Efavirenz (Tablets) Instructions for Use

Instructions
Dosage forms

ATC Code

J05AG03 (Efavirenz)

Active Substance

Efavirenz (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antiviral drug active against HIV

Pharmacotherapeutic Group

Systemic antiviral agents; direct-acting antiviral agents; non-nucleoside reverse transcriptase inhibitors

Pharmacological Action

Antiviral agent. A non-nucleoside inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase.

Pharmacokinetics

It undergoes intensive metabolism in the liver with the participation of the CYP enzyme system. Based on in vitro studies, CYP3A4 and CYP2B6 are considered the main isoenzymes responsible for the metabolism of efavirenz.

According to a number of studies, depending on the dose, Efavirenz is an inhibitor or inducer of CYP3A4.

Less than 1% is excreted unchanged in the urine.

Indications

Infections caused by HIV-1 (as part of combination therapy).

ICD codes

Open the list of ICD codes

ICD-10 code	Indication
B24	Human immunodeficiency virus [HIV] disease, unspecified

ICD-11 code	Indication
1C62.1	HIV disease, clinical stage 2, without mention of tuberculosis or malaria

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Tablets

It is used as part of combination therapy with other antiretroviral drugs (protease inhibitors and/or nucleoside reverse transcriptase inhibitors).

When taken orally for adults and children weighing more than 40 kg, the recommended dose is 600 mg/day.

For children and adolescents (from 3 to 17 years), depending on age, the dose is 200-400 mg/day. The recommended dose for children weighing more than 40 kg is 600 mg/day.

Frequency of administration – once a day, regardless of meals.

Adverse Reactions

Dermatological reactions frequently (especially in children) – maculopapular rash; in isolated cases – severe rash accompanied by blisters, oozing desquamation, and ulcers.

From the digestive system frequently – nausea; diarrhea is possible.

From the CNS dizziness, headache, insomnia, fatigue, and impaired concentration may occur.

Allergic reactions in isolated cases – erythema multiforme, Stevens-Johnson syndrome.

From laboratory parameters increased activity of ALT, AST, GGT, amylase, increased level of total bilirubin, increased blood glucose concentration.

Contraindications

Concomitant use with terfenadine, astemizole, cisapride, midazolam, or triazolam; hypersensitivity to efavirenz.

Use in Pregnancy and Lactation

Adequate and strictly controlled clinical studies on the safety of use during pregnancy have not been conducted. Use is possible only in cases where the intended benefit to the mother outweighs the potential risk to the fetus.

During treatment, women of childbearing age should use reliable methods of contraception. Since the possible interaction of efavirenz with oral contraceptives has not been fully studied, reliable barrier methods of contraception should be used in addition to oral contraceptives.

It is not known whether Efavirenz is excreted in human breast milk.

In experimental studies, it was found that Efavirenz has teratogenic and embryotoxic effects. It has been shown that Efavirenz is excreted in the breast milk of lactating rats.

Use in Hepatic Impairment

Clinical experience with the use of efavirenz in patients with chronic liver diseases is limited. Use with caution in patients with severe liver dysfunction (since Efavirenz undergoes intensive metabolism in the liver with the participation of the CYP enzyme system).

During treatment, it is recommended to constantly monitor the activity of liver transaminases in patients with hepatitis B or C or a history of suspected these infections and in patients receiving other drugs that may have a hepatotoxic effect. In case of a persistent acute increase in transaminase activity to a level more than 5 times the upper limit of normal (ULN), the benefits of continuing treatment should be weighed against the risk of significant hepatotoxicity.

Pediatric Use

In children under 3 years of age or weighing less than 13 kg, the safety and efficacy of efavirenz have not been studied.

Special Precautions

When selecting new antiretroviral drugs for combination therapy, the possibility of cross-resistance of the virus should be taken into account.

When discontinuing efavirenz, the possibility of discontinuing treatment with other antiretroviral drugs should also be considered to avoid the emergence of resistant viruses.

During treatment, cholesterol levels should be constantly monitored.

In children under 3 years of age or weighing less than 13 kg, the safety and efficacy of efavirenz have not been studied.

Drug Interactions

With the simultaneous use of efavirenz with terfenadine, astemizole, cisapride, midazolam, or triazolam, a competitive drug interaction for the CYP3A4 isoenzyme is observed, which can lead to inhibition of the metabolism of these drugs and create the possibility of serious and/or life-threatening consequences – severe arrhythmias, prolonged sedative effect, or respiratory depression.

Under the influence of efavirenz, a decrease in the plasma concentration of drugs that are substrates of the CYP3A4 isoenzyme is possible.

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.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Efavirenz Canon [Canonpharma Production, CJS (Russia)]
Film-coated tablets, 200 mg: 30, 60, or 90 pcs.

Marketing Authorization Holder

Canonpharma Production, CJS (Russia)

Manufactured By

Academician V.P. Filatov Plant, LLC (Russia)

Canonpharma Production, CJS (Russia)

Dosage Form

Efavirenz Canon

Film-coated tablets, 200 mg: 30, 60, or 90 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets brownish-yellow, round, biconvex; the cross-section is almost white.

	1 tab.
Efavirenz	200 mg

Excipients: low-substituted hyprolose (hydroxypropylcellulose) – 10 mg, colloidal silicon dioxide – 4 mg, croscarmellose sodium – 16 mg, lactose monohydrate – 73 mg, magnesium stearate – 4 mg, sodium lauryl sulfate – 4 mg, povidone K-30 – 18 mg, microcrystalline cellulose – 71 mg.

Film coating composition Opadry yellow – 12 mg (hyprolose – 4.2 mg, hypromellose – 4.08 mg, titanium dioxide – 3.222 mg, iron oxide yellow dye – 0.4956 mg, sunset yellow FCF dye – 0.0024 mg).

30 pcs. – polymer jars (1) – cardboard packs.
60 pcs. – polymer jars (1) – cardboard packs.
90 pcs. – polymer jars (1) – cardboard packs.

Efavirenz Canon [Canonpharma Production, CJS (Russia)]
Film-coated tablets, 600 mg: 30, 60 or 90 pcs.

Marketing Authorization Holder

Canonpharma Production, CJS (Russia)

Dosage Form

Efavirenz Canon

Film-coated tablets, 600 mg: 30, 60 or 90 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets brownish-yellow, oval, biconvex; the cross-section is almost white.

	1 tab.
Efavirenz	600 mg

Excipients: low-substituted hyprolose – 30 mg, colloidal silicon dioxide – 12 mg, croscarmellose sodium – 48 mg, lactose monohydrate – 219 mg, magnesium stearate – 12 mg, sodium lauryl sulfate – 12 mg, povidone (K-30) – 54 mg, microcrystalline cellulose – 213 mg.

Film coating composition Opadry yellow – 36 mg (hyprolose – 12.6 mg, hypromellose – 12.24 mg, titanium dioxide – 9.666 mg, iron oxide yellow dye – 1.4868 mg, sunset yellow FCF dye – 0.0072 mg).

30 pcs. – polymer jars (1) – cardboard packs.
60 pcs. – polymer jars (1) – cardboard packs.
90 pcs. – polymer jars (1) – cardboard packs.

Efavirenz-Advansd [Advanced Pharma, LLC (Russia)]
Film-coated tablets, 100 mg: 30 or 100 pcs.
Film-coated tablets, 200 mg: 30 or 100 pcs.
Film-coated tablets, 300 mg: 30 or 100 pcs.
Film-coated tablets, 400 mg: 30 or 100 pcs.
Film-coated tablets, 600 mg: 30 or 100 pcs.

Marketing Authorization Holder

Advanced Pharma, LLC (Russia)

Dosage Forms

	Efavirenz-Advansd	Film-coated tablets, 100 mg: 30 or 100 pcs.
		Film-coated tablets, 200 mg: 30 or 100 pcs.
		Film-coated tablets, 300 mg: 30 or 100 pcs.
		Film-coated tablets, 400 mg: 30 or 100 pcs.
		Film-coated tablets, 600 mg: 30 or 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets round, biconvex, film-coated from yellow to brownish-yellow; the cross-section shows a white or almost white core.

	1 tab.
Efavirenz	100 mg

Excipients: lactose monohydrate – 50 mg, corn starch – 12 mg, croscarmellose sodium – 10 mg, crospovidone XL-10 – 9.33 mg, povidone K-30 – 6.67 mg, sodium lauryl sulfate – 2.83 mg, magnesium stearate – 2 mg.

Film coating: ready coating Wincoat WT-10019P white 3.6 mg (polyvinyl alcohol 45%, soy lecithin 3%, macrogol 4000 11%, titanium dioxide (E171) 30%, talc 11%), quinoline yellow dye (E 104) 0.23 mg.