Relpax

Relpax is a drug with anti-migraine medicinal properties. The active ingredient of the drug, eletriptan, has significant selectivity for serotonin endings located inside the carotid arteries.

The anti-migraine medicinal effect of the drug is associated with the ability of its active substance to constrict intracranial blood vessels, as well as with its intense slowing effect on inflammation of a neurogenic nature.

Indications Relpaxa

It is used to relieve a migraine attack, which may or may not be accompanied by an aura.

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Release form

The component is released in the form of tablets with a volume of 20 or 40 mg.

Pharmacodynamics

Relpax is a selective agonist of serotonin endings of the 5-HT1B form, as well as 5-HT1D, which are located inside the cerebral vessels, and in addition to this on nuclear neurons and receptors of the nervus trigeminus. In addition to disrupting the secretion of algogenic elements from nerve receptors, the drug leads to narrowing of the cranial vessels.

The drug helps to increase the threshold sensitivity of the 3-facet nerve by blocking its nuclei located in the spinal cord. The drug effect develops by reducing the pulsation of the brain vessels and eliminating pain.

Relpax differs from other triptans in that it cannot interact with dopamine, muscarinic, opioid, or α- and β-adrenergic endings.

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Pharmacokinetics

When administered orally, eletriptan is well absorbed within the gastrointestinal tract, with an absorption rate of 81%. Bioavailability values after oral administration are approximately 50%.

The blood Cmax value is reached after 90 minutes from the moment of drug administration. When used after fatty food, this value increases by 20-30%. Eletriptan is synthesized with blood protein by 85%.

The half-life is about 4-5 hours. Metabolic processes occur inside the liver, and excretion occurs through the gastrointestinal tract and kidneys.

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Dosing and administration

The medication must be taken orally, with the tablets washed down with some liquid.

At the initial stage of migraine development, the tablet should be taken as quickly as possible. Although the effect of the drug also develops in the case of use during an already developed migraine attack.

For adults aged 18-65 years, the initial dosage portion size is 40 mg.

If the pain reappears within the next 24 hours, the medication is taken again in the same dosage. If the drug needs to be taken again, it should be taken at least 2 hours after taking the first tablet.

If the migraine does not subside within 2 hours of taking the first dose of Relpax, a second dose should not be taken.

But even if it is not possible to stop the attack, the development of clinical effects may occur during the next migraine attack. If it is impossible to achieve the desired effect by administering a 40 mg dose, during a new attack it is allowed to use 80 mg of the drug.

A maximum of 0.16 g of the drug can be used per day.

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Use Relpaxa during pregnancy

There is no clinical experience of using the drug in pregnant women. No teratogenic effect was detected in animal tests. For this reason, Relpax is only allowed to be used in situations where the probable benefit is more expected than the risks of complications for the fetus.

The drug penetrates into breast milk. With a single administration of 80 mg of the substance, its excretion in the following 24 hours was 0.02% of the entire portion. To reduce the likelihood of the drug's effect on the child, it is necessary not to breastfeed for 24 hours after the administration of eletriptan.

Contraindications

Main contraindications:

• severe sensitivity associated with eletriptan and other drug components;
• use to eliminate migraines of ophthalmoplegic, basilar or hemiplegic nature;
• significant disorders in liver function;
• rare diseases of hereditary origin (glucose-galactose malabsorption, hypolactasia or lactase deficiency);
• administration together with agents that inhibit protease and the CYP3A4 element;
• elevated blood pressure values that cannot be controlled;
• occlusive pathologies affecting peripheral vessels;
• IHD or suspicion of this disease;
• history of cerebral cerebrovascular accident or TIA;
• combination with other drugs that are 5-HT1-agonists.

It should be used with caution in individuals with serotonin intoxication, and also when administered in combination with other medications that have a serotonergic effect.

In doses over 40 mg, use with caution in individuals with renal dysfunction.

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Side effects Relpaxa

Often the medication is tolerated without complications. The side effects that do arise are usually mild, temporary and go away on their own. Possible symptoms of the disorder include:

• pharyngitis or runny nose and infections affecting the respiratory tract;
• anorexia;
• lymphadenopathy;
• mental disorders: problems with thinking, emotional instability, confusion, feelings of euphoria and depression;
• problems with the functioning of the nervous system: drowsiness, myasthenia, hypokinesia, headaches, tremors and dizziness, as well as hypoesthesia or hyperesthesia, speech disorder, myasthenia, ataxia and problems with sensitivity;
• tightness in the throat, dyspnea, asthma, yawning and changes in vocal timbre;
• hyperbilirubinemia;
• visual impairment: visual disturbance, conjunctivitis, photophobia and pain affecting the eyes;
• problems with the cardiovascular system: increased heart rate, tachycardia, bradycardia or angina and increased blood pressure;
• disorders of the hearing organs and balance: vertigo, tinnitus or pain;
• Gastrointestinal tract lesions: nausea, constipation, pain affecting the abdominal area, dry mouth, diarrhea, dyspeptic symptoms and belching;
• signs from the epidermis: itching, hyperhidrosis or urticaria;
• musculoskeletal disorders: arthritis, pain affecting joints, bones, back and muscles, myopathy, arthrosis and cramps;
• problems with the urinary tract: increased frequency of urination or polyuria;
• disorders of the reproductive system: pain affecting the mammary glands, or menorrhagia;
• allergy symptoms;
• asthenia, thirst, hot flashes to the skin of the face, peripheral edema, chills, systemic weakness and discomfort in the sternum area.

Overdose

In case of intoxication, blood pressure may increase, and in addition, other disorders in the functioning of the cardiovascular system may appear.

Gastric lavage and symptomatic measures must be performed immediately.

Since the half-life of the active ingredient is about 4 hours, in case of poisoning the patient must be monitored for at least 20 hours until all signs of the disorder disappear.

There is no information regarding the efficacy of haemodialysis with peritoneal dialysis on blood levels of eletriptan.

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Interactions with other drugs

The pharmacokinetic characteristics of eletriptan may change when combined with certain medications. Combination with ketoconazole or erythromycin leads to an increase in the Cmax level of the substance by 2.7 and 2 times. The half-life of eletriptan is also prolonged.

For this reason, Relpax is not used together with ketoconazole, josamycin, itraconazole, and also with erythromycin, clarithromycin and agents that inhibit the action of protease.

When the drug is used in combination with verapamil, propranolol or fluconazole, the Cmax level of eletriptan increases. However, such changes do not affect the clinical picture.

When ergotamine or caffeine are administered 1-2 hours after the use of Relpax, there is a slight but additive increase in blood pressure. Because of this, drugs containing ergotamine or ergotamine-like medications are prohibited from being administered within 24 hours of using Relpax. It also cannot be taken within 24 hours of using these drugs.

The administration of eletriptan in combination with substances that have serotonergic properties increases the likelihood of developing serotonin intoxication. In the case of simultaneous use of such agents, the patient's condition must be closely monitored.

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Storage conditions

Relpax should be stored in a place closed to small children. The temperature level can be a maximum of 30°C.

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Shelf life

Relpax can be used for a period of 36 months from the date of sale of the drug.

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Application for children

It is prohibited to use the medication in pediatrics (under 18 years of age), because there is no reliable data regarding its safety in this category of patients.

Analogues

The analogs of the drug are Imigran, Amigrenin with Kofetamin and Sumatriptan with Zomig.

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Reviews

Relpax is considered a very effective remedy for the development of migraine attacks - this is stated in many patient reviews. It is claimed that after taking the pill, the signs of migraine completely disappear - a weakening of their intensity is noted after about half an hour.

The disadvantages include the development of side effects, including nausea, tremors, drowsiness, etc. There are also people who did not benefit from the drug at all, but they are a minority.

In the comments, many advise sleeping after taking the medication - this will minimize the likelihood of side effects.