Pramipexole Dihydrochloride

Trade Names:
Mirapex
- Tablets 0.125 mg
- Tablets 0.25 mg
- Tablets 0.5 mg
- Tablets 1 mg
- Tablets 1.5 mg

Pharmacology

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Stimulates dopamine receptors in the corpus striatum.

Pharmacokinetics

Absorption

Rapid absorption. T _max is approximately 2 h; increased 1 h if taken with food. Bioavailability is more than 90%. Steady state is 2 days.

Distribution

Extensively distributed; distributes into red blood cells, as indicated by an erythrocyte to plasma ratio of approximately 2. Vd is 500 L. Protein binding is 15%.

Elimination

Renal (90% mostly as unchanged in urine); nonrenal routes may contribute to a small extent. Renal Cl is 400 mL/min. The terminal t _½ is approximately 8 h (healthy adults) and approximately 12 h (elderly).

Special Populations

Cl is 75% lower in severe impairment (Ccr less than 20 mL/min) and about 60% lower with moderate impairment (Ccr less than 40 mL/min). Recommend lower starting and maintenance dose.

The t _½ increases approximately 40% and Cl decreases approximately 30% in individuals 65 yr of age and older mostly because of reduced renal function with age.

Cl is approximately 30% lower in women.

Cl is reduced approximately 30%; appears to be related to reduced renal function in these individuals.

Indications and Usage

Treatment of the signs and symptoms of idiopathic Parkinson disease (may be used in conjunction with levodopa). Treatment of moderate to severe primary restless legs syndrome (RLS).

Contraindications

Standard considerations.

Dosage and Administration

PO Start with 0.125 mg 3 times daily. After 5 to 7 days, the dose may be increased to 0.25 mg 3 times daily. Further increases in dose may be made in increments of 0.25 mg 3 times daily, at intervals of 5 to 7 days, to a dose of 1.5 mg 3 times daily.

Moderate impairment (Ccr 35 to 59 mL/min): Start with 0.125 mg 2 times daily (max, 1.5 mg 2 times daily). Severe impairment (Ccr 15 to 34 mL/min): Start with 0.125 daily (max, 1.5 daily).

PO Start with 0.125 mg once daily 2 to 3 h before bedtime. If additional symptomatic relief is needed, the dose may be increased to 0.25 mg once daily in 4 to 7 days. If needed, an additional increase in dose to 0.5 mg once daily may be made in 4 to 7 days.

In moderate and severe impairment (Ccr 20 to 60 mL/min), increase the duration between titration steps to 14 days.

General Advice

• Administer without regard to meals. Administer with food if GI upset occurs.

Storage/Stability

Store at 59° to 86°F. Protect from light.

Drug Interactions

May reduce pramipexole efficacy.

May reduce oral Cl of pramipexole. Pramipexole dosage adjustment may be needed if therapy with any of these agents is started or stopped during treatment with pramipexole.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Postural hypotension (53%); blackouts, hypotension, syncope (postmarketing).

CNS

Dyskinesia (47%); extrapyramidal symptoms (28%); insomnia (27%); dizziness (26%); somnolence (22%); hallucinations (17%); headache (16%); asthenia (14%); abnormal dreams (11%); confusion (10%); fatigue (9%); dystonia (8%); abnormal gait, hypertonia (7%); amnesia (6%); abnormal thinking, akathisia, hypesthesia, malaise (3%); paranoid reaction (2%); decreased libido, delusion, myoclonus, sleep disorder (1%); abnormal behavior, hypersexuality, increased and decreased libido, pathological gambling (postmarketing).

Dermatologic

Skin disorders (2%).

EENT

Nasal congestion (6%); accommodation abnormalities (4%); rhinitis, vision abnormalities (3%); diplopia (1%).

GI

Nausea (28%); constipation (14%); diarrhea, dry mouth (7%); anorexia, dyspepsia (4%); dysphagia (2%).

Genitourinary

Urinary frequency (6%); UTI (4%); impotence, urinary incontinence (2%).

Lab Tests

Increased CPK (1%).

Metabolic-Nutritional

General edema, peripheral edema (5%); weight decrease (2%); weight increase (postmarketing).

Musculoskeletal

Pain in extremities (7%); arthritis (3%); bursitis, twitching (2%); myasthenia (1%).

Respiratory

Dyspnea (4%); pneumonia (2%).

Miscellaneous

Accidental injury (17%); influenza (7%); chest pain (3%); fever (1%); compulsive eating, increased eating (including binge eating) (postmarketing).

Precautions

Pregnancy

Category C .

Lactation

Inhibits prolactin secretion. Do not give to breast-feeding mothers.

Children

Safety and efficacy not established.

Renal Function

Use with caution and adjust dose in presence of moderate to severe renal function impairment. Use lower initial and maintenance doses.

Abrupt withdrawal

Rapid withdrawal or dose reduction of antiparkinsonism drugs may produce symptoms resembling neuroleptic malignant syndrome.

CNS effect

Use concomitant CNS depressants with caution because of additive sedative effects.

Concurrent levodopa use

When pramipexole is used in combination with levodopa, the dose of levodopa may be reduced as tolerated.

Dyskinesia

Pramipexole may potentiate dopaminergic side effects of levodopa and may cause or exacerbate preexisting dyskinesias.

Fibrosis

Retroperitoneal fibrosis, pulmonary infiltrates, pleural effusion, pleural thickening, pericarditis, and cardiac valvulopathy have been reported in patients taking ergot-derived dopaminergic agents.

Hallucinations

Can occur during pramipexole therapy. Frequency is greater when used in conjunction with levodopa. Incidence appears to increase with age.

Hypotension

Postural hypotension may occur, especially during dose escalation.

Impulse control

Pathological gambling, hypersexuality, and compulsive eating have been reported.

Melanoma

Can occur at a higher frequency in patients with Parkinson disease.

Rebound RLS

During treatment, shifting of symptoms to early morning hours or earlier in the afternoon has been reported.

Retinal pathology

Pathological changes were observed in the retinas of albino rats receiving dopaminergic receptor agonists. The potential significance of this effect in humans has not been established but cannot be disregarded.

Rhabdomyolysis

Can occur along with elevated CPK levels.

Sleepiness

Patients have reported falling asleep while engaging in activities of daily living (eg, operating a motor vehicle).

Patient Information

• Instruct patient to take exactly as prescribed. Advise patient that dose may be taken without regard to meals but to take with food if nausea occurs.
• Inform patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.
• Instruct patient to avoid sudden position changes to prevent orthostatic hypotension.
• Instruct patient to report the following symptoms to health care provider: dizziness, headache, mood or mental changes, severe or persistent nausea, uncontrollable movements.
• Inform patient that hallucinations can occur and that elderly patients are more susceptible.
• Advise patient to use caution when taking other drugs with CNS depressant effects (eg, alcohol, sedatives).
• Inform patient that impulse control disorders such as pathological gambling, compulsive eating, or hypersexuality can occur.

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