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Currently, the development of active substances to treat HIV infection creates long-term life expectancy for patients. Besides, the current trend is to use products that combine many active ingredients such as Agriptera. So what is Agriptera and how is it used?1. What is Acriptega?
Ingredients Acriptega includes 3 active ingredients: Dolutegravir, Lamivudine, Tenofovir with the following strengths:Dolutegravir: 50mg; Lamivudine: 300mg; Tenofovir disoproxil: 300mg. The active ingredient Lamivudine in Agriptera is rapidly absorbed after oral administration with a bioavailability of about 80-85%. Lamivudine is eliminated mainly unchanged by the kidneys and the half-life ranges from 5 to 7 hours.
Tenofovir disoproxil fumarate is rapidly absorbed and then converted to Tenofovir. Bioavailability is approximately 25% when taken on an empty stomach, increasing with a high-fat meal. Tenofovir in Agriptera is eliminated mainly by the kidneys, both by glomerular filtration and by the renal tubular transport system with approximately 70-80% of the dose excreted unchanged in the urine.
Dolutegravir for rapid absorption after oral administration, average Tmax about 2-3 hours. Food is the factor that increases the extent but slows down the rate of absorption of Dolutegravir. Therefore, Agriptera is recommended to be taken with food in integrase-resistant HIV patients. The drug is metabolised via glucuronide binding and to a small extent via the CYP3A4 system. Unchanged form Dolutegravir is eliminated by the kidneys very little (<1% of the dose), most of which (about 53% of the oral dose) is eliminated unchanged in the faeces.
2. Uses of Acriptega
Acriptega is indicated in the following cases:Treatment of HIV-1 infection in adults and adolescents (aged 12 years and older and weighing more than 40 kg) with viral suppression to HIV1 RNA levels < 50 copies/ml according to current antiretroviral combination regimen for at least 3 months; The patient had no virological failure on previous antiretroviral regimens. Lamivudine is a dideoxynucleoside analogue and Tenofovir disoproxil fumarate is converted into Tenofovir, a Nucleoside Monophosphate analogue. Lamivudine and Tenofovir are phosphorylated via cellular enzymes to form Lamivudine triphosphate and tenofovir diphosphate. These two active ingredients competitively inhibit HIV-1 reverse transcriptase, thereby ending DNA. Therefore, the 2 active ingredients in Agriptera have anti-HIV1 and HIV2 effects, in addition to the ability to fight hepatitis B virus. The other active ingredient in Agriptera is Dolutegravir, which inhibits HIV integrase through binding to the Integrase active site and inhibiting the retroviral Deoxyribonucleic acid (DNA) integration step.
3. How to use Ascriptega?
Agriptera should be prescribed by a physician experienced in the treatment of HIV-1 infection. When using, patients need to swallow Agriptera tablets whole with a sufficient amount of water.Dosage of Agriptera:
Adults and adolescents (from 12 years of age, weighing ≥ 40kg): The recommended dose is 1 Agriptera 50/300/300 tablet, once daily; Agriptera is not recommended for use in patients weighing less than 40 kg because Agriptera is formulated in a fixed-dose combination, so it is not possible to reduce the dose; Agriptera is a fixed-dose combination tablet and is therefore not suitable for HIV-infected patients requiring dose adjustment. The single-agent preparations of Lamivudine, Tenofovir disoproxil fumarate, and Dolutegravir are now available and are preferable in situations where discontinuation or dose adjustment of one of Agriptera's active ingredients is required.
4. What are the side effects of Acriptega?
During the use of Agriptera, patients may experience some unwanted side effects (ADRs). In which very common ADRs include:Hematological disorders such as decreased neutrophil count, anemia (sometimes very severe) or thrombocytopenia; Decrease in blood phosphate levels; Dizziness, headache and insomnia; Cough or symptoms in the nose; Digestive disorders such as diarrhea, nausea, vomiting, abdominal pain, flatulence; skin rash or hair loss; Joint pain or muscle dysfunction; Systemic manifestations such as fatigue, malaise, fever. Some rare side effects of Agriptera drug:
Simple red blood cell aplasia; Lactic acidosis; Peripheral neuropathy; Shortness of breath; Pancreatitis, increased serum amylase or hepatitis; Acute renal failure, proximal tubular disease, increased serum creatinine or acute tubular necrosis.
5. Contraindications of the drug Acriptega
Acriptega should not be used in the following cases:People with a history of allergy to Tenofovir, Lamivudine, Dolutegravir and the excipients in Agriptera tablets; Contraindicated when used in combination with Dofetilide.
6. Some cautions when using Agriptega
Acriptega tablets should not be used at the same time as products containing the active ingredients Dolutegravir, Lamivudine, Tenofovir disoproxil fumarate or Cytidine analogues (such as emtricitabine and adefovir dipivoxil); Possibility of HIV transmission : Treatment with Agriptera does not completely eliminate the possibility of transmitting HIV to others through sex or blood, although the risk may be reduced. Therefore, people living with HIV must continue to use appropriate HIV prevention measures; The safety of dolutegravir has not been studied in patients with severe liver disease. Therefore, Acriptega should only be used in patients with liver disease when the benefits outweigh the risks to health and close monitoring is required for safety; HIV patients who are coinfected with hepatitis B virus or hepatitis C should be aware of this because people with chronic hepatitis B or C on antiretroviral combination therapy have an increased risk of serious adverse effects on the liver, even even fatal; Hypersensitivity reactions related to Dolutegravir in Agriptera have been reported, characterized by rash and sometimes organ dysfunction; Renal function: Tenofovir is eliminated primarily by the kidneys through a combination of glomerular filtration and tubular secretion. Therefore, the clearance of Agriptera may be impaired in patients with impaired renal function; Lactic acidosis is a rare but potentially life-threatening complication associated with Nucleoside reverse transcriptase inhibitors (nNRTIs); Pancreatitis: Treatment with Acriptega should be stopped immediately if clinical symptoms or blood test results suggest pancreatitis; Opportunistic infections: People on antiretroviral therapy such as Agriptera are at increased risk of developing opportunistic infections or other complications of HIV infection. Some cautions about Agriptera in pregnancy:Some animal studies have not shown any direct or indirect effects of Tenofovir disoproxil fumarate on maternal health. fetal development, labor, or postnatal fetal development. In humans, the safety of Tenofovir during pregnancy has not been adequately studied; There are no reports of risk of birth defects in the fetus when pregnant women use Lamivudine . However, this does not completely eliminate the risk of harm to the fetus of Agriptera; There is not too much evidence about the use of dolutegravir in pregnant women. As a result, the effects of this active ingredient on pregnancy have not been fully established, and therefore, dolutegravir should be used during pregnancy only when the potential benefit outweighs the potential risk to the fetus. Some cautions of Agriptera in lactation:
Animal studies indicate that Tenofovir is excreted in human milk, however this ability in humans is not known. Another active ingredient in Agriptera, Lamivudine, has been shown to be excreted in breast milk; It is not known whether Dolutegravir is excreted in human milk, although animal studies have shown the active ingredient to be found in human milk; Current recommendations suggest that HIV-infected women should under no circumstances breastfeed to avoid transmitting HIV to their babies.
7. Agriptera . Drug Interactions
7.1. Lamivudine active ingredient interactions
Co-administration of Lamivudine with Trimethoprim/Sulfamethoxazole may result in a 40% increase in Lamivudine AUC. However, in this case it is not necessary to adjust the dose of Acriptega. In the opposite direction Lamivudine did not affect the pharmacokinetics of Trimethoprim or Sulfamethoxazole.7.2. Tenofovir-related interactions
Didanosine: Concomitant use of products containing Tenofovir disoproxil fumarate (such as Agriptera) and Didanosine is not recommended; Drugs Excreted by Renal: Tenofovir is eliminated mainly by the kidneys, therefore, concomitant administration of Tenofovir disoproxil fumarate with products that may impair renal function or compete for tubular secretion will increase the concentration of Tenofovir. serum and/or concomitant medicinal products; Tenofovir disoproxil fumarate should be avoided concurrently with nephrotoxic drugs, such as Aminoglycoside antibiotics, Amphotericin B, Foscarnet, Ganciclovir, Pentamidine, Vancomycin, Cidofovir or interleukin-2; Tenofovir must be taken with food because food increases the bioavailability of Tenofovir.7.3. Dolutegravir-related interactions
All factors that decrease Dolutegravir exposure should be avoided in the presence of integrase resistance; Dolutegravir is eliminated primarily through the metabolism of UGT1A1, so drugs that induce this enzyme may decrease the plasma concentration of Dolutegravir and reduce its therapeutic effect.Please dial HOTLINE for more information or register for an appointment HERE. Download MyVinmec app to make appointments faster and to manage your bookings easily.
