Zolmigren (Zolmitriptan) 2.5mg 2 tabs — Made in Ukraine — Free Delivery

Pharmacological properties

Pharmacodynamics. Zolmigren is an anti-migraine agent. is a selective agonist of human recombinant 5ht1b / 1d serotonin receptors. has a moderate affinity for serotonin 5ht1a receptors, does not have significant affinity or pharmacological activity in relation to 5ht2-, 5ht3-, 5ht4-serotonin receptors, α1-, α2-, β1-adrenergic receptors, h1-, h2-histamine receptors, m -choline receptors, d1-, d2-dopaminergic receptors. The preparation causes vasoconstriction of mainly 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. stops the development of a migraine attack without a direct analgesic effect. Along with the relief of a migraine attack, it reduces the severity of 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 lasting 2–5 days. highly effective in 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 preparation develops in 15–20 minutes and reaches a maximum in 1 hour after administration. The maximum effect is noted when taken during the development of an attack.

Pharmacokinetics. When taken orally, it is well absorbed in the gastrointestinal tract. The absorption of the preparation does not depend on food intake. The average absolute bioavailability is about 40%. Plasma protein binding - 25%. The time to reach Cmax is 1 hour, the therapeutic concentration in the blood plasma is maintained for the next 4–6 hours. When the preparation is taken again, cumulation is not noted. 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 blood plasma and urine), N-oxide and N-desmethyl analogs. The N-desmethylated metabolite is active, while the other two metabolites are inactive. The average T½ of zolmitriptan is 2.5–3 hours. In women, Cmax and the bioavailability of the preparation are higher, and the total clearance is lower than in men. In patients with moderate and severe renal failure, the renal clearance of zolmitriptan and its metabolites is 7-8 times lower than that in healthy volunteers, T1 / 2 increases by an hour (up to 3-3.5 h), while the bioavailability of zolmitriptan and its the active metabolite increases by only 16 and 35%. In liver failure, the metabolism of zolmitriptan decreases in proportion to its degree.

Indications

Relief of migraine attacks with and without aura.

Application

The preparation is not intended for use in the prevention of a migraine attack. Zolmigren is recommended to be used as early 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 relapse of pain, repeated administration of 1 tablet is possible. If necessary, a repeated dose can be taken no earlier than 2 hours after taking the first dose.

If the dose of 2.5 mg is insufficiently effective, a single dose may be increased to 5 mg (the maximum single dose). The maximum daily dose is 10 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 preparation should not exceed 5 mg.

With a creatinine clearance of 15 ml / min, dose adjustment is not required.

Do not use in elderly patients (over 65 years of age).

Contraindications

Increased individual sensitivity to the components of the preparation.

Moderate or severe hypertension, as well as a mild uncontrolled increase in blood pressure. IHD, including a history of myocardial infarction. Angiospastic angina (Prinzmetal's angina). History of cerebrovascular disorders and transient ischemic attack. Creatinine clearance 15 ml / min. WPW syndrome and arrhythmia associated with other cardiac accessory pathways. Concomitant use of ergotamine, ergotamine derivatives (including methysergide), sumatriptan, naratriptan or other 5HT1B / 1D receptor agonists. Peripheral vascular disease. Do not use in elderly patients (over 65 years of age).

Side effects

They are usually mild, usually reversible, appear within 4 hours after taking the preparation, do not increase after repeated use, and disappear spontaneously without additional treatment.

From the immune system: hypersensitivity reactions, including urticaria, angioedema and anaphylactic reactions.

From the heart: palpitations, tachycardia, myocardial infarction, angina pectoris, coronary spasm.

From the side of the vessels: a slight increase in blood pressure, a temporary increase in blood pressure.

From the nervous system: impaired sensitivity, dizziness, headache, hyperesthesia, paresthesia, drowsiness, feeling of heat.

From the digestive tract: abdominal pain, nausea, vomiting, dry mouth, dysphagia, ischemia or heart attack (for example, intestinal ischemia, intestinal infarction, spleen infarction), which may manifest as diarrhea with blood or pain in the abdominal cavity.

From the kidneys and urinary system: polyuria, increased frequency of urination, urge to urinate.

From the musculoskeletal system and connective tissue: muscle weakness, muscle pain.

General disorders: asthenia, feeling of heaviness, constriction, pain or pressure in the throat, neck, chest and limbs.

Some of the symptoms may belong to the migraine itself.

Special instructions

The preparation should be taken only in cases where the diagnosis of migraine is accurately established. Before starting treatment for headache in patients who have not previously been diagnosed with migraine, other neurological conditions should be excluded. The preparation should not be taken for hemiplegic, basilar and ophthalmoplegic migraines.

In patients taking 5HT1B / 1D receptor agonists, stroke and other side cerebrovascular disorders may occur. It should be noted that individuals with migraine are at increased risk of cerebrovascular disorders.

In isolated cases, as well as with the use of other 5HT1B / 1D agonists, coronary spasm, angina pectoris and myocardial infarction are possible. Zolmigren should not be used in patients with risk factors for the development of coronary artery disease (for example, smoking, high blood pressure, hyperlipidemia, diabetes mellitus, heredity) without prior examination for the presence of diseases of the cardiovascular system. Particular attention should be paid to postmenopausal women and men over the age of 40 with these risk factors. However, examinations do not make it possible to identify every patient with heart disease, therefore, isolated cases of serious cardiac events were noted in patients without a history of cardiovascular disorders.

As with the use of other 5HT1B / 1D agonists, after taking zolmitriptan, a feeling of heaviness, pressure or squeezing in the heart area may appear. If chest pain or symptoms characteristic of ischemic heart disease appear, the use of Zolmigren should be discontinued and the patient should be examined.

As with the use of other 5HT1B / 1D agonists, a transient increase in blood pressure is possible in patients with both a history of elevated blood pressure and normal blood pressure. Very rarely, such an increase in blood pressure was combined with serious clinical manifestations. The recommended dose of Zolmigren should not be exceeded.

With the simultaneous use of triptans and herbal preparations containing St. John's wort, the frequency of adverse reactions may increase.

The occurrence of serotonin syndrome (including changes in mental state, autonomic lability, neuromuscular abnormalities) has been reported after the simultaneous use of triptans and selective serotonin reuptake inhibitors (SSRIs) or serotonin and norepinephrine reuptake inhibitors (SNRIs). These reactions can be severe. If the simultaneous use of zolmitriptan and SSRIs and SNRIs is clinically appropriate, 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 serotonergic agent.

Long-term use of any analgesic for headache can increase its severity. In such a situation, it is necessary to stop treatment and consult a doctor. A diagnosis of overtreatment headache should be suspected in patients with frequent or daily headache that is not relieved by regular medication.

The preparation contains lactose, therefore, in patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome, it should not be used.

Application during pregnancy or lactation

Pregnancy. The safety of using zolmitriptan during pregnancy has not been established. Animal tests have not revealed a direct teratogenic effect. However, some data from embryotoxicity tests indicate a decrease in embryo viability. During pregnancy, Zolmigren can be used only if the potential therapeutic effect for the mother outweighs the potential risk to the fetus / child.

Lactation. Studies have shown that zolmitriptan is absorbed into the milk of lactating animals. There is no data on the penetration of zolmitriptan into human breast milk. Therefore, women during breastfeeding should use the preparation with caution. The effect on the baby must be minimized, for which it should be fed no earlier than 24 hours after taking the preparation.

Children. The preparation should not be used to treat children.

The ability to influence the reaction rate when driving or working with other mechanisms. When the preparation was taken by a small group of healthy volunteers at a dose of up to 20 mg, there was no significant effect on the results of psychomotor tests.

However, vehicle drivers and persons whose work is associated with increased concentration of attention should be warned that in the event of a migraine attack, drowsiness and other symptoms may develop.

Interactions

A combination of the preparation with caffeine, paracetamol, metoclopramide, pizotifen, fluoxetine, rifampicin and propranolol is acceptable.

Given the data obtained with the participation of healthy volunteers, there is no pharmacokinetic interaction or any interaction of clinical significance between zolmitriptan and ergotamine. Since the risk of coronary spasm may theoretically increase, Zolmigren is recommended to be taken no earlier than 24 hours after the use of preparations containing ergotamine. Conversely, a preparation  containing ergotamine is recommended to be taken no earlier than 6 hours after using Zolmigren.

After taking moclobemide, a specific inhibitor of MAO-A, there was a slight increase (26%) in AUC for zolmitriptan and a threefold increase in AUC for the active metabolite. Therefore, for patients using MAO-A inhibitors, it is recommended to take zolmitriptan in a dose of no more than 5 mg / day. The preparations should not be used concurrently while taking moclobemide in a dose over 150 mg 2 times a day.

After taking cimetidine, a common inhibitor of P450, the T1 / 2 of zolmitriptan increased by 44% and the AUC by 48%. In addition, cimetidine doubled the T½ and AUC of the active N-dimethylated metabolite (183C91). For patients using cimetidine, it is recommended to take zolmitriptan in a dose not exceeding 5 mg / day.

Based on the general profile of interaction, the possibility of interaction with specific inhibitors of CYP 1A2 cannot be ruled out. Therefore, when using similar compounds, such as fluvoxamine and quinolones (for example, ciprofloxacin), it is also recommended to reduce the dosage.

From a pharmacokinetic point of view, selegiline (an MAO-B inhibitor) and fluoxetine (SSRI) do not interact with zolmitriptan.

After the simultaneous use of triptans and SSRIs or SNRIs, the appearance of serotonin syndrome (including changes in mental state, autonomic lability, neuromuscular abnormalities) was reported.

Like other 5HT1B / 1D receptor agonists, zolmitriptan can slow the absorption of other preparations.

Avoid the simultaneous use of zolmitriptan with other 5HT1B / 1D agonists for 24 hours and vice versa.

Overdose

A sedative effect was observed in volunteers who used a single dose of 50 mg zolmitriptan.

T1 / 2 of zolmitriptan is 2.5-3 hours, therefore, patients should be observed after an overdose for at least 15 hours or until symptoms disappear. There is no specific antidote.

In case of severe intoxication, intensive care procedures are recommended, including ensuring airway patency, adequate oxygenation and ventilation, monitoring and supporting the functions of the cardiovascular system.

It is not known how hemodialysis and peritoneal dialysis affect serum zolmitriptan concentration.

Storage conditions

In its original packaging at a temperature not exceeding 25 ° c.