Names and pronunciation
(broe-moe-krip′teen) Cycloset, Parlodel
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Drug reference
(broe-moe-krip′teen) Cycloset, Parlodel
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Func. class.: Antiparkinson agent
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Chem. class.: Dopamine receptor agonist
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Do not confuse: Parlodel/pindolol/ bromocriptine/benztropine/brimonidine
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ACTION: Inhibits prolactin release by activating postsynaptic dopamine recep- tors; activation of striatal dopamine receptors may be reason for improve- ment in Parkinson’s disease
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USES: Parkinson’s disease, amenor- rhea/galactorrhea caused by hyperprolac- tinemia, infertility, acromegaly, pituitary adenomas, adjunct for type 2 diabetes
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Unlabeled uses: Neuroleptic malignant syndrome, mastalgia
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CONTRAINDICATIONS: Basilar migraine, hemiplegic migraine, breast- feeding, uncontrolled hypertension, severe peripheral vascular disease; hypersensitiv- ity to ergot, bromocriptine; preeclampsia/ eclampsia Precautions: Pregnancy, breastfeeding, children, renal/hepatic disease, pituitary tumors, peptic ulcer disease, sulfite hyper- sensitivity, pulmonary fibrosis, dementia, GI bleeding, bipolar disorder, abrupt discontinuation, acute MI, angina, type 1 diabetes mellitus
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SIDE EFFECTS CNS: Headache, depression, restlessness, anxiety, nervousness, confusion, seizures, hallucinations, dizziness, fatigue, drowsi- ness, abnormal involuntary movements, psychosis, weakness CV: Orthostatic hypotension, decreased B/P, palpitations, extrasystole, shock, dys- rhythmias, bradycardia, MI EENT: Blurred vision, diplopia, burning eyes, nasal congestion GI: Nausea, vomiting, anorexia, cramps, constipation, diarrhea, dry mouth, GI hemorrhage GU: Frequency, retention, incontinence, diuresis INTEG: Rash on face, arms; alopecia; coolness, pallor of fingers, toes; periph- eral edema META: Hypoglycemia
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INTERACTIONS • Disulfiram-like reaction: alcohol Increase: action of antihypertensives, levodopa, chloramphenicol, probenecid, salicylates, sulfonamides; dose of both products may need to be adjusted Decrease: action of bromocriptine— phenothiazines, oral contraceptives, progestins, estrogens, haloperidol, lox- apine, methyldopa, metoclopramide, MAOIs, reserpine; dose may need to be decreased Decrease/increase: effect of Cycloset— CYP3A4 inhibitors/inducers; use cautiously Decrease: effect of Cycloset—butyrophe- nones, metoclopramide, phenothiazine, thioxanthenes; avoid concurrent use Drug/Lab Test Increase: growth hormone, AST, ALT, CK, BUN, uric acid, alkaline phosphatase
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DOSAGE AND ROUTES Parkinson’s disease (not Cycloset) • Adult: PO 1.25 mg bid with meals; may increase q2-4wk by 2.5 mg/day, max 100 mg/day; levodopa should be continued while bromocriptine is being instituted Amenorrhea/galactorrhea from hyperprolactinemia; hypogonadism, infertility (not Cycloset) • Adult, adolescent ≥16 yr: PO 1.25-2.5 mg with meals; may increase by 2.5 mg q3-7days, usual range 2.5-15 mg/day, max 30 mg/day • Child 11-15 yr: PO 1.25-2.5 mg daily Acromegaly (not Cycloset) • Adult: PO 1.25-2.5 mg at bedtime; may increase by 1.25-2.5 mg q3-7days; usual range 20-30 mg/day, max 100 mg/ day Pituitary adenoma (not Cycloset) • Adult/adolescent ≥16 yr: PO 1.25 mg bid-tid; may increase over several weeks to 10-20 mg/day Type 2 diabetes (Cycloset only) • Adult: PO (initially) 0.8 mg daily in AM within 2 hr of waking; titrate by 0.8 mg/day no more than weekly to max 1.6-4.8 mg/day • CYP3A4 inhibitors: max 1.6 mg daily if used with moderate inhibitors
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Available forms: Capsules 5 mg; tablets 2.5 mg (Parodel), 0.8 mg (Cycloset)
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Administer: • With meal to prevent GI symptoms; Cycloset: give with food in AM within 2 hr of waking • At bedtime so dizziness, orthostatic hypotension do not occur • Store at room temperature in tight, light-resistant container
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Assess: • B/P; establish baseline, compare with other readings; this product decreases B/P and causes orthostatic hypotension; obtain chest x-ray baseline • Monitor for reactions that usually occur at start of treatment (nausea, dizziness, orthostatic hypotension) • Parkinson’s symptoms: pill rolling, shuffling gait, restlessness, tremors, pos- tural instability before and during treat- ment • Neuroleptic malignant syndrome: decrease in temperature and sweating, lower pulse rate, and lessening of sei- zures indicate resolution of symptoms • Change in size of soft tissue volume with acromegaly • CNS symptoms: CNS depression, hal- lucinations, vertigo; report symptoms im- mediately • Pregnancy: fertility may occur before onset of menses after pregnancy; use pregnancy testing q4wk or if menstrua- tion does not occur, use alternative con- traceptive methods other than oral con- traceptives/subdermal implants during treatment; do not use in breastfeeding
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Evaluate: • Therapeutic response (Parkinson’s disease): decreased dyskinesia, drooling, spasm, rigidity
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That tablets may be crushed, mixed with food; Cycloset to be taken within 2 hr of rising; that 8 wk are needed for full effect • To change position slowly to prevent orthostatic hypotension • To use contraceptives during treat- ment with this product; that pregnancy may occur; to use methods other than oral contraceptives/subdermal implants • That therapeutic effect for Parkinson’s disease may take 2 mo, titrate slowly • To avoid hazardous activity if dizziness occurs • To report symptoms of MI immediately • To take with food, avoid alcohol
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PHARMACOKINETICS Onset 2 hr, peak 1-3 hr, duration 4-8 hr, 90%-96% protein bound, half-life 3 hr, metabolized by liver (inactive metabo- lites), 85%-98% excreted in feces, >90% undergoes first-pass metabolism
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• Adult, adolescent ≥16 yr: PO 1.25-2.5 mg with meals; may increase by 2.5 mg q3-7days, usual range 2.5-15 mg/day, max 30 mg/day
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• Adult/adolescent ≥16 yr: PO 1.25 mg bid-tid; may increase over several weeks to 10-20 mg/day Type 2 diabetes (Cycloset only)
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