bromocriptine mesylate

bromocriptine mesylate

[brō′mōkrip′tēn]

a dopamine receptor agonist.

indications It is prescribed for the treatment of amenorrhea and galactorrhea associated with hyperprolactinemia, female infertility, and Parkinson's disease.

contraindications Sensitivity to any ergot alkaloid prohibits its use. The drug was disqualified for use in suppressing postpartum lactation by the FDA in 1994 because of a previously unrecognized increase in intracranial hemorrhages.

adverse effects Among the more severe adverse reactions are palpitations, hypotension, bradycardia, hallucinations, syncope, nausea, ataxia, dyspnea, dysphagia, and confusion.

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bromocriptine mesylate (brō´mōkrip´tēn mes´ilāt´),

n brand name: Parlodel;
drug class: dopamine receptor agonist, ovulation stimulant;
action: inhibits prolactin release by activating postsynaptic dopamine receptors;
uses: treatment of female infertility, Parkinson's disease, amenorrhea.

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bromocriptine mesylate

Alti-Bromocriptine (CA), Apo-Bromocriptine (CA), Parlodel

Pharmacologic class: Ergot-derivative dopamine agonist

Therapeutic class: Antiparkinsonian

Pregnancy risk category B

Action

Directly stimulates dopamine receptors in hypothalamus, causing release of prolactin-inhibitory factors and thereby relieving akinesia, rigidity, and tremors associated with Parkinson's disease. Also restores testicular or ovarian function and suppresses lactation.

Availability

Capsules: 5 mg

Tablets: 2.5 mg

⊘Indications and dosages

➣ Parkinson's disease

Adults: Initially, 1.25 mg P.O. b.i.d. Increase by 2.5 mg/day q 14 to 28 days depending on therapeutic response. Usual therapeutic dosage is 10 to 40 mg/day.

➣ Acromegaly

Adults: Initially, 1.25 to 2.5 mg/day P.O. for 3 days. Increase up to 1.25 to 2.5 mg/day q 3 to 7 days. Usual therapeutic dosage is 20 to 30 mg/day.

➣ Hyperprolactinemia

Adults: Initially, 1.25 to 2.5 mg/day P.O. Increase gradually q 3 to 7 days up to 2.5 mg two to three times daily.

➣ Neuroleptic malignant syndrome

Adults: Initially, 5 mg P.O. once daily. Increase up to 20 mg/day.

➣ Pituitary tumors

Adults: Initially, 1.25 mg P.O. b.i.d. to t.i.d. Adjust dosage gradually over several weeks to a maintenance dosage of 10 to 20 mg/day given in divided doses.

Contraindications

• Hypersensitivity to drug or other ergot derivatives
• Severe peripheral vascular disease
• Uncontrolled hypertension
• Breastfeeding

Precautions

Use cautiously in:
• impaired hepatic or cardiac function, renal disease, hypertension, pituitary tumor
• psychiatric disorders
• pregnant patients
• children younger than age 15.

Administration

• Give with meals or milk.
• If desired, give at bedtime to minimize dizziness and nausea.

Route	Onset	Peak	Duration
P.O.	2 hr	8 hr	24 hr

Adverse reactions

CNS: confusion, headache, dizziness, fatigue, delusions, nervousness, mania, insomnia, nightmares, seizures, cerebrovascular accident

CV: hypotension, palpitations, extrasystoles, arrhythmias, bradycardia, acute myocardial infarction

EENT: blurred vision, diplopia, burning sensation in eyes, nasal congestion

GI: nausea, vomiting, diarrhea, constipation, abdominal cramps, anorexia, dry mouth, GI hemorrhage

GU: urinary incontinence, polyuria, urinary retention

Musculoskeletal: leg cramps

Skin: urticaria, coolness and pallor of fingers and toes, rash on face and arms, alopecia

Other: metallic taste, digital vasospasm (in acromegaly use only)

Interactions

Drug-drug. Amitriptyline, estrogens, haloperidol, hormonal contraceptives, imipramine, loxapine, MAO inhibitors, phenothiazines, progestins, reserpine: interference with bromocriptine effects

Cyclosporine: inhibition of cyclosporine metabolism, leading to cyclosporine toxicity

Erythromycin: increased bromocriptine blood level and greater risk of adverse effects

Levodopa: additive effects of bromocriptine

Risperidone: increased prolactin blood level, interference with bromocriptine effects

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, blood urea nitrogen, creatine kinase, growth hormone, uric acid: increased levels

Drug-herbs. Chaste tree fruit: decreased bromocriptine effects

Drug-behaviors. Alcohol use: disulfiram-like reaction

Patient monitoring

• Monitor blood pressure to detect hypotension.
• When giving drug for hyperprolactinemia, monitor serum prolactin.
• When giving drug for acromegaly, monitor growth hormone levels to help guide dosage adjustment.
• In long-term use, monitor respiratory, hepatic, cardiovascular, and renal function.

Patient teaching

☞ Caution patient not to drink alcohol because of risk of severe reaction.
• Advise patient to have regular dental exams. Drug causes dry mouth, possibly resulting in caries and periodontal disorders.
• To minimize constipation, instruct patient to exercise regularly, increase dietary fiber intake, and drink plenty of fluids (3,000 ml daily).
• Advise patient who doesn't desire pregnancy to use reliable contraceptive, because drug may restore fertility.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.