoA	N0000175763	Serotonin 1b Receptor Agonists
FDA MoA	N0000175764	Serotonin 1d Receptor Agonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D058825	Serotonin 5-HT1 Receptor Agonists
MeSH PA	D018490	Serotonin Agents
MeSH PA	D017366	Serotonin Receptor Agonists

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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
Migraine	indication	37796009	DOID:6364
Myocardial infarction	contraindication	22298006	DOID:5844
Hypertensive disorder	contraindication	38341003	DOID:10763
Hemiplegic migraine	contraindication	59292006
Cerebral arteriosclerosis	contraindication	65312002
Wolff-Parkinson-White pattern	contraindication	74390002	DOID:384
Vascular insufficiency of intestine	contraindication	82196007
Prinzmetal angina	contraindication	87343002
Kidney disease	contraindication	90708001	DOID:557
Angina pectoris	contraindication	194828000

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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	13.47	acidic
pKa2	8.28	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
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN	AGONIST	Ki	8.90	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN	AGONIST	Ki	7.70	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 1E	GPCR	P28566	5HT1E_HUMAN		Ki	7.70	WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	6.60	WOMBAT-PK
5-hydroxytryptamine receptor 1F	GPCR	P30939	5HT1F_HUMAN		Ki	7.45	WOMBAT-PK
D(2) dopamine receptor	GPCR		DRD2_RAT		Kd	10.40	CHEMBL
D(1A) dopamine receptor	GPCR		DRD1_RAT		Kd	9.52	CHEMBL
Adrenergic receptor alpha-2	GPCR		ADA2B_RAT ADA2C_RAT ADA2A_RAT		Kd	8.15	CHEMBL

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External reference:

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ID	Source
006460	NDDF
108406003	SNOMEDCT_US
11471	MMSL
135775	RXNORM
2FS66TH3YW	UNII
363582006	SNOMEDCT_US
4021094	VUID
4021094	VANDF
52759	MMSL
5712	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Zolmitriptan	Human Prescription Drug Label	1	16571-803	TABLET, FILM COATED	2.50 mg	ORAL	ANDA	25 sections
Zolmitriptan	Human Prescription Drug Label	1	16571-804	TABLET, FILM COATED	5 mg	ORAL	ANDA	25 sections
Zolmitriptan	Human Prescription Drug Label	1	27241-021	TABLET	2.50 mg	ORAL	ANDA	24 sections
Zolmitriptan	Human Prescription Drug Label	1	27241-022	TABLET	5 mg	ORAL	ANDA	24 sections
ZOLMITRIPTAN	HUMAN PRESCRIPTION DRUG LABEL	1	31722-458	TABLET, FILM COATED	2.50 mg	ORAL	ANDA	19 sections
ZOLMITRIPTAN	HUMAN PRESCRIPTION DRUG LABEL	1	31722-459	TABLET, FILM COATED	5 mg	ORAL	ANDA	19 sections
zolmitriptan	HUMAN PRESCRIPTION DRUG LABEL	1	45802-711	SPRAY	5 mg	NASAL	ANDA	26 sections
Zolmitriptan	Human Prescription Drug Label	1	46708-181	TABLET, ORALLY DISINTEGRATING	2.50 mg	ORAL	ANDA	25 sections
Zolmitriptan	Human Prescription Drug Label	1	46708-181	TABLET, ORALLY DISINTEGRATING	2.50 mg	ORAL	ANDA	25 sections
Zolmitriptan	Human Prescription Drug Label	1	46708-182	TABLET, ORALLY DISINTEGRATING	5 mg	ORAL	ANDA	25 sections

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