Table 1.
Summary of the basic pharmacological characteristics of each NNRTI. If not specified, data are obtained from European Medicines Agency (EMA) product information. OD: once daily; BD: twice a day.
| NNRTI | Commercial Name | Recommended Dose (Adults) | Bioavailability | Pharmacokinetics Concentrations (μg/mL) | Main Hepatic Metabolism |
|---|---|---|---|---|---|
| Nevirapine | Viramune | 200 mg orally OD for the first 14 days, followed by 200 mg BD or 400 mg OD | After oral administration: >90% | In patients taking 200 mg OD: steady state plasma Cmax of 5.74 (5.0–7.44) and Cmin of 3.73 (3.2–5.08) (median and range) | CYP3A4 CYP2B6 |
| Efavirenz | Sustiva Stocrin |
600 mg orally OD | After oral administration: 40–50% | In patients taking 600 mg OD: steady state plasma Cmax of 4.072 ± 1.167 and Cmin of 1.767 ± 1.01 (mean ± SD) | CYP2B6 CYP3A4 [11] |
| Etravirine | Intelence | 200 mg orally BD | Absolute bioavailability unknown | In patients taking 200 mg BD: Cmax of 0.586 (0.199–3.13) and Cmin of 0.297 (0.075–2.71) (median and range) [12] | CYP3A4 CYP2C9 CYP2C19 |
| Rilpivirine | Edurant Rekambys | 25 mg orally OD, or long-acting intramuscular injection of 900 mg initially followed by 600 mg monthly or 900 mg every 2 months | Absolute bioavailability unknown | Cmax (mean ± SD) in patients taking 25 mg orally OD: 0.134 ± 0.072. In volunteers injected with a loading dose of long-acting RPV of 1200 mg on day 1 was 0.140 ± 0.016, 600 mg on day 29 was 0.120 ± 0.04 and 600 mg on day 57 was 0.132 ± 0.019 [13] | CYP3A4 CYP3A5 [14] |
| Doravirine | Pifeltro | 100 mg orally OD | After oral administration: 64% | In patients taking 100 mg OD: steady state plasma Cmax of 0.962 (19) (geometric mean and % CV) | CYP3A4 CYP3A5 [15] |