Eletriptan (Eletriptanum)

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
  • Relpax®
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    Pfizer Inc.     USA
    • АТХ:

    N.02.C.C.06   Eletriptan

    Pharmacodynamics:

    Means for the treatment of migraine.Selective serotonin 5-HT agonist1B- and 5-HT1D-receptors, which are located mainly in the blood vessels of the brain. With the stimulation of these receptors, there is a narrowing of the vessels, in particular, the carotid artery system, which leads to a reduction in the headache. Eletriptan also has a high affinity for serotonin 5-HT1F-receptors, has a moderate effect on 5-HT1A-, 5-HT2B-, 5-HT1E- and 5-HT7-receptors.

    The antimigraine effect of eletriptan can be due to its ability to narrow the intracranial blood vessels, as well as its inhibitory effect against neurogenic inflammation.

    Pharmacokinetics:

    Quickly absorbed when ingested (81%). Absorption - 50%. Peak plasma concentrations are noted for 1.5 hours. It penetrates into breast milk (the ratio to plasma concentration in the mother is 1: 4). The connection with plasma proteins is 85%. Biotransformation in the liver (CYP34), the only active metabolite - N-demethylated eletriptan. Half-life - 4 hours Time to reach the maximum concentration - 1,5 h (in healthy) and 2 h (with moderate and severe migraine). Elimination by the kidneys and with feces - 90%. The effectiveness of hemodialysis has not been studied.

    Indications:

    Curbing migraine attacks (with aura and without aura).

    ICD-10

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

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

    Contraindications:

    Hypersensitivity; IHD (angina pectoris, myocardial infarction in anamnesis, asymptomatic ischemia, documented); the presence of symptoms or data correlated with coronary artery disease, coronary artery spasm, including variant Prinzmetal angina pectoris, or other cardiovascular diseases transferred or existing; cerebrovascular syndrome, which includes a stroke of any type, as well as transient disorders of the cerebral circulation; peripheral vascular disease, including abdominal ischemia; uncontrolled hypertension; hemiplegic or basilar migraine; period within 24 hours after administration of other 5-HT1 receptor agonists, ergotamine-containing or ergotamine-like drugs such as dihydroergotamine, metisergide; severe hepatic insufficiency.

    Contraindicated in children and adolescents under 18 years.

    Carefully:

    Serotonin syndrome - with the simultaneous use of eletriptan with other drugs that have serotonergic activity,such as selective serotonin reuptake inhibitors and selective serotonin and norepinephrine reuptake inhibitors, caution is necessary, since in some cases there have been reports of the development of serotonin syndrome with the simultaneous administration of eletriptan and other serotonergic drugs; application of the drug in a dose above 40 mg in patients with impaired renal function (since in such patients the effect of eletriptan on blood pressure is enhanced).

    Pregnancy and lactation:

    Action category for the fetus by FDA - C.

    Pregnancy. Adequate and well-controlled studies in pregnant women have not been conducted, eletriptan it is recommended to use during pregnancy only if the expected benefit to the mother exceeds the potential risk to the fetus.

    Lactation. Eletriptan excreted in breast milk. In 8 women who received a single dose of 80 mg, the average content of eletriptan in breast milk after 24 hours was approximately 0.02% of the dose. The ratio between the average concentration of eletriptan in breast milk and in plasma is 1: 4, but differs greatly in variability.The "concentration in breast milk - time" curve for eletriptan is similar to that in plasma for 24 hours (with a mean concentration of 1.7 ng / ml in milk). The level of active N-desmethyl metabolite in breast milk was not measured. Eletriptan should be given to nursing women with caution.

    Dosing and Administration:

    Inside. Selection of the dose is made on an individual basis. Tablets should be swallowed whole, washed down with water.

    When a migraine attack occurs in adults: 20 or 40 mg once (more effective dose of 40 mg, 80 mg dose, despite the greater effectiveness, is associated with an increase in the frequency of side effects, the maximum recommended single dose is 40 mg. If after the initial dose the headache decreased , and then returned again, it is recommended to repeat the reception of eletriptan, but not earlier than 2 hours later. In controlled clinical trials, in the absence of effect from the initial dose, no positive result was found from repeated administration The maximum daily dose should not exceed 80 mg.

    The safety of application for the relief of more than 3 migraine attacks over a 30-day period has not been established.

    Side effects:

    From the side of cardio-vascular system: sensation of heat or hot flushes to the face, palpitations, tachycardia, chest pain, increased blood pressure.

    From the side CNS and peripheral nervous system: drowsiness, dizziness, paresthesia, headache, hypoesthesia, increased sweating, a feeling of "coma" in the throat.

    From the side GIT: abdominal pain, dry mouth, nausea, dyspepsia.

    From the side musculoskeletal system: myasthenia gravis, myalgia.

    From the side respiratory system: pharyngitis.

    Allergic reactions: rash, itching, hives.

    Overdose:

    Symptoms. Premarketing clinical trials did not report a significant overdose. Volunteers (n = 21) who received a single dose of 120 mg did not show clinically significant adverse reactions. In the 3rd phase of the tests, the daily dose reached 160 mg.

    Based on the pharmacodynamics of 5-HT agonists1B / 1D-receptors, overdose may cause hypertension and other, more serious symptoms from the cardiovascular system.

    Treatment: half-life eletriptan - about 4 hours, so the observation of patients after an overdose of eletriptan should last at least about 20 hours or longer, as long as the symptoms and symptoms persist.There is no specific antidote. In case of severe intoxication intensive therapy is recommended, including ventilation to ensure adequate oxygenation and maintenance of the cardiovascular system. It is not known what effect hemodialysis or peritoneal dialysis refuses on the concentration of eletriptan in plasma.

    Interaction:

    When used simultaneously with erythromycin (1 g) and ketoconazole (400 mg), which are potent inhibitors of the CYP3A4 isoenzyme, a significant increase in the maximum concentration in blood plasma, systemic exposure and half-life eletriptan.

    When used simultaneously with caffeine or ergotamine, a small but additive increase in blood pressure is observed.

    Special instructions:

    Eletriptan should be used only in cases when the diagnosis of migraine is undoubted.

    Eletriptan should not be used prophylactically.

    Eletriptan is not indicated for relief of hemiplegic, ophthalmoplegic or basilar migraine.

    Do not prescribe without prior examination of patients who are likely to have a risk of developing cardiovascular disease.

    Do not apply for the treatment of a headache, which can be associated with a stroke, rupture of an aneurysm.

    Eletriptan, taken during the appearance of the aura, does not prevent the development of a headache, so it should not be used only during the phase of the headache.

    Do not use simultaneously with powerful inhibitors of the isoenzyme CYP3A4.

    In patients with impaired renal function, the antihypertensive effect of eletriptan is enhanced. With the use of eletriptan in doses of 60 mg or more (in the range of therapeutic doses), a small and transient increase in blood pressure was recorded. BP increased more in patients with impaired renal function and in elderly patients (no clinical effects were observed).

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