Pramipexole
When ATH:
N04BC05
Characteristic.
White or off-white powdery substance. Its melting occurs in the range from 296 ° C to 301 °C and is accompanied by decomposition. Solubility in water is more 20%, in methanol - about 8%, in ethanol - about 0,5%, practically insoluble in dichloromethane.
Pharmacological action.
Antiparkinsonian.
Application.
Parkinson's Disease.
Contraindications.
Hypersensitivity.
Restrictions apply.
Renal failure, arterial hypertension, cognitive impairment, pregnancy, lactation.
Pregnancy and breast-feeding.
Maybe, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies on the use during pregnancy has not been carried out).
Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)
At the time of treatment should stop breastfeeding (data on the penetration of breast milk in humans are absent).
Side effects.
From the nervous system and sensory organs: asthenia, drowsiness / insomnia, hallucinations, delirium, amnesia, confusion, dizziness, anxiety, depression, dysphagia, dystonia, akathisia, thought disorders, suicidal thoughts, extrapyramidal syndrome, dyskinesia, tremor, giposteziya, gipokineziya, myoclonus, ataxia, dystaxia, diplopia, cycloplegia, conjunctivitis, impaired hearing; in a few cases (with the rapid dose decrease or abrupt cancellation) - neuroleptic malignant syndrome (hyperthermia, muscle rigidity, disturbance of consciousness, vegetative lability).
Cardio-vascular system and blood (hematopoiesis, hemostasis): orthostatic hypotension, tachycardia, arrhythmia.
From the respiratory system: breathlessness, rhinitis, pharyngitis, sinusitis, flu-like symptoms, increased cough.
From the digestive tract: nausea, vomiting, dyspepsia, flatulence, diarrhea, dry mouth, anorexia, constipation.
On the part of the musculoskeletal system: hypertonus muscles, cramps in the muscles of the legs, vellication, myasthenia, arthritis, ʙursit.
Other: fever; peripheral edema, Sweating, increased intraocular pressure, decreased libido, impotence, weight loss; increased urination, urinary tract infection; pain syndrome, incl. chest pain, abdominal pain, pain in the lumbosacral spine, pain in the neck; voice alteration; Increase CPK activity; allergic reactions.
Cooperation.
Increases Cmax levodopы of 40% and reduces the time to achieve a 2,5 to 0,5 no. Cimetidine uvelichivaet AUC pramipexole (on 50%) and T1/2 (on 40%). At the same time taking drugs, which are secreted by the cationic transport system kidney (ranitidine, diltiazem, triamterene, verapamil, quinine and quinidine and others.) Pramipexole clearance is reduced by about 20%. Dopamine antagonists, incl. neuroleptics (fenotiazinы, butyrofenonы, tïoksantenı) metoclopramide, may reduce the effectiveness of.
Overdose.
Treatment: gastric lavage, maintenance therapy - intravenous fluid administration, ECG monitoring; If signs of central nervous system excitation may be shown antipsychotics (fenotiazinы, butyrofenonы). Spetsificheskiy antidote unknown.
Dosing and Administration.
Inside, 3 once a day. Initial dose at any stage of Parkinson's disease - according to 0,375 mg / day. If necessary, increase the dose, but not more than once every 5-7 days (until the optimum therapeutic effect in view of side effects): 2-I'm a week of treatment - 0,75 mg / day, 3-I'm a week - 1,5 mg/day and beyond, increasing the dose by 0,75 mg per week to maximum - 4,5 mg / day. Maintenance dose - 1.5–4.5 mg/day 3 admission. When combined with levodopa dose of levodopa can be reduced.
In patients with renal insufficiency dose depends on creatinine clearance: the Cl creatinine more 60 mL/min-on 0,125 mg 3 once a day (maximum dose - according to 1,5 mg 3 once a day), 35–59 ml/min – by 0,125 mg 2 once a day (maximum - by 1,5 mg 2 once a day), 15–34 ml/min — 0,125 mg 1 once a day (maximum — 1,5 mg 1 once a day).
Precautions.
Patients should be warned about the risk of hallucinations (especially elderly patients), the possibility of orthostatic hypotension (at the beginning of the treatment or the dose is increased). Be wary appoint patients with kidney failure in history. Abolition of pramipexole recommended gradually (during 1 Sun). Should not be used during the drivers of vehicles and people, skills relate to the high concentration of attention.