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Identification
NameZolmitriptan
Accession NumberDB00315  (APRD00376)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Zolmitriptan is a synthetic tryptamine derivative and appears as a white powder that is readily soluble in water. [Wikipedia]

Structure
Thumb
Synonyms
(S)-4-({3-[2-(dimethylamino)ethyl]-1H-indol-5-yl}methyl)-1,3-oxazolidin-2-one
311C90
4-[[3-(2-Dimethylaminoethyl)-1H-indol-5-yl]methyl]oxazolidin-2-one
Zolmitriptan
Zolmitriptanum
Zomig
External Identifiers
  • 311 C 90
  • BW 311 C 90
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ag-zolmitriptan ODTtablet (orally disintegrating)2.5 mgoralAngita Pharma Inc.2015-12-10Not applicableCanada
Dom-zolmitriptantablet2.5 mgoralDominion Pharmacal2013-03-12Not applicableCanada
Dom-zolmitriptan ODTtablet (orally disintegrating)2.5 mgoralDominion PharmacalNot applicableNot applicableCanada
Ipg-zolmitriptantablet2.5 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Jamp-zolmitriptantablet2.5 mgoralJamp Pharma Corporation2014-03-13Not applicableCanada
Jamp-zolmitriptan ODTtablet (orally disintegrating)2.5 mgoralJamp Pharma Corporation2014-09-14Not applicableCanada
Mar-zolmitriptantablet2.5 mgoralMarcan Pharmaceuticals Inc2014-10-27Not applicableCanada
Mint-zolmitriptantablet2.5 mgoralMint Pharmaceuticals Inc2014-03-18Not applicableCanada
Mint-zolmitriptan ODTtablet (orally disintegrating)2.5 mgoralMint Pharmaceuticals Inc2014-03-18Not applicableCanada
Mylan-zolmitriptantablet2.5 mgoralMylan Pharmaceuticals Ulc2011-06-07Not applicableCanada
Mylan-zolmitriptan ODTtablet (orally disintegrating)2.5 mgoralMylan Pharmaceuticals Ulc2012-06-01Not applicableCanada
Nat-zolmitriptantablet2.5 mgoralNatco Pharma (Canada) Inc2015-02-17Not applicableCanada
PMS-zolmitriptantablet2.5 mgoralPharmascience Inc2011-06-07Not applicableCanada
PMS-zolmitriptan ODTtablet (orally disintegrating)2.5 mgoralPharmascience Inc2011-06-07Not applicableCanada
Ratio-zolmitriptan Irtablet (immediate release)2.5 mgoralRatiopharm Inc Division Of Teva Canada LimitedNot applicableNot applicableCanada
Ratio-zolmitriptan ODTtablet (orally disintegrating)2.5 mgoralRatiopharm Inc Division Of Teva Canada LimitedNot applicableNot applicableCanada
Riva-zolmitriptantablet2.5 mgoralLaboratoire Riva Inc2013-07-19Not applicableCanada
Sandoz Zolmitriptantablet2.5 mgoralSandoz Canada Incorporated2011-06-07Not applicableCanada
Sandoz Zolmitriptan ODTtablet (orally disintegrating)2.5 mgoralSandoz Canada Incorporated2011-06-07Not applicableCanada
Septa-zolmitriptan-odttablet (orally disintegrating)2.5 mgoralSepta Pharmaceuticals Inc2014-10-30Not applicableCanada
Teva-zolmitriptantablet1.0 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Teva-zolmitriptantablet2.5 mgoralTeva Canada Limited2011-06-07Not applicableCanada
Teva-zolmitriptan ODtablet (orally disintegrating)1 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Teva-zolmitriptan ODtablet (orally disintegrating)2.5 mgoralTeva Canada Limited2011-06-07Not applicableCanada
Van-zolmitriptantablet2.5 mgoralVanc Pharmaceuticals IncNot applicableNot applicableCanada
Van-zolmitriptan ODTtablet (orally disintegrating)2.5 mgoralVanc Pharmaceuticals Inc2015-11-04Not applicableCanada
Zolmitriptantablet2.5 mgoralJubilant Generics LimitedNot applicableNot applicableCanada
Zolmitriptantablet2.5 mg/1oralGlobal Pharmaceuticals, Division of Impax Laboratories Inc.2013-05-14Not applicableUs
Zolmitriptantablet2.5 mgoralSanis Health Inc2015-10-14Not applicableCanada
Zolmitriptantablet5 mg/1oralGlobal Pharmaceuticals, Division of Impax Laboratories Inc.2013-05-14Not applicableUs
Zolmitriptantablet2.5 mgoralPro Doc Limitee2012-03-29Not applicableCanada
Zolmitriptan ODTtablet (orally disintegrating)2.5 mgoralSanis Health Inc2015-10-14Not applicableCanada
Zolmitriptan ODTtablet (orally disintegrating)2.5 mgoralPro Doc Limitee2012-03-29Not applicableCanada
Zolmitriptan Orally Disintegratingtablet, orally disintegrating5 mg/1oralGlobal Pharmaceuticals, Division of Impax Laboratories Inc.2013-05-14Not applicableUs
Zolmitriptan Orally Disintegratingtablet, orally disintegrating2.5 mg/1oralGlobal Pharmaceuticals, Division of Impax Laboratories Inc.2013-05-14Not applicableUs
Zolmitriptan-odttablet (orally disintegrating)2.5 mgoralJubilant Generics LimitedNot applicableNot applicableCanada
Zomigtablet5 mg/1oralAstra Zeneca Pharmaceuticals Lp1998-01-102016-03-16Us
Zomigspray, metered2.5 mg/1nasalImpax Specialty Pharma2013-12-06Not applicableUs
Zomigtablet5 mg/1oralDispensing Solutions, Inc.2010-05-18Not applicableUs
Zomigtablet2.5 mg/1oralAstra Zeneca Pharmaceuticals Lp1998-01-102016-03-16Us
Zomigspray, metered5 mg/1nasalImpax Specialty Pharma2012-07-02Not applicableUs
Zomigspray, metered5 mg/1nasalAstra Zeneca Pharmaceuticals Lp2003-10-202016-03-16Us
Zomigtablet5 mg/1oralImpax Laboratories, Inc.2012-04-02Not applicableUs
Zomigtablet2.5 mg/1oralImpax Laboratories, Inc.2012-04-02Not applicableUs
Zomigspray, metered5 mg/1nasalRebel Distributors Corp2010-06-08Not applicableUs
Zomig Nasal Sprayspray2.5 mgnasal; oralAstrazeneca Canada Inc2004-12-23Not applicableCanada
Zomig Nasal Sprayspray5.0 mgnasal; oralAstrazeneca Canada Inc2004-12-23Not applicableCanada
Zomig Rapimelttablet (orally disintegrating)2.5 mgoralAstrazeneca Canada Inc2001-03-05Not applicableCanada
Zomig Tab 2.5 mgtablet2.5 mgoralAstrazeneca Canada Inc1998-09-30Not applicableCanada
Zomig Zmttablet, orally disintegrating5 mg/1oralAstra Zeneca Pharmaceuticals Lp2001-10-012016-03-16Us
Zomig Zmttablet, orally disintegrating5 mg/1oralImpax Laboratories, Inc.2012-07-02Not applicableUs
Zomig Zmttablet, orally disintegrating2.5 mg/1oralAstra Zeneca Pharmaceuticals Lp2001-04-022016-03-16Us
Zomig Zmttablet, orally disintegrating2.5 mg/1oralImpax Laboratories, Inc.2012-07-02Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-zolmitriptantablet2.5 mgoralApotex IncNot applicableNot applicableCanada
Apo-zolmitriptan Rapidtablet (orally disintegrating)2.5 mgoralApotex IncNot applicableNot applicableCanada
Zolmiptriptantablet, orally disintegrating5 mg/1oralGlenmark Pharmaceuticals Inc., Usa2013-05-14Not applicableUs
Zolmiptriptantablet, orally disintegrating2.5 mg/1oralGlenmark Pharmaceuticals Inc., Usa2013-05-14Not applicableUs
Zolmitriptantablet, orally disintegrating2.5 mg/1oralApotex Corp2013-05-14Not applicableUs
Zolmitriptantablet, film coated2.5 mg/1oralSun Pharma Global FZE2014-11-24Not applicableUs
Zolmitriptantablet, film coated2.5 mg/1oralMylan Pharmaceuticals Inc.2013-05-14Not applicableUs
Zolmitriptantablet, film coated5 mg/1oralGlenmark Pharmaceuticals Inc., Usa2013-05-14Not applicableUs
Zolmitriptantablet, orally disintegrating5 mg/1oralApotex Corp2013-05-14Not applicableUs
Zolmitriptantablet, film coated5 mg/1oralApotex Corp2013-05-14Not applicableUs
Zolmitriptantablet, orally disintegrating5 mg/1oralMacleods Pharmaceuticals Limited2015-10-22Not applicableUs
Zolmitriptantablet, film coated2.5 mg/1oralGlenmark Pharmaceuticals Inc., Usa2013-05-14Not applicableUs
Zolmitriptantablet, film coated2.5 mg/1oralApotex Corp2013-05-14Not applicableUs
Zolmitriptantablet, orally disintegrating2.5 mg/1oralMacleods Pharmaceuticals Limited2015-10-22Not applicableUs
Zolmitriptantablet, orally disintegrating5 mg/1oralZydus Pharmaceuticals (USA) Inc.2013-05-16Not applicableUs
Zolmitriptantablet, film coated5 mg/1oralMacleods Pharmaceuticals Limited2015-09-30Not applicableUs
Zolmitriptantablet, orally disintegrating2.5 mg/1oralZydus Pharmaceuticals (USA) Inc.2013-05-16Not applicableUs
Zolmitriptantablet, film coated2.5 mg/1oralMacleods Pharmaceuticals Limited2015-09-30Not applicableUs
Zolmitriptantablet, film coated5 mg/1oralRising Pharmaceuticals, Inc.2016-01-04Not applicableUs
Zolmitriptantablet, film coated5 mg/1oralBlue Point Laboratories2014-03-13Not applicableUs
Zolmitriptantablet, film coated2.5 mg/1oralRising Pharmaceuticals, Inc.2016-01-04Not applicableUs
Zolmitriptantablet, film coated2.5 mg/1oralBlue Point Laboratories2014-03-13Not applicableUs
Zolmitriptantablet, film coated5 mg/1oralJubilant Cadista Pharmaceuticals Inc.2014-11-20Not applicableUs
Zolmitriptantablet, film coated5 mg/1oralCamber Pharmaceuticals Inc2015-01-05Not applicableUs
Zolmitriptantablet, orally disintegrating5 mg/1oralCadila Healthcare Limited2013-05-16Not applicableUs
Zolmitriptantablet, film coated2.5 mg/1oralJubilant Cadista Pharmaceuticals Inc.2014-11-20Not applicableUs
Zolmitriptantablet, film coated2.5 mg/1oralCamber Pharmaceuticals Inc2015-01-05Not applicableUs
Zolmitriptantablet, orally disintegrating2.5 mg/1oralCadila Healthcare Limited2013-05-16Not applicableUs
Zolmitriptantablet, film coated5 mg/1oralSun Pharma Global FZE2014-11-24Not applicableUs
Zolmitriptantablet, film coated5 mg/1oralMylan Pharmaceuticals Inc.2013-05-14Not applicableUs
Zolmitriptan ODtablet, orally disintegrating5 mg/1oralJubilant Cadista Pharmaceuticals Inc.2015-09-17Not applicableUs
Zolmitriptan ODtablet, orally disintegrating2.5 mg/1oralJubilant Cadista Pharmaceuticals Inc.2015-09-17Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AscoTopAstraZeneca
NomiSquare
ZolmilesActavis
ZolmitBeximco
ZomigonAstraZeneca
ZomigoroAstraZeneca
ZomitanIncepta
Brand mixturesNot Available
SaltsNot Available
Categories
UNII2FS66TH3YW
CAS number139264-17-8
WeightAverage: 287.3568
Monoisotopic: 287.163376931
Chemical FormulaC16H21N3O2
InChI KeyInChIKey=ULSDMUVEXKOYBU-ZDUSSCGKSA-N
InChI
InChI=1S/C16H21N3O2/c1-19(2)6-5-12-9-17-15-4-3-11(8-14(12)15)7-13-10-21-16(20)18-13/h3-4,8-9,13,17H,5-7,10H2,1-2H3,(H,18,20)/t13-/m0/s1
IUPAC Name
(4S)-4-({3-[2-(dimethylamino)ethyl]-1H-indol-5-yl}methyl)-1,3-oxazolidin-2-one
SMILES
CN(C)CCC1=CNC2=CC=C(C[[email protected]]3COC(=O)N3)C=C12
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as tryptamines and derivatives. These are compounds containing the tryptamine backbone, which is structurally characterized by an indole ring subsituted at the 3-position by an ethanamine.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassIndoles and derivatives
Sub ClassTryptamines and derivatives
Direct ParentTryptamines and derivatives
Alternative Parents
Substituents
  • Tryptamine
  • Indole
  • Aralkylamine
  • Benzenoid
  • Substituted pyrrole
  • Oxazolidinone
  • Heteroaromatic compound
  • Pyrrole
  • Oxazolidine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Oxacycle
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the acute treatment of adult migraine with or without auras.
PharmacodynamicsZolmitriptan is a selective agonist of serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptors. It is structurally and pharmacologically related to other selective 5-HT1B/1D receptor agonists, and has only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity or pharmacological activity at 5-HT2, 5-HT3 or 5-HT4 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Zolmitriptan also activates 5-HT1 receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Zolmitriptan in humans.
Mechanism of actionZolmitriptan binds with high affinity to human 5-HT1B and 5-HT1D receptors leading to cranial blood vessel constriction. Current theories proposed to explain the etiology of migraine headache suggest that symptoms are 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 zolmitriptan for the treatment of migraine headache can most likely be attributed to the agonist effects at the 5HT1B/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.
Related Articles
AbsorptionMean absolute oral bioavailability is approximately 40%. Food has no affect on the rate and extent of absorption.
Volume of distribution
  • 8.4±3.3 L/kg
Protein binding25%
Metabolism

Hepatic. There have been three metabolites identified: indole acetic acid, N -oxide, and N-desmethyl metabolites. However, the N-desmethyl is the only active metabolite.

SubstrateEnzymesProduct
Zolmitriptan
norzolmitripanDetails
Zolmitriptan
Not Available
Indole acetic acidDetails
Route of eliminationNot Available
Half lifeThe mean elimination half-life of zolmitriptan and of the active N-desmethyl metabolite is 3 hours.
Clearance
  • 25.9 mL/min/kg
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3
Gene symbol: GNB3
UniProt: P16520
rs5443 Not AvailableT AlleleBetter response to drug treatment17361120
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.8956
Caco-2 permeable-0.8957
P-glycoprotein substrateSubstrate0.6888
P-glycoprotein inhibitor INon-inhibitor0.8782
P-glycoprotein inhibitor IINon-inhibitor0.8383
Renal organic cation transporterNon-inhibitor0.7674
CYP450 2C9 substrateNon-substrate0.8051
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.5822
CYP450 1A2 substrateNon-inhibitor0.6189
CYP450 2C9 inhibitorNon-inhibitor0.8989
CYP450 2D6 inhibitorNon-inhibitor0.8281
CYP450 2C19 inhibitorNon-inhibitor0.831
CYP450 3A4 inhibitorNon-inhibitor0.8481
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9263
Ames testNon AMES toxic0.7651
CarcinogenicityNon-carcinogens0.9641
BiodegradationNot ready biodegradable0.9961
Rat acute toxicity2.5965 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9301
hERG inhibition (predictor II)Non-inhibitor0.8949
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Astrazeneca pharmaceuticals lp
  • Ipr pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Tablet (immediate release)oral2.5 mg
Tabletoral1.0 mg
Tablet (orally disintegrating)oral1 mg
Tabletoral2.5 mg/1
Tabletoral5 mg/1
Tablet, film coatedoral2.5 mg/1
Tablet, film coatedoral5 mg/1
Tablet, orally disintegratingoral2.5 mg/1
Tablet, orally disintegratingoral5 mg/1
Spray, meterednasal2.5 mg/1
Spray, meterednasal5 mg/1
Spraynasal; oral2.5 mg
Spraynasal; oral5.0 mg
Tablet (orally disintegrating)oral2.5 mg
Tabletoral2.5 mg
Prices
Unit descriptionCostUnit
Zomig 6 5 mg Solution 1 Box = 6 Single Use Bottles235.62USD bottle
Zomig ZMT 6 2.5 mg Dispersible Tablet Box159.66USD box
Zomig 6 2.5 mg tablet 1 Box = 6 tablet147.23USD box
Zomig 3 5 mg tablet Box93.49USD box
Zomig ZMT 3 5 mg Dispersible Tablet Box88.21USD box
Zomig 5 mg nasal spray37.76USD each
Zomig 5 mg tablet28.82USD tablet
Zomig zmt 5 mg tablet28.27USD tablet
Zomig 2.5 mg tablet26.08USD tablet
Zomig zmt 2.5 mg tablet25.59USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2064815 No1999-11-162011-06-06Canada
CA2572508 No2010-03-302016-08-02Canada
US5466699 No1992-11-142012-11-14Us
US6750237 Yes2001-05-282021-05-28Us
US7220767 Yes2001-05-282021-05-28Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP1.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.19 mg/mLALOGPS
logP2.25ALOGPS
logP2.04ChemAxon
logS-3.2ALOGPS
pKa (Strongest Acidic)13ChemAxon
pKa (Strongest Basic)9.55ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area57.36 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity82.44 m3·mol-1ChemAxon
Polarizability31.65 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Islam Aminul, Bhar Chandan, Katam Sahadev, “Process for preparing optically pure zolmitriptan.” U.S. Patent US20050245585, issued November 03, 2005.

US20050245585
General References
  1. Pascual J: [Mechanism of action of zolmitriptan]. Neurologia. 1998 Oct;13 Suppl 2:9-15. [PubMed:9859690 ]
  2. Martin GR: Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine. Cephalalgia. 1997 Oct;17 Suppl 18:4-14. [PubMed:9399012 ]
External Links
ATC CodesN02CC03
AHFS Codes
  • 28:32.28
PDB EntriesNot Available
FDA labelDownload (101 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcepromazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Acetophenazine.
AmisulprideThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Amisulpride.
AripiprazoleThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Aripiprazole.
BenzquinamideThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Benzquinamide.
CabergolineCabergoline may increase the vasoconstricting activities of Zolmitriptan.
CarphenazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Carphenazine.
ChlormezanoneThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Chlorprothixene.
CimetidineThe serum concentration of Zolmitriptan can be increased when it is combined with Cimetidine.
ClozapineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Clozapine.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Zolmitriptan.
DroperidolThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Droperidol.
DroxidopaZolmitriptan may increase the hypertensive activities of Droxidopa.
FencamfamineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Fencamfamine.
FlupentixolThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Fluspirilene.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Zolmitriptan.
GranisetronGranisetron may increase the serotonergic activities of Zolmitriptan.
HaloperidolThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Haloperidol.
LoxapineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Loxapine.
MesoridazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Mesoridazine.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Methotrimeprazine.
MetoclopramideThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Metoclopramide.
MolindoneThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Molindone.
OlanzapineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Ondansetron.
PaliperidoneThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Paliperidone.
PerphenazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Perphenazine.
PhenelzineThe metabolism of Zolmitriptan can be decreased when combined with Phenelzine.
PimozideThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Piperacetazine.
ProchlorperazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Promazine.
PropranololThe serum concentration of Zolmitriptan can be increased when it is combined with Propranolol.
QuetiapineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Quetiapine.
RemoxiprideThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Reserpine.
RisperidoneThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Risperidone.
SertindoleThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Sertindole.
SulpirideThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Sulpiride.
ThioridazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Thiothixene.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Zolmitriptan.
TranylcypromineThe metabolism of Zolmitriptan can be decreased when combined with Tranylcypromine.
TrifluoperazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Triflupromazine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Ziprasidone.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Zuclopenthixol.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of ...
Gene Name:
HTR1B
Uniprot ID:
P28222
Molecular Weight:
43567.535 Da
References
  1. Le Grand B, Panissie A, Perez M, Pauwels PJ, John GW: Zolmitriptan stimulates a Ca(2+)-dependent K(+) current in C6 glioma cells stably expressing recombinant human 5-HT(1B) receptors. Eur J Pharmacol. 2000 Jun 2;397(2-3):297-302. [PubMed:10844127 ]
  2. Johnson DE, Rollema H, Schmidt AW, McHarg AD: Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain. Eur J Pharmacol. 2001 Aug 17;425(3):203-10. [PubMed:11513839 ]
  3. de Almeida RM, Nikulina EM, Faccidomo S, Fish EW, Miczek KA: Zolmitriptan--a 5-HT1B/D agonist, alcohol, and aggression in mice. Psychopharmacology (Berl). 2001 Sep;157(2):131-41. [PubMed:11594437 ]
  4. Reuter U, Salomone S, Ickenstein GW, Waeber C: Effects of chronic sumatriptan and zolmitriptan treatment on 5-HT receptor expression and function in rats. Cephalalgia. 2004 May;24(5):398-407. [PubMed:15096229 ]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  6. Whale R, Bhagwagar Z, Cowen PJ: Zolmitriptan-induced growth hormone release in humans: mediation by 5-HT1D receptors? Psychopharmacology (Berl). 1999 Jul;145(2):223-6. [PubMed:10463324 ]
  7. Hargreaves RJ, Shepheard SL: Pathophysiology of migraine--new insights. Can J Neurol Sci. 1999 Nov;26 Suppl 3:S12-9. [PubMed:10563228 ]
  8. Gowin JL, Swann AC, Moeller FG, Lane SD: Zolmitriptan and human aggression: interaction with alcohol. Psychopharmacology (Berl). 2010 Jul;210(4):521-31. doi: 10.1007/s00213-010-1851-6. Epub 2010 Apr 21. [PubMed:20407761 ]
  9. Pascual J: [Mechanism of action of zolmitriptan]. Neurologia. 1998 Oct;13 Suppl 2:9-15. [PubMed:9859690 ]
  10. Martin GR: Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine. Cephalalgia. 1997 Oct;17 Suppl 18:4-14. [PubMed:9399012 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate c...
Gene Name:
HTR1D
Uniprot ID:
P28221
Molecular Weight:
41906.38 Da
References
  1. Whale R, Bhagwagar Z, Cowen PJ: Zolmitriptan-induced growth hormone release in humans: mediation by 5-HT1D receptors? Psychopharmacology (Berl). 1999 Jul;145(2):223-6. [PubMed:10463324 ]
  2. Hargreaves RJ, Shepheard SL: Pathophysiology of migraine--new insights. Can J Neurol Sci. 1999 Nov;26 Suppl 3:S12-9. [PubMed:10563228 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  4. Le Grand B, Panissie A, Perez M, Pauwels PJ, John GW: Zolmitriptan stimulates a Ca(2+)-dependent K(+) current in C6 glioma cells stably expressing recombinant human 5-HT(1B) receptors. Eur J Pharmacol. 2000 Jun 2;397(2-3):297-302. [PubMed:10844127 ]
  5. Johnson DE, Rollema H, Schmidt AW, McHarg AD: Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain. Eur J Pharmacol. 2001 Aug 17;425(3):203-10. [PubMed:11513839 ]
  6. de Almeida RM, Nikulina EM, Faccidomo S, Fish EW, Miczek KA: Zolmitriptan--a 5-HT1B/D agonist, alcohol, and aggression in mice. Psychopharmacology (Berl). 2001 Sep;157(2):131-41. [PubMed:11594437 ]
  7. Reuter U, Salomone S, Ickenstein GW, Waeber C: Effects of chronic sumatriptan and zolmitriptan treatment on 5-HT receptor expression and function in rats. Cephalalgia. 2004 May;24(5):398-407. [PubMed:15096229 ]
  8. Gowin JL, Swann AC, Moeller FG, Lane SD: Zolmitriptan and human aggression: interaction with alcohol. Psychopharmacology (Berl). 2010 Jul;210(4):521-31. doi: 10.1007/s00213-010-1851-6. Epub 2010 Apr 21. [PubMed:20407761 ]
  9. Pascual J: [Mechanism of action of zolmitriptan]. Neurologia. 1998 Oct;13 Suppl 2:9-15. [PubMed:9859690 ]
  10. Martin GR: Pre-clinical pharmacology of zolmitriptan (Zomig; formerly 311C90), a centrally and peripherally acting 5HT1B/1D agonist for migraine. Cephalalgia. 1997 Oct;17 Suppl 18:4-14. [PubMed:9399012 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity.
Gene Name:
HTR1F
Uniprot ID:
P30939
Molecular Weight:
41708.505 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Reuter U, Salomone S, Ickenstein GW, Waeber C: Effects of chronic sumatriptan and zolmitriptan treatment on 5-HT receptor expression and function in rats. Cephalalgia. 2004 May;24(5):398-407. [PubMed:15096229 ]
  3. Villalon CM, Centurion D, Valdivia LF, de Vries P, Saxena PR: Migraine: pathophysiology, pharmacology, treatment and future trends. Curr Vasc Pharmacol. 2003 Mar;1(1):71-84. [PubMed:15320857 ]
  4. Villalon CM, Centurion D, Valdivia LF, De Vries P, Saxena PR: An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy. Proc West Pharmacol Soc. 2002;45:199-210. [PubMed:12434581 ]
  5. Bhalla P, Sharma HS, Wurch T, Pauwels PJ, Saxena PR: Molecular cloning and expression of the porcine trigeminal ganglion cDNA encoding a 5-ht(1F) receptor. Eur J Pharmacol. 2002 Feb 1;436(1-2):23-33. [PubMed:11834243 ]
  6. Wainscott DB, Johnson KW, Phebus LA, Schaus JM, Nelson DL: Human 5-HT1F receptor-stimulated [35S]GTPgammaS binding: correlation with inhibition of guinea pig dural plasma protein extravasation. Eur J Pharmacol. 1998 Jul 3;352(1):117-24. [PubMed:9718276 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
References
  1. Johnson DE, Rollema H, Schmidt AW, McHarg AD: Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain. Eur J Pharmacol. 2001 Aug 17;425(3):203-10. [PubMed:11513839 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Serotonin binding
Specific Function:
Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. MAOA preferentially oxidizes biogenic amines such as 5-hydroxytryptamine (5-HT), norepinephrine and epinephrine.
Gene Name:
MAOA
Uniprot ID:
P21397
Molecular Weight:
59681.27 Da
References
  1. Rolan P: Potential drug interactions with the novel antimigraine compound zolmitriptan (Zomig, 311C90). Cephalalgia. 1997 Oct;17 Suppl 18:21-7. [PubMed:9399014 ]
  2. Wild MJ, McKillop D, Butters CJ: Determination of the human cytochrome P450 isoforms involved in the metabolism of zolmitriptan. Xenobiotica. 1999 Aug;29(8):847-57. [PubMed:10553725 ]
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Drug created on June 13, 2005 07:24 / Updated on May 25, 2016 03:19