Migraine, although it does not pose a threat to the life of a person suffering from it, but at the same time significantly reduces the quality of its life. For many years, the pharmaceutical industry has worked to create drugs that can eliminate not only the painful symptoms of this disease, but also affect the processes that cause migraines. After all, stopping pain with strong painkillers is possible. But other symptoms of migraine, such as nausea, photosensitivity and intolerance to sounds, can be difficult to eliminate. The drug from migraine Relpaks in this regard, experts consider one of the most effective. What is this medicine? How to take it and what analogues do it have? You can read about all this further.
The composition of the drug, description
The main active ingredient of the Relpaks preparation - eletriptan in the form of hydrobromide is contained in tablets in an amount of 20 mg. There is also a dosage of 40 mg. Excipients are widely used in the pharmaceutical industry lactose monohydrate, magnesium stearate, croscarmellose sodium and MCC. These compounds do not affect the ability of the drug to be absorbed, and also do not affect the body as a whole. Relpax migraine pills are coated with an orange film coating that contains titanium dioxide, dyes, lactose monohydrate, hypromellose and triacetin.
Each tablet is made in a rounded biconvex form. On one side is engraving “REP 20” or “REP 40” (depending on the amount of active substance contained in the tablet) and “Pfizer” on the other. One blister contains 2, 3, 4, 6, or 10 tablets, which, in turn, are packed in cardboard boxes of 1, 2, 3, 4, 5, 6, or 10 pieces.
Pharmacokinetics and pharmacodynamics
The medicine "Relpaks" is quickly and well absorbed after ingestion, especially in combination with fatty foods. The absorption of eletriptan averages about 81%, and the so-called bioavailability is 50%. The maximum content of the active substance in blood plasma is observed within an hour and a half after taking the drug.
The main active ingredient of the Relpaks drug has good performance in relation to plasma proteins (about 85%). The primary metabolism of eletriptan occurs in liver cells. In this case, 2 circulating metabolites are formed, one of which (formed by N-oxidation) does not have activity. The second (formed during N-demethylation) has almost the same properties as the starting substance, but its concentration in blood plasma is only 10-20% of the concentration of eletriptan. Due to this, the active metabolite does not have a tangible therapeutic effect.
Relpaks migraine pills, reviews of which are mostly positive, are effective regardless of the patient’s gender. Excretion of the drug metabolites is carried out to a greater extent through the kidneys (about 90%), as well as through the intestines.
Studies have confirmed the lack of addiction to the main active ingredient of the drug, so today there are no restrictions on the duration of treatment of migraine pain with the help of Relpaks.
Regarding the pharmacodynamics of the Relpax preparation, the instructions for use mention the fact that its main active substance, which belongs to the group of selective antagonists of serotonin vascular and neuronal receptors, has an effect on their other species. In this case, selectivity is manifested to a greater extent with respect to receptors localized in the carotid arteries. The antimengrinous activity of eletriptan is determined not only by its ability to narrow blood vessels located inside the cranium, but also by its positive effect on neurogenic inflammations. In this case, the active substance practically does not affect the receptors of the femoral and coronary arteries.
Indications
The Relpaks drug is recommended for use with two types of migraine:
- With an aura, when symptoms such as visual, tactile, motor, olfactory and auditory disorders are added to severe pain.
- Without an aura, when in addition to the patient's headache, nausea, vomiting, and increased sensitivity to light and sounds are worried.
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 a headache caused by a migraine, you need to contact a specialist and undergo a detailed examination. This will help not only to prescribe adequate treatment, but also to eliminate the immediate risk to the patient’s health.
Contraindications
Consider a list of contraindications for the use of Relpaks. Tablets, as mentioned above, contain eletriptan, which has the ability to systemically affect the body and affects many processes. In which cases the use of the drug is unacceptable or undesirable:
- in the presence of increased sensitivity of the patient to all substances that make up the drug;
- with violations in the liver and kidneys, since metabolism and excretion of the main active substance occurs in them;
- with uncontrolled arterial hypertension;
- with latent or recent heart diseases, including heart attack, angina pectoris, coronary artery disease;
- in the presence of inclusive diseases of the peripheral vessels;
- with a transient or currently existing transient ischemic attack, as well as with any disturbances in cerebral circulation.
The Relpaks drug is categorically not recommended for persons under the age of 18 years. In addition, the drug can not be used to relieve headaches with migraines such as basilar, ophthalmic and hemiplegic.
Use during pregnancy and lactation
The use of Relpax during pregnancy has not been sufficiently studied. However, laboratory studies in animals indicate the effects of eletriptan on the developing fetus. Firstly, a small number of mutated genes (according to the polyploidy principle) were found in embryos. Secondly, the weight of the full-term fetus was significantly lower than in animals that did not receive eletriptan during the gestation period. That is why specialists in his appointment are guided by the rule, which is that the expected benefits for the expectant mother exceed the possible risks to the fetus. It is worth noting that eletriptan, which is part of the drug, is found in breast milk even a day after taking it. Therefore, the use of the drug by nursing mothers is possible only if you refuse to breast-feed for a period of at least 24 hours.
Side effects when using the drug "Relpaks"
Regarding the tolerability of the Relpax drug, reviews of specialists contain information about the low severity of side effects, which independently pass in a relatively short time. It does not matter what dose (20 or 40 mg) the patient took. The most common symptoms observed while taking the drug are:
- inflammatory processes in the nasal cavity and pharynx (pharyngitis and rhinitis);
- disturbances of sensitivity, such as tingling, "goosebumps";
- drowsiness;
- dizziness or headache;
- myasthenia gravis or hypesthesia;
- hypertonicity of muscle fibers;
- pain or constriction in the back and chest;
- heart rhythm disturbance, in particular tachycardia;
- dyspeptic disorders such as pain or discomfort in the abdomen, dry mouth and nausea;
- increased sweating;
- hot flashes of face or chills.
Taking into account the chemical composition of Relpax, experts do not exclude the development of allergic reactions to the components of the drug, which can be expressed in the appearance of a rash, itching or hyperemia. In addition, in rare cases, patients may be disturbed by such phenomena as:
- anorexia;
- lymphadenopathy;
- confusion, euphoria or depression, insomnia or emotional lability;
- photophobia, pain in the eyeball, conjunctivitis, decreased or increased lacrimation;
- violation of taste perception;
- ringing or soreness in the ears;
- increase in blood pressure;
- asthmatic attacks;
- changing the tone of voice;
- swelling in the oral cavity;
- constipation or diarrhea;
- arthritis or arthrosis;
- myalgia or myopathy;
- polyuria or rapid urination;
- menstrual irregularities;
- ischemic colitis.
Given the above side effects, the use of Relpax migraine remedy is recommended to be carried out under the supervision of specialists and only after the necessary studies have been carried out on the subject of existing diseases that may complicate the treatment.
Interaction
Consider the interaction with some drugs anti-migraine Relpaks. A medicine, the instructions for which contain extensive information about its compatibility with other drugs, should not be taken in conjunction with medications of the following groups:
- isoenzyme inhibitors, which include Erythromycin, Ketoconazole, Clarithromycin and Itraconazole;
- protease inhibitors, including Nelfinavir and Indinavir.
Experts also note the fact that the simultaneous use of Relpax with the propanolol and verapamil drugs can not only provoke a significant increase in blood pressure, but also increase the risk of other side effects. An increase in blood pressure can be expected in the case of joint use of the drug with caffeine-containing drugs. That is why experts recommend observing the daily interval between doses of such drugs as Relpaks (analogues also fall under this definition) and ergotamine-like drugs.
It has been clinically proven that the migraine treatment described in this article does not interact with substances related to beta-blockers, estrogen-containing hormone replacement or oral contraceptives, as well as tricyclic antidepressants.
Overdose
If the amount of Relpax drug recommended by the attending physician is exceeded, the instructions for use warn of an overdose that can cause a persistent increase in blood pressure and other disorders of the cardiovascular system. When they occur, symptomatic treatment and, if necessary, gastric lavage is recommended.
Mode of application
Relpax is recommended to be taken by Relpaks with a migraine attack. If a headache and other related ailments bother the patient for several hours, the drug also remains effective. It is worth noting that taking the medicine as a prophylactic for migraine is impractical, as it is proved that in this case it does not have the desired effect. At the same time, with an impending aura (patients suffering from migraine for a long time can determine this condition), taking the drug not only alleviates the pain that follows the aura, but also relieves symptoms such as nausea, drowsiness, and photosensitivity. This does not come immediately, but only after the appearance of headaches. Therefore, patients with migraine should not rush to take a pill every time ailments occur.
The initial dose of the drug for patients 18-65 years old is 40 mg. After stopping a migraine, the pain may resume. In this case, the instruction advises taking the drug again at the same dosage, but not earlier than 2 hours after the first dose. In case of drug failure, when the headache does not subside within 2 hours after the use of the drug, a repeated dose is not recommended. Moreover, specialists indicate that the next migraine attack in the same patient can be stopped with the initial dose of Relpax. Customer reviews on this subject also contain similar information.
The maximum dose of the drug taken during the day should not exceed 160 mg. Drink a tablet should be whole, not chewing, drinking plenty of fluids.
special instructions
The use of Relpax is possible only after confirming the diagnosis of migraine. This is due to the fact that with atypical headaches, which can also be caused by a stroke, rupture of aneurysm and other serious diseases, its use can provoke various complications. In addition, it is undesirable to use this drug to eliminate severe pain during migraines against the background of cardiovascular diseases and disorders in the kidneys and liver, as this can cause an increase in blood pressure to a critical level. The same applies to patients whose risk of developing CVD diseases is high. That is why, before prescribing Relpax, the patient must undergo a full examination. Patients over the age of 65 during the use of the drug should be under the supervision of specialists, since it is they who most often have an increase in blood pressure.
Attention! Regarding the use of the Relpax drug, the instructions for use contain mention of side effects such as dizziness and drowsiness, so special care should be taken when driving cars and when driving complex equipment.
Analogues of the drug "Relpaks", price
Most drugs manufactured by pharmaceutical companies in the West have domestic counterparts. This can also be said in relation to Pfizer, the manufacturer of Relpaks. However, since it was registered relatively recently, to date, there are no drugs that would have the same properties as the Relpaks drug. Analogues of the main active ingredient of eletriptan are also not known, from which we can conclude that the drug is unique. Its cost in Russia is from 380 to 1200 rubles. The exact price depends on how many tablets are in the package and what their dosage is.
According to the method of affecting the vessels of the brain in Relpaks tablets, there are several analogues that not only differ little from it in cost, but also often turn out to be much more expensive. For example, the medicine for migraine "Zomig" can be purchased at a price of about 400 rubles for three tablets. The preparations Imigran and Sumatriptan are also similar to Relpax in terms of the effect and price. The only drug that costs much lower than Relpax tablets is Cofetamine. Their price does not exceed 75 rubles per package.
Reviews about the drug
So, we will pass to the most important question. What do consumers and their attending physicians think about Relpax? What are the pros and cons of this drug? The first thing about 80% of respondents say is that Relpax tablets are highly effective even with a severe migraine attack. According to patients, after taking just one pill, the pain goes away after 30-40 minutes. About 8% of consumers surveyed indicated that after consuming an initial dose of 40 mg, they developed symptoms such as tremor of the extremities and tingling in the face and hands. However, these unpleasant phenomena took place within two hours without any additional action.
Less than 1% of patients who were prescribed Relpax did not feel its effect at all at the first dose. In a third of them, with a second attack, the drug had its effect, and the rest were forced to find a replacement for it.
Experts note among the advantages of the drug its mild effect on the vessels of the head. However, they notice that with the appearance of even the most minor side effects, the patient just needs to sleep. This will be enough to pass all unpleasant phenomena. Experts also note the following: in contrast to similar drugs, which do not contain eletriptan, Relpaks is much easier to tolerate with migraine patients.