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Tenofovir Disoproxil Fumarate (Monograph)

Brand name: Viread
Drug class: HIV Nucleoside and Nucleotide Reverse Transcriptase Inhibitors

Medically reviewed by Drugs.com on Mar 10, 2024. Written by ASHP.

Warning

    Severe Acute Exacerbation of Hepatitis B Virus (HBV) Infection
  • Severe, acute exacerbations of HBV reported following discontinuance of HBV treatment, including tenofovir disoproxil fumarate (tenofovir DF). Monitor hepatic function closely with both clinical and laboratory follow-up for at least several months after tenofovir DF is discontinued. If appropriate, initiation or resumption of HBV treatment may be warranted.

Introduction

Antiretroviral; HIV nucleotide reverse transcriptase inhibitor (NRTI); also has antiviral activity against HBV.

Uses for Tenofovir Disoproxil Fumarate

Treatment of HIV Infection

Treatment of HIV-1 infection in adults, adolescents, and pediatric patients ≥2 years of age weighing ≥10 kg; used in conjunction with other antiretrovirals.

Commercially available as a single entity and in various fixed-combination preparations that contain 2 or 3 additional antiretrovirals; refer to separate combination product monographs for information related to the specific uses of these products.

Tenofovir disoproxil fumarate (tenofovir DF) is commonly used as part of a dual-NRTI “backbone” of a fully suppressive antiretroviral regimen; consult guidelines for the most current information on recommended regimens. Selection of an initial antiretroviral regimen should be individualized based on factors such as virologic efficacy, toxicity, pill burden, dosing frequency, drug-drug interaction potential, resistance test results, comorbid conditions, access, and cost.

Preexposure Prophylaxis for Prevention of HIV-1 Infection

Used in combination with emtricitabine for preexposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection in at-risk HIV-negative adults and adolescents; refer to the combination product monograph for detailed information on this use.

Guideline-recommended options for PrEP include oral emtricitabine/tenofovir DF in sexually active adults and adolescents and men and women who inject drugs, oral emtricitabine/tenofovir alafenamide in men and transgender women who have sex with men, and IM cabotegravir in adults and adolescents.

Postexposure Prophylaxis following Occupational Exposure to HIV

Postexposure prophylaxis of HIV infection following occupational exposure [off-label] (PEP) in health-care personnel and others exposed via percutaneous injury (e.g., needlestick, cut with sharp object) or mucous membrane or nonintact skin (e.g., chapped, abraded, dermatitis) contact with blood, tissue, or other body fluids that might contain HIV. Used in conjunction with other antiretrovirals.

USPHS recommends 3-drug regimen of raltegravir in conjunction with emtricitabine and tenofovir DF as the preferred regimen for PEP following occupational exposures to HIV. Several alternative regimens that include an integrase strand transfer inhibitor (INSTI), nonnucleoside reverse transcriptase inhibitor (NNRTI), or protease inhibitor (PI) and 2 NRTIs (dual NRTIs) also recommended. Preferred dual NRTI option for PEP regimens is emtricitabine and tenofovir DF (may be given as emtricitabine/tenofovir DF; Truvada); alternative dual NRTIs are tenofovir DF and lamivudine, lamivudine and zidovudine (may be given as lamivudine/zidovudine; Combivir), or zidovudine and emtricitabine.

Postexposure Prophylaxis following Nonoccupational Exposure to HIV

Postexposure prophylaxis of HIV infection following nonoccupational exposure [off-label] (nPEP) in individuals exposed to blood, genital secretions, or other potentially infectious body fluids that might contain HIV when the exposure represents a substantial risk for HIV transmission. Used in conjunction with other antiretrovirals.

When nPEP indicated in adults and adolescents ≥13 years of age with normal renal function, CDC states preferred regimen is either raltegravir or dolutegravir used in conjunction with emtricitabine and tenofovir DF (given as emtricitabine/tenofovir DF; Truvada); alternative recommended in these patients is ritonavir-boosted darunavir used in conjunction with emtricitabine/tenofovir DF (Truvada).

Chronic HBV Infection

Treatment of chronic HBV infection in adults and pediatric patients ≥2 years of age weighing ≥10 kg.

Tenofovir DF is a preferred initial treatment option when chronic HBV treatment is indicated; choice of antiviral medication should be individualized based on patient characteristics and comorbidities, treatment tolerability, and cost.

Tenofovir Disoproxil Fumarate Dosage and Administration

General

Pretreatment Screening

Patient Monitoring

Dispensing and Administration Precautions

Administration

Oral Administration

Available as oral tablets or oral powder.

Administer oral tablet once daily without regard to meals.

Administer oral powder once daily. Measure dose using only the scoop provided by the manufacturer. One level scoop delivers 1 g of powder, which contains 40 mg of tenofovir DF. Mix required number of scoops with 2–4 ounces of soft food that can be swallowed without chewing (e.g., applesauce, baby food, yogurt); immediately ingest entire mixture to avoid a bitter taste. Do not administer powder in liquid since powder may float to the top, even after stirring.

Dosage

Available as tenofovir DF; dosage expressed in terms of tenofovir DF.

Pediatric Patients

Treatment of HIV Infection
Oral

In pediatric patients ≥2 years of age weighing ≥35 kg, the recommended dosage is 300 mg once daily.

In pediatric patients ≥2 years of age weighing ≥17 and <35 kg who are able to swallow intact tablets, the recommended dosage is 8 mg/kg (up to a maximum of 300 mg) once daily (see Table 1). Monitor weight periodically and adjust dosage accordingly.

In pediatric patients ≥2 years of age weighing ≥10 kg who are unable to swallow tablets, the recommended dosage is 8 mg/kg (up to a maximum of 300 mg) once daily using the powder (see Table 2). Monitor weight periodically and adjust dosage accordingly.

Table 1. Recommended Dosage of Tenofovir DF (Oral Tablets) in Patients Weighing at Least 17 kg

Weight (kg)

Dosage (as Tablets) Once Daily

17 to <22

150 mg

22 to <28

200 mg

28 to <35

250 mg

≥35

300 mg

Table 2. Recommended Dosage of Tenofovir DF (Oral Powder) in Patients Weighing at least 10 kg1

Weight (kg)

Dosage (as Oral Powder) Once Daily (40 mg of Tenofovir DF per Scoop)

10 to <12

80 mg (2 scoops)

12 to <14

100 mg (2.5 scoops)

14 to <17

120 mg (3 scoops)

17 to <19

140 mg (3.5 scoops)

19 to <22

160 mg (4 scoops)

22 to <24

180 mg (4.5 scoops)

24 to <27

200 mg (5 scoops)

27 to <29

220 mg (5.5 scoops)

29 to <32

240 mg (6 scoops)

32 to <34

260 mg (6.5 scoops)

34 to <35

280 mg (7 scoops)

≥35

300 mg (7.5 scoops)

Preexposure Prophylaxis for Prevention of HIV Infection
Oral

Usual dosage of tenofovir DF for preexposure prophylaxis (PrEP) for prevention of HIV infection (PreP) in adolescents weighing ≥35 kg is 300 mg once daily in conjunction with other antiretrovirals. The fixed-dose combination containing emtricitabine/tenofovir DF (Truvada) is used for PrEP; see the full prescribing information for specific dosage.

Chronic HBV Infection
Oral

In pediatric patients ≥2 years of age weighing ≥35 kg, the recommended dosage is 300 mg once daily. In those ≥2 years of age weighing ≥17 kg but <35 kg who are able to swallow intact tablets, the recommended dosage is 8 mg/kg (up to a maximum of 300 mg) once daily; dosage based on weight (Table 1). Monitor weight periodically and adjust dosage accordingly.

In pediatric patients ≥2 years of age weighing ≥10 kg who are unable to swallow tablets, the recommended dosage of oral powder is 8 mg/kg (up to a maximum of 300 mg) once daily; dosage based on weight (Table 2). Monitor weight periodically and adjust dosage accordingly.

Optimal duration of treatment unknown.

Adults

Treatment of HIV Infection
Oral

300 mg once daily in patients weighing ≥35 kg. Dosage in adults weighing <35 kg is based on weight (see Table 1). Monitor weight periodically and adjust dosage accordingly.

In patients unable to swallow tablets, recommended dosage of oral powder is 8 mg/kg (up to a maximum of 300 mg) once daily with food (see Table 2).

Preexposure Prophylaxis for HIV-1 Infection
Oral

Usual dosage of tenofovir DF for PreP is 300 mg once daily in conjunction with other antiretrovirals. The fixed-dose combination containing emtricitabine/tenofovir DF (Truvada) is used for PrEP; see the full prescribing information for specific dosage.

Postexposure Prophylaxis following Occupational Exposure to HIV† [off-label]
Oral

Usual dosage of tenofovir DF for PEP is 300 mg once daily in conjunction with other antiretrovirals. The preferred dual NRTI backbone option for use in PEP regimens is emtricitabine and tenofovir DF, commonly administered as the fixed-dose combination of emtricitabine/tenofovir DF (Truvada). See the full prescribing information for specific dosage of emtricitabine/tenofovir DF (Truvada).

Postexposure Prophylaxis following Nonoccupational Exposure to HIV† [off-label]
Oral

Usual dosage of tenofovir DF for nPEP is 300 mg once daily in conjunction with other antiretrovirals. The preferred dual NRTI backbone option for use in nPEP regimens is emtricitabine and tenofovir DF, commonly administered as the fixed-dose combination of emtricitabine/tenofovir DF (Truvada). See the full prescribing information for specific dosage of emtricitabine/tenofovir DF (Truvada).

Chronic HBV Infection
Oral

300 mg once daily in patients weighing ≥35 kg. Dosage in patients weighing <35 kg is based on weight (see Table 1).

In patients unable to swallow tablets, recommended dosage of oral powder is 8 mg/kg (up to a maximum of 300 mg) once daily with food (see Table 2).

Special Populations

Hepatic Impairment

No specific dosage recommendations.

Renal Impairment

Reduce dosage in adults with Clcr <50 mL/minute (see Table 3). Dosage adjustments not needed in those with Clcr 50–80 mL/minute; however, monitor Scr, estimated Clcr, serum phosphorus, urine glucose, and urine protein. Dosage recommendations not available for patients with Clcr <10 mL/minute who are not undergoing hemodialysis, or for pediatric patients with renal impairment.

Table 3. Tenofovir DF Dosage Interval Adjustment for Adults with Renal Impairment1

Clcr (mL/minute)

Dosage

30-49

300 mg once every 48 hours

10-29

300 mg once every 72-96 hours

Hemodialysis patients

300 mg once every 7 days or after a total of approximately 12 hours of hemodialysis (assuming 3 hemodialysis sessions/week each lasting approximately 4 hours); give dose after hemodialysis

Geriatric Patients

No specific dosage recommendations. Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.

Cautions for Tenofovir Disoproxil Fumarate

Contraindications

Warnings/Precautions

Warnings

Severe Acute Exacerbation of HBV Infection

Test all patients for presence of chronic HBV before or when initiating tenofovir disoproxil fumarate (tenofovir DF). Severe acute exacerbations of HBV infection may occur following discontinuance of HBV treatment, including tenofovir DF. Closely monitor hepatic function with both clinical and laboratory follow-up for at least several months after tenofovir DF is discontinued. If appropriate, resumption of HBV treatment may be warranted, especially in patients with cirrhosis or advanced liver disease, since posttreatment exacerbation of HBV infection may lead to hepatic decompensation and liver failure. (See Boxed Warning).

Other Warnings/Precautions

New Onset or Worsening Renal Impairment

Renal impairment, including acute renal failure and Fanconi syndrome (renal tubular injury with hypophosphatemia) reported with tenofovir DF.

Assess Scr, estimated Clcr, urine glucose, and urine protein on a clinically appropriate schedule in all patients prior to or when initiating tenofovir DF, and during treatment with the drug. In patients with CKD, also assess serum phosphorus.

In patients with Clcr <50 mL/minute, adjust dosing interval of tenofovir DF and closely monitor renal function. Since no safety or efficacy data are available in patients with renal impairment who received tenofovir DF using dosing guidelines outlined in prescribing information, assess potential benefit of tenofovir DF therapy against potential risk of renal toxicity.

Avoid tenofovir DF in patients who are receiving or recently received nephrotoxic drugs (e.g., high-dose or multiple NSAIAs).

In patients at risk for renal dysfunction, promptly evaluate renal function if manifestations of proximal renal tubulopathy are present (i.e., persistent or worsening bone pain, pain in extremities, fractures, and/or muscular pain or weakness).

Individuals with HBV and HIV Type 1 Coinfection

Test all HIV-infected patients for presence of HBV before initiating tenofovir DF.

Offer HIV-1 testing for all HBV-infected patients before initiating tenofovir DF.

Due to the risk of development of HIV-1 resistance, only use tenofovir DF in patients with HBV and HIV-1 coinfection as part of an appropriate antiretroviral combination regimen.

Lactic Acidosis and Severe Hepatomegaly with Steatosis

Lactic acidosis and severe hepatomegaly with steatosis (sometimes fatal) reported in patients receiving nucleoside analogs, including tenofovir DF, alone or in conjunction with other antiretrovirals.

Suspend tenofovir DF therapy if there are clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity (e.g., hepatomegaly and steatosis even in the absence of marked increases in serum aminotransferase concentrations).

Bone Loss and Mineralization Defects

In patients with HIV-1, tenofovir associated with slightly greater decreases in bone mineral density (BMD) and increases in biochemical markers of bone metabolism, suggesting increased bone turnover compared with other antiretroviral agents.

Increased serum parathyroid hormone and 1,25 vitamin D levels reported in HIV-infected adults receiving tenofovir DF. Similar effects observed in pediatric patients with HIV-1 or HBV infection; however, skeletal growth appeared to be unaffected.

Clinical importance of these changes in BMD and biochemical markers on long-term bone health and fracture risk in adults and pediatric patients unknown.

Consider BMD monitoring in adult and pediatric patients with history of pathologic bone fracture or other risk factors for osteoporosis or bone loss. Effect of calcium and vitamin D supplementation not studied, but may be beneficial. If bone abnormalities suspected, obtain appropriate consultation.

Osteomalacia associated with proximal renal tubulopathy, which may contribute to fractures, reported; arthralgias and muscle pain or weakness also reported in patients with proximal renal tubulopathy. Consider hypophosphatemia and osteomalacia secondary to proximal renal tubulopathy in patients at risk of renal dysfunction who present with persistent or worsening bone or muscle symptoms.

Immune Reconstitution Syndrome

Immune reconstitution syndrome reported in patients with HIV-1 treated with combination antiretroviral therapy, including tenofovir DF. During initial treatment, HIV-infected patients who respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections (e.g., Mycobacterium avium complex [MAC], M. tuberculosis, cytomegalovirus [CMV], Pneumocystis jirovecii [formerly P. carinii]); this may necessitate further evaluation and treatment.

Autoimmune disorders (e.g., Graves' disease, polymyositis, Guillain-Barré syndrome) also reported in the setting of immune reconstitution; time to onset is more variable and can occur many months after initiation of antiretroviral therapy.

Risk of Adverse Reactions Due to Drug Interactions

Concomitant use of tenofovir and certain drugs may result in known or potentially significant drug interactions, some of which may lead to possible clinically important adverse reactions from greater exposures of concomitant drugs. Consult prescribing information for steps to prevent or manage possible and known significant drug interactions.

Consider potential for drug interactions before and during therapy with tenofovir; review concomitant medications during therapy; monitor for adverse reactions associated with concomitant drugs.

Specific Populations

Pregnancy

The Antiretroviral Pregnancy Registry (APR) monitors pregnancy outcomes in women exposed to tenofovir DF during pregnancy. Clinicians are encouraged to register patients in the APR by calling 1-800-258-4263 or visiting [Web].

Based on data from APR, prevalence of birth defects in live births was 2.3% and 2.1% following first and second/third trimester exposure, respectively, to tenofovir DF-containing regimens. Overall risk of birth defects with first-trimester exposure not markedly different compared to background rate for major birth defects in US reference population.

Tenofovir crosses human placenta. In published studies that included HBV-infected pregnant women treated with tenofovir DF, increased risk of adverse pregnancy-related outcomes not observed with use of the drug during third trimester.

No adverse developmental effects observed in animal reproductive studies.

Lactation

Tenofovir distributed into human milk in low concentrations. In a study of breast-feeding women (not infected with HIV) who were on a tenofovir-containing regimen started between 1–24 weeks postpartum, tenofovir was undetectable in the plasma of most infants after 7 days of treatment in mothers. No serious adverse events reported in mothers or infants.

Not known whether tenofovir DF affects human milk production or has effects on the breast-fed infant.

If using tenofovir DF for treatment of HIV-1 infection, instruct HIV-infected women not to breast-feed because of potential for the following: HIV transmission in HIV-negative infants, development of viral resistance in HIV-positive infants, and adverse reactions in the breast-fed infant similar to those observed in adults.

If using tenofovir DF for treatment of HBV infection, consider developmental and health benefits of breast-feeding and the importance of tenofovir DF to the mother along with the potential adverse effects on the breast-fed infant from the drug or underlying maternal condition.

Pediatric Use

Safety and efficacy for treatment of HIV-1 infection established in pediatric patients 2 to <18 years of age. Safety and efficacy not established in children <2 years of age weighing <10 kg.

Safety and efficacy established for treatment of chronic HBV infection in pediatric patients 2 to <18 years of age. Safety and efficacy not established in children <2 years of age weighing <10 kg.

Geriatric Use

Clinical studies did not include sufficient numbers of patients ≥65 years of age to determine whether they respond differently to tenofovir DF than younger adults. Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.

Hepatic Impairment

Pharmacokinetics not substantially altered in patients with moderate or severe hepatic impairment.

Renal Impairment

Principally eliminated by kidneys.

Adjust dosage interval in moderate or severe renal impairment (Clcr<50 mL/minute or end-stage renal disease requiring dialysis).

Common Adverse Effects

Most common adverse effects (incidence ≥10%; grades 2–4) in HIV-infected patients include rash, diarrhea, headache, pain, depression, asthenia, nausea.

Most common adverse effect (all grades) in HBV-infected patients with compensated liver disease was nausea (9%).

Most common adverse effects (incidence ≥10%; all grades) in HBV-infected patients with decompensated liver disease include abdominal pain, nausea, vomiting, pruritus, insomnia, dizziness, pyrexia.

Adverse reactions in pediatric patients were consistent with those observed in adults.

Drug Interactions

Tenofovir DF and tenofovir are not substrates of CYP enzymes; tenofovir does not inhibit CYP3A4, 2D6, 2C9, or 2E1, but may have a slight inhibitory effect on CYP1A.

Substrate of P-glycoprotein (P-gp) transport system.

Substrate of breast cancer resistance protein (BCRP).

The following drug interactions are based on studies using tenofovir DF; refer to the full prescribing information for further details. Additional drug interactions may exist for fixed-combinations containing emtricitabine and tenofovir DF (Truvada); doravirine, lamivudine, and tenofovir DF (Delstrigo); efavirenz, emtricitabine, and tenofovir DF (Atripla); emtricitabine, rilpivirine, and tenofovir DF (Complera); elvitegravir, cobicistat, emtricitabine, and tenofovir DF (Stribild); and efavirenz, lamivudine and tenofovir (Symfi and Symfi Lo).

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

CYP inhibitors or substrates: Pharmacokinetic interactions unlikely.

Drugs Affecting P-glycoprotein Transport System

P-gp inhibitors: Concomitant use may increase absorption of tenofovir DF, resulting in increased plasma concentrations of the drug.

Drugs Affecting Breast Cancer Resistance Protein

BCRP inhibitors: Concomitant use may increase absorption of tenofovir DF, resulting in increased plasma concentrations of the drug.

Nephrotoxic Drugs or Drugs Eliminated by Renal Excretion

Drugs that reduce renal function or compete for active tubular secretion: Potential increased concentrations of tenofovir and/or concomitant drug.

Specific Drugs

Drug

Interaction

Comments

Abacavir

No clinically important effect on abacavir pharmacokinetics

No in vitro evidence of antagonistic antiretroviral effects

Acyclovir, valacyclovir

Possible increased tenofovir and/or acyclovir concentrations and increased risk of adverse effects

Avoid concomitant use

Adefovir dipivoxil

Possible increased tenofovir and/or adefovir concentrations

Do not use concomitantly

Aminoglycosides (gentamicin)

Gentamicin: Possible increased tenofovir and/or aminoglycoside concentrations and increased risk of adverse effects

Avoid concomitant use

Amprenavir

No in vitro evidence of antagonistic antiretroviral effects

Atazanavir

Decreased atazanavir concentrations

Administer atazanavir 300 mg with ritonavir 100 mg

Monitor patients receiving tenofovir DF concomitantly with ritonavir-boosted atazanavir for tenofovir-associated adverse reactions; discontinue tenofovir DF if such adverse events occur

Cidofovir

Possible increased tenofovir and/or cidofovir concentrations and increased risk of adverse effects

Avoid concomitant use

Darunavir

Increased tenofovir concentrations

Monitor patients receiving tenofovir DF concomitantly with ritonavir-boosted darunavir for tenofovir-associated adverse reactions; discontinue tenofovir DF if such adverse events occur

Didanosine

Delayed-release didanosine: Increased didanosine concentrations leading to possible increased risk of didanosine-associated adverse effects (e.g., pancreatitis, neuropathy) and suppression of CD4+ cell counts

Buffered didanosine: No clinically important effect on buffered didanosine pharmacokinetics

No in vitro evidence of antagonistic antiretroviral effects

If tenofovir DF and delayed-release didanosine used concomitantly, use caution and reduce didanosine dosage; closely monitor for didanosine-associated adverse effects and discontinue didanosine if such effects occur

In patients weighing ≥60 kg, reduce didanosine dosage to 250 mg once daily; in those weighing <60 kg, reduce didanosine dosage to 200 mg once daily

May administer didanosine and tenofovir DF at same time without food or with a light meal

Efavirenz

No clinically important interaction

No in vitro evidence of antagonistic antiretroviral effects

Emtricitabine

No clinically important effect on emtricitabine pharmacokinetics

No in vitro evidence of antagonistic antiretroviral effects

Entecavir

No evidence of clinically important pharmacokinetic interaction

No in vitro evidence of antagonistic antiviral effects against HBV

Estrogens/progestins

Hormonal contraceptives: No clinically important pharmacokinetic interaction

Ganciclovir, valganciclovir

Possible increased tenofovir and/or ganciclovir concentrations and increased risk of adverse effects

Avoid concomitant use

Lamivudine

No clinically important effect on lamivudine pharmacokinetics

No in vitro evidence of antagonistic antiretroviral effects

Ledipasvir and sofosbuvir

Fixed combination of ledipasvir and sofosbuvir (ledipasvir/sofosbuvir): Increased tenofovir exposure

Monitor patients receiving tenofovir DF concomitantly with ledipasvir/sofosbuvir without an HIV type 1 (HIV-1) protease inhibitor (PI)/ritonavir or an HIV-1 PI/cobicistat combination, for tenofovir DF-associated adverse effects

In patients receiving tenofovir DF concomitantly with ledipasvir/sofosbuvir and an HIV-1 PI/ritonavir or an HIV-1 PI/cobicistat combination, consider an alternative hepatitis C virus or antiretroviral therapy

If concomitant use necessary, monitor for tenofovir-associated adverse effects

Lopinavir/ritonavir

Increased tenofovir concentrations and AUC; no clinically important effect on lopinavir concentrations and AUC

Monitor for tenofovir toxicity; discontinue tenofovir DF if such effects occur

Methadone

No clinically important pharmacokinetic interactions

Nelfinavir

No effect on pharmacokinetics of either drug

No in vitro evidence of antagonistic antiretroviral effects

Nevirapine

No in vitro evidence of antagonistic antiretroviral effects

NSAIAs

High-dose or multiple NSAIAs: Possible increased concentrations of tenofovir and/or the NSAIAs

Avoid tenofovir DF in patients who are receiving or have recently received a nephrotoxic drug (e.g., high-dose or multiple NSAIAs)

Ribavirin

No clinically important pharmacokinetic interactions

Ritonavir

No in vitro evidence of antagonistic antiretroviral effects

Sofosbuvir

No clinically important effect on tenofovir or sofosbuvir pharmacokinetics

Sofosbuvir and velpatasvir

Fixed combination of sofosbuvir and velpatasvir (sofosbuvir/velpatasvir): Possible increased tenofovir concentrations

Sofosbuvir/velpatasvir: Monitor for tenofovir-associated adverse effects

Sofosbuvir, velpatasvir, and voxilaprevir

Fixed combination of sofosbuvir, velpatasvir, and voxilaprevir (sofosbuvir/velpatasvir/voxilaprevir): Possible increased tenofovir concentrations

Tacrolimus

No evidence of clinically important pharmacokinetic interaction

Tipranavir

Ritonavir-boosted tipranavir: Decreased concentrations and AUC of tenofovir and tipranavir

Zidovudine

No in vitro evidence of antagonistic antiretroviral effects

Tenofovir Disoproxil Fumarate Pharmacokinetics

Absorption

Bioavailability

Pharmacokinetics in healthy individuals similar to those in individuals with HIV-1 infection.

Tenofovir DF is a diester prodrug of tenofovir.

Oral bioavailability of tenofovir from tenofovir DF is approximately 25%; peak plasma concentrations attained in about 1 hour in fasting HIV-infected patients.

In nonfasting individuals, mean peak plasma concentrations were 26% lower when administered as an oral powder compared with administration as tablets; mean AUC was similar with both preparations.

Food

Food delays time to peak plasma tenofovir concentrations by approximately 1 hour. Administration with a high-fat meal increases oral bioavailability of tenofovir (14% increase in peak plasma concentrations; 40% increase in AUC); pharmacokinetics not appreciably affected by administration with a light meal.

Distribution

Extent

Tenofovir distributed into semen and vaginal tissue and cervicovaginal fluid in low concentrations following oral administration. Very low concentrations may be distributed into saliva.

Plasma Protein Binding

In vitro binding to plasma or serum proteins is <0.7 or 7.2%, respectively, over tenofovir concentrations of 0.01–25 mcg/mL.

Elimination

Metabolism

Tenofovir DF requires initial diester hydrolysis for conversion to tenofovir and subsequent phosphorylation by cellular enzymes to form the active tenofovir diphosphate.

Tenofovir and its prodrug are not substrates of CYP enzymes.

Elimination Route

Tenofovir eliminated principally by kidneys using glomerular filtration and active tubular secretion; approximately 32% of an oral dose eliminated in urine within 24 hours.

Tenofovir removed by hemodialysis.

Half-life

Approximately 17 hours.

Special Populations

No substantial changes in tenofovir pharmacokinetics in individuals with moderate to severe hepatic impairment compared with those with normal hepatic function.

Moderate to severe renal impairment (Clcr <50 mL/minute or end-stage renal disease requiring dialysis) results in increased plasma concentrations and AUC.

Stability

Storage

Oral

Powder

25°C (excursions permitted between 15–30°C). Dispense in original container; keep container tightly closed.

Tablets

25°C (excursions permitted between 15–30°C). Dispense in original container; keep container tightly closed.

Actions and Spectrum

Advice to Patients

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Tenofovir Disoproxil Fumarate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Powder

40 mg per g

Viread

Gilead

Tablets, film-coated

150 mg*

Tenofovir Disoproxil Fumarate Tablets

Viread

Gilead

200 mg*

Tenofovir Disoproxil Fumarate Tablets

Viread

Gilead

250 mg*

Tenofovir Disoproxil Fumarate Tablets

Viread

Gilead

300 mg*

Tenofovir Disoproxil Fumarate Tablets

Viread

Gilead

AHFS DI Essentials™. © Copyright 2024, Selected Revisions March 10, 2024. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Off-label: Use is not currently included in the labeling approved by the US Food and Drug Administration.

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