PRAMIPEXOLE DIHYDROCHLORIDE

PRAMIPEXOLE DIHYDROCHLORIDE
(pra-mi-pex'ole)
Mirapex
Classifications: dopamine agonist; antiparkinson agent;
Therapeutic:antiparkinson agent

Prototype: Dopamine
Pregnancy Category: C

Availability

0.125 mg, 0.25 mg, 1 mg, 1.5 mg tablets

Action

Nonergot dopamine receptor agonist structurally similar to ropinirole for treatment of Parkinson's disease. Exhibits high affinity for the D2 subfamily of dopamine receptors in the brain and higher binding affinity to D3 than to D2 or D4 dopamine receptor subtypes.

Therapeutic Effect

Effectiveness is indicated by improved control of neuromuscular functioning.

Uses

Treatment of idiopathic Parkinson's disease and moderate to severe primary restless legs syndrome (RLS).

Contraindications

Hypersensitivity to pramipexole or ropinirole; lactation; pregnancy (category C).

Cautious Use

Renal and liver function impairment; concomitant use of CNS depressants. Safety and efficacy in children are not established.

Route & Dosage

Parkinson's Disease
Adult: PO Start with 0.125 mg t.i.d. x 1 wk, then 0.25 mg t.i.d. for 1 wk, continue to increase by 0.25 mg/dose t.i.d. qwk to a target dose of 1.5 mg t.i.d.

Restless Legs Syndrome
Adult: PO 0.125 mg taken 2–3 h before bed; dose can be increased every 4–7 d

Renal Impairment
Clcr 35–60 mL/min: same titration schedule dosed b.i.d. (max: 1.5 mg b.i.d.); 15–35 mL/min: same titration schedule dosed q.d. (max: 1.5 mg q.d.)

Administration

Oral
  • Titrate dose increments gradually with at least 4–7 d between increases.
  • Reduce doses for creatinine clearance >60 mL/min.
  • Give with food if nausea develops.

Adverse Effects (≥1%)

Body as a Whole: Asthenia, general edema, malaise, fever, decreased weight. CNS: Dizziness, somnolence, sudden sleep attacks, insomnia, hallucinations, dyskinesia, extrapyramidal syndrome, headache, confusion, amnesia, hypesthesia, dystonia, akathisia, myoclonus, peripheral edema. CV: Postural hypotension, chest pain. GI: Nausea, constipation, anorexia, dysphagia, dry mouth. Respiratory: Dyspnea, rhinitis. Urogenital: Decreased libido, impotence, urinary frequency or incontinence. Special Senses: Vision abnormalities.

Interactions

Drug: Cimetidine decreases clearance; butyrophenones, metoclopramide, phenothiazines may antagonize effects.

Pharmacokinetics

Absorption: Rapidly from GI tract, >90% bioavailability. Peak: 2 h. Distribution: 15% protein bound. Metabolism: Minimally in the liver. Elimination: Primarily in urine. Half-Life: 8–12 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor for S&S of orthostatic hypotension, especially when the dosage is increased.
  • Monitor cardiac status, especially in those with significant orthostatic hypotension.
  • Lab tests: Monitor BUN and creatinine periodically; monitor CPK with complaints of muscle pain.
  • Monitor for and report signs of tardive dyskinesia (see Appendix F).

Patient & Family Education

  • Hallucinations are an adverse effect of this drug and occur more often in older adults.
  • Make position changes slowly especially from a lying or sitting to standing.
  • Use caution with potentially dangerous activities until response to drug is known; drowsiness is a common adverse effect.
  • Avoid alcohol and use extra caution if taking other prescribed CNS depressants; both may exaggerate drowsiness, dizziness, and orthostatic hypotension.
  • Do not abruptly stop taking this drug. It should be discontinued over a period of 1 wk.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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