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Pharmacologic class: Ergot-derivative dopamine agonist
Therapeutic class: Antiparkinsonian
Pregnancy risk category B
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. Cycloset's action in glycemic control is unknown.
Capsules: 5 mg
Tablets: 0.8 mg, 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.
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; not to exceed 100 mg/day.
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.
➣ Type 2 diabetes mellitus
Adults: Initially, 0.8 mg P.O. daily within 2 hours of awakening; may increase by one tablet (0.8 mg) weekly until target range (1.6 to 4.8 mg) or maximal tolerance is reached.
• Hypersensitivity to drug, its components, or other ergot-related drugs
• Severe peripheral vascular disease
• Uncontrolled hypertension, syncopal migraines
Use cautiously in:
• impaired hepatic or cardiac function, renal disease, hypertension, pituitary tumor
• psychiatric disorders
• galactose intolerance, severe lactose deficiency, glucose-galactose malabsorption (use not recommended)
• Concomitant use with anti-hypertensives
• Concomitant use with dopamine antagonists such as neuroleptic agents (use not recommended)
• pregnant patients
• children younger than age 15.
• Give with meals or milk.
• If desired, give at bedtime to minimize dizziness and nausea.
• For Cycloset, administer within 2 hours of patient's waking in the morning and with food.
CNS: asthenia, confusion, headache, dizziness, fatigue, delusions, nervousness, mania, insomnia, nightmares, seizures, cerebrovascular accident
CV: hypotension, palpitations, extrasystoles, syncope, arrhythmias, bradycardia, acute myocardial infarction
EENT: blurred vision, diplopia, burning sensation in eyes, amblyopia, rhinitis, sinusitis, nasal congestion
GI: dyspepsia, 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), infection
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
Dopamine receptor antagonists (such as neuroleptics [including phenothiazines, butyrophenones, thioxanthenes]), metoclopramide: diminished effectiveness of Cycloset and these drugs
Ergot-related drugs: increased ergotrelated adverse reactions, such as nausea, vomiting, and fatigue; decreased effectiveness of these drugs
Erythromycin: increased bromocriptine blood level and greater risk of adverse effects
Levodopa: additive effects of bromocriptine
Potent CYP3A4 inhibitors or inducers, substrates of CYP3A4 (such as azole antimycotics, HIV protease inhibitors): increased or decreased Cycloset circulating levels
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
• 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.
• When giving drug for diabetes mellitus, monitor blood glucose and hemoglobin A1C levels.
• In long-term use, monitor respiratory, hepatic, cardiovascular, and renal function.
• Instruct patient to take Cycloset within 2 hours of waking in the morning and with food.
☞ 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.
bromocriptine mesylate (brō´mōkrip´tēn mes´ilāt´),
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.