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almotriptan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| serotonin (5-HT1) receptor agonists, sumatriptan derivatives | 128 | 154323-57-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 12.50 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 µM/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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1 | 34 | |||
| kinase-selectivity-class | AXL | 1 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 4.909 | Moderate | 0.65 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | Moderate | 0.65 | |
| rat-kpuu-brain | Rat brain Kpuu | 0.042 | % | Moderate | 0.65 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 7, 2001 | FDA | JANSSEN PHARMS |
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 |
|---|---|---|---|---|---|---|
| Failed induction of labour | 45.70 | 26.18 | 8 | 1846 | 469 | 90626124 |
| Abortion missed | 45.15 | 26.18 | 10 | 1844 | 1972 | 90624621 |
| Threatened labour | 40.65 | 26.18 | 8 | 1846 | 890 | 90625703 |
| Congenital gastric anomaly | 39.71 | 26.18 | 5 | 1849 | 27 | 90626566 |
| Burns third degree | 35.02 | 26.18 | 6 | 1848 | 310 | 90626283 |
| Placental calcification | 30.09 | 26.18 | 4 | 1850 | 35 | 90626558 |
| Dust allergy | 29.24 | 26.18 | 6 | 1848 | 823 | 90625770 |
| Malignant melanoma in situ | 28.26 | 26.18 | 6 | 1848 | 970 | 90625623 |
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 |
|---|---|---|---|---|---|---|
| Nightmare | 832.12 | 188.65 | 190 | 1405 | 24822 | 42594918 |
| Sedation | 794.76 | 188.65 | 190 | 1405 | 30285 | 42589455 |
| Nephrolithiasis | 619.98 | 188.65 | 162 | 1433 | 36668 | 42583072 |
| Hyperhidrosis | 589.92 | 188.65 | 190 | 1405 | 90322 | 42529418 |
| Product use in unapproved indication | 300.21 | 188.65 | 142 | 1453 | 184314 | 42435426 |
| Nausea | 259.57 | 188.65 | 167 | 1428 | 396632 | 42223108 |
| Drug ineffective | 226.07 | 188.65 | 184 | 1411 | 630013 | 41989727 |
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 |
|---|---|---|---|---|---|---|
| Nightmare | 769.72 | 41.04 | 186 | 3031 | 38677 | 110547405 |
| Sedation | 657.38 | 41.04 | 185 | 3032 | 69498 | 110516584 |
| Nephrolithiasis | 544.10 | 41.04 | 158 | 3059 | 66054 | 110520028 |
| Hyperhidrosis | 532.06 | 41.04 | 200 | 3017 | 187098 | 110398984 |
| Product use in unapproved indication | 245.20 | 41.04 | 155 | 3062 | 447222 | 110138860 |
| Nausea | 171.26 | 41.04 | 193 | 3024 | 1235497 | 109350585 |
| Drug ineffective | 156.17 | 41.04 | 204 | 3013 | 1520336 | 109065746 |
| Product used for unknown indication | 145.64 | 41.04 | 28 | 3189 | 1935 | 110584147 |
| Off label use | 124.60 | 41.04 | 182 | 3035 | 1500003 | 109086079 |
| Medication overuse headache | 49.44 | 41.04 | 11 | 3206 | 1552 | 110584530 |
| Abortion missed | 44.16 | 41.04 | 10 | 3207 | 1527 | 110584555 |
| Burns third degree | 42.62 | 41.04 | 8 | 3209 | 485 | 110585597 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N02CC05 | NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Selective serotonin (5HT1) agonists |
| MeSH PA | D017366 | Serotonin Receptor Agonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
| 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 drug |
| CHEBI has role | CHEBI:35941 | serotonergic agonist |
| CHEBI has role | CHEBI:50514 | vasoconstrictor agent |
Related Drugs by ATC class:
N02CC Selective serotonin (5HT1) agonists 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| 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 | |
| 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 |
🐶 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 4021269 | VUID |
| N0000148709 | NUI |
| D02824 | KEGG_DRUG |
| 181183-52-8 | SECONDARY_CAS_RN |
| 279645 | RXNORM |
| C0914729 | UMLSCUI |
| CHEBI:520985 | CHEBI |
| CHEMBL1505 | ChEMBL_ID |
| CHEMBL1200521 | ChEMBL_ID |
| DB00918 | DRUGBANK_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 |
| 4021269 | VANDF |
| 4021270 | VANDF |
| 009048 | NDDF |
| 009049 | NDDF |
| 129478004 | SNOMEDCT_US |
| 134529000 | SNOMEDCT_US |
| 363569003 | SNOMEDCT_US |
| 1O4XL5SN61 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |