Universal reference book for medicines
Product name: RELPAKS В® (RELPAX В® )

Active substance: eletriptan

Type: Serotonin 5-HT 1 -receptor agonist.
The drug with antimigraine activity
Composition, form of production and packaging
The tablets covered with a film cover of
orange color, round, biconcave, with engraving "REP 40" on one side and "Pfizer" on the other.

1 tab.

eletriptan hydrobromide 48.485 mg,

which corresponds to the contents of eletriptan 40 mg

[PRING] microcrystalline cellulose - 93.015 mg, lactose monohydrate - 46 mg, croscarmellose sodium - 10 mg, magnesium stearate - 2.5 mg.

The composition of the film shell: opadray orange OY-LS-23016 (hypromellose, lactose monohydrate, titanium dioxide (E171), triacetin, dye sunset yellow with aluminum lacquer (E110)) - 6 mg, opadray transparent YS-2-19114-A ( hypromellose, triacetin) - 1 mg.

2 pcs.
- PVC / aluminum foil blisters (1) - cardboard packs with control of the first opening.

Description of the drug approved by the manufacturer for the printed edition of 2015.


Anti-migraine drug.
Eletriptan is the representative of the group of selective agonists of serotonin vascular 5-HT 1B - and neuronal 5-HT 1D- receptors. Eletriptan also has a high affinity for serotonin 5-HT 1F receptors and has a moderate effect on serotonin 5-HT 1A , 5-HT 2B , 5-HT 1E and 5-HT 7 -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 narrow the intracranial blood vessels, as well as its inhibitory effect against neurogenic inflammation, can determine its antimigraine activity.


After ingestion, eletriptan is quickly and sufficiently absorbed from the digestive tract (absorption is about 81%).
In men and women, the absolute bioavailability with oral administration is about 50%. T max after ingestion in the blood plasma averaged 1.5 hours. In the therapeutic dose range (20-80 mg), the pharmacokinetics of eletriptan is characterized by linear dependence.
C max eletriptan in blood plasma and AUC increased by about 20-30% when taking the drug after eating fatty foods.
When ingestion during an attack of migraine AUC decreased by about 30%, T max in blood plasma increased to 2.8 h.
With regular use (20 mg 3 times / day) for 5-7 days, the pharmacokinetics of eletriptan remained linear with predictable cumulation.
When administered at higher doses (40 mg 3 times / day and 80 mg 2 times / day) for 7 days, the cumulation of eletriptan exceeded the expected (by about 40%).

V d of eletriptan when administered iv is 138 l, indicating a good distribution in the tissue.
Eletriptan moderately binds to proteins (approximately 85%).

In vitro studies indicate that the primary metabolism of eletriptan occurs under the action of the CYP3A4 isoenzyme in the liver.
This fact is confirmed by an increase in the concentrations of eletriptan in the blood plasma with the simultaneous use of erythromycin, which is a potent selective inhibitor of CYP3A4. In vitro studies also show a slight involvement of CYP2D6 in the metabolism of eletriptan, although clinical studies have not revealed a clinical effect of polymorphism of this enzyme on the pharmacokinetic parameters 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 14C-labeled eletriptan. The metabolite formed as a result of N-oxidation did not have activity in animal experiments in vitro.
The metabolite formed as a result of N-demethylation was comparable in activity to eletriptan in animal studies in vitro. The third component of radioactive plasma is not identified, it is believed that it is a mixture of hydroxylated metabolites, which are also excreted by the kidneys and through the intestine.
The concentration of active N-demethylated metabolite in blood plasma is only 10-20% of the eletriptan concentration and accordingly does not make a significant contribution to its therapeutic effect.


The total clearance of eletriptan from blood plasma after intravenous administration is an average of 36 l / h, and T 1/2 - about 4 hours. The average renal clearance after oral administration is approximately 3.9 l / h.
The percentage of extrarenal clearance is approximately 90% of the total clearance; this indicates that eletriptan is excreted, mainly in the form of metabolites by the kidneys and through the intestine.
Pharmacokinetics in special clinical cases

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

Older people (65-93 years) showed a slight and statistically insignificant decrease (by 16%) of eletriptan clearance and a statistically significant increase in T 1/2(from about 4.4 to 5.7 hours) compared with those in young adults.
The effect of eletriptan on AD in the elderly can be more pronounced compared with patients of a younger age.
In patients with impaired liver function (classes A and B on the Child-Pugh scale), a statistically significant increase in AUC (by 34%) and T 1/2 , as well as a slight increase in C max (by 18%), however, are considered clinically insignificant.

In patients with a lung (KK 61-89 ml / min), moderate (CK 31-60 ml / min) and severe (QC <30 ml / min) renal dysfunction, no statistically significant changes in the pharmacokinetics of eletriptan or its binding to plasma proteins blood.


- arresting migraine attacks with an aura and without an aura.


The drug is prescribed inside.
Tablets should be swallowed whole, washed down with water.
When migraine headache occurs, RelpaxВ® should be taken as soon as possible after the onset of pain, but the drug is also effective at a later stage of a migraine attack.

For adult patients (aged 18-65 years) the recommended initial dose is 40 mg.

If migraine headache is stopped, but then resumed within 24 hours, Relpax В® can be re-administered at the same dose.
If a second dose is needed, it should be taken no earlier than 2 hours after the first dose.
If the first dose of Relpax В® does not lead to a reduction in the headache within 2 hours, then the second dose should not be taken to stop the same attack, tk.
in clinical trials, the effectiveness of such treatment has not been proven. In this case, patients who did not manage to stop the attack, can give an effective clinical response at the next attack.
If taking the drug at a dose of 40 mg does not allow for an adequate effect, then in subsequent migraine attacks, an effective dose of 80 mg can be effective.

The maximum daily dose is 160 mg.

In patients with mild or moderate impairment of liver function, dose adjustment is not required.


In general, Relpax В® is well tolerated.
Usually, the side effects are transient, mild or moderate, and pass on their own without further treatment. The incidence of adverse reactions in patients taking the drug 2 times for 24 hours in the same dose for arresting an attack is similar to that in patients taking the drug once. The main side effects recorded with treatment with Relpax В® are typical for the entire class of serotonin 5-HT 1 -receptor agonists.
With the use of serotonin 5-HT 1 -receptor agonists, incl.
and Relpax В® , reported cases of serious cardiovascular side effects, in some cases fatal. These reactions were extremely rare and were observed mainly in patients with concomitant risk factors.
In patients taking Relpax ® at therapeutic doses, the following adverse reactions were observed (with a frequency of ≥ 1%, compared with placebo).
Determination of the frequency of adverse reactions: often (? 1/100 to <1/10), infrequently (? 1/1000 to 1/100), rarely (? 1/10 000 to 1/1000).
On the part of the respiratory system: often - pharyngitis, rhinitis, a feeling of "restraint" in the throat;
sometimes - dyspnoea, yawning; rarely - respiratory tract infections, bronchial asthma, change in voice timbre.
From the side of the lymphatic system: rarely - lymphadenopathy.

From the metabolism: infrequently - anorexia.

Mental disorders: infrequent - a violation of thinking, agitation, confusion, depersonalization, euphoria, depression, insomnia;
rarely - emotional lability.
From the nervous system: often - drowsiness, headache, dizziness, a feeling of "pricking" or other sensory disorders, hypertonic muscles, hypoesthesia, myasthenia gravis;
infrequently - tremor, hyperesthesia, ataxia, hypokinesia, speech disturbance, stuporous state, violation of taste sensations.
From the senses: often - vertigo;
infrequently - impaired vision, pain in the eyes, photophobia and tearing, tearing in the ears, ringing in the ears; rarely - conjunctivitis.
From the cardiovascular system: often - a feeling of palpitations, tachycardia;
rarely - angina, increased blood pressure, bradycardia, shock.
From the digestive system: often - abdominal pain, nausea, dry mouth, indigestion;
infrequently diarrhea, glossitis; rarely - constipation, esophagitis, tongue edema, belching, hyperbilirubinemia, increased ACT activity.
From the skin and subcutaneous tissue: often - increased sweating;
infrequently - a rash, itchy skin; rarely - skin diseases, hives.
From the musculoskeletal system: often - back pain, muscle pain;
infrequently - pain in the joints, arthrosis and pain in the bones; rarely - arthritis, myopathy, myalgia, convulsions.
From the urinary system: infrequently - frequent urination, polyuria.

From the side of the reproductive system: rarely - pain in the mammary glands, menorrhagia.

Common disorders: often - a feeling of heat or hot flushes to the face, chills, asthenia, symptoms from the chest (pain, compression, pressure);
infrequently - general weakness, puffiness of the face, thirst, peripheral edema.
Side effects reported in post-marketing studies

From the nervous system: rarely - fainting.

From the side of the cardiovascular system: arterial hypertension.

From the side of the digestive system: rarely - ischemic colitis, vomiting.

Allergic reactions: angioedema.


severe hepatic impairment;

uncontrolled arterial hypertension;

- IHD (angina pectoris, Prinzmetal angina, suffered myocardial infarction, confirmed asymptomatic myocardial ischemia) or suspicion of its presence;

- occlusive diseases of peripheral vessels;

- impaired cerebral circulation or transient ischemic attack in the anamnesis;

- for the purpose of arresting hemiplegic, ophthalmoplegic or basilar migraine;

- joint use with other agonists of serotonin 5-HT 1 -receptors;

- simultaneous administration with inhibitors of CYP3A4 (ketoconazole, itraconazole, erythromycin, clarithromycin, josamycin) and protease inhibitors (ritonavir, indinavir and nelfinavir);

- during 24 hours before or after taking Relpax В® , ergotamine or ergotamine derivatives (including metisergide) should not be used;

- children and adolescents under 18 years of age (data on the effectiveness and safety of the drug in this age group are limited);

- rare hereditary diseases - lactose intolerance, lactase deficiency or malabsorption of glucose / galactose;

- Hypersensitivity to the components of the drug.

Be wary of using Relpax В® concomitantly with other drugs that have serotonergic activity, such as selective serotonin reuptake inhibitors and selective serotonin and noradrenaline reuptake inhibitors (as in some cases, the development of serotonin syndrome with the simultaneous administration of eletriptan and other serotonergic drugs) ;
in a dose of more than 40 mg in patients with impaired renal function (because in such patients the influence of eletriptan on blood pressure is increased).

Clinical experience with the use of Relpax В® in pregnancy is absent.
The use of the drug is only possible in cases where the intended benefit of therapy for the mother exceeds the potential risk to the fetus.
Eletriptan is excreted in breast milk in women.
With a single administration of the drug Relpax В® at a dose of 80 mg excretion in breast milk for 24 hours was an average of 0.02% of the dose. The risk of exposure to eletriptan on a newborn can be minimized if you do not breast-feed it within 24 hours after taking Relpax В® .
In experimental animal studies Relpax В® did not have a teratogenic effect.


In patients with a lung (KK 61-89 ml / min), moderate (CK 31-60 ml / min) and severe (QC <30 ml / min) renal dysfunction, no statistically significant changes in the pharmacokinetics of eletriptan or its binding to plasma proteins blood.

In patients with impaired renal function, the hypertensive effect of Relaks is increased, so caution should be given in doses exceeding 40 mg.
When Relpaks was used at doses of 60 mg or more (in the range of therapeutic doses), a small and transient increase in blood pressure was recorded, which increased more in the case of renal dysfunction and in elderly patients (such changes were not accompanied by clinical consequences).

Contraindications: severe liver dysfunction

In patients with impaired liver function (classes A and B on the Child-Pugh scale), a statistically significant increase in AUC (by 34%) and T 1/2 , as well as a slight increase in C max (by 18%), however, are considered clinically insignificant.

In patients with mild or moderate dysfunction of the liver, a dose change is not required.
In patients with severe impairment of liver function, the efficacy and safety of Relpax have not been studied, so in such cases the drug is contraindicated.

Contraindication: children and adolescents under 18 years of age (data on the effectiveness and safety of the drug in this age group are limited).


The use of Relpax В® in combination with potent inhibitors of the isoenzyme CYP3A4 is not recommended, in particular, with ketoconazole, itraconazole, erythromycin, clarithromycin, josamycin and protease inhibitors such as ritonavir, indinavir and nelfinavir.
In addition, Relpax В® should not be taken within 72 hours after the completion of the intake of inhibitors of the isoenzyme CYP3A4.
Like other serotonin 5-HT 1 -receptor agonists, Relpax В® should be used only in those cases when the diagnosis of migraine is undoubted.

Relpax В® , like other serotonin 5-HT 1 -receptor agonists, should not be prescribed for the treatment of "atypical" headaches, which can be associated with serious diseases (stroke, aneurysm rupture), when narrowing of the cerebral vessels may be harmful.

Against the background of the use of serotonin 5-HT 1 -receptor agonists, cases of cerebral hemorrhage, subarachnoid hemorrhage, stroke or other cerebrovascular disorders, in some cases fatal, have been observed.
In several cases, cerebrovascular disease was the main disease and serotonin 5-HT 1 -receptor agonists did not apply correctly, treating symptoms as signs of migraine. It should be noted that patients with migraine may be at increased risk of cerebrovascular complications (for example, stroke, hemorrhage and transient ischemic attack).
With the simultaneous use of eletriptan and SSRIs (eg, fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram) and SSRIs (for example, venlafaxine, duloxetine), potentially life-threatening serotonin syndrome is possible.
This syndrome can be manifested by the following symptoms: violation of mental status (eg, agitation, hallucinations, coma), instability of the autonomic nervous system (eg, tachycardia, fluctuations in blood pressure, hyperthermia), dysfunction of the neuromuscular system (eg, hyperreflexia, impaired coordination) and / or symptoms of dysfunction of the digestive system (eg, nausea, vomiting, diarrhea).
It is not recommended to use Relpax В® in patients with risk factors for the development of IHD (eg, hypertension, hypercholesterolemia, smoking, obesity, diabetes mellitus, family history, women undergoing surgical or physiological menopause or men over the age of 40) a thorough examination of the circulatory system will not be carried out and cardiovascular disease will not be ruled out.

The sensitivity of methods for assessing the state of the cardiovascular system is rather small.
In this regard, if it is not recommended to use eletriptan in a patient's history, ECG or other diagnostic procedures, which are characteristic of arterial vasospasm or myocardial ischemia.
In patients with risk factors for cardiovascular disease, but in which the assessment of the cardiovascular system showed a satisfactory result, it is recommended that the first dose of eletriptan be taken under the supervision of a physician, in addition to patients who previously received eletriptan.
Because myocardial ischemia can occur in the absence of clinical symptoms, it should consider the possibility of ECG immediately after taking the drug Relpax В® .
Patients with risk factors for cardiovascular disease, as described above, receiving eletriptan prolonged, but with interruptions, should undergo periodic examination of the cardiovascular system, as they continue therapy eletriptanom.
Systematic following guidelines set forth above leads to a decrease in the number of cases where patients with unidentified cardiovascular diseases eletriptanom receive therapy.
With agonists of serotonin 5-HT 1 receptor reported cases of severe disorders of cardiac function, including myocardial infarction, of life-threatening cardiac arrhythmias and deaths that have developed in the first few hours after ingestion. Given the breadth of application of the serotonin 5-HT 1receptors in patients with migraine, the incidence of these reactions is very low.
During clinical trials, the following messages were received. Among patients who performed the diagnostic coronary angiography, one patient receiving eletriptan in / (C max of 127 ng / ml, equivalent to 60 mg of eletriptan for ingestion) angina history, hypertension and hypercholesterolemia, a feeling of tightness in thorax and coronary vasoconstriction was identified (confirmed by angiography) without ECG changes typical of ischemia. In addition, it was reported one case of atrial fibrillation in a patient with arrhythmia history.
In the post-marketing period, reported cases of severe cardiovascular complications, some of which are fatal. In very rare cases, these complications occurred in the absence of any signs of cardiovascular disease. Nevertheless, given the difficulty of control messages received in the postmarketing period, it is impossible to definitively determine the relationship between these cases taking eletriptan.
Relpaks В® should not be administered to patients without prior examination, who likely to have cardiovascular disease or at increased risk of their development. Systematic study of eletriptan in patients with heart failure have not been performed. The use of eletriptan, like other agonists of serotonin 5-HT 1receptors, in these patients is not recommended.
Relpaks В® effective in the treatment of migraine with aura and migraine without aura and accompanying menstrual cycle. Relpaks В® , received at the time of the appearance of the aura, it does not prevent the development of a headache, so it should only be taken during the headache phase.
In clinical studies have shown that Relpaks В® is also effective for the relief of symptoms associated with migraine, such as nausea, vomiting, photophobia, phonophobia, and return to treat headache during attack.
Relpaks В® should not be taken preventively.
In applying the drug Relpaks В®therapeutic doses of 60 mg or more recorded small and transient increase in blood pressure.
Blood pressure rises to a greater degree in patients with impaired renal function and the elderly.
Note that unlimited use protivomigrenoznyh drugs can lead to chronic daily headaches. Any cases of excessive use of triptans is most often seen in patients with daily headaches.
Influence on the ability to manage motor vehicles and work with mechanisms

In some cases, migraine itself or reception agonists of serotonin 5-HT 1 receptors, including Relpaks В® , may be accompanied by sleepiness or a giddiness. Patients in the performance of work requiring attention, such as driving vehicles and work with complex mechanisms, caution should be exercised during migraine attacks and after taking the drug Relpaks В® .

Symptoms may develop hypertension or other violations of the cardiovascular system.
Treatment: gastric lavage, symptomatic therapy.
T 1/2 eletriptan is about 4 hours, so in case of an overdose should monitor the status of patients for at least 20 hours or until the disappearance of clinical symptoms overdose. Effect of hemodialysis and peritoneal dialysis, the concentration of eletriptan in unknown plasma.

The effect of other drugs on eletriptan
When concomitant administration of erythromycin (1 g) and ketoconazole (400 mg), which are potent specific inhibitors of isoenzyme CYP3A4, revealed a significant increase in C max (2 and 2.7 times, respectively) and AUC (3.6 and 5.9 times, respectively, ) eletriptan. These effects were accompanied by an increase in T 1/2 eletriptan from 4.6 to 7.1 hours when using erythromycin and from 4.8 to 8.3 hours when using ketoconazole. Therefore Relpaks В® should not be used in combination with potent inhibitors isoenzyme CYP3A4, particularly with ketoconazole, itraconazole, erythromycin, clarithromycin, josamycin and protease inhibitors (ritonavir, indinavir and nelfinavir).
Interaction Relpaks preparation В® with beta-blockers, tricyclic antidepressants, selective serotonin reuptake inhibitors and flunarizine have been identified, but the results of specific clinical studies on the interaction of these drugs currently available (except propranolol).
Population pharmacokinetic analysis of clinical studies have shown that the effect of these drugs on the pharmacokinetics of the drug Relpaks В® unlikely: beta-blockers, tricyclic antidepressants, selective serotonin reuptake inhibitor, estrogenosoderzhaschie preparations for hormone replacement therapy and estrogenosoderzhaschie oral contraceptives, calcium channel blockers.
Eletriptan is not a substrate of MAO. In this regard, no drug interaction is assumed Relpaks В® and MAO inhibitors, special studies of their interactions was conducted.
With simultaneous use of propranolol (160 mg), verapamil (480 mg) and fluconazole (100 mg) C max eletriptan increased respectively 1.1, 2.2 and 1.4 times, and its AUC - 1.3, 2.7 and 2 times. These changes are considered clinically insignificant, because They were not accompanied by increases in blood pressure or increase in frequency of adverse events as compared with that in the application of eletriptan.
Receiving caffeine / ergotamine inwardly after 1 and 2 hours after taking the drug Relpaks В®It leads to a small, but increased blood pressure additive, which could have been predicted based on the pharmacological properties of these preparations. In this connection, preparations containing ergotamine or ergotamine derivatives (including dihydroergotamine) should not be administered within 24 hours after administration of the drug Relpaks В® .
Conversely, Relpaks В® may be administered no sooner than 24 h after administration ergotaminosoderzhaschih preparations.
Effect of eletriptan on other drugs
in therapeutic doses revealed no influence (inhibition or induction) on drug cytochrome P450 system.
Interaction with serotonergic drugs
The simultaneous use of agonists of serotonin 5-HT receptors, including eletriptan, with drugs having serotonergic activity such as selective serotonin reuptake inhibitor and a selective serotonin reuptake inhibitor and a norepinephrine, may increase the risk for serotonin syndrome. In the case of clinical necessity of simultaneous use of eletriptan and serotonergic drugs requires caution. Such patients should be carefully monitored, especially at the beginning of treatment and when increasing the dose of each drug.

The drug is released by prescription.


The drug should be stored out of reach of children at a temperature of no higher than 30 В° C.
Shelf life - 3 years.
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