bromocriptine (Cycloset, Parlodel)
Classes: Hyperprolactinemia; Antiparkinson Agents, Dopamine Agonists; Metabolic & Endocrine, Other
Dosing and uses of Cycloset, Parlodel (bromocriptine)
Adult dosage forms and strengths
capsule
- 5mg
tablet
- 0.8mg
- 2.5mg
Hyperprolactinemia (Parlodel)
Initial: 1.25-2.5 mg PO qDay
May increase by 2.5 mg/day q2-7Days
Usual therapeutic dosage 5-7.5 mg/day, ranges from 2.5-15 mg/day
Up to 30 mg/day has been used in some patients with amenorrhea &/or galactorrhea
Parkinson Disease (Parlodel)
1.25 mg PO q12hr
May increase dose by 2.5 mg/day q2-4Weeks
Safety >100 mg/day not established
Acromegaly (Parlodel)
1.25-2.5 mg PO qHS for 3 days
May increase by 1.25-2.5 mg/day at q3-7Days
Not to exceed 100 mg/day
Diabetes (Cycloset)
Quick release formulation (Cycloset) is the only bromocriptine product indicated for diabetes mellitus type 2 as adjunct to diet and exercise to improve glycemic controL
Initial dose: 1 tablet (0.8 mg) PO qDay increased weekly by 1 tablet until maximal tolerated daily dose of 1.6-4.8 mg is achieved
Take within 2 hours after waking in the morning with food
Note: Cycloset is not indicated for hyperprolactinemia, Parkinson disease, or acromegaly
Neuroleptic Malignant Syndrome (Off-label)
2.5-5 mg PO 2-3 times/day; not to exceed 45 mg/day
Administration: take with food
Hepatic Impairment
Dose adjustment may be necessary; there are no guidelines
Dosing Considerations
Not for treatment of type 1 diabetes or diabetic ketoacidosis
Limited efficacy data in combination with thiazolidinediones
Efficacy has not been confirmed in combination with insulin
Pediatric dosage forms and strengths
capsule
- 5mg
tablet
- 2.5mg
Hyperprolactinemia (Parlodel)
11-15 years: 1.25-2.5 mg PO qDay (initially)
Maintenance: 2.5-10 mg/day
Take with food
Geriatric dosage forms and strengths
Hyperprolactinemia (Parlodel)
Initial: 1.25-2.5 mg PO qDay
May increase by 2.5 mg/day q2-7Days
Usual therapeutic dosage 5-7.5 mg/day, ranges from 2.5-15 mg/day
Up to 30 mg/day has been used in some patients with amenorrhea &/or galactorrhea
Parkinson disease (Parlodel)
1.25 mg PO q12hr
May increase dose by 2.5 mg/day q2-4Weeks
Safety >100 mg/day not established
Acromegaly (Parlodel)
1.25-2.5 mg PO qHS for 3 days
May increase by 1.25-2.5 mg/day at q3-7Days
Not to exceed 100 mg/day
Diabetes (Cycloset)
Quick release formulation (Cycloset) is the only bromocriptine product indicated for diabetes mellitus type 2 as adjunct to diet and exercise to improve glycemic controL
Initial dose: 1 tablet (0.8 mg) PO qDay increased weekly by 1 tablet until maximal tolerated daily dose of 1.6-4.8 mg is achieved
Take within 2 hours after waking in the morning with food
Note: Cycloset is not indicated for hyperprolactinemia, Parkinson disease, or acromegaly
Neuroleptic malignant syndrome (Off-label)
2.5-5 mg PO 2-3 times/day; not to exceed 45 mg/day
Administration: take with food
Cycloset, Parlodel (bromocriptine) adverse (side) effects
>10%
Nausea (49%)
Hypotension (30%)
Headache (19%)
Dizziness (17%)
1-10%
Abdominal cramps
Anorexia
Constipation
Dyspepsia
Dysphagia
Epigastric pain
GI hemorrhage
Vomiting
Drowsiness
Fatigue
Faintness
Hallucinations VisuaL
Insomnia
Lightheadedness
Nighmares
Paranoia
Psychosis
Seizure
Vertigo
Arrhythmias
Bradycardia
Hypertension
MI
Mottled skin
Orthostasis
Vasospasm
Palpitations
Pericardial effusions
Raynaud's syndrome exacertabtion
Syncope
Blepharospasm
BUN increased
Burning discomfort of the eye
Diplopia
Facial pallor
Leg cramps
Nasal congestion
Rash
Urticaria
Warnings
Contraindications
Sensitivity to ergot alkaloids
Uncontrolled hypertension
Toxemia
Nursing
Cycloset: type I DM, DKA, patients with syncopal migraine
Cautions
Monitor blood pressure: risk of orthostatic hypotension
Concurrency with other hypotensive drugs concomitantly
Hepatic/renal impairment
In patients undergoing treatment for macroadenoma-related hyperprolactinemia or who have undergone transsphenoidal surgery, a persistent watery nasal discharge may be sign of CSF rhinorrhea
May impair ability to drive/operate heavy machinery
History of MI and a residual atrial, nodal or ventricular arrhythmia, especially with Parkinson disease
Use for prevention of postpartum lactation no longer recommended
Postmarketing reports suggest that patients treated with anti-Parkinson medications can experience intense urges to gamble, increased sexual urges, intense urges to spend money uncontrollably, and other intense urges
Epidemiological studies have shown that patients with Parkinson’s disease have a higher risk (2 to 6-fold higher) of developing melanoma than the general population (unsure if related to the disease or drug therapy)
Avoid abrupt withdrawal (associated with neuroleptic malignant syndrome-like symptoms); discontinue gradually
Concomitant use with other receptor agonists not recommended
Conclusive evidence of macrovascular risk reduction with bromocriptine or other antidiabetic agents not demonstrated
Increased risk for abnormal valvular regurgitation possibly due to excess serotonin activity leading to valve thickening and stiffening
Pregnancy and lactation
Pregnancy category: B
Lactation: should not be used during lactation
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Cycloset, Parlodel (bromocriptine)
Mechanism of action
Semisynthetic ergot alkaloid, dopamine receptor agonist, inhibits prolactin secretion, and lowers blood levels of growth hormone in acromegaly
Quick-release formulation of bromocriptine (Cycloset) is thought to act on circadian neuronal activities within the hypothalamus to reset abnormally elevated hypothalamic drive for increased plasma glucose, triglyceride, and free fatty acid levels in fasting and postprandial states in patients with insulin-resistant
Pharmacokinetics
Half-life elimination: 4-4.5 hr (initial phase); 8-20 hr (terminal phase)
Excretion: 85% feces (via biliary elimination); urine (2.5-5.5%)
Protein bound: 90-96% (to albumin)
Peak plasma time: 1-3 hr
Vd: 61L
Absorption: 28% from GI tract
Bioavailability: 28% (parlodel); 65-95% (cycloset)
Metabolism: Completely in liver, principally by hydrolysis of the amide bond to produce lysergic acid and a peptide fragment
