Atazanavir (Atazanavirum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Means for the treatment of HIV infection

Included in the formulation
  • Atazanavir Canon
    capsules inwards 
    CANONFARMA PRODUCTION, CJSC     Russia
  • Atazanavir-TL
    capsules inwards 
    TECHNOLOGY OF DRUGS, LTD.     Russia
  • Reatase®
    capsules inwards 
    Bristol-Myers Squibb Company     USA
  • Reatase®
    capsules inwards 
    Bristol-Myers Squibb Company     USA
  • Simanod
    capsules inwards 
    FARMASINTEZ, JSC (Irkutsk)     Russia
    • АТХ:

    J.05.A.E.   Protease Inhibitors

    J.05.A.E.08   Atazanavir

    Pharmacodynamics:

    Competitively inhibits the protease of the human immunodeficiency virus (HIV), leading to disruption of the gag-pol polypeptide cleavage by reverse transcriptase, integrases and proteases. Forms inactive viral particles that are unable to infect other cells. Inhibits UDP-glucuronyl transferase, as well as the isoenzyme CYP3A4, preventing the maturation of infected cells.

    Pharmacokinetics:

    Absorbed in the gastrointestinal tract, binds to plasma proteins up to 86%. Biotransformation in the liver.

    The half-life is 7 hours. If liver function is insufficient, up to 12 hours. Elimination with feces (up to 80%) and kidneys (up to 20%). Unchanged in the amount of 20% and 13% respectively.

    Indications:

    Active with HIV-1 and HIV-2. The drug is used in complex therapy.

    ICD-10

    I.B20-B24   Disease caused by the human immunodeficiency virus [HIV]

    Contraindications:

    Severe hepatic insufficiency.

    Individual intolerance.

    Carefully:Hepatic insufficiency of medium and mild degree, viral hepatitis B and C, pregnancy, diabetes mellitus.
    Pregnancy and lactation:

    Pregnancy and lactation: recommendations for FDA - Category B. At pregnancy it is applied on vital indications, at a lactemia - reception is counter-indicative.

    Dosing and Administration:

    It is taken orally, once a day for 400 mg.

    The highest daily dose: 400 mg.

    The highest single dose: 400 mg.

    Side effects:

    General reactions of the body: weakness, fever. Rarely - gynecomastia.

    Central nervous system: headache, peripheral neuropathy, insomnia. Rarely - cognitive disorders, depression.

    Musculoskeletal system: muscular atrophy, arthralgia.

    Digestive system: jaundice, diarrhea, indigestion, nausea and vomiting. Less often - necrotic pancreatitis (up to a lethal outcome).

    Urinary system: dysuric disorders, rarely - hematuria, proteinuria.

    Skin: itching, rash. Rarely, alopecia.

    Allergic reactions.

    Overdose:

    Anxious state, drowsiness, convulsive syndrome, indomitable vomiting.

    Treatment is symptomatic.

    Interaction:

    Rifapicin reduces the effectiveness of atanasivir up to 90%.

    Ritonavir enhances the action of anatasivir.

    Simultaneous use with indinavir leads to hyperbilirubinemia.

    Reduces the effectiveness of saquinavir with simultaneous admission.

    Slows the metabolism of irinotecan, increasing its toxicity.

    Strengthens the action of lidocaine, amiodarone, quinidine, diltiazem.

    Strengthens the effect of warfarin, which can lead to bleeding.

    Absorption of the drug is significantly reduced with the use of antacids, due to a decrease in the acidity of gastric juice.

    Proton pump inhibitors and histamine H blockers2-receptors reduce the concentration of atanasivir in the blood plasma, reducing the effectiveness of the drug.

    Reduces the effectiveness of hormonal contraceptives containing estradiol.

    Special instructions:

    Monitoring the number of CD4 + lymphocytes, indices of peripheral blood, viral load, cholesterol concentration, glucose, triglycerides, blood bilirubin, activity alanine aminotransferase and aspartate aminotransferase, alkaline phosphatase, amylase, lipase.

    If necessary, the appointment with nifedipine, vertapamil, flodipine,nicardipine it is necessary to titrate the dose of calcium channel blockers under the control of the electrocardiogram.

    Instructions
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