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
Tigan Pharmacology, Pharmacokinetics, Studies, Metabolism - Trimethobenzamide hydrochloride
Tigan Pharmacology, Pharmacokinetics, Studies, Metabolism - Trimethobenzamide hydrochloride
CLINICAL PHARMACOLOGY
Mechanism of Action
The mechanism of action of Tigan® as determined in animals
is obscure, but may involve the chemoreceptor trigger zone (CTZ), an area in
the medulla oblongata through which emetic impulses are conveyed to the vomiting
center; direct impulses to the vomiting center apparently are not similarly
inhibited. In dogs pretreated with trimethobenzamide HCl, the emetic response
to apomorphine is inhibited, while little or no protection is afforded against
emesis induced by intragastric copper sulfate.
Pharmacokinetics
The pharmacokinetics of trimethobenzamide have been studied
in healthy adult subjects. Following administration of 200 mg (100 mg/mL) Tigan
I.M. injection, the time to reach maximum plasma concentration (Tmax)
was about half an hour, about 15 minutes longer for Tigan 300 mg oral capsule
than an I.M. injection. A single dose of Tigan 300 mg oral capsule provided
a plasma concentration profile of trimethobenzamide similar to Tigan 200 mg
I.M. The relative bioavailability of the capsule formulation compared to the
solution is 100%. The mean elimination half-life of trimethobenzamide is 7 to
9 hours.
Special Populations
Gender
Systemic exposure to trimethobenzamide was similar between
men (N=40) and women (N=28).
Race
Pharmacokinetics appeared to be similar for Caucasians (N=53)
and African Americans (N=12).
top
