Мирапекс

Мирапекс – drug for symptomatic therapy of crushing idiopathic damages of the central nervous system.

Form of release and structure

• Tablets of 0,25 mg: oval, with slanted edge, on both sides flat, white color; on one of the parties on both parts from deep risks marking of "P7", on another – on both sides risks marking of a logo of the company - "BI" (on 10 tablets in the blister from Pas/aluminium/PVC, 3 blisters in a pack cardboard);
• Tablets of 1 mg: round, with slanted edge, on both sides flat, white color; on one of the parties on both parts from deep risks marking of "P9", on another – on both sides risks marking of a logo of the company - "BI" (on 10 tablets in the blister from Pas/aluminium/PVC, 3 blisters in a pack cardboard).

Structure of 1 tablet:

• Active ingredient: a pramipeksola of dihydrochloride monohydrate of 0,25 mg or 1 mg (corresponds to the maintenance of a pramipeksol of the basis – 0,18 or 0,7 mg);
• Auxiliary components: starch corn, Mannitolum, silicon dioxide colloid, magnesium stearate, povidone.

Indications to use

• Parkinsonism (Parkinson's disease) – for symptomatic monotherapy or as a part of complex treatment with a levodopa;
• Idiopathic syndrome of uneasy legs – for symptomatic therapy.

Contraindications

Absolute:

• Lactation (breastfeeding period);
• Children's and teenage age up to 18 years;
• Hypersensitivity to a pramipeksol, other components of medicine.

Relative (drug is taken with caution, owing to the increased probability of side effects):

• Renal failure;
• Arterial hypotension;
• Pregnancy (drug is used in case of considerable exceeding of estimated advantage for mother over potential risk for a fruit).

Route of administration and dosage

Pill is taken inside, irrespective of meal, washed down with water.

The daily dose should be divided into 3 receptions evenly.

At the beginning of therapy the daily dose of 0,375 mg, each 5-7 days it gradually is recommended increase before achievement of the maximum therapeutic effect.

It is necessary to observe the following scheme of increase in a dose:

• I week: 0,375 mg the day divided into 3 receptions on 0,125 mg;
• II week: 0,75 mg the day divided into 3 receptions on 0,25 mg;
• III week: 1,5 mg the day divided into 3 receptions on 0,5 mg.

If further increase in a daily dose is recommended, every week it is necessary to add 0,75 mg before achievement of the most admissible size – 4,5 mg a day.

For a maintenance therapy the individual daily dose varies 0,375-4,5 mg in repartitions. Irrespective of a disease stage Mirapeks's efficiency was noted at a daily dose 1,5 mg, at the same time is not excluded that in some cases reception more than 1,5 mg of drug a day can have additional therapeutic effect, in particular at later stages of a disease when doses of a levodopa are shown to be reduced.

The treatment termination pramipeksoly is required to be carried out gradually, for several days.

The patients using drug as a part of complex therapy with a levodopa in the period of the supporting course, and also at increase in a dose of a pramipeksol, need to reduce a dose of a levodopa to avoid the increased dofaminergichesky stimulation.

Initial therapy with a renal failure at KK ≥ 50 ml/min. does not demand reduction of a daily dose from patients. If KK from 20 to 50 ml/min., then reception begin with the daily dose 0,25 mg divided into 2 times on 0,125 mg. At KK ≤ 20 ml/min. treatment begin with reception 0,125 mg once a day.

When function of kidneys worsens during a maintenance therapy, the daily dose of a pramipeksol needs to be lowered by the same percent by which KK decreases (for example, KK 30% less, therefore, it is necessary to lower a daily dose of a pramipeksol by 30%).

At KK from 20 to 50 ml/min. the daily dose can be divided into two receptions and if KK ≤ 20 ml/min. – to accept it for once.

Dose adjustment is not required to patients with a liver failure.

Side effects

As the most frequent side reactions at therapy by Mirapeks at early stages of a disease the konstipation (lock) and drowsiness are registered. At later stages of a disease when прамипексол accept in a combination with a levodopa, hallucinations and dyskinesia are more often observed. These undesirable effects decrease in case of treatment continuation, and nausea, the lock and dyskinesia tend to disappearance.

Other side reactions from systems and bodies:

• Nervous system: ZNS – a malignant antipsychotic syndrome (an akathisia, muscular rigidity, a hyperthermia, disturbance of consciousness, disturbance of thinking, vegetative lability), confusion of consciousness, sleeplessness, dizzinesses, an extrapyramidal syndrome, nonsense, amnesia, an adynamy, an ataxy, a hypesthesia, dystonia, a tremor, a depression, a myoclonus, uneasiness, a hypokinesia, a suicide mood;
• Musculoskeletal system: myotonia of legs, a hyper tone of muscles, muscular twitchings, a bursitis, arthritis, a myasthenia, neck pains, thorax pain, pain in lumbar and sacral departments of a backbone;
• Alimentary system: appetite reduction, dyspepsia, a dysphagy, an abdominal pain, diarrhea, a meteorism, vomiting, dryness in a mouth;
• Respiratory system: sinusitis, pharyngitis, rhinitis, short wind, grippopodobny syndrome, change of a voice, strengthening of cough;
• Urinogenital system: infections of urinary tract, frequent urination;
• Cardiovascular system: arrhythmias, tachycardia, stenocardia, orthostatic hypotension, increase in activity of KFK enzyme (kreatinfosfokinaza);
• Sense bodys: accommodation paralysis, conjunctivitis, diplopia, increase in intraocular pressure, cataract, hearing easing;
• Allergic reactions, other: retroperitoneal fibrosis, hyperthermia, pleural exudate, pulmonary infiltration, decrease in body weight, hyperhidrosis, peripheral hypostases, decrease or increase in a libido.

Episodes of a morbid attraction to gamblings against the background of reception of a pramipeksol, especially in high doses which passed with drug withdrawal are described.

Development of arterial hypotension in case of Mirapeks's reception was noted not more often than from placebo use. Developing of arterial hypotension was observed at certain patients at the beginning of therapy, especially in case of too bystry increase in a dose of drug.

Special instructions

The most known side reactions at therapy by dopamine agonists and a levodopa – confusion of consciousness and a hallucination. It is noted that the levodopa combination with Mirapeks at late stages of a disease caused hallucinations more often, than monotherapy pramipeksoly at early stages.

It is necessary to inform patients and persons who care for them, that therapy by dopaminergic drugs can cause abnormal behavior with symptoms of compulsive and impulsive actions: a hyperphagia (tendency to an overeating), pathological shopping (persuasive desire to buy), hyper sexuality, and also pathological thirst for gamblings. At manifestation of such effects it is necessary to make the decision on a dose decline of drug or the gradual termination of therapy.

At psychotic frustration to appoint dopamine agonists with pramipeksoly the risk/advantage is allowed only after comprehensive preliminary estimate of a ratio. Reception of antipsychotic means along with pramipeksoly should be avoided.

Through certain time from the beginning of reception, or right after purpose of drug (in case of visual disturbances) it is necessary to undergo testing at the oculist.

At heavy cardiovascular pathologies it is required to show care, accepting Mirapeks as there is a probability of development of orthostatic hypotension owing to reception of dopaminergic drugs. Control of the arterial pressure (AP), especially at the beginning of a therapy course is recommended.

It is necessary to consider probability of sedative effect of drug which can be observed in the course of treatment at any time. There are reliable data about backfilling of patients at daily activity that became the reason of accidents.

As a result of epidemiological researches it is revealed that at Parkinson's disease the risk of development of a melanoma is 2-6 times higher. It is authentically unknown whether such increased probability is a consequence of the disease, or it is connected with reception of medicines which are used for therapy of parkinsonism. Patients and persons who look after them need to be informed on the increased risk of development of a melanoma.

At parkinsonism, in case of the sharp termination of treatment, the symptom complex similar to manifestations of a malignant antipsychotic syndrome is observed.

Therapy of a syndrome of uneasy legs drugs of dopaminergic action can become the reason of its strengthening which is characterized by earlier manifestation of symptoms on time (early evening or even the second half of day), and also strengthening of this symptomatology and distribution of effects on other extremities. However by results of carrying out a special research, an essential difference in strengthening of a clinical picture between the patients accepting прамипексол and group of placebo it was not revealed.

The attending physician is obliged to inform patients on probability of developing of hallucinations, preferential visual, and development of sedations, including drowsiness and backfilling during daily activity, capable to exert impact on driving of the car. In this regard it is not recommended to work with difficult mechanisms and to manage motor transport before acquisition of the sufficient experience in treatment by Mirapeks allowing to estimate his influence on intellectual and/or motive activity. In cases of the increased drowsiness or at spontaneous backfilling in daily activity, for example, during communication, meal, etc., from the types of activity demanding the increased concentration of attention and speed of psychomotor reactions it is necessary to refuse and address the doctor.

Medicinal interaction

Pramipeksol slightly (<20%) contacts proteins of plasma and biotransformirutsya owing to what his interaction with other substances / drugs influencing removal at the expense of biotransformation or linkng with proteins is improbable.

Interaction with pramipeksoly inhibitors of active secretion of cationic drugs through renal tubules (Cimetidinum), or the substances which are removed by active secretion through renal tubules, expressed in decrease in clearance of one or both drugs is possible. At simultaneous use of Mirapeks with such drugs (including амантадин) it is recommended to trace symptoms of excessive dopamine stimulation: excitement, dyskinesia or hallucinations. In similar cases it is necessary to lower a dose.

Levodopa and селегилин do not exert impact on pharmacokinetics of a pramipeksol who, in turn, does not influence absorption or elimination of a levodopa.

Medicinal interaction of antikholinergetik and amantadin was not studied, but it is supposed that it is possible as at drugs the similar mechanism of removal. As anticholinergic drugs, generally are exposed to metabolism, with pramipeksoly their interaction is improbable.

In case of increase in a dose of a pramipeksol it is necessary to reduce a levodopa dose, but at the same time other protivoparkinsonichesky medicines accept in an invariable dosage.

Owing to possible cumulative effects it is recommended to show care at a concomitant use of ethanol, other psikholeptik, and also the medicines increasing concentration of a pramipeksol (Cimetidinum) in plasma in combination with Mirapeks.

It is necessary to avoid reception of a pramipeksol along with antipsychotic substances / drugs, for example, in case of the expected antagonism.

Terms and storage conditions

To store in unavailable to children, the dry, dark place, at a temperature up to 30 °C.

Period of validity – 3 years.