|
Dose
(mg/kg) |
Route |
Subjects
(n)* |
Cmax
(µg/l) |
tmax
(h) |
t½
(h) |
ka
(1/h) |
V/F
(l/kg) |
CL/F
(l/h/kg) |
Ref. |
|
5.3 |
oral |
10; H |
260 |
1.0 |
1.9 |
1.3 |
- |
- |
134 |
|
5.3 |
i.m. |
10;
H |
209 |
3.4 |
7.4 |
0.44 |
- |
|
134
|
|
10 |
oral |
12;
H |
391 |
1.8 |
2.6 |
1.2 |
19.4 |
51 |
42 |
|
9.5 |
oral
- SD
oral
- MD |
19;
P |
588
116 |
2.4
3.1 |
2.3
2.2 |
- |
32
184 |
6.0
35.8 |
51 51 |
|
9.3
9.1 |
oral
oral
+ M |
18;
P
20;
P |
587
818 |
2.5
2.0 |
2.2
2.5 |
- |
29
18 |
5.8
3.5 |
2
2
|
|
500
mg |
oral
- SD
oral
- MD |
9;
P |
428
161 |
1.6
2.0 |
2.5
3.2 |
- |
- |
- |
7
7
|
|
500
mg |
oral
- Fs |
12;
H |
391 |
1.8 |
2.6 |
|
19.4 |
- |
141
|
|
600
mg |
rectal |
8;
PF |
105 |
7.2 |
3.1 |
|
80.8 |
- |
141
|
|
6.2 |
oral |
6;
H |
360 |
1.7 |
a
= 2.6
b
= 4.3 |
1.2 |
32.6 |
6.3 |
20
|
|
6.8 |
oral |
4;
H |
150 |
- |
2.3 |
- |
- |
16 |
123
|
|
9.1 |
oral |
11;
P |
364 |
2.9 |
2.7 |
0.9 |
22.8 |
7.8 |
40
|
|
10.4 |
oral
- F
oral
- CC |
6;
H |
623
483 |
2.7
1.8 |
2.5
2.6 |
0.75
1.0 |
16.4
16.2 |
5.4
6.7 |
41
41
|
|
10
10.8 |
oral
oral |
23;CPF
31;PF |
- |
- |
1.8
2.6 |
-
1.7
†‡ |
37.9
34.4 |
14.4
9.3 |
124 124 |
|
9.1 |
oral
- D1‡
oral
- D4‡
oral
- D7‡
oral
- D21‡ |
10;
H
10;
H
10;
H
7;
H |
311
148
110
195 |
- |
3.0
3.8
4.8
2.7 |
|
- |
9.1
55.1
146.3
10.1 |
|
|
12.2 |
rectal |
8;
PF |
108 |
6.5 |
- |
|
- |
- |
71
|
|
4.6
9.3
18.5 |
oral |
8;
H |
205
450
792 |
2.8
2.3
2.8 |
1.4
2.0
2.8 |
|
38.4
35.5
33.7 |
8.9
7.8
6.2 |
4
|
|
9.8 |
oral
- SD
oral
- MD |
15;
PF |
706
134 |
2.5
2.0 |
2.0
1.9 |
|
- |
5.8
31.7 |
6
|
|
10.0 |
rectal
- SD
rectal
- MD |
15;
PF |
185
41 |
4.0
2.5 |
2.0
3.5 |
|
- |
- |
6
|
|
500
mg |
oral
- D1
oral
- D7 |
9;
H |
501
125 |
|
3.0
2.5 |
|
|
|
129
|
|
7.3
10.0 |
rectal
(Std)
rectal
(PEG) |
8;
H
6;
H |
100
75 |
7.1
6.7 |
|
|
89
72 |
25
20 |
72
|
|
9.4 |
oral |
6;
Cirr |
332 |
3.0 |
4.0 |
|
39 |
7.2 |
39
|
* H = healthy adult volunteers, P = adult patients, CPF = child patients with falciparum malaria, PF adult patients with falciparum malaria = , M = mefloquine, SD = single dose, MD = multiple doses, F = fasting, CC = with food, † = pooled data for adults and children, Fs = fasting, Cirr = hepatic cirrhosis, rectal (Std) = conventional suppositories, rectal (PEG) = polyethylene glycol suppositories. Cmax=maximum plasma concentration; tmax=time of maximum concentration; t1/2=elimination half-life; ka=first order absorption rate constant; V/F= volume of distribution after non-i.v. administration; CL/F=clearance after non-i.v. administration;
‡ Subjects received 500 mg daily for 7 days, followed by a washout period of 14 days, and a single dose on day 21 (at the end of the washout period). Pharmacokinetic parameters were determined on days 1, 4, 7 and 21.