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CRIXIVAN ( Indinavir )

CRIXIVAN ( Indinavir ). Mr.Somjed Sahasitiwat ( Clinical group ). What is CRIXIVAN . CRIXIVAN ™ is the trade name of Indinavir sulfate, member of PI. It’s a white to off-white , hygroscopic , crystalline powder , MW. is 711.88 Is an oral capsule used for treatment of HIV.

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CRIXIVAN ( Indinavir )

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  1. CRIXIVAN ( Indinavir) Mr.Somjed Sahasitiwat ( Clinical group )

  2. What is CRIXIVAN  • CRIXIVAN ™ is the trade name of Indinavir sulfate, member of PI. • It’s a white to off-white , hygroscopic , crystalline powder , MW. is 711.88 • Is an oral capsule used for treatment of HIV. • Present in 200 mg., 333 mg. and 400 mg.

  3. Microbiology • HIV protease is an enzyme required for proteolytic cleavage . • Indinavir binds to the protease active site and inhibits activity of enzyme • Prevents cleavage of viral polyproteins. • Formation of immature non-infectious viral particles

  4. Pharmacology • Rapidly absorbed in the fasted state , Tmax = 0.8 + 0.3 hr. • Meal with high calories,fat and protein reduction in AUC and Cmax. • Light meal is little or no change in AUC,Cmax or trough concentration

  5. Pharmacology • Approximately 60% bound to plasma proteins. • Excrete in feces 83 + 1% and urine 19 + 3% • Less than 20% excreted unchanged in urine • Half-life = 1.8 + 0.4 hours • Major metabolisms in P-450 (3A4)

  6. Pharmacology • Mild to moderate hepatic insufficiency . • Decreased metabolism of Indinavir. • 60% higher mean AUC • T1/2 increased to 2.8 + 0.5 hours

  7. Pharmacology • Renal insufficiency : pharmacokinetics have not been studied • Gender : comparable in men and women • Race : comparable in Caucasians and Blacks

  8. CRIXIVAN should not take with : • seldane ™ (terfenadine) , hismanal ™ (astemizole) • versed™ (midazolam) , halcion™ (triazolam) • propulsid ™ (cisapride) • ergot medications (Wigrane ™ and Cafegot ™ ) • Rifampin ( rifadin ™ ,rifamate ™ , rifater ™ or rimactane ™ ) potent inducer of P-450 ( 3a4 )

  9. Drugs you can take with CRIXIVAN • RETROVIR ™ ( zidovudine , AZT ) , EPIVIR ™ ( lamivudine .3TC ) , ZERIT ™ ( stavudine.D4t ) • isoniazid ( INH ) • BACTRIM ™ ( trimetroprim/sulfamethoxazole ) • DIFLUCAN ™ ( fluconazole )

  10. Drugs you can take with CRIXIVAN • BIAXIN ™ ( clarithromycin ) • ORTHO-NOVUM 1/35 ( oral contraceptive ) • TAGAMET ™ ( cimetidine ) • Methadone

  11. Drugs Requiring Dose Modification • Delaverdine • Efavirenz • Itraconazole , Ketoconazole • Rifabutin

  12. Indication and usage • In combination with antiretroviral agents is indicated for treatment of HIV infection

  13. Dosage and administration • Recommended dosage is 800 mg. Orally every 8 hr • Administered without food • Take with water 1 hr.before or 2 hrs. after meal • May be take with light meal • For adequate hydration drink at least 1.5 L./ 24 hr.

  14. Dose in drugs combination • Delavirdine • dose reduction of CRIXIVAN to 600 mg. Every 8 hr • Didanosine • should be take CRIXIVAN at least one 1 hr. apart on empty stomach

  15. Dose in drugs combination • Efavirenz • increase of CRIXIVAN to 1000 mg every 8 hr. • Itraconazole and Ketoconazole • reduction of CRIXIVAN to 600 mg every 8 hr.

  16. Dose in drugs combination • Rifabutin • reduction of rifabutin to half the standard dose • increase of CRIXIVAN to 1000 mg every 8 hr.

  17. Specials condition • Hepatic Insufficiency • mild to moderate hepatic insufficiency due to cirrhosis • dosage reduced to 600 mg every 8 hr.

  18. Specials condition • Nephrolithiasis • in addition to adequate hydration • who experience nephrolithiasis may include temporary interruption or discontinuation of therapy

  19. WARNING • Nephrolithiasishas occurred. • Adequate hydration is recommended . • Hemolytic anemia • appropriate measures for the treatment and discontinuation of CRIXIVAN

  20. WARNING • Hepatitis • majority of these patients had confounding medication conditions and/or receiving concomitant therapy.

  21. WARNING • Hypoglycemia • in some cases, diabetic ketoacidosis has occurred. • Drug interaction • risk of myopathy may increase when use with HMG-CoA reductase inhibitors.

  22. Pregnancy • CRIXIVAN is the pregnancy category C • hyperbillirubinemia has occurred • Should be used if potential benefit justifies the potential risk to the fetus.

  23. Nursing Mothers • Study in lactating rats CRIXIVAN excreted in milk. • Not known whether CRIXIVAN is excreted in human milk. • Should be discontinue nursing if receiving CRIXIVAN

  24. Information for patients • CRIXIVAN is not a cure for HIV infection. • Patients may to develop opportunistic infections. • Not shown reduce the risk of transmission of HIV to other through sexual contact or blood contamination.

  25. Information for patients • If a dose is missed, should take the next dose at regularly time. • Should not double dose. • For optimal absorption , should take without food

  26. Storage • Store in a tightly-closed container at room temp. , 15-30 C • Protect from moisture. • Should be stored in original container. • The desiccant should remain in the bottle

  27. Special Thanks. • Professor John Essigmann, MIT • Professor Ram Sasisekharan, MIT • Dr. Ganesh Vengataraman, MIT • Dr. Maria Kartalou, MIT • Dr. Suvit Loprasert, CRI

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