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. 2005 May;49(5):1733–1738. doi: 10.1128/AAC.49.5.1733-1738.2005

TABLE 2.

Pharmacokinetic parameters for each isoniazid preparation according to the number of “wild-type” high-activity (NAT2*4) and low-activity (NAT2*X) allelesa

Dose (mg) No. of NAT2*4 alleles (n)b AUC/dose (h/liter) Cmax/dose (1/liter) tmax (h) t1/2 (h) Bioavailability (%) Vdss (liters)
100, oral 0 (13) 0.091 (0.067-0.132)** 0.021 (0.015-0.037)* 0.50 (0.33-1.00) 3.58 (1.70-10.40) 90.5 (79.2-113.3)
1 (2) 0.048** 0.017* 1.25 2.20 87.4
0.048** 0.009* 0.50 6.02 92.8
2 (3) 0.031 (0.027-0.037)** 0.012 (0.0117-0.015) 0.33 3.82 (2.55-4.75) 78.4 (74.7-89.3)
300, oral 0 (13) 0.107 (0.077-0.154)** 0.026 (0.015-0.039) 0.50 (0.33-2.50) 4.40 (2.44-5.86) 107.2 (91.8-115.9)
1 (2) 0.066** 0.026 0.50 2.52 118.8
0.048** 0.015 0.33 6.57 92.0
2 (3) 0.041 (0.036-0.042)** 0.018 (0.017-0.027) 0.33 (0.33-0.50) 3.39 (2.46-3.93) 100.1 (98.2-105.9)
200, i.v. 0 (13) 0.102 (0.066-0.138)** 0.034 (0.019-0.041) 4.18 (2.08-5.02) 51.8 (30.0-71.1)
1 (2) 0.055** 0.031 1.96 43.6
0.051** 0.029 5.32 98.2
2 (3) 0.040 (0.036-0.042)** 0.026 (0.019-0.029) 4.27 (2.76-4.38) 77.5 (77.1-109)
a

The parameters were derived directly from the data using the standard noncompartmental approach. AUC, area under the concentration-time curve; Cmax, maximal plasma concentration; tmax, time of occurrence of Cmax; t1/2, apparent elimination half-life; Vdss, volume of distribution at steady state; i.v., intravenous. The 300-mg isoniazid dose was administered in combination with 60 mg vitamin B6. *, P < 0.05; **, P < 0.01 in the Kruskal-Wallis test comparing genotypes. For all other parameters, there was no significant difference. Values are medians (range).

b

For n = 2, both values are shown.