A dopaminergic agonists, for treatment of galactorrhea, amenorrhea, infertility, acromegaly, Parkinsonism.
藥理
Bromocriptine mesylate, an ergot-derivative dopamine receptor agonist and a prolactin inhibitor, is an antiparkinsonian agent and also causes sustained suppression of somatropin (growth hormone) secretion in acromegaly.
藥動學
Approximately 28% of an oral dose of the drug is absorbed from the GI tract following oral administration; however, because of a substantial first-pass effect, only 6% of the dose reaches systemic circulation unchanged. Following oral administration of a single 1.25- to 5-mg dose of bromocriptine, serum prolactin decreases within 2 hours, is maximally decreased at 8 hours, and is still decreased at 24 hours. Bromocriptine is 90–96% bound to serum albumin. Bromocriptine mesylate is completely metabolized in the liver, principally by hydrolysis of the amide bond to produce lysergic acid and a peptide fragment. The metabolites apparently are not pharmacologically active or toxic. Bromocriptine and its metabolites are excreted principally in feces via biliary elimination; approximately 2.5–5.5% of a single dose is excreted in urine. Within 5 days, about 85% of a dose is excreted in feces. The elimination half-life of bromocriptine is 4–4.5 hours for the initial phase and 45–50 hours for the terminal phase.
1. For the prevention of puerperal lactation: initially 1.25mg a day, then 2.5mg BID for 4-14 days. 2. For galactorrhea, amenorrhea infertility & acromegaly: initially 1.25mg (at night with food) increased by 1.25mg every third day, as necessary, up to 15mg a day (but up to 30mg daily may be required), usually in three divided doses with meals. 3. For Parkinsonism: up to 100mg a day (but up to 300mg daily has been used) in divided doses.