Tuesday 28 April 2020

How Darunavir Ritonavir combination is useful in the treatment of HIV

Darunavir Ritonavir for HIV treatment

Darunavir: 

Darunavir (DRV), is an antiretroviral medication, which is sold under the brand name Prezista in order to treat as well as prevent HIV/AIDS.
DRV (Darunavir) is generally recommended for use with other antiretrovirals. It is often used with low doses of ritonavir or cobicistat with the motive of increasing the levels of darunavir. Darunavir, combines with the ritonavir 100 mg antiretroviral and with some other antiretroviral agents, for the treatment of human immunodeficiency virus (HIV) infection in antiretroviral treatment experienced adult patients, such as those with Human Immunodeficiency Virus-1 (HIV-1) strains resistant to more than one protease inhibitor.

Darunavir comes as the strengths which are as follows:



Side Effects of Darunavir: 

This is a quite well-tolerated medication and sometimes it may leave some adverse reactions, which are as follows:

  • Skin rash
  • Hepatotoxicity
  • Diarrhea
  • Nausea
  • Headache
  • Hyperlipidemia
  • Serum transaminase elevation
  • Hyperglycemia
  • Fat maldistribution

Ritonavir:

Ritonavir (RTV), an antiretroviral medication, which is sold under the trade name Norvir in order to treat HIV/AIDS.
Ritonavir is generally prescribed for use along with other medications. When Ritonavir is used with the other medications, then this combination treatment is called HAART, which stands for highly active antiretroviral therapy. Often a low dose this medication is used with other protease inhibitors. It may also be used in combination with other medications for hepatitis C.

How Does Ritonavir Works: 

Initially, ritonavir was developed as an inhibitor of Human Immunodeficiency Virus (HIV) protease, which is one of a family of pseudo-C2-symmetric small molecule inhibitors.
The role of Ritonavir is as a booster. It is rarely used for its own antiviral activity.  This medication is mostly as well as widely used as a booster of other protease inhibitors.
Most important aspect of ritonavir is that it is used in order to inhibit a particular enzyme, in the liver, intestines, and elsewhere, that normally metabolizes protease inhibitors, cytochrome P450-3A4 (CYP3A4).
The drug binds to and inhibits CYP3A4 so that a low dose can be used in order to enhance the other protease inhibitors.
This medication comes as the strength of Ritonavir 100mg.

Side Effects of Ritonavir: 

Ritonavir most widely used as a lower dose. Its activity is mainly based on a CYP3A4 inhibitor.
The most common side effects of ritonavir are as follows:

  • Asthenia, malaise
  • Diarrhea
  • Nausea and Vomiting
  • Abdominal Pain
  • Dizziness
  • Insomnia
  • Sweating
  • Taste Abnormality
  • Metabolic Effects

How Combination Of Darunavir/Ritonavir is Effective:

The reason behind taking both the protease inhibitors (darunavir, ritonavir) is that ritonavir has the potential that it will boost the level of darunavir and also it increases the effect of darunavir.

The recommended oral dose of darunavir tablets should be taken according to the prescribed by your healthcare provider. This medication should be taken with food. The sort of meal/food may not affect the exposure to darunavir.

Interaction: Darunavir ritonavir are both inhibitors of the CYP3A4 isoform.
Darunavir/Ritonavir should not be used in combination with rifampicin, as this may cause significant decreases in darunavir plasma concentrations. This may result in loss of therapeutic effect to Darunavir.

Read:- Carvedilol uses and its side effects.

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