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Pronunciation |
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(PER
go
lide) |
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U.S. Brand
Names |
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Permax® |
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Generic
Available |
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No |
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Synonyms |
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Pergolide Mesylate |
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Pharmacological Index |
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Anti-Parkinson's Agent (Dopamine Agonist); Ergot Derivative |
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Use |
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Adjunctive treatment to levodopa/carbidopa in the management of Parkinson's
disease |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to pergolide mesylate or other ergot
derivatives |
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Warnings/Precautions |
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Symptomatic hypotension occurs in 10% of patients; use with caution in
patients with a history of cardiac arrhythmias, hallucinations, or mental
illness |
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Adverse
Reactions |
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>10%:
Central nervous system: Dizziness, somnolence, confusion, hallucinations,
dystonia
Gastrointestinal: Nausea, constipation
Neuromuscular & skeletal: Dyskinesia
Respiratory: Rhinitis
1% to 10%:
Cardiovascular: Myocardial infarction, postural hypotension, syncope,
arrhythmias, peripheral edema, vasodilation, palpitations, chest pain,
hypertension
Central nervous system: Chills, insomnia, anxiety, psychosis, EPS,
incoordination
Dermatologic: Rash
Gastrointestinal: Diarrhea, abdominal pain, xerostomia, anorexia, weight
gain, dyspepsia, taste perversion
Hematologic: Anemia
Neuromuscular & skeletal: Weakness, myalgia, tremor, NMS (with rapid dose
reduction), pain
Ocular: Abnormal vision, diplopia
Respiratory: Dyspnea, epistaxis
Miscellaneous: Flu syndrome, hiccups |
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Overdosage/Toxicology |
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Symptoms of overdose include vomiting, hypotension, agitation,
hallucinations, ventricular extrasystoles, possible seizures; data on overdose
is limited
Treatment is supportive and may require antiarrhythmias and/or neuroleptics
for agitation; hypotension, when unresponsive to I.V. fluids or Trendelenburg
positioning, often responds to norepinephrine infusions started at 0.1-0.2
mcg/kg/minute followed by a titrated infusion. If signs of CNS stimulation are
present, a neuroleptic may be indicated; antiarrhythmics may be indicated,
monitor EKG; activated charcoal is useful to prevent further absorption and to
hasten elimination. |
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Drug
Interactions |
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Use caution with other highly plasma protein bound drugs
Dopamine antagonists (ie, antipsychotics, metoclopramide) may diminish the
effects of pergolide; these combinations should generally be avoided
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Mechanism of
Action |
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Pergolide is a semisynthetic ergot alkaloid similar to bromocriptine but
stated to be more potent (10-1000 times) and longer-acting; it is a
centrally-active dopamine agonist stimulating both D1 and
D2 receptors. Pergolide is believed to exert its therapeutic effect
by directly stimulating postsynaptic dopamine receptors in the nigrostriatal
system. |
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Pharmacodynamics/Kinetics |
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Absorption: Oral: Well absorbed
Protein binding: Plasma 90%
Metabolism: Extensive in the liver (on first-pass)
Half-life: 27 hours
Elimination: ~50% excreted in urine and 50% in feces |
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Usual Dosage |
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When adding pergolide to levodopa/carbidopa, the dose of the latter can
usually and should be decreased. Patients no longer responsive to bromocriptine
may benefit by being switched to pergolide. |
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Monitoring
Parameters |
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Blood pressure (both sitting/supine and standing), symptoms of parkinsonism,
dyskinesias, mental status |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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Pergolide may decrease or inhibit salivary flow; normal salivary flow will
resume with cessation of drug therapy; prolonged salivary reduction could
enhance development of periodontal disease, oral candidiasis and
discomfort |
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Patient
Information |
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Take exactly as directed (may be prescribed in conjunction with
levodopa/carbidopa); do not change dosage or discontinue without consulting
prescriber. Therapeutic effects may take several weeks or months to achieve and
you may need frequent monitoring during first weeks of therapy. Take with meals
if GI upset occurs, before meals if dry mouth occurs, after eating if drooling
or if nausea occurs. Take at the same time each day. Maintain adequate hydration
(2-3 L/day of fluids unless instructed to restrict fluid intake); void before
taking medication. Do not use alcohol and prescription or OTC sedatives or CNS
depressants without consulting prescriber. You may experience drowsiness,
dizziness, confusion, or vision changes (use caution when driving, climbing
stairs, or engaging in tasks requiring alertness until response to drug is
known); orthostatic hypotension (use caution when changing position - rising to
standing from sitting or lying); constipation (increased exercise, fluids, or
dietary fruit and fiber may help); runny nose or flu-like symptoms (consult
prescriber for appropriate relief); nausea, vomiting, loss of appetite, or
stomach discomfort (small frequent meals, frequent mouth care, chewing gum, or
sucking lozenges may help); photosensitivity (use sunscreen, wear protective
clothing and eyewear, and avoid direct sunlight). Report unresolved constipation
or vomiting; chest pain, palpitations, irregular heartbeat; ringing in ears; CNS
changes (hallucination, loss of memory, seizures, acute headache, nervousness,
etc); painful or difficult urination; increased muscle spasticity, rigidity, or
involuntary movements; skin rash; or significant worsening of condition.
Breast-feeding precautions: Breast-feeding is not
recommended. |
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Nursing
Implications |
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Monitor closely for orthostasis and other adverse effects; raise bed rails
and institute safety measures; aid patient with ambulation, may cause postural
hypotension and drowsiness |
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Dosage Forms |
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Tablet, as mesylate: 0.05 mg, 0.25 mg, 1 mg |
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References |
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Collier DS, Berg MJ, and Fincham RW,
"Parkinsonism Treatment: Part III - Update," Ann Pharmacother, 1992,
26(2):227-33.
Koller WC, Silver DE, and Lieberman A,
"An Algorithm for the Management of Parkinson's Disease," Neurology,
1994, 44(12 Suppl 10):S1-52.
Staedt J, Wassmuth F, Ziemann U, et al,
"Pergolide: Treatment of Choice in Restless Legs Syndrome (RLS) and Nocturnal Myoclonus Syndrome (NMS): A Double-Blind Randomized Crossover Trial of Pergolide Versus L-Dopa,"
J Neural Transm, 1997, 104(4-5):961-8.
Stern MB,
"Contemporary Approaches to the Pharmacotherapeutic Management of Parkinson's Disease: An Overview,"
Neurology, 1997, 49(1 Suppl 1):S2-9.
Watts RL, "The Role of Dopamine Agonists in Early Parkinson's Disease,"
Neurology, 1997, 49(1 Suppl 1):S34-48.
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