Description
Migrapam Pharmacodynamics
Zolmitriptan is a selective agonist of serotonin 5NT1B/1D receptors, stimulation of which leads to vasoconstriction. It has high affinity for recombinant human serotonin 5NT1B/1D receptors and moderate affinity for serotonin 5NT1A receptors. Zolmitriptan has no affinity and shows no significant pharmacological activity towards serotonin 5NT2, 5NT3, 5NT4, 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 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 from 2 to 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
Cure of migraine attacks with and without aura.
Contraindications
Hypersensitivity to zolmitriptan and other components of the drug.
Age under 18 years.
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, glucose-galactose malabsorption (the drug contains lactose).
Caution: Severe hepatic impairment. pregnancy and lactation.
Dosage and administration
- Tablets are taken orally with water.
- Recommended dose for migraine attack 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 occur again within 24 hours, a second dose of Migrapam® may be taken. Do not take the 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 beneficial to take the drug again during the same attack.
- If the patient did not achieve therapeutic effect after taking 2.5 mg dose, for relieving subsequent migraine attacks it is possible to use Migrapam® in dose of 5 mg (2 tablets).
- Do not take more than 2 doses of Migrapam® per day. The total dose of zolmitriptan taken during a day should not exceed 10 mg (4 tablets).
- Migrapam® is not indicated for migraine prophylaxis.
- Use in special groups of patients
- Childhood and adolescence
Efficacy and safety of use of zolmitriptan in children under 12 years of age has not been studied. Efficacy of zolmitriptan in placebo controlled clinical trials in patients aged 12 to 17 years old has not been established. The use of Migrapam® 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, the use of Migrepam® in elderly patients is not recommended. - Impaired liver function
No dose adjustment is required in mild to moderate hepatic impairment. For patients with severe hepatic impairment, 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.
