Telzir (Tablets, Suspension) Instructions for Use

ATC Code

J05AE07 (Fosamprenavir)

Active Substance

Fosamprenavir (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antiviral drug active against HIV

Pharmacotherapeutic Group

Antiviral [HIV] agent

Pharmacological Action

Antiviral agent, is a prodrug of amprenavir. Amprenavir is a non-peptide competitive inhibitor of HIV protease.

It blocks the ability of the viral protease to cleave the precursor polyproteins necessary for viral replication.

Amprenavir is a selective inhibitor of HIV-1 and HIV-2 replication.

Indications

Treatment of HIV infection (in combination with ritonavir).

ICD codes

Dosage Regimen

Administer Telzir in combination with ritonavir and other antiretroviral agents. Do not use as monotherapy.

For treatment-naïve adults, the recommended dosage is Telzir 700 mg plus ritonavir 100 mg, both taken twice daily.

For protease inhibitor-experienced adults with no mutations, the recommended dosage is Telzir 700 mg plus ritonavir 100 mg, both taken twice daily.

For adults taking efavirenz, the recommended dosage is Telzir 700 mg plus ritonavir 100 mg, both taken twice daily.

An alternative regimen for treatment-naïve adults is Telzir 1400 mg plus ritonavir 100 mg or 200 mg, both taken once daily.

Take orally, with or without food. Swallow tablets whole; do not chew, crush, or split.

Adjust the dosage when co-administered with specific drugs. Increase the dose to Telzir 700 mg twice daily plus ritonavir 100 mg twice daily when given with fosamprenavir.

For patients with mild hepatic impairment (Child-Pugh Class A), reduce the dosage to Telzir 700 mg twice daily without ritonavir. Contraindicated in moderate or severe hepatic impairment.

No dosage adjustment is required for patients with renal impairment.

The safety and efficacy in pediatric patients have not been established.

Adverse Reactions

From the digestive system frequently – nausea, diarrhea, abdominal pain, vomiting, increased activity of AST and ALT.

From the CNS frequently – headache.

Other frequently – increased lipase content, triglycerides.

Contraindications

Moderate or severe liver dysfunction; simultaneous use (in combination with ritonavir) with drugs with a narrow therapeutic index that are substrates of CYP3A4, with drugs metabolized by the CYP2D6 isoenzyme; simultaneous use (in combination with ritonavir) with rifampicin; lactation period (breastfeeding); hypersensitivity to fosamprenavir, amprenavir, ritonavir.

Use in Pregnancy and Lactation

Use during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.

Use during the lactation period (breastfeeding) is contraindicated.

Use in Hepatic Impairment

Contraindicated in moderate or severe liver dysfunction.

Safety data on the use of fosamprenavir in patients with liver dysfunction are limited.

Use in Renal Impairment

Safety data on the use of fosamprenavir in patients with renal impairment are limited.

Pediatric Use

The safety and efficacy of fosamprenavir in children and adolescents have not been established.

Special Precautions

The safety and efficacy of fosamprenavir in children and adolescents have not been established.

Safety data on the use of fosamprenavir in patients with liver and/or kidney dysfunction are limited.

There are reports that in patients with hemophilia A and B taking protease inhibitors, hemorrhagic complications increased, including spontaneous skin hematomas and hemarthroses. Some of these patients were additionally administered factor VIII. In more than half of the described cases, treatment with protease inhibitors was continued or resumed after their temporary withdrawal. Patients with hemophilia should be warned about the possible increase in bleeding during treatment with protease inhibitors.

Treatment with antiretroviral drugs, including fosamprenavir, does not prevent the risk of transmitting HIV to other people through sexual contact or blood transfusion, so patients must take appropriate precautions.

Effect on the ability to drive vehicles and mechanisms

No specific studies have been conducted to study the effect of amprenavir on the ability to drive a car and operate moving machinery and complex equipment.

Drug Interactions

Fosamprenavir is characterized by a wide range of drug interactions, since it is an inhibitor of the CYP3A4 isoenzyme, and in combination with ritonavir – also of CYP2D6 (if it is necessary to use other drugs during therapy with this combination, the possibility of developing adverse effects should be taken into account and the doses of drugs and the treatment regimen should be adjusted accordingly).

In vitro, a synergistic effect of amprenavir is noted when combined with nucleoside analogues (including didanosine, zidovudine, abacavir) and with the protease inhibitor saquinavir. In combination with indinavir, ritonavir and nelfinavir, amprenavir has an additive effect.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°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.