Migraine tablets Relpax: instructions for use, price, reviews and analogues

Release form

The product is available in the form of tablets of 20 and 40 mg, which are packaged in foil blisters placed in cardboard boxes.

Tablets, 20 mg, orange, biconvex, round. They are covered with a film coating, on one side of the tablet there is an engraving “REP 20”, on the other - “Pfizer”.
Tablets, 40 mg, orange, biconvex, round. They are covered with a film coating, on one side of the tablet there is an engraving “REP 40”, on the other - “Pfizer”.

Pharmacokinetics and pharmacodynamics

After oral administration, eletriptan is actively absorbed from the digestive tract, absorption occurs by 81%. The level of bioavailability when taken internally is approximately 50%.

The highest concentration in the blood is observed 1.5 hours after internal administration. The maximum concentration of the active substance increased by 20–30% if the medicine was taken after a fatty meal. Eletriptan is 85% bound to blood proteins.

The half-life is approximately 4-5 hours. Metabolism occurs in the liver, after which excretion occurs through the kidneys and gastrointestinal tract.

Pharmacological properties of the drug Eletriptan

A drug used for migraine, a selective agonist of serotonin 1B/1D (5-HT1B/1D) receptors. Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has moderate affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors and does not exhibit affinity for 5-HT2A-, 5-HT2C-, 5-HT3-, 5-HT4-, 5-HT5A-, and 5-HT6 receptors. Eletriptan has no pharmacological activity at α1-, α2-, β-adrenergic, D1-, D2-dopaminergic, muscarinic and opioid receptors. The effectiveness of serotonin receptor agonists in the treatment of migraine is explained by the trigeminovascular hypothesis, according to which, on the one hand, by stimulating 5-HT1 receptors located on the sensory nerve endings of the trigeminal nerve, they inhibit the conduction of pain impulses and the release of proinflammatory neuropeptides, and, on the other hand, by stimulating similar receptors of cerebral vessels, including arteriovenous anastomoses, increase their tone. It has been experimentally established that eletriptan inhibits the activity of the trigeminal nerve and also causes a decrease in blood flow in the carotid system in combination with a slight increase in blood pressure when used in high doses. Despite the predominantly selective effect on blood flow in the carotid arterial bed, a decrease in the diameter of the coronary arteries was also observed. Eletriptan is well absorbed after oral administration, with maximum plasma concentrations achieved approximately 1.5–2 hours after administration. Absolute bioavailability is about 50%. The AUC and maximum concentration of eletriptan increase by approximately 20–30% after coadministration with a fatty meal. The volume of distribution of eletriptan after intravenous administration is 138 l. Plasma protein binding - 85%. The only known active metabolite of eletriptan is the N-demethylated metabolite. The estimated half-life of the N-demethylated metabolite is about 13 hours, and its concentration in the blood plasma is 10–20% of the concentration of the parent compound. Eletriptan is metabolized primarily with the participation of the cytochrome P450 isoenzyme CYP 3A4. The terminal half-life of eletriptan is approximately 4 hours. The average renal clearance after oral administration is approximately 3.9 L/h, extrarenal clearance accounts for about 90% of the total clearance. The main pharmacokinetic parameters of eletriptan are generally independent of the age and gender of patients.

Contraindications

The following contraindications for taking the drug Relpax are defined:

high sensitivity of the patient to eletriptan and other components of the drug;
reception for the purpose of relieving basilar , ophthalmoplegic , hemiplegic migraine ;
serious liver dysfunction;
rare hereditary diseases ( glucose-lactose malabsorption , lactase deficiency, lactose intolerance);
concomitant use with CYP3A4 inhibitors and protease inhibitors;
uncontrolled arterial hypertension
age under 18 years;
occlusive diseases of peripheral vessels;
coronary heart disease or suspicion of having this disease;
of transient ischemic attack and cerebral circulatory disorders;
simultaneous treatment with other drugs - 5-HT1 receptor agonists.

The drug is prescribed with caution to patients with serotonin syndrome . You should also be careful when using Relpax simultaneously with other drugs with serotonergic activity.

Caution should be exercised when taking medication at a dose of more than 40 mg to people who have impaired renal function.

Eletriptan

The use of Eletriptan in combination with potent inhibitors of the CYP3A4 isoenzyme, in particular ketoconazole, itraconazole, erythromycin, clarithromycin, josamycin and HIV protease inhibitors such as ritonavir, indinavir and nelfinavir, is not recommended (see section “Interaction with other drugs”). In addition, Eletriptan should not be taken within 72 hours after completion of CYP3A4 inhibitors.

Like other 5-HT1 serotonin receptor agonists, Eletriptan should be used only in cases where the diagnosis of migraine is beyond doubt. Eletriptan, like other 5-HT1-serotonin receptor agonists, should not be prescribed for the treatment of “atypical” headaches that may be associated with serious diseases (stroke, ruptured aneurysm) where cerebral vasoconstriction may be harmful.

During the use of 5-HT1-serotonin receptor agonists, cases of cerebral hemorrhage, subarachnoid hemorrhage, stroke or other cerebrovascular disorders, in some cases fatal, have been reported.

In several cases, cerebrovascular disorder was the underlying disease and 5-HT1-serotonin receptor agonists were used incorrectly, interpreting the symptoms as signs of migraine. It should be taken into account that patients with migraine may have an increased risk of cerebrovascular complications (eg, stroke, hemorrhage and transient ischemic attack).

With the simultaneous use of eletriptan and SSRIs (for example, fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram) and SNRIs (for example, venlafaxine, duloxetine), the development of potentially life-threatening serotonin syndrome is possible (see sections “With caution” and “Interaction with other drugs”). means"). This syndrome may present with the following symptoms: mental status disturbance (eg, agitation, hallucinations, coma), autonomic instability (eg, tachycardia, blood pressure fluctuations, hyperthermia), neuromuscular dysfunction (eg, hyperreflexia, incoordination), and/or symptoms of digestive system dysfunction (for example, nausea, vomiting, diarrhea).

It is not recommended to use Eletriptan in patients with risk factors for the development of coronary artery disease (for example, hypertension, hypercholesterolemia, smoking, obesity, diabetes mellitus, family history, women in surgical or physiological menopause, or men over 40 years of age) until a thorough examination of the circulatory system will not be carried out and cardiovascular disease will not be excluded. The sensitivity of methods for assessing the state of the cardiovascular system is quite low. In this regard, if the patient’s history, ECG or other diagnostic procedures revealed signs characteristic of arterial vasospasm or myocardial ischemia, the use of eletriptan is not recommended (see section “Contraindications”).

In patients with risk factors for cardiovascular disease (CVD), but whose CV assessment has shown a satisfactory result, it is recommended that the first dose of eletriptan be taken under medical supervision, except for patients who have previously received eletriptan. Since myocardial ischemia can occur in the absence of clinical symptoms, an electrocardiographic study should be considered immediately after taking Eletriptan.

Patients with CV risk factors as described above who are receiving eletriptan long-term but intermittently should undergo periodic CV monitoring as they continue eletriptan therapy.

Systematic adherence to the above recommendations leads to a decrease in the incidence of patients with undiagnosed CVD receiving eletriptan therapy.

Cases of severe cardiac dysfunction, including myocardial infarction, life-threatening cardiac arrhythmias, and death, have been reported with the use of 5-HT1-serotonin receptor agonists in the first few hours after taking the drug. Given the widespread use of 5-HT1-serotonin receptor agonists in patients with migraine, the incidence of these reactions is extremely low.

During clinical trials, the following reports were received: among patients undergoing diagnostic coronary angiography, one patient receiving intravenous eletriptan (Cmax-127 ng/ml, equivalent to 60 mg oral eletriptan) with a history of angina pectoris had hypertension. and hypercholesterolemia, a feeling of tightness in the chest arose, and an episode of coronary vasospasm (confirmed by angiography) was detected without ECG changes characteristic of ischemia. In addition, one case of atrial fibrillation has been reported in a patient with a history of the same arrhythmia.

Eletriptan should not be prescribed without prior evaluation to patients who are likely to have CVD or are at increased risk of developing it (see section “Contraindications”). Systemic studies of eletriptan in patients with heart failure have not been conducted. The use of eletriptan, as well as other 5-HT1-serotonin receptor agonists, is not recommended in these patients.

Eletriptan is effective in the treatment of migraine with and without aura and migraine associated with the menstrual cycle. Eletriptan taken during the onset of an aura does not prevent the development of headaches, so it should only be taken during the headache phase. Clinical studies have found that Eletriptan is also effective in relieving symptoms accompanying migraine, such as nausea, vomiting, photophobia, phonophobia, and in treating the return of headaches during an attack.

Eletriptan should not be taken prophylactically.

When using the drug Eletriptan in therapeutic doses of 60 mg or more, a slight transient increase in blood pressure was recorded. Blood pressure increased more often in patients with impaired renal function (maximum systolic pressure increased by 14-17 mm Hg, and diastolic pressure by 14-21 mm Hg from the initial level and 3-4 mm Hg higher, than in healthy volunteers) and elderly people.

It should be borne in mind that unlimited use of antimigraine drugs can lead to chronic daily headaches. Cases of overuse of any triptans most often occur in patients with daily headaches.

Side effects

In most cases, patients tolerate Relpax well. As a rule, side effects are mild, they disappear on their own and are transient.

The following side effects may occur while taking the drug:

rhinitis , pharyngitis , respiratory tract infections;
lymphadenopathy;
anorexia;
mental disorders : confusion, thinking disorders, depression , euphoria , emotional lability;
disorders of the nervous system: headaches , drowsiness , dizziness , hypoesthesia , hypokinesia , sensitivity disorders, myasthenia gravis , hyperesthesia , tremor , ataxia , speech impairment;
feeling of tightness in the throat, yawning , dyspnea , change in voice timbre, asthma ;
hyperbilirubinemia;
functions of the visual organs: eye pain, blurred vision, photophobia, conjunctivitis;
functions of the heart and blood vessels: tachycardia , rapid heartbeat, angina pectoris , bradycardia, increased blood pressure;
organs of hearing, balance: ringing and pain in the ears, vertigo ;
gastrointestinal functions: abdominal pain, nausea, dry mouth, dyspepsia, diarrhea , constipation, belching;
skin: severe sweating, itching , urticaria ;
musculoskeletal system: pain in the back, joints and muscles, arthritis , bone pain, arthrosis, myopathy, cramps;
urinary system: polyuria , frequent urination ;
reproductive system: menorrhagia , pain in the mammary glands;
allergic reactions;
feeling of hot flushes to the face, asthenia, chills, discomfort in the chest, general weakness, feeling of thirst, peripheral edema.

Relpax 40 mg 2 pcs. film-coated tablets

pharmachologic effect

Antimigraine.

Composition and release form Relpax 40 mg 2 pcs. film-coated tablets

Tablets - 1 tablet:

active substance: eletriptan (in the form of hydrobromide) - 20/40 mg;
excipients: MCC; lactose monohydrate; croscarmellose sodium; magnesium stearate;
film shell: Opadry orange OY-LS-23016 (hypromellose, lactose monohydrate, titanium dioxide (E171), triacetin, Sunset yellow dye with aluminum varnish (E110); Opadry transparent YS-2-19114-A (hypromellose, triacetin )

Film-coated tablets, 20 mg, 40 mg. In PVC/aluminum foil blister, 2, 3, 4, 6 or 10 pcs. 1, 2, 3, 4, 5, 6 or 10 blisters in a cardboard box.

Description of the dosage form

Tablets, 20 mg: orange, round, biconvex, film-coated, debossed with "REP 20" on one side and "Pfizer" on the other side.

Tablets, 40 mg: orange, round, biconvex, film-coated, debossed with "REP 40" on one side and "Pfizer" on the other side.

Directions for use and doses

Inside, swallow whole, with water.

When a migraine headache occurs, Relpax® should be taken as early as possible, but the drug is also effective at a later stage of a migraine attack.

Adults (18–65 years old)

The recommended starting dose is 40 mg.

If the headache returns within 24 hours: If the migraine headache stops, but then recurs within 24 hours, then Relpax® can be re-prescribed at the same dose. If a second dose is necessary, it should be taken no earlier than 2 hours after the first dose.

If there is no effect: if the first dose of Relpax® does not reduce the headache within 2 hours, then to relieve the attack, you should not take the second dose, because The effectiveness of this treatment has not been proven in clinical studies. At the same time, patients who failed to stop an attack can give an effective clinical response during the next attack.

If taking the drug at a dose of 40 mg does not achieve an adequate effect, then for subsequent migraine attacks a dose of 80 mg may be effective.

The daily dose should not exceed 160 mg.

In patients with mild or moderate liver dysfunction, no dose change is required.

Pharmacodynamics

Eletriptan is a member of a group of selective agonists of serotonin vascular 5-HT1B and neuronal 5-HT1D receptors. Eletriptan also has high affinity for 5-HT1F receptors and has moderate effects on 5-HT1A, 5-HT2B, 5-HT1E and 5-HT7 receptors.

Compared with sumatriptan, eletriptan exhibits significantly greater selectivity for serotonin receptors located in the carotid arteries than for serotonin receptors located in the coronary and femoral arteries. The ability of eletriptan to constrict intracranial blood vessels, as well as its inhibitory effect on neurogenic inflammation, may contribute to its antimigraine activity.

Pharmacokinetics

Suction. After oral administration, eletriptan is quickly and fairly completely absorbed into the gastrointestinal tract, absorption is about 81%. Absolute bioavailability when taken orally in men and women is about 50%. Tmax in plasma averaged 1.5 hours after oral administration. In the range of therapeutic doses from 20 to 80 mg, the pharmacokinetics of eletriptan is characterized by a linear dependence.

Eletriptan Cmax and AUC increased by approximately 20–30% when taking the drug after consuming a fatty meal. When taken orally during a migraine attack, AUC decreased by approximately 30%, and Tmax in blood plasma increased to 2.8 hours.

With regular use (20 mg 3 times a day) for 5–7 days, the pharmacokinetics of eletriptan remained linear with predictable accumulation. When prescribed in higher doses (40 mg 3 times a day and 80 mg 2 times a day) for more than 7 days, the accumulation of eletriptan was higher than expected (by approximately 40%).

Distribution. Vd of eletriptan with intravenous administration is 138 l, which indicates good distribution in tissues. Eletriptan is moderately bound to plasma proteins (approximately 85%).

Metabolism. In vitro studies indicate that the primary metabolism of eletriptan occurs under the influence of the cytochrome P450 isoenzyme CYP3A4 in the liver. This fact is confirmed by an increase in the concentration of eletriptan in the blood plasma while taking erythromycin, which is a powerful selective inhibitor of the CYP3A4 isoenzyme. In vitro studies also demonstrate that the CYP2D6 isoenzyme makes a certain contribution to the metabolism of eletriptan, although clinical studies have not revealed the effect of polymorphism of this enzyme on the pharmacokinetics of eletriptan.

Two main circulating metabolites have been identified, the proportion of which constitutes a significant part of the total radioactivity of the blood plasma after administration of eletriptan, labeled with the 14C carbon isotope.

In in vitro experiments, the metabolite formed as a result of N-oxidation had no activity, while the metabolite formed as a result of N-demethylation was comparable in activity to eletriptan. The third component of the radioactive plasma has not been identified. It is believed to be a mixture of hydroxylated metabolites, which are also excreted by the kidneys and intestines.

The concentration of the active N-demethylated metabolite in the blood plasma is only 10–20% of the concentration of eletriptan and, accordingly, does not make a significant contribution to its therapeutic effect.

Excretion. The total clearance of eletriptan from blood plasma after intravenous administration averages 36 l/h, and T1/2 is about 4 hours. The average renal clearance after oral administration is about 3.9 l/h. The proportion of non-renal clearance is about 90% of the total clearance; this indicates that eletriptan is excreted primarily as metabolites by the kidneys and intestines.

Special patient groups

Floor. The results of a meta-analysis of clinical pharmacological studies and population pharmacokinetic analysis indicate that gender does not have a clinically significant effect on the concentration of eletriptan in blood plasma.

Elderly people (over 65 years old). In elderly people (65–93 years), a small and statistically insignificant decrease in the clearance of eletriptan by 16% and a statistically significant increase in T1/2 (from approximately 4.4 to 5.7 hours) was detected compared with these indicators in young people. The effect of eletriptan on blood pressure may be more pronounced in older people compared to younger patients.

Liver dysfunction. In patients with impaired liver function (stages A and B according to the Child-Pugh classification), a statistically significant increase in AUC (by 34%) and T1/2 was detected, as well as a slight increase in Cmax (by 18%), but these changes are not clinically significant .

Renal dysfunction. In patients with mild (Cl creatinine 61–89 ml/min), moderate (Cl creatinine 31–60 ml/min) or severe (Cl creatinine

Indications for use Relpax 40 mg 2 pcs. film-coated tablets

Relief of migraine attacks with or without aura.

Contraindications

hypersensitivity to eletriptan or any other component of the drug;
severe liver dysfunction;
simultaneous use with CYP3A4 inhibitors (ketoconazole, itraconazole, erythromycin, clarithromycin, josamycin) and protease inhibitors (ritonavir, indinavir and nelfinavir);
within 24 hours before or after taking eletriptan, you should not use ergotamine or ergotamine derivatives, incl. methysergide;
relief of hemiplegic, ophthalmoplegic or basilar migraine;
rare hereditary diseases (lactose intolerance, lactase deficiency or glucose-lactose malabsorption);
age under 18 years (data on the effectiveness and safety of the drug in this age group are limited).

As with other 5-hydroxytryptamine type I (5-HT1) receptor agonists, the following contraindications to the use of eletriptan are based on its pharmacodynamic properties:

uncontrolled arterial hypertension;
coronary heart disease (angina pectoris, Prinzmetal's angina, previous myocardial infarction, confirmed asymptomatic myocardial ischemia) or suspicion of its presence;
occlusive diseases of peripheral vessels;
a history of cerebrovascular accident or transient ischemic attack;
combined use with other 5-HT1 receptor agonists.

With caution: serotonin syndrome - when simultaneous use of eletriptan with other drugs that have serotonergic activity, such as SSRIs and SNRIs, caution must be exercised, because in some cases, there have been reports of the development of serotonin syndrome while taking eletriptan and other serotonergic drugs; use of the drug at a dose higher than 40 mg in patients with impaired renal function (since in such patients the effect of eletriptan on blood pressure is enhanced).

Application of Relpax 40 mg 2 pcs. film-coated tablets during pregnancy and breastfeeding

There is no experience of clinical use of the drug Relpax® in pregnant women. In animal studies, the drug did not have a teratogenic effect. Relpax® should be prescribed only in cases where the expected benefit to the mother significantly outweighs the possible risk to the fetus.

Relpax® is excreted in breast milk in women. With a single dose of Relpax® in a dose of 80 mg, excretion into breast milk over 24 hours averaged 0.02% of the dose taken. The risk of neonatal exposure to the drug can be minimized by not breastfeeding for 24 hours after taking eletriptan.

special instructions

The use of Relpax® in combination with potent inhibitors of the CYP3A4 isoenzyme, in particular ketoconazole, itraconazole, erythromycin, clarithromycin, josamycin and HIV protease inhibitors such as ritonavir, indinavir and nelfinavir, is not recommended (see section “Interaction with other drugs”). In addition, Relpax® should not be taken within 72 hours after completion of CYP3A4 inhibitors.

Like other 5-HT1 serotonin receptor agonists, Relpax® should be used only in cases where the diagnosis of migraine is beyond doubt. Relpax®, like other 5-HT1 serotonin receptor agonists, should not be prescribed for the treatment of “atypical” headaches that may be associated with serious diseases (stroke, ruptured aneurysm) where cerebral vasoconstriction may be harmful.

During the use of 5-HTV serotonin receptor agonists, cases of cerebral hemorrhage, subarachnoid hemorrhage, stroke or other cerebrovascular disorders, in some cases fatal, have been reported. In several cases, cerebrovascular disorder was the underlying disease and 5-HT1-serotonin receptor agonists were used incorrectly, interpreting the symptoms as signs of migraine. It should be taken into account that patients with migraine may have an increased risk of cerebrovascular complications (eg, stroke, hemorrhage and transient ischemic attack).

With the simultaneous use of eletriptan and SSRIs (for example, fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram) and SNRIs (for example, venlafaxine, duloxetine), potentially life-threatening serotonin syndrome may develop. This syndrome may present with the following symptoms: mental status disturbance (eg, agitation, hallucinations, coma), autonomic nervous system instability (eg, tachycardia, blood pressure fluctuations, hyperthermia), neuromuscular dysfunction (eg, hyperreflexia, incoordination), and/ or symptoms of digestive system dysfunction (eg, nausea, vomiting, diarrhea).

It is not recommended to use the drug Relpax® in patients with risk factors for the development of coronary heart disease (for example, arterial hypertension, hypercholesterolemia, smoking, obesity, diabetes mellitus, family history, women in surgical or physiological menopause, or men over the age of 40 years) until until a thorough examination of the circulatory system has been carried out and cardiovascular disease has been ruled out.

The sensitivity of methods for assessing the state of the cardiovascular system is quite low. In this regard, if the patient's history, ECG, or other diagnostic procedures revealed signs characteristic of arterial vasospasm or myocardial ischemia, the use of eletriptan is not recommended.

In patients with risk factors for cardiovascular disease, but in whom the assessment of the state of the cardiovascular system has shown a satisfactory result, it is recommended that the first dose of eletriptan be taken under the supervision of a physician, except for patients who have previously received eletriptan. Since myocardial ischemia can occur in the absence of clinical symptoms, an electrocardiographic study should be considered immediately after taking Relpax®.

Patients with cardiovascular risk factors as described above who are receiving eletriptan long-term but intermittently should undergo periodic cardiovascular evaluations as they continue eletriptan therapy. Systematic adherence to the above recommendations leads to a decrease in the incidence of patients with undiagnosed cardiovascular diseases receiving eletriptan therapy.

When using 5HT1-serotonin receptor agonists, cases of severe cardiac dysfunction, including myocardial infarction, life-threatening cardiac arrhythmias and deaths, have been reported in the first few hours after taking the drug. Considering the widespread use of 5HT1-serotonin receptor agonists in patients with migraine, the incidence of these reactions is extremely low.

The following reports were received during clinical studies. Among patients undergoing diagnostic coronary angiography, one patient receiving intravenous eletriptan (Cmax 127 ng/mL, equivalent to 60 mg oral eletriptan) with a history of angina pectoris, hypertension, and hypercholesterolemia experienced chest tightness, and an episode of coronary vasospasm (confirmed by angiography) was detected without ECG changes characteristic of ischemia. In addition, one case of atrial fibrillation has been reported in a patient with a history of the same arrhythmia.

In the post-marketing period, cases of severe cardiovascular complications, some of which were fatal, have been reported. In very rare cases, these complications occurred in the absence of any signs of cardiovascular disease. However, given the difficulty of monitoring reports received in the post-marketing period, it is impossible to definitively determine the relationship of these cases with eletriptan. Relpax® should not be prescribed without prior examination to patients who are likely to have cardiovascular diseases or are at increased risk of developing them (see section “Contraindications”). Systemic studies of eletriptan in patients with heart failure have not been conducted. The use of eletriptan, like other 5HT1 serotonin receptor agonists, is not recommended in these patients.

Relpax® is effective in the treatment of migraine with and without aura and migraine accompanying the menstrual cycle. Relpax® taken during the onset of an aura does not prevent the development of headaches, so it should only be taken during the headache phase.

Clinical studies have found that Relpax® is also effective in relieving symptoms accompanying migraine, such as nausea, vomiting, photophobia, phonophobia, and in treating the return of headaches during an attack.

Relpax® should not be taken prophylactically.

When using the drug Relpax® in therapeutic doses of 60 mg or more, a slight transient increase in blood pressure was recorded. Blood pressure increased more often in patients with impaired renal function (maximum systolic pressure increased by 14-17 mm Hg, and diastolic pressure by 14-21 mm Hg from the initial level and by 3-4 mm Hg higher than in healthy volunteers) and older people.

It should be borne in mind that unlimited use of antimigraine drugs can lead to chronic daily headaches. Cases of overuse of any triptans most often occur in patients with daily headaches.

Impact on the ability to drive vehicles and operate machinery

In some patients, migraine or taking 5HT1-serotonin receptor agonists, including eletriptan, may be accompanied by drowsiness or dizziness. When performing tasks that require increased attention, such as driving a car and operating complex machinery, caution should be exercised during migraine attacks and after taking Relpax®.

Overdose

Symptoms: development of arterial hypertension and other cardiovascular disorders.

Treatment: gastric lavage, symptomatic therapy. Since T1/2 of eletriptan is about 4 hours, in case of drug overdose, patients should be observed for at least 20 hours or until clinical symptoms of overdose disappear. The effect of hemodialysis and peritoneal dialysis on plasma concentrations of eletriptan is unknown.

Side effects Relpax 40 mg 2 pcs. film-coated tablets

In general, Relpax® is well tolerated. Typically, side effects are transient, mild or moderate and go away on their own, without additional treatment. The frequency and severity of adverse reactions in patients taking the same dosage twice to relieve an attack are similar to those in patients taking it once. The main side effects recorded during treatment with Relpax® are typical for the entire class of 5-HT1 receptor agonists.

In patients taking Relpax® in therapeutic doses, the following adverse reactions were observed (with an incidence of ≥ 1% or higher compared to placebo). These events were classified into the following categories according to frequency: common - ≥ 1/100 to

Infections: often - pharyngitis and rhinitis; rarely - respiratory tract infections.

From the lymphatic system: rarely - lymphadenopathy.

Eating and metabolic disorders: uncommon - anorexia.

Mental disorders: infrequently - impaired thinking, agitation, confusion, depersonalization, euphoria, depression, insomnia; rarely - emotional lability.

From the nervous system: often - drowsiness, headache, dizziness, tingling sensation or other sensitivity disorders, muscle hypertonicity, hypoesthesia, myasthenia gravis; infrequently - tremor, hyperesthesia, ataxia, hypokinesia, speech impairment, stupor, impaired taste.

On the part of the organ of vision: infrequently - blurred vision, eye pain, photophobia and impaired lacrimation; rarely - conjunctivitis.

From the organs of hearing and balance: often - vertigo; infrequently - ear pain, ringing in the ears.

From the cardiovascular system: often - rapid heartbeat and tachycardia; rarely - angina pectoris, increased blood pressure, bradycardia, shock.

Respiratory, thoracic and mediastinal disorders: often - a feeling of tightness in the throat; infrequently - dyspnea, yawning; rarely - asthma and change in voice timbre.

From the digestive system: often - abdominal pain, nausea, dry mouth and dyspepsia; infrequently - diarrhea, glossitis; rarely - constipation, esophagitis, swelling of the tongue, belching.

From the hepatobiliary system: rarely - hyperbilirubinemia, increased AST activity.

From the skin and subcutaneous tissue: often - increased sweating; uncommon - rash, itching; rarely - skin diseases, urticaria.

From the musculoskeletal system, connective and bone tissues: often - back pain, muscle pain; infrequently - joint pain, arthrosis and bone pain; rarely - arthritis, myopathy, myalgia, convulsions.

From the urinary system: infrequently - disorders of the urinary tract (frequent urination, polyuria).

From the reproductive system and mammary gland: rarely - pain in the mammary glands, menorrhagia.

General disorders: often - a feeling of warmth or hot flashes to the face, chills, asthenia, chest symptoms (pain, feeling of constriction, pressure); infrequently - general weakness, swelling of the face, thirst, peripheral edema.

The following adverse effects have been reported in post-marketing studies.

From the immune system: allergic reactions.

From the nervous system: rare cases of fainting.

From the vascular system: arterial hypertension.

From the digestive system: like some other 5-HT1B/1D agonists, rare reports of ischemic colitis and vomiting have been received.

Drug interactions

Effect of other drugs on the pharmacokinetics of eletriptan

With the simultaneous administration of erythromycin (1000 mg) and ketoconazole (400 mg), which are powerful specific inhibitors of the CYP3A4 isoenzyme, the Cmax of eletriptan increased by 2 and 2.7 times, respectively, and the AUC of eletriptan increased by 3.6 and 5.9 times, respectively. At the same time, T1/2 of eletriptan increased from 4.6 to 7.1 hours when using erythromycin and from 4.8 to 8.3 hours when using ketoconazole. Thus, Relpax® should not be used in combination with strong inhibitors of the CYP3A4 isoenzyme, in particular ketoconazole, itraconazole, erythromycin, clarithromycin, josamycin and protease inhibitors (ritonavir, indinavir and nelfinavir).

The interaction of the drug Relpax® with β-blockers, tricyclic antidepressants, SSRIs and flunarizine has not been identified, however, the results of special clinical studies of drug-drug interactions are not yet available (with the exception of propranolol).

Population pharmacokinetic analysis of clinical studies showed that the following drugs are unlikely to affect the pharmacokinetics of eletriptan: β-blockers, tricyclic antidepressants, SSRIs, estrogen-containing hormone replacement drugs, estrogen-containing oral contraceptives, and CCBs.

Since eletriptan is not a MAO substrate, pharmacokinetic interaction between Relpax® and MAO inhibitors is unlikely, and specific interaction studies have not been conducted.

With simultaneous use of propranolol at a dose of 160 mg, verapamil at a dose of 480 mg, or fluconazole at a dose of 100 mg, Cmax of eletriptan increased by 1.1, 2.2 and 1.4 times, and AUC by 1.3, 2.7 and 2 times respectively. These changes are not clinically significant, because they are not accompanied by an increase in blood pressure or an increase in the frequency of adverse events compared with the use of eletriptan alone.

Taking caffeine/ergotamine orally 1 and 2 hours after taking Relpax® leads to a small but additive increase in blood pressure, which could be predicted based on the pharmacological properties of these drugs. In this regard, drugs containing ergotamine or ergotamine-like drugs, in particular dihydroergotamine, should not be prescribed within 24 hours after taking Relpax®. Relpax® can be prescribed no earlier than 24 hours after taking ergotamine-containing drugs.

Effect of eletriptan on other drugs

At therapeutic doses, no effect (inhibition or induction) of the drug on the cytochrome P450 system was detected.

Interaction with serotonergic drugs

Simultaneous use of 5-HT receptor agonists, incl. eletriptan, with drugs that have serotonergic activity, such as SSRIs and SNRIs, may increase the risk of developing serotonin syndrome. If there is a clinical need for the simultaneous use of eletriptan and serotonergic drugs, caution should be used. Such patients should be monitored carefully, especially during initiation of treatment and as the dose of each drug is increased.

Instructions for use of Relpax (Method and dosage)

Instructions for use of Relpax include oral administration of the drug. In this case, the tablets should be taken with liquid.

If the patient is just beginning to develop migraine headaches, it is necessary to take the tablets as early as possible. But the pronounced effectiveness of its action is also noted when taken during a developed migraine attack.

Adult patients aged 18 to 65 years are recommended to take an initial dose of 40 mg.

If the headache returns during the day, you can re-take the drug in a similar dose. If there is a need to take the tablets again, this can be done no earlier than 2 hours after taking the first tablet.

If after taking the first dose of Relpax the headache does not decrease within 2 hours, then the second dose of the drug should not be taken.

But if the attack cannot be stopped, then an effective clinical response may appear during the next migraine attack. If a dose of 40 mg does not achieve the desired effect, you can take Relpax at a dose of 80 mg at the next attack.

The total daily dose of the drug should not exceed 160 mg.

People with mild or moderate liver dysfunction do not need dosage adjustments.

Special instructions for the use of Eletriptan

Eletriptan is not intended for the prevention of migraine attacks or for the treatment of hemiplegic or basilar migraine. The safety and effectiveness of eletriptan in the treatment of cluster (cluster, serial) headaches, which are characteristic mainly in elderly men, have not been established. Eletriptan should not be prescribed to patients with severe liver failure, since the metabolism of drugs in them has not been studied. No dose adjustment is required in people with mild or moderate hepatic impairment. There have been no adequate and well-controlled studies in pregnant women, so the use of eletriptan during pregnancy is only possible if the expected benefit to the mother outweighs the potential risk to the fetus. Eletriptan is excreted in breast milk. In 8 women receiving a single dose of 80 mg, the average eletriptan concentration in breast milk after 24 hours was approximately 0.02% of the dose taken. The ratio between the average concentration of eletriptan in breast milk and in blood plasma is 1:4, but is highly variable. Eletriptan should be administered to breastfeeding women with caution.

Overdose

In case of overdose, the patient may develop arterial hypertension, as well as other dysfunctions of the cardiovascular system. It is necessary to immediately perform gastric lavage and symptomatic treatment.

Since the half-life of the active substance is approximately 4 hours, in case of overdose, the patient must be observed for at least 20 hours until all symptoms disappear.

There is no data on the effect of peritoneal dialysis and hemodialysis on the blood concentration of eletriptan.

Eletriptan overdose, symptoms and treatment

Volunteers receiving eletriptan at a dose of 120 mg once did not experience clinically significant side effects. In phase 3 clinical trials, the daily dose reached 160 mg. In case of overdose, hypertension (arterial hypertension) and other symptoms of the cardiovascular system may occur. Treatment: The half-life of eletriptan is approximately 4 hours, so patients following an eletriptan overdose should be monitored for at least approximately 20 hours or longer while symptoms and signs of overdose persist. There is no specific antidote. In case of severe intoxication, monitoring of vital signs, mechanical ventilation to ensure adequate oxygenation, and supportive care are indicated.

List of pharmacies where you can buy Eletriptan:

Moscow
Saint Petersburg

Interaction

The pharmacokinetics of eletriptan may be affected by concomitant use of other drugs. If Erythromycin and Ketoconazole , the Cmax of eletriptan increased by 2 and 2.7 times, respectively. The half-life of eletriptan was also increased.

Therefore, Relpax is not prescribed simultaneously with the drugs Itraconazole, Ketoconazole, Clarithromycin, Erythromycin, Josamycin , as well as protease inhibitors.

There was no interaction between Relpax and tricyclic antidepressants, β-blockers, SSRIs and flunarizine .

Erapamil or Luconazole are taken simultaneously of eletriptan increases. However, such changes have no clinical significance.

ergotamine is taken 1-2 hours after taking Relpax , this leads to a small but additive increase in blood pressure . Therefore, products containing ergotamine or ergotamine-like drugs should not be prescribed within 24 hours after taking Relpax. Similarly, Relpax can only be taken 24 hours after taking such medications.

When taking eletriptan concomitantly with drugs that demonstrate serotonergic activity, the risk of developing serotonin syndrome increases. With this combination, patients should be closely monitored.

Contraindications to the use of Eletriptan

Hypersensitivity to eletriptan, coronary artery disease (angina pectoris, history of myocardial infarction, asymptomatic ischemia, documented); cerebrovascular syndrome, including stroke of any type, as well as transient cerebrovascular accidents; peripheral vascular diseases, including abdominal ischemia; uncontrolled hypertension (arterial hypertension); a period within 24 hours after taking other 5-HT1 receptor agonists, ergotamine-containing or ergotamine-like drugs; severe liver failure.

special instructions

It is advisable to use Relpax only if the diagnosis of migraine is definitely confirmed. This drug is not prescribed for the treatment of atypical headaches that develop as a result of serious illnesses.

This remedy should not be prescribed until a thorough examination of the patient, who may have vascular and heart disease, has been carried out and a diagnosis has been established.

The effectiveness of Relpax tablets is noted both in the treatment of migraine with aura, and in the treatment of migraine without aura and migraine, which manifests itself in relation to the menstrual cycle. If the tablets are used when an aura appears, it does not prevent the development of headaches. Tablets should be taken at the onset of headache development.

Relpax also relieves other symptoms that occur with migraine: nausea , vomiting , phonophobia , photophobia .

Prophylactic use of the drug is not allowed.

When using the drug in a dose of 60 mg or more, a slight increase in blood pressure may be observed. This phenomenon is more often observed in older people and in patients with impaired renal function.

Many people experience dizziness and drowsiness , so during attacks of the disease you should carefully perform those actions that require increased attention.

Relpax®

With the simultaneous use of eletriptan and SSRIs (for example, fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram) and SNRIs (for example, venlafaxine, duloxetine), the development of potentially life-threatening serotonin syndrome is possible (see sections “With caution” and “Interaction with other drugs”). means). This syndrome may present with the following symptoms: mental status disturbance (eg, agitation, hallucinations, coma), autonomic nervous system instability (eg, tachycardia, blood pressure fluctuations, hyperthermia), neuromuscular dysfunction (eg, hyperreflexia, incoordination), and/ or symptoms of digestive system dysfunction (eg, nausea, vomiting, diarrhea).

The sensitivity of methods for assessing the state of the cardiovascular system is quite low. In this regard, if the patient’s history, ECG or other diagnostic procedures revealed signs characteristic of arterial vasospasm or myocardial ischemia, the use of eletriptan is not recommended (see section “Contraindications”).

Relpax® should not be taken prophylactically.

It should be borne in mind that unlimited use of antimigraine drugs can lead to chronic daily headaches. Cases of overuse of any triptans most often occur in patients with daily headaches.

Relpax's analogs

Level 4 ATC code matches:
Zolmitriptan

Rapidmed

Imigran

Zomig

Sumamigren

Amigrenin

Sumatriptan

Analogues of Relpax are the drugs Imigran , Caffetamine , Zomig , Amigrenin , Sumatriptan , which have a similar effect on the body.

Some of these medications cost about the same as Relpax. However, there are medicines whose price significantly exceeds its cost.

During pregnancy and lactation

There is no clinical experience with the use of Relpax during pregnancy . No teratogenic effects were observed in animal studies. Therefore, prescribing the drug is advisable only if the expected benefit significantly exceeds the level of risk to the fetus. Passes into breast milk.

If you take a dose of 80 mg once, then over 24 hours the excretion was 0.02% of the total dose. The risk of the drug affecting the baby can be minimized by stopping natural feeding for 24 hours after taking eletriptan.

Reviews of Relpax

Reviews of Relpax indicate that the drug is very effective against migraines. The reviews say that after taking the pill, the symptoms of migraine attacks completely disappeared in patients. The intensity of symptoms decreases approximately 30 minutes after taking the tablet.

Side effects may include drowsiness, tremor, nausea, and other side effects. Reviews note that it is advisable to sleep after taking the pills to minimize the risk of developing side effects. However, some migraine sufferers report that Relpax is not effective for them.

Relpax price, where to buy

The price of migraine tablets Relpax 40 mg averages from 430 to 540 rubles per pack of 2 tablets.

The price of eletriptan (Relpax) in Ukraine is 350 hryvnia.

Online pharmacies in RussiaRussia

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