A1,
A2,
B,
C1,
C2,
D,
E,
F,
G-H,
I-K,
L,
M,
N,
O,
P1,
P2,
Q-R,
S,
T,
U-V,
W-Z
Carafate Pharmacology, Pharmacokinetics, Studies, Metabolism - Sucralfate
Carafate Pharmacology, Pharmacokinetics, Studies, Metabolism - Sucralfate
CLINICAL PHARMACOLOGY
Sucralfate is only minimally absorbed from the gastrointestinal tract. The
small amounts of the sulfated disaccharide that are absorbed are excreted primarily
in the urine.
Although the mechanism of sucralfate's ability to accelerate healing of duodenal
ulcers remains to be fully defined, it is known that it exerts its effect through
a local, rather than systemic, action. The following observations also appear
pertinent:
- Studies in human subjects and with animal models of ulcer disease have shown
that sucralfate forms an ulcer-adherent complex with proteinaceous exudate
at the ulcer site.
- In vitro, a sucralfate-albumin film provides a barrier to diffusion of hydrogen
ions.
- In human subjects, sucralfate given in doses recommended for ulcer therapy
inhibits pepsin activity in gastric juice by 32%.
- In vitro, sucralfate adsorbs bile salts.
These observations suggest that sucralfate's antiulcer activity is the result
of formation of an ulcer-adherent complex that covers the ulcer site and protects
it against further attack by acid, pepsin, and bile salts. There are approximately
14 to 16 mEq of acid-neutralizing capacity per 1-g dose of sucralfate.
CLINICAL TRIALS
In a multicenter, double-blind, placebo-controlled study of CARAFATE Suspension,
a dosage regimen of 1 g (10 mL) four times daily was demonstrated to be superior
to placebo in ulcer healing.
|
Results From Clinical Trials
Healing Rates for Acute Duodenal Ulcer
|
|
Treatment
|
n |
Week 2
Healing
Rates |
Week 4
Healing
Rates |
Week 8
Healing
Rates |
|
CARAFATE
Suspension
|
145 |
23(16%) * |
66(46%) ** |
95(66%) *** |
|
Placebo
|
147 |
10(7%) |
39(27%) |
58(39%) |
|
* P =0.016
** P =0.001
*** P =0.0001
|
Equivalence of sucralfate suspension to sucralfate tablets has not been demonstrated.
top
