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 |
|---|---|
|
Synonyms:
|
an antimigraine compound; a serotonin (5HT)-1D receptor agonist
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:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 20 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 8 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.50 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 45 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.80 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 6.70 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.75 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 3.60 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 25, 1997 | FDA | IPR |
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 | 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 |
| Reversible cerebral vasoconstriction syndrome | 36.49 | 15.67 | 14 | 9329 | 2644 | 63477035 |
| Temperature intolerance | 35.71 | 15.67 | 20 | 9323 | 8944 | 63470735 |
| Depression | 34.66 | 15.67 | 84 | 9259 | 196408 | 63283271 |
| Urticaria chronic | 31.80 | 15.67 | 9 | 9334 | 656 | 63479023 |
| Lymphocyte count abnormal | 31.15 | 15.67 | 9 | 9334 | 706 | 63478973 |
| Vertigo | 30.90 | 15.67 | 41 | 9302 | 59846 | 63419833 |
| Nervous system disorder | 30.68 | 15.67 | 24 | 9319 | 18742 | 63460937 |
| Dyspnoea exertional | 29.16 | 15.67 | 40 | 9303 | 60262 | 63419417 |
| Blood thyroid stimulating hormone normal | 28.84 | 15.67 | 6 | 9337 | 117 | 63479562 |
| Polymenorrhagia | 27.14 | 15.67 | 5 | 9338 | 50 | 63479629 |
| Tuberculosis | 26.68 | 15.67 | 18 | 9325 | 11193 | 63468486 |
| Otitis media | 25.35 | 15.67 | 13 | 9330 | 4878 | 63474801 |
| Drug abuser | 25.09 | 15.67 | 11 | 9332 | 2912 | 63476767 |
| Thunderclap headache | 25.08 | 15.67 | 6 | 9337 | 225 | 63479454 |
| Colitis ischaemic | 25.02 | 15.67 | 17 | 9326 | 10691 | 63468988 |
| Oligohydramnios | 24.81 | 15.67 | 14 | 9329 | 6352 | 63473327 |
| Neutropenic sepsis | 24.68 | 15.67 | 20 | 9323 | 16418 | 63463261 |
| Oral herpes | 23.86 | 15.67 | 24 | 9319 | 26050 | 63453629 |
| Burns third degree | 23.48 | 15.67 | 6 | 9337 | 296 | 63479383 |
| Tuberculin test positive | 23.16 | 15.67 | 11 | 9332 | 3500 | 63476179 |
| Vitreous detachment | 21.97 | 15.67 | 9 | 9334 | 2018 | 63477661 |
| Insomnia | 20.56 | 15.67 | 74 | 9269 | 215178 | 63264501 |
| Dizziness | 19.61 | 15.67 | 119 | 9224 | 429806 | 63049873 |
| Mouth ulceration | 19.23 | 15.67 | 24 | 9319 | 32960 | 63446719 |
| Tension headache | 19.12 | 15.67 | 11 | 9332 | 5175 | 63474504 |
| Dust allergy | 18.46 | 15.67 | 6 | 9337 | 698 | 63478981 |
| Therapy partial responder | 18.22 | 15.67 | 14 | 9329 | 10644 | 63469035 |
| Myalgia | 18.12 | 15.67 | 55 | 9288 | 146474 | 63333205 |
| Arthropathy | 18.09 | 15.67 | 6 | 9337 | 234786 | 63244893 |
| Prinzmetal angina | 17.98 | 15.67 | 6 | 9337 | 758 | 63478921 |
| Renal infarct | 17.66 | 15.67 | 7 | 9336 | 1440 | 63478239 |
| Broad ligament tear | 17.64 | 15.67 | 3 | 9340 | 18 | 63479661 |
| Palpitations | 17.54 | 15.67 | 46 | 9297 | 112724 | 63366955 |
| Nausea | 17.47 | 15.67 | 197 | 9146 | 854274 | 62625405 |
| Nasal oedema | 17.32 | 15.67 | 7 | 9336 | 1515 | 63478164 |
| Serotonin syndrome | 16.93 | 15.67 | 21 | 9322 | 28661 | 63451018 |
| Patient isolation | 16.38 | 15.67 | 3 | 9340 | 29 | 63479650 |
| Carotid artery dissection | 16.01 | 15.67 | 4 | 9339 | 180 | 63479499 |
| Foetal hypokinesia | 15.98 | 15.67 | 5 | 9338 | 515 | 63479164 |
| Hemianopia | 15.80 | 15.67 | 6 | 9337 | 1101 | 63478578 |
| Dysphagia | 15.72 | 15.67 | 38 | 9305 | 88547 | 63391132 |
| Muscle discomfort | 15.72 | 15.67 | 4 | 9339 | 194 | 63479485 |
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 |
|---|---|---|---|---|---|---|
| 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 |
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 | 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 |
| Depression | 37.13 | 17.18 | 76 | 8525 | 216714 | 79519073 |
| Insomnia | 35.17 | 17.18 | 80 | 8521 | 245090 | 79490697 |
| Renal infarct | 32.96 | 17.18 | 12 | 8589 | 2679 | 79733108 |
| Blood thyroid stimulating hormone normal | 30.60 | 17.18 | 6 | 8595 | 119 | 79735668 |
| Polymenorrhagia | 28.78 | 17.18 | 5 | 8596 | 49 | 79735738 |
| Tuberculin test positive | 26.76 | 17.18 | 11 | 8590 | 3397 | 79732390 |
| Otitis media | 26.44 | 17.18 | 13 | 8588 | 6093 | 79729694 |
| Nervous system disorder | 25.52 | 17.18 | 22 | 8579 | 26834 | 79708953 |
| Palpitations | 24.81 | 17.18 | 47 | 8554 | 126563 | 79609224 |
| Colitis ischaemic | 24.25 | 17.18 | 17 | 8584 | 15342 | 79720445 |
| Drug abuser | 23.67 | 17.18 | 12 | 8589 | 6001 | 79729786 |
| Thunderclap headache | 23.58 | 17.18 | 6 | 8595 | 399 | 79735388 |
| Paraesthesia | 23.58 | 17.18 | 56 | 8545 | 176267 | 79559520 |
| Temperature intolerance | 23.36 | 17.18 | 14 | 8587 | 9691 | 79726096 |
| Dust allergy | 23.19 | 17.18 | 8 | 8593 | 1528 | 79734259 |
| Nausea | 23.09 | 17.18 | 179 | 8422 | 957017 | 78778770 |
| Nasal oedema | 22.28 | 17.18 | 8 | 8593 | 1716 | 79734071 |
| Vertigo | 22.12 | 17.18 | 32 | 8569 | 69050 | 79666737 |
| Antibody test positive | 21.88 | 17.18 | 9 | 8592 | 2783 | 79733004 |
| Meningoencephalitis bacterial | 21.35 | 17.18 | 5 | 8596 | 235 | 79735552 |
| Dysphagia | 21.10 | 17.18 | 43 | 8558 | 122093 | 79613694 |
| Throat tightness | 20.90 | 17.18 | 20 | 8581 | 27887 | 79707900 |
| Trigemino-cardiac reflex | 20.78 | 17.18 | 5 | 8596 | 264 | 79735523 |
| Vitreous detachment | 20.18 | 17.18 | 8 | 8593 | 2251 | 79733536 |
| Disturbance in attention | 19.99 | 17.18 | 26 | 8575 | 50775 | 79685012 |
| Dry eye | 19.60 | 17.18 | 22 | 8579 | 36909 | 79698878 |
| Neutropenic sepsis | 19.53 | 17.18 | 19 | 8582 | 27045 | 79708742 |
| Nasal discharge discolouration | 19.33 | 17.18 | 8 | 8593 | 2513 | 79733274 |
| Mouth ulceration | 18.90 | 17.18 | 22 | 8579 | 38372 | 79697415 |
| Bronchial obstruction | 18.61 | 17.18 | 8 | 8593 | 2760 | 79733027 |
| Vasospasm | 17.48 | 17.18 | 6 | 8595 | 1128 | 79734659 |
| Coronary artery dissection | 17.43 | 17.18 | 6 | 8595 | 1138 | 79734649 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N02CC03 | NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Selective serotonin (5HT1) 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 |
| CHEBI has role | CHEBI:35472 | anti-inflammatory drugs |
| CHEBI has role | CHEBI:35941 | serotonin 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 |
Drug Use | Suggest Off label Use Form| |View source of the data|
| 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 | |
| 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 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Peripheral vascular disease | contraindication | 400047006 | |
| Disorder of coronary artery | contraindication | 414024009 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
| Hypertensive urgency | contraindication | 443482000 |
🐶 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1D | GPCR | AGONIST | Ki | 8.90 | WOMBAT-PK | CHEMBL | |||
| 5-hydroxytryptamine receptor 1B | GPCR | AGONIST | Ki | 7.70 | WOMBAT-PK | CHEMBL | |||
| 5-hydroxytryptamine receptor 1E | GPCR | Ki | 7.70 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 6.60 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 1F | GPCR | Ki | 7.45 | WOMBAT-PK | |||||
| D(2) dopamine receptor | GPCR | Kd | 10.40 | CHEMBL | |||||
| D(1A) dopamine receptor | GPCR | Kd | 9.52 | CHEMBL | |||||
| Adrenergic receptor alpha-2 | GPCR | Kd | 8.15 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021094 | VUID |
| N0000148550 | NUI |
| D00415 | KEGG_DRUG |
| 4021094 | VANDF |
| C0528166 | UMLSCUI |
| CHEBI:10124 | CHEBI |
| CHEMBL1185 | ChEMBL_ID |
| DB00315 | DRUGBANK_ID |
| C089750 | MESH_SUPPLEMENTAL_RECORD_UI |
| 60857 | PUBCHEM_CID |
| 60 | IUPHAR_LIGAND_ID |
| 7408 | INN_ID |
| 2FS66TH3YW | UNII |
| 135775 | RXNORM |
| 11471 | MMSL |
| 52759 | MMSL |
| 5712 | MMSL |
| d04253 | MMSL |
| 006460 | NDDF |
| 108406003 | SNOMEDCT_US |
| 363582006 | SNOMEDCT_US |
Pharmaceutical products:
| 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 |
| ZOMIG | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-955 | SPRAY, METERED | 5 mg | NASAL | NDA | 28 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 |
| Zolmitriptan | Human Prescription Drug Label | 1 | 46708-182 | TABLET, ORALLY DISINTEGRATING | 5 mg | ORAL | ANDA | 25 sections |
| Zolmitriptan | Human Prescription Drug Label | 1 | 46708-462 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 25 sections |
| Zolmitriptan | Human Prescription Drug Label | 1 | 46708-462 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 25 sections |
| Zolmitriptan | Human Prescription Drug Label | 1 | 46708-463 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 25 sections |
| Zolmitriptan | Human Prescription Drug Label | 1 | 46708-463 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 25 sections |
| Zolmitriptan | Human Prescription Drug Label | 1 | 50742-625 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 25 sections |
| Zolmitriptan | Human Prescription Drug Label | 1 | 50742-626 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 25 sections |
| Zolmitriptan | Human Prescription Drug Label | 1 | 55700-943 | TABLET | 2.50 mg | ORAL | ANDA | 24 sections |
| Zolmitriptan | Human Prescription Drug Label | 1 | 55700-943 | TABLET | 2.50 mg | ORAL | ANDA | 24 sections |
| Zolmitriptan | Human Prescription Drug Label | 1 | 55700-944 | TABLET | 5 mg | ORAL | ANDA | 24 sections |
| Zolmitriptan | Human Prescription Drug Label | 1 | 55700-944 | TABLET | 5 mg | ORAL | ANDA | 24 sections |
| Zolmitriptan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59746-432 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 25 sections |
| Zolmitriptan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59746-433 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 25 sections |
| Zolmitriptan OD | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59746-461 | TABLET, ORALLY DISINTEGRATING | 2.50 mg | ORAL | ANDA | 26 sections |
| Zolmitriptan OD | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59746-462 | TABLET, ORALLY DISINTEGRATING | 5 mg | ORAL | ANDA | 26 sections |
| ZOMIG | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60846-2383 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 26 sections |
| ZOMIG | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60846-2384 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 26 sections |
| Zolmitriptan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63548-0101 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 25 sections |
| Zolmitriptan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63548-0101 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 25 sections |