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Anti-HIV drugs



  1. Zidovudine
    1. Prodrug
    2. Requires intracellular phosphorylation
    3. Resistance develops due to mutation in reverse transcriptase enzyme
    4. Short acting; half life=1 hour
    5. Undergoes glucoronidation
    6. Toxocity of zidovudine can occur when given with NSAIDS; as they compete with glucoronidation  

Side effect

  1. Anemia is MC (Macrocytic)       
  2. Sensory neuropathy    
  3. Myopathy                        
  4. Bone marrow depression 



  1. To reduce needle prick transmission of HIV (normal risk=0.03%; 1 out of 300)
  2. It is used with lamivudine for this indication (for 1 month)    
  3. To reduce mother to child transmission (zidovudine is given with nevirapine)
    1. Best time is at the ONSET of labour
    2. Normal possibility is 20-30%
    3. With drugs; 8%
    4. Routine strategy in India in states with high prevalence of HIV 


b. Lamivudine

  1. DOC for hepatitis B (chronic)
  2. Does not cause neuropathy
  3. Drugs are NOT useful for acute hepatis B


  1. -In hepatitis B, with raised liver enzymes; lamivudine is given with interferon-2-alpha
  2. -Resistance to lamivudine calls for use of adeforvir, entecavir, tiprinavir  


c. Stavudine

  1. MC anti-HIV drug causing neuropathy
  2. Also causes hepatic stetosis & lactic acidosis 

d. Diadanosine

  1. Causes neuroathy, pancreatitis

e. Zalcitabine

  1. Causes pancreatitis more than neuropathy
  2. Not combined with lamivudine because resistance develops


f. Abacavir

  1. Anti-HIV drug with highest risk of hypersenstivity (5%); could be fatal
  2. Hardly used 

g. Tenofovir

  1. RTI and is a NUCLEOTIDE, NOT a nucleoside
  2. Other RTI are nucleoside analgues

2. Protease inhibitors

—Inhibit interaction between gag-pol gene

  1. Genes code for viral components
  2. Inhibit viral replication
  3. Well absorbed, food increases absorption
  5. Most potent ritonavir, least potent is saquinavir
  6. Lipodystrophy is their MC side effect
  7. Others side effects are:  Hyperlipidemia, Hypergylecemia, Obesity
  8. Indinavir causes renal stones, indirect hyperbilirubinemia (sufonamides also cause)
  9. Ritonavir is used as BOOSTING agent

3. Fusion inhibitors

Enfuvirtide (Glycoprotein-41 blocker)

  1. Blocks viral entry into cells
  2. Long acting drug
  3. Used in resistant infections
  4. Given subcutaneously
  5. Eliminated unchganged
  6. Resistance-mutation in env gene



  1. Nevirapine
    1. Enzyme inducer (remember, protease inhibitors are enzyme inhibitors)
    2. Side effects are rashed, diarrohea, hepetistis (could be fatal)
  2. Delavirdine
    i. Diarrhea
  3. Efavirenz
    1. Induces & inhibits liver enzymes
    2. CNS toxicity is side effect
    3. Food increases its absorption


NNRTIs are used in combination as a part of HAART



New Drugs: Recent Advances

  1. Entry inhibitor:
    Maraviroc and vicriviroc: Acts by inhibiting virus entry via CCR5 coreceptors.
    It doesn’t inhibit virus taking entry with the help of CXCR4.
    Very potent drug and resistance is difficult to develop
    Side effects are hypotension due to alpha blocking action and hepatotoxicity.
  2. Tesamorelin: new drug approved for the treatment of lipodystrophy caused by anti HIV drugs. 
  3. Viral integrase inhibitor
    Oral integrase inhibitor
    Used in resistant HIV infection
    Used in combination as a part of HAART (highly active anti retroviral treatment)
    Does not cause lipodystrophy     
  4. Rilpivirine – recently approved most potent NNRTI

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