Ropinirole - instructions for use, dose, side effects, contraindications

Well absorbed in the digestive tract. It is well distributed in tissues, penetrates the placenta and into breast milk (in studies on rats). Relationship with plasma proteins 40%. Biotransformation occurs in the liver with the help of cytochromes P450 (CYP1A2). The half-life is6 hours. The maximum concentration in plasma is detected through1.5 hours (up to 2.5-4 hours when eating). Elimination is carried out by the kidneys (10% - unchanged).

Indications:

Parkinson's disease.

ICD-10

VI.G20-G26.G20 Parkinson's disease

Contraindications:

Hypersensitivity, hallucinations.

Carefully:

Hypotension, orthostatic hypotension, kidney disease.

Pregnancy and lactation:

Adequate and well-controlled studies in humans are not conducted. Ropinirole should be used during pregnancy only if the potential benefit exceeds the potential risk to the fetus. Ropinirole and its metabolites penetrate into the milk of rats.Do not apply!

Recommendations for FDA - Category C.

Dosing and Administration:The recommended initial dose is 2 mg once a day for one week. Subsequently, the dose is increased by 2 mg at intervals of not less than 1 week to 8 mg per day. If, after choosing a dose, the therapeutic effect is not sufficiently pronounced or unstable, you can continue increasing the daily dose of the drug by 4 mg at intervals of 1-2 weeks (until the desired therapeutic effect is achieved). The dose can be changed depending on the therapeutic effect and increased to a maximum dose of 24 mg once a day.

Side effects:

From the side CNS: dizziness, drowsiness, nervousness, behavioral disorders, hypersexuality, psychotic reactions, sudden falling asleep, hallucinations, dyskinesia.

From the side digestive system: dyspeptic reactions (including nausea, heartburn), dry mouth, constipation, vomiting.

From the side musculoskeletal system: arthralgia, myalgia.

From the side of cardio-vascular system: orthostatic hypotension, arterial hypertension.

From the side respiratory system: bronchitis, nasopharyngitis.

Other: increased sweating, reactions of hypersensitivity, pain in the chest.

Overdose:

Symptoms: agitation, chest pain (heart), anxiety, increased dyskinesia (including oral automatisms), nausea, orthostatic hypotension, dizziness.

Treatment: lavage of the stomach (to reduce absorption). Hemodialysis is ineffective.

Interaction:

Levodopa enhances the side effect of ropinirole. Reducing the dose of levodopa reduces this effect.

Nicotine (smoking) and omeprazole increase the metabolism of ropinirole.

Estrogens increase the clearance of ropinirole by 36%.

Ciprofloxacin increases the concentration of ropinirole in plasma by 60%.

Special instructions:

With Parkinson's disease with motor complications ropinirole like bromocriptine affects the shutdown period and allows you to lower the dose of levodopa drugs (without increasing adverse effects, including dyskinesia). However, studies are not sufficient to detect clinically significant differences between dopamine receptor agonists.

Treatment with ropinirole can reduce the dose of levodopa, but enhances dyskinesia.Exact exposure to the turn-off period has not been proven (possibly due to inadequate selection data, short or medium term follow-up). It is necessary to further study ropinirole in comparison with the studied agonists of dopamine receptors.

Ropinirole can be considered as a neuroprotector in Parkinson's disease.

Has an effect on tremor in the early stages of Parkinson's disease.

Levodopa is a more effective drug for the treatment of Parkinson's disease, but in patients in its initial stage ropinirole showed the best results.

Instructions

Ropinirole (Ropinirolum)