Active material: Piriʙedil
When ATH: N04BC08
CCF: Противопаркинсонический препарат – стимулятор допаминергической передачи в ЦНС
ICD-10 codes (testimony): F07, G20, G21, H35.0, H53.1, H53.4, I73.9, I79.2
When CSF: 01.14.04
Manufacturer: Servier Laboratories (France)
Controlled release tablets, coated of red color, round, lenticular; Slight heterogeneity of staining, degree of gloss and the presence of small inclusions.
| 1 tab. | |
| piriʙedil | 50 mg |
Excipients: magnesium stearate, povidone, talc, carmellose sodium, polysorbate 80, carmine dye (Ponceau 4R), natriya carbonate, colloidal silicon dioxide, sucrose, Titanium dioxide, beeswax white.
15 PC. – блистеры (2) – пачки картонные.
30 PC. – блистеры (1) – пачки картонные.
Of anti-drug, dopamine receptor agonist. It enters the blood stream of the brain, where it binds to dopamine receptors in the brain, displaying high affinity and selectivity to dopamine D-type2 and D3.
The mechanism of action causes piribedil main clinical features of the drug for the treatment of Parkinson's disease as initial, and in the later stages of the disease with exposure to all major motor symptoms. Piribedil addition effects on dopamine receptor antagonist activity exhibits two major α-adrenergic receptors in the CNS (типа a2A и a2A).
The synergistic effect of piribedil, how α antagonist2-adrenoceptor agonist and dopamine receptors in the brain, It has been demonstrated in various animal models of Parkinson's disease: piribedil prolonged use leads to the development of less severe dyskinesia, than the use of levodopa, with similar efficiency against the reversible akinesia, associated disease, Parkinson.
During pharmacodynamic studies in humans have shown cortical arousal electrogenesis dopaminergic type as the awakening, and during sleep with the manifestation of clinical activity against various functions, controlled by dopamine. This activity has been demonstrated using behavioral and psychometric scales. It has been shown, In healthy volunteers piribedil improves attention and vigilance, associated with cognitive tasks.
Efficiency Pronoran® as monotherapy or in combination with levodopa in the treatment of Parkinson's disease has been evaluated in three double-blind, placebo-controlled clinical trials (2 study compared to placebo, and 1 study compared to bromocriptine). The study involved 1103 patient 1-3 step on the scale and Hyun Yar), 543 of whom received Pronoran®. Displaying, that Pronoran® dose 150-300 mg / day efffektiven the action of all motor symptoms with 30% improvement on the Unified Parkinson's Disease Rating Scale (UPDRS) Part III (motor) over a 7 months as monotherapy and 12 months in combination with levodopa. Улучшение части “активность в повседневной жизни” по шкале UPDRS II было оценено в тех же значениях.
When monotherapy statistically significant proportion of patients, in need of emergency treatment of levodopa, receiving piribedil (16.6%) was less, than in patients, placebo (40.2%).
The presence of dopamine receptors in the blood vessels of the lower extremities explains vasodilating action piribedil (It increases blood flow in the vessels of the lower extremities).
Absorption and distribution
Piribedil rapidly and almost completely absorbed from the gastrointestinal tract and rapidly distributed.
Cmax plasma levels achieved after 3-6 hours after receiving controlled release tablets. Plasma protein binding average (unbound fraction of 20-30%), so the risk of drug interactions when used with other drugs Low.
Metabolism
Piribedil extensively metabolized by the liver and excreted primarily in the urine: 75% piribedil absorbed is excreted by the kidneys as metabolites.
Deduction
The plasma elimination is biphasic piribedil and consists of an initial phase and a second slower phase, leading to the maintenance of a stable concentration in the blood plasma piribedil for more than 24 hours. During the combined pharmacokinetic analysis showed, that T1/2 piribedil after the on / in the averages 12 h and is independent of the administered dose.
By all indications (except for Parkinson's disease) the drug is prescribed in a dose 50 mg (1 tab.) 1 time / day. If necessary, may increase the dose to 100 mg / day (by 50 mg 2 times / day).
At Parkinson's disease monotherapy appointed 150-250 mg / day (3-5 tab. / day), divided by 3 admission. If necessary, the drug dose 250 mg is recommended to take 2 tab. by 50 mg in the morning and 2 tab. by 50 mg and day 1 tab. 50 mg in the evening.
At used in combination with levodopa daily dose is 150 mg (3 tab.) in 3 admission.
In the selection of dose in the case of increasing the recommended dose titrate, gradually increasing to 1 tab. (50 mg) every 2 of the week.
The tablets are taken orally, after meal, without chewing, drinking 1/2 cup water.
Reported adverse reactions when taking piribedil are dose-dependent and, mainly, associated with its dopaminergic activity. Adverse reactions are moderate, found, mainly, at the beginning of treatment and disappear after drug withdrawal.
Before the drug can occur following adverse reactions.
From the digestive system: often (>1/100, <1/10) – незначительные желудочно-кишечные симптомы (nausea, vomiting, flatulence), these adverse reactions are reversible in the selection of the appropriate individual dose. Titration, by gradually increasing the dose (by 50 mg every 2 weeks to reach the recommended dose), It leads to a significant reduction of manifestation of side effects data.
CNS: often (>1/100, <1/10) – могут отмечаться спутанность сознания, hallucinations, anxiety or dizziness, disappearing to remove the drug. Admission piribedil accompanied by sleepiness, and in very rare cases may be accompanied by severe sleepiness during the day until the sudden sleep.
Cardio-vascular system: rarely (< 1/10 000) – гипотензия, orthostatic hypotension with loss of consciousness or malaise or labile blood pressure.
Allergic reactions: the risk of allergic reactions to the dye carmine, part of the drug.
In patients with Parkinson's disease, treated with dopamine agonists, especially in patients receiving high doses and in combination with levodopa, noted gambling, increased libido and hypersexuality, these symptoms were generally reversible with dose reduction or interruption of treatment.
Because, that is formulated with sucrose, patients with fructose intolerance, glucose or galactose, as well as patients with a deficit sukrozoizomaltazy (a rare metabolic disorder) taking medication is not recommended.
The drug used mainly in elderly patients, at which the occurrence of pregnancy is unlikely. It has been shown, that mice piribedil crosses the placental barrier and is distributed in the organs of the fetus.
Due to the lack of data the drug should not be used during pregnancy and lactation.
The dye crimson, part of the drug, some patients have an increased risk of allergic reactions.
Effects on ability to drive vehicles and management mechanisms
Some patients (especially for patients with Parkinson's disease) while taking piribedil sometimes suddenly a state of severe sleepiness until sudden sleep. This phenomenon is very rare, but, Nonetheless, Patients, to drive and / or operate the equipment, It requires a high degree of attention, You should be warned about this. In the event of such reactions should consider dose reduction or cessation of therapy piribedil this drug.
Symptoms: vomiting (due to the action of piribedil on chemoreceptor trigger zone), labile blood pressure (increase or decrease), dysfunction of the gastrointestinal tract (nausea, vomiting).
Treatment: removal of the drug, symptomatic therapy.
Contraindicated in combination
Antipsychotics (except clozapine)
Mutual antagonism between antipsychotics and antiparkinsonian drugs
Patients with extrapyramidal syndrome, caused by taking neuroleptics, therapy should be prescribed anticholinergic drugs, and should not be prescribed dopaminergic antiparkinsonian drugs (due to blocking dopamine receptors neuroleptics).
Patients with Parkinson's disease, receiving treatment with dopaminergic antiparkinsonian agents, and requires the appointment of neuroleptics, should not continue to take levodopa due to the increasing incidence of mental illness, and also due to the blocking of dopamine receptors neuroleptics.
It is used antiemetic drugs, cause extrapyramidal symptoms.
The preparation is available on medical prescription.
The drug should be stored out of reach of children. No special storage conditions requires. Shelf life - 3 year.
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