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Tenofovir disoproxil is a type of medicine known as an antiretroviral drug, which is used to treat HIV and chronic hepatitis B. HIV is a sexually transmitted illness that eventually progresses to Acquired Immunodeficiency Syndrome. Chronic hepatitis B is a prolonged viral infection caused by the hepatitis B virus. It is a nucleotide reverse transcriptase inhibitor that interferes with the normal function of enzymes required for viral generation. It successfully alleviates symptoms associated with HIV and chronic hepatitis B infection. It was first authorized in 2001.

BRAND NAMES:

Atripla: It is the combination of efavirenz, emtrcitibine, and tenofovir. It is available in the form of tablets used to treat HIV-1 infection.

Complera: It is a combination of emtricitabine, rilpivirine, and tenofovir. It is available in the form of tablets used to treat a complete regimen for the treatment of HIV-1 infection.

MECHANISM OF ACTION:

Tenofovir diphosphate inhibits HIV-1 reverse transcriptase and Hepatitis B polymerase by direct binding competition with the natural DNA substrate and incorporation into DNA, resulting in viral DNA chain termination.

PHARMACOKINETICS:

Absorption: Tenofovir oral dosing resulted in a peak plasma time of 1 hour while fasting and 2 hours after meal consumption. Tenofovir has a bioavailability of 25%, which climbs to 40% following a high-fat diet.

Distribution: The volume of distribution of tenofovir at steady-state is 1.3 L/kg and 1.2 L/kg.

Metabolism: Tenofovir bisoprolol fumarate is quickly converted to tenofovir, which is then metabolized intracellularly to the active metabolite tenofovir diphosphate, which inhibits HIV-1 reverse transcriptase and ends the developing DNA chain. Tenofovir is not metabolized by any cytochrome P450.

Excretion:Tenofovir is excreted through urine.

PHARMACODYNAMICS:

This medication reduces viral DNA chain elongation in HIV-1 and hepatitis B infections by inhibiting enzymes required for host cell infection and viral replication.

DOSAGE AND ADMINISTRATION:

Tenofovir is available as a tablet to be taken orally. Typically, the pill is taken once a day, with or without meals. The powder is typically consumed with meals once a day. It is available as tablets with strengths of 150mg, 200mg, 250mg, and 300mg.

DRUG INTERACTIONS:

Drug interactions with tenofovir may include

  • Bacterial infection medicines: aminoglycosides, vancomycin
  • Hepatitis B virus drugs: adefovir, dipivoxil
  • Antifungal medicine—amphotericin B
  • Anti-viral drugs: didanosine and ganciclovir
  • Immunotherapy: interleukin-2
  • Immune suppressant: tacrolimus

SIDE EFFECTS:

Side effects of tenofovir may include

  • Depression
  • Diarrhea
  • Headache
  • Fever
  • Rash
  • Itching
  • Weight loss
  • Difficulty falling asleep

Some side effects can be serious; they may include

  • Swelling of feet
  • Decreased urination
  • Pain in the arms, hands, feet, or legs
  • Dizziness
  • Cold hands
  • Irregular heartbeat
  • Pain in the upper right part of the stomach
  • Shortness of breath

OVERDOSE:

Symptoms of overdose may include

  • Trouble breathing
  • Unusual muscle pain
  • Stomach pain
  • Vomiting
  • Fast heartbeat
  • Dizziness
  • Feeling weak or tired

TOXICITY:

Tenofovir is an antiretroviral therapy drug that can cause toxicity to the kidneys and bones.

 

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Tenofovir
Tenofovir Disoproxil Fumarate Standard

Tenofovir Disoproxil Fumarate Standard

CAS Number
202138-50-9
Tenofovir Disoproxil  Standard

Tenofovir Disoproxil Standard

CAS Number
201341-05-1
Tenofovir Impurity

Tenofovir Impurity

CAS Number
107021-12-5
Tenofovir Disoproxil Dimer

Tenofovir Disoproxil Dimer

CAS Number
1093279-76-5
Tenofovir Disoproxil Carbamate

Tenofovir Disoproxil Carbamate

CAS Number
1244022-54-5
Tenofovir Mono-POC PMPA

Tenofovir Mono-POC PMPA

CAS Number
211364-69-1
Mono-POC Tenofovir Fumarate Salt

Mono-POC Tenofovir Fumarate Salt

CAS Number
1534434-02-0