HIV - Aids

Naivex is an antiviral drug designed to treat HIV-1 infection in adults and children 12 years of age and weighing 40 kg or more as part of combination antiretroviral therapy. The drug is recommended for use in patients who have not received therapy ("naive"), and in patients with HAART. In some cases, it can be used in patients with partial resistance to integrase inhibitors.

Manufacturer - Hetero Ltd, India. The active substance is Dolutegravir. Dolutegravir in 2013-2014 is approved in many countries of the world as one of the components of highly active antiretroviral therapy, such as the USA, Canada, Mexico, Brazil, the EU, Russia, Japan, Australia, South Africa.

Dolutegravir inhibits HIV integration by binding to the active region of integrase and blocking the chain transfer during the integration of retroviral deoxyribonucleic acid (DNA), which is necessary for the HIV replication cycle. In vitro, dolutegravir is slowly separated from the active site of the wild-type DNA integrase complex (half-life of 71 hours).

Contraindications

- Hypersensitivity reactions to dolutegravir (and auxiliary substances). 
- Admission of anti-arrhythmic drug Dofetilide (English name Tikosyn) 
- Age is less than 12 years and body weight is less than 40 kg

Dolutegravir is rapidly absorbed after ingestion. The average time to reach the maximum concentration is 2-3 hours. When you take 1 time per day, the pharmacokinetic steady state is reached approximately 5 days after the beginning of the oral administration. Food increases the degree and reduces the rate of absorption of dolutegravir. These changes are generally clinically insignificant, so Instgra can be taken regardless of food intake. However, patients infected with HIV-1 with a certain resistance to integrase inhibitors are advised to take Naivex with food.

Co-infection with hepatitis C does not matter for the pharmacokinetics of dolutegravir. Data on co-infection with hepatitis B are limited.

Side effects

- Impaired immune system. Infrequently: a hypersensitivity reaction, a syndrome of a restoration of immunity. 
- Disorders of the psyche. Often: insomnia. 
- Disorders of the nervous system. Very often: a headache. Often: dizziness, unusual dreams. 
- Disorders of the digestive tract. Very often: nausea, diarrhea. Often: vomiting, flatulence, pain in the upper abdomen. Infrequent: pain in the abdomen, discomfort in the abdomen. 
- Disorders of the liver and biliary tract. Infrequently: hepatitis. 
- Impaired skin and subcutaneous tissue. Often: rash, itching. General disorders and disorders at the site of administration. Often: fatigue.

Interaction

- The simultaneous use of dolutegravir and other drugs that inhibit UDP-HT 1A1, UDF-GT1A3, UDF-GT1A9, CYP3A4 and/or Pgp, may increase the concentration of dolutegravir in blood plasma. 
- Contraindicated simultaneous reception with dofetilide. 
- The simultaneous use of dolutegravir and etravirine is not recommended unless the patient receives simultaneously atazanavir/ritonavir, lopinavir/ritonavir or darunavir/ritonavir. 
- The drug should not be administered together with antacids containing polyvalent cations. It is recommended to use dolutegravir 2 hours before or 6 hours after the application of these agents. 
- Dolutegravir may increase the concentrations of metformin. It is necessary to monitor patients during therapy, and metformin dosages may need to be adjusted.

Keep the drug in a dry place, protected from sun and inaccessible to children, at a temperature of 15 to 30 ° C. Date of manufacture and shelf life are indicated on the packaging.

The combination of efavirenz, emtricitabine, and tenofovir is used alone or along with other medications to treat human immunodeficiency virus (HIV) infection in adults and children weighing more than 40 kg (88 lb). Efavirenz is in a class of medications non-nucleoside reverse transcriptase inhibitors (NNRTIs). Emtricitabine and tenofovir are in a class of medications called nucleoside reverse transcriptase inhibitors (NRTIs). They work by decreasing the amount of HIV in the body. Although efavirenz, emtricitabine, and tenofovir will not cure HIV, these medications may decrease your chance of developing acquired immunodeficiency syndrome (AIDS) and HIV-related illnesses such as serious infections or cancer.