eletriptan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| serotonin (5-HT1) receptor agonists, sumatriptan derivatives | 995 | 143322-58-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors. Migraines are likely due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of Eletriptan for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 40 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 4 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 5 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.49 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 1.60 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 5.30 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.15 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 4.20 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 26, 2002 | FDA | PFIZER IRELAND |
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 |
|---|---|---|---|---|---|---|
| Migraine | 185.18 | 16.23 | 122 | 7155 | 75158 | 50522689 |
| Rheumatoid factor negative | 78.24 | 16.23 | 18 | 7259 | 582 | 50597265 |
| Recalled product administered | 77.35 | 16.23 | 17 | 7260 | 445 | 50597402 |
| Drug dependence | 63.47 | 16.23 | 38 | 7239 | 19721 | 50578126 |
| Medication overuse headache | 61.63 | 16.23 | 15 | 7262 | 620 | 50597227 |
| Headache | 51.07 | 16.23 | 174 | 7103 | 506361 | 50091486 |
| Drug ineffective | 47.46 | 16.23 | 237 | 7040 | 819096 | 49778751 |
| Feeling abnormal | 39.10 | 16.23 | 67 | 7210 | 125425 | 50472422 |
| Intentional product misuse | 38.15 | 16.23 | 40 | 7237 | 46694 | 50551153 |
| Hepatic infiltration eosinophilic | 38.06 | 16.23 | 6 | 7271 | 21 | 50597826 |
| Paraesthesia | 30.83 | 16.23 | 59 | 7218 | 120184 | 50477663 |
| Serotonin syndrome | 29.33 | 16.23 | 26 | 7251 | 24687 | 50573160 |
| Throat tightness | 28.95 | 16.23 | 24 | 7253 | 20823 | 50577024 |
| Withdrawal syndrome | 26 | 16.23 | 21 | 7256 | 17569 | 50580278 |
| Lichen planus | 25.88 | 16.23 | 10 | 7267 | 1969 | 50595878 |
| Product dispensing error | 25.72 | 16.23 | 16 | 7261 | 8875 | 50588972 |
| Death | 23.05 | 16.23 | 9 | 7268 | 325370 | 50272477 |
| Drug abuse | 22.76 | 16.23 | 35 | 7242 | 59811 | 50538036 |
| Basilar migraine | 21.63 | 16.23 | 4 | 7273 | 42 | 50597805 |
| Neck pain | 21.17 | 16.23 | 33 | 7244 | 57034 | 50540813 |
| Pleural rub | 21.14 | 16.23 | 4 | 7273 | 48 | 50597799 |
| Oral mucosal exfoliation | 20.83 | 16.23 | 8 | 7269 | 1551 | 50596296 |
| Disturbance in attention | 20.77 | 16.23 | 24 | 7253 | 31162 | 50566685 |
| Chest discomfort | 20.74 | 16.23 | 43 | 7234 | 92679 | 50505168 |
| Vasoconstriction | 20.66 | 16.23 | 6 | 7271 | 491 | 50597356 |
| Cerebral vasoconstriction | 20.40 | 16.23 | 7 | 7270 | 985 | 50596862 |
| Vomiting | 20.21 | 16.23 | 124 | 7153 | 460634 | 50137213 |
| Cholecystitis chronic | 19.73 | 16.23 | 14 | 7263 | 9655 | 50588192 |
| Drug hypersensitivity | 19.10 | 16.23 | 79 | 7198 | 250931 | 50346916 |
| Therapeutic product effect incomplete | 18.81 | 16.23 | 41 | 7236 | 91474 | 50506373 |
| Joint swelling | 18.70 | 16.23 | 6 | 7271 | 245280 | 50352567 |
| Reversible cerebral vasoconstriction syndrome | 18.45 | 16.23 | 8 | 7269 | 2111 | 50595736 |
| Blindness transient | 18.13 | 16.23 | 9 | 7268 | 3229 | 50594618 |
| Anxiety | 17.74 | 16.23 | 61 | 7216 | 177545 | 50420302 |
| Drug abuser | 16.24 | 16.23 | 8 | 7269 | 2820 | 50595027 |
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 |
|---|---|---|---|---|---|---|
| Medication overuse headache | 85.68 | 35.64 | 12 | 829 | 112 | 29573574 |
| Drug abuse | 66.43 | 35.64 | 36 | 805 | 79847 | 29493839 |
| Therapy partial responder | 49.97 | 35.64 | 14 | 827 | 5185 | 29568501 |
| Insomnia | 47.24 | 35.64 | 30 | 811 | 88731 | 29484955 |
| Drug dependence | 40.70 | 35.64 | 17 | 824 | 20964 | 29552722 |
| Paraesthesia | 38.41 | 35.64 | 22 | 819 | 53823 | 29519863 |
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 |
|---|---|---|---|---|---|---|
| Migraine | 198.10 | 19.12 | 103 | 5977 | 62574 | 64430078 |
| Medication overuse headache | 117.29 | 19.12 | 24 | 6056 | 686 | 64491966 |
| Recalled product administered | 81.67 | 19.12 | 18 | 6062 | 738 | 64491914 |
| Drug ineffective | 75.40 | 19.12 | 210 | 5870 | 840037 | 63652615 |
| Headache | 73.79 | 19.12 | 157 | 5923 | 529310 | 63963342 |
| Rheumatoid factor negative | 69.93 | 19.12 | 17 | 6063 | 1076 | 64491576 |
| Drug dependence | 57.50 | 19.12 | 37 | 6043 | 33275 | 64459377 |
| Drug abuse | 53.33 | 19.12 | 64 | 6016 | 132310 | 64360342 |
| Paraesthesia | 41.51 | 19.12 | 57 | 6023 | 134465 | 64358187 |
| Intentional product misuse | 34.20 | 19.12 | 38 | 6042 | 72257 | 64420395 |
| Feeling abnormal | 33.05 | 19.12 | 51 | 6029 | 133551 | 64359101 |
| Therapeutic product effect incomplete | 30.63 | 19.12 | 43 | 6037 | 103439 | 64389213 |
| Throat tightness | 28.75 | 19.12 | 21 | 6059 | 23139 | 64469513 |
| Drug hypersensitivity | 27.84 | 19.12 | 66 | 6014 | 237749 | 64254903 |
| Pain | 26.81 | 19.12 | 113 | 5967 | 553398 | 63939254 |
| Product dispensing error | 25.57 | 19.12 | 15 | 6065 | 11435 | 64481217 |
| Oral mucosal exfoliation | 25.00 | 19.12 | 8 | 6072 | 1387 | 64491265 |
| Acute kidney injury | 24.73 | 19.12 | 6 | 6074 | 449234 | 64043418 |
| Vomiting | 24.00 | 19.12 | 109 | 5971 | 551008 | 63941644 |
| Death | 23.71 | 19.12 | 8 | 6072 | 482697 | 64009955 |
| Pleural rub | 23.23 | 19.12 | 4 | 6076 | 43 | 64492609 |
| Basilar migraine | 22.00 | 19.12 | 4 | 6076 | 60 | 64492592 |
| Lichen planus | 20.99 | 19.12 | 8 | 6072 | 2320 | 64490332 |
| Reversible cerebral vasoconstriction syndrome | 20.95 | 19.12 | 8 | 6072 | 2334 | 64490318 |
| Chest discomfort | 20.31 | 19.12 | 38 | 6042 | 116068 | 64376584 |
| Disturbance in attention | 20.12 | 19.12 | 22 | 6058 | 41052 | 64451600 |
| Withdrawal syndrome | 19.88 | 19.12 | 17 | 6063 | 23475 | 64469177 |
| Therapy partial responder | 19.21 | 19.12 | 12 | 6068 | 10236 | 64482416 |
| Injury | 19.19 | 19.12 | 25 | 6055 | 55967 | 64436685 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N02CC06 | 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Migraine | indication | 37796009 | DOID:6364 |
| Hypercholesterolemia | contraindication | 13644009 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Coronary artery spasm | contraindication | 23687008 | DOID:11840 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Hemiplegic migraine | contraindication | 59292006 | |
| Hepatic failure | contraindication | 59927004 | |
| 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 Cardiovascular 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 | 13.9 | acidic |
| pKa2 | 8.57 | 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 | Kd | 8.52 | CHEMBL | CHEMBL | |||
| 5-hydroxytryptamine receptor 1D | GPCR | AGONIST | Kd | 9.05 | CHEMBL | CHEMBL | |||
| 5-hydroxytryptamine receptor 1A | GPCR | AGONIST | Ki | 7.40 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1F | GPCR | AGONIST | Ki | 8 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1E | GPCR | AGONIST | Ki | 7.20 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4021372 | VUID |
| N0000148791 | NUI |
| D01973 | KEGG_DRUG |
| 177834-92-3 | SECONDARY_CAS_RN |
| 4021372 | VANDF |
| C0759933 | UMLSCUI |
| CHEBI:50922 | CHEBI |
| CHEMBL1510 | ChEMBL_ID |
| DB00216 | DRUGBANK_ID |
| CHEMBL1201003 | ChEMBL_ID |
| C115647 | MESH_SUPPLEMENTAL_RECORD_UI |
| 77993 | PUBCHEM_CID |
| 40 | IUPHAR_LIGAND_ID |
| 7426 | INN_ID |
| 22QOO9B8KI | UNII |
| 231049 | RXNORM |
| 17144 | MMSL |
| 260414 | MMSL |
| 46299 | MMSL |
| d04849 | MMSL |
| 009521 | NDDF |
| 009522 | NDDF |
| 395255007 | SNOMEDCT_US |
| 410843003 | SNOMEDCT_US |
| 425436002 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Relpax | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0049-2330 | TABLET, FILM COATED | 20 mg | ORAL | NDA | 29 sections |
| Relpax | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0049-2340 | TABLET, FILM COATED | 40 mg | ORAL | NDA | 29 sections |
| Eletriptan Hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-8310 | TABLET, FILM COATED | 20 mg | ORAL | ANDA | 25 sections |
| Eletriptan Hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-8311 | TABLET, FILM COATED | 40 mg | ORAL | ANDA | 25 sections |
| Eletriptan Hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-4287 | TABLET, FILM COATED | 20 mg | ORAL | ANDA | 26 sections |
| Eletriptan Hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-4288 | TABLET, FILM COATED | 40 mg | ORAL | ANDA | 26 sections |
| Relpax | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-201 | TABLET, FILM COATED | 40 mg | ORAL | NDA | 28 sections |
| Relpax | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-871 | TABLET, FILM COATED | 40 mg | ORAL | NDA | 28 sections |
| eletriptan hydrobromide | Human Prescription Drug Label | 1 | 27241-039 | TABLET, FILM COATED | 20 mg | ORAL | ANDA | 24 sections |
| eletriptan hydrobromide | Human Prescription Drug Label | 1 | 27241-040 | TABLET, FILM COATED | 40 mg | ORAL | ANDA | 24 sections |
| Relpax | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5528 | TABLET, FILM COATED | 40 mg | ORAL | NDA | 28 sections |
| Eletriptan Hydrobromide | Human Prescription Drug Label | 1 | 59651-104 | TABLET, FILM COATED | 20 mg | ORAL | ANDA | 24 sections |
| Eletriptan Hydrobromide | Human Prescription Drug Label | 1 | 59651-105 | TABLET, FILM COATED | 40 mg | ORAL | ANDA | 24 sections |
| Eletriptan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59762-2321 | TABLET, FILM COATED | 20 mg | ORAL | NDA AUTHORIZED GENERIC | 26 sections |
| Eletriptan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59762-2322 | TABLET, FILM COATED | 40 mg | ORAL | NDA AUTHORIZED GENERIC | 26 sections |
| Eletriptan Hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-8320 | TABLET, FILM COATED | 40 mg | ORAL | ANDA | 24 sections |
| Eletriptan hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68382-922 | TABLET, FILM COATED | 20 mg | ORAL | ANDA | 24 sections |
| Eletriptan hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68382-923 | TABLET, FILM COATED | 40 mg | ORAL | ANDA | 24 sections |
| Eletriptan hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70771-1107 | TABLET, FILM COATED | 20 mg | ORAL | ANDA | 1 sections |
| Eletriptan hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70771-1108 | TABLET, FILM COATED | 40 mg | ORAL | ANDA | 1 sections |
| eletriptan hydrobromide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71335-1830 | TABLET, FILM COATED | 40 mg | ORAL | ANDA | 24 sections |