Ropinirole

Ropinirole is indicated for the treatment of the signs and symptoms of idiopathic Parkinson’s disease. It is also indicated for the treatment of moderate-to-severe primary Restless Legs Syndrome (RLS).

Ropinirole is a non-ergoline dopamine agonist. Ropinirole has the highest affinity at the D3 receptors, which are concentrated in the limbic areas of the brain and may be responsible for some of the neuropsychiatric effects. The exact mechanism of action of ropinirole as a treatment for Parkinson’s disease is unknown, however, it is believed to be related to its ability to selectively stimulate dopamine D2 receptors within the caudate-putamen system in the brain. This system affects body movement. Negligible affinity is seen for ropinirole at α2 adrenoreceptors in the periphery and 5HT-1 receptor. Ropinirole has no affinity at the D1-like receptors, benzodiazepine or GABA receptors. The precise mechanism of action of ropinirole as a treatment for Restless Legs Syndrome is unknown, however, it is believed to be related to its ability to stimulate dopamine receptors.

Dosing for Parkinson’s disease: The recommended starting dose for Parkinson’s disease is 0.25 mg three times daily. Based on individual patient therapeutic response and tolerability, if necessary, the dose should then be titrated with weekly increments as described below. Maximum recommended total daily dose of 24 mg (8 mg three times daily).

• Week 1: 0.25 mg 3 times daily. Total Daily Dose 0.75 mg
• Week 2: 0.5 mg 3 times daily. Total Daily Dose 1.50 mg
• Week 3: 0.75 mg 3 times daily. Total Daily Dose 2.25 mg
• Week 4: 1 mg 3 times daily. Total Daily Dose 3 mg

Dosing for Restless Legs Syndrome: The recommended adult starting dose for RLS is 0.25 mg once daily 1 to 3 hours before bedtime. After 2 days, if necessary, the dose can be increased to 0.5 mg once daily, and to 1 mg once daily at the end of the first week of dosing, then as shown below as needed to achieve efficacy. Titration should be based on individual patient therapeutic response and tolerability, up to a maximum recommended dose of 4 mg daily.

• Days 1 and 2: 0.25 mg, 1 to 3 hours before bedtime, to be taken once daily
• Days 3-7: 0.5 mg, 1 to 3 hours before bedtime, to be taken once daily
• Days 2: 1 mg, 1 to 3 hours before bedtime, to be taken once daily
• Days 3: 1.5 mg, 1 to 3 hours before bedtime, to be taken once daily
• Days 4: 2 mg, 1 to 3 hours before bedtime, to be taken once daily
• Days 5: 2.5 mg, 1 to 3 hours before bedtime, to be taken once daily
• Days 6: 3 mg, 1 to 3 hours before bedtime, to be taken once daily
• Days 7: 4 mg, 1 to 3 hours before bedtime, to be taken once daily

Because Ropinirole is a dopamine agonist, it is possible that dopamine antagonists such as neuroleptics (phenothiazines, butyrophenones, thioxanthenes) or metodopramide may reduce the efficacy of Ropinirole.

It is contraindicated in patients known to have a hypersensitivity to Ropinirole.

The most common side effects of Ropinirole include fainting, drowsiness, hallucinations, dizziness, nausea or vomiting, uncontrolled sudden movements, leg swelling, fatigue, confusion, headache, upset stomach, abdominal pain or discomfort, increased sweating etc.

Pregnancy category C. There is no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit outweighs the potential risk to the fetus. Ropinirole inhibits prolactin secretion in human and could potentially inhibit lactation.

Patients treated with Ropinirole have reported falling asleep while engaged in activities of daily living. Dopamine agonists in clinical trials and clinical experience appear to impair the systemic regulation of blood pressure, with resulting orthostatic hypotension.

Antiparkinson drugs

Protect from light and moisture, store below 25°C. Keep out of the reach of children.