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Active component eletriptan is a part of tablets of Relpaks (in the form of hydrobromide).
And also additional components: lactoses monohydrate, MKTs, magnesium stearate, croscarmellose sodium.
Means in the form of tablets on 20 and 40 mg which are packed into the blisters from a foil placed in cardboard packs is issued.
- Tablets, 20 mg of orange color, biconvex, round form. They are covered by a film cover, on the one hand tablets are an engraving of "REP 20", with another — "Pfizer".
- Tablets, 40 mg of orange color, biconvex, round form. They are covered by a film cover, on the one hand tablets are an engraving of "REP 40", with another — "Pfizer".
Relpaks – drug with protivomigrenozny action. Active ingredient eletriptan shows the expressed selectivity relatively to serotoninovy receptors which are located in carotid arteries.
Protivomigrenozny activity of means is connected with ability of an eletriptan to narrow blood vessels in a skull and with its inhibiting influence in relation to a neurogenic inflammation.
Pharmacokinetics and pharmacodynamics
After reception orally eletriptan it is actively absorbed in a digestive tract, absorption happens for 81%. Bioavailability level at internal reception — about 50%.
The highest concentration in blood is noted in 1,5 h after internal reception. The maximum concentration of active agent increased by 20–30% if medicine was taken after fat food. eletriptan contacts blood proteins for 85%.
The elimination half-life is equal to about 4-5 hours. The metabolism occurs in a liver then removal happens through kidneys and a gastrointestinal tract.
Indications to use
It is applied for the purpose of stopping of attacks of migraine with manifestation of aura or without it.
The following contraindications for administration of drug of Relpaks are defined:
- high sensitivity of the patient to an eletriptan and other components of means;
- reception for the purpose of stopping of basilar, ophthalmoplegic, hemiplegic migraine;
- serious violations of function of a liver;
- rare diseases of hereditary character (glyukozo-lactose malabsorption, lactase shortage, lactose intolerance);
- reception along with CYP3A4 inhibitors and inhibitors of protease;
- arterial hypertension with an uncontrollable current;
- age till 18 flyings;
- occlusal diseases of peripheral vessels;
- coronary heart disease or suspicion on existence of this disease;
- tranzitorny ischemic attack and disturbances of blood circulation in a brain in the anamnesis;
- simultaneous treatment by other drugs — agonists of 5-HT1-receptors.
Carefully means is appointed the patient with a serotoninovy syndrome. It is also necessary to be careful, applying Relpaks along with other means with serotonergic activity.
It is necessary to be careful at drug intake in a dose more than 40 mg to people at whom disturbance of functions of kidneys is noted.
In most cases Relpaks patients transfer well. As a rule, by-effects are expressed poorly, they disappear independently and are passing.
Perhaps manifestations of the following side effects in the course of reception of means:
- rhinitis, pharyngitis, respiratory infections;
- mental disturbances: confusion of consciousness, disturbance of thinking, depression, euphoria, emotional lability;
- disturbances in work of a nervous system: headaches, drowsiness, dizziness, hypesthesia, hypokinesia, sensitivity disturbances, myasthenia, hyperesthesia, tremor, ataxy, disturbance of the speech;
- feeling of constraint in a throat, yawning, dispnoe, change of a timbre of a voice, asthma;
- functions of organs of sight: eye pain, vision disorder, photophobia, conjunctivitis;
- functions of heart and vessels: tachycardia, tachycardia, stenocardia, bradycardia, increase in indicators of the ABP;
- acoustic organs, balance: ring and ear pain, vertigo;
- gastrointestinal tract function: abdominal pains, nausea, feeling of dryness in a mouth, the dispepsichesky phenomena, diarrhea, a lock, an eructation;
- integuments: strong sweating, itch, small tortoiseshell;
- musculoskeletal system: dorsodynia, joints and muscles, arthritis, ostealgia, arthrosis myopathy, spasms;
- urinary system: polyuria, frequent urination;
- reproductive system: menorrhagia, mammary gland pains;
- allergic reactions;
- feeling of inflow of heat to the person, adynamy, fever, discomfort in a thorax, the general weakness, feeling of thirst, peripheral hypostases.
Application instruction of Relpaks (Way and dosage)
The application instruction of Relpaks provides the drug use inside. At the same time tablets need to be washed down with liquid.
If at the patient the migrenozny headache only begins to develop, it is necessary to take a pill as soon as possible. But the expressed efficiency of its action is noted also at reception at the developed migraine attack.
Aged from 18 till 65 flyings it is recommended to adult patients to accept an initial dose of 40 mg.
When resuming a headache for days it is possible to accept repeatedly means in a similar dose. If there is a need to take a pill repeatedly, then it can be done not earlier than 2 hours later after reception of the first tablet.
If after reception of the first dose of drug of Relpaks the headache within 2 hours does not decrease, then the second dose of drug should not be accepted.
But if it was not succeeded to stop an attack, then the effective clinical answer can be shown at the following attack of migraine. If the dose of 40 mg does not allow to gain desirable effect, at the following attack it is possible to accept Relpaks in a dose of 80 mg.
The general daily dose of means should not be more than 160 mg.
The people suffering from easy or moderate abnormal liver functions do not need to adjust a dose.
At overdose at the patient arterial hypertension, and also other disturbances of functions of cardiovascular system can develop. It is necessary to carry out a gastric lavage, a symptomatic treatment at once.
As the elimination half-life of active agent is equal to about 4 hours, at overdose it is necessary to observe the patient not less than 20 hours until all symptoms disappear.
There are no data on influence of a peritoneal dialysis and hemodialysis and on concentration in blood of an eletriptan.
Simultaneous use of other drugs can influence pharmacokinetics of an eletriptan. If Erythromycin and Ketokonazol is at the same time appointed, Cmax of an eletriptan increased in 2 and 2,7 times respectively. The elimination half-life of an eletriptan also increased.
Therefore Relpaks is not appointed along with drugs Itrakonazol, Ketokonazol, Klaritromitsin, Erythromycin, Dzhozamitsin, and also with protease inhibitors.
Interaction of means of Relpaks and tricyclic antidepressants, β-adrenoblockers, SIOZS and a flunarizina is not revealed.
If after reception of Relpaks in 1-2 hours caffeine or ergotamine is accepted, then it leads to small, but the additive increase of arterial pressure. Therefore it is impossible to appoint means as a part of which there is an ergotamine or ergotaminpodobny means for 24 hours after medicine of Relpaks. Similar to Relpaks it is possible to accept only in 24 hours after reception of such drugs.
At a concomitant use of an eletriptan with drugs which show serotonergic activity the risk of manifestation of a serotoninovy syndrome increases. At such combination for patients it is necessary to conduct careful supervision.
Terms of sale
It is implemented in drugstores according to the recipe
It is necessary to protect Relpaks from children and to store at a temperature which is not exceeding 30 °C.
Period of validity
It is possible to store 3 years.
Relpaks it is reasonable to apply only if the diagnosis migraine is precisely confirmed. For treatment of atypical headaches which develop owing to serious diseases this drug is not appointed.
It is not necessary to appoint this means before carrying out careful inspection of the patient at which existence of diseases of vessels and heart, and establishment of the diagnosis is possible.
Efficiency of tablets of Relpaks is noted both at therapy of migraine with aura, and in the course of treatment of migraine without aura and migraine which is shown relatively to a menstrual cycle. If to apply tablets at manifestation of aura, he does not warn to development of headaches. A pill needs to be taken in a phase of the beginning of development of a headache.
Relpaks also stops other symptoms which are noted at migraine: nausea, vomiting, phonophobia, photophobia.
Preventive reception of means is not allowed.
At the use of means in a dose of 60 mg and more small increase of the ABP can be noted. This phenomenon is more often it is noted at elderly people and at patients with an impaired renal function.
At many people at migraine dizziness and drowsiness therefore during attacks of an illness it is necessary to perform carefully those operations which require special attention is noted.
Cost of some of these drugs approximately same, as well as price of drug of Relpaks. However there are drugs which price considerably exceeds its cost.
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Drugstore of IFC
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