Antiretroviral History

Antiretrovirals are a specific form of medication useful in the treatment of retroviruses such as AIDS. This class of medicine is currently the main workhorse of medical professionals combating the progression of HIV. Because there are a great variety of antiretrovirals, their use has to be carefully watched, particularly in combination with other antiretrovirals. Properly treating patients with antiretrovirals is a difficult, but ultimately necessary, procedure. The history of these medications stretches back to the 1960s, well before AIDS became the health scare it is today.

Synthesis

• Zidovudine was the first antiretroviral medication. It was first synthesized in 1964 at Barbara Ann Karmanos Cancer Institute in Detroit. Jerome Horwitz headed the Wayne State University School of Medicine that first synthesized zidovudine.

Treatment Use

• The original intent of zidovudine was to use as a cancer treatment. Horwitz's team began testing the drug under the name AZT. Unfortunately, it did not perform as planned, causing severe side effects in mice. Not only were side effects severe, but AZT was not particularly effective in combating tumors. It seemed as if the drug was a failure.

Rediscovery

• Ten years later, in 1974 a doctor at the Max Planck Institute in Gottingen, Germany, discovered that AZT was effective in fighting a mouse retrovirus that was similar to the human HIV virus. It wasn't until 1984 that the exciting possibilities of the 1974 results came to fruition. 1984 was the year that HIV was confirmed to be the cause of AIDS. Scientists immediately began searching for a compound that would attack the initial virus. AZT fit the bill.

Technology

• Reverse transcriptase was the key to early antiretroviral work. A viral enzyme, reverse transcriptase allows HIV to replicate. AZT, labeled in BW A509U in the first study, showed signs of disrupting HIV's ability to reproduce. AZT became the first of a number of powerful antiretrovirals that attack different elements of HIV's development and replication.

Diversification

• The most important trend in Antiretroviral treatment of HIV came with the development of HAART, or Highly Active Antiretroviral Therapy. HAART uses a combination of antiretroviral drugs to target HIV. AZT is just one element of HAART treatment. Other drugs include protease and integrase inhibitors, which attack viral enzymes. Entry inhibitors interfere with HIV's ability to bind with cells within the body.

Antiretroviral Limitations

• Unfortunately, none of the variety of antiretrovirals has the ability to cure HIV or AIDS. In fact, it is only with a potent combination of drugs that symptoms can be alleviated and the onset of AIDS delayed. In addition to its ultimate inefficacy, antiretroviral drugs have a number of other downsides. One of the most detrimental, particularly in treating HIV in the poorer nations of Africa, is the drugs' expense, which makes their use prohibitively difficult from a financial standpoint. In addition to expense, antiretroviral medications have a number of severe side effects which can have negative consequences on the quality of life of those treated with them.