Bromocriptine mesylate
Bromocriptine mesylate (Parlodel)
Bromocriptine mesylate
(broh-moh- KRIP-teen)
Pregnancy Category: B Apo-Bromocriptine Parlodel (Rx)

Classification: Prolactin secretion inhibitor; antiparkinson agent

Action/Kinetics: Nonhormonal agent that inhibits the release of the hormone prolactin by the pituitary. Use only when prolactin production by pituitary tumors has been ruled out. Effect in parkinsonism is due to a direct stimulating effect on dopamine type 2 receptors in the corpus striatum. Use for parkinsonism may allow the dose of levodopa to be decreased, thus decreasing the incidence of severe side effects following long-term levodopa therapy. Less than 30% of the drug is absorbed from the GI tract. Onset, lower prolactin: 2 hr; antiparkinson: 30-90 min; decrease growth hormone: 1-2 hr. Peak plasma concentration: 1-3 hr. t 1/2, plasma: 6-8 hr; terminal: 15 hr. Duration, lower prolactin: 24 hr (after a single dose); decrease growth hormone: 4-8 hr. Significant first-pass effect. Metabolized in liver, excreted mainly through bile and thus the feces.

Uses: Short-term treatment of amenorrhea with or without galactorrhea, infertilitiy, or hypogonadism. Alone or as an adjunct in the treatment of acromegaly. As adjunctive therapy with levodopa in the treatment of idiopathic or postencephalitic Parkinson's disease. May provide additional benefit in clients who are taking optimal doses of levodopa, in those who are developing tolerance to levodopa therapy, or in those who are manifesting levodopa ``end of dose failure.'' Clients unresponsive to levodopa are not good candidates for bromocriptine therapy. No longer recommended to suppress postpartum lactation. Investigational: Hyperprolactinemia due to pituitary adenoma, neuroleptic malignant syndrome, cocaine dependence, cyclical mastalgia.

Contraindications: Sensitivity to ergot alkaloids. Pregnancy, lactation, children under 15 years of age. Peripheral vascular disease, ischemic heart disease.

Special Concerns: Geriatric clients may manifest more CNS effects. Use with caution in liver or kidney disease.

Side Effects: The type and incidence of side effects depend on the use of the drug. When used for hyperprolactinemia. GI: N&V;, abdominal cramps, diarrhea, constipation. CNS: Headache, dizziness, fatigue, drowsiness, lightheadedness, psychoses. Other: Nasal congestion, hypotension, CSF rhinorrhea.
When used for acromegaly. GI: N&V;, anorexia, dry mouth, dyspepsia, indigestion, GI bleeding. CNS: Dizziness, syncope, drowsiness, tiredness, headache, lightheadedness, lassitude, vertigo, sluggishness, paranoia, insomnia, heavy headedness, decreased sleep requirement, delusional psychosis, visual hallucinations. CV: Orthostatic hypotension, digital vasospasm, Raynaud's syndrome; rarely, arrhythmias, ventricular tachycardia, bradycardia, vasovagal attack. Respiratory: Nasal stuffiness, SOB. Other: Potentiation of effects of alcohol, hair loss, paresthesia, tingling of ears, muscle cramps, facial pallor, reduced tolerance to cold.

Laboratory Test Alterations: BUN, AST, ALT, GGPT, CPT, alkaline phosphatase, uric acid.

Drug Interactions: Alcohol / Chance of GI toxicity; alcohol intolerance Antihypertensives / Additive BP Butyrophenones / Effect of bromocriptine due to dopamine antagonism Diuretics / Avoid diuretics Erythromycins / Levels of bromocriptine pharmacologic and toxic effects Phenothiazines / Effect of bromocriptine due to dopamine antagonism Sympathomimetics / Side effects of bromocriptine, including VT and cardiac dysfunction

How Supplied: Capsule: 5 mg; Tablet: 2.5 mg

Dosage
?Capsules, Tablets For hyperprolactinemic conditions.
Adults, initial: 0.5-2.5 mg/day with meals; then, increase dose by 2.5 mg q 3-7 days until optimum response observed (usual: 5-7.5 mg/day; range: 2.5-15 mg/day). For amenorrhea/galactorrhea, do not use for more than 6 months. Side effects may be reduced by temporarily decreasing the dose to 1/2 tablet 2-3 times/day.
Parkinsonism.
Initial: 1.25 mg ( 1/2 tablet) b.i.d. with meals while maintaining dose of levodopa, if possible. Dosage may be increased q 14-28 days by 2.5 mg/day with meals. The usual dosage range is 10-40 mg/day. Any decrease in dosage should be done gradually in 2.5-mg decrements.
Acromegaly.
Initial: 1.25-2.5 mg for 3 days with food and on retiring; then, increased by 1.25-2.5 mg q 3-7 days until optimum response observed. Usual optimum therapeutic range: 20-30 mg/day, not to exceed 100 mg/day. Clients should be reevaluated monthly and dosage adjusted accordingly.
Hyperprolactinemia associated with pituitary adenomas.
Maintenance: 0.625-10 mg/day for 6 to 52 months.