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HIV Drugs & Side effects - Coggle Diagram

- - - - Mechanism:
        
        Inhibition of mitochondrial DNA polymerase gamma:
        
        NRTIs are designed to inhibit HIV reverse transcriptase, but they can also inadvertently inhibit polymerase gamma, the enzyme responsible for replicating mitochondrial DNA (mtDNA).
        
        Mitochondrial dysfunction:
        
        This leads to decreased mtDNA content, which impairs the mitochondria’s ability to generate energy through oxidative phosphorylation.
        
        The electron transport chain becomes less functional, and cells switch to anaerobic metabolism, increasing lactate production.
  - - - Thymine analog
        
        ZDV: usually only used in babies & during pregnancy for short courses
      - Most common side effect is bone-marrow suppression --> macrocytic, megoblastic anemia); NRTI w/ the highest risk of mitochondrial toxicity & Lactic acidosis with hepatic steatosis
    - - Abacavir
        
        Serum levels of drug are increased with alcoholic beverages; HLA-B*5701 genotype increases likelihood of a hypersensitivity reaction; higher risk of myocardial infarction
        
        well absorbed orally
        
        Ab --> Alcoholic Beverages
    - - Lamivudine
        
        mild GI discomfort
      - EMTRICITABINE
        
        Longer half-life (> 24 hrs); once daily dosing
        
        used in PrEP
    - - TENOFOVIR DISOPROXIL FUMARATE (TDF)
        
        loss of renal function has been observed, should be used with caution in patients at risk for renal dysfunction
        
        Too Darn Frail: nephrotoxicity and a decrease in bone mineral density are when TDF is used in combination with an inhibitor of CYP34A, like ritonavir
        
        can be used in PrEP
      - TENOFOVIR ALAFENAMIDE FUMERATE (TAF)
        
        TAF has more selective cellular uptake & is more stabile in serum --> Likely accounts for less loss of renal function and bone mineral density (compared to TDF)
        
        can be associated with triglyceride elevation (check lipid profiles)
        
        can be used in PrEP
- - - - side-effect
        
        injection site reactions, consisting of painful erythematous nodules
- - - - SEs:
        
        Hepatotoxicity, Systemic hypersensitivity (w/ skin rash), elevated creatinine levels but Kidney is OK!
    - - High barrier to resistance
      - SEs: can decrease tubular secretion of creatinine in the kidneys --> Serum creatinine inc. but kidney is OK!
    - - SEs: injection site reactions are common but typically low-grade
      - Patients take cabotegravir/rilpivirine orally for a month to monitor potential adverse reactions. If tolerated, will be injected every 1 to 2 months; extended-release injectables have a long tail meaning they last for a long time at subtherapeutic levels --> if patient wants to wean off they must start taking another drug to avoid resistan e
- - - - SEs: Liver toxicity (severe hepatitis) Hypersensitivity w/ Sulfa Allergy, rash
    - - Nephrotoxicity
      - Insulin Resistance, Hyperglycemia
    - - SEs: 1) Nephrolithiasis/ Kidney stones/cholelithiasis/Gallstones 2) Jaundice-Inderect Hyperbilirubinemia, Nephrotoxicity
      - Kid's are being stoned to death in Tanzania