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bromocriptine (Parlodel, Cycloset)
Tradename: Parlodel.
Indications:
1) treatment of idiopathic or post-encephalitic parkinsonism
a) permits lower doses of Sinemet
b) improves the side-effect profile (including dyskinesia)
2) hyperprolactinemia
a) amenorrhea
b) hypogonadism
c) infertility
3) ovulation induction in appropriately selected anovulatory women
4) acromegaly
5) type-2 diabetes (Cycloset)
6) neuroleptic malignant syndrome [7]
Contraindications: Caution:
1) avoid alcohol
2) avoid exposure to cold
Dosage:
1) start 1.25 mg PO BID with meals
2) max 40 mg/day
3) take with milk or food
Tabs: 2.5 & 5 mg, 0.8 mg (Cycloset)
Pharmacokinetics:
1) extensive 1st pass effect, only 6% of ingested drug reaches systemic circulation
2) 1/2 life biphasic
a) 4-4.5 hours for initial phase
b) 45-50 hours for terminal phase
3) onset of action:
a) serum prolactin-lowering effect: 2 hours
b) anti-parkinsonian effect: 30-90 minutes
c) growth hormone-lowering effect: 1-2 hours
4) duration of action
a) serum prolactin-lowering effect: 24 hours
b) growth hormone-lowering effect: 4-8 hours
Adverse effects:
1) common with initial treatment & with doses > 20 mg/day
2) postural hypotension
3) dizziness
4) neurologic
a) psychosis - hallucinations
b) confusion
c) delusions
d) depression
e) dyskinesias
f) drowsiness#
5) GI effects
a) nausea* & vomiting
b) exacerbation of peptic ulcer disease
c) constipation
d) anorexia
6) cardiovascular
a) erythromelagia
b) leg cramps
c) Raynaud's phenomenon
d) syncope
7) dry mouth
8) metallic taste
9) uncommon (< 1%)
- hypertension, fatigue, insomnia, headache, abdominal cramps, myocardial infarction, seizures
# common with initiation of therapy
* most common side effect (68%)
Drug interactions:
1) ergot alkaloids & MAO inhibitors: hypertension
2) decreased alcohol tolerance
3) excessive hypotension when used with antihypertensives
Mechanism of action:
1) prolactin inhibitor (inhibits release of prolactin from the anterior pituitary gland):
a) direct action on the pituitary gland, or
b) stimulating post-synaptic dopamine D2 receptors in the hypothalamus to induce prolaction inhibitory factor
2) dopamine D2 receptor agonist
a) stimulates dopamine receptors in the striatum to produce its therapeutic effects in parkinsonism
b) may directly on dopamine D2 receptors in the ovary
3) dopamine D1 receptor antagonist
Interactions
drug interactions
drug adverse effects (more general classes)
Related
carbidopa/levodopa (Sinemet, Parcopa, Atamet, Crexont)
dopamine (Inotropin, Dopastat)
dopamine receptor
prolactin; lactogenic hormone (PRL)
General
dopaminergic receptor agonist
endocrine agent
ergot alkaloid
pharmacologic agents for treatment of Parkinson's disease
Properties
AGONIST-FOR: adrenergic receptor
MISC-INFO: elimination route LIVER
1/2life 4-4.5 HOURS
45-50 HOURS
pregnancy-category -
safety in lactation -
Database Correlations
PUBCHEM correlations
References
- Goodman and Gilman's The Pharmacological Basis of
Therapeutics, 8th ed. Gilman et al, eds.
Permagon Press/McGraw Hill, 1990
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Saunders Manual of Medical Practice, Rakel (ed),
WB Saunders, Philadelphia, 1996, pg 1051
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Prescriber's Letter 18(2): 2011
COMMENTARY: Cycloset: A New Bromocriptine Formulation for
Diabetes
CHART: Drug Classes for Type 2 Diabetes
Detail-Document#: 270205
(subscription needed) http://www.prescribersletter.com
- Deprecated Reference