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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
SynonymLanguageCode
(S)-4-({3-[2-(dimethylamino)ethyl]-1H-indol-5-yl}methyl)-1,3-oxazolidin-2-oneNot AvailableIUPAC
ZolmitriptanNot AvailableUSAN, BAN
ZolmitriptanumLatinINN
SaltsNot Available
Brand names
NameCompany
AscoTopAstraZeneca
NomiSquare
ZolmilesActavis
ZolmitBeximco
ZomigAstraZeneca
Zomig RapimeltAstraZeneca
ZomigonAstraZeneca
ZomigoroAstraZeneca
ZomitanIncepta
Brand mixturesNot Available
Categories
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[C@H]3COC(=O)N3)C=C12
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassHeterocyclic Compounds
ClassIndoles and Derivatives
SubclassTryptamines and Derivatives
Direct parentTryptamines and Derivatives
Alternative parentsIndoles; Oxazolidinediones; Benzene and Substituted Derivatives; Substituted Pyrroles; Tertiary Amines; Carbamic Acids and Derivatives; Polyamines
Substituentsindole; oxazolidinedione; substituted pyrrole; benzene; pyrrole; oxazolidine; carbamic acid derivative; tertiary amine; polyamine; amine; organonitrogen compound
Classification descriptionThis compound belongs to the tryptamines and derivatives. These are compounds containing the tryptamine backbone, which is structurally characterized by an indole ring subsituted at the thrid position by an ethanamine.
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.
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
    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
    Property Value Probability
    Human Intestinal Absorption + 1.0
    Blood Brain Barrier + 0.8956
    Caco-2 permeable - 0.8957
    P-glycoprotein substrate Substrate 0.6888
    P-glycoprotein inhibitor I Non-inhibitor 0.8782
    P-glycoprotein inhibitor II Non-inhibitor 0.8383
    Renal organic cation transporter Non-inhibitor 0.7674
    CYP450 2C9 substrate Non-substrate 0.8051
    CYP450 2D6 substrate Non-substrate 0.9116
    CYP450 3A4 substrate Substrate 0.5822
    CYP450 1A2 substrate Non-inhibitor 0.6189
    CYP450 2C9 substrate Non-inhibitor 0.8989
    CYP450 2D6 substrate Non-inhibitor 0.8281
    CYP450 2C19 substrate Non-inhibitor 0.831
    CYP450 3A4 substrate Non-inhibitor 0.8481
    CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9263
    Ames test Non AMES toxic 0.7651
    Carcinogenicity Non-carcinogens 0.9641
    Biodegradation Not ready biodegradable 0.9961
    Rat acute toxicity 2.5965 LD50, mol/kg Not applicable
    hERG inhibition (predictor I) Weak inhibitor 0.9301
    hERG inhibition (predictor II) Non-inhibitor 0.8949
    Pharmacoeconomics
    Manufacturers
    • Astrazeneca pharmaceuticals lp
    • Ipr pharmaceuticals inc
    Packagers
    Dosage forms
    FormRouteStrength
    SprayNasal
    TabletOral
    Prices
    Unit descriptionCostUnit
    Zomig 6 5 mg Solution 1 Box = 6 Single Use Bottles235.62USDbottle
    Zomig ZMT 6 2.5 mg Dispersible Tablet Box159.66USDbox
    Zomig 6 2.5 mg tablet 1 Box = 6 tablet147.23USDbox
    Zomig 3 5 mg tablet Box93.49USDbox
    Zomig ZMT 3 5 mg Dispersible Tablet Box88.21USDbox
    Zomig 5 mg nasal spray37.76USDeach
    Zomig 5 mg tablet28.82USDtablet
    Zomig zmt 5 mg tablet28.27USDtablet
    Zomig 2.5 mg tablet26.08USDtablet
    Zomig zmt 2.5 mg tablet25.59USDtablet
    DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
    Patents
    CountryPatent NumberApprovedExpires (estimated)
    United States67502372001-05-282021-05-28
    United States54666991992-11-142012-11-14
    Canada25725082010-03-302016-08-02
    Canada20648151999-11-162011-06-06
    Properties
    Statesolid
    Experimental Properties
    PropertyValueSource
    logP1.6Not Available
    Predicted Properties
    PropertyValueSource
    water solubility1.90e-01 g/lALOGPS
    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 area57.36ChemAxon
    rotatable bond count5ChemAxon
    refractivity82.44ChemAxon
    polarizability31.65ChemAxon
    number of rings3ChemAxon
    bioavailability1ChemAxon
    rule of fiveYesChemAxon
    Ghose filterYesChemAxon
    Veber's ruleNoChemAxon
    MDDR-like ruleNoChemAxon
    Spectra
    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 Reference
    1. Pascual J: [Mechanism of action of zolmitriptan] Neurologia. 1998 Oct;13 Suppl 2:9-15. Pubmed
    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
    External Links
    ResourceLink
    KEGG DrugD00415
    KEGG CompoundC07218
    ChEBI10124
    ChEMBLCHEMBL1185
    Therapeutic Targets DatabaseDAP000077
    PharmGKBPA451975
    Drug Product Database2243045
    RxListhttp://www.rxlist.com/cgi/generic2/zolmit.htm
    Drugs.comhttp://www.drugs.com/cdi/zolmitriptan.html
    WikipediaZolmitriptan
    ATC CodesN02CC03
    AHFS Codes
    • 28:32.28
    PDB EntriesNot Available
    FDA labelshow(101 KB)
    MSDSNot Available
    Interactions
    Drug Interactions
    Drug
    AlmotriptanConcomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and almotriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
    AmitriptylineUse of two serotonin modulators, such as zolmitriptan and amitriptyline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    AmoxapineUse of two serotonin modulators, such as zolmitriptan and amoxapine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    BromocriptineConcomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, bromocriptine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated. Use of two serotonin modulators, such as zolmitriptan and bromocriptine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    BuspironeUse of two serotonin modulators, such as zolmitriptan and buspirone, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    CabergolineConcomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, carbergoline, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated. Use of two serotonin modulators, such as zolmitriptan and carbergoline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    CitalopramThe use of two serotonin modulators, such as zolmitriptan and citalopram, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    ClomipramineUse of two serotonin modulators, such as zolmitriptan and clomipramine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    D-TryptophanUse of two serotonin modulators, such as zolmitriptan and D-tryptophan, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    DesipramineUse of two serotonin modulators, such as zolmitriptan and desipramine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    DesvenlafaxineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
    DextromethorphanUse of two serotonin modulators, such as zolmitriptan and dextromethorphan, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    DihydroergotamineConcomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, dihydroergotamine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
    DoxepinUse of two serotonin modulators, such as zolmitriptan and doxepin, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    DuloxetineUse of two serotonin modulators, such as zolmitriptan and duloxetine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    EletriptanConcomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and eletriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
    Ergoloid mesylateConcomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, ergoloid mesylate, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
    ErgonovineConcomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, ergonovine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
    ErgotamineConcomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, ergotamine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
    EscitalopramUse of two serotonin modulators, such as zolmitriptan and escitalopram, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    FluoxetineUse of two serotonin modulators, such as zolmitriptan and fluoxetine, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    FluvoxamineUse of two serotonin modulators, such as zolmitriptan and fluvoxamine, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    FrovatriptanConcomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and frovatriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
    FurazolidoneThe MAO inhibitor, furazolidine, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing furazolidine are contraindicated.
    ImipramineUse of two serotonin modulators, such as zolmitriptan and imipramine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    IsocarboxazidThe MAO inhibitor, isocarboxazid, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing isocarboxazid are contraindicated.
    L-TryptophanUse of two serotonin modulators, such as zolmitriptan and L-tryptophan, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    LinezolidThe MAO inhibitor, linezolid, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing linezolid are contraindicated.
    LithiumUse of two serotonin modulators, such as zolmitriptan and lithium, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    MaprotilineUse of two serotonin modulators, such as zolmitriptan and maprotiline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    MethylergometrineConcomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, methylergonovine, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
    MethysergidePossible severe and prolonged vasoconstriction
    MilnacipranUse of two serotonin modulators, such as zolmitriptan and milnacipran, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    MirtazapineUse of two serotonin modulators, such as zolmitriptan and mirtazapine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    MoclobemideThe MAO inhibitor, moclobemide, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing moclobemide are contraindicated.
    NaratriptanConcomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and naratriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
    NefazodoneUse of two serotonin modulators, such as zolmitriptan and nafazodone, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    NortriptylineUse of two serotonin modulators, such as zolmitriptan and nortriptyline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    ParoxetineUse of two serotonin modulators, such as zolmitriptan and paroxetine, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    PergolideConcomitant use of the serotonin 5-HT1D receptor agonist, zolmitriptan, and the ergot derivative, pergolide, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
    PethidineUse of two serotonin modulators, such as zolmitriptan and meperidine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    PhenelzineThe MAO inhibitor, phenelzine, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing phenelzine are contraindicated.
    ProcarbazineThe MAO inhibitor, procarbazine, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing procarbazine are contraindicated.
    PromethazineUse of two serotonin modulators, such as zolmitriptan and promethazine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    ProtriptylineUse of two serotonin modulators, such as zolmitriptan and protriptyline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    RasagilineThe MAO inhibitor, rasagiline, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing rasagiline are contraindicated.
    RizatriptanConcomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and rizatriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
    S-AdenosylmethionineUse of two serotonin modulators, such as zolmitriptan and S-adenosylmethionine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    SelegilineThe MAO inhibitor, selegiline, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing selegiline are contraindicated.
    SertralineUse of two serotonin modulators, such as zolmitriptan and sertraline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    SibutramineUse of sibutramine, which inhibits serotonin reuptake, and zolmitriptan, a serotonin 5-HT1D receptor agonist, may cause serotonin syndrome. Concomitant therapy is contraindicated.
    St. John's WortUse of two serotonin modulators, such as zolmitriptan and St. John's Wort, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    SumatriptanConcomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and sumatriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
    TapentadolUse of two serotonin modulators, such as zolmitriptan and tapentadol, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    TramadolThe use of two serotonin modulators, such as zolmitriptan and tramadol, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    TranylcypromineThe MAO inhibitor, tranylcypromine, may increase the serum concentration of zolmitriptan by decreasing its metabolism. Concomitant therapy and use of zolmitriptan within two weeks of discontinuing tranylcypromine are contraindicated.
    TrazodoneUse of two serotonin modulators, such as zolmitriptan and trazodone, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    TrimipramineUse of two serotonin modulators, such as zolmitriptan and trimipramine, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    VenlafaxineUse of two serotonin modulators, such as zolmitriptan and venlafaxine, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
    Food InteractionsNot Available

    1. 5-hydroxytryptamine receptor 1B

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: agonist

    Components

    Name UniProt ID Details
    5-hydroxytryptamine receptor 1B P28222 Details

    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 receptors. Eur J Pharmacol. 2000 Jun 2;397(2-3):297-302. Pubmed
    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
    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
    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
    5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
    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
    7. Hargreaves RJ, Shepheard SL: Pathophysiology of migraine—new insights. Can J Neurol Sci. 1999 Nov;26 Suppl 3:S12-9. Pubmed
    8. Gowin JL, Swann AC, Moeller FG, Lane SD: Zolmitriptan and human aggression: interaction with alcohol. Psychopharmacology (Berl). 2010 Jul;210(4):521-31. Epub 2010 Apr 21. Pubmed
    9. Pascual J: [Mechanism of action of zolmitriptan] Neurologia. 1998 Oct;13 Suppl 2:9-15. Pubmed
    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

    2. 5-hydroxytryptamine receptor 1D

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: agonist

    Components

    Name UniProt ID Details
    5-hydroxytryptamine receptor 1D P28221 Details

    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
    2. Hargreaves RJ, Shepheard SL: Pathophysiology of migraine—new insights. Can J Neurol Sci. 1999 Nov;26 Suppl 3:S12-9. Pubmed
    3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
    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 receptors. Eur J Pharmacol. 2000 Jun 2;397(2-3):297-302. Pubmed
    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
    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
    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
    8. Gowin JL, Swann AC, Moeller FG, Lane SD: Zolmitriptan and human aggression: interaction with alcohol. Psychopharmacology (Berl). 2010 Jul;210(4):521-31. Epub 2010 Apr 21. Pubmed
    9. Pascual J: [Mechanism of action of zolmitriptan] Neurologia. 1998 Oct;13 Suppl 2:9-15. Pubmed
    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

    3. 5-hydroxytryptamine receptor 1F

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: agonist

    Components

    Name UniProt ID Details
    5-hydroxytryptamine receptor 1F P30939 Details

    References:

    1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
    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
    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
    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
    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
    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

    4. 5-hydroxytryptamine receptor 1A

    Kind: protein

    Organism: Human

    Pharmacological action: yes

    Actions: agonist

    Components

    Name UniProt ID Details
    5-hydroxytryptamine receptor 1A P08908 Details

    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

    1. Cytochrome P450 1A2

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate

    Components

    Name UniProt ID Details
    Cytochrome P450 1A2 P05177 Details

    References:

    1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
    2. 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. Epub 2009 Nov 24. Pubmed

    2. Amine oxidase [flavin-containing] A

    Kind: protein

    Organism: Human

    Pharmacological action: unknown

    Actions: substrate

    Components

    Name UniProt ID Details
    Amine oxidase [flavin-containing] A P21397 Details

    References:

    1. Rolan P: Potential drug interactions with the novel antimigraine compound zolmitriptan (Zomig, 311C90). Cephalalgia. 1997 Oct;17 Suppl 18:21-7. Pubmed
    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

    Comments
    Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:09