Zolmitriptan
Class:Antimigraine
Mechanism of action
Selective agonist for
serotonin (5-HT1B and 5-HT1D receptors) in cranial arteries to cause
vasoconstriction and reduce sterile inflammation associated with antidromic
neuronal transmission correlating with relief of migraine.
Pharmacokinetics
Onset of action :within
30 minutes to 1 hour.Distribution:vd: 7 L/kg.Protein binding:25 percent.Metabolism:converted
to an active N-desmethyl metabolite that is 2-6 times more potent than
zolmitriptan.Half life:2.8-3.7 hours.Bioavailability,absolute:49 percent.Time
to peak serum concentrations:2-3.5 hours.Elimination:urine and feces.
Indications
Migraine with or
without aura.
Contraindications
Hypersensitivity,uncontrolled
hypertension,ischaemic heart disease coronary vasospasm/prinzmetal angina.
Precautions
Care must be taken to
exclude potentially serious neurological conditions.No data for the use in
basilar or hemiplegic migraine.Given to patients with wolf-parkinson white syndrome
or arrhythmias associated with other cardiac accessory conduction pathways.
Side effects
Rare cases:with other
5HT1B/1D agonists,angina pectoris and myocardial
infarction.Commonly:nausea,dizziness,somnolence,warm sensation,asthenia and dry
mouth,heaviness,lightness,pain or pressure may occur in the throat,neck,limbs
and chest(no evidence of ischemic ECG changes),as may myalgia,muscle
weakness,paraesthesia,dysesthesia.
Dosage
Migraine attack:2.5
mg.If symptoms persist or return within 24 hours,a second dose of 2.5 mg has
been shown to be effective.If second dose is required ,it should not be taken
within 2 hours of the initial dose.
Brands
Tabs.Limigzol
2.5mg,Tabs.Zomig 2.5mg.
