bromocriptine (Parlodel, Cycloset)
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Introduction
Tradename: Parlodel.
Indications
- treatment of idiopathic or post-encephalitic parkinsonism
- permits lower doses of Sinemet
- improves the side-effect profile (including dyskinesia)
- hyperprolactinemia
- ovulation induction in appropriately selected anovulatory women
- acromegaly
- type-2 diabetes (Cycloset)
- neuroleptic malignant syndrome[7]
Contraindications
Caution:
- avoid alcohol
- avoid exposure to cold
Dosage
Tabs: 2.5 & 5 mg, 0.8 mg (Cycloset)
Pharmacokinetics
- extensive 1st pass effect, only 6% of ingested drug reaches systemic circulation
- 1/2 life biphasic
- 4-4.5 hours for initial phase
- 45-50 hours for terminal phase
- onset of action:
- serum prolactin-lowering effect: 2 hours
- anti-parkinsonian effect: 30-90 minutes
- growth hormone-lowering effect: 1-2 hours
- duration of action
- serum prolactin-lowering effect: 24 hours
- growth hormone-lowering effect: 4-8 hours
elimination via liver
1/2life = 4-4.5 hours
1/2life = 45-50 hours
Adverse effects
- common with initial treatment & with doses > 20 mg/day
- postural hypotension
- dizziness
- neurologic
- psychosis - hallucinations
- confusion
- delusions
- depression
- dyskinesias
- drowsiness#
- GI effects
- nausea* & vomiting
- exacerbation of peptic ulcer disease
- constipation
- anorexia
- cardiovascular
- dry mouth
- metallic taste
- uncommon (< 1%)
# common with initiation of therapy
* most common side effect (68%)
- drug adverse effects of adrenergic receptor agonists
- drug adverse effects of dopaminergic receptor agonists
- drug adverse effects of sympathomimetic(s)
Drug interactions
- ergot alkaloids & MAO inhibitors: hypertension
- decreased alcohol tolerance
- excessive hypotension when used with antihypertensives
Mechanism of action
- prolactin inhibitor (inhibits release of prolactin from the anterior pituitary gland):
- direct action on the pituitary gland, or
- stimulating post-synaptic dopamine D2 receptors in the hypothalamus to induce prolaction inhibitory factor
- dopamine D2 receptor agonist
- stimulates dopamine receptors in the striatum to produce its therapeutic effects in parkinsonism
- may directly on dopamine D2 receptors in the ovary
- dopamine D1 receptor antagonist
More general terms
- ergot alkaloid
- dopaminergic receptor agonist
- pharmacologic agents for treatment of Parkinson's disease
- endocrine agent
Additional terms
- carbidopa/levodopa (Sinemet, Parcopa, Atamet)
- dopamine (Inotropin, Dopastat)
- dopamine receptor
- prolactin; lactogenic hormone (PRL)
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#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=270205&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 7.0 7.1 Deprecated Reference
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=31101
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=31100
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2443
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5284352
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=28693