Stem definition | Drug id | CAS RN |
---|---|---|
serotonin (5-HT1) receptor agonists, sumatriptan derivatives | 2869 | 139264-17-8 |
Dose | Unit | Route |
---|---|---|
2.50 | mg | N |
2.50 | mg | O |
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 ยตM/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 |
Date | Agency | Company | Orphan |
---|---|---|---|
Nov. 25, 1997 | FDA | IPR |
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 | 146.22 | 17.44 | 108 | 7605 | 75172 | 50522239 |
Medication overuse headache | 113.99 | 17.44 | 25 | 7688 | 610 | 50596801 |
Paranasal cyst | 44.00 | 17.44 | 10 | 7703 | 288 | 50597123 |
Vascular malformation | 43.83 | 17.44 | 10 | 7703 | 293 | 50597118 |
Monocyte count abnormal | 43.22 | 17.44 | 9 | 7704 | 170 | 50597241 |
Infrequent bowel movements | 39.02 | 17.44 | 12 | 7701 | 1126 | 50596285 |
Mastoiditis | 38.15 | 17.44 | 11 | 7702 | 827 | 50596584 |
Headache | 34.99 | 17.44 | 161 | 7552 | 506374 | 50091037 |
Urticaria chronic | 33.87 | 17.44 | 9 | 7704 | 500 | 50596911 |
Skin candida | 33.18 | 17.44 | 11 | 7702 | 1315 | 50596096 |
Lymphocyte count abnormal | 31.97 | 17.44 | 9 | 7704 | 621 | 50596790 |
Dyspnoea exertional | 31.60 | 17.44 | 39 | 7674 | 51194 | 50546217 |
Antibody test positive | 30.70 | 17.44 | 12 | 7701 | 2299 | 50595112 |
Depression | 29.97 | 17.44 | 73 | 7640 | 165350 | 50432061 |
Temperature intolerance | 29.97 | 17.44 | 17 | 7696 | 7522 | 50589889 |
Vertigo | 29.65 | 17.44 | 38 | 7675 | 51794 | 50545617 |
Blood thyroid stimulating hormone normal | 28.63 | 17.44 | 6 | 7707 | 117 | 50597294 |
Polymenorrhagia | 27.44 | 17.44 | 5 | 7708 | 45 | 50597366 |
Oral herpes | 25.85 | 17.44 | 23 | 7690 | 20702 | 50576709 |
Oligohydramnios | 25.68 | 17.44 | 14 | 7699 | 5736 | 50591675 |
Tuberculosis | 25.41 | 17.44 | 17 | 7696 | 10066 | 50587345 |
Drug abuser | 25.07 | 17.44 | 11 | 7702 | 2817 | 50594594 |
Insomnia | 24.37 | 17.44 | 70 | 7643 | 174795 | 50422616 |
Vitreous detachment | 22.72 | 17.44 | 9 | 7704 | 1785 | 50595626 |
Tension headache | 22.21 | 17.44 | 10 | 7703 | 2721 | 50594690 |
Colitis ischaemic | 21.55 | 17.44 | 15 | 7698 | 9468 | 50587943 |
Tuberculin test positive | 20.74 | 17.44 | 10 | 7703 | 3176 | 50594235 |
Drug effect less than expected | 20.62 | 17.44 | 6 | 7707 | 466 | 50596945 |
Otitis media | 20.57 | 17.44 | 11 | 7702 | 4338 | 50593073 |
Dry mouth | 20.12 | 17.44 | 33 | 7680 | 56145 | 50541266 |
Myalgia | 19.52 | 17.44 | 52 | 7661 | 124267 | 50473144 |
Dizziness | 18.13 | 17.44 | 102 | 7611 | 346267 | 50251144 |
Renal infarct | 17.85 | 17.44 | 7 | 7706 | 1353 | 50596058 |
Broad ligament tear | 17.53 | 17.44 | 3 | 7710 | 18 | 50597393 |
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 |
---|---|---|---|---|---|---|
Therapy partial responder | 48.90 | 29.70 | 14 | 894 | 5185 | 29568434 |
Paraesthesia | 39.46 | 29.70 | 23 | 885 | 53822 | 29519797 |
Migraine | 36.92 | 29.70 | 14 | 894 | 12416 | 29561203 |
Insomnia | 33.41 | 29.70 | 25 | 883 | 88736 | 29484883 |
Craniosynostosis | 32.65 | 29.70 | 6 | 902 | 307 | 29573312 |
Drug abuse | 31.17 | 29.70 | 23 | 885 | 79860 | 29493759 |
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 | 161.88 | 18.41 | 95 | 6981 | 62582 | 64429074 |
Medication overuse headache | 131.03 | 18.41 | 27 | 7049 | 683 | 64490973 |
Therapy partial responder | 56.83 | 18.41 | 26 | 7050 | 10222 | 64481434 |
Vascular malformation | 47.14 | 18.41 | 10 | 7066 | 292 | 64491364 |
Headache | 46.27 | 18.41 | 145 | 6931 | 529322 | 63962334 |
Paranasal cyst | 45.84 | 18.41 | 10 | 7066 | 334 | 64491322 |
Insomnia | 42.43 | 18.41 | 77 | 6999 | 197759 | 64293897 |
Mastoiditis | 35.80 | 18.41 | 11 | 7065 | 1434 | 64490222 |
Depression | 35.12 | 18.41 | 68 | 7008 | 183223 | 64308433 |
Renal infarct | 34.05 | 18.41 | 12 | 7064 | 2399 | 64489257 |
Skin candida | 34.03 | 18.41 | 11 | 7065 | 1692 | 64489964 |
Burns third degree | 33.52 | 18.41 | 8 | 7068 | 401 | 64491255 |
Blood thyroid stimulating hormone normal | 30.50 | 18.41 | 6 | 7070 | 119 | 64491537 |
Paraesthesia | 29.62 | 18.41 | 53 | 7023 | 134469 | 64357187 |
Polymenorrhagia | 29.18 | 18.41 | 5 | 7071 | 44 | 64491612 |
Tuberculin test positive | 24.26 | 18.41 | 10 | 7066 | 3058 | 64488598 |
Palpitations | 24.07 | 18.41 | 42 | 7034 | 104446 | 64387210 |
Drug abuser | 23.87 | 18.41 | 12 | 7064 | 5796 | 64485860 |
Vertigo | 22.52 | 18.41 | 30 | 7046 | 58981 | 64432675 |
Meningoencephalitis bacterial | 22.45 | 18.41 | 5 | 7071 | 184 | 64491472 |
Nasal oedema | 22.15 | 18.41 | 7 | 7069 | 1001 | 64490655 |
Drug effect less than expected | 21.91 | 18.41 | 6 | 7070 | 521 | 64491135 |
Dust allergy | 21.85 | 18.41 | 7 | 7069 | 1046 | 64490610 |
Dry eye | 21.82 | 18.41 | 21 | 7055 | 28998 | 64462658 |
Throat tightness | 21.79 | 18.41 | 19 | 7057 | 23141 | 64468515 |
Otitis media | 21.71 | 18.41 | 11 | 7065 | 5402 | 64486254 |
Colitis ischaemic | 21.31 | 18.41 | 15 | 7061 | 13399 | 64478257 |
Vitreous detachment | 21.22 | 18.41 | 8 | 7068 | 1936 | 64489720 |
Trigemino-cardiac reflex | 21.18 | 18.41 | 5 | 7071 | 239 | 64491417 |
Disturbance in attention | 20.68 | 18.41 | 24 | 7052 | 41050 | 64450606 |
Nausea | 20.15 | 18.41 | 151 | 6925 | 785649 | 63706007 |
Tension headache | 20.07 | 18.41 | 9 | 7067 | 3374 | 64488282 |
Temperature intolerance | 19.92 | 18.41 | 12 | 7064 | 8243 | 64483413 |
Tinnitus | 18.97 | 18.41 | 21 | 7055 | 34112 | 64457544 |
Vasospasm | 18.50 | 18.41 | 6 | 7070 | 932 | 64490724 |
None
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 |
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 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 13.47 | acidic |
pKa2 | 8.28 | Basic |
None
None
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 |
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 |
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 | 46708-182 | 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 | 46708-463 | 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 | 55700-944 | 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 |
Zolmitriptan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63548-0101 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 25 sections |
Zolmitriptan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63548-0102 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 25 sections |
ZOMIG | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64896-671 | TABLET | 2.50 mg | ORAL | NDA | 25 sections |
ZOMIG | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64896-672 | TABLET | 5 mg | ORAL | NDA | 25 sections |
ZOMIG | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64896-681 | SPRAY, METERED | 5 mg | NASAL | NDA | 26 sections |
ZOMIG | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64896-682 | SPRAY, METERED | 2.50 mg | NASAL | NDA | 26 sections |
ZOMIG ZMT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64896-691 | TABLET, ORALLY DISINTEGRATING | 2.50 mg | ORAL | NDA | 25 sections |
ZOMIG ZMT | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64896-692 | TABLET, ORALLY DISINTEGRATING | 5 mg | ORAL | NDA | 25 sections |
Zolmitriptan | Human Prescription Drug Label | 1 | 64980-203 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 25 sections |
Zolmitriptan | Human Prescription Drug Label | 1 | 64980-204 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 25 sections |