We studied the effects of glycopyrrolate on oral mucous host defenses. Sing
le IV doses of glycopyrrolate (4 mu g/ kg) or placebo were administered to
12 healthy volunteers in a randomized, double-blinded, cross-over study. Sa
livary flow rates and the concentrations/ activities of total protein, amyl
ase, and nonimmunologic (lysozyme, lactoferrin, myeloperoxidase, total sali
vary peroxidase, and thiocyanate) and immunologic (total immunoglobulin A,
immunoglobulin G, and immunoglobulin M) mucous host defense factors were de
termined for paraffin-stimulated whole saliva before and 1, 3, 6, 12, 24, a
nd 48 h after drug administration. Glycopyrrolate serum concentrations were
determined before and 2, 4, 6, 10, 15, and 30 min and 1, 2, 3, 6, 12, and
24 h after IV drug injection. Salivary flow rates were decreased significan
tly for 12 h after glycopyrrolate injection, compared with saline injection
. The concentrations of immunologic and nonimmunologic defense factors were
increased in the glycopyrrolate group, and differences between the groups
were found for all factors (P < 0.05-0.001) except lysozyme and total saliv
ary peroxidase. In contrast, because of the reduced flow rate, the output o
f all defense factors into the saliva was decreased after glycopyrrolate in
jection, compared with saline injection. Glycopyrrolate thus decreases the
output of salivary host defense factors into the oral cavity.