Table 5.
Predicted indices of foetal exposure to efavirenz and thalidomide in the foetal plasma and umbilical cord during pregnancy.
| Pharmacokinetic parameter (units) | Second trimester n = 100 |
Third trimester n = 100 |
Second trimester n = 100 |
Third trimester n = 100 |
|---|---|---|---|---|
| Thalidomide | 200 mg | 400 mg | ||
| Foetal plasma | ||||
| Thalidomide concentration (mg/L) | 2.15 (1.47–3.56) | 2.15 (1.53–3.18) | 4.27 (2.68–8.19) | 4.31 (3.07–6.37) |
| AUC0–24 (mg.h/L) | 51.1 (35.0–84.1) | 51.1 (36.5–75.5) | 101 (63.8–192) | 102 (72.9–151) |
| F:M | 4.69 (3.06–9.57) | 4.55 (3.06–9.57) | 4.59 (3.21–8.85) | 4.55 (3.06–9.57) |
| Umbilical vein | ||||
| Thalidomide concentration (mg/L) | 0.537 (0.352–0.899) | 0.555 (0.352–0.899) | 1.14 (0.729–2.06) | 1.11 (0.704–1.80) |
| AUC0–24 (mg.h/L) | 12.7 (8.33–21.2) | 13.1 (8.33–21.2) | 27.0 (17.2–48.5) | 26.2 (16.7–42.3) |
| C:M | 1.09 (0.89–1.73) | 1.09 (0.89–1.58) | 1.05 (0.85–1.54) | 1.09 (0.89–1.58) |
| Efavirenz | 400 mg | 600 mg | ||
| Foetal plasma | ||||
| Efavirenz concentration (mg/L) | 0.720 (0.223–2.72) | 1.06 (0.499–4.30) | 1.02 (0.333–5.65) | 1.52 (0.700–6.31) |
| AUC0–24 (mg.h/L) | 16.7 (5.19–62.9) | 24.7 (11.7–99.2) | 23.6 (7.75–130) | 35.4 (16.4–145) |
| F:M | 0.47 (0.17–0.74) | 0.89 (0.73–1.05) | 0.47 (0.17–0.76) | 0.89 (0.73–1.06) |
| Umbilical vein | ||||
| Efavirenz concentration (mg/L) | 0.159 (0.022–0.869) | 0.445 (0.204–1.74) | 0.232 (0.033–1.71) | 0.642 (0.288–2.56) |
| AUC0–24 (mg.h/L) | 3.70 (0.509–20.1) | 10.3 (4.75–40.2) | 5.36 (0.760–39.3) | 14.9 (6.73–59.0) |
| C:M | 0.10 (0.02–0.23) | 0.41 (0.25–0.57) | 0.10 (0.02–0.23) | 0.41 (0.25–0.58) |
Data presented as median (range).