DRUG TITLE

Requip (Ropinirole)

Pharmacological action

Antiparkinsonian drug, dopamine receptor agonist of non-ergoline structure. Its structure is similar to dopamine and it binds especially actively to D2- and D3-subtype receptors, acting also on presynaptic autoreceptors. In the early stage of Parkinson's disease, ropinirole is as effective as levodopa and more effective than bromocriptine. During the 3-year study ropinirole provided adequate correction of antiparkinsonian symptoms in 60% of patients. In late-stage Parkinson's disease, ropinirole in combination with levodopa reduced the duration of the off period by 12% and allowed a 31% reduction in the levodopa dose.

Pharmacokinetics

After oral administration, it is rapidly absorbed from the gastrointestinal tract. Cmax in plasma is reached after 1-2 hours. Bioavailability is about 85%. Binding to plasma proteins is about 40%. Metabolized in the liver to form inactive metabolites. Vd - 7.5 l/kg.

Contraindications for use

Severe renal insufficiency, severe hepatic insufficiency, pregnancy, lactation (breast-feeding), hypersensitivity to ropinirole.

Administration during pregnancy and lactation

It is contraindicated for use during pregnancy and lactation (breast-feeding).

Administration in patients with liver dysfunction

Acute hepatic insufficiency is contraindicated.

Administration in patients with kidney dysfunction

Contraindicated in severe hepatic insufficiency.

Administration in children

It is not recommended to use in children and teenagers below 18 years of age.

Indications of the active substance ROPINIROL

Parkinson's disease.

Dosage regimen

It is taken orally. During 1 week - 25 mcg 3 times/day, during 2 weeks - 500 mcg 3 times/day, during 3 weeks - 750 mcg 3 times/day, during 4 weeks - 1 mg 3 times/day. Later the dose may be increased by 0.5-1 mg three times a day (1.5-3 mg/day). Therapeutic effect is usually achieved at doses of 3-9 mg/day. If symptoms persist, the dose may be increased to 24 mg/day.