pergolide (Permax, pergolidum)
Jump to navigation
Jump to search
Introduction
Withdrawn from US Market 2007
Tradename: Permax.
Indications
- symptomatic treatment of Parkinson's disease
- adjunctive treatment to L-dopa/carbidopa
- used to permit a reduction in dosage of Sinemet with improvement of side-effect profile
Dosage
- start 0.05 mg PO QD
- increase by 0.1-0.15 mg every 3rd day over 12 days to 1 mg PO TID
- max 5 mg/day (no added benefit of higher doses)
Tabs: 0.05, 0.25, 1 mg
Pharmacokinetics
- 90% of drug is protein-bound
- at least 10 metabolites are known; it is not known if any of them are active
- eliminated in the urine
elimination via kidney
Adverse effects
- high incidence of syncope & orthostatic hypotension upon initiation of therapy
- common (> 10%)
- less common (1-10%)
- diarrhea, abdominal pain, asthenia, chest pain, flu-like syndrome, chills, vasodilation, palpitations, arrhythmias, vomiting, dry mouth, anorexia, dyspnea, peripheral edema, weight gain, insomnia, abnormal vision
- valvular heart disease
- mitral regurgitation (RR = 6.3)
- aortic regurgitation (RR = 4.2)[6]
- withdrawn from US Market 2007[7]
- drug adverse effects of adrenergic receptor agonists
- drug adverse effects of dopaminergic receptor agonists
- drug adverse effects of sympathomimetic(s)
Drug interactions
- dopamine antagonists, methyldopa, reserpine, metoclopramide may diminish the effectiveness of pergolide
- meperidine in combination may cause lethal seizures
Mechanism of action
- mixed dopamine D1 & D2 receptor agonist
- directly stimulate post-synaptic dopamine receptors in the nigrostriatal system
- 5-HT2B receptor agonist
More general terms
References
- ↑ 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
- ↑ Bronstein J, In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 29-Oct 2, 2004
- ↑ 6.0 6.1 Schade R et al, Dopamine agonists and the risk of cardiac-valve regurgitation. N Engl J Med 2007 Jan 4; 356:29-38
Zanettini R et al, Valvular heart disease during treatment with dopamine agonists for Parkinson's disease. N Engl J Med 2007 Jan 4; 356:39-46 PMID: https://www.ncbi.nlm.nih.gov/pubmed/17202454
Roth BL. Drugs and valvular heart disease. N Engl J Med 2007 Jan 4; 356:6-9 PMID: https://www.ncbi.nlm.nih.gov/pubmed/17202450
Prescriber's Letter 14(2): 2007 Drug-induced heart valve dysfunction Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230206&pb=PRL (subscription needed) http://www.prescribersletter.com - ↑ 7.0 7.1 FDA MedWatch http://www.fda.gov/medwatch/safety/2007/safety07.htm#Pergolide