One tablet Mirapex includes 0.25 mg or 1 mg pramipexole monohydrate dihydrochloride (0.18 mg or 0.7 mg pramipexole) Additionally: colloidal silicon dioxide, magnesium stearate, mannitol, povidone, corn starch.
One tablet Mirapex PD (prolonged action) includes 0.375 mg / 0.75 mg / 1.5 mg / 3 mg / 4.5 mg pramipexole monohydrate dihydrochloride (0.26 mg / 0.52 mg / 1.05 mg / 2.1 mg / 3.15 mg pramipexole) Additionally: corn starch, hypromellose 2208, colloidal silicon dioxide, carbomer 941, magnesium stearate.
The therapeutic agent Mirapex (INN - Pramipexole, Pramipexole) is produced in the form of tablets No. 30 and tablets PD No. 10 or No. 30.
Pharmacodynamics and pharmacokinetics
Dopamine receptor agonist - pramipexolehas a high specific and selective ability to bind to the D2 subgroup dopamine receptors, of which the most pronounced affinity for D3 receptors. Through stimulation dopamine receptorslocated in the striatum, the drug helps to reduce the patient’s motor deficiency observed with parkinson's disease.
Characteristic of pramipexoleis its inhibitory effect on synthesis, subsequent release and further metabolism dopamine. In vitro pramipexoleprotects dopamine neurons from the process of their degeneration, developing during methamphetamine neurotoxicity or ischemia.
Treatment restless legs syndrome Mirapex (RLS) has not been fully studied, since the pathophysiology of this disease state is not completely known. Despite this, neuropharmacological evidence of primary involvement in therapy is present. dopaminergic system. The studies using PET (positron emission tomography) revealed the possibility of moderate influence in the striatum dopaminergic presynaptic dysfunction on the pathogenesis of RLS.
In vitro pramipexoleprotects neurons from neurotoxicimpacts levodopa. Depending on the dose taken, reduces secretion prolactin.
Prolonged use of the drug (more than 3 years) for the treatment of patients suffering parkinson's disease, as well as his treatment of patients with RLS for 1 year, showed no signs of a decrease in its effectiveness.
With oral administration, absorption of pramipexole from the gastrointestinal tract occurs rather quickly. Plasma Cmax is observed after approximately 120 minutes. The absolute bioavailability indicator exceeds 90%. The degree of absorption of pramipexole does not depend on its intake during meals, but increases the time to reach plasma Cmax by about 60 minutes. Css is noted 48 hours after the start of taking Mirapex.
Pramipexole has a wide distribution in the human body, Vd is approximately 500 liters (with a variation of 20%). Approximately 15% of the drug binds to plasma proteins. The accumulation of pramipexole in red blood cells, as evidenced by the ratio of its concentrations in red blood cellscompared to a plasma concentration of 2. In healthy young volunteers, T1 / 2 of the drug is 8 hours, in older volunteers - 12 hours.
Excretion of pramipexole is carried out mainly by the kidneys, 90% of the drug is determined in the urine almost completely in unchanged form. Extrarenal pathways of pramipexole excretion may play some role in its elimination, although no products of its metabolism have been detected in urine and plasma. The renal clearance of the drug is approximately 400 ml / min (with a variation of 25%), which is approximately three times the speed glomerular filtration. Thus secretion pramipexole occurs through renal tubulespossibly using a system for transporting organic cations.
In women, the indicator pramipexole clearanceapproximately 30% lower than this indicator in men, although this difference may largely depend on the difference in weight. There is no difference in T1 / 2 values between women and men.
Pramipexole clearance rate decreases with age. In elderly patients (after 65 years), T1 / 2 of the drug increases by approximately 40% (from 8.5 hours to 12 hours). Compared to healthy young volunteers (under 40) total clearance of pramipexole decreases by about 30%.
In patients with parkinson's diseasecompared with healthy elderly volunteers, a decrease was observed pramipexole clearance up to 30%. The reason for this difference in performance may be reduced renal function, observed with parkinson's disease.
Pharmacokinetic features pramipexoleregarding patients with liver failure not studied. In connection with 90% excretion of the drug by the kidneys in unchanged form, we can assume the absence of a significant effect of impaired hepatic function on the excretion of pramipexole.
In case of severe renal impairment (with CC 20 ml / min) a decrease is noted pramipexole clearance approximately 75%, with impaired renal function moderate (with CC 40 ml / min) clearance decreases by 60%. Patients in these categories need to reduce the initial and maintenance dosages of Mirapex. In patients undergoing the procedure hemodialysisextremely low pramipexole clearance, since during dialysis, a small amount is excreted.
In the children's age group, the pharmacokinetics of pramipexole has not been studied.
Indications for use
Mirapex is indicated for symptomatic therapy. parkinson's disease (monotherapy is used, as well as concomitant use with Levodopa) and treatment of negative symptoms restless legs syndrome.
Mirapex is contraindicated in patients with personal hypersensitivity to pramipexoleor other components of the tablets, as well as under the age of 18 years.
Patients with low blood pressure and renal failureas well as nursing and pregnant women.
Therapy with Mirapex can lead to the following negative side effects:
- decreased appetite;
- abnormal dreams;
- itching/rashand other phenomena hypersensitivity;
- behavioral disorders (symptomatology of compulsive and impulsive actions, including hypersexuality, overeatingobsessive shopping desirepathological gambling attachment etc.);
- heart failure;
- decrease / increase in weight;
- confused consciousness;
- decrease in visual acuity / clarity;
- sudden falling asleep;
- visual impairment (including diplopia);
- decrease in blood pressure;
- decreased secretion of antidiuretic hormone;
- peripheral edema;
- nausea, vomiting;
- sex drive.
Instructions for use
Mirapex tablets are intended for oral (oral) administration in conjunction with water and regardless of the meal time. All daily dosages of the drug in milligrams are calculated by pramipexole dihydrochloride monohydrate and evenly divided into 3 doses.
Instructions for the use of Mirapex in the treatment of Parkinson's disease
The first week of therapy using Mirapex is shown to be carried out in a daily dose of 0.375 mg divided into three doses of 0.125 mg. If the treatment is not effective enough, in the second week you can increase the daily dosage to 0.75 mg (three times 0.25 mg), and in the third week to 1.5 mg (three times 0.5 mg). In the future, it is possible to increase the daily dosage of the drug by 0.75 mg per week, up to the maximum daily dose of 4.5 mg. Such a gradual increase (1 time in 5-7 days) of daily doses is carried out with the aim of reducing the possible manifestations of side effects of Mirapex and is carried out until the optimal therapeutic effect of therapy is obtained.
Supportive treatment is carried out using individually selected daily dosages of Mirapex, ranging from 0.375 mg to 4.5 mg. At all stages of the disease (from early to late), the effectiveness of the drug was observed, starting with the use of a daily dosage of 1.5 mg. Moreover, in some patients, the possibility of an additional therapeutic effect of Mirapex therapy in a daily dose exceeding 1.5 mg, especially in the late stage of the development of the disease, when dosage reduction is practiced, is not ruled out levodopa.
The cessation of therapy with Mirapex is carried out by a gradual daily decrease in its daily dosages by 0.75 mg until a daily dose of 0.75 mg is reached, after which the dose is further reduced by 0.375 mg.
In parallel therapy with levodoparecommend increasing the dosage of Mirapex, as well as in the process of supporting treatment, to reduce the dose taken levodopain order to prevent excessive dopaminergic stimulation organism.
At kidney pathologies Mirapex initial therapy for patients with CC greater than 50 ml / min is performed in the dosage regimen recommended above. With a CC of 20-50 ml / min, the daily initial dosage of the drug should be reduced by a third and be 0.25 mg (0.125 mg twice in 24 hours). The maximum allowable daily maintenance dose of Mirapex for such patients should not exceed 2.25 mg. With CC less than 20 ml / min, a single dose of the drug is prescribed per day, starting with a dose of 0.125 mg. Such patients, as a maintenance dose, can take a maximum of 1.5 mg of Mirapex in 24 hours.
When decreased renal function during maintenance treatment, the daily dose of Mirapex should be reduced by a percentage reduction in CC (that is, with a decrease in CC by 30%, also reduce the dose of the drug by 30%). With a CC of 20-50 ml / min, the daily dosage of Mirapex is divided into two doses, with a CC of less than 20 ml / min, the daily dose is taken once.
The need to adjust the dosage regimen for the treatment of patients with liver pathologies does not exist.
Instructions for use of Mirapex in the treatment of restless legs syndrome
In the treatment of this pathology, Mirapex is initially prescribed in a daily dosage of 0.125 mg, with a single dose for 2-3 hours before bedtime. If it is necessary to further reduce the negative symptoms of the disease, the daily dose can be gradually increased every 4-7 days, initially up to 0.25 mg, after up to 0.5 mg and up to a maximum of 0.75 mg.
Supportive treatment is carried out in an individually selected daily dose of Mirapex, ranging from 0.125 mg to 0.75 mg.
Discontinuation of therapy does not require a gradual reduction in the dosage of the drug. In clinical trials, the phenomenon of worsening of the negative symptoms of the disease after the simultaneous cessation of therapy at any daily dose was observed in only 10% of patients.
At kidney pathologiesexcretion of pramipexole depends on their functional state and is determined by the indices of QC. Results of pharmacokinetic studies in patients with renal failure (with QC greater than 20 ml / min) showed no need to adjust the dosage regimen. The use of Mirapex in patients with Scand insufficient renal function not studied.
At liver pathologies dose reduction of Mirapex is not required, due to the fact that about 90% of the absorbed active ingredient of the drug is excreted in the urine.
The safety and effectiveness of Mirapex for the treatment of patients in the children's age group (up to 18 years old) has not been established.
Episodes of severe overdose during treatment with Mirapex are not described. Presumably, when taking excessive doses of the drug, negative symptoms characteristic of the pharmacodynamic profile of dopamine receptor agonists may occur: excitation, nausea, vomiting, hallucinations, hyperkinesiadecreased blood pressure.
An antidote to pramipexole does not exist. Overdose treatment should include gastrointestinal tract cleaning, dynamic observation and symptomatic therapy. Performance hemodialysis being questioned. In case of observation in a patient CNS excitation allow application antipsychotics.
Since the binding of pramipexole with plasma proteins is carried out to a small extent (less than 20%), and also due to the low biotransformation of this drug, its interaction with other therapeutic agents that affect protein bonds or excretion due to the biotransformation process is unlikely.
Secretion inhibitors cationic substances through the renal tubules (Cimetidine), as well as drugs that are independently excreted by the renal tubules, can interact with the active ingredient of Mirapex - pramipexole and lead to a decrease in clearance of one drug or both therapeutic agents. When used concomitantly with pramipexole, such drugs (including amantadine) you need to pay attention to the phenomena of excessive dopamine stimulation (overexcitation, hallucinations, dyskinesia) and timely adjust the dosage regimen of therapy.
Selegilineand levodopa do not affect the pharmacokinetic parameters of pramipexole, which, in turn, does not affect the general parameters of absorption and excretion of levodopa.
The interaction of pramipexole with anticholinergic drugs and amantadinepurposefully not studied. However, due to a similar excretion mechanism, the interaction of pramipexole and amantadine is possible. Anticholinergic drugs are mainly subject to metabolic transformations, and therefore, their interaction with pramipexole is doubtful.
With an increase in the dosage of pramipexole, it is recommended to reduce the dose of levodopa taken together. Dosages of other antiparkinsonian drugs are maintained at a constant level.
Due to the potential for cumulative effects, caution must be exercised in the case of combined use with ethanol or mirapex or sedativesas well as drugs that increase plasma concentration pramipexole(cimetidine).
In the treatment pramipexoleconcurrent administration should be avoided antipsychotic drugs (e.g. with expected antagonism).
Terms of sale
Mirapex is a prescription drug.
Mirapex tablets should be stored at ambient temperatures up to 30 ° C.
Mirapex is suitable for use for 3 years from the date of tablet production.
Manifestations hallucinationsand confused consciousness are the most common side effects when taken dopamine agonists (including Mirapex) and levodopa. In the case of concurrent administration of pramipexole and levodopa at a late stage of the disease, manifestations hallucinationswere noted more often in comparison with Mirapex monotherapy in patients at an early stage of the disease. Mirapex host patients should be informed of the possibility of development hallucinations(usually visual), which can affect their ability to perform hazardous work and driving a car.
Patients Undergoing Treatment Using dopaminergic drugsas well as those caring for them, they should be aware of the possibility of the occurrence of symptoms of abnormal behavior (symptoms of compulsive and impulsive actions), including: hypersexualityhyperphagia (overeating), pathological shopping (constant desire for purchases) and pathological passion for gambling. If this abnormal symptom manifests itself, a decision should be made to reduce the dose of Mirapex and possibly to phase out the therapy.
In patients with psychotic disordersuse of pramipexole in conjunction with dopamine agonists possible only with an adequate assessment of the risk / benefit ratio of such treatment. The combined use of antipsychotic medications and pramipexole should be avoided.
At the stage of treatment, Mirapex recommend at regular intervals to check the patient's vision. Also subject to availability visual impairment an eye test should be performed immediately after the first dose of the drug.
Cautious use of Mirapex is required by patients with severe cardiovascular pathologies. Due to possible formation orthostatic hypotension, during treatment with dopaminergic drugs should be taken to control the patient's blood pressure, especially at the beginning of therapy.
Patients should be warned of the possibility of manifestation. sedative action Mirapex. There are reports of feelings drowsinessand subsequent sudden falling asleep during the usual daily activities of the patient (including the performance of hazardous work and driving a car), noted at any stage of therapy.
Epidemiological studies have revealed an increased risk of melanomasin patients with Parkinson's disease (2-6 times higher in comparison with the general population). It is not known whether this increased risk of formation melanomasconsequence of most parkinson's disease, or is associated with other factors, including taking medications used to treat this pathology. Due to the above reasons, patients themselves and their caregivers should be informed about the possible formation of melanomas while taking dopaminergic drugs, including pramipexole.
It was reported that during therapy parkinson's disease a sharp cessation of dopaminergic drugs led to the development of negative symptoms similar to the manifestations malignant antipsychotic syndrome.
The messages described in the literature indicate the possibility of amplification restless legs syndrome in case of treatment with dopaminergic drugs. This increase was manifested by an earlier onset of development evening symptoms disease (sometimes after lunch) and the spread of similar negative phenomena to other limbs. However, the 26-week clinical controlled trials devoted to the study of this particular effect did not reveal a significant difference in the increase in the clinical symptoms of RLS in the pramipexole and placebo.
Inform patients of potential formation hallucinations(usually visual), negatively affecting the ability to drive vehicles. When taking Mirapex may be observed sedative effect feeling medication drowsinessand instant sleep during everyday life. Due to the fact that drowsinessis a fairly frequent negative phenomenon of dopaminergic drug therapy and can lead to potentially fatal consequences, patients should abandon hazardous work and drive a car until they have sufficient experience with Mirapex therapy and the ability to adequately assess its effect on their own motorand / or mental activity. In case of manifestations during everyday life, increased drowsinessor sudden falling asleep (during food, conversation, etc.) during the treatment, patients are not recommended to engage in hazardous work and driving vehicles.
Analogs of MirapexMatches for ATX Level 4 code:PramipexolePronoran
Mirapex's analogs are represented by therapeutic drugs similar to it in their main action:
- Rolprina SR;
- Requip Modutab;
In pediatrics (up to 18 years) Mirapex is not used.
Throughout the treatment process using Mirapex, the patient should exclude drinks containing alcohol.
During pregnancy and lactation
The effect of Mirapex on pregnant and lactating women has not been investigated.
Surveys conducted on animals to determine the effects of pramipexole on their reproductive function did not show teratogenic effects of the drug, but revealed some embryotoxicity. In this regard, the appointment of Mirapex at pregnancyallowed only in cases of obvious excess of the benefits of such treatment in comparison with the possible risk to the fetus.
The excretion of pramipexole with milk from a nursing mother has not been studied. Since one of the effects of pramipexole is inhibition of secretion prolactinsuggest its overwhelming effect on lactation. For this reason, Mirapex should not be prescribed during breastfeeding.
Reviews about Mirapex
Mirapex reviews in the discussion forums on therapeutic drugs used for therapy parkinson's disease, in comparison with reviews of other similar medicines, are more positive. Relatives of patients observe a lower frequency and severity of side effects of Mirapex, including drowsinessand hallucinations, as well as the greater effectiveness of this drug. Among the negative aspects of such treatment, a gradual decrease in the effect of Mirapex can be noted, which leads to the need to search for its substitutes.
Mirapeks price, where to buy
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Average buy Mirapex PD it is possible for: 0.375 mg No. 30 - 140 rubles; 1.5 mg No. 30 - 1,500 rubles; 3 mg No. 30 - 3000 rubles.
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