Zolmigren (zolmitriptan) coated tablets 2.5 mg. №10

$34.00

Stopping a migraine attack with an aura and without an aura. Means used for migraine. Selective agonists of 5HT1 serotonin receptors.

Category:

Description

Dosage form

Film-coated tablets 2.5 mg

Composition

One tablet contains

active substance – zolmitriptan in terms of 100% substance – 2.5 mg auxiliary substances: lactose monohydrate, microcrystalline cellulose 102, sodium starch glycolate, magnesium stearate

shell composition: Sepifilm 752 Blanc **, iron (III) oxide yellow Е172

** Shell composition: methylhydroxypropyl cellulose, microcrystalline cellulose, macrogol-40, titanium dioxide E 171

Description

Round tablets with a biconvex surface, film-coated, pale brownish-yellow color.

Pharmacotherapeutic group

Analgesics. Anti-migraine drugs. Stimulants of 5HT1D-serotonin receptors. Zolmitriptan

ATX code N02CC03

Pharmacological properties

Pharmacokinetics

When taken orally, it is well absorbed in the digestive tract. The absorption of the drug does not depend on food intake. The average absolute bioavailability is about 40%. Plasma protein binding – 25%. The time to reach the maximum concentration is 1 hour, the therapeutic plasma concentration is maintained for the next 4-6 hours. With repeated administration, the cumulation of the drug is not observed. It undergoes intensive biotransformation in the liver with the formation of N-desmethyl derivative, which has 2-6 times higher pharmacological activity than the parent compound, and a number of inactive metabolites. It is excreted from the body mainly by the kidneys in the form of metabolites, about 30% – by the intestines unchanged. There are three main metabolites of zolmitriptan: indoleacetic acid (the main metabolite in plasma and urine), N-oxide and N-desmethyl analogs. The N-desmethylated metabolite is active, and the other two metabolites are inactive. The average half-life (T1 / 2) of zolmitriptan is 2.5-3 hours. In women, the maximum concentration and bioavailability of the drug is higher, and the total clearance is lower than in men. In patients with moderate and severe renal insufficiency, the renal clearance of zolmitriptan and its metabolites is 7-8 times less than in healthy volunteers, the half-life increases by an hour (up to 3-3.5 hours), while the bioavailability of zolmitriptan and its active metabolite increases only by 16 and 35%.

Pharmacodynamics

Anti-migraine agent

It is a selective agonist of human recombinant 5-HT1B / 1D serotonin receptors. It has a moderate affinity for serotonin 5-HT1A receptors, does not have significant affinity or pharmacological activity in relation to 5HT2-, 5HT3-, 5HT4-serotonin receptors, 1-, 2-, 1-adrenergic receptors, H1-, H2 -histamine receptors, M-choline receptors, D1-, D2-dopaminergic receptors. The drug causes vasoconstriction, predominantly of cranial vessels, blocks the release of neuropeptides, in particular vasoactive intestinal peptide, which is the main effector transmitter of reflex excitation that causes vasodilation, which is the basis of the pathogenesis of migraine. Suspends the development of a migraine attack without direct analgesic action. Along with the relief of a migraine attack, it weakens nausea, vomiting (especially with left-sided attacks), photo- and phonophobia. In addition to peripheral action, it affects the centers of the brain stem associated with migraine, which explains the persistent repeated effect in the treatment of a series of several migraine attacks in one patient. It is highly effective in the complex treatment of migraine status (a series of several severe, following one after another migraine attacks lasting 2-5 days). Eliminates the migraine associated with menstruation. High doses are sedative and cause drowsiness.

The effect of the drug develops in 15-20 minutes and reaches a maximum one hour after administration. The maximum effect is observed when taken during the development of an attack.

Indications for use

migraine attack with an aura (visual, auditory, movement and mental disorders) and without aura

Method of administration and dosage

The drug is not intended for use in the prevention of migraine attacks. Zolmigren is recommended to be used as soon as possible after the onset of a migraine attack.

Adults are prescribed 1 tablet (2.5 mg zolmitriptan). In the absence of effect or in case of recurrence of pain, repeated administration of 1 tablet is possible. If necessary, a repeated dose can be taken no earlier than 2 hours after the first dose. If the dose of 2.5 mg is insufficiently effective, a single dose may be increased to 5.0 mg (the highest single dose). The highest daily dose is 10.0 mg.

No dose adjustment is required for patients with mild to moderate hepatic impairment. For patients with severely impaired liver function, the daily dose of the drug should not exceed 5 mg.

Side effects

Often:

  • abnormalities or abnormalities of the sensory organs, dizziness, headache, hyperesthesia, a feeling of heat, drowsiness, sensory disturbances in the neck, limbs and chest, paresthesia, dysesthesia
  • myalgia, muscle weakness
  • palpitations
  • asthenia, a feeling of heaviness and constriction in the throat, neck, chest, and limbs

Seldom:

  • tachycardia, transient increase in blood pressure
  • polyuria, frequent urination
  • hypersensitivity reactions, including urticaria, Quincke’s edema and anaphylactic reactions

Contraindications

  • increased individual sensitivity to drug components
  • severe arterial hypertension
  • cardiac ischemia
  • previous myocardial infarction
  • angiospastic angina (Prinzmetal’s angina)
  • history of stroke or transient ischemic attack (TIA)
  • Wolff-Parkinson-White syndrome or arrhythmias associated with accessory pathways
  • hemiplegic and basilar migraine
  • children and adolescents up to 18 years old
  • advanced age (over 65)

Drug interactions

It is possible to use the drug simultaneously with caffeine, ergotamine, dihydroergotamine, paracetamol, metoclopramide, pizotifen, rifampicin and propronalol. There were no clinically significant interactions between zolmitriptan and ergotamine, including pharmacokinetic ones. However, theoretically, the risk of coronary spasm may increase. It is recommended to take Zolmigren no earlier than 24 hours after the use of preparations containing ergotamine. Conversely, it is recommended to take a preparation containing ergotamine no earlier than 6 hours after using Zolmigren.

Simultaneous use with other drugs of the 5-HT1B / 1D agonist group is not recommended.

When taken together with moclobemide (a specific MAO-A inhibitor), the bioavailability of zolmitriptan increases, and therefore, for patients taking moclobemide, the recommended daily dose of zolmitriptan should not exceed 5 mg. The drugs should not be used concurrently when taking moclobemide in doses over 150 mg twice a day.

When taken together with cimetidine, the half-life and bioavailability of zolmitriptan increase, and therefore for patients taking cimetidine, the recommended daily dose of zolmitriptan should not exceed 5 mg. The possibility of interaction of zolmitriptan with inhibitors of the CYP1A2 isoenzyme of cytochrome P450 cannot be ruled out. Based on this, with the combined use of zolmitriptan with drugs, the metabolism of which occurs with the participation of this enzyme, the daily dose should not exceed 5 mg.

From the point of view of pharmacokinetics, selegiline (MAO-B inhibitor) and fluoxetine (SSRI) do not interact with zolmitriptan. After the simultaneous use of triptans and selective serotonin reuptake inhibitors (SSRIs) or serotonin and norepinephrine reuptake inhibitors (SSRIs), serotonin syndrome has been reported (including changes in mental state, autonomic lability, neuromuscular disorders). These reactions can be severe. If the simultaneous use of zolmitriptan and SSRIs and SSRIs is clinically advisable, it is recommended to conduct an appropriate examination of the patient, especially at the beginning of treatment, with an increase in the dose or the use of another serotoninergic agent. Like other 5HT1B / 1D receptor agonists, zolmitriptan can slow the absorption of other drugs.

Special instructions

The drug should be used only in cases where the diagnosis is accurately established.

migraine

Before starting treatment for headaches in patients who have not been diagnosed with migraine before or in patients prone to migraine who have atypical symptoms, other neurological conditions should be excluded.

In isolated cases, as well as with the use of other 5HT1B / 1D agonists, coronary spasm, angina attacks and myocardial infarction have been reported. In the presence of factors that contribute to the development of coronary heart disease (for example, tobacco smoking, high blood pressure, hyperlipidemia, diabetes mellitus, heredity), the drug should be prescribed only after examining the patient for the presence of diseases from the cardiovascular system.

In some patients, after taking zolmitriptan, there may be a feeling of heaviness, pressure or compression in the heart area. If chest pain or symptoms characteristic of coronary heart disease appear, the drug should be discontinued and the patient examined. In patients with both a history of high blood pressure and normal blood pressure, a transient increase in blood pressure has been reported. Very rarely, such an increase in blood pressure is manifested by serious clinical manifestations. Zolmigren should be used in a dose not exceeding the recommended dose. The drug contains lactose, so it should be used with caution in patients with congenital lactose deficiency.

Application during pregnancy or lactation

The safety of using the drug during pregnancy has not been established. During pregnancy and lactation, Zolmigren is used only if the possible therapeutic effect for the mother outweighs the potential risk to the fetus. There is no data on the penetration of zolmitriptan into breast milk. Therefore, it is necessary to prescribe Zolmigren with caution to women who are breastfeeding. The impact on the child must be minimized; for this, you should breastfeed no earlier than 24 hours after taking the drug.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

The drug should not be used during work by drivers of vehicles and persons whose work is associated with increased concentration of attention, since drowsiness may develop.

Overdose

Symptoms:

taking a single dose of zolmitriptan at a dose of 50 mg, a sedative effect was observed.

Treatment:

gastric lavage, the use of activated carbon, symptomatic therapy, incl. ensuring airway patency, monitoring and maintaining the functions of the cardiovascular system. There is no specific antidote.

Storage conditions

Store in a dark place at a temperature not exceeding 25 ° C.

Keep out of the reach of children!

Storage period

3 years

Do not use the drug after the expiration date indicated on the package.

Terms of dispensing from pharmacies

On prescription