Table 4.

Pentamidine: primary and secondary pharmacokinetic parameters

Study	Patients	Weight (kg)	Daily dose	Sampling day	C max (ng/mL)	C trough (ng/mL)	t max (h)	V 1/F (L)	V ss/F (L)	CL/F (L/h)	AUC (ng·h/mL)	t ½ (h)
Non-compartmental
Bronner et al. [47]a	African trypanosomiasis patients	54 (34–66)	3.5–4.5 mg base/kg, 10 days			At 48 h:					0–48 h:
				Day 1	813 ± 1257	14 (7–16)	~1 hb	NA	NA	NA	2699 ± 1364c	23 ± 13 (n = 7)
				Day 10	825 ± 783	78 (57–92)	~1 hb	NA	NA	NA	5887 ± 1881c	47 ± 13 (n = 9)
Bronner et al. [51]a	African trypanosomiasis patients	63 (50–84)	3.0–4.8 mg base/kg	Single dose	393 ± 168	NA	End of infusion	NA	11,817 ± 4510	67±21	0–168 h: 2494 ± 1550	Terminal t ½: 11 ± 5c days
Compartmental
Conte et al. [53]	AIDS patients/Pneumocystis carinii pneumonia	62 ± 17	4.0 mg salt/kg IM	Single dose	209 ± 48	6.55 ± 3.51	0.67 ± 0.26	924 ± 404	2724 ± 1066	305 ± 81	NA	t ½,α: 0.90 ± 0.18 t ½,β: 9.4 ± 2.0
			4.0 mg salt/kg IV	Single dose	612 ± 371	2.90 ± 1.44		140 ± 93	821 ± 535	248 ± 91		t ½,α: 0.30 ± 0.22 t ½,β: 6.4 ± 1.3
Conte et al. [57]d	AIDS patients/P. carinii pneumonia	64 ± 8 (excluding 2 children: 5.7/20 kg)	4 mg/kge Various lengths of treatment	Different	NA	NA	NA	205 ± 54	1000 ± 506	411 ± 55	NA	6.2 ± 1.2
Conte et al. [54]	AIDS patients/P. carinii pneumonia	66 ± 10	3 mg/kge, 9–18 days	Day 1	282 ± 72f	2.1 ± 1.4	NA	38.2 ± 27.3	3500 ± 3800	268 ± 70	AUC∞: 748 ± 211	t ½,α: 1.2 ± 0.6 g t ½,β: 29 ± 25
	Volunteer haemodialysis patients	73 ± 10	3 mg/kge, single dose	Single dose	275 ± 184	1.1 ± 0.8	NA	218 ± 295	12,400 ± 3900	592 ± 472	578 ± 407	t ½,α: 1.8 ± 0.6 g t ½,β: 72.6 ± 38.1
			4 mg/kge, single dose	Single dose	227 ± 110	1.7 ± 0.5	NA	218 ± 200	32,400 ± 45,300	329 ± 58	747 ± 158	t ½,α: 3.5±1.6 g t ½,β: 118±119
	P. carinii pneumonia patients	80 ± 8	3–4 mg/kge, 12–21 days	Last dose	NA	NA	NA	NA	NA	NA	N/A	Terminal t ½: 12.0 ± 2.3 days
Thomas et al. [49]	AIDS patients	60.2 (58–65)	~2.3 mg base/kg	Single dose	NA	NA	NA	26 ± 8	825 ± 458	73.6 ± 35.8	AUC∞: 2500 ± 1700	t ½,α: 5.4 ± 2.4 min t ½,β: 11.2 ± 7.8

Data given as either mean ± standard deviation or median (range), unless indicated otherwise

AUC area under the concentration–time curve, AUC _∞ AUC from time zero to infinity, CL clearance, C _max peak plasma concentration, C _trough trough plasma concentration 24 h after dose, F bioavailability, IM intramuscular, IV intravenous, NA not available, t _½ plasma elimination half-life, t _½,α distribution half-life, t _½,β elimination half-life, t _max time to C _max, V ₁ central volume of distribution, V _ss volume of distribution at steady state

^aAll concentrations were reported in nmol/L and were translated into ng/mL with a molecular weight of 340.42 g/mol

^b C _max for most patients reached within 1 h. For 3 patients, C _max was noted 12–24 h after the dose [47]

^cPatients excluded if plasma concentration substantially increased after initial decrease, if concentrations were below quantitation limit or if the terminal slope was very different

^dOnly reported for 5 adult patients without renal failure (IV)

^eUnclear whether dose is reported as base or salt

^fOnly including patients with extensive sampling scheme

^gIn addition to reported slower distribution phase, a rapid distribution to peripheral tissues (mean 0.07–0.19 h⁻¹) was observed in the three-compartment model