BROMOCRIPTINE MESYLATE (broe-moe-krip'teen) Parlodel Classifications: autonomic nervous system agent; ergot alkaloid; antiparkinsonism agent Prototype: Ergotamine Pregnancy Category: C
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2.5 mg tablets; 5 mg capsules
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.
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.
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.
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.
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.
Hepatic and renal dysfunction; history of psychiatric disorder; history of MI with residual arrhythmia.
Amenorrhea or Galactorrhea, Female Infertility Adult: PO 1.252.5 mg/d (max: 2.5 mg 23 times/d)
Suppression of Postpartum Lactation Adult: PO 2.5 mg b.i.d. starting at least 4 h after delivery for 1421 d
Parkinson's Disease Adult: PO 1.252.5 mg/d (max: 100 mg/d in divided doses)
Acromegaly Adult: PO 1.252.5 mg/d for 3 d, then increase by 1.252.5 mg q37d until desired effect is achieved, usually 3060
mg/d in divided doses
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Oral
- Do not begin therapy unless vital signs are stabilized.
- Give with meals, milk, or other food to reduce incidence of GI side effects.
- Have patient in supine position before receiving first dose because dizziness and fainting may occur. For this reason, initial
dose is usually prescribed for evening administration.
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Note: Withhold therapy until 4 h after delivery and then begin only if vital signs have stabilized.
- Store in tightly closed, light-resistant containers, preferably at 15°30° C (59°86° F) unless
otherwise directed.
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.
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.
Absorption: Approximately 28% absorbed from GI tract. Peak: 12 h. Duration: 48 h. Metabolism: Metabolized in liver. Elimination: 85% excreted in feces in 5 d; 36% eliminated in urine. Half-Life: 50 h.
Assessment & Drug Effects
- Monitor vital signs closely during the first few days and periodically throughout therapy.
- Lab tests: Periodic CBC, liver functions and renal functions with prolonged therapy.
- Monitor for and report psychotic symptoms and other adverse reactions in Parkinson's patients because larger doses are used.
- Improvement in Parkinson's disease may be noted in 3090 min following administration of bromocriptine, with maximum
effect in 2 h.
Patient & Family Education
- Make position changes slowly and in stages, especially from lying down to standing, and to dangle legs over bed for a few
minutes before walking. Lie down immediately if light-headedness or dizziness occurs.
- Do not drive or engage in other potentially hazardous activities until response to drug is known.
- Avoid exposure to cold and report the onset of pallor of fingers or toes.
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Note: Patients taking bromocriptine to suppress postpartum lactation may have temporary rebound breast enlargement and pain following
drug withdrawal.
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Note: Restoration of regular menses usually occurs in 68 wk. Since fertility may be restored during therapy, advise patients
being treated for amenorrhea and galactorrhea to use barrier-type contraceptive measures until normal ovulating cycle is restored.
Oral contraceptives are contraindicated.
- Inform physician immediately, if pregnancy occurs during therapy. Bromocriptine should be discontinued without delay.
- Do not breast feed while taking this drug.