Table 7.

Plasma and epithelial lining fluid concentrations of tetracyclines

Antibacterial agent	Dosage regimen	Subjects [n]	Sampling time [h]a	ELF to plasma ratio based on AUC	Plasma concentration [µg/mL]b	ELF concentration [µg/mL]b	References
Tigecycline	100 mg IV 0.5 h infusion × 1 dose, then 50 mg IV 0.5 h infusion q12h × 6 doses	4	2	1.71c	0.217 ± 0.051	0.553 ± 0.497	[94]
		5	4		0.159 ± 0.026	0.233 ± 0.070
		4	6		0.157 ± 0.036	0.268 ± 0.097
		4	12		0.121 ± 0.036d	0.149 ± 0.028e
Omadacycline	100 mg IV 0.5 h infusion q12h × 2 doses, then 100 mg IV 0.5 h infusion q24h × 3 doses	6	0.5	1.47f	1.80 ± 0.13	1.73 ± 1.01	[94]
		6	1		0.89 ± 0.19	2.25 ± 0.72
		5	2		0.93 ± 0.33	1.51 ± 0.94
		6	4		0.54 ± 0.12	0.95 ± 0.33
		6	8		0.56 ± 0.12	0.58 ± 0.19
		6	12		0.42 ± 0.07	0.61 ± 0.29
		6	24		0.27 ± 0.05	0.41 ± 0.13
Eravacycline	1 mg/kg (maximum 100 mg) IV 1 h infusion q12h × 7 doses	5	2	6.44g	0.083 ± 0.012h	0.70 ± 0.30	[100]
		5	4		0.065 ± 0.011h	0.57 ± 0.20
		5	6		0.054 ± 0.009h	0.34 ± 0.16i
		5	12		0.037 ± 0.009h	0.25 ± 0.13j

ELF epithelial lining fluid, AUC area under the concentration-time curve, IV intravenously, BLQ below the lower limit of quantification, qxh every x hours, SD standard deviation

^aSampling time after the last dose

^bTotal plasma and ELF concentrations expressed as mean ± SD

^cBased on the ratio of AUC₁₂ in ELF to AUC₁₂ in total plasma

^dThree concentrations were available at this sampling time

^eTwo of the four subjects had ELF concentrations BLQ (< 1 ng/mL)

^fBased on the ratio of AUC₂₄ in ELF to AUC₂₄ in total plasma

^gBased on the ratio of AUC₁₂ in ELF to AUC₁₂ in unbound plasma, assuming protein binding between 79.3 and 87.1% in plasma

^hTwenty concentrations were available at each sampling time

ⁱTwo of the five subjects had ELF concentrations BLQ (< 0.5 µg/mL)

^jThree of the five subjects had ELF concentrations BLQ (< 0.5 µg/mL)