Релпакс

Релпакс – protivomigrenozny medicine.

Form of release and structure

Dosage form – tablets, film coated: orange color, a round biconvex form, on one party the engraving of "Pfizer", is applied on another – "REP 20" or "REP 40" (on 20 mg or 40 mg: on 2, 3, 4, 6 or 10 pieces in the blister, in a cardboard pack of 1, 2, 3, 4, 5, 6 or 10 blisters).

Active ingredient of Relpaks – элетриптан (in the form of hydrobromide), in 1 tablet – 20 mg or 40 mg.

Auxiliary components: croscarmellose sodium, magnesium stearate, lactoses monohydrate, cellulose microcrystallic.      

Structure of a film cover: Opadry orange OY-LS-23016 – lactoses monohydrate, a gipromelloz, triacetin, dye a sunset yellow with a varnish aluminum (E110), titanium dioxide (E171); Opadry transparent YS-2-19114-A – triacetin, a gipromelloz.

Indications to use

Relpaks's use is shown for stopping of attacks of migraine without aura and with aura.

Contraindications

• Uncontrollable arterial hypertension;
• Suspicion of the coronary heart disease (CHD) or its existence: the postponed myocardial infarction, the stenocardia, asymptomatic ischemia of a myocardium (confirmed), Printsmetal's stenocardia;
• Disturbance of cerebral circulation or the instruction in the anamnesis on the tranzitorny ischemic attack;
• Occlusal pathologies of peripheral vessels;
• The expressed abnormal liver functions;
• Stopping of ophthalmoplegic, basilar or hemiplegic migraine;
• Simultaneous use of other agonists of serotoninovy _{5-HT1-receptors};
• Simultaneous use of erythromycin, ketokonazol, itrakonazol, klaritromitsin, dzhozamitsin (CYP3A4 inhibitors) and/or ritonavira, nelfinavira, indinavira (protease inhibitors);
• Age up to 18 years;
• Deficit of lactase, lactose intolerance, syndrome of glyukozo-galaktozny malabsorption;
• Hypersensitivity to drug components.

Besides, use of ergotamine and its derivatives (including метисергид) within 24 hours to or after Relpaks's reception is contraindicated.

With care it is necessary to appoint drug sick at the accompanying therapy selective serotonin reuptake inhibitors and selective serotonin reuptake inhibitors and noradrenaline (because of risk of development of a serotoninovy syndrome against the background of a concomitant use of an eletriptan and other serotonergic drugs), and also in a dose it is higher than 40 mg at a renal failure.

Route of administration and dosage

Pill is taken inside, without chewing, washing down with enough water.

Relpaks's reception needs to be begun at emergence of the first symptoms of migraine though it is effective at all stages of an attack of disease.

The recommended initial dose for patients aged from 18 up to 65 years – 40 mg.

If the headache ceased, but within 24 hours after administration of drug renews, then for its stopping repeated reception of 40 mg, but not earlier than in 2 hours after the first tablet is shown.

Patients at whom reception of an initial dose did not give clinical effect within the first two hours are not recommended to accept the second dose for stopping of this attack.

In case of lack of adequate effect of a dose of 40 mg when stopping the following attack of migraine it is possible to accept 80 mg of drug as an initial dose.

The maximum daily dose – 160 mg.

At easy or moderate degree of an abnormal liver function dose adjustment is not required.

Side effects

The undesirable effects of Relpaks registered in clinical trials:

• Cardiovascular system: often – tachycardia, tachycardia; seldom – increase in the arterial pressure (AP), stenocardia, bradycardia, shock;
• Mental disturbances: infrequently – confusion of consciousness, sleeplessness, disturbance of thinking, depersonalization, agitation, euphoria, a depression; seldom – emotional lability;
• Nervous system: often – a headache, drowsiness, dizziness, a myasthenia, sensitivity disturbances (feeling of a pricking), a hyper tone of muscles, a hypesthesia; infrequently – disturbance of the speech, a hyperesthesia, an ataxy, a tremor, disturbance of flavoring feelings, a hypokinesia, a struporous state;
• Organs of equilibrium and hearing: often – вертиго; infrequently – a ring and/or ear pain;
• Lymphatic system: seldom – a lymphadenopathy;
• Organ of sight: infrequently – eye pain, a vision disorder, disturbance of a slezootdeleniye, a photophobia; seldom – conjunctivitis;
• Metabolism: infrequently – anorexia;
• Gepatobiliarny system: seldom – increase in activity of aspartate aminotransferase, a hyperbilirubinemia;
• Alimentary system: often – dryness in a mouth, nausea, dyspepsia, an abdominal pain; infrequently – a glossitis, diarrhea; seldom – a paraglossa, a lock, an eructation, an esophagitis;
• Dermatological reactions: often – the increased sweating; infrequently – a skin itch, rash; seldom – urticaria, skin pathologies;
• Urinary system: infrequently – the speeded-up urination, a polyuria;
• Musculoskeletal system: often – a dorsodynia and/or muscles; infrequently – arthrosis, a joint pain, an ostealgia; seldom – a myopathy, arthritis, spasms, a mialgiya;
• Reproductive system and mammary glands: seldom – a menorrhagia, mammary gland pain;
• Mediastinal, respiratory, thoracic disturbances: often – feeling of constraint in a throat; infrequently – yawning, диспноэ; seldom – change of a timbre of a voice, asthma;
• Infections: often – rhinitis, pharyngitis; seldom – respiratory infections;
• General disturbances: often – inflows of heat to the person, a caumesthesia, a fever, pain or feeling of compression and/or pressure in a thorax, an adynamy; infrequently – thirst, the general weakness, peripheral hypostases, puffiness of the person.

Besides, the side effects established during the post-market researches:

• Cardiovascular system: arterial hypertension;
• Immune system: allergic reactions;
• Alimentary system: seldom – ischemic colitis, vomiting;
• Nervous system: seldom – unconscious states.

Special instructions

Релпакс it is necessary to appoint only for treatment of migraine with the confirmed diagnosis. Drug cannot be accepted at atypical headaches as the narrowing effect of drug on vessels of a brain can be dangerous if pain is connected with a rupture of aneurism, a stroke or other serious pathologies.

Besides, at appointment the doctor has to consider results of preliminary survey of the patient regarding existence or risk of development of cardiovascular diseases.

Pill is recommended to be taken only during a headache phase because administration of drug during emergence of aura, does not interfere with development of a headache.

Clinical trials confirmed therapeutic action of Relpaks on stopping of the symptoms (photophobia, nausea, vomiting, phonophobia) accompanying migraine and treatment of the headache which is returned during an attack.

Drug is not intended for use as prevention.

The patient, especially at advanced age or with an impaired renal function, it is necessary to consider that the dose of 60 mg can cause passing, slight increase of the ABP also above.

Because of possible emergence of drowsiness or dizziness against the background of administration of drug or the disease, patients are recommended to be careful at control of vehicles and mechanisms both in the period of a migraine attack, and after direct use of Relpaks.

Medicinal interaction

It is not established clinically significant interaction of Relpaks with tricyclic antidepressants, beta adrenoblockers, the selective serotonin reuptake inhibitors (SSRI), flunariziny.

Researches confirmed lack of influence on pharmacokinetics of an eletriptan of beta adrenoblockers, SIOZS, tricyclic antidepressants, estrogensoderzhashchy hormonal replaceable medicines, blockers of calcium channels, oral estrogensoderzhashchy contraceptives.

At simultaneous use with monoamine oxidase inhibitors (MAO) pharmacokinetic interaction is improbable as элетриптан MAO substrate is not.

Intake of caffeine in 1 hour or ergotamine in 2 hours after Relpaks's reception brings to the additive, though insignificant, to increase in the ABP. Therefore it is necessary to observe an interval at 24 o'clock between use of an eletriptan and ergotaminsoderzhashchy or ergotaminpodobny means, including dihydroergotamine.

Influence of therapeutic doses of drug on system _{of P450 cytochrome} is not established.

The combination to serotonergic means increases risk of development of a serotoninovy syndrome.

Terms and storage conditions

To store at a temperature up to 30 °C. To protect from children.

Period of validity – 3 years.