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ANTIRETROVIRAL DRUGS - Coggle Diagram
ANTIRETROVIRAL DRUGS
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INTEGRASE INHIBITORS
- Class of agents bind Integrase- a viral enzyme essential to replication of both HIV-1 & HIV-2
- Inhibits strand transfer→ final step of provirus integration
- Hence interfere with integration of reverse-transcribed HIV DNA into host cell chromosome
RALTEGRAVIR
- 1st integrase inhibitor
- Prevents integration of proviral DNA
- Active against both HIV-1 & 2
- No cross resistance with other ARVs
- Clinical efficacy demonstrated in treatment of naive & previously treated patients
PHARMACOKINETICS :check:
- Rapidly abs. orally
- Extensive glucuronide conj. in liver
- Rifampin induces metabolism → dose doubled
- Admn. of Ca & Mg containing antacids or Ca & Fe supplements to be avoided : chelating property
ADVERSE EFFECTS :warning:
- Nausea, headache, fatigue, muscle ache
- ↑ serum amylase & aminotransferases
- Myopathy
- Severe fatal skin reactions reported
○ SJS
○ HS reactions
○ Toxic epidermal necrolysis
DOLUTEGRAVIR
- 2nd gen integrase inhibitor
- Active against both HIV 1 & 2
- No cross resistance
- Dolutegravir + 2NRTIs yielded superior results
PHARMACOKINETICS :check:
- Slow abs.
- Glucuronide conj. & eliminated with T½ = 12hrs
- Dose doubled when admn with enzyme inducers like rifampin & efavirenz
○ Its combi with NVP & Etravirine to be avoided
- Cationic medications avoided/ staggered with dolutegravir
- Potent activity, good tolerability, OD dosing
○ Doluegravir + 2NRTIs → gaining popularity as 1st line regimen for trt naive HIV patients (but costly)
ADVERSE EFFECTS :warning:
- Insomnia, headache
- Hypersensitivity reaction: drug to be immediately discontinued
- Occassional hepatotoxicity
ENTRY FUSION INHIBITOR
ENFUVIRTIDE
- HIV derived synthetic peptide
- Acts by binding to HIV-1 envelope transmembrane glycoprotein(gp41)
- Preventing fusion of viral & cellular membranes
- Not active against HIV-2
- No cross resistance
- Admn: Subcutaneously BD
- Add on drug to optimized regimen in selected patients
○ Who have failed many earlier regimens or have multidrug resistant HIV
- Costly
ADVERSE EFFECTS :warning:
- Injections are painful, cause local nodules/cysts
- Eosinophilia
- Hypersensitivity
CCR5 RECEPTOR INHIBITOR
MARAVIROC
- Binds specifically and selectively to the host protein CCR5- one of the two chemokine receptors necessary for entry of HIV into CD4+ cells
- Most HIV are CCR5 tropic
- No effect on strains that are CXCR4 tropic or dual tropic
- Added to optimized background therapy in patients already treated with several regimens
- Active orally
- No cross resistance
- But CCR5 tropism must be proved before use
ADVERSE EFFECTS :warning:
- Cough, fever, abd. pain, rashes
- Postural hypotension