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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.
An ergoline derivative which reduces pituitary prolactin secretion and size of pituitary tumours.
Hyperprolactinemia, pituitary tumours, amenorrhoea, female infertility, hypogonadism, acromegaly, Parkinson’s disease, neuroleptic malignant syndrome, type-2 diabetes.
Orthostatic hypotension, vomiting, vertigo, headaches, upset stomach, coronary vasospasm, pulmonary fibrosis, hepatotoxicity.
A dopamine D2-receptor inhibitor which inhibits T-cell-dependent induction of macrophage tumouricidal activity.