Index of drugs

Treatment of acute phase of migraine headache accompanied with or without aura in adults.

1 RPD oral lyophilisate contains 10 mg of rizatriptan in the form of benzoate.

The drug interrupts the onset of migraine. A selective agonist with high affinity for 5-HT serotonergic receptors_1B and 5-HT_1D, with no significant activity relative to 5-HT₂, 5-HT₃ and α-, α-, β-adrenergic receptors, D₁ and D₂ dopaminergic, H1 histamine, muscarinic, benzodiazepine. It causes selective contraction of intracranial vessels by agonistic effects on 5HT receptors₁ and 5-HT₂ and simultaneous inhibition of the secretion of a gene-related peptide for calcitonin (CGRP), neurokine A and substance P. Shrinkage during extrasystemic seizure and the influence on the sensory part of the trigeminal nerve reduce the tissue inflammatory response and pain stimulation through the trigeminal nerve to o.u.n. This reduces the pain and associated symptoms: nausea, vomiting, hypersensitivity to light and sounds. Rapidly absorbed from the gastrointestinal tract (the average bioavailability for the form of a lyophilisate is about 40%), within 1.6-2.5 hours it reaches the maximum concentration in the blood. Admission with food delays absorption by about 1 hour. To a small extent (14%) is associated with plasma proteins, T_0,5 is about 2-3 h. It is metabolized mainly in the liver by oxidative deamination with the participation of monoamine oxidase type A (MAO-A) to pharmacologically inactive metabolite, which is an indole derivative of acetic acid; N-monodemetylorizatriptan having activity on 5-HT receptors_{1B / 1D} to a degree that does not significantly affect the pharmacological activity of rizatriptan and low-level other inactive metabolites (N-oxide, 6-hydroxy derivative, 6-hydroxy derivative conjugated to sulphates). It is excreted mainly in the urine: about 14% in unchanged form, in 51% as indole derivative of acetic acid, in about 1% in the form of the active N-monodemethyl metabolite.

Hypersensitivity to rizatriptan or other ingredients of the preparation. Concomitant treatment with MAO inhibitors (and before 2 weeks from the end of MAO inhibitor treatment), severe liver or kidney failure, condition after stroke or transient ischemic attack, moderately severe, severe or untreated, mild hypertension, coronary artery disease, including ischemic heart disease (angina pectoris, myocardial infarction, documented asymptomatic myocardial ischemia), signs or symptoms of ischemic heart disease or Prinzmetal's angina, peripheral vascular disease; simultaneous use of ergotamine, rizatriptan, ergot derivatives (including metyzergide), other 5-HT receptor agonists_{1B / 1D}.

Do not use in the prophylaxis of migraine or in the treatment of basal and hemiplegic headache; in unusual headaches, without a confirmed diagnosis of migraine. Do not use below 17 years and over 65 years (no safety studies). Do not use without prior diagnosis in patients with probability or increased risk of heart disease or coronary arteries (patients with hypertension, diabetes, tobacco smokers or people using nicotine replacement therapies, males> 40 years, postmenopausal women, Hiss bundle branch block, aggravating an interview for coronary artery disease). If you have had pain or tightness in the chest or neck after taking the medicine, do not take more rizatriptan before completing the diagnosis to rule out cardiac ischemic disease. Due to the content in the aspartame preparation, the drug may be harmful in patients with phenylketonuria.

In pregnancy, it can only be used in cases of extreme necessity. In animal studies, it has been shown that the medicine is excreted in breast milk; no adequate human studies. If breastfeeding mothers need to take this medicine, breast-feeding should be discontinued for 24 hours after taking the medicine.

Common: insomnia, dizziness, paresthesia, headache, reduced pain perception, decreased mental performance; palpitations, feeling of tightness in the throat, nausea, dry mouth, vomiting, diarrhea, indigestion; redness of the face, feeling of heaviness, neck pain, muscle stiffness, weakness, fatigue, abdominal or chest pain. Uncommon: confusion, nervousness, ataxia, dizziness, taste disturbance or unpleasant taste, tremor, fainting, blurred vision, arrhythmia, ECG abnormalities, tachycardia, hypertension, hot flushes, facial flushing, shortness of breath, feeling thirsty, pruritus, urticaria, angioedema (eg swelling of the face, tongue, throat), rash, excessive sweating, feeling of local pressure, muscle weakness, facial pain, muscle pain. Rarely: hypersensitivity reactions, anaphylactic or anaphylactoid reactions, cerebrovascular events (most of these side effects were in patients with risk factors for ischemic heart disease), bradycardia, wheezing. In addition: convulsive seizure, serotonin syndrome, ischemia or myocardial infarction (mainly in patients with risk factors for ischemic heart disease), limb ischemia, ischemic colitis, toxic epidermal necrolysis.

Adults, orally: in a migraine attack of 10 mg. If the drug worked effectively and the pain returned - the dose can be repeated, not earlier than after 2 hours. Do not take more than 2 doses in 24 hours. If a new migraine attack occurred within 24 hours and the drug was effective during the first attack - you can take another dose of the drug so that you do not exceed 2 doses / day. Do not take a second dose of the same pain attack if the first one was ineffective. Patients treated with propranolol (should have at least 2 hours before or after using propranolol), mild to moderate renal failure, mild or moderate hepatic insufficiency - should use 5 mg doses.