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Identification
Name Zolmitriptan
Accession Number DB00315 (APRD00376)
Type small molecule
Groups approved
Description

Zolmitriptan is a synthetic tryptamine derivative and appears as a white powder that is readily soluble in water. [Wikipedia]
Structure Thumb
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms
ZMT
Salts Not Available
Brand names
Name Company
AscoTop
Zomig
Zomig Rapimelt
Zomigon
Brand mixtures Not Available
Categories
  • Vasoconstrictor Agents
  • Anti-inflammatory Agents
  • Anti-migraine Agents
  • Selective Serotonin Agonists
  • Serotonin Agonists
CAS number 139264-17-8
Weight Average: 287.3568
Monoisotopic: 287.163376931
Chemical Formula C16H21N3O2
InChI Key InChIKey=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
Plain Text
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
Plain Text
Mass Spec Not Available
Taxonomy
Kingdom Not Available
Classes Not Available
Substructures Not Available
Pharmacology
Indication For the acute treatment of adult migraine with or without auras.
Pharmacodynamics Zolmitriptan 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 action Zolmitriptan 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.
Absorption Mean 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 binding 25%
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.
Route of elimination Not Available
Half life The mean elimination half-life of zolmitriptan and of the active N-desmethyl metabolite is 3 hours.
Clearance
  • 25.9 mL/min/kg
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
Pharmacoeconomics
Manufacturers
  • Astrazeneca pharmaceuticals lp
  • Ipr pharmaceuticals inc
Packagers
Dosage forms
Form Route Strength
Spray Nasal
Tablet Oral
Prices
Unit description Cost Unit
Zomig 6 5 mg Solution 1 Box = 6 Single Use Bottles 235.62 USD bottle
Zomig ZMT 6 2.5 mg Dispersible Tablet Box 159.66 USD box
Zomig 6 2.5 mg tablet 1 Box = 6 tablet 147.23 USD box
Zomig 3 5 mg tablet Box 93.49 USD box
Zomig ZMT 3 5 mg Dispersible Tablet Box 88.21 USD box
Zomig 5 mg nasal spray 37.76 USD each
Zomig 5 mg tablet 28.82 USD tablet
Zomig zmt 5 mg tablet 28.27 USD tablet
Zomig 2.5 mg tablet 26.08 USD tablet
Zomig zmt 2.5 mg tablet 25.59 USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Country Patent Number Approved Expires (estimated)
United States 6750237 2001-05-28 2021-05-28
United States 5466699 1992-11-14 2012-11-14
Canada 2572508 2010-03-30 2016-08-02
Canada 2064815 1999-11-16 2011-06-06
Properties
State solid
Experimental Properties
Property Value Source
logP 1.6 Not Available
Predicted Properties
Property Value Source
water solubility 1.90e-01 g/l ALOGPS
logP 2.25 ALOGPS
logP 2.04 ChemAxon
logS -3.2 ALOGPS
pKa (strongest acidic) 13 ChemAxon
pKa (strongest basic) 9.55 ChemAxon
physiological charge 1 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 2 ChemAxon
polar surface area 57.36 ChemAxon
rotatable bond count 5 ChemAxon
refractivity 82.44 ChemAxon
polarizability 31.65 ChemAxon
References
Synthesis Reference Not Available
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
Resource Link
KEGG Drug D00415 Link_out
KEGG Compound C07218 Link_out
ChEBI 10124 Link_out
ChEMBL 10124 Link_out
Therapeutic Targets Database DAP000077 Link_out
PharmGKB PA451975 Link_out
Drug Product Database 2243045 Link_out
RxList http://www.rxlist.com/cgi/generic2/zolmit.htm Link_out
Drugs.com http://www.drugs.com/cdi/zolmitriptan.html Link_out
Wikipedia http://en.wikipedia.org/wiki/Zolmitriptan Link_out
ATC Codes
  • N02CC03
AHFS Codes
  • 28:32.28
PDB Entries Not Available
FDA label show (101 KB)
MSDS Not Available
Interactions
Drug Interactions
Drug Interaction
Almotriptan Concomitant 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.
Amitriptyline Use 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.
Amoxapine Use 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.
Bromocriptine Concomitant 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.
Buspirone Use 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.
Cabergoline Concomitant 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.
Citalopram The 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.
Clomipramine Use 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-Tryptophan Use 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.
Desipramine Use 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.
Desvenlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Dextromethorphan Use 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.
Dihydroergotamine Concomitant 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.
Doxepin Use 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.
Duloxetine Use 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.
Eletriptan Concomitant 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 mesylate Concomitant 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.
Ergonovine Concomitant 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.
Ergotamine Concomitant 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.
Escitalopram Use 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.
Fluoxetine Use 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.
Fluvoxamine Use 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.
Frovatriptan Concomitant 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.
Furazolidone The 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.
Imipramine Use 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.
Isocarboxazid The 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-Tryptophan Use 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.
Linezolid The 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.
Lithium Use 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.
Maprotiline Use 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.
Meperidine Use 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.
Methylergonovine Concomitant 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.
Methysergide Possible severe and prolonged vasoconstriction
Milnacipran Use 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.
Mirtazapine Use 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.
Moclobemide The 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.
Naratriptan Concomitant 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.
Nefazodone Use 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.
Nortriptyline Use 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.
Paroxetine Use 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.
Pergolide Concomitant 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.
Phenelzine The 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.
Procarbazine The 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.
Promethazine Use 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.
Protriptyline Use 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.
Rasagiline The 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.
Rizatriptan Concomitant 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-Adenosylmethionine Use 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.
Selegiline The 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.
Sertraline Use 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.
Sibutramine Use 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 Wort Use 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.
Sumatriptan Concomitant 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.
Tapentadol Use 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.
Tramadol The 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.
Tranylcypromine The 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.
Trazodone Use 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.
Trimipramine Use 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.
Venlafaxine Use 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 Interactions Not Available
Targets

1. 5-hydroxytryptamine 1B receptor

Pharmacological action: yes
Actions: agonist

This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity

Organism class: human
UniProt ID: P28222 Link_out
Gene: HTR1B Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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 1D receptor

Pharmacological action: yes
Actions: agonist

This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity

Organism class: human
UniProt ID: P28221 Link_out
Gene: HTR1D Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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 1F receptor

Pharmacological action: yes
Actions: agonist

This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity

Organism class: human
UniProt ID: P30939 Link_out
Gene: HTR1F Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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 1A receptor

Pharmacological action: yes
Actions: agonist

This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity

Organism class: human
UniProt ID: P08908 Link_out
Gene: HTR1A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
Enzymes

1. Cytochrome P450 1A2

Actions: substrate

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 N3-demethylation. Also acts in the metabolism of aflatoxin B1 and acetaminophen

UniProt ID: P05177 Link_out
Gene: CYP1A2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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

Actions: substrate

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

UniProt ID: P21397 Link_out
Gene: MAOA Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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 February 08, 2013 16:19