Eletriptan

When ATH:
N02CC06

Pharmacological action

The agent for the treatment of migraine. Селективный агонист серотониновых 5-HT1B- and 5-HT1D-receptor, which are located mainly, in blood vessels Golon brain. Upon stimulation of these receptors occurs vasoconstriction, in particular, of the carotid arteries, which reduces headache. Eletriptan has also high affinity to serotonin 5-HT1F-receptors, It has a moderate effect on the 5-HT1A-, 5-HT2B-, 5-HT1E- and 5-HT7-receptors.

Protivomigrenoznoe action of eletriptan may be due to its ability to narrowing of intracranial blood vessels, and its inhibitory activity against neurogenic inflammation.

Pharmacokinetics

After ingestion eletriptan quickly and sufficiently absorbed from the gastrointestinal tract (81%). The absolute bioavailability of approximately 50%. The time to reach Cmax plasma levels of about 1.5 no.

The on / in the introduction of Vd 138 l. Protein binding - about 85%.

In in vitro studies show, eletriptan that is metabolized in the liver with the participation of CYP3A4, and to a small extent - CYP2D6. Identified 2 osnovnыh tsirkuliruyushtih metabolite, which are formed by N-oxidation of (inactive) and by N-demethylation (in activity comparable to eletriptanom). Plasma concentration of the active metabolite is likely 10-20% the concentration of eletriptan and not of great importance for the development of its therapeutic effect.

After the on / in the T1 / 2 of eletriptan is about 4 no, total clearance of plasma - 36 l /. After ingestion average renal clearance is about 3.9 l /. The share of extrarenal clearance is approximately 90% of the total clearance; this indicates, that eletriptan output, mainly, in the form of metabolites in urine and faeces.

Elderly patients may be increased T1 / 2 approximately 4.4 h to 5.7 no.

In patients with impaired liver function (Classes A and B on the Child-Pugh) staticticheski revealed a significant increase in AUC and T1 / 2, and a small increase in plasma Cmax

Testimony

Relief of migraine attacks (with aura and without aura).

Dosage regimen

Is the inside. The initial single dose - 40 mg. The multiplicity of the application depends on the clinical response to the reception.

The maximum daily dose is 160 mg.

Side effect

Cardio-vascular system: sensation of heat or hot flashes to the face, heartbeat, tachycardia, chest pain, increased blood pressure.

From the central and peripheral nervous system: drowsiness, dizziness, paresthesia, headache, gipesteziya, increased perspiration, feeling “coma” in the throat.

On the part of the digestive tract: stomach ache, dry mouth, nausea, dyspepsia.

On the part of the musculoskeletal system: myasthenia, myalgia.

The respiratory system: pharyngitis.

Allergic reactions: rash, itch, hives.

Contraindications

Serious liver, uncontrolled hypertension, CHD (incl. Prinzmetal angina, myocardial infarction, silent myocardial ischemia) or suspected it, occlusive peripheral vascular disease, cerebrovascular accident or transient ischemic attack in history, use of ergotamine or its derivatives for 24 hours before or after administration of eletriptan, simultaneous with other agonists of serotonin 5-HT1-receptors, childhood and adolescence up 18 years, Hypersensitivity to eletriptanu.

Cautions

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

Eletriptan should not be used prophylactically.

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

It should not be given without prior examination of patients, who is probably the presence or increased risk of cardiovascular disease.

Do not use to treat headaches, which may be associated with stroke, aneurysm rupture.

Eletriptan, received during the occurrence of the aura does not hinder the development of the headache, so it should not be applied only during the phase of headache.

should not be used concurrently with potent inhibitors of CYP3A4.

In patients with impaired renal function enhances the hypotensive effect of eletriptan. When applied in doses of eletriptan 60 mg, and more (in the therapeutic dose range) recorded a slight and transient increase in blood pressure. Blood pressure rises to a greater degree in patients with impaired renal function and in elderly patients (clinical effects were observed).

Drug Interactions

When applied simultaneously with erythromycin (1 g) and ketokonazolom (400 mg), is a potent inhibitor of CYP3A4 showed a significant increase in Cmax in plasma, AUC and T1 / 2 eletriptan.

While the use of caffeine or ergotamine, a slight, but an additive increase in blood pressure.