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Active ingredients
Pramipexole
Release form
Pills
Composition
Active ingredient: Pramipexol. Concentration of active ingredient (mg): 1 mg
Pharmacological effect
Pramipexol is an agonist of dopamine receptors, with high selectivity and specificity binds to the dopamine receptors of the D2 subgroup, of which has the most pronounced affinity for the D3 receptors. Reduces the lack of motor activity in Parkinson's disease by stimulating dopamine receptors in the striatum. Pramipexol inhibits the synthesis, release and metabolism of dopamine. In vitro Pramipexol protects dopamine neurons from degeneration arising in response to ischemia or methamphetamine neurotoxicity. The exact mechanism of action of the drug in the treatment of the syndrome is currently not known. Despite the fact that the pathophysiology of tired leg syndrome is not fully understood, there is neuropharmacological information involving the dopaminergic system in the process. Studies using positron emission tomography (PET), showed the anthogenesis of restless legs syndrome. moderate presynaptic dopaminergic dysfunction in the striatum may be involved. In vitro Pramipexol protects neurons from levodopa neurotoxicity. Reduces the secretion of prolactin (dose-dependent). With prolonged use (more than 3 years) of pramipexole in patients with Parkinson's disease, there was no sign of a decrease in effectiveness. When using pramipexole in patients with restless legs syndrome for 1 year, the effectiveness of the drug was maintained.
Pharmacokinetics
After oral administration, pramipexol is rapidly and completely absorbed. Absolute bioavailability is more than 90%, and maximum plasma concentrations are observed after 1-3 hours. Absorption rate decreases with food intake, however, food intake does not affect the total amount of absorption. Pramipexole is characterized by linear kinetics and relatively small concentration variability between patients. Pramipexol binds to proteins to a very small extent (less than 20%), and has a large volume of distribution (400 liters). Metabolized to an insignificant degree. About 90% of the dose is excreted through the kidneys (80% unchanged) and less than 2% is found in the feces.The total clearance of pramipexole is about 500 ml / min, the renal clearance is about 400 ml / min. The half-life (MS) ranges from 8 hours in young people and up to 12 hours in the elderly.
Indications
The drug Mirapex is indicated for: idiopathic Parkinson’s disease (symptomatic therapy with Mirapex only or a combination of Mirapex + levodopa), idiopathic restless legs syndrome (symptomatic therapy).
Contraindications
The drug Mirapex is not prescribed for: indications in children, pregnancy, indications in adolescents, hypersensitivity to pramipexole. hypersensitivity to auxiliary components. With caution, Mirapex pills are prescribed for: hypotension, renal failure.
Use during pregnancy and lactation
The effect on pregnancy and lactation in humans has not been studied. The possible effects of pramipexole on reproductive function were investigated in animal experiments. Pramipexol does not exhibit teratogenicity in rats and rabbits, but at doses toxic to pregnant females, it was embryotoxic in rats. During pregnancy, the drug should be prescribed only if the potential benefit to the mother outweighs the potential risk to the fetus. Removal of the drug in breast milk has not been studied. Since pramipexol inhibits prolactin secretion, it can be assumed that it also suppresses lactation. Therefore, the drug should not be taken during lactation.
Dosage and administration
Tablets are taken inside. You can take the dosage form at any time with a glass of water. The daily dose is recommended to be divided into three doses. Symptomatic therapy of Parkinson's disease is carried out according to the scheme: the beginning of therapy - 375 mcg per day, the continuation of therapy (after a week) - 750 mcg per day, the further continuation (2 weeks after the start of therapy) - 1.5 mg per day. A further dosage increase of 750 mcg per day every week is possible. The maximum daily dose is 4, 5 mg. Maintenance therapy is carried out with dosages of 375 mg-4, 5 mg. Cancellation of the drug Mirapex should occur gradually. In combinatorial treatment with levodopa, it is necessary to adjust dosages in time to prevent excessive dopamine stimulation.Correction of dosages in case of renal failure: in case of CC 20-50 ml min - 250 mcg per day in two doses. A gradual increase in dosages to 2, 25 mg per day is possible, with CC less than 20 ml min - 125 mcg per day in a single dose. Perhaps a gradual increase in dosages up to 1, 5 mg per day. Symptomatic therapy of restless legs syndrome is carried out according to the following scheme: the beginning of therapy - 125 mcg in the evening, the continuation of therapy (after a week) - 250 mcg in the evening, the further treatment (after 2 weeks) - 500 mcg in the evening. Perhaps an increase in daily dosage up to 750 mg. Maintenance therapy is carried out in doses of 125 - 750 mg per day. The increase in dosage is carried out only with a lack of therapeutic effect.
Side effects
The use of the drug Mirapex may be accompanied by: anomalies of behavior, hyperphagia, insomnia, confusion, pathological shopping, paranoid thoughts, delusions, increased libido, dizziness, fainting, decreased libido, abnormal dreams, dyskinesia, heterosexuality, amnesia, anxiety, anxiety, anxiety, anxiety, dyskinesia, anxiety, dyskinesia, heterosexuality, amnesia, anxiety, anxiety, dyskinesia, anxiety, dyskinesia, heterosexuality, amnesia, anxiety, dyskinesia, anxiety, dyskinesia, heterosexuality, amnesia, anxiety, dyskinesia, anxiety, dyskinesia, heterosexuality, amnesia, anxiety, dyskinesia, anxiety. , sudden sleep, gambling, dyspnea.
Overdose
Cases of overdose are not described. Estimated symptoms characteristic of the pharmacodynamic profile of dopamine receptor agonists: nausea, vomiting, hyperkinesia, hallucinations, agitation and lowering blood pressure. Treatment: the established antidote does not exist, at overdose gastric lavage, symptomatic therapy, dynamic observation is recommended. The effectiveness of hemodialysis has not been established. When signs of excitation of the central nervous system may appoint neuroleptics.
Interaction with other drugs
Pramipexol is slightly (less than 20%) bound to plasma proteins and undergoes biotransformation. Therefore, interactions with other drugs that affect the binding to plasma proteins, or elimination due to biotransformation are unlikely. Drugs that inhibit the active secretion of cationic drugs through the renal tubules (for example, cimetidine), or that are themselves excreted through active secretion through the renal tubules, can interact with pramipexol, resulting in reduced clearance of one or both drugs. In the case of simultaneous use of such drugs (includingamantadine) and pramipexole should pay attention to such signs of excessive dopamine stimulation as dyskinesia, agitation or hallucinations. In such cases, it is necessary to reduce the dose. Selegiline and levodopa do not affect the pharmacokinetics of pramipexole. Paramipexol does not affect the total absorption or elimination of levodopa. Interaction with anticholinergic drugs and amantadine has not been studied. However, interaction with amantadine is possible, since drugs have a similar elimination mechanism. Anticholinergic drugs are mainly metabolized, so interaction with pramipexol is unlikely. When increasing the dose of pramipexole, a decrease in the dose of levodopa is recommended, while the dose of other anti-Parkinsonian drugs must be maintained at a constant level. Because of the possible cumulative effects, patients should be advised to exercise caution when taking other sedative drugs or alcohol in combination with Mirapex, as well as while taking drugs that increase the concentration of pramipexole in plasma. Concurrent use of pramipexole with antipsychotics should be avoided (for example, if antagonism is expected).