Mirapex pd coated pills prolonged 1.5 mg N30
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Active ingredients
Pramipexole
Release form
Pills
Composition
Pramipexole dihydrochloride monohydrate 1.5 mg, which corresponds to the content of pramipexole 1.05 mg; Excipients: hypromellose 2208 - 157.5 mg, corn starch - 169.65 mg, carbomer 941 - 17.5 mg, colloid silicon dioxide - 2.1 mg, magnesium stearate - 1.75 mg.
Pharmacological effect
Anti-Parkinsonian, dopamine receptor agonist. The mechanism of action is believed to be related to the ability of pramipexole to stimulate dopamine receptors in the striatum. This is confirmed by the effect on the level of impulses in the striatal neurons due to the activation of dopamine receptors in the striatum and the substantia nigra. We cannot exclude the possibility that pramipexol inhibits prolactin secretion in humans.
Pharmacokinetics
After oral administration, pramipexol is rapidly absorbed from the gastrointestinal tract, Cmax in plasma is reached after approximately 2 hours. Pramipexole has an absolute bioavailability of more than 90%. Food does not affect the degree of absorption of pramipexol, although the time to reach Cmax in plasma increases by about 1 hour when taking the drug during a meal.; Css is reached after 2 days from the start of pramipexole.; It is widely distributed in the body, Vd is about 500 liters ( variations - 20%). Plasma protein binding is about 15%. Pramipexol accumulates in erythrocytes, which is confirmed by the ratio of concentration in erythrocytes to plasma concentration equal to 2.; T1 / 2 is 8 hours in young healthy volunteers and about 12 hours in elderly volunteers; Pramipexol is excreted mainly by the kidneys; in the urine, 90% of the administered dose is almost completely unchanged. Non-renal excretion pathways may play a role in the elimination of pramipexole, although its metabolites have not been detected in plasma and urine. Renal clearance of pramipexole is about 400 ml / min (coefficient of variation - 25%), which is about 3 times higher than the glomerular filtration rate. Pramipexol is thus secreted by the renal tubules, possibly through the organic cation transport system.; Pramipexole clearance is about 30% lower in women than in men, but this difference can be largely due to the difference in body mass.There is no difference in T1 / 2 values in men and women. With age, the clearance of pramipexole decreases, while in older people (aged 65 and over) T1 / 2 increases by about 40% (from 8.5 hours to 12 hours), and total pramipexole clearance is reduced by 30% compared with young, healthy volunteers (aged less than 40 years); in patients with Parkinson's disease, pramipexole clearance may be reduced by up to 30% compared with healthy elderly subjects. The reason for this difference seems to be a decrease in kidney function in patients with Parkinson's disease. The pharmacokinetics of pramipexole in patients with liver failure has not been studied. Since approximately 90% of the excreted dose is excreted in the urine unchanged, it can be expected that an abnormal liver function does not significantly affect the excretion of pramipexol. In severe renal impairment (CC at about 20 ml / min), the clearance of pramipexole decreases by about 75%, with moderate renal dysfunction (CC approximately 40 ml / min) - by 60%, compared with healthy subjects. In such patients, it is recommended to use the drug in lower initial and maintenance doses. The clearance of pramipexole is extremely low in patients on hemodialysis because dialysis produces small amounts of pramipexole. The pharmacokinetics of pramipexole in children has not been studied.
Indications
Treatment of Parkinson's disease (as monotherapy and in combination with levodopa).
Contraindications
Hypersensitivity to pramipexole.
Use during pregnancy and lactation
Adequate and strictly controlled studies of the safety of pramipexole in pregnancy have not been conducted. It is believed that the use is possible in cases where the intended benefit to the mother outweighs the potential risk to the fetus. It is not known whether pramipexole is excreted in breast milk. If necessary, use during lactation should stop breastfeeding.
Dosage and administration
For adults, when taken orally, the initial dose is 375 mcg / day in 3 doses. The dose should be increased every 5-7 days to achieve the maximum therapeutic effect, which is observed when taking 1.5-4.5 mg / day. In patients with impaired renal function, the initial dose is 125 μg / day, the frequency of reception is 1-3 times / day, depending from the values of KK.; Maximum dose: single dose - 1.5 mg; daily dose with QC more than 60 ml / min - 4.5 mg in 3 doses, with KK 35-59 ml / min - 3 mg in 2 doses, with KK 15-34 ml / min - 1.5 mg in 1 dose; To stop the treatment is recommended within 1 week.
Side effects
From the side of the central nervous system and peripheral nervous system: drowsiness, dyskinesias, hallucinations; in some cases - insomnia. With a rapid decrease in the dose of pramipexol, as well as with abrupt cancellation, the development of the CNS is possible. On the part of the digestive system: nausea, constipation too short time); Other: in some cases, peripheral edema.
Overdose
Symptoms: not installed. Clinical experience with a significant overdose of Mirapex is absent. One patient with a 10-year history of schizophrenia took 11 mg / day of pramipexole for 2 days; this is 2-3 times more than the daily dose recommended by the protocol. No adverse effects were noted due to an increase in dose. Blood pressure remained stable, although the heart rate increased to 100-120 beats / min; Treatment: pramipexole's antidote is unknown. When symptoms of CNS stimulation appear, neuroleptics can be used - derivatives of phenothiazine or butyrophenone, but the effectiveness of these drugs in eliminating the effects of Mirapex overdose has not been evaluated. In the treatment of overdose may require maintenance therapy, gastric lavage, the use of means for rehydration and detoxification of the body, ECG monitoring.
Interaction with other drugs
With simultaneous use with drugs that are derived cationic transport system of the kidneys, it is possible to increase the concentration of pramipexole in the blood plasma. With simultaneous use with levodopa may develop dyskinesia; with cimetidine - a decrease in the clearance of pramipexole and an increase in its concentration in the blood plasma.
special instructions
It is used with caution in patients with impaired renal function. In patients with QA less than 15 ml / min, experience with pramipexole is insufficient. The safety and efficacy of pramipexole in children has not been established .