HIV in Children

ANTIRETROVIRAL DRUGS

Dr. Ira Shah
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Last Updated : 1st September 2012

Protease Inhibitors (PIs)


The PIs inhibit the protease enzyme (See chapter on Transmission and Pathogenesis) by binding to the active site of the enzyme, thus preventing cleavage of precursor polyproteins at a late stage of viral replication. Virions are produced, but they are incomplete and non-infectious. PIs were the third class of ARVs to be developed. They are highly potent. They are active against both HIV-1 and HIV-2. PIs have a high genetic barrier to resistance, and PI resistance at regimen failure is uncommon.
The various PIs used for treatment of HIV infection are:
  • Nelfinavir (NFV)

  • Ritonavir (RTV)

  • Lopinavir / Ritonavir (LPVr)

  • Amprenavir

  • Indinavir (IDV)

  • Saquinavir (SQV)

  • Atazanavir

  • Darunavir

  • Tipranavir

Boosted PIs


Low-dose ritonavir (RTV), itself a potent PI acts as a potent inhibitor of the cytochrome P450 3A4 (CYP3A4) isoenzyme, thereby inhibiting the metabolism of other PIs, and has been used in low doses combined with another PI as a “pharmacokinetic booster,” increasing drug exposure by prolonging the second drug’s half-life. Boosted PI-based regimens are commonly used in treatment of adults, but adequate pediatric data are only available for co-formulated lopinavir/ritonavir in children older than 6 weeks of age and for atazanavir, fosamprenavir, darunavir, and tipranavir with low-dose ritonavir in children age >6 years.

ANTIRETROVIRAL DRUGS
Dr. Ira Shah
Incharge Pediatric HIV and TB Clinic, B.J.Wadia Hospital for Children, Mumbai, India Consultant in Pediatric Infectious Diseases, Nanavati Hospital, Mumbai, India.
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