Relpaks

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

The antimigraine medicinal effect of the drug is associated with the ability of its active ingredient to narrow intracranial blood vessels, as well as its intense inhibitory effect against the neurogenic nature of inflammation.

Indications Relpaksa

It is used to get rid of a migraine attack, which may be accompanied by aura or not.

[1],

Release form

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

Pharmacodynamics

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

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

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

[2],

Pharmacokinetics

When used orally, eletriptan is well absorbed inside the gastrointestinal tract, while the absorption rate is 81%. Bioavailability values after oral administration are approximately 50%.

The blood index Cmax is reached after the expiration of 90 minutes from the moment of using the drug. When consumed after ingestion of fatty foods, this value increases by 20-30%. With blood protein, eletriptan is synthesized by 85%.

The term half-life is about 4-5 hours. Metabolic processes are carried out inside the liver, and excretion develops through the gastrointestinal tract and kidneys.

[3], [4], [5], [6],

Dosing and administration

It is required to apply a medicine orally, washing down tablets with any liquid.

At the initial stage of development of migraine pill should be consumed as quickly as possible. Although the effect of the use of drugs develops in the case of use already with a developed migraine attack.

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

If the pain reappears within the next day, the medication is re-used in the same dosage. With the need to re-use the drug should do this at least after 2 hours from the time of use of the 1st pill.

If the migraine does not weaken within 2 hours from the moment of applying the 1st portion of Relpax, the 2nd dose should not be consumed.

But even if the attack did not stop, the development of clinical influence can occur during the next migraine attack. If it is impossible to achieve the desired effect by the introduction of a portion of 40 mg, during the new attack, the use of 80 mg of the drug is allowed.

During the day, in general, you can use a maximum of 0.16 g of the drug.

[8]

Use Relpaksa during pregnancy

The experience of clinical use of the drug in pregnant women is absent. In tests involving animals, no teratogenic effect was detected. Because of this, use of Relpax is allowed only in situations where the likely benefits are more expected than the risks of complications to the fetus.

The drug penetrates into the mother's milk. With a single injection of 80 mg of the substance, its excretion in the next 24 hours amounted to 0.02% of the entire batch. To reduce the likelihood of drug exposure to the baby, it is necessary not to breastfeed for 24 hours after eletriptan is administered.

Contraindications

The main contraindications:

• strong sensitivity associated with eletriptan and other medication elements;
• use to eliminate migraine, having ophthalmoplegic, basilar or hemiplegic character;
• significant disorders in the liver;
• rare diseases of hereditary nature (glucose-galactose malabsorption, hypolactasia, or lactase deficiency);
• the introduction together with the means of slowing down the protease and the element CYP3A4;
• elevated blood pressure values that cannot be controlled;
• occlusive pathologies affecting peripheral vessels;
• IHD or the presence of suspicion of this disease;
• history of cerebral blood flow disorders or TIA;
• combination with other drugs that are agonists of 5-HT1-terminations.

It is used with caution in individuals with serotonin intoxication, and in addition, when combined with other medications that have serotonergic effects.

In servings of more than 40 mg, caution is used in patients with impaired renal function.

[7]

Side effects Relpaksa

Often the drug is transferred without the appearance of complications. The resulting adverse signs usually have a weak intensity, are temporary and pass on their own. Among the possible symptoms of a disorder:

• pharyngitis or runny nose and infections affecting the respiratory ducts;
• anorexia;
• lymphadenopathy;
• mental disorders: problems with thinking, emotional instability, confusion, feelings of euphoria and depression;
• problems with the work of NA: drowsiness, myasthenia, hypokinesia, headaches, tremor and dizziness, and in addition, hypoesthesia or hyperesthesia, speech disorder, myasthenia, ataxia and problems with sensitivity;
• constriction in the area of the throat, dyspnea, asthma, yawning, and change in voice tone;
• hyperbilirubinemia;
• disorders of visual activity: visual disturbance, conjunctivitis, photophobia and pain affecting the eyes;
• problems with the function of the cardiovascular system: increased heart rate, tachycardia, bradycardia or angina and increased blood pressure values;
• hearing and balance disorders: vertigo, ear ringing or pain;
• gastrointestinal lesions: nausea, constipation, pain affecting the abdominal area, dry mouth, diarrhea, dyspeptic symptoms and belching;
• signs of the epidermis: itching, hyperhidrosis, or urticaria;
• dysfunction of the musculoskeletal system: arthritis, pain affecting the joints, bones, back and muscles, myopathy, arthrosis and convulsions;
• problems with the work of the urethra: increased urination or polyuria;
• disorders of the reproductive system: pain affecting the breasts, or menorrhagia;
• allergy symptoms;
• asthenia, thirst, flushes of heat to the skin of the face, peripheral puffiness, chills, systemic weakness and discomfort in the sternum area.

Overdose

In case of intoxication, an increase in BP values is possible, and in addition, the appearance of other disorders in the work of the CAS.

Gastric lavage and symptomatic intervention are required immediately.

Because the term half-life of the active element is about 4 hours, in case of poisoning the patient must be followed for at least 20 hours, until all signs of the disorder disappear.

Information regarding the effectiveness of hemodialysis with peritoneal dialysis for blood indicators eletriptan is missing.

[9], [10],

Interactions with other drugs

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

Because of this, Relpax is not used with ketoconazole, josamycin, itraconazole, and in addition with erythromycin, clarithromycin and agents that slow down the action of the protease.

With the combined use of the drug with verapamil, propranolol or fluconazole, an increase in the Cmax level of eleptriptan occurs. But such changes do not affect the clinical picture.

With the introduction of ergotamine or caffeine after 1-2 hours after the use of Relpaksa, there is a slight but additive increase in blood pressure. Because of this, drugs that include ergotamine or ergotamine-like medications are prohibited to be administered within 24 hours from the time Relpaks is applied. Also, it should not be taken in the period of 24 hours from the time of use of these drugs.

The introduction of eletriptan in combination with substances with serotonergic properties, increases the likelihood of developing serotonin intoxication. In the case of simultaneous use of such funds is required to carefully monitor the patient's condition.

[11]

Storage conditions

Relpaks need to be kept in the place closed from small children. The temperature level can be a maximum of 30 ° C.

[12],

Shelf life

Relpax can be used for a 36-month period from the moment the medication is sold.

[13]

Application for children

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

Analogs

Analogues of drugs are drugs Imigran, Amigrenin with Cofetamine and Sumatriptan with Zomig.

[14], [15]

Reviews

Relpax is considered to be very effective in the development of migraine attacks - this is stated in many patient reviews. It is argued that after taking a pill, the signs of migraine completely disappear - a decrease in their intensity is observed approximately in half an hour.

Of the minuses, the development of adverse symptoms, including nausea, tremor, drowsiness, and so on, is distinguished. There are also people to whom the use of the drug did not help at all, but their minority.

In the comments, many advise to sleep after taking the medication - this minimizes the likelihood of side effects.