Pharmacological Effects Entacapone:
Entacapone Antiparkinsonian agent, used in conjunction with levodopa. Reversible dose-dependent manner inhibits COMT mainly in peripheral tissues. Prevents the metabolic destruction of levodopa and its transformation into 3-O-methyldopa, which leads to increased bioavailability and increase the number of levodopa reaching the brain. Increases the “inclusion” of 16%, while “off” – at 24%.
Indications Entacapone:
As part of therapy with levodopa + carbidopa and levodopa + benserazide: Parkinson’s disease and Parkinson’s syndrome (with low efficiency of the above-mentioned combined drugs).
Contraindications Entacapone:
Hypersensitivity, pregnancy, lactation, hepatic insufficiency, pheochromocytoma, simultaneous use of MAO inhibitors, neuroleptic malignant syndrome and / or non-traumatic rhabdomyolysis (including history). C care. Age 18 years.
Side effects Entacapone:
Nausea, vomiting, constipation or diarrhea, dry mouth, abdominal pain, hyperkinesis, tremor, dizziness, headache, insomnia, unusual fatigue, hallucinations, increased sweating, muscle cramps calf muscles, disorientation, “nightmarish” dream, orthostatic hypotension, anemia , the decline in hematocrit, eritropeniya; increased activity of liver transaminases and CPK. Very rarely: paradoxical enhancement phenomena of parkinsonism, severe dyskinesia or neuroleptic malignant syndrome, which manifested hyperthermia, movement disorders (rigidity, myoclonus, tremor), changes of mind and consciousness (excitation, disorientation, coma), dysfunction of autonomic nervous system (tachycardia, unstable BP), rhabdomyolysis.
Dosage and administration Entacapone:
Oral, 200 mg (regardless of the meal) together with each dose of levodopa + carbidopa or levodopa + benserazide. To reduce the dopaminergic side effects of levodopa (including dyskinesia, nausea, vomiting and hallucinations), in the first days and weeks after initiation of therapy entacapone shall adjust the dosage regimen of levodopa (daily dose reduced by 10-30%, increasing the intervals between doses and / or loss of a single dose). In the event of termination of treatment entacapone, in order to achieve adequate control of symptoms of Parkinson’s disease, it is necessary to adjust the dosing regimen other antiparkinsonian drugs, particularly levodopa.
Special instructions Entacapone:
Entacapone is always used as an additional tool to the treatment of levodopa (contraindications and warnings are available to the appointment of levodopa should be considered in the treatment of entacapone). Under the influence of entacapone levodopa bioavailability in the application of levodopa + benserazide increased slightly more (5-10%) than with levodopa + carbidopa. In this regard, early treatment of patients receiving levodopa + benserazide, you may need a more substantial reduction in levodopa dose. When CRF is not necessary to modify the dosing regimen (only in patients on hemodialysis, the interval between doses of the drug increase). Most of the adverse effects caused by entacapone relate to increased dopaminergic activity and are usually observed at the beginning of treatment. At lower doses of levodopa reduced the severity and frequency of occurrence of these phenomena. Under the influence of entacapone urine can acquire a reddish-brown (the clinical significance has not). Abolition of entacapone have been slow, if necessary, increase the dose of levodopa. During the period of treatment should refrain from activities potentially hazardous activities that require increased attention and rapid physical and mental reactions.
Interaction Entacapone:
Alter the metabolism and enhances the action of drugs metabolised by COMT (including rimiterol, isoprenaline, epinephrine and norepinephrine, dopamine, dobutamine, alpha-methyldopa and apomorphine). Entacapone in the digestive tract can form chelates with Fe (time interval between administration of at least 2-3 hours). Compatible with imipramine, moclobemide, selegiline (daily dose of the latter must not exceed 10 mg). Not recommended for concomitant use with MAO inhibitors-A, tricyclic antidepressants, norepinephrine reuptake inhibitors (including desipramine, maprotiline, venlafaxine).
