Drugs used in STI

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yuenyan
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235958
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Drugs used in STI
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2013-09-20 04:08:50
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Pharmacology
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Drugs used in STI
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  1. Chlamydia trachomatis
    • ADO
    • A- azithromycin (single oral dose)
    • D- Doxycycline (bis 7D oral)
    • O- ofloxacin
  2. Adverse rxn of drugs for chlamydia trachomatis
    • mostly GI
    • mild to moderate
  3. Gonococcal
    • ceftriaxone - single IM + single oral of azithromycin
    • cefixime - single oral
  4. PID (in-patient)
    • cefoxitin/ cefotetan (IV) + doxycyline (oral)
    • clindamycin + amyloglycoside
  5. PID (out-patient)
    ceftriaxone (IM) + doxycycline +/- metronidazole for 14D
  6. Bacterial vagionosis
    • infected by anaerobes
    • metroniazole (oral 7D/ intravaginal gel)
    • clidamycin (oral/ intravaginal)
  7. Trichomoniasis
    • infected by protozoa
    • metronidazole/ tinidazole (single dose)
  8. Vulvovaginal candidiasis
    • infected by fungi
    • ropical azole antifungal agents
  9. Syphilis
    • penicillin G (all stages)
    • benzathine penicillin G (single IM as slow release for early latent stage)
  10. Genital warts
    • podofilax (gel on visible lesion)
    • imiquimod, 5-flurouracil, trichoroacetic acid
    • intralesional alpha interferon (inject into warts; for recurrences)
  11. mechanism of imiquimod, 5-flurouracil, trichloroacetic acid
    denatures proteins and warts
  12. mechanism of intralesional alpha interferon
    cytokines
  13. Genital Herpes
    • acyclovir (prototype)
    • valacyclovir, famciclovir (prodrugs/ ACV derivatives)
    • foscarnet, cidofovir (reserved for severe/ complications)
  14. mechanism of acyclovir
    • ACV -> ACV triphosphate (active form)
    • first phosphorylation -> viral thymidine kinase; second and third phosphorylation -> host's cellular kinases
    • competitive inhibition of viral DNA polymerase by ACV triphosphate -> chain termination -> incorporation into viral DNA
  15. pharmacology of acyclovir
    • an acyclic guanosine derivative with clinical activity against herpes infections
    • first clinical -> oral, severe -> IV
    • oral less effective for recurrences
    • long term prophylaxis -> lower recurrences 
    • low bioavailability (15%)
  16. mechanism and pharmacology of valacyclovir
    • an ester of ACV being converted to ACV by hepatic and intestinal enzymes
    • only first clinical & recurrent
    • bioavailability: 15-55%
  17. mechanism and pharmacology of famciclovir
    • converted to penciclovir with similar action as ACV in viral shedding, lesion healing and resolution of symptoms
    • only first clinical and recurrent
  18. HIV 
    HAART highly active antiretroviral therapy
    • NRTI/ NtRTI (nucleoside/nucleotide reverse transcriptase inhibitor)
    • NNRTI (non-nucleoside reverse transcriptase inhibitor)
    • PIs (protease inhibitor)
    • Entry inhibitor
    • INSTI (intergrase inhibitor)
  19. Primary Goals of HAART
    • prolong duration & quality of survival + reduce HIV-associated morbidity
    • restore/preserve immunity
    • maximally & durably suppress viral load
    • prevent transmission
  20. example of NRTI/ NtRTI
    • Zidovudine (NRTI)
    • Tenofofir (NtRTI)
  21. mechanism of NRTI/ NtRTI
    • active form: triphosphate form
    • competitively inhibit HIV reverse transcriptase + viral DNA chain termination
  22. common toxicities of NRTI/ NtRTI
    • lactic acidosis
    • hepatic steatosis
    • lipodystrophy
  23. example of NNRTI
    • nevirapine
    • efavirenz
    • delavirdine
    • etravirine
    • rilpivirine
  24. mechanism of NNRTI
    directly inhibit HIV-1 reverse transcriptase in a reversible and non-competitive manner
  25. common toxicities of NNRTI
    • rash
    • CNA
    • interaction (met. by P450)
  26. toxicities of nevirapine
    • hepatotoxicity
    • rash e.g. Steven- Johnson Syndrome
  27. toxicities of efavirenz
    • neuropsychiatric (vivid dreams)
    • tetragenic (not prescribed in preg)
  28. use of NRTI
    • slow disease progression
    • prolong survival
  29. use of NNRTI
    • suppress viral replication
    • prevent perinatal HIV transmission
  30. examples of PIs
    • saquinavir
    • ritonavir
    • lopinavir
    • atazanavir
    • darunavir
    • fosamprenavir
  31. mechanism of PI
    specifically inhibit HIV-1 protease
  32. toxicities of PI
    • hyperlipidemia
    • insulin resistance and diabetes
    • lipodystrophy
    • increase liver function test 
    • increase risk of bleeding in hemophiliacs
    • interaction (P450)
  33. examples of entry inhibitors
    • enfuvirtide
    • maraviroc
  34. mechanism of enfuvirtide
    inhibit fusion of viral gp41 with host cell
  35. mechanism of maraviroc
    antagonise CCR5 chemokine co-receptor on CD4 T cells
  36. use of entry inhibitors
    treatment of multi-drug resistance (MDR) CCR5- trophic HIV-1
  37. example of INSTI
    • raltegravir
    • dolutegravir
  38. mechanism of INSTI
    inhibit HIV-1 intergrase -> prevent propagation of viral infection
  39. indication of INSTI
    treatment of HIV-1 infection in treatment-experienced adult patients who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents

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