Zolmigren

Zolmigren is a medication used to treat migraines. Is selective agonist of special serotonin 5HT1-terminations and contains a component zolmitriptan.

Indications Zolmigrena

It is used for arresting a migraine attack (accompanied or not accompanied by an aura).

Release form

Release of the substance is made in tablets, packed in blister plates of 2 or 10 pieces. In the box - 1 packing plate.

Pharmacodynamics

Zolmitriptan is a selective agonist of specific serotonin 5-HT1B / 1D endings of the recombinant type within human vessels. The medication exhibits a moderate affinity with the aforementioned endings without showing a significant affinity or therapeutic activity with respect to 5HT2-, and in addition 5HT3- and 5HT4-endings of serotonin, α1-, α2-, β1-adrenergic endings, and in addition H1- and H2- endings of histamine, M-choline ends and D1- from D2-terminations of dopamine.

The drug has a vasoconstrictor effect on the cranial vessels, and in combination with this blocks the release of neuropeptides (among which the vasoactive peptide is of an intestinal nature, which acts as the main effector excitation modulator of the reflex type, it causes the process of vasodilation, which is the main one in migraine pathogenesis). Also, it stops the process of occurrence of a migraine attack, along with this without direct analgesic influence.

Combined with the relief of migraine attacks, the drug reduces the severity of nausea with vomiting (especially with the development of attacks of the left-side type), as well as background and photophobia. In addition to the peripheral influence, it affects the brain stem cells associated with migraine attacks, which explains the repeated result during the treatment of the series, consisting of several successive seizures in one patient.

Zolmigren demonstrates high effectiveness in combination with other drugs of therapy of migraine status (a series of several heavy, sequential migraine attacks lasting for 2-5 days). Eliminates also migraines, appearing against the background of menstruation. Large portions of drugs have a sedative effect and lead to a feeling of drowsiness.

The drug effect develops after 15-20 minutes, reaching its maximum after 60 minutes after ingestion. The maximum therapeutic effect is observed with the use of drugs during the development of a migraine attack.

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Pharmacokinetics

When ingested, the drug is well absorbed, penetrating the digestive tract. The degree of its absorption is not tied to the reception of food. The average absolute bioavailability is about 40%. Synthesis with blood proteins inside the plasma - 25%. It takes 60 minutes to reach the Cmax level of the drug; therapeutic values of drugs inside the plasma are maintained for the next 4-6 hours. After repeated use, the therapeutic component does not accumulate.

The drug undergoes intensive hepatic biotransformation, in which the N-desmethyl derivative is formed, which exerts a stronger (2-6 times) therapeutic effect than the source element and some inactive metabolic products.

The excretion of most of the medication occurs through the kidneys - in the form of metabolic products, and about 30% is excreted unchanged through the intestine.

Three main metabolic products of zolmitriptan were detected: heteroauxin (considered the main element inside urine with plasma), N-desmethyl-, and also N-oxide analogues. N-desmethylated substance has activity, and 2 other decay products are inactive.

The average half-life of zolmitriptan is 2.5-3 hours.

In females, Cmax and bioavailability are higher than in males (with lower clearance values).

In patients treated with moderate and also severe degree of renal insufficiency, the indicators of renal clearance of the active element and its metabolic products are 7-8 times lower in comparison with the indices of volunteers. The half-life increases by 60 minutes (maximum 3-3.5 hours), while the level of bioavailability of zolmitriptan with its active metabolic product increases only by 16%, and also by 35%.

In persons with a deficiency of the hepatic function, the metabolism of the active component of the drug decreases in accordance with the severity of the disease.

Dosing and administration

It is prohibited to use the medicine for prophylactic prevention of migraine attacks. Take it as soon as possible after the onset of a pain attack.

You need to take the first pill of drugs (contains 2.5 mg of the substance). If the effect of the application is absent, or a relapse occurred, another pill can be taken. Repeated doses should be taken at least after 2 hours from the moment of using the first dose.

If the dosage of 2.5 mg had a weak effect, it is possible to increase it to 5 mg (the maximum permissible 1-time dose). For a day it is allowed to take a maximum of 10 mg of the drug.

People with severe stages of disorders of liver activity can consume a maximum of 5 mg of the drug per day.

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Use Zolmigrena during pregnancy

The safety of the use of medication during pregnancy is not defined. Animal tests did not determine the direct teratogenic effects of drugs, but individual data from embryotoxicity tests indicate that embryonic viability is decreasing. Pregnant women can take Zolmigren only in situations where the probability of helping a woman is higher than the risk of complications in the fetus.

Tests also show that the medication is excreted with milk from nursing animals. There is no information on the passage of the substance into human breast milk. Because of this, lactating women should take the medicine very carefully. Influence of drugs on the baby should be minimized, so feeding should be done at least after 24 hours after using Zolmigren.

Contraindications

The main contraindications:

• presence of strong sensitivity with respect to medicinal elements;
• increased values of blood pressure of moderate or severe severity, and also having a weak intensity of uncontrolled increase in the level of pressure;
• IHD or similar manifestations that include a history of myocardial infarction;
• spontaneous angina;
• cerebrovascular disorders or TIA, present in the anamnesis;
• level of QC, reaching values below the 15 ml mark per minute;
• combined administration with ergotamine or substances that are its derivatives (among these are metisergide), and in addition to naratriptan or sumatriptan, and in addition other agonists of the 5HT1B / 1D;
• diseases affecting the function of peripheral vessels;
• use in the elderly (age over 65 years).

Side effects Zolmigrena

Negative symptoms when taking Zolmigren are often of a mild severity and usually temporary. They occur during the first 4 hours after the use of drugs, but do not increase with repeated admission; disappear independently, without the use of additional therapeutic measures. Among other side effects:

• Deficiency of immunity: symptoms of intolerance, including Quincke edema, urticaria and anaphylactic manifestations;
• disorders of the heart: tachycardia, a feeling of heartbeat, angina or myocardial infarction, as well as coronarospasm;
• problems in the operation of blood vessels: a slight increase in blood pressure, as well as a transient increase in blood pressure;
• dysfunction of the NS: dizziness, paresthesia, a strong feeling of heat, a noticeable sensitivity disorder or a significant feeling of drowsiness, hyperesthesia and headaches;
• manifestations affecting the functioning of the digestive tract: nausea, dysphagia, abdominal pain, dry mouth mucosa, vomiting, and also ischemia or infarction (for example, intestinal form or spleen infarction), manifested in the form of bloody diarrhea or pain in the peritoneum;
• disorders of urinary or renal function: increased frequency of urination, polyuria, and also imperative urges to urinate;
• lesions of the musculoskeletal structure and connective tissues: pain or weakness in the muscles;
• systemic disorders: a feeling of squeezing, severe gravity or pressure, or pain in the neck or throat region, and in addition, inside the sternum or extremities or asthenia.

Individual signs may be a consequence of the migraine itself.

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Overdose

Those who took a 1-fold dose of zolmitriptan (amounting to 0.05 g) of volunteers had a sedative effect.

The half-life of the element is 2.5-3 hours, which is why, in an overdose situation, the condition of the victim should be monitored for a minimum of 15 consecutive hours or until the symptoms disappear. The medicine does not have an antidote.

In case of severe poisoning, intensive care measures should be carried out, including free air flow through respiratory currents, adequate ventilation with oxygenation, and, in conjunction with this, control and support of CCC activities.

There is no data on how peritoneal dialysis with hemodialysis affect the serum values of the component.

Interactions with other drugs

Combination of the drug component with paracetamol or rifampicin, caffeine, and also with metoclopramide, propranolol, fluoxetine and pisotifenum is allowed.

Due to the fact that the probability of a coronarospasm arising in a patient may increase in a theory, the medicine should be consumed at least 24 hours after taking the medicines containing ergotamine. Also, on the contrary, ergotamine-containing medications use a minimum after 6 hours from the time of taking Zolmigren.

After using moclobemide (a specific preparation of IMAO-A), there was a slight increase in AUC (by 26%) for zolmitriptan, as well as a 3-fold increase in the same index for the active metabolic product. In this regard, those using MAOA-A should take a maximum of 5 mg Zolmitriptan per day. Medicines are not allowed to be consumed simultaneously when moclobemide is administered in a dose of more than 0.15 g 2 times a day.

With the use of cimetidine (a systemic inhibitor of element P450), the half-life of zolmitriptan increases by 44%, and the value of AUC by 48%. In addition, cimetidine doubles the half-life and the AUC value of the active metabolic product, the N-dimethylated component (183C91). People using cimetidine should use a maximum of 5 mg Zolmigrena per day.

Taking into account the general parameters of the interaction, it is quite probable that it is possible to bind with specific medicaments that slow down the activity of the CYP 1A2 component. Because of this, when combining such compounds (fluvoxamine and quinolones (this group includes ciprofloxacin)), it is also necessary to lower dosages.

When combined with the use of triptans with SSRIs or SSRIs, there was a development of serotonin intoxication (among the signs - vegetative instability, changes in mental state and neuromuscular anomalies).

Like the other agonists of the 5HT1B / 1D endings, the medication is able to inhibit the rate of absorption of other therapeutic drugs.

It is necessary to abandon the combined use of the drug with the remaining 5-HT1B / 1D element agonists for a period of time not less than 24 hours after their administration, and vice versa.

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Storage conditions

Zolmigren should be kept in a place that is closed from penetration of children. Temperatures are a maximum of 25 ° C.

Shelf life

Zolmigren can be used within 3 years of the manufacture of the drug.

Application for children

The medicine is not prescribed in pediatrics.

Analogues

The analogues of the drug are the drugs Rapimig, Antimigren, Relpax with Migrepam and Imigran, and in addition Amigrenin, Rizamigren, Stopmigren with Sumygren and Flamigran with Migranol. The list also includes Risatriptan-Pharmaten, Rapimed, Amigren, Sumatriptan and Antimigren-Health.

Reviews

Zolmigren receives many good reviews. Most patients who took the medicine to eliminate migraine attacks, mark its high efficiency. For many, this tool was generally the only one that brings the result.