| TENOFOVIR DISOPROXIL FUMARATE
(ten-o-fo'vir di-so-prox'il fum'a-rate)
Classifications: antiretroviral agent; nucleoside reverse transcriptase inhibitor (nrti); Therapeutic: antiretroviral; nrti
Pregnancy Category: B
300 mg tablets
Tenofovir is a potent inhibitor of retroviruses, including HIV-1. It may be active against nucleoside-resistant HIV strains.
The active form of tenofovir persists in HIV-infected cells for prolonged periods, thus, it results in sustained inhibition
of HIV replication.
It reduces the viral load (plasma HIV-RNA), and CD4 counts.
In combination with other antiretrovirals for the treatment of HIV.
Hypersensitivity to tenofovir; hepatitis; lactic acidosis; concurrent administration of nephrotoxic agents, renal failure;
Hepatic dysfunction, alcoholism; renal impairment; obesity; children, pregnancy (category B).
Route & Dosage
Adult: PO 300 mg once daily with meal
Clcr 3049 mL/min: dose q48h, 1029 mL/min dose twice weekly
Hemodialysis: Dose weekly or after 12 h of dialysis
- Give at the same time each day with a meal.
- Give 2 h before or 1 h after didanosine (if ordered concurrently).
- Store at room temperature; excursions to 15°30° C (59°80° F) are permitted.
Adverse Effects (≥1%)Body as a Whole:
Headache. GI: Nausea,
, flatulence, abdominal pain, anorexia. Hematologic: Neutropenia
Increased creatine kinase,
AST, ALT, serum
amylase, triglycerides, serum
May increase didanosine toxicity
; acyclovir, amphotericin B, cidofovir, foscarnet, ganciclovir, probenecid, valacyclovir, valganciclovir
may increase tenofovir toxicity
by decreasing its renal
Food increases absorption.
Bioavailability 25% fasting, 40% with high fat meal. Peak:
1 h. Distribution:
<7% protein bound. Metabolism:
Not metabolized by CYP450 enzyme system. Elimination:
Renally eliminated. Half-Life:
Assessment & Drug Effects
- Lab tests: Monitor baseline and periodic renal function and LFTs; monitor periodically serum electrolytes, and ABGs if lactic
acidosis is suspected.
- Monitor for S&S of bone abnormalities (e.g., bone pain, stress fractures).
- Monitor closely patients receiving other nephrotoxic agents for changes in serum creatinine and phosphorus. Withhold drug
and notify physician for creatinine clearance <60 mL/min.
- Withhold drug and notify physician if patient develops clinical or lab findings suggestive of lactic acidosis or pronounced
hepatotoxicity (e.g., hepatomegaly and steatosis even in the absence of marked transaminase elevations).
Patient & Family Education
- Take this drug exactly as prescribed. Do not miss any doses. If you miss a dose, take it as soon as possible and then take
your next dose at its regular time. If it is almost time for your next dose, do not take the missed dose. Wait and take
the next dose at the regular time. Do not double the next dose.
- Report any of the following to physician: unexplained anorexia, nausea, vomiting, abdominal pain, fatigue, dark urine.