Pramipexole is a dopamine agonist of the non-ergoline class indicated for treating Parkinson's disease (PD) and restless legs syndrome (RLS).
The exact mechanism of action of pramipexole as a treatment for Parkinson's disease is unknown at this time. It is thought, however, that the ability of pramipexole to cause stimulation of the dopamine receptors in the striatum of the brain, a region that receives a vast array of neurological input and is responsible for a wide variety of functions, may be involved. Studies performed in animals show that pramipexole influences striatal neuronal transmission rates following activation of dopamine receptors. Pramipexole is considered a non-ergot dopamine agonist that shows specificity and strong activity at the D2 subfamily of dopamine receptors in vitro, binding selectively and dopamine D2 receptors and showing a preference for the dopamine D3 receptor subtype rather than other subtypes. The clinical significance of this binding specificity is unknown.
Parkinson’s disease, used alone or as an adjunct to cobeneldopa or co-careldopa BY MOUTH USING IMMEDIATE-RELEASE MEDICINES Adult: Initially 88 micrograms 3 times a day, if tolerated dose to be increased by doubling dose every 5-7 days, increased to 350 micrograms 3 times a day, then increased in steps of 180 micrograms 3 times a day if required, dose to be increased at weekly intervals, during dose titration and maintenance, levodopa dose may be reduced, maximum daily dose to be given in 3 divided doses; maximum 3.3 mg per day BY MOUTH USING MODIFIED-RELEASE MEDICINES Adult: Initially 260 micrograms once daily, dose to be increased by doubling dose every 5-7 days, increased to 1.05 mg once daily, then increased in steps of 520 micrograms every week if required, during dose titration and maintenance, levodopa dose may be reduced according to response; maximum 3.15 mg per day Moderate to severe restless legs syndrome BY MOUTH USING IMMEDIATE-RELEASE MEDICINES Adult: Initially 88 micrograms once daily, dose to be taken 2-3 hours before bedtime, dose to be increased by doubling dose every 4-7 days if necessary, repeat dose titration if restarting treatment after an interval of more than a few days; maximum 540 micrograms per day DOSE EQUIVALENCE AND CONVERSION Doses and strengths are stated in terms of pramipexole (base). Equivalent strengths of pramipexole (base) in terms of pramipexole dihydrochloride monohydrate (salt) for immediate-release preparations are as follows: 88 micrograms base :125 micrograms salt; 180 micrograms base:250 micrograms salt; 350 micrograms base:500 micrograms salt; 700 micrograms base:1mg salt. Equivalent strengths of pramipexole (base) in terms of pramipexole dihydrochloride monohydrate (salt) for modified-release preparations are as follows: 260 micrograms base:375 micrograms salt; 520 micrograms base:750 micrograms salt; 1.05 mg base :1.5mg salt; 1.57 mg base :2.25mg salt; 2.1mg base :3 mg salt; 2.62 mg base :3.75 mg salt; 3.15 mg base :4.5mg salt.
Pramipexole is the only dopamine agonist not appreciably metabolized by the P450 system which minimizes about possible drug-drug interactions. Cimetidine and amantadine may reduce the renal clearance of pramipexole. Sedating medicinal products or alcohol in combination with pramipexole may cause additive effects.
Psychotic disorders . risk of visual disorders (ophthalmological testing recommended) . severe cardiovascular disease
Common or very common Confusion . constipation . decreased appetite . dizziness . drowsiness . dyskinesia . hallucinations . headache . hyperkinesia . hypotension . nausea . peripheral oedema . postural hypotension . restlessness . sleep disturbances . sudden onset of sleep . visual disturbances . vomiting . weight changes Uncommon Amnesia . binge eating . cardiac failure . compulsive behaviour . delusion . dyspnoea . hiccups . paranoia . pneumonia . pruritus . rash . syncope Frequency not known Paradoxical worsening of restless legs syndrome
PREGNANCY Use only if potential benefit outweighs risk? no information available. BREAST FEEDING May suppress lactation; avoid?present in milk in animal studies.
There is no clinical experience with massive overdose. Symptoms of overdose are nausea, vomiting, hyperkinesia, hallucinations, agitation and hypotension. There is no established antidote. If signs of central nervous system stimulation are present, a neuroleptic agent may be indicated. Management of the overdose may require general supportive measures, along with gastric lavage, intravenous fluids, administration of activated charcoal and electrocardiogram monitoring.
Store in a cool and dry place. Protect from light.
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