OralParkinson's diseaseAdult: As an adjunct to levodopa therapy: As HCl: Initially, 125 mcg tid on the 1st wk, increased to 250 mcg tid on the 2nd wk and 500 mcg tid on the 3rd wk according to response. Daily dose may be increased by 750 mcg at wkly intervals. Max: 4.5 mg/day. Elderly: No dosage adjustment needed.
OralRestless leg syndromeAdult: As HCl: 125 mcg once daily 2-3 hr before bedtime. May increase, if necessary by 250 mcg every 4-7 days. Max: 750 mcg/day. Elderly: No dosage adjustment needed.
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Pexole 0.25/Pexole 1
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Sifrol
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Restless leg syndrome:
CrCl (mL/min) |
Dosage |
20-60 |
Increase titration interval to 14 days. |
Parkinson's disease:
CrCl (mL/min) |
Dosage |
<20 |
125 mcg once daily. Max: 1.5 mg daily. |
20-50 |
125 mcg bid. Max: 2.25 mg daily. |
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No dosage adjustment needed.
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Pramipexole May be taken with or without food. May be taken w/ meals to minimise GI side effects such as nausea.
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Psychotic disorder, severe CV disease, augmentation (earlier onset, increase and spread of symptoms). Risk of neuroleptic malignant syndrome w/ abrupt withdrawal. Taper dose at 750 mcg/day for a wk, then reduce by 375 mcg/day thereafter. Renal impairment. Pregnancy and lactation.
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Dyskinesia, sudden onset of sleep and somnolence, hallucinations, abnormal dreams, insomnia, confusion, headache, nausea, dizziness, vomiting, fatigue, constipation, peripheral oedema, visual impairment, decreased appetite.
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Patients should be informed to refrain from activities involving mental alertness and physical coordination after drug intake.
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Monitor BP, signs and symptoms of fibrosis and orthostatic hypotension, development of impulse control disorder, behavioural changes. Perform periodic skin examinations. Regular ophthalmological testing due to risk of visual disorders.
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Symptoms: Nausea, vomiting, hyperkinesia, hallucinations, agitation and hypotension. Management: Symptomatic and supportive treatment accompanied w/ gastric lavage, IV fluids, activated charcoal admin and ECG monitoring.
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Antagonism of effects occur w/ concomitant use w/ antipsychotics or methyldopa. Increased plasma concentration w/ cimetidine. Additive sedative effect w/ CNS depressants. May increase orthostatic hypotensive effect w/ MAOI.
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Avoid concomitant use w/ valerian, St John's wort. May increase sedative effect w/ alcohol.
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Description: Mechanism of Action: Pramipexole is a nonergot-derivative dopamine receptor agonist which alleviates Parkinsonian motor deficits by directly stimulating postsynaptic dopamine activity on the striatum and substantia nigra It is used as an adjunct to levodopa for the symptomatic management of parkinsonian syndrome in patients w/ advanced disease. It is also used as monotherapy for the initial symptomatic management of parkinsonian syndrome. Pharmacokinetics: Absorption: Readily absorbed. Oral bioavailability: Approx 90%. Time to peak plasma concentration: Fasted state: 2 hr; w/ food: 3 hr. Distribution: Volume of distribution: Approx 500 L. Plasma protein binding: <20%. Metabolism: Minimal metabolism. Excretion: Via renal tubular secretion into the urine >90% (unchanged). Elimination half-life: 8-12 hr.
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Do not store above 25°C. Protect from light and moisture.
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