Reverse transcriptase inhibitors, non-nucleosidal

Drugs that bind directly to the enzyme reverse transcriptase of HI viruses and thus inhibit the conversion of retroviral RNA into DNA.

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.

Therapy of HIV infections; preparations are prescribed in combination with other antiretroviral drugs (see also HAART).

S.u. HIV infection.

The most important adverse effects of the respective drugs are listed in table form under HIV infection.

Viramune, Sustiva

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.