tenofovir disoproxil fumarate

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Related to tenofovir disoproxil fumarate: emtricitabine

tenofovir disoproxil fumarate


Pharmacologic class: Nucleoside analog reverse transcriptase inhibitor

Therapeutic class: Antiretroviral

Pregnancy risk category B

FDA Box Warning

Severe acute exacerbations of hepatitis have been reported in patients with hepatitis B virus (HBV) infection who have discontinued anti-hepatitis B therapy. Monitor hepatic function closely with both clinical and laboratory follow-up for at least several months in patients who discontinue anti-hepatitis B therapy. If appropriate, resumption of anti-hepatitis B therapy may be warranted.

Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogs, including tenofovir.

Drug should not be given with adefovir dipivoxil.

Because of risk of development of human immunodeficiency virus-1 (HIV-1) resistance, drug should only be used in HIV-1 and HBV co-infected patients as part of an appropriate antiretroviral combination regimen.

HIV-1 antibody testing should be offered to all HBV-infected patients before start of therapy. It is also recommended that all patients with HIV-1 infection be tested for presence of chronic HBV infection before start of drug therapy.

Drug's effects on bone haven't been studied in patients with chronic HBV infection.

In HIV-infected patients, redistribution or accumulation of body fat, including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and cushingoid appearance, has been observed in patients receiving combination antiretroviral therapy.

Immune reconstitution syndrome has been reported in HIV-infected patients treated with combination antiretroviral therapy.


Inhibits activity of HIV by competing with natural substrate deoxyadenosine 5'-triphosphate; disrupts cellular DNA by causing chain termination


Powder, oral: 40 mg/scoop

Tablets: 150 mg, 200 mg, 250 mg, 300 mg

Indications and dosages

HIV-1 infection, chronic hepatitis B infection

Adults and adolescents age 12 and older weighing 35 kg (77 lb) or more: 300 mg P.O. daily; for patients unable to swallow tablets, give 7.5 scoops of oral powder.

HIV-1 infection

Children ages 2 to younger than 12: 8 mg/kg (to maximum of 300 mg) P.O. once daily as oral powder or tablets

Dosage adjustment

• Baseline creatinine clearance less than 50 ml/minute


• None


Use cautiously in:

• renal impairment

• lactic acidosis

• exacerbation of hepatitis, hepatomegaly with steatosis

• co-administration of adefovir dipivoxil or other tenofovir-containing products

• concurrent or recent use of nephrotoxic drugs.

• decreased bone marrow density

• redistribution or accumulation of body fat

• immune reconstitution syndrome

• elderly patients

• pregnant or breastfeeding patients

• children younger than age 2 with HIV-1 infection and younger than age 12 or less than 35 kg (77 lb) with chronic hepatitis B infection (safety and efficacy not established).


• Assess creatinine clearance before starting drug.

• Give tablets without regard to meals.

• Give oral powder with 2 to 4 oz of soft foods that can be swallowed without chewing (such as applesauce, baby food, or yogurt). Don't mix with liquids. Give dose immediately after mixing.

• Know that drug is usually given with other antiretrovirals for HIV infection.

Adverse reactions

CNS: headache, asthenia, depression

GI: nausea, vomiting, diarrhea, abdominal pain, flatulence, anorexia

GU: new-onset or worsening renal impairment (including acute renal failure and Fanconi syndrome)

Skin: rash

Hepatic: severe hepatomegaly with steatosis

Metabolic: hyperglycemia, lactic acidosis

Other: body fat redistribution, pain, immune reconstitution syndrome


Drug-drug. Acyclovir, cidofovir, didanosine, ganciclovir, indinavir, lopinavir, probenecid, ritonavir, valacyclovir, valganciclovir, other drugs eliminated by active tubular secretion (such as adefovir dipivoxil): increased blood level of either drug

Atazanavir, lopinavir/ritonavir: increased tenofovir concentration

Drug-diagnostic tests. Alanine aminotransferase, amylase, aspartate aminotransferase, blood and urine glucose, creatine kinase, triglycerides: increased levels

Neutrophils: decreased count

Drug-food. Any food: decreased drug bioavailability and efficacy

Patient monitoring

Watch for and report signs and symptoms of lactic acidosis or hepatotoxicity.

• Monitor bone mineral density in patients with history of pathologic fractures or who are at risk for osteopenia.

Monitor for signs of immune reconstitution syndrome, especially during initial phase of combination antiretroviral treatment when patients whose immune systems respond may develop an inflammatory response to indolent or residual opportunistic infections (such as Mycobacterium avium infection, cytomegalovirus, Pneumocystis jiroveci pneumonia, or tuberculosis), which may necessitate further evaluation and treatment.

• Monitor kidney and liver function tests.

• Assess nutritional status and hydration in light of adverse GI reactions and underlying disease.

Patient teaching

• Tell patient to take tablets once daily at the same time every day with or without food and take oral powder at the same time every day with food.

• Tell patient not to mix oral powder with liquids. Tell patient to use only the dosing scoop supplied, to mix only with 2 to 4 oz of soft foods that can be swallowed without chewing (such as baby food, applesauce, or yogurt), and to take entire dose immediately after mixing.

Instruct patient to immediately report unusual tiredness or yellowing of skin or eyes.

• Tell patient drug may cause weakness and headache. Caution him to avoid driving and other hazardous activities until he knows how drug affects performance.

• Caution female patient not to breastfeed.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and foods mentioned above.

tenofovir disoproxil fumarate

a prodrug of tenofovir, used in the treatment of HIV-1 (human immunodeficiency virus-1) infection.
References in periodicals archive ?
Regression of cirrhosis during treatment with tenofovir disoproxil fumarate for chronic hepatitis B: A 5-year open-label follow-up study.
It does not appear to cause kidney problems or loss of BMD as can be seen with tenofovir disoproxil fumarate.
Daily tenofovir disoproxil fumarate / emtricitabine is recommended for use as preexposure prophylaxis to prevent HIV infection in persons at high risk.
Participants were given access to a PrEP regimen of daily, oral tenofovir disoproxil fumarate and emtricitabine during clinical visits at 4, 12, 24, 36, and 48 weeks.
Tenofovir disoproxil fumarate {9-[(R)-2-[[bis [[isopropoxycarbonyl] oxy] methoxy] phosphonyl] methoxy] propyl] adenine fumarate} is a nucleotide analog reverse transcriptase inhibitor (NRTI) and is used for treating HIV infection in adults, in combination with other antiretroviral agents [3, 4].
Emtricitabine is marketed by Gilead under the brand name Emtriva, and a fixed-dose combination of Emtricitabine and Tenofovir Disoproxil Fumarate is made available under the brand name Truvada.
President's Emergency Plan for AIDS Relief (PEPFAR) for its New Drug Application for Dolutegravir, Lamivudine and Tenofovir Disoproxil Fumarate (TLD) tablets, 50mg/300mg/300mg.
M2 EQUITYBITES-August 21, 2017-Aurobindo Pharma gets tentative FDA approval for dolutegravir, lamivudine and tenofovir disoproxil fumarate tablets
M2 PHARMA-August 21, 2017-Aurobindo Pharma gets tentative FDA approval for dolutegravir, lamivudine and tenofovir disoproxil fumarate tablets
Tenofovir disoproxil fumarate shows promise as a highly effective therapy for HIV-positive patients with hepatitis B infections who have not responded to treatment with interferon-[alpha] and lamivudine, Maria B.
On October 3 the FDA's Antiviral Drugs Advisory Committee will hold a public hearing on tenofovir (full chemical name tenofovir disoproxil fumarate, or tenofovir DF; new brand name Viread[TM]), an antiretroviral developed by Gilead Sciences and currently in pre-approval expanded access.