Tenofovir disoproxil fumarate

What is Tenofovir disoproxil fumarate?

• Tenofovir disoproxil fumarate (VIREAD) is a nucleotide analog HIV-1 reverse transcriptase inhibitor and an HBV reverse transcriptase inhibitor used to treat chronic hepatitis B and to prevent and treat HIV/AIDS.

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What are the uses of this medicine?

This medicine is used to:

• treat HIV-1 infection when used with other anti-HIV-1 medicines in adults and children 2 years of age and older who weigh at least 22 pounds (10 kg). HIV is the virus that causes AIDS (Acquired Immune Deficiency Syndrome).
• treat HBV infection in adults and children 2 years of age and older who weigh at least 22 pounds (10 kg). It is not known if VIREAD is safe and effective in children under 2 years of age.

How does this medicine work?

• Tenofovir disoproxil fumarate is an antiviral drug.
• Tenofovir disoproxil fumarate is an acyclic nucleoside phosphonate diester analog of adenosine monophosphate.
• Tenofovir disoproxil fumarate requires initial diester hydrolysis for conversion to tenofovir and subsequent phosphorylations by cellular enzymes to form tenofovir diphosphate (TFV-DP), an obligate chain terminator.
• Tenofovir diphosphate inhibits the activity of HIV-1 reverse transcriptase (RT) and HBV RT by competing with the natural substrate deoxyadenosine 5'-triphosphate and, after incorporation into DNA, by DNA chain termination.
• Tenofovir diphosphate is a weak inhibitor of mammalian DNA polymerases α, β, and mitochondrial DNA polymerase γ.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Tenofovir disoproxil fumarate increases didanosine concentrations. Dose reduction and close monitoring for didanosine toxicity are warranted.
• Coadministration decreases atazanavir concentrations. When coadministered with VIREAD, use atazanavir given with ritonavir.
• Coadministration of VIREAD with certain HIV-1 protease inhibitors or certain drugs to treat HCV increases tenofovir concentrations. Monitor for evidence of tenofovir toxicity.

Is this medicine FDA approved?

• Initial U.S. Approval: 2001

How should this medicine be used?

• Prior to or when initiating VIREAD test for hepatitis B virus infection and HIV-1 infection.
• Prior to initiation and during use of VIREAD, on a clinically appropriate schedule, assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all patients.
• In patients with chronic kidney disease, also assess serum phosphorous.

Recommended dosage:

• Recommended tablet dosage in adults and pediatric patients weighing at least 35 kg: One VIREAD 300 mg tablet once daily taken orally without regard to food.

Recommended dosage in pediatric patients at least 2 years of age and adults:

• Tablets: For patients weighing at least 17 kg who can swallow an intact tablet, one VIREAD tablet (150 mg, 200 mg, 250 mg, or 300 mg based on body weight) once daily taken orally without regard to food.
• Oral powder: For patients weighing at least 10 kg and unable to swallow a tablet, 8 mg per kg VIREAD oral powder (up to a maximum of 300 mg) taken once daily with food.

Recommended dosage in renally impaired adult patients:

• Creatinine clearance (CrCl) 30–49 mL/min: 300 mg every 48 hours.
• CrCl 10–29 mL/min: 300 mg every 72 to 96 hours.
• Hemodialysis: 300 mg every 7 days or after approximately 12 hours of dialysis.

Administration:

• Take VIREAD exactly as your healthcare provider tells you to take it.
• Do not change your dose or stop taking VIREAD without first talking with your healthcare provider. Stay under a healthcare provider's care when taking VIREAD.
• Take VIREAD at the same time every day.
• For adults and children 2 years of age and older who weigh at least 77 pounds (35 kg), the usual dose of VIREAD is one 300 mg tablet each day.
• For children 2 years of age and older who weigh between 37 pounds (17 kg) and 77 pounds (35 kg), your healthcare provider will prescribe the right dose of VIREAD tablets based on your child's body weight.
• Adults and children 2 years of age and older who weigh at least 22 pounds (10 kg) and who are unable to swallow VIREAD tablets whole, may take VIREAD powder. Your healthcare provider will prescribe the right dose of VIREAD powder based on your or your child's body weight.
• Tell your healthcare provider if you or your child has problems with swallowing tablets.
• If your healthcare provider prescribes VIREAD powder for you or your child, see the "INSTRUCTIONS FOR USE" that comes with your VIREAD powder for information about the right way to measure and take VIREAD powder.
• Take VIREAD tablets by mouth, with or without food.
• Do not miss a dose of VIREAD. Missing a dose lowers the amount of medicine in your blood. Refill your VIREAD prescription before you run out of medicine.
• If you take too much VIREAD, call your local poison control center or go right away to the nearest hospital emergency room.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 150 mg, 200 mg, 250 mg, and 300 mg of tenofovir disoproxil fumarate.
• Oral Powder: 40 mg per 1 g of oral powder of tenofovir disoproxil fumarate.

This medicine is available in fallowing brand namesː

• VIREAD

What side effects can this medication cause?

The most common side effects in all people taking VIREAD are:

• nausea
• rash
• diarrhea
• headache
• pain
• depression
• weakness

In some people with advanced HBV-infection, other common side effects may include:

• fever
• itching
• vomiting
• stomach-area pain
• dizziness
• sleeping problems

VIREAD may cause serious side effects, including:

• Worsening of Hepatitis B virus infection (HBV)
• New or worse kidney problems, including kidney failure
• Changes in your immune system (Immune Reconstitution Syndrome)
• Bone problems
• Too much lactic acid in your blood (lactic acidosis)
• Severe liver problems

What special precautions should I follow?

• Tenofovir is principally eliminated by the kidney. Renal impairment, including cases of acute renal failure and Fanconi syndrome (renal tubular injury with severe hypophosphatemia), has been reported with the use of VIREAD. Avoid administering VIREAD with concurrent or recent use of nephrotoxic drugs.
• HIV antibody testing should be offered to all HBV-infected patients before initiating therapy with VIREAD. VIREAD should only be used as part of an appropriate antiretroviral combination regimen in HIV-infected patients with or without HBV coinfection.
• Immune reconstitution syndrome has been reported in HIV-1 infected patients treated with combination antiretroviral therapy, including VIREAD. May necessitate further evaluation and treatment.
• Decreases in bone mineral density (BMD) may occour. Consider assessment of BMD in patients with a history of pathologic fracture or other risk factors for osteoporosis or bone loss.
• Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogs, including TDF, alone or in combination with other antiretrovirals. Discontinue treatment in patients who develop symptoms or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity.

What to do in case of emergency/overdose?

• If overdose occurs, the patient must be monitored for evidence of toxicity, and standard supportive treatment applied as necessary.
• Tenofovir is efficiently removed by hemodialysis. A four-hour hemodialysis session removed approximately 10% of the administered tenofovir dose.

Can this medicine be used in pregnancy?

• There is a pregnancy registry for women who take VIREAD during pregnancy.
• The purpose of this registry is to collect information about the health of you and your baby. Talk to your healthcare provider about how you can take part in this registry.
• Published studies in HBV-infected subjects do not report an increased risk of adverse pregnancy-related outcomes with the use of VIREAD during the third trimester of pregnancy.

Can this medicine be used in children?

• Safety and effectiveness of VIREAD in pediatric patients younger than 2 years of age and weighing less than 10 kg with HIV-1 infection have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient: tenofovir disoproxil fumarate

Inactive ingredients:

• VIREAD tablets: croscarmellose sodium, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and pregelatinized starch.
• VIREAD powder: mannitol, hydroxypropyl cellulose, ethylcellulose, and silicon dioxide.

Tablet coating:

• VIREAD tablets 300 mg: Opadry II Y-30-10671-A, which contains FD&C blue #2 aluminum lake, hypromellose 2910, lactose monohydrate, titanium dioxide, and triacetin.
• VIREAD tablets 150, 200, and 250 mg: Opadry II 32K-18425, which contains hypromellose 2910, lactose monohydrate, titanium dioxide, and triacetin.

Who manufactures and distributes this medicine?

• Manufactured for and distributed by: Gilead Sciences, Inc. Foster City, CA

VIREAD is a trademark of Gilead Sciences, Inc.

What should I know about storage and disposal of this medication?

• Store VIREAD tablets or powder at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep VIREAD in the original container.
• Keep the bottle tightly closed.
• Do not use VIREAD if the seal over the bottle opening is broken or missing.
• Keep VIREAD and all medicines out of the reach of children.

• Dailymed label info on Tenofovir disoproxil fumarate
• FDA Tenofovir disoproxil fumarate

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