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Pramipexole is antiparkinsonian drug. Pramipexole is a dopamine receptor agonist with high selectivity and specificity associated with dopamine receptor subgroups D2, has a strong affinity for D3 receptors. Reduce physical inactivity in Parkinson’s disease by stimulating dopamine receptors in the striatum Pramipexole inhibits the synthesis release and metabolism of dopamine dopamine protects neurons from degeneration that occurs in response to ischemia or methamphetamine neurotoxicity.
Reduces the secretion of prolactin dose-dependent With prolonged use more than 3 years) evidence of reduced efficacy have not been established. Pharmacokinetics after ingestion Pramipexole is rapidly and completely absorbed. Absolute bioavailability is greater than 90% and maximum plasma concentrations observed after 1-3 hours The rate of absorption is reduced by food intake but on the total volume of the suction does not affect food intake Pramipexole is characteristic for linear kinetics and a relatively small concentration variability between individual patients Pramipexole binds to proteins in a very small extent (<20% and has a large volume of distribution 400 l). Is metabolized to a minor extent About 90% of the dose is excreted through the kidneys (80 unchanged and less than 2 is found in feces. Total clearance of Pramipexole is about 500 ml min renal clearance is about 400 ml min. The half-life (T varies from 8 o’clock in the young and to 12 hours in the elderly. Indications: Treatment of symptoms of Parkinson’s disease (monotherapy or in combination with Levodopa Category effects on the fetus impact on pregnancy and lactation has not been investigated in humans During pregnancy, the drug Pramipexole should be used only if the potential benefit to the mother outweighs the potential risk to the fetus Excretion of the drug in breast milk has not been studied Since Pramipexole inhibits prolactin secretion it may be assumed that it also suppresses lactation.
Therefore, the drug should not be taken during breastfeeding.
If you are going to use Pramipexole, please consider contraindications before use.
Hypersensitivity to Pramipexole or to any component of the drug Pramipexole With caution. Renal failure hypotension In the study of carcinogenicity in animals observed degeneration and loss of photoreceptor cells in the retina of albino rats The potential importance of this effect in humans has not been established, but it cannot be ignored because of a possible violation of the mechanism erosion disk universal for all vertebrates.
If you want to use Pramipexole, please read about its recommended dosage.
Orally, regardless of the meal, washed down with water Daily dose evenly divided into 3 admission Initial therapy As described below the initial daily dose of 0. 375 mg increase every 5-7 days To reduce the adverse effects the dose should be selected to gradually achieve maximal therapeutic effect. Scheme increase the dose Pramipexole Week 1: Dose (mg 3 x 0. 125 the total daily dose mg) 0. 375 Week 2 Dose (mg 3 x 0. 25 the total daily dose mg) 0. 75 Week 3: Dose (mg) – 3 x 0. 5, the total daily dose (mg) – 1. 50 If required, further increasing the daily dose, was added 0. 75 mg per week to a maximum dose of 4. 5 mg per day. Supportive therapy: Individual dose should be in the range from 0. 375 mg to 4. 5 mg per day. Both early and late stages of the disease the drug was effective, starting with a daily dose of 1. 5 mg. This does not exclude that an individual patient doses above 1. 5 mg per day may provide an additional therapeutic effect, especially for late stage disease when levodopa dose reductions shown. Discontinuation of treatment: Pramipexole should be withdrawn gradually over several days. The dose for patients receiving concomitant therapy with levodopa: If concurrent therapy with levodopa, it is recommended as the dose, as well as during maintenance therapy with Pramipexole reduce levodopa dose. This is to avoid excessive dopaminergic stimulation. Dose for patients with renal insufficiency: For the initial therapy: patients with a creatinine clearance greater than 50 mL/min does not require reducing the daily dose. Creatinine clearance 20 – 50 mg/ml initial daily dose is administered in two divided doses, starting with 0. 125 mg 2 times a day (0. 25 mg daily). Creatinine clearance less than 20 ml/min the daily dose administered once a day, starting with 0. 125 mg. If during maintenance therapy reduced renal function, the daily dose is reduced by the same percentage, which reduced creatinine clearance, ie if creatinine clearance is reduced by 30 %, the daily dose should be reduced by 30%. The daily dose can be divided into two doses if creatinine clearance is in the range of 20 – 50 ml/min, or administered once daily if creatinine clearance less than 20 mL/min. The doses to patients with liver failure: no need to reduce the dosage in patients with hepatic failure.
Pramipexole: Side effects
Before deciding to use Pramipexole, please consider possible side effects.
In the early stages of the disease more common adverse events were somnolence and constipation, and at a later stage in the treatment of disease in combination with levodopa, dyskinesia, were more common and hallucinations. These adverse events decreased with continued therapy, constipation, nausea and dyskinesia tended to disappear. The nervous system: confusion, neuroleptic malignant syndrome (hyperthermia, muscle rigidity, altered mental status, akathisia, vegetative lability, thought disorder), insomnia, extrapyramidal syndrome, dizziness, asthenia, amnesia, hypesthesia, dystonia, myoclonus, tremor, depression, anxiety, ataxia, hypokinesia, delirium, suicidal tendencies.