There are currently five classes of antiretroviral medications: nucleoside reverse transcriptase inhibitors, nonnucleoside reverse transcriptase inhibitors, protease inhibitors, fusion inhibitors, and Integrase inhibitors. There have not always been so many medications to treat HIV, in fact, in the very beginning there was only one. In 1987 nucleoside reverse transcriptase inhibitors (NRTI’s) were approved for use by the FDA. NRTI’s help in the attack on HIV by interfering with its protein called reverse inhibitor which is important in HIV replicating itself.
These were the first class of drugs introduced following the first report of AIDS in the summer of 1981. Zidovudine was the first drug approved by the FDA. In History of Drugs3 History of Drugs Used To Treat HIV/AIDS 1964 a chemist named Jerome Horwitz, at the Michigan Cancer Foundation, synthesized Zidovudine for treatment with cancer. Many tests were conducted by Horwitz and his partners on the effectiveness of Zidovudine with cancer and it was found to be ineffective. It was not until 1974 that the drug was shown to have antiviral potential.
Six NRTI’s have been approved since the introduction of Zidovudine: didanosine, zalcitabine, stavudine, lamivudine, abacavir, emtricitabine. The first decade after the first reports of HIV in 1981,and its identification as a retrovirus, showed little in the creation of new drugs. It did however show the introduction of the first immunoassay test and the introduction of the first drug to treat AIDS, AZT. It was not until between 1991 and 1994 that newer drugs were beginning to make it onto the market.
Up to this point, those infected with the virus were only using monotherapy for treatment. During this three year period the first non blood-based collection system was approved to test for HIV, and a barrier product for women, the female condom, was introduced. The end of the century the first protease inhibitor was approved and issued as a new class of drugs for treating HIV. HIV uses the enzyme protease in its final stages of replication within the cell. Protease Inhibitors block the enzyme within the cell during its final stages.
The process of blocking protease slows or stops the replication of that particular strand of HIV by replicating itself, and these new copies cannot infect new cells. Of all the drugs developed so far, protease inhibitors are considered the most potent. The drugs in this class were also the first drugs to be approved and used for once daily dosing. “ Reyataz received approval from the U. S. Food and Drug Administration (FDA) in Mid-2003 and was the first protease inhibitor approved for once daily voting” (LoBuono, 2003).
The first decade of the new century saw many new drug formulas and combination drugs. These new combination drug therapies not only helped to reduce pill burden in infected patients, but it also showed great signs in combating HIV. The first nucleic acid test for plasma screening, the first rapid History of Drugs4 History of Drugs Used To Treat HIV/AIDS HIV test for use in outreach settings, the first fusion inhibitor for treatment of HIV/AIDS, and the first generic version of an HIV therapeutic agent were also approved (Food and Drug Administration, 2012).
With the introduction of fusion inhibitors, it was possible to stop the virus from actually entering the cell. Fusion inhibitors stop the virus from entering the CD4+ cell by not allowing it to fuse with proteins on the surface of the cell, specifically gp41 and gp120, and therefore inhibits it from affecting the cell. The first fusion inhibitor drug approved on the market was Enfuvirtide and is still in use today. It is now 2012 and the introduction of antiviral medication used in combination has allowed for great advances in the history of HIV/AIDS.
Combination or highly active antiretroviral therapy (cART or HAART) has helped in narrowing down HIV in more than one angle, if one drug fails there is another drug to take up the charge and suppress the viral replication. New diagnostic assays have been introduced to help shorten the time in which new infections can be detected and less drugs are being used and are helping in diminishing the harsh side effects associated with old therapy, and new drugs and advancements are being developed everyday along with lower costs for generic drugs.
Untreated case fatality rates initially approached 100%. With the introduction of combination or highly active antiretroviral therapy, the HIV-related death rate has declined 70% since 1995 ( Lutz and Przytulski, 2011). Even with all of these advancements, there is a ways to go until a cure is found, but everyday society is a little bit closer. On a personal note, I remember back in 1991 when my Uncle was diagnosed with HIV. It was a different time and those individuals infected were pretty much handed a death sentence. I will never forget how overwhelmed he was with this news.
He was only 26 years old and had to come to the realization that he was going to die way before he ever thought he would. Those in the family who History of Drugs5 History of Drugs Used To Treat HIV/AIDS cared and did not criticize him for being gay, stayed with him until the end. We all hoped for the best and prayed that a cure might be found, or a medication to at least suppress the virus could be found. At that time, it was not. The development of the National Task Force on AIDS Drug Development had not yet been formed, and the few drugs on the market where too expensive.
In one week I watched him go from a healthy looking 26 year old man to a 90 pound year old frail individual. It only took two week from the time that he ate a piece of contaminated food for him to develop pneumonia and die. Over the last 16 years I have known many friends with HIV/AIDS. Being a major supporting and active member in the gay community I have met many. I know of 33 very close people in my heart who I have watched go down that very lonely, terrifying, and sad road of dying from the virus. I have watched the emotional toll on all of their family members, co-workers, and close friends.