Nikavir (Tablets) Instructions for Use

ATC Code

J05AD (Phosphonic acid derivatives)

Active Substance

Phosphazide (Group Name)

Clinical-Pharmacological Group

Antiviral drug active against HIV

Pharmacotherapeutic Group

Antiviral [HIV] agent

Pharmacological Action

Antiviral agent active against HIV. It suppresses the activity of HIV-1 reverse transcriptase by being incorporated into the viral DNA, disrupts its chain elongation, and stops the growth of the viral DNA molecule.

It suppresses the replication of other retroviruses.

It is active against Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans.

Pharmacokinetics

Absorption is high (time to complete absorption is 3 hours), bioavailability is 83.7%.

It penetrates the blood-brain barrier and placenta; the concentration in the cerebrospinal fluid is 15-64% of the initial dose.

T_1/2 is 2.5 hours.

It is metabolized in the liver to form a glucuronide, which is excreted by the kidneys.

Indications

HIV infection: stage of secondary diseases (3A, 3B, 3C according to the Pokrovsky classification), stage of acute infection (2A), primary clinical manifestations (2B, 2C), decrease in the number of CD4 T-lymphocytes to less than 400-500/µl, increase in HIV RNA to more than 20 thousand copies per 1 ml (when determined by RT PCR), incubation stage (stage 1).

Prophylaxis in case of risk of HIV infection with contaminated biological material due to needle sticks, cuts, contact with mucous membranes in laboratories, during surgical, gynecological, dental operations and manipulations, during sexual contacts and intravenous drug use.

ICD codes

Dosage Regimen

Tablets

Take orally, before meals. The daily dose is taken in 2 divided doses.

Adults: 0.6-1.2 g/day; children: 10-20 mg/kg/day.

For CNS lesions, the daily dose is 1.2 g; if side effects develop, the dose is 0.4 g/day.

It is prescribed for a long, unlimited period; if necessary, in intermittent courses of at least 3 months.

According to the continuous regimen, treatment is carried out in patients with acute HIV infection (stage 2A) for the period of clinical manifestations (plus 1 month after, but not less than 3 months); in stage 3C – continuously; in stages 3A and 3B – for atypical manifestations.

In stages 3A and 3B (in the phase of absence of clinical manifestations), 2B and 2C, it is prescribed when the number of CD4 T-lymphocytes is from 200/µl to 500/µl in courses of 3 months, with 3-month intervals.

For prophylaxis of HIV infection, take no later than 72 hours after the suspected infection, 0.6 g twice a day, for 4 weeks.

Adverse Reactions

Possible nausea, headache, diarrhea; skin rashes, itching, weakness, decreased appetite, anemia.

Contraindications

Vomiting, anemia (Hb less than 50 g/l), increased activity of hepatic transaminases (more than 5 times the upper limit of normal), hypercreatininemia, neutropenia (less than 500/µl), thrombocytopenia (less than 25,000/µl); pregnancy (first 14 weeks), lactation period, hypersensitivity to the active substance.

Use in Pregnancy and Lactation

Contraindicated during pregnancy (first 14 weeks) and during lactation.

Use in Hepatic Impairment

Contraindicated in cases of increased activity of hepatic transaminases (more than 5 times the upper limit of normal).

Special Precautions

It is used in combination with other antiretroviral agents in combined treatment regimens, except for the combination with zidovudine and didanosine.

Irregular intake (violation of the treatment regimen) may lead to the development of resistance, reduced therapy effectiveness, and the need to replace the drug.

If severe side effects develop, treatment is discontinued until the normal condition is restored.

When assessing drug tolerance, it should be taken into account that the indicated side effects may be a manifestation not only of therapy but also of the HIV infection itself and concomitant diseases.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.