Tolcapone

Chemical name

3,4-Дигидрокси-4'-метил-5 -нитробензофенон

Gross

C14-H11-N-O5

Of drugs

The drugs - противопаркинсоничес кое. Lock катехол-О-метилтрансф еразу and biotransformatia down at the same time appointed levodopa, stabilizing its content in the plasma and increasing the therapeutic effect (down education 3 -метокси-4-гидрокси-L-ф��нилаланина and thus decreases the likelihood of side). If ingestion is rapidly absorbed (food slows absorption). C_mah achieved through two hours (at the dose of 100 mg or 200 mg three times a day at 3 µ g / ml and 5 µ g / mL, respectively). Absolute bioavailability of 65% relative-80-90%. Plasma proteins (mainly albuminami) related to (over 99.9%). Poor penetrates the tissues (volume distribution is 9 litres). Metabolised by the kongugirovania glukuronova acid 20/23 (with the participation of катехол-О-метилтрансф еразы becoming 3-o-metiltolcapon) or oxidation (zitohroma P450 3A4 and P450 2A6) with the formation of primary alcohol, and then carbokislota. Neither can recover before amine followed N-azetilirovaniem. T_1/2 ultimate phase-2 p.m. 60% return with urine (in the form of unmodified 0.5% dose, and in the form of biotransformation products), 40% from faeces. System Cl-7 l / h. In moderately expressed cirrhosis of the liver Cl reduced by 50%, with a concentration tolkapona plasma doubled. When used together with levodopa increases its relative bioavailability (twice), lengthens the terminal T_1/2 or change C_mah plasma. The starting from the first reception, the best therapeutic effect achieved with the dose of 100-200 mg.

Indications

Parkinson's disease (with the drug levodopa / benserazida and levodopa / carbidopa).

Contraindications

Hypersensitivity, simultaneous selective MAO inhibitors, pregnancy, breast-feeding (at the time of treatment should stop breastfeeding).

Side-Effects

Insomnia, psoriasis; Following a sharp decline dose or lifting противопаркинсоничес ких Drug-neirolepticeski malignant syndrome (muscle rigidity, temperature increases, changes in mental state); nausea, anorexia, diarrhoea, increasing transaminaz liver.

Patient interaction

Against the backdrop of levodopa, carbidopa, benserazida greatly reduces the plasma concentration 3-метокси-4-гидрокси-L-ф енилаланина.

Overdosing

Symptoms : dizziness, nausea, Rvota.lechenie : recommended hospitalization and supporting activities (Hepatology little effective).

Precautions

Be wary appoint patients with acute human liver and kidneys. Prior to the start of treatment and every 6 weeks for the first six months of therapy to monitor the level transaminaz; In ALT activity more than 10 times larger than the upper limit of the rules or develop jaundice, a product hereof; Persistent and severe diarrhea also calls for the end of the reception. Against the backdrop to the increase in the daily dose of levodopa.

Dosing and Administration

Inside, coupled with all forms of drug levodopa / benserazida and levodopa / carbidopa. Initial dose is 100 mg three times a day (by combining the first reception with the first dose of levodopa that day, and then at 6 and 12 h). After selection levodopa dose, and in the absence of side effects tolkapona dose increase to 200 mg three times a day. Supporting dose-200 mg three times a day, excluding patients with human liver moderate.

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