Relpax, 40 mg, film-coated tablets, 2 pcs.

Relpax is a medicine intended for the immediate relief of migraine attacks of varying severity.

The composition of this drug includes : the main substance - eletriptan hydrobromide and auxiliary components: lactose monohydrate, microcrystalline cellulose, magnesium stearate, croscarmellose sodium.

Shell composition: orange opadry (lactose monohydrate, hypromellose, triacetin, titanium dioxide, dye); transparent opadry (triacetin, hypromellose).

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”.

General information about the drug

The drug is used in the treatment of neurological diseases, in particular the treatment of migraine both without aura and its classic manifestation. Relpax belongs to the group of anti-migraine drugs. The international nonproprietary name is eletriptan.

Release form, prices

Relpax is produced by the Italian pharmacological company Pfaizer in the form of gelatin-coated tablets in a dosage of 40 mg. The average price for Relpax is presented in the table. The cost of the medicine in various regions of the Russian Federation ranges from 380 to 450 rubles for 2 tablets.

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

Pharmacodynamics

The active substance of Relpax, eletriptan, is part of the group of selective agonists of neuronal 5-HT1D and serotonin vascular 5-HT1B receptors. The substance is also characterized by high affinity for 5-HT1F serotonin receptors and a moderate effect on the functioning of 5-HT7, 5-HT1E, 5-HT2B and 5-HT1A serotonin receptors.

Eletriptan has a more pronounced selective effect on serotonin receptors located in the carotid arteries than on serotonin receptors located in the femoral and coronary arteries. The antimigraine activity of Relpax may be explained by the ability of its active component to constrict intracranial blood vessels, as well as to be an inhibitor of neurogenic inflammation.

Pharmacokinetics

After oral administration, eletriptan is absorbed quite completely and quickly into the gastrointestinal tract (absorption reaches approximately 81%). Absolute bioavailability when taken orally in patients of both sexes is approximately 50%. The maximum concentration of eletriptan in blood plasma is observed on average 1.5 hours after administration. The pharmacokinetics of the substance when prescribing therapeutic doses in the range of 20–80 mg is characterized by a linear relationship.

The maximum level of eletriptan and the area under the concentration-time curve (AUC) increase by approximately 20-30% when taking the drug after consuming a fatty meal. When taken orally during a migraine attack, AUC is reduced by approximately 30%, and the time to reach maximum plasma concentration is increased to 2.8 hours.

With regular use at a dosage of 20 mg 3 times a day for 5–7 days, the pharmacokinetics of the active substance Relpax remains linear with predictable cumulation. When taken in higher daily doses (40 mg 3 times a day or 80 mg 2 times a day) and a course of treatment of more than 7 days, the accumulation of eletriptan exceeds the expected by ~ 40%.

When administered intravenously, the volume of distribution of eletriptan is 138 liters, which indicates effective distribution in tissues. The substance binds to plasma proteins to a moderate extent (about 85%).

In vitro studies prove that the primary metabolism of eletriptan is due to the action of the cytochrome P450 isoenzyme CYP3A4 in the liver. This is confirmed by an increase in the content of this compound in the blood plasma when combined with erythromycin, which is a powerful selective inhibitor of the CYP3A4 isoenzyme. It was found that the CYP2D6 isoenzyme is also involved in the metabolism of eletriptan, although clinical studies have not revealed the effect of polymorphism of this element on the pharmacokinetics of Relpax.

When taking eletriptan, two main circulating metabolites of this substance are formed, which are primarily responsible for the increase in total radioactivity of the blood plasma after administration of eletriptan containing the labeled carbon isotope C14.

The metabolite formed due to N-oxidation has no pharmacological activity, while the metabolite formed due to N-demethylation has activity comparable to that of eletriptan. The third substance of radioactive plasma has not yet been identified. It is believed to be a mixture of hydroxylated metabolites that are excreted through the kidneys and intestines.

The content of the active N-demethylated metabolite in the blood plasma does not exceed 10–20% of the total concentration of eletriptan in the body, and therefore does not have a significant effect on the therapeutic effect of Relpax.

After intravenous administration, the total clearance of the active substance of the drug is approximately 36 l/h, and the half-life reaches 4 hours. The average renal clearance after oral administration is approximately 3.9 L/h. Non-renal clearance accounts for about 90% of the total clearance, which indicates that eletriptan is excreted from the body in the form of metabolites, mainly in urine and feces.

Clinical-pharmacological studies and pharmacokinetic analysis indicate that the gender of the patient has virtually no effect on the level of eletriptan in the blood plasma.

In patients aged 65–93 years, a slight and statistically non-significant decrease in the clearance of eletriptan by 16% and a statistically significant increase in the half-life (from approximately 4.4 to 5.7 hours) were found compared with these indicators in younger patients. The effect of eletriptan on blood pressure fluctuations in older people may be greater than in younger patients.

In patients with liver dysfunction (stages A and B according to the Child-Pugh classification), a statistically significant increase in AUC (by 34%) and half-life was found, as well as a slight increase in the maximum concentration of eletriptan in the blood (by 18%), but these phenomena are not clinically significant.

In patients with mild (creatinine clearance 61–89 ml/min), moderate (creatinine clearance 31–60 ml/min) or severe (creatinine clearance less than 30 ml/min) renal dysfunction, no changes were detected in the pharmacokinetics of eletriptan or its degree of binding to blood proteins.

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.

Pharmacokinetics

Relpax is a triptan of the latest generation with all the attendant circumstances. It has a high selective ability for neuronal and vascular seratonin receptors. As a result, it received high pharmacokinetics in comparison with the oldest analogues.

The degree of absorption of the drug through the gastrointestinal tract is about 81%. Bioavailability for men and women will be 50%. The half-life of this drug from the body does not exceed 4-5 hours.

The process of drug metabolism by the body occurs in the liver, excretion occurs through the kidneys and gastrointestinal tract.

Read more about triptans in our article.

Specific and effective drugs for the relief of migraine pain triptans - reviews Triptans are drugs based on serotonin agonists that selectively act on certain serotonin (5-hydroxytryptamine) receptors. Dan…

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

Film-coated 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.

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: often - ≥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.

Reviews from doctors and patients

Reviews about Relpax tablets indicate that they are very good for migraines.

Reviews from doctors

Reviews from experienced doctors:

1. Vasiliev K.R., therapist. A drug such as Relpax completely relieves a severe migraine attack. After about half an hour, the pain goes away and the attacks no longer recur. In the package of this drug you will find 2 tablets, but sometimes one half of the tablet may be enough. After taking the medicine, it is best to just rest in complete silence for about an hour. After the headache disappears, you may be drawn to sleep. Relax! But we should not forget about the large number of side effects.
2. Parkhomenko P.R., therapist. The drug is not always predictable. In some cases it acts instantly, in others it does not produce the desired effect at all. It is also difficult to predict side effects. However, it is irreplaceable in the treatment of migraine.

Patient reviews

Patients echo doctors:

1. Margarita, 35 years old. This drug helps well, completely relieves an early attack, but not quickly enough. Sometimes unpleasant feelings arise. After the headache disappears, a slight tingling sensation in the face and tremors are felt. It's best to lie down and sleep right away. Sometimes taking the drug is accompanied by vomiting.
2. Victoria, 41 years old. I have such migraines that sparks just pour out of my eyes! Especially on certain days of the month! That’s why ordinary painkillers don’t help, I need super strong ones, so I take Relpax. It’s the only thing that saves me, it’s an excellent medicine!
3. Edward, 45 years old. After a head injury, very often there are severe migraines, which are even accompanied by nausea and vomiting. So, during one of these attacks, the doctor recommended that I try Relpax. Indeed, headaches subside within 30-40 minutes immediately after using the drug. Now I use it during periods of exacerbation of migraines.

Advice from patients on taking the drug

It is worth noting that:

• It’s better to try first with half of one tablet;
• carefully read the instructions for the drug, there are many restrictions and contraindications;
• very soft effect.

Pros and cons, based on experience and feedback from practical use

Minuses:

• if there is no result from using this drug, then it is better to immediately look for another medicine;
• too many admission restrictions;
• not always stable results;
• Increasing the dosage does not lead to relief.

Pros:

• the effect of the drug is tolerated an order of magnitude easier than the effect of analogues;
• quickly eliminated from the body;
• quickly relieves pain.

The process by which accumulated blood enters the brain is called cerebral hemorrhage - consequences, symptoms and treatment.

Facial nerve paresis in a newborn occurs due to damage to the facial nerve during childbirth. How to avoid this?

About migraine treatment seriously:

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.

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.

Indications

The instructions for use recommend taking the drug "Relpax" for two types of migraine:

1. With aura, when severe pain is accompanied by symptoms such as visual, tactile, motor, olfactory and auditory disturbances.
2. Without an aura, when in addition to headaches the patient is bothered by nausea, vomiting, and increased sensitivity to light and sounds.

In the presence of other forms of the disease, the use of this drug not only does not have a positive effect, but can also lead to a number of complications. Therefore, before using this medicine to eliminate headaches caused by migraine, you need to consult a specialist and undergo a detailed examination. This will help not only prescribe adequate treatment, but also eliminate the immediate risk to the patient’s health.

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.

Drug analogues

Treatment of migraine is a complex process due to the lack of understanding of the pathophysiological mechanisms of pain. The following analogues of Relpax are also used for its therapy:

1. NSAIDs. Taking non-steroidal anti-inflammatory drugs during a migraine attack is one of the basic means of drug therapy. It is assumed that the mechanism of analgesia is carried out by reducing the inflammatory component in the area of ​​​​excitation of the cortex, as well as thinning the blood due to a decrease in platelet aggregation.

   
   Mechanism of action of NSAIDs

   The main drugs in this group that are used in the treatment of this condition are Aspirin and Paracetamol. Another important feature of these drugs is their low price.

2. Calcium channel blockers. The main representative of this group of drugs is Verapamil. The mechanism of its action is associated with blocking the release of calcium from cells and reducing the concentration of sodium in them. Due to hyperpolarization, myocardial vessels dilate, and at the same time the automatism of the heart muscle decreases, which is accompanied by normalization of blood pressure levels, and, as a consequence, a decrease in pain during migraines.

3. 
   Non-selective 5HT1 receptor agonists. A representative of this class is Dihydroergotamine and other ergot-based drugs. The anti-migraine effect is achieved not only by influencing various types of receptors, but also by influencing alpha-adrenergic receptors in the vessels.

   The effect of the latter is manifested by a narrowing of the lumen of cerebral vessels, a decrease in intracranial pressure and a decrease in the neurological symptoms of the disease. However, the use of these medications is contraindicated for people with chronic renal and heart failure due to the peculiarities of the therapeutic effect.

4. Selective agonists of 5HT1 receptors. Sumatriptan is a synthetic analogue of tryptamine. The mechanism of action and therapeutic manifestations are similar to Relpax, but sumatriptan has higher bioavailability. Also convenient are various forms of drug release, for example, in the form of intranasal drops or rectal suppositories, which makes it possible to take the drug even if the patient has nausea or vomiting.

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

LuxPharma* special offer

• Relpax tab.
  40 mg No. 2!!! RUB 3,200 order

ZdravCity

• Relpax tablets p.p.o. 40 mg 2 pcs Pfizer Italy S.r.L./R-Pharm Germany GmbH

  602 rub. order