Which medications in the drug class Nucleoside or Nucleotide Reverse Transcriptase Inhibitors are used in the treatment of Pediatric HIV Infection?

Updated: Mar 05, 2020
  • Author: Delia M Rivera, MD; Chief Editor: Russell W Steele, MD  more...
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Answer

Nucleoside or Nucleotide Reverse Transcriptase Inhibitors

NRTIs are nucleoside or nucleotide reverse transcriptase inhibitor analogs with antiretroviral activity. They are indicated for the treatment of HIV infection, and they delay the progression of the disease.

Abacavir (ABC, Ziagen)

Patients and parents must be cautioned about the risk of serious hypersensitivity reaction (HSR). Provide a medication guide and warning card. Test patients for the HLA-B*5701 allele before starting therapy to predict risk of HSR. Indicated for children aged 3 months or older.

Didanosine (ddI, dideoxyinosine, Videx, Videx EC)

This agent is a purine nucleoside analog with antiviral activity. Indicated for children (including neonates aged 2 week or older); however, because of significant toxicity (eg, peripheral neuropathy, lactic acidosis, hepatomegaly), it is not typically prescribed since there are safer agents available.

Lamivudine (3TC, Epivir, Epivir HBV)

Lamivudine is a dideoxynucleoside analog with antiretroviral activity. In combination with oral zidovudine, it produces substantial and sustained increases in CD4+ counts and decreases in viral load in HIV-infected patients. It is approved by the FDA for children aged ≥ 3 months for HIV and is a common component of most nucleoside backbone regimens. It is also approved to treat hepatitis B.

Stavudine (d4T, Zerit)

Stavudine is a synthetic thymidine nucleoside analog active against HIV-1. Although stavudine is approved by the FDA for use in infants and children, it is not typically prescribed because it carries a higher risk of adverse effects associated with mitochondrial toxicity and a higher incidence of lipoatrophy than other NRTIs.

Zidovudine (ZDV, AZT, Retrovir)

This agent is a thymidine analog that inhibits viral replication. It inhibits activity of HIV reverse transcriptase by competing with natural substrate for use by and incorporation into viral DNA. Frequent choice of NRTI backbone for ART. It has extensive experience in pediatrics including treatment and prevention of perinatal transmission.

Emtricitabine (Emtriva)

A synthetic nucleoside cytosine analog, emtricitabine competes with deoxycytidine-5'-triphosphate and incorporates into viral DNA, causing chain termination. It is approved by the FDA in children (starting at birth). It has minimal toxicity and is administered once daily as part of a dual-NRTI backbone.

Tenofovir DF (TDF, Viread)

This antiretroviral agent used in treatment of AIDS inhibits activity of HIV reverse transcriptase by competing with natural substrate deoxyadenosine 5'-triphosphate and, after incorporation into DNA, by causing DNA chain termination. It is administered as prodrug bis-isopropoxycarbonyloxymethyl ester derivative of tenofovir, which is converted, in various enzymatic processes, to tenofovir, an acyclic nucleoside phosphonate (nucleotide) analog of adenosine 5'-monophosphate.

Administration with a high-fat meal enhances bioavailability. Prolonged intracellular levels allows for once-daily dosing. It is approved by the FDA for children aged 2 years or older.


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