TREATMENT OF HIVGROUP-5

MAHETA MIHIRBORISAGAR ABHISHEK

DESAI ASHISHAMDANI AKRAM

GOSWAMI ALPESH

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

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

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

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

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

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 

Example:- Tipranavir Nelfinavir Saquinavir Darunavir Ritonavir

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

Example:- ENFUVIRTIDE MARAVIROC

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

Example:- RALTERGRAVIR