pramipexole MIRAPEX

Class: Dopamine Agonist
FDA Indications: Parkinson's Disease, Restless Legs Syndrome
Off-Label Use: Fibromyalgia, SSRI-induced Sexual Dysfunction, Treatment-resistant Depression, Bipolar Depression
Prescribing
Forms: 0.125, 0.25, 0.5, 0.75, 1, 1.5mg tablet; 0.375, 0.75, 1.5, 2.25, 3, 3.75, 4.5mg extended-release tablet
Dose Range: 0.125-5 mg/day
Starting: Parkinson Disease: 0.125 mg tid, ↑ gradually Q5-7 days; maintenance: 0.5-1.5 mg tid
RLS: 0.125 mg qd 2-3° before bedtime; dose may be doubled Q 4-7 days up to 0.5 mg
Bipolar depression: 0.125 mg bid to tid; ↑ gradually by 0.125-0.25 mg Q 3-7 days to a target range of 1-3 mg/day in divided doses
Stopping: Worsening of symptoms may occur with abrupt discontinuation; a gradual dose reduction every 4 to 7 days has been recommended

NAMI drug fact sheet

Precautions
Side Effects: headache, dizziness, confusion, weakness/asthenia, constipation, xerostomia, nausea, insomnia, abnormal dreams, orthostatic hypotension, somnambulism, EPS, edema, drowsiness, hallucinations, impulse control disorder, sleep attacks (rare)
Pharmacodynamics
1° MOA: Dopamine receptor agonism (D3 > D2). Activity at striatal D2 confers anti-parkinson effects; activity at mesolimbic D3 receptors theorized to be responsible for motoric and hedonic deficits in depression
Target: Agonism at D2, D3, and D4
Pharmacokinetics
t½: 8.8° TMAX:
Substrate of: Renally cleared
Inhibits: ∅ ; Induces:
Active Metabolites:
DDIs
  • - may diminish the therapeutic effect of antipsychotic agents
  • - caution when prescribed with blood pressure lowering agents
  • - caution when co-prescribed with CNS depressants; co-administered stimulants may enhance the adverse/toxic effect of anti-parkinson agents
Misc
  • - There are 2 small studies (n ≈ 20 in both) supporting off-label use for treatment of bipolar depression
  • - There is some evidence supporting use for anhedonic treatment-refractory patients (n ≈ 42, combination of MDD and bipolar patients)
Special Populations

Category —Adverse events were observed in animal reproduction studies. Information related to the use of pramipexole for the treatment of Parkinson disease or RLS in pregnant women is limited. Current guidelines note that the available information is insufficient to make a recommendation for the treatment of RLS in pregnant women.

No reports describing the use of pramipexole during human lactation have been located. Its molecular weight and low protein binding (about 15%) suggest that it will be excreted into breast milk. The effect of this exposure on a nursing infant is unknown, but pramipexole inhibits prolactin secretion and may inhibit lactation.

The half-life increases approximately 40% and clearance decreases approximately 30% in patients 65 years and older mostly because of reduced renal function with age.

Clearance is 75% lower with severe impairment (CrCl ~20 mL/min) and approximately 60% lower with moderate impairment (CrCl ~40 mL/min)

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Last updated December 05 2018 19:19:12. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.