Indinavir is an HIV protease inhibitor used in combination with other medicines to manage human immunodeficiency virus (HIV).
Other names for this medication: Avirodin, Avural, Ciplaindivan, Cirixivan, Compound j, Crixivan, Elvenavir, Flamind, Forli, Virixit, Virotec .
Pharmachologic effect:
Antiviral drug, a specific inhibitor of HIV proteases. Active against HIV – inhibits HIV replication, incl. with resistance to reverse transcriptase inhibitors. By binding to the active site, it inhibits the HIV-1 protease (and to a lesser extent the HIV-2 protease), which participates in the assembly of the viral virion (which is considered the transport form of the virus) at the exit from the affected cell. As a result of the inhibition of HIV protease activity, inactive virus particles are formed.
Pharmacokinetics:
After ingestion, the fasting is quickly absorbed (high-calorie foods, especially rich in fats and proteins, slow down absorption, reduce Cmax and AUC). TCmax – 45-50 min. Communication with plasma proteins – 60%. It is metabolized in the liver with the participation of cytochrome CYP3A4, CYP3A5 and CYP3A7 with the formation of 6 oxidation products and one conjugate with glucuronic acid. It is an inhibitor of isoenzymes CYP3A4, CYP3A5 and CYP3A7. T1 / 2 – 1.5-2 hours. Not cumulated. About 80% of the accepted dose is excreted as metabolites (approximately in the same ratio by the kidneys and with bile), and 20% is excreted by the kidneys unchanged. In patients with liver failure, an increase in T1 / 2 to 2.8 h.
Indications:
Diseases caused by HIV-1 in adult patients: not previously treated with antiretroviral drugs (in combination with antiretroviral drugs or as monotherapy at the beginning of treatment of patients who are clinically inappropriate to administer nucleoside analogues); previously received antiretroviral drugs and having contraindications or resistance to drugs – reverse transcriptase inhibitors (in combination with antiretroviral drugs or as monotherapy).
Contraindications:
Hypersensitivity, pregnancy, lactation period. C caution. Hemophilia, liver failure, children and old age (safety and efficacy have not been established).
Side effects:
On the part of the digestive system: aphthous stomatitis, abdominal pain, heartburn, diarrhea, dry mouth, dyspepsia, flatulence, nausea, vomiting, taste disturbance, increased activity of liver transaminases, cholecystitis (including calculous), cholestatic hepatitis , hyperbilirubinemia (total bilirubin more than 2.5 mg / dL due to indirect bilirubin). Nervous system disorders: asthenia, dizziness, headache, hypoesthesia, sleep disturbances (drowsiness), nervousness, depression, paresthesias, tremor, peripheral polyneuropathy. On the part of the musculoskeletal system: arthralgia, myalgia, muscle cramps, stiff muscles, chest pain. On the part of the respiratory system: cough, respiratory failure, sinusitis, upper respiratory tract infections, pneumonia. On the part of the urinary system: dysuria, nocturia, nephrourolithiasis, pain in the kidney area, hematuria, proteinuria, hypercreatininemia. For the skin: dry skin, itching, dermatitis (including contact, seborrheic). From the side of blood-forming organs and the hemostatic system: spontaneous bleeding in patients with hemophilia A and B (who received protease inhibitors). Other: lymphadenopathy, fever, increased sweating, flu-like syndrome, hemolytic anemia.
Interaction:
Enhances (mutually) the effect of reverse transcriptase inhibitors. Increases rifabutin concentration. With the simultaneous appointment of zidovudine and indinavir, AUC indinavir increases by 13%, zidovudine – by 17%; with simultaneous use of indinavir, zidovudine and lamivudine, the AUC of indinavir does not change, the AUC of zidovudine is increased by 36%, and the AUC of lamivudine is reduced by 6% (dose adjustment is not required). Decreases the metabolic rate and increases the toxicity of terfenadine, astemizole and cisapride, midazolam and thiazolide, which can lead to the occurrence of cardiac arrhythmias (simultaneous administration of drugs is not recommended). Ketoconazole increases the concentration of indinavir, and rifampicin reduces. In combination therapy with didanosine, drugs are taken on an empty stomach with an interval between doses of 1 hour.
Special instructions:
To ensure adequate hydration and prevention of nephroluritiasis, 1.5-2 liters of fluid should be drunk per day. During treatment, it is recommended to control the activity of amylase, ALT, AST, the concentration of bilirubin and glucose in plasma. Care should be taken when prescribing to patients with hemophilia (isolated cases of spontaneous bleeding of unknown etiology have been reported).
The information provided in this section is intended for medical and pharmaceutical professionals and should not be used for self-medication. The information is given for familiarization and can not be considered as official.
