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

Stem definition	Drug id	CAS RN
serotonin (5-HT1) receptor agonists, sumatriptan derivatives	128	154323-57-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: almotriptan almotriptan malate almogran axert LAS-31416	Molecular weight: 335.47 Formula: C17H25N3O2S CLOGP: 1.79 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 56.41 ALOGS: -3.44 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

almotriptan
almotriptan malate
almogran
axert
LAS-31416

Molecular weight: 335.47
Formula: C17H25N3O2S
CLOGP: 1.79
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 56.41
ALOGS: -3.44
ROTB: 5

Status: OFP

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

Drug dosage:

Dose	Unit	Route
12.50	mg	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	8.90 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	70 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	40 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	3.40 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	2.20 L/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.06 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
fu (Fraction unbound in plasma)	0.60 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
May 7, 2001	FDA	JANSSEN PHARMS

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
Failed induction of labour	47.58	29.43	8	1354	352	63487308
Threatened labour	40.68	29.43	8	1354	846	63486814
Burns third degree	35.01	29.43	6	1356	296	63487364
Placental calcification	31.22	29.43	4	1358	24	63487636
Dust allergy	29.94	29.43	6	1356	698	63486962

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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
Nightmare	334.58	115.62	73	633	14318	34941907
Sedation	307.09	115.62	73	633	20933	34935292
Nephrolithiasis	280.44	115.62	73	633	30260	34925965
Hyperhidrosis	214.51	115.62	73	633	75619	34880606
Product used for unknown indication	161.12	115.62	26	680	957	34955268
Nausea	117.13	115.62	76	630	339832	34616393

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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
Nightmare	224.55	39.29	62	1868	25799	79716659
Sedation	178.05	39.29	61	1869	51834	79690624
Nephrolithiasis	176.47	39.29	61	1869	53230	79689228
Hyperhidrosis	156.37	39.29	75	1855	151417	79591041
Product used for unknown indication	137.85	39.29	25	1905	1519	79740939
Medication overuse headache	63.64	39.29	12	1918	900	79741558
Nausea	49.68	39.29	85	1845	957111	78785347
Burns third degree	44.63	39.29	8	1922	453	79742005
Failed induction of labour	41.48	39.29	7	1923	278	79742180

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N02CC05	NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Selective serotonin (5HT1) agonists
CHEBI has role	CHEBI:35475	non-steroidal anti-inflammatory agent
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	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
Hypercholesterolemia	contraindication	13644009
Myocardial infarction	contraindication	22298006	DOID:5844
Hypertensive disorder	contraindication	38341003	DOID:10763
Conduction disorder of the heart	contraindication	44808001
Acute nephropathy	contraindication	58574008
Hemiplegic migraine	contraindication	59292006
Diabetes mellitus	contraindication	73211009	DOID:9351
Vascular insufficiency of intestine	contraindication	82196007
Prinzmetal angina	contraindication	87343002

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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	13.02	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 1B	GPCR	P28222	5HT1B_HUMAN	AGONIST	Ki	8	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN	AGONIST	Ki	7.50	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 1F	GPCR	P30939	5HT1F_HUMAN	AGONIST	Ki	7.20	WOMBAT-PK

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External reference:

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ID	Source
009048	NDDF
009049	NDDF
123606	PUBCHEM_CID
129478004	SNOMEDCT_US
134529000	SNOMEDCT_US
16028	MMSL
181183-52-8	SECONDARY_CAS_RN
1O4XL5SN61	UNII
234759	MMSL
279645	RXNORM

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
almotriptan	Human Prescription Drug Label	1	27241-041	TABLET, FILM COATED	6.25 mg	ORAL	ANDA	26 sections
almotriptan	Human Prescription Drug Label	1	27241-041	TABLET, FILM COATED	6.25 mg	ORAL	ANDA	26 sections
almotriptan	Human Prescription Drug Label	1	27241-042	TABLET, FILM COATED	12.50 mg	ORAL	ANDA	26 sections
almotriptan	Human Prescription Drug Label	1	27241-042	TABLET, FILM COATED	12.50 mg	ORAL	ANDA	26 sections
Almotriptan Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5260	TABLET, FILM COATED	6.25 mg	ORAL	ANDA	27 sections
Almotriptan Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-5261	TABLET, FILM COATED	12.50 mg	ORAL	ANDA	27 sections
Almotriptan Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5245	TABLET, FILM COATED	6.25 mg	ORAL	ANDA	27 sections
Almotriptan Malate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-5246	TABLET, FILM COATED	12.50 mg	ORAL	ANDA	27 sections
Axert	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5527	TABLET, COATED	12.50 mg	ORAL	NDA	29 sections

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