Short answer: Bromocriptine has a half-life of about 6 hours. Levels peak 53 minutes fasting; 90 to 120 minutes after a high-fat meal after a dose. People vary, so treat these as estimates.
Bromocriptine is a dopamine agonist, an ergot-derived drug that acts like the brain chemical dopamine. A quick-release form taken in the morning, Cycloset, is approved to help lower blood sugar in type 2 diabetes. Other bromocriptine products are used for other conditions and have their own labels; this page covers Cycloset.
Also known as: Cycloset, bromocriptine mesylate.
Cycloset comes as a 0.8 mg tablet, so the daily dose is a number of tablets (2 to 6 tablets is 1.6 to 4.8 mg).
The Cycloset label approves it, with diet and exercise, to improve blood sugar control in adults with type 2 diabetes; it is not for type 1 diabetes or diabetic ketoacidosis. Label dosing: one 0.8 mg tablet once a day within 2 hours after waking, with food, going up by one tablet each week to 6 tablets (4.8 mg) or the most tolerated between 2 and 6. A missed morning dose is skipped and the usual dose taken the next morning, not doubled.
The label has no boxed warning. Its first warning is low blood pressure on standing and fainting, especially when starting or raising the dose. It may worsen psychotic disorders, and can cause impulse-control problems and sleepiness. It is not used with an allergy to ergot drugs, syncopal migraine, after giving birth, or while breastfeeding. In the 52-week safety trial of 3,070 people, nausea affected 32.2% vs 7.6% on placebo, dizziness 14.8% vs 9.2%, fatigue 13.9% vs 6.7% and vomiting 8.1% vs 3.1%, mostly during the first dose increases. See Cycloset side effects, Cycloset dosing schedule and missed Cycloset dose.
The Cycloset label says 65% to 95% of a dose is absorbed but only about 7% reaches the blood, because most is broken down on first pass through the gut and liver (mainly by CYP3A4). Levels peak 53 minutes after a dose when fasting and about 90 to 120 minutes after a high-fat meal, which also raises exposure by about 55% to 65%. The elimination half-life is about 6 hours.
Numbers shown are taken from the source above. Half-life varies from person to person.
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