Bromocriptine Mesylate(broe moe krip’ teen mess’ ah late)
Apo-Bromocriptine (CAN), Cycloset, Parlodel, Parlodel SnapTabs
PREGNANCY CATEGORY B
Drug Classes
Antidiabetic
Antiparkinsonian
Dopamine receptor agonist
Semisynthetic ergot derivative
Therapeutic Actions
Parkinsonism: Acts as an agonist directly on postsynaptic dopamine receptors of neurons in the brain, mimicking the effects of the neurotransmitter dopamine, which is deficient in parkinsonism. Unlike levodopa, bromocriptine does not require biotransformation by the nigral neurons that are deficient in parkinsonism patients; thus, bromocriptine may be effective when levodopa has begun to lose its efficacy.
Hyperprolactinemia: Acts directly on postsynaptic dopamine receptors of the prolactin-secreting cells in the anterior pituitary, mimicking the effects of prolactin inhibitory factor, inhibiting the release of prolactin and galactorrhea. Also restores normal ovulatory menstrual cycles in patients with amenorrhea or galactorrhea, and inhibits the release of growth hormone in patients with acromegaly.
Diabetes: Stimulates CNS dopamine activity, which indirectly improves glycemic control; exact mechanism of action not known, but these patients may have decreased dopamine activity as part of their metabolic syndrome.
Indications
Treatment of postencephalitic or idiopathic Parkinson’s disease; may provide additional benefit in patients currently maintained on optimal dosages of levodopa with or without carbidopa, beginning to deteriorate or develop tolerance to levodopa, and experiencing “end of dose failure” on levodopa therapy; may allow reduction of levodopa dosage and decrease the dyskinesias and “on-off” phenomenon associated with long-term levodopa therapy
Short-term treatment of amenorrhea or galactorrhea associated with hyperprolactinemia due to various etiologies, excluding demonstrable pituitary tumors
Treatment of hyperprolactinemia associated with pituitary adenomas to reduce elevated prolactin levels, cause shrinkage of macroprolactinomas; may be used to reduce the tumor mass before surgery
Female infertility associated with hyperprolactinemia in the absence of a demonstrable pituitary tumor
Acromegaly; used alone or with pituitary irradiation or surgery to reduce serum growth hormone level
Treatment of type 2 diabetes as monotherapy or in combination with other antidiabetics (Cycloset only)
Unlabeled uses: Hepatic encephalopathy, traumatic brain injury
Contraindications and Cautions
Contraindicated with hypersensitivity to bromocriptine or any ergot alkaloid; severe ischemic heart disease or peripheral vascular disease; uncontrolled hypertension; pregnancy, lactation.
Use cautiously with history of MI with residual arrhythmias (atrial, nodal, or ventricular); renal or hepatic disease, history of peptic ulcer (fatal bleeding ulcers have occurred in patients with acromegaly treated with bromocriptine).
Available Forms
Capsules—5 mg; tablets—0.8, 2.5 mg
