INDINAVIR (Indinavir).

     (? R? S, 2S)? Benzil-2- - (tert butilkarbamoil)? oksi-N--[(1S, 2R) -2 - oksi-1- indanil] -4 - (3-piridilmetil ) -1 - piperazinvaleramid.

     Synonym : Kriksivan, Crixivan.

     Available in the idea sulfate.

     White or colourless crystalline powder. Well soluble in water.

    The structure and operation is a relatively new (mid-1990). Antiviral drug used to treat HIV infection. In the operation differs from the anti-NUCLEOSIDE (see Zidovudin). If recent inhibit reverse transcriptase of HIV, the indinavir-protease involved in the assembly of viral viriona (who believe the transport of the virus) out of the infected cells. Diluted ingibiruet HIV-1 protease (to a lesser degree HIV protease-2).

     Features of the mechanisms of indinavir and NUCLEOSIDE an opportunity to enhance therapeutic effect when combined application for the treatment of HIV infection.

     Once inside the shock is rapidly absorbed (if dietary intake is slowing stripping), C max of 40-50 min, T? 2-h; metabolised in the liver with the formation and oxidation products Algae with glyukuronovoy acid appears mostly in the form of metabolites in urine and faeces.

     Applied with HIV infection in adults, including in the case of resistance to antiretroviral drugs, inhibiting reverse transcriptase.

      Is inside capsules (for 1 hour before or 2 hours after meals, squeezed water) to 0.8 g every 8 h (2.4 g / day).

     When expressed violations of liver and kidney dose of indinavir reduced to 0.6 g three times a day.

     Often appointed with zinovudinom and lamivudine or similar (anti-retroviral) drugs (AZT for 0.2 g three times a day, lamivudine, for 0.15 g, 2 times a day, for ribafutin - 0.4 g 3 times day). Taking these drugs at intervals of not less than 1 hour between tricks indinavir.

     When using indinavir various possible side effects : fatigue, insomnia, dry mouth and skin, taste perversion, stomach pain, nausea, vomiting, diarrhoea, headache, dizziness, hematuria, kristalluriya, stone, proteinuriya, disruption of the liver, neutropenia, hyperglycemia, gipertriglitseridemiya and others.

     If the drug to women of child-bearing period should simultaneously apply effective contraception and pregnancy to take into account the risk to the foetus (ratio of benefits and risks "). Not recommended breast milk to feed the child during the mother's treatment indinavir.

     In cases of other LS should keep in mind that inducible enzyme tsitohroma P 450 (see Barbituraty) reduce its concentration in the blood.

     Product : capsules to 0.2 g (N. 360), 0.33 g (N. 135) and 0.4 g (N. 180).

     Storage : List B.

Materials allowed to copy only with the active hyperlink to the handbook of medicines