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Pronunciation:

(pra mi PEKS ole)

U.S. Brand Names:

Mirapex®

Generic Available:

Canadian Brand Names:

Mirapex®

Use:

Treatment of the signs and symptoms of idiopathic Parkinson's disease

Use - Unlabeled/Investigational:

Treatment of depression

Pregnancy Risk Factor:

Pregnancy Implications:

Early embryonic loss and postnatal growth inhibition were observed in animal studies. There are no adequate and well-controlled studies in pregnant women.

Lactation:

Excretion in breast milk unknown/not recommended

Contraindications:

Hypersensitivity to pramipexole or any component of the formulation

Warnings/Precautions:

Caution should be taken in patients with renal insufficiency and in patients with pre-existing dyskinesias. May cause orthostatic hypotension; Parkinson's disease patients appear to have an impaired capacity to respond to a postural challenge. Use with caution in patients at risk of hypotension (such as those receiving antihypertensive drugs) or where transient hypotensive episodes would be poorly tolerated (cardiovascular disease or cerebrovascular disease). Parkinson's patients being treated with dopaminergic agonists ordinarily require careful monitoring for signs and symptoms of postural hypotension, especially during dose escalation, and should be informed of this risk. May cause hallucinations, particularly in older patients. Pathologic degenerative changes were observed in the retinas of albino rats during studies with this agent, but were not observed in the retinas of pigmented rats or in other species. The significance of these data for humans remains uncertain.

Although not reported for pramipexole, other dopaminergic agents have been associated with a syndrome resembling neuroleptic malignant syndrome on withdrawal or significant dosage reduction after long-term use. Dopaminergic agents from the ergot class have also been associated with fibrotic complications, such as retroperitoneum, lungs, and pleura.

Pramipexole has been associated with somnolence, particularly at higher dosages (>1.5 mg/day). In addition, patients have been reported to fall asleep during activities of daily living, including driving, while taking this medication. Whether these patients exhibited somnolence prior to these events is not clear. Patients should be advised of this issue and factors which may increase risk (sleep disorders, other sedating medications, or concomitant medications which increase pramipexole concentrations) and instructed to report daytime somnolence or sleepiness to the prescriber. Patients should use caution in performing activities which require alertness (driving or operating machinery), and to avoid other medications which may cause CNS depression, including ethanol.

Adverse Reactions:

>10%:

Cardiovascular: Postural hypotension

Central nervous system: Asthenia, dizziness, somnolence, insomnia, hallucinations, abnormal dreams

Gastrointestinal: Nausea, constipation

Neuromuscular & skeletal: Weakness, dyskinesia, EPS

1% to 10%:

Cardiovascular: Edema, syncope, tachycardia, chest pain

Central nervous system: Malaise, confusion, amnesia, dystonias, akathisia, thinking abnormalities, myoclonus, hyperesthesia, paranoia, fever

Endocrine & metabolic: Decreased libido

Gastrointestinal: Anorexia, weight loss, xerostomia, dysphagia

Genitourinary: Urinary frequency, impotence, urinary incontinence

Neuromuscular & skeletal: Muscle twitching, leg cramps, arthritis, bursitis, myasthenia, gait abnormalities, hypertonia

Ocular: Vision abnormalities

Respiratory: Dyspnea, rhinitis

<1%: Liver transaminases increased

Postmarketing and/or case reports: Rhabdomyolysis

Frequency not defined, dose related: Falling asleep during activities of daily living

Drug Interactions:

Antipsychotics: May decrease the efficiency of pramipexole due to dopamine antagonism

Cationic drugs: Drugs secreted by the cationic transport system (diltiazem, triamterene, verapamil, quinidine, quinine, ranitidine) decrease the clearance of pramipexole by ~20%

Cimetidine: May increase serum concentrations; cimetidine in combination with pramipexole produced a 50% increase in AUC and a 40% increase in half-life

Metoclopramide: May decrease the efficiency of pramipexole due to dopamine antagonism

Ethanol/Nutrition/Herb Interactions:

Ethanol: Avoid ethanol (may increase CNS depression).

Food: Food intake does not affect the extent of drug absorption, although the time to maximal plasma concentration is delayed by 60 minutes when taken with a meal.

Herb/Nutraceutical: Avoid valerian, St John's wort, SAMe, kava kava (may increase risk of serotonin syndrome and/or excessive sedation).

Mechanism of Action:

Pramipexole is a nonergot dopamine agonist with specificity for the D2 subfamily dopamine receptor, and has also been shown to bind to D3 and D4 receptors. By binding to these receptors, it is thought that pramipexole can stimulate dopamine activity on the nerves of the striatum and substantia nigra.

Pharmacodynamics/Kinetics:

Protein binding: 15%

Bioavailability: 90%

Half-life elimination: ~8 hours; Elderly: 12-14 hours

Time to peak, serum: ~2 hours

Excretion: Urine (90% as unchanged drug)

Dosage:

Adults: Oral: Initial: 0.375 mg/day given in 3 divided doses, increase gradually by 0.125 mg/dose every 5-7 days; range: 1.5-4.5 mg/day

Dosage adjustment in renal impairment:

Clcr 35-59 mL/minute: Initial: 0.125 mg twice daily (maximum dose: 1.5 mg twice daily)

Clcr 15-34 mL/minute: Initial: 0.125 mg once daily (maximum dose: 1.5 mg once daily)

Clcr<15 mL/minute (or hemodialysis patients): Not adequately studied

Administration:

Doses should be titrated gradually in all patients to avoid the onset of intolerable side effects. The dosage should be increased to achieve a maximum therapeutic effect, balanced against the side effects of dyskinesia, hallucinations, somnolence, and dry mouth.

Monitoring Parameters:

Monitor for improvement in symptoms of Parkinson's disease (eg, mentation, behavior, daily living activities, motor examinations), blood pressure, body weight changes, and heart rate

Dietary Considerations:

May be taken with food to decrease nausea.

Patient Education:

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Take exactly as directed. Avoid alcohol. May cause drowsiness and extreme sedation or somnolence (use caution when driving or engaging in hazardous activities until response to drug is known); postural hypotension (use caution when changing position - rise slowly from sitting or lying position to standing and use caution when climbing stairs); constipation (increased exercise, fluids, fruit, or fiber may help); or urinary frequency. Consult prescriber about persistent adverse effects. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Breast-feeding is not recommended.

Dental Health: Effects on Dental Treatment:

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Dosage Forms:

Tablet, as dihydrochloride monohydrate: 0.125 mg, 0.25 mg, 0.5 mg, 1 mg, 1.5 mg

International Brand Names:

Mirapex® (CA); Mirapexin® (ES, PL); Pexola® (CO); Sifrol® (FI)

References

Guttman M, "Double-Blind Comparison of Pramipexole and Bromocriptine Treatment With Placebo in Advanced Parkinson's Disease," International Pramipexole-Bromocriptine Study Group, Neurology, 1997, 49(4):1060-5.

Lieberman A, Ranhosky A, and Korts D, "Clinical Evaluation of Pramipexole in Advanced Parkinson's Disease: Results of a Double-Blind, Placebo-Controlled, Parallel-Group Study,"Neurology, 1997, 49(1):162-8.

Molho ES, Factor SA, Weiner WJ, et al, "The Use of Pramipexole, a Novel Dopamine (DA) Agonist, in Advanced Parkinson's Disease,"J Neural Trans, 195, 45(Suppl):225-30.

Piercey MF, Hoffman WE, Smith MW, et al, "Inhibition of Dopamine Neuron Firing by Pramipexole, a Dopamine D(3) Receptor-Preferring Agonist: Comparison to Other Dopamine Receptor Agonists,"Eur J Pharmacol, 1996, 312(1):35-44.

"Safety and Efficacy of Pramipexole in Early Parkinson Disease. Parkinson Study Group,"JAMA, 1997, 278(2):125-30.

Shannon KM, Bennet JP Jr, and Friedman JH, "Efficacy of Pramipexole, A Novel Dopamine Agonist, as Monotherapy in Mild to Moderate Parkinson's Disease," The Pramipexole Study Group, Neurology, 1997, 49(3):724-8.

Stern MB, "Contemporary Approaches to the Pharmacotherapeutic Management of Parkinson's Disease: An Overview,"Neurology, 1997, 49(1 Suppl 1):2-9.

Szegedi A, Wetzel H, Hillert A, et al, "Pramipexole, A Novel Selective Dopamine Agonist, in Major Depression,"Mov Disord, 1996, 11(Suppl):266.

Ting RM and Force RW, "Pramipexole for Parkinson's Disease,"J Fam Pract, 1998, 46(1):19-20.

Watts RL, "The Role of Dopamine Agonists in Early Parkinson's Disease,"Neurology, 1997, 49(1 Suppl 1):34-48.

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