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Drug overview for TENOFOVIR DISOPROXIL FUMARATE (tenofovir disoproxil fumarate):
Generic name: tenofovir disoproxil fumarate (ten-OF-oh-vir)
Drug class: Antiviral-HIV(Antiretroviral) Nucleoside/-tide RT Inhibitors
Therapeutic class: Anti-Infective Agents
Tenofovir disoproxil fumarate (tenofovir DF), an antiretroviral agent, is a human immunodeficiency virus (HIV) nucleotide reverse transcriptase inhibitor that is active against HIV and hepatitis B virus (HBV).
No enhanced Uses information available for this drug.
Generic name: tenofovir disoproxil fumarate (ten-OF-oh-vir)
Drug class: Antiviral-HIV(Antiretroviral) Nucleoside/-tide RT Inhibitors
Therapeutic class: Anti-Infective Agents
Tenofovir disoproxil fumarate (tenofovir DF), an antiretroviral agent, is a human immunodeficiency virus (HIV) nucleotide reverse transcriptase inhibitor that is active against HIV and hepatitis B virus (HBV).
No enhanced Uses information available for this drug.
DRUG IMAGES
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The following indications for TENOFOVIR DISOPROXIL FUMARATE (tenofovir disoproxil fumarate) have been approved by the FDA:
Indications:
Chronic hepatitis B
HIV infection
Professional Synonyms:
Chronic hepatitis B virus infection
Chronic hepatitis due to HBV
Human immunodeficiency virus disease
Human immunodeficiency virus infection
Indications:
Chronic hepatitis B
HIV infection
Professional Synonyms:
Chronic hepatitis B virus infection
Chronic hepatitis due to HBV
Human immunodeficiency virus disease
Human immunodeficiency virus infection
The following dosing information is available for TENOFOVIR DISOPROXIL FUMARATE (tenofovir disoproxil fumarate):
Although tenofovir DF is a prodrug that requires metabolism for activation, dosage of the drug is expressed in terms of the prodrug diester (i.e., tenofovir DF).
Dosage of tenofovir DF oral powder containing 40 mg/g is expressed as the number of scoops of powder.
Dosage of tenofovir DF oral powder containing 40 mg/g is expressed as the number of scoops of powder.
Single-entity tenofovir DF is commercially available as tablets or oral powder. Tenofovir DF tablet is administered orally once daily without regard to meals. Tenofovir DF oral powder is administered once daily.
Measure the appropriate dosage of the oral powder using only the scoop provided by the manufacturer. One level scoop delivers 1 g of powder, which contains 40 mg of tenofovir DF. Mix the required number of scoops of the powder with 2-4 ounces of soft food that can be swallowed without chewing (e.g., applesauce, baby food, yogurt), and ingest the entire mixture immediately to avoid a bitter taste.
Do not administer the oral powder in a liquid since the powder may float to the top of the liquid, even after stirring. Store tenofovir DF oral power and tablets at 25oC (excursions permitted to 15-30oC). Dispense in the original container, and keep the container tightly closed.
Measure the appropriate dosage of the oral powder using only the scoop provided by the manufacturer. One level scoop delivers 1 g of powder, which contains 40 mg of tenofovir DF. Mix the required number of scoops of the powder with 2-4 ounces of soft food that can be swallowed without chewing (e.g., applesauce, baby food, yogurt), and ingest the entire mixture immediately to avoid a bitter taste.
Do not administer the oral powder in a liquid since the powder may float to the top of the liquid, even after stirring. Store tenofovir DF oral power and tablets at 25oC (excursions permitted to 15-30oC). Dispense in the original container, and keep the container tightly closed.
No dosing information available.
No generic dosing information available.
The following drug interaction information is available for TENOFOVIR DISOPROXIL FUMARATE (tenofovir disoproxil fumarate):
There are 0 contraindications.
There are 0 severe interactions.
There are 0 moderate interactions.
The following contraindication information is available for TENOFOVIR DISOPROXIL FUMARATE (tenofovir disoproxil fumarate):
Drug contraindication overview.
*None.
*None.
There are 1 contraindications.
Absolute contraindication.
| Contraindication List |
|---|
| Lactic acidosis |
There are 8 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Acute renal failure |
| Chronic kidney disease stage 3B (moderate) GFR 30-44 ml/min |
| Chronic kidney disease stage 4 (severe) GFR 15-29 ml/min |
| Chronic kidney disease stage 5 (failure) GFr<15 ml/min |
| Fanconi syndrome |
| Hypophosphatemia |
| Osteomalacia |
| Pathological fracture |
There are 2 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Chronic kidney disease stage 3A (moderate) GFR 45-59 ml/min |
| Osteopenia |
The following adverse reaction information is available for TENOFOVIR DISOPROXIL FUMARATE (tenofovir disoproxil fumarate):
Adverse reaction overview.
The most common adverse effects (incidence >=10%; grades 2-4) in HIV-infected patients receiving tenofovir DF are rash, diarrhea, headache, pain, depression, asthenia, and nausea. The most common adverse effect (all grades) in HBV-infected patients with compensated liver disease was nausea (9%). The most common adverse effects (incidence >=10%; all grades) in HBV-infected patients with decompensated liver disease were abdominal pain, nausea, vomiting, pruritus, insomnia, dizziness, and pyrexia. Adverse reactions in pediatric patients were consistent with those observed in adults.
The most common adverse effects (incidence >=10%; grades 2-4) in HIV-infected patients receiving tenofovir DF are rash, diarrhea, headache, pain, depression, asthenia, and nausea. The most common adverse effect (all grades) in HBV-infected patients with compensated liver disease was nausea (9%). The most common adverse effects (incidence >=10%; all grades) in HBV-infected patients with decompensated liver disease were abdominal pain, nausea, vomiting, pruritus, insomnia, dizziness, and pyrexia. Adverse reactions in pediatric patients were consistent with those observed in adults.
There are 27 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Depression |
Hypercholesterolemia Increased alanine transaminase Increased aspartate transaminase Osteopenia Pneumonia |
| Rare/Very Rare |
|---|
|
Abnormal hepatic function tests Acute renal failure Angioedema Dyspnea Fanconi syndrome Graves' disease Guillain-barre syndrome Hepatitis Hypokalemia Hypophosphatemia Interstitial nephritis Kidney disease with reduction in glomerular filtration rate (GFr) Lactic acidosis Nephrogenic diabetes insipidus Osteomalacia Pancreatitis Peripheral neuropathy Polymyositis Renal tubular necrosis Rhabdomyolysis Steatosis of liver |
There are 33 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Acute abdominal pain Back pain Cough Diarrhea Dizziness Dyspepsia Fatigue Fever General weakness Headache disorder Insomnia Nausea Pain Pruritus of skin |
Anorexia Arthralgia Chest pain Elevated serum amylase Elevated serum lipase Flatulence Myalgia Pharyngitis Polyuria Proteinuria Sinusitis Skin rash Vomiting Weight loss |
| Rare/Very Rare |
|---|
|
Hyperhidrosis Hypertriglyceridemia Muscle weakness Myopathy Urticaria |
The following precautions are available for TENOFOVIR DISOPROXIL FUMARATE (tenofovir disoproxil fumarate):
Safety and efficacy of tenofovir DF for treatment of HIV-1 infection in pediatric patients 2 to <18 years of age are supported by data from 2 randomized controlled trials. Peak plasma concentrations and AUC of tenofovir in HIV-1-infected pediatric patients 2 to <18 years of age receiving 8 mg/kg of tenofovir DF (up to 300 mg) once daily as oral powder or receiving 300 mg once daily as tablets were similar to peak plasma concentrations and AUC reported in adults receiving 300 mg once daily. Safety and efficacy of tenofovir DF for treatment of HIV-1 infection have not been established in children <2 years of age weighing <10 kg.
In HBV-infected pediatric patients 12 to <18 years of age receiving tenofovir DF 300 mg once daily as tablets, and pediatric patients 2 to <12 years of age receiving 8 mg/kg of tenofovir DF (up to 300 mg) once daily as tablets or oral powder, tenofovir exposures were similar to those reported in HIV-1-infected adults receiving identical doses. Safety and efficacy of tenofovir DF for treatment of chronic HBV infection have not been established in children <2 years of age weighing <10 kg.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
In HBV-infected pediatric patients 12 to <18 years of age receiving tenofovir DF 300 mg once daily as tablets, and pediatric patients 2 to <12 years of age receiving 8 mg/kg of tenofovir DF (up to 300 mg) once daily as tablets or oral powder, tenofovir exposures were similar to those reported in HIV-1-infected adults receiving identical doses. Safety and efficacy of tenofovir DF for treatment of chronic HBV infection have not been established in children <2 years of age weighing <10 kg.
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
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 https://www.apregistry.com/.
Based on prospective data from the APR, the 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.
The overall risk of birth defects with first-trimester exposure for tenofovir DF was not markedly different compared to the background rate for major birth defects of 2.7% in the United States reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP). Limitations of using an external comparator (the MACDP) include differences in populations and methodology, and confounding due to the underlying disease.
The rate of miscarriage is not reported in the APR. Tenofovir crosses the human placenta. In published studies that included HBV-infected pregnant women treated with tenofovir DF, an increased risk of adverse pregnancy-related outcomes was not observed with use of tenofovir DF during the third trimester.
Two stillbirths were identified, and there was 1 major birth defect (talipes) and 1 occurrence of multiple congenital abnormalities (not further specified) in infants exposed to tenofovir DF. No clinically relevant drug-related safety findings were found in infants exposed to tenofovir DF during late gestation. Animal reproduction studies did not find any adverse developmental effects when tenofovir DF was administered at doses >=14 (tenofovir DF) and exposures 2.7 (tenofovir) times the recommended daily dose of tenofovir DF in humans.
Based on prospective data from the APR, the 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.
The overall risk of birth defects with first-trimester exposure for tenofovir DF was not markedly different compared to the background rate for major birth defects of 2.7% in the United States reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP). Limitations of using an external comparator (the MACDP) include differences in populations and methodology, and confounding due to the underlying disease.
The rate of miscarriage is not reported in the APR. Tenofovir crosses the human placenta. In published studies that included HBV-infected pregnant women treated with tenofovir DF, an increased risk of adverse pregnancy-related outcomes was not observed with use of tenofovir DF during the third trimester.
Two stillbirths were identified, and there was 1 major birth defect (talipes) and 1 occurrence of multiple congenital abnormalities (not further specified) in infants exposed to tenofovir DF. No clinically relevant drug-related safety findings were found in infants exposed to tenofovir DF during late gestation. Animal reproduction studies did not find any adverse developmental effects when tenofovir DF was administered at doses >=14 (tenofovir DF) and exposures 2.7 (tenofovir) times the recommended daily dose of tenofovir DF in humans.
Tenofovir is 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 were reported in mothers or infants.
It is not known whether tenofovir DF affects human milk production or has effects on the breast-fed infant. The HHS perinatal HIV transmission guideline provides updated recommendations on infant feeding. The guideline states that patients with HIV should receive evidence-based, patient-centered counseling to support shared decision making about infant feeding.
During counseling, patients should be informed that feeding with appropriate formula or pasteurized donor human milk from a milk bank eliminates the risk of postnatal HIV transmission to the infant. Additionally, achieving and maintaining viral suppression with antiretroviral therapy during pregnancy and postpartum reduces the risk of breastfeeding HIV transmission to <1%, but does not completely eliminate the risk. Replacement feeding with formula or banked pasteurized donor milk is recommended when patients with HIV are not on antiretroviral therapy and/or do not have a suppressed viral load during pregnancy (at a minimum throughout the third trimester), as well as at delivery. If using tenofovir DF for the treatment of HBV infection, consider the 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 from the underlying maternal condition.
Precaution Exists
Precaution exists. (No data or inconclusive human data.) Use of this drug by breast feeding mothers should be evaluated carefully.
It is not known whether tenofovir DF affects human milk production or has effects on the breast-fed infant. The HHS perinatal HIV transmission guideline provides updated recommendations on infant feeding. The guideline states that patients with HIV should receive evidence-based, patient-centered counseling to support shared decision making about infant feeding.
During counseling, patients should be informed that feeding with appropriate formula or pasteurized donor human milk from a milk bank eliminates the risk of postnatal HIV transmission to the infant. Additionally, achieving and maintaining viral suppression with antiretroviral therapy during pregnancy and postpartum reduces the risk of breastfeeding HIV transmission to <1%, but does not completely eliminate the risk. Replacement feeding with formula or banked pasteurized donor milk is recommended when patients with HIV are not on antiretroviral therapy and/or do not have a suppressed viral load during pregnancy (at a minimum throughout the third trimester), as well as at delivery. If using tenofovir DF for the treatment of HBV infection, consider the 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 from the underlying maternal condition.
Precaution Exists
Precaution exists. (No data or inconclusive human data.) Use of this drug by breast feeding mothers should be evaluated carefully.
| Drug Name | Excretion Potential | Effect on Infant | Notes |
|---|---|---|---|
| Tenofovir | Excreted.This drug is known to be excreted in human breast milk. | It is not known whether this drug has an adverse effect on the nursing infant. (No data or inconclusive human data) | No known infant adv effects; breastfeeding not rec in hiv positive women |
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 in geriatric patients with caution because of the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease or drug therapy. Pharmacokinetic studies have not been conducted in patients >=65 years of age.
Precaution Exists
Geriatric management or monitoring precaution exists.
Precaution Exists
Geriatric management or monitoring precaution exists.
| Drug Name | Narrative | REN | HEP | CARDIO | NEURO | PULM | ENDO |
|---|---|---|---|---|---|---|---|
| Tenofovir Disoproxil | Renal-Adjust dosing interval for CrCL<50mL/min. Fixed dose combinations containing tenofovir are not appropriate if dose adjustment is required. Musculoskeletal-Decreases in bone mineral density have been observed. Consider calcium and vitamin D3 supplementation. | Y | Y | Y | N | N | N |
The following prioritized warning is available for TENOFOVIR DISOPROXIL FUMARATE (tenofovir disoproxil fumarate):
WARNING: If you have hepatitis B infection, your hepatitis symptoms may get worse or become very serious if you stop taking tenofovir. Talk with your doctor before stopping this medication. Your doctor will monitor liver tests for several months after you stop tenofovir. Tell your doctor right away if you develop symptoms of worsening liver problems.
WARNING: If you have hepatitis B infection, your hepatitis symptoms may get worse or become very serious if you stop taking tenofovir. Talk with your doctor before stopping this medication. Your doctor will monitor liver tests for several months after you stop tenofovir. Tell your doctor right away if you develop symptoms of worsening liver problems.
The following icd codes are available for TENOFOVIR DISOPROXIL FUMARATE (tenofovir disoproxil fumarate)'s list of indications:
| Chronic hepatitis B | |
| B18.0 | Chronic viral hepatitis B with delta-agent |
| B18.1 | Chronic viral hepatitis B without delta-agent |
| HIV infection | |
| B20 | Human immunodeficiency virus [HIv] disease |
| B97.35 | Human immunodeficiency virus, type 2 [HIV 2] as the cause of diseases classified elsewhere |
| O98.7 | Human immunodeficiency virus [HIv] disease complicating pregnancy, childbirth and the puerperium |
| O98.71 | Human immunodeficiency virus [HIv] disease complicating pregnancy |
| O98.711 | Human immunodeficiency virus [HIv] disease complicating pregnancy, first trimester |
| O98.712 | Human immunodeficiency virus [HIv] disease complicating pregnancy, second trimester |
| O98.713 | Human immunodeficiency virus [HIv] disease complicating pregnancy, third trimester |
| O98.719 | Human immunodeficiency virus [HIv] disease complicating pregnancy, unspecified trimester |
| O98.72 | Human immunodeficiency virus [HIv] disease complicating childbirth |
| O98.73 | Human immunodeficiency virus [HIv] disease complicating the puerperium |
| Z21 | Asymptomatic human immunodeficiency virus [HIv] infection status |
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