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1. Question
Which drug is a non-ergot dopamine agonist and has a side-effect profile different from the rest of the dopaminergic agents?
Correct
The answer is C
Explanation:
Non-ergot dopamine agonists such as ropinirole are indicated for both early and advanced stages of Parkinson disease. Th ese drugs selectively bind to dopamine receptors and activate the D2-receptor but have little or no affi nity for the D1-receptor. Th ey have a greater affi nity for the D3-receptor than for the D2- receptor. Th e incidence of adverse events (e.g., pleuropulmonary fibrosis and retroperitoneal fi brosis, coronary vasoconstriction, erythromelalgia, and Raynaud phenomenon) is low compared to nonselective dopamine agonists. Non- ergot dopamine agonists have a low potential for the devolvement of motor fluctuations and dyskinesia.
Incorrect
The answer is C
Explanation:
Non-ergot dopamine agonists such as ropinirole are indicated for both early and advanced stages of Parkinson disease. Th ese drugs selectively bind to dopamine receptors and activate the D2-receptor but have little or no affi nity for the D1-receptor. Th ey have a greater affi nity for the D3-receptor than for the D2- receptor. Th e incidence of adverse events (e.g., pleuropulmonary fibrosis and retroperitoneal fi brosis, coronary vasoconstriction, erythromelalgia, and Raynaud phenomenon) is low compared to nonselective dopamine agonists. Non- ergot dopamine agonists have a low potential for the devolvement of motor fluctuations and dyskinesia.
Ropinirole (Requip) NAPLEX Review
Mechanism of action is similar to pramipexole.
Administration and dosage
Initial treatment: 0.25 mg three times daily
Titrate weekly increments
Aft er week 4, if necessary, daily dosage may be increased by 1.5 mg/day on a weekly basis up to 9 mg/day, to a total of 24 mg/day.
Discontinue gradually over a 7-day period. Decrease the frequency of administration from three times to two times daily for 4 days and then once daily for the remainder of the week.
When given in combination with levodopa, consider reduction of levodopa dose.
May be taken with food to reduce the occurrence of nausea. Food decreases the rate of absorption but not the extent of absorption.
Metabolized by the liver (cytochrome P450 1A2) and fi rst-pass eff ect
Smoking induces the liver metabolism.
Between 30% and 40% protein bound
Precautions and monitoring effects
Bradycardia is observed in patients treated with ropinirole. Most cases occur within the fi rst 4 weeks of therapy and are usually associated with a recent increase of dose.
Binds to melanin-containing tissues like the eyes and skin
Symptomatic hypotension
Dopaminergic agents appear to impair the systemic regulation of blood pressure,
which results in orthostatic hypotension.
Monitoring and education of the patient is necessary, especially during doseescalation periods.