Generic
Tenofovir Disoproxil Fumarate
12 brands available in the market
At a glance
Tenofovir Disoproxil Fumarate is a nucleotide reverse transcriptase inhibitor (NRTI) used for the treatment of HIV-1 infection and chronic hepatitis B (HBV) infection. It inhibits viral replication.
Description
Tenofovir Disoproxil Fumarate is a diester prodrug of tenofovir that is rapidly converted to tenofovir after oral absorption. Tenofovir is phosphorylated to tenofovir diphosphate, which competes with natural deoxyadenosine triphosphate and incorporates into viral DNA, causing chain termination.
Indications
- HIV-1 infection (in combination with other antiretrovirals)
- Chronic hepatitis B (HBV) infection (adults)
Therapeutic class
HIV/Anti-retroviral & Hepatic Viral Infections Drugs
Pharmacological class
Nucleotide Reverse Transcriptase Inhibitor (NRTI)
Pharmacology
Tenofovir Disoproxil Fumarate is a prodrug of tenofovir that is converted intracellularly to tenofovir diphosphate. It competes with the natural substrate deoxyadenosine triphosphate for HIV-1 reverse transcriptase and HBV polymerase, incorporating into viral DNA and causing chain termination.
Mechanism of action
Inhibits viral reverse transcriptase to stop DNA replication.
Dosage
Adult Dose (Oral):
- HIV-1/HBV: 300 mg (245 mg tenofovir DF) once daily
- May be taken with or without food
Pediatric Dose (≥12 years, ≥35 kg):
- 245 mg tenofovir DF once daily
Administration
- Take with or without food
- Swallow tablet whole; do not chew, crush, or break
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember; if almost time for the next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Headache, diarrhea, nausea
- Weakness, rash, abdominal pain
- Dyspepsia, chest pain, drowsiness
Serious:
- Lactic acidosis/severe hepatomegaly with steatosis
- Renal impairment (Fanconi syndrome)
- Decreased bone mineral density (osteoporosis)
Precautions & warnings
- Do not use alone in HIV-1 coinfected patients (risk of HIV-1 resistance)
- Severe exacerbation of hepatitis B may occur upon discontinuation
- Renal impairment: Adjust dosing interval for CrCl <50 mL/min
- Suspend if lactic acidosis is suspected
- Long-term use may cause bone loss
Contraindications
- Previously demonstrated hypersensitivity to tenofovir
Drug interactions
- Didanosine: Risk of pancreatitis and peripheral neuropathy; avoid
- Atazanavir (without ritonavir): Monitoring required with tenofovir
- Nephrotoxic drugs (aminoglycosides, amphotericin B, vancomycin): Risk of renal impairment
Food interactions
It is not known whether alcohol is safe with Tenofovir Disoproxil Fumarate; consult your doctor.
Use in pregnancy
Use in Pregnancy: Generally safe; animal studies show low or no adverse effects; limited human data; consult your doctor.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably safe; limited data suggests no significant risk; HIV-1 infected mothers should not breastfeed; consult your doctor.
Pediatric use
Indicated for children ≥12 years, ≥35 kg
Geriatric use
Insufficient numbers of patients ≥65 years included in trials; caution required
Renal / hepatic impairment
Renal Impairment: CrCl 30-49: 300 mg every 48 hours; CrCl 10-29: 300 mg every 72-96 hours; Hemodialysis: every 7 days or after 12 hours of dialysis; consult your doctor.
Hepatic Impairment: Safe in liver disease; dose adjustment may not be needed; consult your doctor.
Overdose effects
In overdose, provide general supportive measures and monitor vital signs; tenofovir is removed by hemodialysis.
Storage conditions
Store below 25°C in a cool and dry place, protected from light; keep out of reach of children.
Chemical structure
Tenofovir Disoproxil Fumarate