Zolmitriptan (Zolmitriptanum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Serotonergic agents

Included in the formulation
  • Zomig®
    pills inwards 
    AstraZeneca UK Ltd     United Kingdom
  • Zomig® Rapimlt
    pills inwards 
    AstraZeneca UK Ltd     United Kingdom
  • Migrepam®
    pills inwards 
    OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC     Russia
    • АТХ:

    N.02.C.C.03   Zolmitriptan

    Pharmacodynamics:

    A selective serotonin receptor (5-hydroxytryptamine) agonist of the 5-HT1D and 5-HT1B, located in the vessels. Causes vasoconstriction when interacting with the 5-HT receptors of the intracranial vessels and the sensitive nerve endings of the trigemino-vascular system, thereby suppressing the release of CGRP, VIP and substance P, which facilitates the course of migraine attacks by reducing the intensity of pain. Reduction of the release of serotonin and a decrease in its content in the postsynaptic gap by the negative feedback mechanism leads to a decrease in the severity of photo and phonophobia, nausea and vomiting. A stable repeated effect is caused by the action on the brain stem cells responsible for the development of migraine.

    Pharmacokinetics:

    After ingestion, up to 40% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 2 hours. The connection with plasma proteins is 25%.

    Therapeutic effect develops after 1 has after the reception. Metabolism in the liver to active N-desmethyl metabolite and two inactive - indoleacetic acid and N-oxide metabolite. The pharmacological activity of N-desmethyl metabolite in relation to 5-HT1B-receptors exceeds in 2-6 times the action of zolmitriptan.

    The half-life is 3 hours. Elimination by the kidneys in the form of an indole acetic metabolite and with feces in unchanged form (about 30%).

    Indications:

    It is used to treat migraine with an aura or without an aura.

    ICD-10

    VI.G40-G47.G43.0   Migraine without aura [simple migraine]

    VI.G40-G47.G43.1   Migraine with aura [classic migraine]

    Contraindications:Uncontrolled arterial hypertension, peripheral arterial disease, severe renal failure, Prinzmetal angina, individual intolerance, children under 18 years.
    Carefully:

    Ischemic heart disease, hypersensitivity.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. It is used with caution during pregnancy and lactation in cases where the intended benefit exceeds the risk to the fetus and newborn.

    Dosing and Administration:

    Inside for 2.5 mg. With normal tolerability of the drug, but insufficient effectiveness, it is possible to increase the dose to 5 mg after 24 hours.

    The highest daily dose: 15 mg.

    The highest single dose: 5 mg.

    Side effects:

    Central and peripheral nervous system: asthenia, sensitivity disorders, dizziness, paresthesia, drowsiness, a feeling of stiffness in the limbs.

    Respiratory system: a feeling of heaviness and compression in the throat.

    The cardiovascular system: tachycardia, transient arterial hypertension, rarely - spasm of coronary vessels, myocardial infarction.

    Digestive system: dry mouth, nausea, rarely - ischemic colitis, spleen or bowel infarction, hemorrhagic diarrhea.

    Musculoskeletal system: muscle weakness, myalgia.

    Dermatological reactions: hives.

    Urinary system: polyuria, pollakiuria.

    Allergic reactions.

    Overdose:

    Significant sedation.

    Treatment is symptomatic.

    Interaction:

    Simultaneous use with St. John's Wort preparations (Hypericum perforatum) may increase the risk of unwanted effects.

    Metoclopramide (monoamine oxidase inhibitor) increases the concentration of the drug in the blood plasma - a reductionthe maximum dose of zolmitriptan to 7.5 mg.

    Special instructions:

    Zolmitriptan is not used to prevent migraine attacks.

    It is not recommended simultaneous reception with other drugs from the group of 5-HT agonists1D receptors.

    Care should be taken when treating vehicles while driving vehicles.

    Instructions
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