Reverse transcriptase inhibitors, non-nucleosidal
Synonym(s)
NNRTI; non-nucleosidal reverse transcriptase inhibitors; Non nucleoside reverse transcriptase inhibitor
DefinitionThis section has been translated automatically.
Drugs that bind directly to the enzyme reverse transcriptase of HI viruses and thus inhibit the conversion of retroviral RNA into DNA.
Pharmacodynamics (Effect)This section has been translated automatically.
NNRTI were first described in 1990. As with nucleoside analogues (NRTI), the reverse transcriptase is the drug's point of attack. The binding to the enzyme induces the blocking of a catalytically active binding site and leads to a conformational change. Consecutively, fewer nucleosides can now bind to the enzyme, which results in a slowdown of polymerisation. The viral genesis is disturbed by this process. In contrast to the nucleoside analogues, this does not lead to the generation of wrong building blocks, but to a direct and non-competitive inhibition of the reverse transcriptase.
IndicationThis section has been translated automatically.
Therapy of HIV infections; preparations are prescribed in combination with other antiretroviral drugs (see also HAART).
Dosage and method of useThis section has been translated automatically.
S.u. HIV infection.
Undesirable effectsThis section has been translated automatically.
The most important adverse effects of the respective drugs are listed in table form under HIV infection.
Note(s)This section has been translated automatically.
Resistance test recommended before starting therapy. In 2001/2002, NNRTI resistance was detected in almost 10% of all therapy-naïve HIV-positive patients in Europe.
LiteratureThis section has been translated automatically.
- Sheran M (2005) The NNRTIs efavirenz and nevirapine in the treatment of HIV. HIV Clin Trials 6: 158-168
- Wensing AM et al (2005) Prevalence of drug-resistant HIV-1 variants in untreated individuals in Europe: implications for clinical management. J Infect Dis 192: 958-966