Emtricitabine And Tenofovir Disoproxil Fumarate

What is Emtricitabine And Tenofovir Disoproxil Fumarate?

11 DESCRIPTION Emtricitabine and tenofovir disoproxil fumarate tablets are fixed-dose combination tablets containing emtricitabine (FTC) and tenofovir disoproxil fumarate (TDF). FTC is a synthetic nucleoside analog of cytidine. TDF is converted in vivo to tenofovir, an acyclic nucleoside phosphonate (nucleotide) analog of adenosine 5′-monophosphate. Both FTC and tenofovir exhibit inhibitory activity against HIV-1 reverse transcriptase. Emtricitabine: The chemical name of FTC is 5-fluoro-1-(2 R ,5 S )-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl] cytosine. FTC is the (-) enantiomer of a thio analog of cytidine, which differs from other cytidine analogs in that it has a fluorine in the 5-position. It has a molecular formula of C 8 H 10 FN 3 O 3 S and a molecular weight of 247.24. It has the following structural formula: FTC is a white to off-white crystalline powder with a solubility of approximately 112 mg/mL in water at 25°C. The partition coefficient (log p) for emtricitabine is -0.43 and the pKa is 2.65. Tenofovir Disoproxil Fumarate: TDF is a fumaric acid salt of the bis-isopropoxycarbonyloxymethyl ester derivative of tenofovir. The chemical name of tenofovir DF is 9-[( R )-2 [[bis[[(

Uses of Emtricitabine And Tenofovir Disoproxil Fumarate

Established uses

1 INDICATIONS AND USAGE HIV-1 Treatment ( 1.1 ) Emtricitabine and tenofovir disoproxil fumarate tablet is a two-drug combination of emtricitabine (FTC) and tenofovir disoproxil fumarate (TDF), both HIV-1 nucleoside analog reverse transcriptase inhibitors, and is indicated: • in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 17 kg.
HIV-1 PrEP ( 1.2 ): • Emtricitabine and tenofovir disoproxil fumarate tablet is indicated in at-risk adults and adolescents weighing at least 35 kg for pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection.
Individuals must have a negative HIV-1 test immediately prior to initiating emtricitabine and tenofovir disoproxil fumarate tablet for HIV-1 PrEP.
1.1 Treatment of HIV-1 Infection Emtricitabine and tenofovir disoproxil fumarate tablet is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 17 kg [see Clinical Studies ( 14 )] .
1.2 HIV-1 Pre-Exposure Prophylaxis (PrEP) Emtricitabine and tenofovir disoproxil fumarate tablet is indicated in at-ri

How Emtricitabine And Tenofovir Disoproxil Fumarate works

In more detail: 12.1 Mechanism of Action Emtricitabine and tenofovir disoproxil fumarate is a fixed-dose combination of antiviral drugs FTC and TDF [see Microbiology ( 12.4 )] .

How to take Emtricitabine And Tenofovir Disoproxil Fumarate

2 DOSAGE AND ADMINISTRATION • Testing: Prior to or when initiating emtricitabine and tenofovir disoproxil fumarate tablets test for hepatitis B virus infection. Prior to initiation and during use of emtricitabine and tenofovir disoproxil fumarate tablets, on a clinically appropriate schedule, assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all individuals. In individuals with chronic kidney disease, also assess serum phosphorus. ( 2.1 ) • HIV-1 Screening: Screen all individuals for HIV-1 infection immediately prior to initiating emtricitabine and tenofovir disoproxil fumarate tablets for HIV-1 PrEP and at least once every 3 months while taking emtricitabine and tenofovir disoproxil fumarate tablets, and upon diagnosis of any other sexually transmitted infections (STIs). ( 2.2 ) Treatment of HIV-1 Infection • Recommended dosage in adults and pediatric patients weighing at least 35 kg: One emtricitabine and tenofovir disoproxil fumarate tablet (containing 200 mg of FTC and 300 mg of TDF) once daily taken orally with or without food. ( 2.3 ) • Recommended dosage in pediatric patients weighing at least 17 kg: One emtricitabine and tenofovir

Dosage

Follow the dose prescribed by your doctor or pharmacist. The ranges below are general information, not a personal prescription.

Adults: 2 DOSAGE AND ADMINISTRATION • Testing: Prior to or when initiating emtricitabine and tenofovir disoproxil fumarate tablets test for hepatitis B virus infection. Prior to initiation and during use of emtricitabine and tenofovir disoproxil fumarate tablets, on a clinically appropriate schedule, assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all individuals. In individuals with chronic kidney disease, also assess serum phosphorus. ( 2.1 ) • HIV-1 Screening: Screen all individuals for HIV-1 infection immediately prior to initiating emtricitabine and tenofovir disoproxil fumarate tablets for HIV-1 PrEP and at least once every 3 months while taking emtricitabine and tenofovir disoproxil fumarate tablets, and upon diagnosis of any other sexually transmitted infections (STIs). ( 2.2 ) Treatment of HIV-1 Infection • Recommended dosage in adults and pediatric patients weighing at least 35 kg: One emtricitabine and tenofovir disoproxil fumarate tablet (containing 200 mg of FTC and 300 mg of TDF) once daily taken orally with or without food. ( 2.3 ) • Recommended dosage in pediatric patients weighing at least 17 kg: One emtricitabine and tenofovir

Side effects of Emtricitabine And Tenofovir Disoproxil Fumarate

Common

6 ADVERSE REACTIONS The following adverse reactions are discussed in other sections of the labeling: • Severe Acute Exacerbations of Hepatitis B in Patients with HBV Infection [see Warnings and Precautions ( 5.1 )] .
New Onset or Worsening Renal Impairment [see Warnings and Precautions ( 5.3 )] .
Immune Reconstitution Syndrome [see Warnings and Precautions ( 5.4 )] .
Bone Loss and Mineralization Defects [see Warnings and Precautions ( 5.5 )].
Lactic Acidosis/Severe Hepatomegaly with Steatosis [see Warnings and Precautions ( 5.6 )] .
In HIV-1 infected patients, the most common adverse reactions (incidence greater than or equal to 10%) are diarrhea, nausea, fatigue, headache, dizziness, depression, insomnia, abnormal dreams, and rash.

Warnings and who should not take it

Who should NOT take Emtricitabine And Tenofovir Disoproxil Fumarate?

4 CONTRAINDICATIONS Emtricitabine and tenofovir disoproxil fumarate tablets for HIV-1 PrEP are contraindicated in individuals with unknown or positive HIV-1 status [see Warnings and Precautions ( 5.2 )] .
Emtricitabine and tenofovir disoproxil fumarate tablets for HIV-1 PrEP are contraindicated in individuals with unknown or positive HIV-1 status.
( 4 )

Overdose

10 OVERDOSAGE If overdose occurs, the patient must be monitored for evidence of toxicity, and standard supportive treatment applied as necessary. Emtricitabine: Hemodialysis treatment removes approximately 30% of the FTC dose over a 3-hour dialysis period starting within 1.5 hours of FTC dosing (blood flow rate of 400 mL/min and a dialysate flow rate of 600 mL/min). It is not known whether FTC can be removed by peritoneal dialysis. Tenofovir Disoproxil Fumarate: Tenofovir is efficiently removed by hemodialysis with an extraction coefficient of approximately 54%. Following a single 300 mg dose of TDF, a four-hour hemodialysis session removed approximately 10% of the administered tenofovir dose.

Safety at a glance

PregnancyCaution

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to emtricitabine and tenofovir disoproxil fumarate during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Data on the use of emtricitabine and tenofovir disoproxil fumarate during pregnancy from observational studies have shown no increased risk of major birth defects. Available data from the APR show no significant difference in the overall risk of major birth defects with first trimester exposure for emtricitabine (FTC) (2.3%) or tenofovir disoproxil fumarate (TDF) (2.1%) compared with the background rate for major birth defects of 2.7% in a U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP) (see Data) . The rate of miscarriage for individual drugs is not reported in the APR. In the U.S. general population, the estimated background risk of miscarriage in clinically recognized pregnancies is 15 to 20%. In animal reproduction studies, no adverse developmental effects were observed when the components of emtrici

Children and elderly

Children

8.4 Pediatric Use Treatment of HIV-1 Infection No pediatric clinical trial was conducted to evaluate the safety and efficacy of emtricitabine and tenofovir disoproxil fumarate tablets in patients with HIV-1 infection. Data from previously conducted trials with the individual drug products, FTC and TDF, were relied upon to support dosage recommendations for emtricitabine and tenofovir disoproxil fumarate. For additional information, consult the prescribing information for EMTRIVA and VIREAD. Emtricitabine and tenofovir disoproxil fumarate should only be administered to HIV-1 infected pediatric patients with body weight greater than or equal to 17 kg and who are able to swallow a tablet. Because it is a fixed-dose combination tablet, emtricitabine and tenofovir disoproxil fumarate cannot be adjusted for patients of lower weight [see Warnings and Precautions ( 5.5 ), Adverse Reactions ( 6.1 ) and Clinical Pharmacology ( 12.3 )] . Emtricitabine and tenofovir disoproxil fumarate is not approved for use in pediatric patients weighing less than 17 kg. HIV-1 PrEP The safety and effectiveness of emtricitabine and tenofovir disoproxil fumarate for HIV-1 PrEP in at-risk adolescents weighing a

Elderly

8.5 Geriatric Use Clinical trials of FTC, TDF, or emtricitabine and tenofovir disoproxil fumarate did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.

Interactions

Medicine and medicine

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

Frequently asked questions

What is Emtricitabine And Tenofovir Disoproxil Fumarate used for?

1 INDICATIONS AND USAGE HIV-1 Treatment ( 1.1 ) Emtricitabine and tenofovir disoproxil fumarate tablet is a two-drug combination of emtricitabine (FTC) and tenofovir disoproxil fumarate (TDF), both HIV-1 nucleoside analog reverse transcriptase inhibitors, and is indicated: • in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 17 kg., HIV-1 PrEP ( 1.2 ): • Emtricitabine and tenofovir disoproxil fumarate tablet is indicated in at-risk adults and adolescents weighing at least 35 kg for pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection., Individuals must have a negative HIV-1 test immediately prior to initiating emtricitabine and tenofovir disoproxil fumarate tablet for HIV-1 PrEP., 1.1 Treatment of HIV-1 Infection Emtricitabine and tenofovir disoproxil fumarate tablet is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients weighing at least 17 kg [see Clinical Studies ( 14 )] ., 1.2 HIV-1 Pre-Exposure Prophylaxis (PrEP) Emtricitabine and tenofovir disoproxil fumarate tablet is indicated in at-ri.

How should I take Emtricitabine And Tenofovir Disoproxil Fumarate?

2 DOSAGE AND ADMINISTRATION • Testing: Prior to or when initiating emtricitabine and tenofovir disoproxil fumarate tablets test for hepatitis B virus infection. Prior to initiation and during use of emtricitabine and tenofovir disoproxil fumarate tablets, on a clinically appropriate schedule, assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all individuals. In individuals with chronic kidney disease, also assess serum phosphorus. ( 2.1 ) • HIV-1 Screening: Screen all individuals for HIV-1 infection immediately prior to initiating emtricitabine and tenofovir disoproxil fumarate tablets for HIV-1 PrEP and at least once every 3 months while taking emtricitabine and tenofovir disoproxil fumarate tablets, and upon diagnosis of any other sexually transmitted infections (STIs). ( 2.2 ) Treatment of HIV-1 Infection • Recommended dosage in adults and pediatric patients weighing at least 35 kg: One emtricitabine and tenofovir disoproxil fumarate tablet (containing 200 mg of FTC and 300 mg of TDF) once daily taken orally with or without food. ( 2.3 ) • Recommended dosage in pediatric patients weighing at least 17 kg: One emtricitabine and tenofovir

What are the common side effects?

6 ADVERSE REACTIONS The following adverse reactions are discussed in other sections of the labeling: • Severe Acute Exacerbations of Hepatitis B in Patients with HBV Infection [see Warnings and Precautions ( 5.1 )] ., New Onset or Worsening Renal Impairment [see Warnings and Precautions ( 5.3 )] ., Immune Reconstitution Syndrome [see Warnings and Precautions ( 5.4 )] ., Bone Loss and Mineralization Defects [see Warnings and Precautions ( 5.5 )]., Lactic Acidosis/Severe Hepatomegaly with Steatosis [see Warnings and Precautions ( 5.6 )] ., In HIV-1 infected patients, the most common adverse reactions (incidence greater than or equal to 10%) are diarrhea, nausea, fatigue, headache, dizziness, depression, insomnia, abnormal dreams, and rash..

Who should not take Emtricitabine And Tenofovir Disoproxil Fumarate?

4 CONTRAINDICATIONS Emtricitabine and tenofovir disoproxil fumarate tablets for HIV-1 PrEP are contraindicated in individuals with unknown or positive HIV-1 status [see Warnings and Precautions ( 5.2 )] .; Emtricitabine and tenofovir disoproxil fumarate tablets for HIV-1 PrEP are contraindicated in individuals with unknown or positive HIV-1 status.; ( 4 ).

Can I take Emtricitabine And Tenofovir Disoproxil Fumarate during pregnancy?

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to emtricitabine and tenofovir disoproxil fumarate during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Data on the use of emtricitabine and tenofovir disoproxil fumarate during pregnancy from observational studies have shown no increased risk of major birth defects. Available data from the APR show no significant difference in the overall risk of major birth defects with first trimester exposure for emtricitabine (FTC) (2.3%) or tenofovir disoproxil fumarate (TDF) (2.1%) compared with the background rate for major birth defects of 2.7% in a U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP) (see Data) . The rate of miscarriage for individual drugs is not reported in the APR. In the U.S. general population, the estimated background risk of miscarriage in clinically recognized pregnancies is 15 to 20%. In animal reproduction studies, no adverse developmental effects were observed when the components of emtrici

Can children take Emtricitabine And Tenofovir Disoproxil Fumarate?

8.4 Pediatric Use Treatment of HIV-1 Infection No pediatric clinical trial was conducted to evaluate the safety and efficacy of emtricitabine and tenofovir disoproxil fumarate tablets in patients with HIV-1 infection. Data from previously conducted trials with the individual drug products, FTC and TDF, were relied upon to support dosage recommendations for emtricitabine and tenofovir disoproxil fumarate. For additional information, consult the prescribing information for EMTRIVA and VIREAD. Emtricitabine and tenofovir disoproxil fumarate should only be administered to HIV-1 infected pediatric patients with body weight greater than or equal to 17 kg and who are able to swallow a tablet. Because it is a fixed-dose combination tablet, emtricitabine and tenofovir disoproxil fumarate cannot be adjusted for patients of lower weight [see Warnings and Precautions ( 5.5 ), Adverse Reactions ( 6.1 ) and Clinical Pharmacology ( 12.3 )] . Emtricitabine and tenofovir disoproxil fumarate is not approved for use in pediatric patients weighing less than 17 kg. HIV-1 PrEP The safety and effectiveness of emtricitabine and tenofovir disoproxil fumarate for HIV-1 PrEP in at-risk adolescents weighing a

Does Emtricitabine And Tenofovir Disoproxil Fumarate interact with other medicines?

7 DRUG INTERACTIONS • Tenofovir disoproxil fumarate increases didanosine concentrations.; Dose reduction and close monitoring for didanosine toxicity are warranted.; ( 7.2 ) • Coadministration decreases atazanavir concentrations.; When coadministered with emtricitabine and tenofovir disoproxil fumarate, use atazanavir given with ritonavir.; ( 7.2 ) • Coadministration of emtricitabine and tenofovir disoproxil fumarate with certain HIV-1 protease inhibitors or certain drugs to treat HCV increases tenofovir concentrations.; Monitor for evidence of tenofovir toxicity..