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Pergolide
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Monitoring Parameters
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(PER go lide)

U.S. Brand Names
Permax®

Generic Available

No


Synonyms
Pergolide Mesylate

Pharmacological Index

Anti-Parkinson's Agent (Dopamine Agonist); Ergot Derivative


Use

Adjunctive treatment to levodopa/carbidopa in the management of Parkinson's disease


Pregnancy Risk Factor

B


Contraindications

Hypersensitivity to pergolide mesylate or other ergot derivatives


Warnings/Precautions

Symptomatic hypotension occurs in 10% of patients; use with caution in patients with a history of cardiac arrhythmias, hallucinations, or mental illness


Adverse Reactions

>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


Overdosage/Toxicology

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.


Drug Interactions

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


Mechanism of Action

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.


Pharmacodynamics/Kinetics

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


Usual Dosage

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.


Monitoring Parameters

Blood pressure (both sitting/supine and standing), symptoms of parkinsonism, dyskinesias, mental status


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

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


Patient Information

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.


Nursing Implications

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


Dosage Forms

Tablet, as mesylate: 0.05 mg, 0.25 mg, 1 mg


References

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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