BROMOCRIPTINE MESYLATE
(broe-moe-krip'teen)
Parlodel
Classifications: autonomic nervous system agent; ergot alkaloid; antiparkinsonism agent
Prototype: Ergotamine
Pregnancy Category: C

Availability

2.5 mg tablets; 5 mg capsules

Actions

Semisynthetic ergot alkaloid derivative, but devoid of oxytocic activity generally attributed to drugs of this class. Reduces elevated serum prolactin levels in men and women by activating postsynaptic dopaminergic receptors in hypothalamus to stimulate release of prolactin-inhibiting factor and possibly luteinizing hormone release factor.

Therapeutic Effects

Restores ovulation and ovarian function in amenorrheic women, thus correcting female infertility secondary to elevated prolactin levels. Activates dopaminergic receptors in neostriatum of CNS, which may explain action in parkinsonism.

Uses

Short-term management of amenorrhea/galactorrhea or female infertility associated with hyperprolactinemia (when there is no indication of pituitary tumor). Also used as adjunctive to levodopa or levodopa/carbidopa therapy to relieve symptoms of Parkinson's disease and to lower plasma growth hormone in patients with acromegaly.

Unlabeled Uses

To prevent postpartum lactation, to relieve premenstrual symptoms, to treat hypogonadism and galactorrhea in hyperprolactinemic men; for management of hepatic encephalopathy, Cushing's syndrome, drug-induced neuroleptic malignant syndrome, and cocaine withdrawal.

Contraindications

Hypersensitivity to ergot alkaloids; uncontrolled hypertension; severe ischemic heart disease or peripheral vascular disease; pituitary tumor; normal prolactin levels, lactation. Safe use during pregnancy (category C) or in children <15 y is not established.

Cautious Use

Hepatic and renal dysfunction; history of psychiatric disorder; history of MI with residual arrhythmia.

Route & Dosage

Amenorrhea or Galactorrhea, Female Infertility
Adult: PO 1.25–2.5 mg/d (max: 2.5 mg 2–3 times/d)

Suppression of Postpartum Lactation
Adult: PO 2.5 mg b.i.d. starting at least 4 h after delivery for 14–21 d

Parkinson's Disease
Adult: PO 1.25–2.5 mg/d (max: 100 mg/d in divided doses)

Acromegaly
Adult: PO 1.25–2.5 mg/d for 3 d, then increase by 1.25–2.5 mg q3–7d until desired effect is achieved, usually 30–60 mg/d in divided doses

Administration

Oral

Adverse Effects (1%)

Body as a Whole: Mostly dose related. CNS: Headache, dizziness, vertigo, light-headedness, fainting, sedation, nightmares, insomnia, dyskinesia, ataxia; mania, nervousness, anxiety, depression. CV: Orthostatic hypotension, shock, postpartum hypertension, palpitation, extrasystoles, Raynaud's phenomenon, red, tender, hot, edematous extremities (erythromelalgia), exacerbation of angina, arrhythmias, acute MI. Special Senses: Blurred vision, burning sensation in eyes, blepharospasm, diplopia. GI: Nausea, vomiting, abdominal cramps, epigastric pain, constipation (long-term use) or diarrhea; metallic taste, dry mouth, dysphagia, anorexia, peptic ulcers. Skin: Urticaria, rash, mottling, livedo reticularis. Other: Fatigue, nasal congestion, asthenia.

Interactions

Drug: Possibility of decreased tolerance to alcohol; antihypertensive agents add to hypotensive effects; oral contraceptives, estrogen, progestins may interfere with effect of bromocriptine by causing amenorrhea and galactorrhea; phenothiazines, tricyclic antidepressants, methyldopa, reserpine can cause an increase in prolactin, which may interfere with bromocriptine activity.

Pharmacokinetics

Absorption: Approximately 28% absorbed from GI tract. Peak: 1–2 h. Duration: 4–8 h. Metabolism: Metabolized in liver. Elimination: 85% excreted in feces in 5 d; 3–6% eliminated in urine. Half-Life: 50 h.

Nursing Implications

Assessment & Drug Effects

Patient & Family Education


Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug