Treatment of acute migraine pain with or without aura.
Composition:
1 tabl powl. contains 2.5 mg of zolmitriptan.
Action:
A selective agonist of vascular 5HT receptors1B / 1Dthat are responsible for the contraction of the vessels. It has high affinity for human recombinant 5HT receptors1B and 5HT1D and moderate to 5HT receptors1A. Zolmitriptan does not show significant affinity or pharmacological activity towards other 5HT receptor subtypes (5HT2, 5HT3, 5HT4) or to the adrenergic, histamine, muscarinic and dopaminergic receptors. After oral administration zolmitriptan well (at least 64%) and quickly absorbed from the gastrointestinal tract. Bioavailability is about 40%. To a small extent (25%) is bound to plasma proteins. It is metabolised mainly in the liver to indolylacetic acid and the N-oxide derivative and the active N-demethyl derivative. Metabolites are mainly excreted (60%) in the urine, in 30% excreted unchanged with faeces. T0,5 is 4.7 h, in patients with moderate hepatic insufficiency0,5 is 7.3 h, and with severe hepatic impairment it extends to 12 h.
Contraindications:
Hypersensitivity to zolmitriptan or other components of the drug. Moderate or severe hypertension and mild and poorly controlled hypertension. Patients with myocardial infarction or with ischemic heart disease, with coronary spasm (Prinzmetal angina), peripheral vascular disease or patients who exhibit signs and symptoms of ischemic heart disease. Co-administration of zolmitriptan with ergotamine, ergotamine derivatives (including methysergide), Sumatriptan, naratriptan and other 5HT receptor agonists1B / 1D. Cerebral stroke (CVA) or transient cerebral ischemia (TIA). Patients with a creatinine clearance less than 15 ml / min.
Precautions:
Use only if the migraine is clearly identified, excluding other possible causes of headaches. Zolmitriptan is not indicated for the treatment of hemiplegic, basal or ophthalmoplegic migraine. Do not use in patients with symptoms of Wolff-Parkinson-White syndrome or arrhythmias associated with other, additional conduction pathways. In patients with ischemic heart disease risk factors such as smoking, hypertension, hyperlipidemia, diabetes, hereditary factors, the drug should not be used without previous studies to exclude cardiovascular disease; this recommendation applies primarily to postmenopausal women and men over 40 years of age who have risk factors. In the event of chest pain or other signs of ischemic heart disease, zolmitriptan should be discontinued and appropriate tests performed. Similar to other preparations from the 5HT receptor agonist group1B / 1D zolmitriptan may cause a transient increase in blood pressure in both hypertensive patients and in patients with normal pressures; Do not exceed the recommended doses of zolmitriptan. In the event of a headache, the use of any analgesic can make the condition worse. If you experience these symptoms, ask your doctor for advice and stop treatment. Drug abuse should be considered in patients who have frequent or daily headaches, despite (or because of) the regular use of antimigraine drugs. The drug is not suitable for use in the prevention of migraines. The safety and efficacy of zolmitriptan tablets in children have not been studied; drug is not recommended for use in children. During placebo-controlled clinical trials in patients aged 12 to 17 years, the efficacy of zolmitriptan tablets has not been demonstrated; drug is not recommended for use in adolescents. The safety and efficacy of zolmitriptan has not been demonstrated in people over the age of 65; it is not recommended for use in the elderly.
Pregnancy and lactation:
Zolmitriptan can be used during pregnancy only if the expected benefit to the mother outweighs the potential risk to the fetus. The safety of the medicine during pregnancy has not been established. Animal studies did not show any direct teratogenic effects. However, the embryotoxicity test results showed a possible side effect on the viability of the fetus. Studies have shown that zolmitriptan is excreted in the milk of lactating animals. Caution is advised when using zolmitriptan in breast-feeding women. After intake of zolmitriptan, breast-feeding should be discontinued for 24 hours to minimize the absorption of zolmitriptan by the child.
Side effects:
Common: palpitations; abnormal or disturbed perception, central dizziness, headache, hyperaesthesia, paresthesia, drowsiness, feeling hot; abdominal pain, nausea, vomiting, dry mouth; muscle weakness, muscle pain; asthenia, heaviness, tightness, pain or tightness in the throat, neck, limbs or chest. Uncommon: tachycardia, mild hypertension, transient increase in systemic arterial pressure; polyuria, increase the frequency of urination. Rare: hypersensitivity reactions including urticaria, angioneurotic edema and anaphylactic reactions. Very rare: heart attack; angina pectoris, spasm of coronary vessels; ischaemia or infarction (e.g., small intestinal ischemia, intestinal infarction, spleen infarction) whose symptoms may be bloody diarrhea or abdominal pain; urinary urgency. Some symptoms may be part of the same migraine attack.
Dosage:
Orally. Adults: 2.5 mg daily. The drug should be taken as soon as possible after the onset of migraine pain. The drug is also effective if taken at a later stage. The second dose can be taken if the symptoms of migraine return within 24 hours after the first response to treatment. If it is necessary to take a second dose, it can be used at least 2 hours after the first dose. If you do not respond to the first dose, it is unlikely that you will benefit from the second dose during the same episode of migraine. The total daily dose should not exceed 10 mg. Do not take more than 2 doses of the drug within 24 hours. Table. should be swallowed whole (they should not be chewed), washed down with water.