almotriptan ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
serotonin (5-HT1) receptor agonists, sumatriptan derivatives 128 154323-57-6

Description:

MoleculeDescription

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:

DoseUnitRoute
12.50 mg O

ADMET properties:

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

Approvals:

DateAgencyCompanyOrphan
May 7, 2001 FDA JANSSEN PHARMS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Failed induction of labour 48.54 28.66 8 1093 307 50603716
Threatened labour 41.22 28.66 8 1093 779 50603244
Placental calcification 31.17 28.66 4 1097 24 50603999
Medication overuse headache 30.47 28.66 6 1095 629 50603394
Malignant melanoma in situ 28.91 28.66 6 1095 819 50603204

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Nightmare 166.04 92.74 36 324 11381 29562786
Sedation 150.93 92.74 36 324 17369 29556798
Nephrolithiasis 137.50 92.74 36 324 25298 29548869
Hyperhidrosis 104.26 92.74 36 324 64504 29509663

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Nightmare 95.79 38.79 30 1398 20963 64476341
Sedation 72.33 38.79 29 1399 41433 64455871
Nephrolithiasis 70.87 38.79 29 1399 43654 64453650
Hyperhidrosis 70.12 38.79 40 1388 124880 64372424
Medication overuse headache 67.72 38.79 12 1416 698 64496606
Failed induction of labour 43.25 38.79 7 1421 235 64497069
Burns third degree 39.58 38.79 7 1421 402 64496902

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N02CC05 NERVOUS SYSTEM
ANALGESICS
ANTIMIGRAINE PREPARATIONS
Selective serotonin (5HT1) agonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018490 Serotonin Agents
MeSH PA D017366 Serotonin Receptor Agonists
FDA MoA N0000175763 Serotonin 1b Receptor Agonists
FDA MoA N0000175764 Serotonin 1d Receptor Agonists
FDA EPC N0000175765 Serotonin-1b and Serotonin-1d Receptor Agonist
CHEBI has role CHEBI:35475 non-steroidal anti-inflammatory agent
CHEBI has role CHEBI:35941 serotonin agonists

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

DiseaseRelationSNOMED_IDDOID
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
Angina pectoris contraindication 194828000
Cerebrovascular accident contraindication 230690007
Disease of liver contraindication 235856003 DOID:409
Transient ischemic attack contraindication 266257000 DOID:224
Raynaud's phenomenon contraindication 266261006
Cerebral ischemia contraindication 287731003
Serotonin syndrome contraindication 371089000
Cardiovascular event risk contraindication 395112001
Peripheral vascular disease contraindication 400047006
Disorder of coronary artery contraindication 414024009
Myocardial ischemia contraindication 414795007 DOID:3393
Obesity contraindication 414916001 DOID:9970
Hypertensive urgency contraindication 443482000
Smokes tobacco daily contraindication 449868002
Familial History of Ischemic Heart Disease contraindication




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
5-hydroxytryptamine receptor 1B GPCR AGONIST Ki 8 WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 1D GPCR AGONIST Ki 7.50 WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 1F GPCR AGONIST Ki 7.20 WOMBAT-PK

External reference:

IDSource
4021269 VUID
N0000148709 NUI
D02824 KEGG_DRUG
181183-52-8 SECONDARY_CAS_RN
279645 RXNORM
C0914729 UMLSCUI
CHEBI:520985 CHEBI
CHEMBL1505 ChEMBL_ID
DB00918 DRUGBANK_ID
CHEMBL1200521 ChEMBL_ID
C409045 MESH_SUPPLEMENTAL_RECORD_UI
123606 PUBCHEM_CID
7110 IUPHAR_LIGAND_ID
7463 INN_ID
1O4XL5SN61 UNII
16028 MMSL
234759 MMSL
41391 MMSL
d04757 MMSL
009048 NDDF
009049 NDDF
4021269 VANDF
4021270 VANDF
129478004 SNOMEDCT_US
134529000 SNOMEDCT_US
363569003 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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
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
Axert HUMAN PRESCRIPTION DRUG LABEL 1 54868-5527 TABLET, COATED 12.50 mg ORAL NDA 29 sections