Generic Epivir – Antiviral Agent for HIV and HIB
Epivir is an antiviral agent. It belongs to the group of nucleoside reverse transcriptase inhibitor. Penetrating into cells, it is metabolized to 5-triphosphate, which inhibits HIV reverse transcriptase. It contributes to inhibition of viral replication. It is active against strains resistant to zidovudine. When used in combination with it, it slows down the development of viral resistance to zidovudine (in previously untreated patients). It has a higher in vitro therapeutic index than zidovudine. It slightly affects the metabolism of cellular deoxynucleotides and the DNA content in the mitochondria of intact cells. Lamivudine is highly active against hepatitis B virus (HBV) in all studied cell lines and in all experimentally infected animals.
When this medicine is applied?
- Treatment of HIV infection in adults and children (as part of combination therapy with other antiretroviral drugs);
- Chronic viral hepatitis B associated with HBV replication in patients aged 16 and over.
The main contraindication is hypersensitivity to lamivudine or any drug excipients. If you have any specific diagnosis, inform your doctor, in any case. The doctor will assess the condition and decide whether this drug suits you or not.
Is it possible to apply this medicine during pregnancy and lactation?
There is data from pregnant women (over 1000 pregnancy outcomes) that indicate no malformative toxicity. Generic Epivir can be used during pregnancy if the drug is indicated for clinical reasons.
For patients with hepatitis co-infection who receive lamivudine and subsequently become pregnant, the possibility of hepatitis recurrence should be considered if lamivudine is withdrawn.
Nucleoside and nucleotide analogs have been shown in in vivo and in vitro studies to cause mitochondrial damage of varying degrees. There have been reports of mitochondrial dysfunction in children exposed to nucleoside analogs in the womb and/or postnatal period. After oral administration, lamivudine is excreted in breast milk; at the same time, its concentration in breast milk practically does not differ from its concentration in serum. Because HIV and lamivudine pass into breast milk, women taking lamivudine are recommended to discontinue breastfeeding.
Mode of application and dosage
The appointment of Epivir is allowed only by a specialist with experience in the treatment of HIV infection. It is administered orally regardless of food intake (before, during or after meals).
To ensure the accuracy of dosage, the tablets are recommended to be swallowed without chewing.
For the treatment of children and those patients who find it difficult to swallow tablets, an oral solution is used. The entire amount of the resulting mixture must be taken orally immediately.
Possible side effects
- The hematopoietic and lymphatic system: eutropenia and anemia (sometimes severe), thrombocytopenia; aplasia of the erythroid lineage of the bone marrow.
- The nervous system: headache, insomnia; peripheral neuropathy (or paresthesia).
- The respiratory system and mediastinal organs: cough, nasal symptoms.
- The gastrointestinal tract: nausea, vomiting, abdominal pain or colic, diarrhea; pancreatitis, increased serum amylase activity.
- The hepatobiliary system: a transient increase in the activity of hepatic enzymes; hepatitis.
- Skin and subcutaneous tissue disorders: rash, alopecia, angioedema.
- The musculoskeletal system and connective tissue: arthralgia, muscle disorders; rhabdomyolysis.
- General disorders and reactions at the injection site: a feeling of fatigue, malaise, fever.
Is an overdose possible?
There are few data on the consequences of acute overdose of lamivudine in humans. There were no lethal outcomes, the condition of all patients returned to normal. There were no specific signs or symptoms of lamivudine overdose.
Treatment: it is recommended to monitor the patient’s state and carry out standard supportive therapy. Since lamivudine is eliminated from the body through dialysis, continuous hemodialysis is possible, but no specific studies have been conducted.
The likelihood of metabolic interaction is low, considered the limited metabolism of the drug and the low level of its binding to proteins, as well as its almost complete excretion by the kidneys unchanged.
Epivir (Lamivudine) is excreted mainly by active organic cationic secretion. It is necessary to take into account the possibility of interaction with drugs that are used simultaneously with lamivudine, especially when the main route of excretion is active renal secretion with the participation of an organic cationic transport system (for example, trimethoprim). Other active substances (eg ranitidine, cimetidine) are only partially secreted in this way, so they do not interact with lamivudine. Active substances, that are excreted mainly by active organic anionic secretion or glomerular filtration, obviously do not contribute to clinically significant interactions with lamivudine.
There is a moderate increase in the maximum level of zidovudine (28%) with the simultaneous administration of zidovudine and lamivudine, although in general the concentration does not change significantly. Zidovudine does not affect the pharmacokinetics of lamivudine.
Epivir can suppress intracellular phosphorylation with zalcitabine while using these drugs. Therefore, this drug is not recommended for use in combination with zalcitabine.