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
Glucagon Pharmacology, Pharmacokinetics, Studies, Metabolism - Glucagon
Glucagon Pharmacology, Pharmacokinetics, Studies, Metabolism - Glucagon
CLINICAL PHARMACOLOGY
Glucagon increases blood
glucose concentration
and is used in the treatment
of hypoglycemia. Glucagon acts only on liver glycogen, converting
it to glucose. Glucagon administered through a parenteral route
relaxes smooth muscle
of the stomach, duodenum,
small bowel, and colon.
Pharmacokinetics
Glucagon has been studied following intramuscular, subcutaneous,
and intravenous
administration
in adult volunteers. Administration
of the intravenous
glucagon showed dose
proportionality of the pharmacokinetics between 0.25 and 2.0 mg.
Calculations from a 1 mg
dose showed a small volume
of distribution
(mean, 0.25 L/ kg) and a moderate clearance
(mean, 13.5 mL/ min/ kg). The half- life
was short, ranging from 8 to 18 minutes.
Maximum plasma concentrations
of 7.9 ng/ mL were achieved approximately 20 minutes after subcutaneous
administration (see Figure 1A). With intramuscular
dosing, maximum plasma
concentrations of 6.9 ng/ mL were attained approximately 13 minutes
after dosing. Glucagon is extensively degraded in liver,
kidney, and plasma. Urinary
excretion of intact glucagon
has not been measured.
Pharmacodynamics
In a study of 25 volunteers, a subcutaneous dose of 1 mg
glucagon resulted in
a mean peak glucose
concentration
of 136 mg/ dL 30 minutes after injection
(see Figure 1B). Similarly, following intramuscular injection,
the mean peak glucose
level was 138 mg/ dL, which occurred at 26 minutes after injection.
No difference in maximum
blood glucose concentration
between animal- sourced and rDNA glucagon
was observed after subcutaneous
and intramuscular
injection.
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