The human immunodeficiency virus (HIV) is a retrovirus characterized by a
reverse transcriptase enzyme and is known for causing acquired immune deficiency
syndrome (AIDS), a chronic condition with progressive failure of the immune system.
HIV poses a major health issue globally, infecting cells containing CD4+ and CCR5 or
CXCR4 receptor sites, i.e., T-lymphocytes, macrophages, monocytes, and dendritic
cells. HIV infects the T-lymphocytes by suppressing the immune system leading to
several pathogenic infections, thus critically demands healthy measures to strengthen
the immune system. For this purpose, diverse classes of drugs have been developed that
effectively decrease the viral load in the patients, inhibiting the replicative cycle of
HIV at a specific point. These specific inhibitors (drugs) may include inhibitors of
entry/fusion, protease, nucleotide reverse transcriptase, non-nucleotide reverse
transcriptase, and integrase. This chapter provides an overview of the drugs used to
treat HIV, their mechanism of action and side effects, as well as their dosage
recommended for the treatment of HIV. Notable examples are zidovudine, abacavir,
lamivudine, didanosine, tenofovir, stavudine, emtricitabine, nevirapine, delavirdine,
efavirenz, etravirine, dolutegravir, bictegravir, raltegravir, cobicistat, indinavir,
ritonavir, nelfinavir, saquinavir, darunavir, atazanavir, lopinavir, tipranavir, fusion
inhibitors (enfuvirtide) and chemokine CCR5 receptor antagonist. These drugs are
administered to HIV patients throughout their life mostly as a combination therapy as
HIV can become resistant to these drugs after some period. Additionally, these drugs
have several side effects such as nausea, dizziness, liver diseases, kidney disorders, and
heart diseases. Many of the above-mentioned side effects are temporary and are
resolved spontaneously. However, some of these (hepatic, renal, or cardiac failure) can
lead to the death of the patient. Another drawback of antiretroviral drugs is their
latency for HIV and its reactivation. By determining and controlling all the factors that
regulate the gene expression of HIV, such as HSP90, required for HIV gene
expression, reactivation of HIV can be stopped from latency. Moreover, the latency of HIV can also be controlled by studying its mechanism, thus enhancing the
effectiveness of antiretroviral treatment (ART). The development of plant-based drugs
exhibiting improved inhibition of HIV replication compared to available antiretroviral
drugs has also been reported.
Keywords: Antiretroviral drugs, Antiretroviral treatment, Cardiac failure, Human
immunodeficiency virus, Macrophages, T-lymphocytes.
