Chemical Property of Zolmitriptan
Chemical Property:
- Appearance/Colour:White or kind of white powder
- Vapor Pressure:1.03E-12mmHg at 25°C
- Melting Point:136-141 °C
- Refractive Index:1.619
- Boiling Point:563.3 °C at 760 mmHg
- PKA:9.64(at 25℃)
- Flash Point:294.5 °C
- PSA：57.36000
- Density:1.217 g/cm3
- LogP:2.25170
- Storage Temp.:Refrigerator
- Solubility.:Soluble in DMSO at 5mg/ml
- XLogP3:2.2
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:3
- Rotatable Bond Count:5
- Exact Mass:287.16337692
- Heavy Atom Count:21
- Complexity:375
- Purity/Quality:
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99%-101% *data from raw suppliers
Zolmitriptan *data from reagent suppliers
Safty Information:
- Pictogram(s):
Xi
- Hazard Codes:Xi,Xn
- Statements:
36/37/38-22
- Safety Statements:
26-36
- MSDS Files:
-
SDS file from LookChem
Useful:
- Canonical SMILES:CN(C)CCC1=CNC2=C1C=C(C=C2)CC3COC(=O)N3
- Isomeric SMILES:CN(C)CCC1=CNC2=C1C=C(C=C2)C[C@H]3COC(=O)N3
- Recent ClinicalTrials:A Study to Compare the Efficacy and Safety of HB1801 to Taxotere in Advanced Non-Small Cell Lung Cancer (NSCLC)
- Recent EU Clinical Trials:A Multicenter, Double-blind, Randomized, Placebo-controlled, 4-Armed
- Recent NIPH Clinical Trials:MATRIX(Migrainer Assess TRiptane eXamination)
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Description
Zolmitriptan is a selective serotonin receptor agonist of the 1B and 1D subtypes. It is mainly used in the acute treatment of migraine attacks with or without aura and cluster headaches. Zolmitriptan takes effect through binding to human 5-HT1Band 5-HT1Dreceptors, leading to cranial blood vessel constriction and the release of sensory neuropeptides through nerve endings in the trigeminal system.
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Uses
Zolmitriptan is a serotonin 5HTID-receptor agonist and used to treat migraine (1,2,3). A Serotonin 5HTID-receptor agonist adrenergic agonist, nasal decongestant
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Clinical Use
Zomig was launched in Germany, Denmark, Sweden and the UK for use as
an antimigraine agent (with and without aura). It can be prepared by three related
routes of 5 to 7 steps starting from L-4-nitrophenylalanine. Zomig is a 5-HT1D/1B receptor agonist (10 fold ratio) with modest (< 100x) affinity for 5-HT1A and 5-HT1F receptors. It has no affinity for other serotonin receptors or receptors of other
neurotransmitters. It has a novel dual action mechanism: centrally it acts on the
trigeminal nucleus caudalis and peripherally is acts on the trigeminovascular system.
Zomig was effective in treating headaches and nonheadache (photophobia,
phonophobia and nausea) symptoms. It was 2-3 times more potent than sumatriptan
and is metabolized to three compounds, one of which is 2-8 times more active than the
parent. It caused a 40-50% decrease in headache after 1 h and a 73-77% after 4 h.
There was a 30% reoccurance of headache but 90% effective treatment with a second
dose. It blocks neurogenic inflammation by inhibiting release of peptides, causes
vasoconstriction, and inhibits neuronal depolarization at peripheral sites in the
cranium. It is 40% bioavailable and a 10 time theraputic dose showed no safety
concerns.
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Drug interactions
Potentially hazardous interactions with other drugs
Antibacterials: quinolones possibly inhibit
metabolism - reduce dose of zolmitriptan.
Antidepressants: increased risk of CNS toxicity
with citalopram - avoid; risk of CNS toxicity
with MAOIs and moclobemide - reduce dose
of zolmitriptan to max 7.5 mg; SSRIs inhibit
metabolism of zolmitriptan, reduce dose with
fluvoxamine; possibly increased serotonergic
effects with duloxetine and venlafaxine; increased
serotonergic effects with St John’s wort - avoid
concomitant use.
Cimetidine: inhibits metabolism of zolmitriptan;
maximum dose is 5 mg.
Dapoxetine: possible increased risk of serotonergic
effects - avoid for 2 weeks after stopping 5HT1
agonists.
Ergot alkaloids: increased risk of vasospasm.
Linezolid: risk of CNS toxicity - reduce dose of
zolmitriptan.
