Mirapeks

Мирапекс Drug photo

The description is actual on 08.06.2016

  • Latin name: Mirapex
  • ATH code: N04BC05
  • Active ingredient: Pramipeksol (Pramipexole)
  • Producer: Boehringer Ingelheim Pharma (Germany)

Structure

One tablet of Mirapeks includes 0,25 mg or 1 mg of dihydrochloride of monohydrate of a pramipeksol (0,18 mg or 0,7 mg of a pramipeksol). In addition: colloid silicon dioxide, magnesium stearate, Mannitolum, povidone, corn starch.

One tablet of Mirapeks PA (the prolonged action) includes 0,375 mg / 0,75 mg / 1,5 mg / 3 mg / 4,5 mg of dihydrochloride of monohydrate of a pramipeksol (0,26 mg / 0,52 mg / 1,05 mg / 2,1 mg / 3,15 mg of a pramipeksol). In addition: corn starch, gipromelloz 2208, colloid silicon dioxide, carbomer 941, magnesium stearate.

Release form

The remedy of Mirapeks (MNN – Pramipexole, Pramipeksol) to be made in the form of tablets No. 30 and tablets PD No. 10 or No. 30.

Pharmacological action

Protivoparkinsonichesky, dofaminergichesky.

Pharmacodynamics and pharmacokinetics

The agonist of dopamine receptors – pramipeksol possesses high specific and selection ability contacts D2 subgroup of receptors of a dopamine from which the most expressed affinity shows to D3 receptors. By means of stimulation of the dopamine receptors which are in a striate body, drug promotes decrease in insufficiency of a physical activity of the patient who is observed at Parkinson's illness.

Its inhibiting impact on synthesis, the subsequent release and a further metabolism of a dopamine is characteristic of a pramipeksol. In vitro pramipeksol protects dopamine neurons from the process of their degeneration developing at a metamfetaminovy neurotoxicity or ischemia.

Treatment of a syndrome of uneasy legs Mirapeksy (SBN) is up to the end not studied as the pathophysiology of this disease state is completely not known. Despite it, there are neuropharmacological certificates on primary involvement in therapy of dopaminergic system. The conducted researches using PET (positron emission tomography), revealed a possibility of influence in a striate body of moderate dopaminergic presynaptic dysfunction on SBN pathogeny.

In vitro pramipeksol protects neurons from neurotoxic influence of a levodopa. Depending on the accepted dose reduces prolactin secretion.

Long use of drug (it is more than 3 years) for therapy of the patients having Parkinson's illness and also treatment of patients by it with SBN during 1 year, did not reveal signs of lowering of its efficiency.

At oral administration absorption of a pramipeksol comes from a gastrointestinal tract quickly enough. Plasma Cmax is observed approximately after 120 minutes. The indicator of absolute bioavailability exceeds 90%. Extent of absorption of a pramipeksol does not depend on its inclusion in food time, but increases time of achievement of plasma Cmax approximately for 60 minutes. Css is noted in 48 hours after the beginning of reception of Mirapeks.

Pramipeksol differs in wide distribution in a human body, Vd equals to about 500 liters (with a variation of 20%). About 15% of drug contact plasma proteins. Accumulation of a pramipeksol in erythrocytes is noted what the ratio of its concentration in erythrocytes in comparison with concentration in plasma, equal 2 testifies to. At healthy young volunteers of T1/2 of drug it is equal to 8 hours, at elderly volunteers – to 12 hours.

Removal of a pramipeksol is carried out mainly by kidneys, 90% of drug are defined in urine almost completely in not changed form. Extrarenal ways of excretion of a pramipeksol can play some role in its elimination though in urine and plasma products of its metabolism were not revealed. The renal clearance of drug makes about 400 ml/min. (with a variation of 25%) that approximately three times exceeds a glomerular filtration rate. Thus, secretion of a pramipeksol happens by means of renal tubules, it is possible by means of system of transportation of organic cations.

At women the indicator of clearance of a pramipeksol is about 30% lower than this indicator at men though such distinction considerably can depend on a difference in weight. Difference in T1/2 values at women and men is absent.

The indicator of clearance of a pramipeksol decreases with age. At elderly patients (after 65 years) T1/2 of drug increases approximately by 40% (from 8,5 to 12 o'clock). In comparison with healthy young volunteers (till 40 flyings) the general clearance of a pramipeksol decreases approximately by 30%.

At patients with Parkinson's illness, in comparison with healthy elderly volunteers, observed decrease in clearance of a pramipeksol to 30%. The reduced renal function noted at Parkinson's illness can be the cause of this distinction in indicators.

Pharmacokinetic features of a pramipeksol concerning patients with insufficiency of hepatic function are not studied. Due to 90% drug removal by kidneys in not changed form it is possible to assume lack of significant influence of disturbances of hepatic function on excretion of a pramipeksol.

In case of heavy disturbances of renal function (at KK of 20 ml/min.) decrease in clearance of a pramipeksol approximately for 75% is noted, at disturbances of renal function of moderate character (at KK of 40 ml/min.) the clearance goes down for 60%. Patients of these categories need decrease in the initial and supporting Mirapeks's dosages. At the patients undergoing procedure of a hemodialysis extremely low clearance of a pramipeksol as when carrying out a dialysis its insignificant quantity is output is observed.

In a children's age group the pharmacokinetics of a pramipeksol was not studied.

Indications to use

Mirapeks's appointment is shown for symptomatic therapy of an illness of Parkinson (it is used both monotherapy, and parallel reception with the Levodopa) and treatment of negative symptomatology of a syndrome of uneasy legs.

Contraindications

Mirapeks it is contraindicated to patients with personal hypersensitivity to a pramipeksol or other components of tablets, and also aged till 18 years.

Careful purpose of drug is demanded by the patients with the reduced arterial pressure and a renal failure and also feeding and pregnant women.

Side effects

Therapy using Mirapeks can lead to the following negative side effects:

  • loss of appetite;
  • abnormal dreams;
  • syncope;
  • amnesia;
  • itch/rash and other phenomena of hypersensitivity;
  • behavioural disturbances (symptomatology of compulsive and impulsive actions, including hyper sexuality, an overeating, persuasive desire of purchases, pathological attachment to gamblings and so forth);
  • heart failure;
  • reduction/increase in weight;
  • the confused consciousness;
  • decrease in sharpness/clearness of visual perception;
  • lock;
  • concern;
  • nonsense;
  • drowsiness;
  • hyperkinesia;
  • dizziness;
  • hiccups;
  • dyskinesia;
  • headache;
  • hyperphagia;
  • asthma;
  • sudden backfilling;
  • fatigue;
  • pneumonia;
  • hallucinations;
  • vision disorder (including diplopia);
  • decrease in the ABP;
  • paranoia;
  • decrease in secretion of antidiuretic hormone;
  • peripheral hypostases;
  • sleeplessness;
  • nausea/vomiting;
  • frustration of sexual desire.

Application instruction

Mirapeks's tablets are intended for peroral (in) reception together with water and irrespective of meal time. All daily dosages of drug in milligrams are calculated on dihydrochloride to monohydrate of a pramipeksol and evenly divided into 3 receptions.

Application instruction of Mirapeks at therapy of an illness Parkinson

The first week of therapy with Mirapeks's use is shown to carry out in a daily dose 0,375 mg divided into three receptions on 0,125 mg. At insufficient efficiency of the carried-out treatment, in the second week it is possible to increase a daily dosage to 0,75 mg (three times on 0,25 mg), and in the third week to 1,5 mg (three times on 0,5 mg). Further increase of daily dosages of drug on 0,75 mg a week is possible, up to achievement of the maximum daily dose – 4,5 mg. Such gradual increase (1 time in 5-7 days) daily doses is carried out about the purpose of reduction of possible manifestations of side effects of Mirapeks and carried out before receiving optimum therapeutic effect of therapy.

The supporting treatment is carried out with use of individually picked up daily dosages of Mirapeks, components from 0,375 mg to 4,5 mg. At all stages of a disease (from early to late) efficiency of drug was observed, since use of a daily dosage of 1,5 mg. At the same time at certain patients the possibility of additional therapeutic effect of therapy by Mirapeks in the daily dose exceeding 1,5 mg, in particular at a late stage of development of a disease when reduction of dosages of a levodopa practices is not excluded.

The termination of therapy by Mirapeks is carried out by gradual daily decrease in its daily dosages by 0,75 mg up to achievement of a daily dose of 0,75 mg then reduce a dose by 0,375 mg.

At parallel therapy using a levodopa recommend in process of increase of a dosage of Mirapeks, and also in the course of carrying out the supporting treatment, to reduce a dose of the accepted levodopa, for the purpose of the prevention of excessive dopaminergic stimulation of an organism.

At pathologies of kidneys initial therapy of patients by Mirapeks with KK takes place more than 50 ml/min. in the dosing mode recommended above. At KK of 20-50 ml/min. the daily initial dosage of drug has to be lowered on a third and make 0,25 mg (on 0,125 mg twice at 24 o'clock). The most admissible daily maintenance dose of Mirapeks for such patients should not exceed 2,25 mg. At KK less than 20 ml/min. appoint a single dose of drug in days, since a dose of 0,125 mg. Such patients as a maintenance dose can accept at most 1,5 mg of Mirapeks at 24 o'clock.

In case of decrease in renal function during the supporting treatment, it is necessary to reduce a daily dose of Mirapeks by percent of decrease in KK (that is at decrease in KK by 30% to reduce a drug dose also by 30%). At KK of 20-50 ml/min. the daily dosage of Mirapeks is divided into two receptions, at KK less than 20 ml/min. accept a daily dose once.

Need for correction of the dosing mode for therapy of patients with pathologies of a liver does not exist.

The application instruction of Mirapeks at therapy of a syndrome of uneasy legs

At therapy of this pathology initially appoint Mirapeks in a daily dosage of 0,125 mg, with a single dose of a dose in 2-3 hours before going to bed. In case of need additional decrease in negative symptomatology of a disease it is possible to raise a daily dose step by step each 4-7 days, to 0,25 mg, later to 0,5 mg and as much as possible to 0,75 mg in the beginning.

The supporting treatment is carried out in individually picked up daily dose of Mirapeks which is in borders from 0,125 mg to 0,75 mg.

The termination of therapy does not demand gradual reduction of dosages of drug. In the conducted clinical trials of the phenomenon of weighting of negative symptoms of a disease after the single-step termination of therapy in any daily dose it was observed only at 10% of patients.

At pathologies of kidneys removal of a pramipeksol depends on their functional state and is caused by KK indicators. Results of pharmacokinetic researches concerning patients with insufficiency of renal function (at KK more than 20 ml/min.) showed lack of need of correction of the dosing mode. Mirapeks's use for patients with SBN and insufficient function of kidneys was not studied.

At liver pathologies decrease in doses of Mirapeks is not required in view of the fact that about 90% of the absorbed active ingredient of drug are removed with urine.

Safety and Mirapeks's efficiency for therapy of patients of a children's age group (till 18 years) is not established.

Overdose

Episodes of the expressed overdose at treatment by Mirapeks are not described. Allegedly at reception of excessive dosages of drug the negative symptoms characteristic of a farmakodinamichesky profile of agonists of dopamine receptors can be shown: excitement, nausea/vomiting, hallucinations, hyperkinesia, decrease in the ABP.

The antidote to a pramipeksol does not exist. Treatment of cases of overdose has to include cleaning of bodies of a gastrointestinal tract, dynamic supervision and symptomatic therapy. Productivity of a hemodialysis is called into question. In case of supervision at the patient of excitement of TsNS allow use of neuroleptics.

Interaction

As linkng of a pramipeksol with plasma proteins is carried out in an insignificant measure (less than 20%), and also because of small biotransformation of this drug, its interaction with the other remedies influencing proteinaceous bonds or removal due to process of biotransformation is improbable.

The drugs oppressing secretion of cationic substances by means of renal tubules (Cimetidinum), as well as medicines, which are independently removed renal tubules can interact with active ingredient of Mirapeks – pramipeksoly and to lead to lowering of clearance of one drug or both remedies. At parallel use with pramipeksoly such medicines (including amantadin) it is necessary to pay attention to the phenomena of excessive dopamine stimulation (overexcitation, hallucinations, dyskinesia) and in time to adjust the dosing mode of therapy.

Selegilin and levodopa do not exert impact on pharmacokinetic indicators of a pramipeksol who, in turn, does not influence the general parameters of absorption and excretion of a levodopa.

Interaction of a pramipeksol with anticholinergic medical drugs and amantadiny purposefully was not studied. Nevertheless, thanks to the similar mechanism of removal, interaction of a pramipeksol and amantadin is possible. Anticholinergic medical drugs are generally subject to metabolic transformations in this connection, their interaction with pramipeksoly is doubtful.

At increase of a dosage of a pramipeksol recommend to reduce doses jointly of the accepted levodopa. Dosages of other protivoparkinsonichesky drugs support at the constant level.

Because of a possibility of cumulative effects it is necessary to show care in case of the combined reception with Mirapeks of ethanol or sedative drugs, and also medicines increasing plasma concentration of a pramipeksol (Cimetidinum).

At treatment pramipeksoly it is necessary to avoid parallel reception of antipsychotic means (for example, at the expected antagonism).

Terms of sale

Mirapeks treats the remedies which are on sale according to the recipe.

Storage conditions

It is necessary to keep tablets of Mirapeks at surrounding air temperature to 30 °C.

Period of validity

Mirapeks it is suitable for use for 3 years from the moment of production of tablets.

Special instructions

Displays of hallucinations and the confused consciousness are the most known by-effects at reception of dopamine agonists (including Mirapeks) and levodopas. In case of parallel reception of a pramipeksol and a levodopa at a late stage of a disease, display of hallucinations were noted more often, in comparison with monotherapy by Mirapeks of the patients who are at an early stage of a disease. Accepting Mirapeks of patients follow to inform on a possibility of development of the hallucinations (as a rule, visual) able to influence their ability to performance of dangerous works and driving of the car.

The patients passing therapy with use of dopaminergic drugs as well as the persons caring for them have to know about an opportunity emergence of symptoms of abnormal behavior (symptomatology of compulsive and impulsive actions), including: hyper sexuality, hyperphagia (overeating), pathological shopping (constant desire of purchases) and pathological passion to gamblings. At manifestation of this abnormal symptomatology it is necessary to make the decision on reduction of a dose of Mirapeks and it is possible about the gradual termination of therapy.

At patients with psychotic frustration use of a pramipeksol together with dopamine agonists is possible only at an adequate assessment of a ratio of risk/advantage of such treatment. It is necessary to avoid the combined purpose of antipsychotic remedies and a pramipeksol.

At a stage of carrying out treatment by Mirapeks recommend to check sight of the patient at regular intervals. Also in the presence of visual disturbances it is necessary to carry out a sight inspection at once after the first administration of drug.

Careful use of Mirapeks is demanded by patients with heavy cardiovascular pathologies. Because of possible forming of orthostatic hypotension, during treatment by dopaminergic drugs it is necessary to take on control of the ABP of the patient, in particular at the beginning of therapy.

Patients need to be warned about a possibility of manifestation of sedative action of Mirapeks. There are messages on emergence of feeling of drowsiness and the subsequent sudden backfilling during usual daily activity of the patient (including performance of dangerous works and driving of the car) noted at any stage of carrying out therapy.

The conducted epidemiological researches revealed the increased risk of forming of a melanoma at patients with Parkinson's illness (2-6 times higher in comparison with the general population). It is not known whether this increase in risk of forming of a melanoma is a consequence of the illness of Parkinson, or it is connected with other factors, including reception of the medical drugs used for treatment of this pathology. Owing to the above-stated reasons, patients and persons caring for them it is necessary to inform on possible forming of a melanoma during reception of dopaminergic drugs, including pramipeksol.

It was reported that at therapy of an illness of Parkinson the sharp termination of reception of dopaminergic drugs led to development of negative symptoms similar to manifestations of a malignant antipsychotic syndrome.

The messages described in special literature confirm a possibility of strengthening of a syndrome of uneasy legs in case of its treatment by dopaminergic drugs. Such strengthening was shown by earlier beginning of development of evening symptoms of a disease (sometimes after a lunch) and distribution of the similar negative phenomena on other extremities. However the conducted 26-week clinical controlled trials devoted to studying of this effect did not reveal a significant difference in strengthening of clinical symptoms of SBN in groups of reception of a pramipeksol and placebo.

It is necessary to inform patients on potentiality of forming of the hallucinations (as a rule, visual) which are negatively influencing ability of driving of motor transport. At Mirapeks's reception the sedative effect of drug which is shown feeling of drowsiness and instant backfilling during everyday life can be observed. Because drowsiness is quite frequent negative phenomenon of therapy by dopaminergic drugs and is capable to lead to potentially deadly effects, patients have to refuse dangerous works and driving until acquisition of sufficient experience of therapy by Mirapeks and ability to adequately estimate his influence on own motor and/or intellectual performance. In case of manifestations during everyday life of the increased drowsiness or sudden backfilling (during food, conversation and so forth) in the course of carrying out treatment, to patients do not recommend to be engaged in dangerous works and driving of motor transport.

Mirapeks's analogs

Coincidence on the ATH code of the 4th level:

Mirapeks's analogs are provided by medical drugs similar to him the main action:

Zdravzona

  • Mirapeks 1 mg No. 30 tabletkiberinger Ingelkhaym
  • Mirapeks 0,25mg No. 30 tabletkiberinger Ingelkhaym
  • Mirapeks No. 30 PD 1,5mg tabletkiberinger Ingelkhaym
  • Mirapeks PD 375 of mg No. 10 of a tablet of the Farm prolonged a deystviyaberenger Ingelkhaym Gmbh and To. KG
  • Mirapeks PD 3 of mg No. 30 of a tablet prolong.deystviyaberinger Ingelkhaym

Drugstore of IFC

  • Mirapeks tbl 0,25 mg No. 30, Pharmacia & Upjohn/Pfizerssha
  • Mirapeks tbl 1 mg No. 30, Beringer Ingelkhaym Farma Gmbh and To. Kggermaniya
  • Mirapeks PD tbl 0,375 mg No. 10, Boehringer Ingelheimgermaniya
to show still

Apteka24

  • Mirapeks PD
  • Mirapeksboehringer Ingelheim Pharma (Germany)
  • Mirapeks PD
  • Mirapeks PD
  • Mirapeks tablets 1 of mg No. 30beringer Ingelkhaym (Italy)
Section: For a nervous system
in more detail

Education: Graduated from the Vinnytsia national medical university of N. I. Pirogov, pharmaceutical faculty, the higher pharmaceutical education – the specialty "Pharmacist".

Experience: Work in Koneks and Bios-Media pharmacy chains as "Druggist". Work as "Pharmacist" in Avicenna pharmacy chain of the city of Vinnytsia.

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