The instruction for medical use of medicine Pramiksol the Trade name Pramiksol Mezhdunarodnoye the unlicensed name Pramipeksol Lekarstvennaya the Tablet Structure form 1 tablet contains active agent – a pramipeksol of dihydrochloride of monohydrate of 0.25 mg or 1.0 mg, excipients: mannitol (Mannitolum) (E 421), starch corn, silicon dioxide colloidal anhydrous, povidone, magnesium stearate. The description of the Tablet on 0.25 mg – white or almost white color, ploskotsilindrichesky, with a notch in the form of a cross, a tablet on 1.0 mg – white or almost white color, ploskotsilindrichesky, with risky. Pharmacotherapeutic group Nervous system. Antiparkinsonichesky drugs. Dopaminergic drugs. Dopamine agonists. Pramipeksol the ATX N04B C05 Code the Pharmacological Pramipeksol Pharmacokinetics properties is quickly and completely soaked up after oral administration. The absolute bioavailability is more than 90%. The maximum concentration in plasma are registered between the 1st and 3rd hour. Speed of absorption does not decrease at a concomitant use of food, but the general level of absorption decreases. Pramipeksolu is inherent linear kinetics and, irrespective of a dosage form, rather insignificant fluctuations of plasma level at different patients. People have a linking of a pramipeksol with proteins very low (& lt, 20%), and distribution volume – big (400 l). Pramipeksol is metabolized at people only in insignificant quantity. Removal by kidneys of not changed pramipeksol is the most important way of elimination. About 90% of a dose, marked 14C, are removed by kidneys whereas less than 2% are defined in Calais. The general clearance of a pramipeksol is about 500 ml/min., and renal – about 400 ml/min. Elimination half-life (t ½) – of 8 o’clock at young patients till 12 o’clock at elderly people. The pharmacodynamics Pramipeksol is dopamine agonist with high selectivity and specificity of rather dopamine receptors of D2 subtype and has primary relationship with D3 receptors, it differs in total internal activity. Pramipeksol facilitates parkinsonichesky motive disturbances by stimulation of dopamine receptors of striatum (corpus striatum). Pramipeksol suppresses synthesis, release and a turn of a dopamine. The exact mechanism of action of a pramipeksol at treatment of restless legs syndrome is unknown. Though the pathophysiology of restless legs syndrome is generally unknown, neuropharmacological data indicate attraction of primary dopaminergic system. Indications Treatment of signs and symptoms of idiopathic Parkinson’s disease at adults as monotherapy (without levodopa) or in a combination with a levodopa during a disease to late stages when the effect of a levodopa decreases or becomes unstable and arises fluctuation of therapeutic effect (phenomenon of inclusion switching off). Symptomatic treatment of idiopathic restless legs syndrome from moderated to heavy degree at adults in doses is not higher than 0.75 mg. The route of administration and doses of the Tablet accept orally, irrespective of meal, washing down with water. Parkinson’s disease. The daily dose is divided into 3 receptions in equal parts. Initial treatment. As shown below, the dose of drug needs to be increased gradually, from initial 0.375 mg in every day of 5-7 days. In cases when patients have no intolerable by-effects, the dose needs to be titrated before achievement of the maximum therapeutic effect. The scheme of increase in a dose of the drug Pramiksol Nedelya Dose (Mg) the General daily dose (mg) the 1st 3 x 0,125 0,375 the 2nd 3 x 0,25 0,75 the 3rd 3 x 0,5 1,5 In need of further increase in a dose the daily dose should be increased by 0.75 mg every week to maximum which makes 4.5 mg a day. However it should be noted that the frequency of emergence of drowsiness increases at use of doses higher than 1.5 mg a day. Maintenance therapy. The individual dose fluctuates from 0.375 mg to the maximum 4.5 mg a day. At increase in a dose the effect of treatment was observed, since a daily dose of 1.5 mg. The subsequent dose adjustment should be carried out, considering the clinical answer and emergence of side reactions. During the researches about 5% of patients accepted doses less than 1.5 mg. At the progressing Parkinson’s disease purpose of a dose higher than 1.5 mg can be reasonable for patients to whom reduction of a dose of a levodopa in combination therapy with a levodopa is planned. The levodopa dose decline at increase in a dose of drug is recommended Pramiksol and at maintenance therapy depending on reaction of the patient (see the section Medicinal Interactions). Treatment termination. The sudden termination of dopaminergic therapy can lead ment of an antipsychotic malignant syndrome. The dose of a pramipeksol should be reduced by 0.75 mg a day to a daily dose of 0.75 mg. After that the dose should be reduced to 0.375 mg a day (see the section Special Instructions). Dosing for patients with a renal failure. Removal of a pramipeksol depends on function of kidneys. The following scheme of dosing is offered for initial therapy. Patients with clearance of creatinine more than 50 ml/min. do not need reduction of a daily dose or frequency of dosing. The patient with clearance of creatinine of 20-50 ml/min. the initial daily dose of drug Pramiksol is appointed in two steps, since 0.125 mg twice a day (0.25 mg/days). It is not necessary to exceed the maximum daily dose of a pramipeksol of 2.25 mg. To patients with clearance of creatinine lower than 20 ml/min. Pramiksol appoint a daily dose of drug in one step, since 0.125 mg/days. It is not necessary to exceed the maximum daily dose of a pramipeksol of 1.5 mg. At deterioration in function of kidneys against the background of maintenance therapy the daily dose of drug Pramiksol is reduced by so many percent as far as there was a reduction of level of clearance of creatinine. For example, at decrease in clearance of creatinine by 30% the daily dose of drug Pramiksol is reduced by 30%. It is possible to appoint a daily dose in two steps if the clearance of creatinine is in limits of 20-50 ml/min., and in one if the clearance of creatinine is lower than 20 ml/min. Dosing for patients with an abnormal liver function. For patients with an abnormal liver function the dose decline is not considered necessary as nearly 90% of the acquired drug are removed by kidneys. Potential influence of an abnormal liver function on pharmacokinetics of a pramipeksol was not investigated. Restless legs syndrome. The recommended initial dose of drug Pramiksol makes 0.125 mg in 2-3 hours prior to a dream once a day. For the patients needing additional relief of symptoms, it is possible to increase a dose each 4-7 days to the maximum dose of 0.75 mg a day (as shown lower in the table): Scheme of increase in a dose of the drug Pramiksol Etap of titration Single daily evening dose (mg) 1 0,125 2 * 0.25 3 * 0.50 4 * 0.75 * in case of need treatment Termination. As the daily dose for treatment of restless legs syndrome does not exceed 0.75 mg, use of the drug Pramiksol can be stopped without gradual dose decline. Resuming of symptoms of restless legs syndrome (strengthening of weight of symptoms in comparison with initial level) at 10% of patients after sudden phase-out of a pramipeksol can be observed. Such effect is possible for all dosed Dosing for patients with a renal failure. Removal of the drug Pramiksol from an organism depends on function of kidneys. For patients with clearance of creatinine of 20 ml/min. there is no need to reduce a daily dose. Use of a pramipeksol was not studied at the patients who are on a hemodialysis and patients with heavy degree have renal failures. Dosing for patients with an abnormal liver function. For patients with an abnormal liver function the dose decline is not considered necessary as nearly 90% of the acquired drug are removed by kidneys. Side effects Side reactions are provided on classes of systems of bodies and frequency of emergence: very often (& gt, 1/10), it is frequent (& gt, 1/100 – & lt, 1/10), infrequently (& gt, 1/1000 – & lt, 1/100), is rare (& gt, 1/10,000 – & lt, 1/1000), is very rare (& lt, 1/10,000). Parkinson’s disease. Patients with Parkinson’s disease at treatment pramipeksoly in comparison with placebo the most frequent side reactions (& gt, 5%) had a nausea, dyskinesia, arterial hypotension, dizziness, drowsiness, insomnia, a constipation, hallucinations, a headache and fatigue. Frequency of emergence of drowsiness increases at use of doses higher than 1.5 mg a day (see the section Route of Administration and Doses). Dyskinesia was the most frequent side reaction at inclusion in combinations with a levodopa. Arterial hypotension can arise in an initiation of treatment, especially if pramipeksol it is titrated too quickly. Infections and invasions: infrequently – pneumonia. From an endocrine system: infrequently – disturbance of secretion of antidiuretic hormone. From mentality: often – a sleep disorder, symptoms of disorder of control over motivation and compulsive behavior, confusion of consciousness, a hallucination, insomnia, infrequently – overeating, persuasive desire to make purchases, a hyperphagia, hyper sexuality, libido disorders, paranoia, morbid attraction to gamblings, concern, nonsense, a delirium, is rare – a mania. From nervous system: very often – dizziness, dyskinesia, drowsiness, is frequent – a headache, infrequently – amnesia, a hyperkinesia, a sudden attack of drowsiness, faints. From organs of sight: often – a disorder of vision, including a diplopia, illegibility of sight and deterioration in visual acuity. From a cardiovascular system: often – arterial hypotension, infrequently – heart failure. From a respiratory system: infrequently – an asthma, a hiccups. From digestive system: very often – nausea, it is frequent – a constipation, vomiting. From skin and hypodermic cellulose: infrequently – hypersensitivity, an itching, rash. General disorders: often – increased fatigue, peripheral hypostases. Researches: often – degrowth of a body, including a loss of appetite, infrequently – increase in body weight. Restless legs syndrome. Patients with restless legs syndrome at treatment pramipeksoly the most frequent side reactions (& gt, 5%) had a nausea, a headache, dizziness and increased fatigue. Nausea and increased fatigue were more often observed at women in comparison with men at treatment pramipeksoly. Infections and invasions: infrequently – pneumonia. From an endocrine system: infrequently – disturbance of secretion of antidiuretic hormone. From mentality: often – a sleep disorder, insomnia, infrequently – symptoms of disorder of control over motivation and compulsive behavior, such as overeating, morbid attraction to visit of shops, hyper sexuality and morbid attraction to gamblings, confusion of consciousness, a mania, hallucinations, a hyperphagia, libido disorders, paranoia, concern, nonsense, a delirium. From nervous system: often – dizziness, a headache, drowsiness, infrequently – amnesia, dyskinesia, a hyperkinesia, a sudden attack of drowsiness, faints. From organs of sight: often – a disorder of vision, including a diplopia, illegibility of sight and deterioration in visual acuity. From a cardiovascular system: infrequently – heart failure, arterial hypotension. From a respiratory system: infrequently – an asthma, a hiccups. From digestive system: very often – nausea, it is frequent – a constipation, vomiting. From skin and hypodermic cellulose: infrequently – hypersensitivity, an itching, rash. General disorders: often – increased fatigue, infrequently – peripheral hypostases. Researches: infrequently – degrowth of a body, including a loss of appetite, increase in body weight. Contraindications – hypersensitivity to a pramipeksol or to any other component of drug. – children’s and teenage age up to 18 years Medicinal interactions Linking with proteins of plasma. Pramipeksol contacts proteins of plasma very slightly (& lt, 20%) and has low biotransformation. Therefore interaction with other drug which influences binding of proteins of plasma or elimination by biotransformation is improbable. As anticholinergics eliminirutsya mainly by metabolism in a liver, interaction is improbable. Interaction with anticholinergics was not investigated. There is no pharmacokinetic interaction with selegiliny and a levodopa. Inhibitors/competitors of an active way of renal elimination. Cimetidinum reduces renal clearance of a pramipeksol approximately by 34% probably by suppression of a system of transport of cationic renal canalicular secretion. Drugs which suppress active renal canalicular secretion or eliminirutsya this way, such as Cimetidinum, amantadin, meksiletin, the zidovudine, Cisplatinum, quinine and procaineamide, can interact with pramipeksoly and lead to reduction of clearance of a pramipeksol. At simultaneous use of these medicines with the drug Pramiksol it is necessary to consider the possibility of a dose decline of a pramipeksol. A combination with a levodopa. At increase in a dose of the drug Pramiksol the levodopa dose decline is recommended to patients with Parkinson’s disease, and doses of other protivoparkinsonichesky means leave invariable. Because of potential additive impact it is necessary to show care if the patient applies other sedative medicines or alcohol in combination with pramipeksoly (see the sections Special Instructions, Features of Influence of Medicine on Ability to Run Vehicles and Other Potentially Dangerous Mechanisms and Side effects). Antipsychotic medicines. It is necessary to avoid simultaneous use of antipsychotic medicines with pramipeksoly (see the section Special Instructions) if antagonistic effects are possible. Special instructions Renal failure. Pramiksol, tablets, once with care patients appoint with a renal failure as pramipeksol it is allocated through kidneys. Prescribing of the drug Pramiksol is offered to patients with Parkinson’s disease and a renal failure in the reduced doses according to the section Route of Administration and Doses. Hallucinations. Hallucinations – the known side reactions of treatment by dopamine agonists and a levodopa. Patients need to be informed that there can be hallucinations (in most cases visual). Dyskinesia. At combination therapy with a levodopa at the progressing Parkinson’s disease the dyskinesia can develop at the beginning of drug Pramiksol titration. In that case the dose of a levodopa needs to be lowered. Sudden attack of drowsiness and drowsiness. Use of a pramipeksol is connected with drowsiness and episodes of a sudden attack of drowsiness, especially at patients with Parkinson’s disease. There were infrequent messages about a sudden attack of drowsiness during day activity, in certain cases – without understanding or the warning signs. In this regard patients need to be informed on need to be careful at control of motor transport or work with other mechanisms during the Pramiksol drug treatment. Patients with drowsiness and/or episodes of a sudden attack of drowsiness should abstain from driving and work with the equipment. Besides, it is necessary to consider the possibility of a dose decline or reduction of term of treatment. Because of potential additive impact it is necessary to show care if the patient applies other sedative medicines in a combination with pramipeksoly or takes alcohol (see the sections Medicinal Interactions, Features of Influence of Medicine on Ability to Run Vehicles and Other Potentially Dangerous Mechanisms and Side effects). Disorders of control over motivation and compulsive behavior. Patsiyentov it is necessary to control carefully concerning development of disorders of control over motivation. Patients and persons who look after them have to know that at treatment by dopamine agonists, including the drug Pramiksol symptoms of disorder of control over motivation, including morbid attraction to gamblings, increase in a libido, hyper sexuality, compulsive waste or purchase, overeating and compulsive consumption of food can be observed. At development of such symptoms it is necessary to consider the possibility of reduction the dose/termination of administration of drug. Mania and delirium. Patsiyen
ov it is necessary to control carefully concerning development of a mania and a delirium. Patients and persons who look after them have to know that the mania and a delirium can arise at the patients receiving therapy pramipeksoly. At development of such symptoms it is necessary to consider the possibility of decrease in the dose/termination of administration of drug. Serious cardiovascular illness. In a serious cardiovascular illness it is necessary to appoint drug especially carefully. Monitoring of arterial blood pressure, especially in an initiation of treatment, taking into account the general risk of the postural hypotension connected with dopaminergic therapy is recommended. Patients with mental disorders. Patients with mental disorders should be treated by dopamine agonists only in case the potential advantage of treatment exceeds risks. It is necessary to avoid simultaneous use of antipsychotic medicines with pramipeksoly. Antipsychotic malignant syndrome. The symptoms reminding an antipsychotic malignant syndrome were observed after sharp cancellation of dopaminergic treatment. Ophthalmologic inspection. Regular ophthalmologic inspection in case of a visual disturbance is recommended. Augmentation (strengthening of symptoms). Messages indicate that treatment of restless legs syndrome dopaminergic drugs can cause augmentation. Augmentation is shown by early emergence of symptoms in the evening (or even in the afternoon), strengthening of symptomatology and distribution of symptoms on upper extremities. Rhabdomyolysis. The only case of a rhabdomyolysis took place at patients with the progressing Parkinson’s disease at treatment pramipeksoly. At the patient observed the increased kreatinfosfokinaza level (SRK – 10.631 ME/l). Symptoms disappeared after the treatment termination. Children. Parkinson’s disease. Safety and efficiency of the drug Pramiksol for children (age up to 18 years) are not established. Justification of a possibility of use to children in Parkinson’s disease is not present. Restless legs syndrome. Use of the drug Pramiksol is not recommended to children (age up to 18 years) because of insufficient data on safety and efficiency. Turett’s syndrome. The drug Pramiksol should not be used to children (age up to 18 years) with Turett’s syndrome because of a negative ratio of advantage/risk for this disease. Use during pregnancy or feeding by a breast. Influence on pregnancy at women was not investigated. Pramiksol it is possible to apply during pregnancy only in case the potential advantage is more, than risk for a fruit. As the Pramiksol drug treatment suppresses prolactin secretion, reduction of a lactation is possible. Excretion of the drug Pramiksol in breast milk is not studied at women therefore drug is not recommended to be used during feeding by a breast. If it is impossible to avoid drug Pramiksol use, it is necessary to stop feeding by a breast. Researches of influence on fertility of the person were not conducted. Features of influence medicinal drug on ability to run vehicles and other potentially dangerous Pramiksol mechanisms can have considerable influence on ability to run motor transport or to work with other mechanisms. Appearance of hallucinations or drowsiness is possible. Patients with drowsiness and/or episodes of a sudden attack of drowsiness should abstain from driving and potentially dangerous activity when deterioration in attention increases risk of serious damage or a fatal consequence during use of a pramipeksol. The overdose Clinical experience of considerable overdose is absent. The expected side effects connected with a pharmakodinamichesky profile of dopamine agonist include nausea, vomiting, a hyperkinesia, hallucinations, excitement and arterial hypotension. Antidote at overdose by dopamine agonist is not established. In case of signs of excitement of the central nervous system it is possible to appoint neuroleptics. Treatment of patients with overdose can demand the general supporting measures together with gastric lavage, intravenous administration of liquid, use of activated carbon and control of the electrocardiogram. A form of release and packing On 10 tablets in blister strip packaging from a film of polyvinylchloride and printing aluminum foil of the varnished or aluminum foil and printing aluminum foil varnished. On the 3rd blister strip packagings together with the instruction for medical use in the state and Russian languages put in a cardboard pack. To Store storage conditions in original packing at a temperature not above 25 °C. To store out of children’s reach! Period of storage 2 years. Not to apply after an expiration date Prescription status According to the prescription LLC Pharm Start Producer. Ukraine, Kiev, I. Leps Blvd., 8. Holder of the registration certificate of LLC Pharm Start. Ukraine, Kiev, I. Leps Blvd., 8. The name, the address and a contact information (phone, the fax, e-mail) of the organization in the territory of the Republic of Kazakhstan, the accepting claim (offer) on quality of medicines from consumers and responsible for post-registration observation of safety of medicine: Atsino Kaz LLP, Republic of Kazakhstan, 050010, Almaty, Begalin St., 136 A Phone number: 8 (727-2) 91-61-51 Fax: 8 (727-2) 91-61-51
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