Pramipexole
Pramipexole: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Pramipexole
ATX code: N04BC05
Active ingredient: pramipexole (pramipexole)
Manufacturer: Synthon Hispania (Spain), Synthon (Netherlands), Pharmzashchita NPC (Russia)
Description and photo update: 2018-21-11
Prices in pharmacies: from 171 rubles.
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Pramipexole is a drug with antiparkinsonian action.
Release form and composition
Pramipexole dosage form - tablets: almost white or white; 0.25 and 0.5 mg - flat, oblong, on one side there is a wide risk, on the other - engraving "P9AL 0.18" or "P9AL 0.35", respectively; 1 or 1.5 mg - round biconvex shape, on both sides of the risk, on one side engraving "P9AL 0.7" or "P9AL 1.1", respectively (in a cardboard box 3 blisters of 7 or 10 tablets).
Composition of 1 tablet:
- active substance: pramipexole dihydrochloride monohydrate - 0.25; 0.5; 1 or 1.5 mg (pramipexole - 0.18; 0.35; 0.7 or 1.1 mg);
- auxiliary components (0.25 / 0.5 / 1 / 1.5 mg): magnesium stearate - 1.52 / 3.05 / 3.05 / 4.57 mg; pregelatinized starch - 39.9 / 79.8 / 79.8 / 119.7 mg; colloidal silicon dioxide - 1.17 / 2.33 / 2.33 / 3.5 mg; mannitol - 61 / 121.99 / 121.49 / 182, 24 mg; povidone (K-29/32) - 1.17 / 2.33 / 2.33 / 3.5 mg.
Pharmacological properties
Pharmacodynamics
Pramipexole is a dopamine receptor agonist. Possesses high specificity and selectivity. Binds to D 2 -dopamine receptors, the most pronounced affinity is manifested for D 3 -dopamine receptors.
The use of the drug helps to reduce the deficit of motor activity in Parkinson's disease, which is due to the stimulation of dopamine receptors in the striatum.
The main properties of pramipexole:
- inhibition of dopamine synthesis, release and metabolism;
- ensuring the protection of dopaminergic neurons from degeneration, which occurs as a response to methamphetamine neurotoxicity or ischemia;
- decrease in prolactin secretion (it is dose-dependent).
Pharmacokinetics
The absorption of pramipexole is fast and occurs in full. Food intake slows down the rate of absorption (does not affect the total volume).
Absolute bioavailability - more than 90%, Cmax (maximum concentration of the substance) in blood plasma is achieved in 60-180 minutes.
The substance is characterized by linear kinetics and relatively little variability in concentration between individual patients.
It undergoes biological transformation and binds to plasma proteins to a very small extent (less than 20%), the volume of distribution is 400 liters.
It is slightly metabolized. Most of the dose (about 90%) is excreted through the kidneys (unchanged - 80%), less than 2% is excreted through the intestines. The total clearance of pramipexole is approximately 500 ml / min, renal clearance is 400 ml / min. T 1/2 (half-life) varies from 8 hours (in young patients) to 12 hours (in elderly patients).
Indications for use
According to the instructions, Pramipexole is prescribed for the symptomatic treatment of the following diseases / conditions:
- idiopathic Parkinson's disease in adults (as monotherapy or in combination with levodopa) in the late stage of the disease with weakening of the effects of levodopa or their instability and the appearance of fluctuations in the therapeutic effect (fluctuations of the end of dose or "on-off");
- idiopathic restless legs syndrome.
Contraindications
Absolute:
- age up to 18 years;
- lactation period;
- individual intolerance to the components of the drug.
Relative (Pramipexole is prescribed under medical supervision):
- renal failure;
- arterial hypotension;
- psychotic disorders;
- visual impairment;
- diseases of the cardiovascular system in severe course;
- pregnancy.
Instructions for the use of Pramipexole: method and dosage
Pramipexole is taken orally with a small amount of water, regardless of the meal.
The daily dose should be divided into three equal parts.
In the first week of treatment, a single dose is 0.125 mg. Until the best therapeutic effect is achieved, the dose is increased to 0.25 mg (second week of use) and 0.5 mg (from 15 to 21 days of therapy).
In the future, if necessary, once a week, the daily dose is increased by 0.75 mg. The maximum daily dose is 4.5 mg.
It should be borne in mind that when a dose is taken above 1.5 mg per day, the incidence of drowsiness increases.
With maintenance therapy, the dose should be in the range of 0.375–4.5 mg per day. In both early and late stages of Parkinson's disease, Pramipexole is effective starting from a daily dose of 1.5 mg. The dose change depends on the patient's response to treatment and the occurrence of adverse reactions. At the same time, it is possible that in some patients, a dose of more than 1.5 mg per day may have an additional therapeutic effect, especially in the late stage of the disease.
Pramipexole should be withdrawn gradually - 0.75 mg per day until complete withdrawal, since a sudden cessation of therapy can lead to the appearance of neuroleptic malignant syndrome.
The dose of the drug during initial therapy in patients with renal insufficiency is determined by CC (creatinine clearance):
- 20-50 ml / min: 2 times a day, 0.125 mg;
- less than 20 ml / min: 1 time per day, 0.125 mg.
If renal function decreases during maintenance therapy, then the daily dose of Pramipexole is reduced by the same percentage by which the CC decreases. With a CC of 20-50 ml / min, the daily dose can be divided into two doses, with CC less than 20 ml / min, the drug is taken once a day.
When conducting combination therapy, as the dose of Pramipexole is increased, the dose of levodopa should be adjusted to avoid excessive dopamine stimulation.
The recommended starting dose for symptomatic treatment of idiopathic restless legs syndrome is 0.125 mg once daily at bedtime for 2-3 hours. If it is necessary to prescribe additional symptomatic therapy, the dose of Pramipexole can be increased to reach a maximum of 0.75 mg (every 4-7 days to 0.25; 0.5 and 0.75 mg, respectively).
The therapeutic effect should be assessed after 3 months of using the drug. Gradual withdrawal of therapy is not required. However, the possibility of recurrence of symptoms cannot be ruled out. In clinical studies, after a sharp discontinuation of Pramipexole, only 10% of cases showed signs of worsening of symptoms, and a violation can occur after any dose.
Side effects
Adverse reactions usually appear at the beginning of the course of therapy, with prolonged use of the drug, they disappear.
The severity of disorders and the frequency of their development are reversible and dose-dependent.
The expected side effects may be related to the doses used and the pharmacodynamic profile of the drug. These include nausea, vomiting, hyperkinesia, hallucinations, agitation, and orthostatic hypotension. A decrease in blood pressure can be observed in some patients at the beginning of therapy, especially if the dose is titrated too quickly.
In Parkinson's disease, a sharp dose reduction / withdrawal of Pramipexole can lead to the development of neuroleptic malignant syndrome. When taken simultaneously with levodopa, dyskinesia was recorded as an adverse reaction.
The incidence of adverse reactions (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01%, including individual messages - very rare).
Parkinson's disease:
- invasions and infections: infrequently - pneumonia and other infections of the upper / lower respiratory tract;
- endocrine system: infrequently - violation of the secretion of antidiuretic hormone;
- nervous system: very often - dizziness, dyskinesia, drowsiness; infrequently - amnesia, hyperkinesia, sudden falling asleep, fainting;
- digestive system: very often - nausea; often - vomiting, constipation;
- cardiovascular system: often - lowering blood pressure; infrequently - heart failure;
- respiratory system: infrequently - hiccups, dyspnea;
- psyche: often - hallucinations, amnesia, abnormal dreams, behavior disorder (symptoms of compulsive / impulsive actions), confusion, insomnia; infrequently - compulsive overeating, pathological shopping (an obsessive desire to shop), hypersexuality, paranoia, pathological craving for gambling, delirium, impaired libido, anxiety;
- subcutaneous tissue and skin: infrequently - itching, rash;
- organ of vision: often - visual impairment, including diplopia, decreased clarity of perception / visual acuity;
- general disorders: often - peripheral edema, fatigue;
- violations that were recorded during special studies: often - a decrease in body weight, a decrease in appetite; infrequently - an increase in body weight.
Idiopathic Restless Legs Syndrome:
- psyche: often - insomnia, abnormal dreams; infrequently - behavioral disturbances (symptoms of compulsive / impulsive actions), pathological craving for gambling, delirium, confusion, hyperphagia, hypersexuality, hallucinations, libido disorders, anxiety, paranoia;
- infections and infestations: infrequently - pneumonia and other infections of the upper / lower respiratory tract;
- endocrine system: infrequently - violation of the secretion of antidiuretic hormone;
- nervous system: often - dizziness, drowsiness, headache, fatigue; infrequently - sudden falling asleep, dyskinesia, amnesia, hyperkinesia, fainting;
- digestive system: very often - nausea; often - vomiting, constipation;
- cardiovascular system: infrequently - lowering blood pressure; infrequently - heart failure;
- respiratory system: infrequently - dyspnea, hiccups;
- skin and subcutaneous tissue: infrequently - itching, rash and other symptoms of hypersensitivity;
- organ of vision: infrequently - visual impairment, including diplopia, decreased clarity of perception / visual acuity;
- general disorders: often - fatigue; infrequently - peripheral edema;
- violations that were recorded during special studies: infrequently - a decrease / increase in body weight, a decrease in appetite.
Overdose
Expected symptoms of overdose (typical for the pharmacodynamic profile of drugs related to dopamine receptor agonists): agitation, nausea, vomiting, hallucinations, hyperkinesia, decreased blood pressure.
There is no specific antidote. The effectiveness of hemodialysis has not been established.
In case of an overdose, symptomatic treatment is indicated, which involves gastric lavage, intake of activated charcoal and ECG monitoring. A 0.9% sodium chloride solution may be prescribed intravenously, and if signs of stimulation of the central nervous system appear, antipsychotics.
special instructions
Due to the likelihood of orthostatic hypotension, it is recommended to monitor blood pressure, especially at the beginning of use.
During therapy, patients and their caregivers should take into account the possibility of hallucinations (mainly visual) and confusion.
When combined therapy with levodopa in the late stages of Parkinson's disease, dyskinesia may appear at the initial stage of dose selection (the dose of levodopa should be reduced).
While taking Pramipexole, cases of sudden falling asleep in active daytime were recorded, while drowsiness did not develop. In daily activities, falling asleep, sometimes without any antecedent signs, has been reported infrequently. Therapy may be accompanied by drowsiness, sometimes excessively expressed.
In cases of visual impairment, regular ophthalmic examination is recommended.
If there is a development of cases of pathological passion, hypersexuality and increased libido, it may be necessary to reduce the dose of Pramipexole, or to completely cancel it.
Patients with psychotic disorders should be prescribed the drug after a preliminary assessment of the balance of benefits and risks.
Against the background of the use of Pramipexole, the risk of primary heart failure may increase.
There is evidence that patients' condition worsens during the treatment of restless legs syndrome (earlier onset of symptoms in the evening or even in the daytime, increased severity and spread to the upper limbs).
In cases of severe cardiovascular pathologies, the appointment of Pramipexole requires special care. Blood pressure monitoring is recommended.
While taking Pramipexole, there is a decrease in the secretion of prolactin, an increase in the activity of creatine phosphokinase.
Influence on the ability to drive vehicles and complex mechanisms
During the period of taking Pramipexole, it is recommended to refuse to drive vehicles, which is associated with the likelihood of adverse reactions, including drowsiness and hallucinations.
Application during pregnancy and lactation
- pregnancy: therapy should be carried out under medical supervision and only in cases of extreme necessity, when the benefits of treatment for the mother significantly outweigh the risk for the fetus;
- lactation period: Pramipexole is contraindicated.
Pediatric use
Treatment with Pramipexole in patients under 18 years of age is contraindicated.
With impaired renal function
Pramipexole against the background of renal failure should be used under medical supervision.
Drug interactions
Possible interactions:
- levodopa: it is recommended to reduce its dose, and the dose of other antiparkinsonian drugs should be maintained at a constant level when the dose of pramipexole is increased;
- antipsychotics: possible antagonistic action; combinations are recommended to be avoided;
- drugs with a sedative effect, alcohol: an additive effect is possible; the combination requires caution;
- inhibitors / competitors of the active renal route of excretion: renal clearance of pramipexole decreases; during the period of combined use, the appearance of signs of dopamine overstimulation should be monitored, the dose of pramipexole should be reduced;
- dopamine receptor blockers: metoclopramide, derivatives of butyrophenone, phenothiazine, thioxanthene: the effectiveness of treatment is reduced.
Analogs
Pramipexole analogs are Pramipexol-Teva, Mirapex, Mirapex PD.
Terms and conditions of storage
Store at temperatures up to 25 ° C in a place protected from light. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Pramipexole
According to reviews, Pramipexole is an effective drug used both in monotherapy and as part of complex treatment. It is noted that with Parkinson's disease, the rate of its progression slows down. Also, therapy is prescribed to correct unexpressed depressive symptoms.
Of the shortcomings, they point to the development of side reactions, manifested in the form of dizziness, slight anxiety, dyspepsia, flatulence, xerostomia, and in some cases, diarrhea.
The price of Pramipexole in pharmacies
The approximate price of Pramipexole for 30 tablets of 0.25 mg, 1 mg or 1.5 mg is 170–220 rubles, 515–867 rubles. or 1329 rub. respectively.
Pramipexole: prices in online pharmacies
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Drug name Price Pharmacy |
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Pramipexole 0.25 mg tablets 30 pcs. 171 r Buy |
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Pramipexole 1 mg tablets 30 pcs. RUB 499 Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
