Description
Zolmitriptan Pharmacodynamics
Zolmitriptan is a selective agonist of 5HT1B/1D receptors, stimulation of which leads to vasoconstriction. It has high affinity for recombinant human 5HT1B/1D receptors and moderate affinity for 5HT1A receptors. Zolmitriptan has no affinity and shows no significant pharmacological activity towards 5HT2, 5HT3, 5HT4, adrenergic, histamine, muscarinic and dopaminergic receptors.
Administration of zolmitriptan to laboratory animals resulted in vasoconstriction in the carotid artery basin. In addition, the results of studies on laboratory animals indicate that zolmitriptan blocks the central and peripheral trigeminal nerve activity by inhibiting the release of calcitonin gene-related peptide, vasoactive intestinal peptide and substance P.
In clinical trials, the effect of zolmitriptan on headache and other migraine symptoms (such as nausea, photophobia, phonophobia) was noted after 1 hour and increased between 2 and 4 hours after taking the drug.
Zolmitriptan is equally effective for migraine with aura, migraine without aura and migraine associated with menstruation. Taking zolmitriptan during aura did not prevent migraine headache, so the drug should be taken after the onset of a pain attack.
Indications
Treatment of migraine attacks with or without aura.
Contraindications
Hypersensitivity to any component of the drug.
Childhood age – up to 18 years old.
Older age – over 65 years (effectiveness and safety of use have not been studied).
Pregnancy period (safety of use has not been studied).
Hemiplegic, basilar and ophthalmoplegic migraine.
Uncontrolled arterial hypertension.
Coronary heart disease.
Coronary vasospasm/Prinzmetal’s angina.
Peripheral arterial disease.
History of cerebral circulation disorders (including stroke or transient ischemic attack).
Wolff-Parkinson-White syndrome or arrhythmias associated with other accessory pulse pathways.
Severe renal insufficiency (creatinine clearance less than 15 ml/min).
Concomitant use with other serotonin 5NT1B/1D receptor agonists (e.g. sumatriptan, naratriptan), ergotamine or its derivatives (including methysergide), and within 24 hours after their withdrawal.
Concomitant use with MAO-A inhibitors and within 14 days after their withdrawal.
Lactose intolerance, lactase deficiency or glucose-galactose malabsorption.
Dosage and administration
- Tablets should be taken orally with water.
- Recommended dose for migraine relief is 2.5 mg (1 tablet). It is recommended to take the drug as soon as possible after the beginning of headache, but the drug is also effective when taken later after the attack.
- If migraine symptoms arise again within 24 hours, a second dose of Zolmitriptan-SZ may be taken. Do not take a second dose earlier than 2 hours after the first dose. If no clinical effect is noted after the first dose, it is unlikely to be useful to take the drug again during the same attack.
- If the patient did not achieve therapeutic effect after the dose of 2.5 mg, for relieving further migraine attacks it is possible to use Zolmitriptan-SZ preparation in dose of 5 mg (2 tablets).
- Do not take more than 2 doses of Zolmitriptan-SZ per day. The total dose of Zolmitriptan taken during a day should not exceed 10 mg (4 tablets).
- Zolmitriptan-SZ is not indicated for migraine prophylaxis.
Administration in special groups of patients - Childhood and adolescence
Efficacy and safety of Zolmitriptan in children less than 12 years old has not been studied. Efficacy of zolmitriptan in placebo controlled clinical trial in patients aged 12 to 17 years old has not been established. The use of Zolmitriptan-SZ in children and adolescents is not recommended. - Older age.
Efficacy and safety of Zolmitriptan in patients over 65 years old have not been established. Therefore, it is not recommended to use Zolmitriptan-SZ in elderly patients. - Impairment of liver function
No dose adjustment is required in mild and moderate hepatic dysfunction. For patients with severe liver dysfunction the total dose of zolmitriptan taken during a day should not exceed 5 mg. - Renal failure
No dose adjustment is required if creatinine clearance is higher than 15 ml/min. The drug is contraindicated in severe renal failure (creatinine clearance less than 15 ml/min). - Interaction with other medicinal products, requiring dosage adjustment
For patients taking cimetidine or selective CYP1A2 isoenzyme inhibitors (e.g. fluvoxamine, ciprofloxacin and other quinolones) the total dose of zolmitriptan taken during a day should not exceed 5 mg.
