Heptavir

Heptavir is an antiviral medication with a direct type of therapeutic activity. It is included in the group of nucleoside-type agents that slow down the action of reverse transcriptase.

Once inside the cell, lamivudine undergoes phosphorylation with the formation of a 5-3-phosphate metabolic element with activity - lamivudine-3-phosphate, which is a substrate for hepatovirus B polymerase; this component slows down the activity of HIV reverse transcriptase. Lamivudine-3-phosphate does not interfere with normal cell DNA metabolism. [1]

Indications Heptavir

It is used in complex therapy along with other antiretroviral substances in people with HIV infection .

Release form

The release of drugs is realized in tablet form - 10 pieces inside the contour packs; the box contains 10 such packs.

Pharmacokinetics

Lamivudine has good absorption within the digestive system; after oral administration, the bioavailability values in an adult are 80-85%. Protein synthesis rate - 36%. Serum Cmax is noted after 60 minutes. In the case of administration of therapeutic portions, it is approximately 1.1-1.5 μg / ml; the minimum values are equal to 0.015-0.02 μg / ml.

The level of the distribution volume is 1.3 ± 0.4 l / kg.

The consumption of lamivudine with food prolongs the period required to obtain the Cmax level and its indicators themselves (up to 47%), but at the same time does not change the total value of the absorbed element, which allows the drug to be taken with food.

The mean total clearance of lamivudine is 0.3 l / h / kg. The half-life is in the range of 5-7 hours. For the most part, the substance is excreted in the urine in an unchanged state - through active excretion and CF. Intrarenal clearance rates are about 70% of the excreted lamivudine.

Dosing and administration

Adults need to orally consume 0.15 g of the medication 2 times a day. Treatment is carried out in combination with other antiretroviral drugs.

In the case of Heptavir therapy in people who are infected with 2 viruses at once - HBV and HIV - the portion recommended for HIV treatment should be used as an integral part of the selected complex therapy regimen.

• Application for children

For a child weighing less than 40 kg, you need to use other forms of release of this medication.

Contraindications

It is contraindicated to prescribe a medication to people with diagnosed clinical intolerance to the elements of the medication.

Women with HIV infection are prohibited from breastfeeding, as this can lead to infection of the infant.

Side effects Heptavir

Among the side symptoms:

• problems with digestive function: diarrhea, discomfort and pain in the epigastric zone, vomiting, weakening or loss of appetite, nausea, and also pancreatitis and an increase in plasma amylase values or intrahepatic transaminase activity;
• disorders of hematopoietic processes: thrombocytopenia or neutropenia, as well as anemia;
• disorders associated with the work of the central nervous system: headaches, polyneuropathy, fatigue and paresthesia;
• others: fever, alopecia and respiratory tract infections.

Overdose

Potentiation of side symptoms is a sign of drug poisoning.

Gastric lavage, forced diuresis and the appointment of activated carbon are performed. In addition, symptomatic actions are performed.

Interactions with other drugs

The combined use of the medication with interferon leads to a slight decrease in the AUC indicator of lamivudine (by 10%); the pharmacokinetics of interferon remains unchanged. No interactions between these drugs are recorded.

The combination of Heptavir with sulfonamides, didanosine or zalcitabine increases the likelihood of pancreatitis.

Administration with myelosuppressive (sulfanamides, amphotericin with ganciclovir, flucytocin trimetrexate and pyrimethamine with dapsone) or cytotoxic agents can provoke the development of hematotoxicity.

The combination with drugs with nephrotoxic activity (aminoglycosides, pentamidine with amphotericin and foscarnet with cidofovir) increases the values of lamivudine.

The use together with didanosine, zalcitabine, and in addition with isoniazid, dapsone and stavudine increases the likelihood of developing polyneuropathy.

Storage conditions

Keep Heptavir out of the reach of young children. The temperature level is in the range of 15-30 ° С.

Shelf life

Heptavir can be used within a 2-year term from the date of manufacture of the therapeutic product.

Analogs

Analogues of drugs are Sebivo, Baraklud and Stag with Zeffix, and in addition, Retrovir, Viread with Tenofovir-tl, Azidothimin and Ziagen with Emtricitabine.