Telaprevir (Telaprevir)

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

Antiviral drugs (excluding HIV)

Included in the formulation
  • Insivo
    pills inwards 
    Johnson & Johnson, LLC     Russia
    • АТХ:

    J.05.A.E.11   Telaprevir

    Pharmacodynamics:

    The protease inhibitor NS3 / 4A of the hepatitis C virus, involved in viral replication. The blockade of the viral protease leads to a disruption in the maturation of viral particles of the hepatitis C virus of genotypes 1a and 1b.

    Pharmacokinetics:

    After oral administration, it is completely absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 4 hours. The connection with plasma proteins is 79%.

    Therapeutic effect develops after the reception. Metabolism in the liver.

    The half-life is 4-4.7 hours. Elimination with feces.

    Indications:

    It is used in complex therapy with ribavirin and peginterferon alfa for the treatment of chronic hepatitis C of genotype 1.

    ICD-10

    I.B15-B19.B18.2   Chronic viral hepatitis C

    Contraindications:

    Individual intolerance, children under 18 years of age (efficacy and safety not established).

    Carefully:

    Elderly (over 65 years of age), severe renal failure.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. Contraindicated in pregnancy and during lactation, as well as for men during pregnancy partners.

    Dosing and Administration:

    Inside, 750 mg every 8 hours during a meal.

    The highest daily dose: 2250 mg.

    The highest single dose: 750 mg.

    Side effects:

    Central and peripheral nervous system: faint.

    Circulatory system: peripheral edema.

    Hematopoietic system: anemia, lymphopenia, thrombocytopenia, and leukopenia.

    Respiratory system: shortness of breath.

    Digestive system: diarrheal phenomena, diarrhea.

    Endocrine system: hypothyroidism.

    Sense organs: rarely - retinopathy.

    Dermatological reactions: rash, photosensitivity reactions.

    Allergic reactions.

    Overdose:

    Cases of overdose are not described.

    Treatment is symptomatic.

    Interaction:

    Rifampicin reduces the effectiveness of telaprevir up to 90%.

    Ritonavir potentiates the action of telaprevir.

    Simultaneous use with indinavir leads to hyperbilirubinemia.

    Reduces the effectiveness of saquinavir with simultaneous admission.

    Slows the metabolism of irinotecan, increasing its toxicity.

    Potentiates 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 antacid agents (due todecrease in acidity of gastric juice).

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

    Reduces the effectiveness of hormonal contraceptives containing estradiol.

    Special instructions:

    It is not used as a monotherapy.

    If it is necessary to appoint with nifedipine, verapamil, felodipine, nicardipine, it is necessary to titrate the dose of calcium channel blockers under ECG control.

    Instructions
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