Delmigren (Tablets) Instructions for Use

Marketing Authorization Holder

Grotex, LLC (Russia)

ATC Code

N02CC06 (Eletriptan)

Active Substance

Eletriptan (Rec.INN registered by WHO)

Dosage Forms

	Delmigren	Film-coated tablets, 20 mg: 2, 4, 6, 8, 10, 12, 18, 20, 30, 40, 50, 60 or 90 pcs.
		Film-coated tablets, 40 mg: 2, 4, 6, 8, 10, 12, 18, 20, 30, 40, 50, 60 or 90 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, round, biconvex.

Excipients: microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate.

Film coating composition: polyvinyl alcohol, titanium dioxide (E171), polyethylene glycol (macrogol) 4000, talc.

2 pcs. – contour cell packaging (1) – cardboard packs.
2 pcs. – contour cell packaging (2) – cardboard packs.
2 pcs. – contour cell packaging (3) – cardboard packs.
2 pcs. – contour cell packaging (4) – cardboard packs.
2 pcs. – contour cell packaging (5) – cardboard packs.
2 pcs. – contour cell packaging (6) – cardboard packs.
2 pcs. – contour cell packaging (9) – cardboard packs.
10 pcs. – contour cell packaging (1) – cardboard packs.
10 pcs. – contour cell packaging (2) – cardboard packs.
10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (4) – cardboard packs.
10 pcs. – contour cell packaging (5) – cardboard packs.
10 pcs. – contour cell packaging (6) – cardboard packs.
10 pcs. – contour cell packaging (9) – cardboard packs.

Film-coated tablets white or almost white, round, biconvex.

Excipients: microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate.

Film coating composition: polyvinyl alcohol, titanium dioxide (E171), polyethylene glycol (macrogol) 4000, talc.

2 pcs. – contour cell packaging (1) – cardboard packs.
2 pcs. – contour cell packaging (2) – cardboard packs.
2 pcs. – contour cell packaging (3) – cardboard packs.
2 pcs. – contour cell packaging (4) – cardboard packs.
2 pcs. – contour cell packaging (5) – cardboard packs.
2 pcs. – contour cell packaging (6) – cardboard packs.
2 pcs. – contour cell packaging (9) – cardboard packs.
10 pcs. – contour cell packaging (1) – cardboard packs.
10 pcs. – contour cell packaging (2) – cardboard packs.
10 pcs. – contour cell packaging (3) – cardboard packs.
10 pcs. – contour cell packaging (4) – cardboard packs.
10 pcs. – contour cell packaging (5) – cardboard packs.
10 pcs. – contour cell packaging (6) – cardboard packs.
10 pcs. – contour cell packaging (9) – cardboard packs.

Clinical-Pharmacological Group

Serotonin 5-HT₁ receptor agonist. Agent with antimigraine activity

Pharmacotherapeutic Group

Analgesics; antimigraine preparations; selective agonists of serotonin 5-HT₁ receptors

Pharmacological Action

An agent for the treatment of migraine. A selective agonist of serotonin 5-HT_1B and 5-HT_1D receptors, which are located mainly in the blood vessels of the brain. Stimulation of these receptors causes vasoconstriction, in particular, of the carotid artery system, which leads to a reduction in headache.

Eletriptan also has a high affinity for serotonin 5-HT_1F receptors and has a moderate effect on 5-HT_1A, 5-HT_2B, 5-HT_1E, and 5-HT₇ receptors.

The antimigraine effect of eletriptan may be due to its ability to constrict intracranial blood vessels, as well as its inhibitory effect on neurogenic inflammation.

Pharmacokinetics

After oral administration, Eletriptan is rapidly and sufficiently absorbed from the gastrointestinal tract (81%). The absolute bioavailability is about 50%. The time to reach C_max in blood plasma is about 1.5 hours.

In vitro studies have shown that Eletriptan is metabolized in the liver with the participation of the CYP3A4 isoenzyme and, to a lesser extent, CYP2D6. Two main circulating metabolites have been identified, formed by N-oxidation (inactive) and by N-demethylation (comparable in activity to eletriptan).

The concentration of the active metabolite in blood plasma is only 10-20% of the concentration of eletriptan and is not of great importance for the development of its therapeutic effect.

After oral administration, the average renal clearance is about 3.9 L/h. The proportion of non-renal clearance is approximately 90% of the total clearance; this indicates that Eletriptan is excreted mainly as metabolites in urine and feces.

Indications

Relief of migraine attacks (with and without aura).

ICD codes

Dosage Regimen

Administer orally at the first sign of a migraine headache.

Take a single 40 mg tablet as the recommended initial dose.

If headache recurs, a second dose may be taken after a minimum 2-hour interval.

Do not exceed a single dose of 40 mg.

The maximum daily dose is 160 mg.

If inadequate response is observed with the 40 mg dose, a 20 mg dose may be effective for subsequent attacks.

Do not use for the prophylaxis of migraine.

Initiate treatment during the headache phase of the migraine attack; administration during the aura phase will not prevent the headache.

If a patient does not experience response to the first dose, re-evaluate the diagnosis before administering eletriptan for subsequent attacks.

Do not use concomitantly with ergotamine derivatives or other 5-HT1 receptor agonists.

Avoid concurrent use with potent CYP3A4 inhibitors.

Adverse Reactions

Infections often – pharyngitis, rhinitis; rarely – respiratory tract infections.

Metabolism and nutrition disorders infrequently – anorexia.

Psychiatric disorders infrequently – thinking disturbances, agitation, confusion, depersonalization, euphoria, depression, insomnia; rarely – emotional lability.

Nervous system disorders often – drowsiness, headache, dizziness, sensation of “tingling” or other sensitivity disorders, muscle hypertonia, hypesthesia, myasthenia; infrequently – tremor, hyperesthesia, ataxia, hypokinesia, speech disorder, stupor, syncope, taste disturbance.

Eye disorders infrequently – vision disorders, eye pain, photophobia, lacrimation disorder; rarely – conjunctivitis.

Ear and labyrinth disorders often – vertigo; infrequently – ear pain, tinnitus.

Cardiac disorders often – palpitations, tachycardia; rarely – angina pectoris, increased blood pressure, bradycardia, shock, myocardial ischemia or infarction, coronary artery spasm.

Respiratory, thoracic and mediastinal disorders often – throat tightness; infrequently – dyspnea, yawning; rarely – bronchospasm, voice change.

Gastrointestinal disorders often – abdominal pain, nausea, dry mouth, dyspepsia; infrequently – diarrhea, glossitis; rarely – constipation, esophagitis, tongue edema, eructation, ischemic colitis.

Hepatobiliary disorders rarely – hyperbilirubinemia, increased AST activity.

Skin and subcutaneous tissue disorders often – hyperhidrosis; infrequently – rash, pruritus; rarely – skin diseases, urticaria.

Musculoskeletal and connective tissue disorders often – back pain, myalgia; infrequently – arthralgia, arthrosis, bone pain; rarely – arthritis, myopathy, muscle cramps.

Renal and urinary disorders infrequently – pollakiuria, polyuria.

Reproductive system and breast disorders rarely – breast pain, menorrhagia.

General disorders and administration site conditions often – feeling of warmth or facial flushing, chills, asthenia, pain, feeling of tightness, pressure in the chest; infrequently – allergic reactions, malaise, facial edema, thirst, peripheral edema; rarely – lymphadenopathy.

Contraindications

Hypersensitivity to eletriptan; severe hepatic impairment, uncontrolled arterial hypertension, coronary artery spasm, ischemic heart disease (including angina pectoris, Prinzmetal’s angina, history of myocardial infarction) or suspicion thereof, arrhythmias, heart failure, occlusive peripheral vascular diseases, history of cerebrovascular accident or transient ischemic attack; use of ergotamine or its derivatives within 24 hours before or after taking eletriptan, concurrent use with CYP3A4 inhibitors (ketoconazole, itraconazole, erythromycin, clarithromycin, josamycin) and protease inhibitors (ritonavir, indinavir, nelfinavir), concurrent use with other serotonin 5-HT₁ receptor agonists; children and adolescents under 18 years of age.

Eletriptan is not indicated for the relief of hemiplegic, ophthalmoplegic, or basilar migraine.

With caution

Concomitant use of eletriptan with other drugs possessing serotonergic activity, such as SSRIs. Use in doses above 40 mg in patients with renal impairment (the effect of eletriptan on blood pressure is enhanced).

Use in Pregnancy and Lactation

During pregnancy, it can be used if the expected benefit to the mother outweighs the potential risk to the fetus.

If use during lactation is necessary, breastfeeding should be discontinued for 24 hours after taking eletriptan.

Use in Hepatic Impairment

Contraindicated in severe hepatic impairment.

Use in Renal Impairment

In patients with renal impairment, the hypotensive effect of eletriptan is enhanced.

Pediatric Use

Contraindicated in children and adolescents under 18 years of age.

Geriatric Use

Should be used with caution in elderly patients, as the effect of eletriptan on blood pressure in the elderly may be more pronounced compared to younger patients.

Special Precautions

Eletriptan should be used only in cases where the diagnosis of migraine is not in doubt.

Eletriptan should not be used prophylactically.

Eletriptan is effective in treating migraine with and without aura and menstrually associated migraine. Eletriptan taken during the aura phase does not prevent the development of headache, so it should be taken only during the headache phase. Eletriptan has been found to be effective also in relieving symptoms associated with migraine, such as nausea, vomiting, photophobia, phonophobia, and in treating headache recurrence during an attack.

Eletriptan is not indicated for the relief of hemiplegic, ophthalmoplegic, or basilar migraine.

Eletriptan should not be prescribed without prior examination to patients who are likely to have or are at increased risk of developing cardiovascular diseases.

Do not use to treat headache that may be associated with stroke, ruptured aneurysm.

Eletriptan should not be used concurrently with potent inhibitors of the CYP3A4 isoenzyme.

Cases of cerebral hemorrhage, subarachnoid hemorrhage, stroke, or other cerebrovascular events, sometimes fatal, have been reported with the use of 5-HT1 serotonin receptor agonists.

When eletriptan and SSRIs (e.g., fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram) and SNRIs (e.g., venlafaxine, duloxetine) are used concomitantly, a potentially life-threatening serotonin syndrome may develop. This syndrome may manifest with the following symptoms: mental status changes (e.g., agitation, hallucinations, coma), autonomic instability (e.g., tachycardia, blood pressure lability, hyperthermia), neuromuscular system dysfunction (e.g., hyperreflexia, incoordination) and/or gastrointestinal symptoms (e.g., nausea, vomiting, diarrhea).

It should be considered that uncontrolled use of antimigraine drugs can lead to chronic daily headaches. Cases of overuse of any triptans are most often observed in patients with daily headaches.

Effect on ability to drive vehicles and operate machinery

When using eletriptan, patients should exercise caution when driving vehicles and operating machinery, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Concomitant use with erythromycin (1 g) and ketoconazole (400 mg), which are potent inhibitors of the CYP3A4 isoenzyme, revealed a significant increase in the C_max in plasma, AUC, and T_1/2 of eletriptan.

Concomitant use with caffeine or ergotamine results in a slight but additive increase in blood pressure.

Concomitant use of 5-HT serotonin receptor agonists, including eletriptan, with drugs possessing serotonergic activity, such as SSRIs and SNRIs, may increase the risk of developing serotonin syndrome.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.