Tenviral®

Therapeutic Area:

,

Generic Name:

Tenofovir

Dosage Form:

tablet

Drug Dose

Therapeutic Indications:

Chronic hepatitis B: Treatment of chronic hepatitis B virus (HBV) in patients ≥2 years of age weighing

≥10 kg

HIV-1 infection, treatment: Treatment of HIV-1 infection in patients ≥2 years of age weighing ≥10 kg, in

combination with other antiretroviral agents

Mechanism of Action:

Tenofovir disoproxil fumarate (TDF), a nucleotide reverse transcriptase inhibitor, is an analog of adenosine 5′-monophosphate; it interferes with the HIV viral RNA dependent DNA polymerase resulting in inhibition of viral replication. TDF is first converted intracellularly by hydrolysis to tenofovir and subsequently phosphorylated to the active tenofovir diphosphate. Tenofovir inhibits replication of HBV by inhibiting HBV polymerase.

Method of Administration:

Hepatitis B infection: Oral: 300 mg once daily

HIV-1 infection, treatment: Oral: 300 mg once daily

Notes

Contraindications:

Hypersensitivity to tenofovir or any component of the formulation

Interactions:

Acyclovir-Valacyclovir: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Acyclovir-Valacyclovir. Risk C: Monitor therapy

Aminoglycosides: May increase the serum concentration of Tenofovir Products. Tenofovir Products may increase the serum concentration of Aminoglycosides. Risk C: Monitor therapy

Atazanavir: Tenofovir Disoproxil Fumarate may decrease the serum concentration of Atazanavir. Atazanavir may increase the serum concentration of Tenofovir Disoproxil Fumarate. Management: Use boosted atazanavir in adults; give combo (atazanavir/ritonavir or atazanavir/cobicistat with tenofovir) as a single daily dose with food. Pediatric patients, pregnant patients, and use of H2-blockers require dose changes. Risk D: Consider therapy modification

Ledipasvir: May increase the serum concentration of Tenofovir Disoproxil Fumarate. Management: Avoid this combination if TDF is used as part of the elvitegravir/cobicistat/emtricitabine/TDF product. Consider alternatives when TDF is used with a ritonavir or cobicistat boosted protease inhibitor. Monitor for increased TDF toxicities if combined. Risk D: Consider therapy modification

Nonsteroidal Anti-Inflammatory Agents: May enhance the nephrotoxic effect of Tenofovir Products. Management: Seek alternatives to these combinations whenever possible. Avoid use of tenofovir with multiple NSAIDs or any NSAID given at a high dose due to a potential risk of acute renal failure. Diclofenac appears to confer the most risk. Risk D: Consider therapy modification

Pregnancy and Lactation:

No increased risk of overall teratogenic effects has been observed following first trimester exposure according to data collected by the antiretroviral pregnancy registry.

Tenofovir disoproxil fumarate is a recommended component of a regimen when acute HIV infection is detected in patients who are breastfeeding.

Warning and Precaution:

  • Chronic hepatitis B: Severe, acute exacerbation of hepatitis B may occur upon discontinuation. Monitor hepatic function several months after discontinuing treatment; reinitiation of antihepatitis B therapy may be required. Posttreatment hepatitis B exacerbation may lead to hepatic decompensation and hepatic failure, especially in patients with advanced hepatic disease or cirrhosis. Treatment of HBV in patients with unrecognized/untreated HIV may lead to HIV resistance; patients should be tested for presence of HIV infection prior to initiating therapy
  • Hepatic impairment: Use with caution in patients with hepatic impairment. Limited data supporting treatment of chronic hepatitis B in patients with decompensated liver disease; observe for increased adverse reactions, including renal dysfunction.
  • Renal impairment: Use with caution in patients with renal impairment

Adverse Reactions:

Central nervous system: Insomnia (3% to 18%), headache (5% to 14%), pain (12% to 13%), dizziness (8% to 13%), depression (4% to 11%)

Dermatologic: Skin rash (includes maculopapular, pustular, or vesiculobullous rash; pruritus; or urticaria: 5% to 18%), pruritus (16%)

Endocrine & metabolic: Hypercholesterolemia (19% to 22%), increased serum triglycerides (1% to 4%)

Gastrointestinal: Abdominal pain (4% to 22%), nausea (8% to 20%), diarrhea (9% to 16%), vomiting (2% to 13%)

Neuromuscular & skeletal: Decreased bone mineral density (28%; ≥5% at spine or ≥7% at hip), increased creatine phosphokinase (2% to 12%), weakness (6% to 11%)

Storage:

Store below 30ºC and protect from light and moisture.