treatment overview

1. TREATMENT OF HIV
GROUP-5
MAHETA MIHIR
BORISAGAR ABHISHEK
DESAI ASHISH
AMDANI AKRAM
GOSWAMI ALPESH

2. SELECTION OF APPROPRIATE COMBINATION
1. avoid use of 2 agents of the same nucleoside analog
2. avoid overlapping toxicities and genotypic and phenotypic
characteristic of virus
3. patient factors (disease symptoms and concurrent illness)
4. impact of drug interactions
5. Ease of adherence to frequently complex administration regimen

3. Goal of therapy
 Maximally and durably suppress viral load replication
 To restore and preserve immunologic function
 Reduce HIV-related morbidity and mortality
 Improve quality of life

4. Types of HIV/AIDS Antiretroviral Drugs
 01) NUCLIOSIDE REVERSE TRASCRIPTASE INHIBITORS (NRTI)
 02) NON NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
 03) HIV PROTEASE INHIBITORS
 04) ENTRY INHIBITORS
 05) INTEGRASE INHIBITOR

5. Nucleoside reverse transcriptase inhibitors
(NRTI)
 Mechanism of action:-
 3’OH group is not present 3’-5’ phosphodiester bond between an incoming
nucleoside triPO4 and growing DNA chain cannot be formed DNA chain
elongation is terminated
 Example:-
 zidovudine
 Lamivudine
 Tenofovir
 Didanosine

7. Non nucleoside reverse transcriptase
inhibitors
 Mechanism of action:-

NNRTIs work by disabling a protein that HIV needs to replicate.
 They reverse transcriptase consequently blocking it from altering the RNA to DNA.
 In effect, this strengthens the genetic material of the cell such that the genetic
information of HIV cannot cause it to replicate the virus
 Example:-
 Delivirdine
 Efavirenz
 Etravirine(second generation)
 Nevirapine

9. Protease inhibitors
 Mechanism of action:-
 Protease inhibitors serve to prevent infected T-cells from replicating the
virus.
 They cover the active sites of the protease enzyme in order to inhibit the HIV
polyprotein.
 This brings down the level of the virus in the blood boosting the patient’s
immune system.
 Resistance to protease inhibitors comes from mutation of the viral protease
enzyme

10.  Example:-
 Tipranavir
 Nelfinavir
 Saquinavir
 Darunavir
 Ritonavir

11. Entry inhibitors
 Mechanism of action:-
 Entry or fusion inhibitors prevent HIV from entering CD4 cells.
Contact between gp120-CD4 complex and chemokine receptor CCR5 or CXCR4
causes a change that the viral membrane to a fusogenic state which control the
fusion process

12.  Example:-
 ENFUVIRTIDE
 MARAVIROC

13. INTEGRASE INHIBITOR
 Mechanism of action:-
 Integrase inhibitors embed themselves on reverse transcriptase after it has
created the viral DNA strand and hooks onto the last two nucleotides from the
end of the DNA strand.
 This is termed as 3A2 processing. After this, integrase inhibitor forms a
preintegrase complex that carries a ring shaped viral DNA and host proteins.
 It is this preintegrase complex that helps the viral DNA pass through cell
cytoplasm and into the cell nucleus.
 The integrase inhibitor prevents strand transfer and viral replication

14.  Example:-
 RALTERGRAVIR