Integrase Inhibitors

Integrase Inhibitors belong to the antiretroviral drug class. These drugs are designed to control the viral enzyme called integrase that can affect the DNA of the patient. The integrase virus, normally found in patients suffering from HIV, inserts a viral genome which integrates into the DNA of the patient thus converting the genetic material. Such integration into the host cell is called retroviral replication and by halting this process, Integrase Inhibitors treat HIV infection. Integrase Inhibitors, like Isentress, offer a new ray of hope to people suffering from HIV; including those who have developed resistance to other drugs.

The integrase enzyme produced by the HIV virus integrates into the CD4 cells of the human being and the “infected cell” replicates or makes new copies thus spreading HIV. This is done by the HIV virus converting its own RNA into DNA by an enzyme called reverse transcriptase. Once the process is complete, the converted DNA is incorporated into the CD4 machinery of the human being. This process is called integration. Integrase Inhibitors block the process of re-conversion. This means that once the HIV RNA is converted to DNA, they are blocked from integrating into the CD4 cells, thus controlling the replication process of the diseased cells. Integrase Inhibitors need to be taken with other HIV treatment medications to minimize the virus’s adaptation. Integrase Inhibitors is also useful for those who have developed resistance to other drugs in the treatment of HIV. The virus mutates and acquires resistance to drugs that target another viral enzyme, the protease.

The first drug to be researched in this class was the Raltegravir (commercially being produced under the brand name of Isentress) and the results of the research were published in the 2008 July 24 edition of the New England Journal of Medicine. The research concluded that patients who were given “raltegravir plus”, along with optimized background therapy, showed better results over a period of 48 weeks.

Isentress is the first integrase inhibitor, produced by Merck, to get approval from the US-FDA in October 2007. The Elvitegraviz drug, being produced by Gilead, is in its advanced stage of clinical trials.

Integrase Inhibitors should be taken under the guidance of a doctor. Once the medications have been started, the patient may develop immune reconstitution syndrome wherein inflammation from infections may occur. This happens as the medication strengthens the natural immune system of the patient. Some patients are also believed to have complained about tenderness, weakness and muscle pain. Some of the side effects observed were nausea, tiredness, headaches and general weakness. Prior to starting this medication, inform your doctor of your overall health condition and other status like allergies, pregnancy, breastfeeding, and details of prescriptive drugs and herbal supplements or vitamins being consumed. Pregnant women should not take Integrase inhibitors. The medication is given in dosage of 200, 400 or 600 mg, depending on various factors. It is generally taken twice daily. Patients undergoing the treatment should be under the regular care of a doctor and should inform the doctor of any change in their health condition immediately.

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