Zidovudine + Lamivudine - instructions for use, dose, side effects, contraindications

Synthetic analogue of thymidine,under the action of cellular kinases phosphorylated in zidovudine monophosphate, and then under the influence of the enzymes of the host cell is converted to di- and triphosphate, which, due to competition with deoxythymidine triphosphate, suppresses the replication of the human immunodeficiency virus by inhibiting the HIV reverse transcriptase. Thus, the synthesis of mRNA and, correspondingly, the proteins of the virus is disrupted.

Lamivudine

The synthetic analogue of thymidine, under the action of cellular kinases, is phosphorylated into 5-phosphate, which, due to competition with deoxythymidine triphosphate, suppresses replication of the human immunodeficiency virus by inhibiting HIV reverse transcriptase. Thus, the synthesis of mRNA and, correspondingly, the proteins of the virus is disrupted. It is active against the hepatitis B virus.

Pharmacokinetics:

Zidovudine

After oral ingestion, up to 65% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 0.5-1.5 hours. The connection with plasma proteins is 38%.

Penetrates through the blood-brain and placental barrier. Metabolism in the liver.

The elimination half-life is 1 hour. Elimination by the kidneys.

Lamivudine

After oral administration, up to 88% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 1 hour. The connection with plasma proteins is 36%.

Penetrates through the blood-brain and placental barrier. Metabolism in the liver.

The half-life is 5-7 hours. Elimination by the kidneys.

Indications:

It is used to treat HIV infection.

ICD-10

I.B20-B24 Disease caused by the human immunodeficiency virus [HIV]

Contraindications:

Violations of kidney function, neutropenia, anemia, peripheral neuropathy, individual intolerance, children under 12 years.

Carefully:

Dysfunction of the liver, hypersensitivity.

Pregnancy and lactation:

Recommendations for FDA - Category C. When pregnancy is used with caution, in those cases where the predicted benefit overcomes the risk to the fetus. According to existing recommendations, HIV-infected women are recommended to avoid breastfeeding because of the risk of infection of the child. Given these recommendations, patients receiving zidovudine, breastfeeding should be prohibited.

Dosing and Administration:

Inside, regardless of food intake, 1 tablet 2 times a day.

Side effects:

Central and peripheral nervous system: asthenia, headache, hallucinations, insomnia, paresthesia, peripheral neuropathy.

Respiratory system: cough.

Hemopoietic system: anemia, leukopenia, thrombocytopenia, pancytopenia.

Digestive system: anorexia, pancreatitis, dyspepsia, flatulence, increased levels of hepatic transaminases, hepatomegaly with fatty liver dystrophy.

Musculoskeletal system: arthralgia, myalgia.

Dermatological reactions: hyperpigmentation of the mucous membrane of the mouth, skin, nails.

Allergic reactions.

Overdose:

Increased side effects, neuropathy.

Treatment is symptomatic, continuous hemodialysis.

Interaction:

Simultaneous use with myelosuppressive and nephrotoxic drugs (dapsone, pentamidine, pyrimethamine, amphotericin, co-trimoxazole, doxorubicin, ganciclovir, flucytosine, interferon, vinblastine, vincristine) increases the risk of side effects.

Ribavirin blocks the antiviral activity of zidovudine.

Trimethoprim increases the concentration of lamivudine by 40%.

Special instructions:

Monitoring of the cellular composition of peripheral blood.

Admission of the drug does not prevent the development of opportunistic infections and does not reduce the risk of HIV infection through the blood and during sexual intercourse.

In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

Instructions

Zidovudine + Lamivudine (Zidovudinum + Lamivudinum)