Azvudine (Tablets) Instructions for Use

Marketing Authorization Holder

Beijing Union Pharmaceutical Factory Ltd. (China)

ATC Code

J05AX (Other antiviral drugs)

Active Substance

Azvudine (Grouping name)

Dosage Form

Azvudine

Tablets 1 mg: 35 pcs.

Dosage Form, Packaging, and Composition

Tablets are round, biconvex, white or almost white in color.

Excipients: lactose monohydrate – 26.75 mg, microcrystalline cellulose – 105 mg, croscarmellose sodium – 12 mg, povidone (K30) – 4.5 mg, magnesium stearate – 0.75 mg.

35 pcs. – high-density polyethylene bottles (1) – cardboard packs.

Clinical-Pharmacological Group

Antiviral drug

Pharmacotherapeutic Group

Systemic antiviral agents; direct-acting antiviral agents; other antiviral agents

Pharmacological Action

Azvudine is a dual-target inhibitor of HIV reverse transcriptase and the accessory protein Vif. It is a synthetic nucleoside analogue that can be phosphorylated in cells to become the active metabolite 5'-triphosphate (azvudine triphosphate). Azvudine triphosphate inhibits the activity of recombinant HIV reverse transcriptase, leading to the termination of viral DNA chain synthesis. Azvudine is a broad-spectrum RNA virus inhibitor that can inhibit the novel coronavirus RNA-dependent RNA polymerase (RdRp).

In vitro tests have shown that the active metabolite of azvudine, azvudine monophosphate, has in vitro antiviral activity against coronaviruses and novel coronaviruses.

Pharmacokinetics

When taken orally at a dose of 2 mg, C_max was reached in 1.1-1.94 hours and was 1.95-2.17 ng/ml, and T_1/2 was 7.43-9.69 hours. It has been shown that taking it after a meal increases the exposure of azvudine in the body. It practically does not bind to plasma proteins. The excretion of azvudine within 0-12 hours after a single oral dose on an empty stomach accounts for more than 70% of the total excretion within 0-24 hours. The total excretion of azvudine in urine increased with increasing dose.

Indications

Treatment of novel coronavirus infection (COVID-19), confirmed by diagnostic test results for SARS-CoV-2, with mild or moderate severity in adult patients.

ICD codes

Dosage Regimen

Administer orally at a dose of 5 mg once daily.

Complete the full treatment course of 14 days.

Initiate therapy as early as possible after a confirmed diagnosis of novel coronavirus infection (COVID-19).

Begin treatment within 5 days of the onset of the first symptoms.

Take the tablet with food to increase systemic exposure.

For patients with moderate or severe renal impairment (GFR less than 70 ml/min/1.73 m²), use with caution and monitor blood biochemical parameters.

For patients with moderate or severe hepatic impairment, use with caution and monitor blood biochemical parameters.

Do not use in children and adolescents under 18 years of age.

Contraindicated during pregnancy, pregnancy planning, and breastfeeding.

Women of childbearing potential must use effective contraception during treatment and for 4 days after the last dose.

Adverse Reactions

Digestive system frequently – diarrhea, heartburn, abdominal bloating, nausea, abdominal pain; rarely – vomiting, abnormal stool.

Nervous system rarely – headache.

Musculoskeletal system rarely – back pain.

Respiratory system frequently – respiratory failure.

Laboratory and instrumental data frequently – increased ALT concentration, increased AST concentration, increased glucose concentration, increased GGT concentration, thrombocytosis.

Contraindications

Hypersensitivity to azvudine; pregnancy or pregnancy planning, breastfeeding period; children and adolescents under 18 years of age.

With caution

Moderate and severe renal failure (GFR less than 70 ml/min/1.73 m²) and in patients with moderate and severe hepatic impairment, monitoring of blood biochemical parameters is necessary.

Use in Pregnancy and Lactation

Since reproductive toxicity was observed in animal studies of azvudine, its use is contraindicated in cases of confirmed or suspected pregnancy.

Women of childbearing potential should be informed about the potential risk to the fetus. During treatment and for 4 days after taking the last dose of azvudine, effective methods of contraception should be used.

If necessary, use in women capable of childbearing (including those with less than 2 years of postmenopause) requires confirmation of a negative pregnancy test result before starting treatment. A repeat pregnancy test should be performed after the completion of azvudine use.

Use is contraindicated during breastfeeding.

Use in Hepatic Impairment

Use with caution in patients with moderate and severe hepatic impairment.

Use in Renal Impairment

Use with caution in moderate and severe renal failure (GFR less than 70 ml/min/1.73 m²).

Pediatric Use

Use is contraindicated in children and adolescents under 18 years of age.

Special Precautions

Use of azvudine is possible only under medical supervision.

Effect on ability to drive vehicles and operate machinery

During treatment, one should refrain from driving a car, as well as engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Concomitant administration of azvudine and tenofovir may reduce the C_max and AUC of tenofovir by 18% and 6%, respectively. There is no need to adjust the tenofovir dose.

When azvudine was co-administered with efavirenz, the steady-state C_max and AUC of azvudine were 177% and 189%, respectively, of the values for each active substance separately. Efavirenz significantly increased the exposure of azvudine in vitro.

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.