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
Neostigmine Pharmacology, Pharmacokinetics, Studies, Metabolism - Neostigmine Methylsulfate (injection)
Neostigmine Pharmacology, Pharmacokinetics, Studies, Metabolism - Neostigmine Methylsulfate (injection)
CLINICAL PHARMACOLOGY
Neostigmine inhibits the hydrolysis of acetylcholine by competing with
acetylcholine for attachment to acetylcholinesterase at sites of cholinergic
transmission. It enhances cholinergic action by facilitating the transmission
of impulses across neuromuscular junctions. It also has a direct cholinomimetic
effect on skeletal muscle and possibly on autonomic ganglion cells and
neurons of the central nervous system (CNS). Neostigmine undergoes hydrolysis
by cholinesterase and is also metabolized by microsomal enzymes in the
liver. Protein binding to human serum albumin ranges from 15 to 25%.
Following IM administration, neostigmine is rapidly absorbed and eliminated.
In a study of five patients with myasthenia gravis, peak plasma levels
were observed at 30 minutes, and the half-life ranged from 51 to 90 minutes.
Approximately 80% of the drug was eliminated in urine within 24 hours;
approximately 50% as the unchanged drug, and 30% as metabo-lites. Following
IV administration, plasma halflife ranges from 47 to 60 minutes have been
reported with a mean half-life of 53 minutes.
The clinical effects of neostigmine usually begin within 20 to 30 minutes
after IM injection and last from 2.5 to 4 hours.
top
