Enantiomer/
Treatment

Variables

Cmax,
(ng/mL)

tmax,
(h)

t1/2
(h)

AUC
(ng*h/mL)

Cl /F
(L/h/kg)

Vz
(L/kg)

AUCoral/AUCIV

(R)-enantiomer desvenlafaxine

IV desvenlafaxine
50 mg/1 h

Mean (SD)
%CV
Geo. Mean
Min-Max

111.5 (25.5)
23%
108.8
78.4–156.1

1.0 (0.03)
3%
1.0
1.0–1.1

9.9 (3.1)
31%
9.5
6.2–17.7

1173 (291)
25%
1134
577–1590

0.280 (0.076)
27%
0.272
0.192–0.450

3.857 (1.058)
27.4%
3.736

2.055–6.772

 

Oral desvenlafaxine
100 mg

Mean (SD)
%CV
Geo. Mean
Min-Max

76.7 (20.0)
26%
74.2
41.8–115.1

7.0 (2.6)
37%
6.6
4.0–12.0

10.3 (1.9)
19%
10.1
6.7–14.0

1915 (615)
32%
1785
481–2828

 

 

0.804
(0.155)
19.3%
0.787

0.417–
1.053

(S)-enantiomer desvenlafaxine

IV desvenlafaxine
50 mg/1 h

Mean (SD)
%CV
Geo. Mean
Min-Max

120.2 (27.6)
23%
117.3
85.0–176.0

1.0 (0.03)
3%
1.0
1.0–1.1

9.5 (2.0)
21%
9.3
6.4–12.2

1262 (299)
24%
1224
652–1634

0.259 (0.065)
25%
0.252
0.185–0.398

3.397 (0.504)
14.8%
3.362
2.441–4.295

 

Oral desvenlafaxine
100 mg

Mean (SD)
%CV
Geo. Mean
Min-Max

83.1 (22.3)
27%
80.2
47.7–128.2

6.6 (2.1)
33%
6.3
4 .0–12.0

10.2 (2.0)
20%
10.0
6.9–14.5

2057 (643)
31%
1925
542–3017

 

 

0.804
(0.155)
19.3%
0.787

0.416–
1.050

Racemic (R+S) desvenlafaxine

IV desvenlafaxine
50 mg/1 h

Mean (SD)
%CV
Geo. Mean
Min-Max

231.6 (53.0)
23%
226.2
163.4–332.1

1.0 (0.03)
3%
1.0
1.0–1.1

9.8 (2.1)
21%
9.6
7.3–13.9

2442 (585)
24%
2366
1233–3261

0.268 (0.068)
26%
0.260
0.188–0.420

3.664 (0.546)
14.9%
3.624
2.529–4.468

 

Oral desvenlafaxine
100 mg

Mean (SD)
%CV
Geo. Mean
Min-Max

159.6 (42.2)
27%
154.3
89.4–243.3

6.4 (2.1)
33%
6.1
4.0–12.0

10.4 (2.0)
19%
10.2
6.9–14.3

3993 (1271)
32%
3728
1023–5844

 

 

0.805
(0.157)
19.6%
0.788

0.415–
1.059

Abbreviations: AUC: Area Under the Plasma Concentration-time Curve; Cl/F: Apparent Oral-dose Clearance (dose/AUC); Cmax: Peak Plasma Concentration; CV: Coefficient of Variation; Geo. Mean: Geometric Mean; IV: Intravenous; Max: Maximum; Min: Minimum; SD: Standard Deviation; t1/2: Terminal-phase Elimination Half-life; tmax: Time to Peak Concentration; Vz: Apparent Volume of Distribution after Administration Based on the Terminal Phase
Table 2: Summary of Plasma Desvenlafaxine Pharmacokinetic Parameters.
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