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Tenofovir And Emtricitabine Combination

Tenofovir And Emtricitabine Combination

General Information

Tenofovir is an anti-retroviral. Anti-retrovirals are drugs that suppress the activity or replication of retroviruses such as HIV. This specific anti-viral combination is classified as a reverse transcriptase inhibitor, meaning that it blocks an enzyme which is essential for the retrovirus to multiply.

In South Africa the combination of emtricitabine and tenofovir is registered for the treatment of infection with the human immunodeficiency virus (HIV), often in combination with other anti-retroviral drugs.

If not treated, HIV will advance to weaken the body's immune system, gradually chipping away to create grounds for other infections, against which the body will find more and more difficult to protect itself. HIV develops into acquired immune deficiency syndrome (Aids) when your immune system has been severely weakened.

For this combination to be effective, it has to be taken regularly. By skipping even a few doses, the risk for treatment failure increases substantially. Try to ensure that you take all your doses, and at the correct time.

It should be understood that this medicine is not a cure for HIV or Aids, but is one of a variety of drugs that only restrict the advance of the virus, keeping the immune system up and running. It is used in combination with other anti-retroviral drugs and should not be prescribed on its own

The combination of emtricitabine and tenofovir does not reduce transmission of HIV; you can still infect another person with the virus and the use of appropriate precautions to prevent spread to other persons is highly recommended.

User information

Dietary advice: this combination should be taken with or after food.

Stopping this medicine: do not stop taking this drug without consulting your doctor.

Prolonged use: side effects may develop with long-term use; frequent blood tests may be required with prolonged therapy to determine liver and kidney function.

Special precautions

Consult your doctor before using this drug if:

  • you have known liver or kidney problems
  • you are obese
  • you have hepatitis
  • you have a history of alcohol abuse
  • you are taking other medication

Pregnancy: avoid. Potential risk to the foetus has been reported. Consult your doctor before use, or if you are planning to fall pregnant.

Breastfeeding: avoid. Not only can HIV-infection be passed to your baby through breast milk, but tenofovir is also present and transmitted in breast milk.

Porphyria: avoid. This medication may cause serious adverse effects. Consult your doctor before use.

The elderly: caution is advised in the elderly as side effects may be more severe.

Infants and children: this medication is not intended for use in children under the age of 18 years.

Driving and hazardous work: caution is advised as use of this medication may lead to dizziness. Avoid such activities until you know how this medication affects you.

Alcohol: avoid concomitant use of alcohol with this medication

How does this combination work?

When HIV infects a human T-cell, a type of white blood cell that plays a key role in the functioning of the immune system, viral genetic information in the form of RNA needs to be converted to DNA for the virus to have any effect. It makes use of an enzyme called reverse transcriptase to achieve this conversion. The combination of emtricitabine and tenofovir targets and inhibits this enzyme, thus preventing the spread of HIV.

Drug interactions

Atazanavir reduced bioavailability of atazanavir

Didanosine increased bioavailability of didanosine

Caution is advised when used concomitantly with medicines that are known to affect kidney function.

Many other drugs may interact with this combination. It is important to consult your doctor or pharmacist before combining any drug with tenofovir.

Disease interactions

Contact your doctor if you have a liver or kidney disease.

Overdose action

This combination, when taken in overdose is capable of having serious consequences. Seek immediate medical attention.

Recommended dosage

Adults, oral: 1 tablet (200 mg emtricitabine, 300 mg tenofovir) once daily.

Combination of Tenofovir and Emtricitabine plus Efavirenz: In Vitro Modulation of ABC Transporter and Intracellular Drug Accumulation

Efflux proteins have been shown to greatly affect the uptake of antiretroviral drugs by cells and to hamper their access to the human immunodeficiency virus type 1 replication site. This study evaluated the factors that may lead to drug-drug interactions between emtricitabine (FTC), tenofovir (TFV), and efavirenz (EFV), including the modulation of efflux transporter expression and function. Peripheral blood mononuclear cells from healthy volunteers were used to determine whether or not an interaction between antiretroviral drugs and target cells occurred in any combination of FTC, TFV, EFV, FTC-TFV, TFV-EFV, or FTC-TFV-EFV. Following 20 h of treatment, intracellular drug concentrations were measured by liquid chromatography-tandem mass spectrometry.

Efflux transporter functionality and inhibitor drug properties were assessed by measuring fluorescent dye efflux. ABCB1 (P-glycoprotein), ABCC 1 to 6 (multidrug resistance-associated protein), and OAT (organic anion transporter) expression in response to the treatments was quantified by semiquantitative real-time PCR. Cells treated with a double combination (FTC-TFV or TFV-EFV) or the triple combination (FTC-TFV-EFV) produced higher FTC and TFV intracellular concentrations than cells treated with FTC or TFV alone. However, no change in the EFV intracellular concentration was observed.

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