Active Ingredients

Elvitegravir – Effect, Application & Risks

Elvitegravir

Elvitegravir is a drug that is one of the active ingredients in integrase inhibitors In human medicine, elvitegravir is primarily used as a drug to treat infections with the HIV-1 virus . Doctors always use the active ingredient together with other drugs that are characterized by an antiretroviral effect. Doctors often combine elvitegravir with the substance cobicistat , which is a so-called booster.

What is elvitegravir?

Elvitegravir is a potent inhibitor of integrase (a retroviral enzyme), making it a good candidate for treating HIV-1 virus infection. The pharmaceutical manufacturer Gilead Sciences developed the drug elvitegravir, which received approval as a drug from the Food and Drug Administration in 2012. Elvitegravir is mainly used for drug therapy in adult patients.

Elvitegravir is a derivative of dihydroquinoline and appears as a white to yellowish powder at room temperature. In addition, elvitegravir is characterized by relatively poor solubility in water.

The active ingredient is particularly suitable for people whose drug therapy for HIV is just beginning. In many cases, elvitegravir is a first-line medication. Pharmaceutical manufacturers sometimes combine elvitegravir with the active ingredient tenofovir . This combination of two drugs improves the effectiveness, while some of the disadvantages decrease.

People who are infected with HIV often receive elvitegravir as a single drug under the trade name Vitekta®. In addition, physicians often combine the active ingredient with ritonavir . Ritonavir is a pharmacological substance used in many anti-HIV drugs. Ritonavir usually acts as a booster that increases the effectiveness of the actual drug.

Pharmacological effect on body & organs

The effect of elvitegravir is mainly due to inhibition of integrase. This results in the good suitability of elvitegravir as an HIV drug. Because elvitegravir inhibits the enzyme integrase of viruses , especially HIV-1 viruses. Elvitegravir is somewhat less effective on HIV-2 viruses. Viruses need this enzyme to transfer their genetic information into the host ‘s DNA .

In this way, elvitegravir has a strong antiviral effect. Elvitegravir is usually used in combination with CYP inhibitors, which slow down the metabolism of elvitegravir and thereby increase its effectiveness in the organism. Elvitegravir is cleared primarily by CYP3A. Therefore, simultaneous intake with inducers of the enzyme should be avoided. These include, for example, phenytoin or St. John’s wort .

Elvitegravir hardly affects the function of the kidneys . Patients take elvitegravir in pill form. If it is taken at the same time as ritonavir and a meal, the active substance reaches its highest concentration in the blood plasma after about four hours . Studies show that high-fat foods increase the bioavailability of elvitegravir. In the circulating blood , most of the elvitegravir binds to plasma proteins . The body excretes almost 95 percent of the active ingredient in the stool . The rest enters with the urineout of the body. The plasma half-life of elvitegravir in combination with ritonavir ranges from 9 to 13 hours.

Medicinal Application & Use for Treatment & Prevention

Elvitegravir is an HIV-1 drug that is commonly used in fixed-dose combination with pharmacological boosters. Patients take elvitegravir orally as a film-coated tablet. It is sufficient to consume a single tablet of the active ingredient elvitegravir per day. It is recommended that elvitegravir be taken with a meal to increase its effectiveness.

It is mandatory to administer the active ingredient elvitegravir together with a booster that inhibits the protease. For this reason, elvitegravir is usually available in a fixed combination with a corresponding booster. The dose depends primarily on the protease inhibitor administered at the same time. However, doctors are currently still using the drug Elvitegravir as a reserve drug.

Risks & side effects

Side effects sometimes associated with taking elvitegravir are similar to those of many other HIV medications. The administration of elvitegravir most frequently results in complaints of the digestive tract such as nausea , vomiting and diarrhea . In addition, some patients report headaches and fatigue . In addition, some people develop rashes on their skin .

The pharmaceutical manufacturers generally describe Elvitegravir as a well-tolerated drug. Therapy with the active ingredient is generally ruled out if the patient suffers from an intolerance to the active ingredient. Even with resistance to elvitegravir, taking it makes no medical sense. For pregnant and breastfeeding women, there are sometimes special requirements for therapy with elvitegravir.

Before taking elvitegravir, certain interactions with other pharmaceutical substances must be considered. Elvitegravir is primarily metabolised in the liver by the enzyme CYP3A. For this reason, concomitant use of elvitegravir and phenytoin, rifampicin and carbamazepine should be avoided. A combination with St. John’s wort should also be avoided. Elvitegravir is characterized by cross-resistance to the active ingredient raltegravir.

In general, elvitegravir is considered a reserve drug for drug therapy of infections with the HIV-1 virus. Clinical experience has so far been comparatively limited. The advantage of elvitegravir, however, is that one dose per day is sufficient for therapy.

Lisa Newlon
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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.