DRUGS FOR THE

TREATMENT OF AIDS

Dwi Indria Anggraini

Medical School Lampung University
 Introduction

Viruses structures

Main types of
viruses

Antiviral

Target therapeutic
Virus multiplication and modes of action of antiviral agents
Chemical structure of virustatic antimetabolites
Activation of acyclovir and inhibition of viral DNA synthesis
Inhibitor of DNA polymerase (Foscarnet)
Prophylaxis for viral flu
RNA Retroviruses
Drugs for the Treatment of AIDS (ARV)

I. Inhibitors of Reverse Transcriptase

• IA. Nucleoside agents
• IB. Non-nucleoside inhibitors

II. HIV protease inhibitors

IA. Nucleoside agents
Analogues of thymine (azidothymidine,
stavudine), adenine (didanosine),
cytosine (lamivudine, zalcitabine), and
guanine (carbovir, a metabolite of
abacavir).

Undergo triphosphorylation, giving rise

to nucleotides that both inhibit reverse
transcriptase and cause strand breakage
following incorporation into viral DNA.
 IB. Non-nucleoside inhibitors

The non-nucleoside inhibitors of reverse

transcriptase (nevirapine, delavirdine,
efavirenz) are not phosphorylated.

They bind to the enzyme with high

selectivity and thus prevent it from
adopting the active conformation.

Inhibition is noncompetitive.
 HIV protease inhibitors

Viral protease cleaves precursor proteins into proteins required

for viral replication.

Saquinavir, ritonavir, indinavir, and nelfinavir represent abnormal

proteins that possess high antiviral efficacy and are generally well
tolerated in the short term.

Prolonged adm is associated with occasionally severe

disturbances of lipid and carbohydrate metabolism.

Biotransformation of these drugs involves cytochrome P450 (CYP 3A4)

and is therefore subject to interaction with various other drugs
inactivated via this route.
 Combination Regimens

For the dual purpose of increasing

Combination regimens are
the effectiveness of antiviral
designed in accordance with
therapy and preventing the
substance specific development
development of a therapy-limiting
of resistance and
viral resistance, inhibitors of
pharmacokinetic parameters (CNS
reverse transcriptase are
penetrability, “neuroprotection,”
combined with each other and/or
dosing frequency).
with protease inhibitors.
 CONCLUSIONS

I. Inhibitors of Reverse
Transcriptase

II. HIV protease inhibitors