General pharmacology of nizatidine in animals.
Nizatidine (N-[2-[[[2-[(dimethylamino)methyl-4-thiazolyl]- methyl]thio]ethyl]-N'-methyl-2-nitro-1,1-ethenediamine, LY139037, Axid) is a novel, potent, and selective H2-antagonist. The potential secondary pharmacologic effects of this agent on the cardiovascular, respiratory, gastrointestinal, renal, hepatic, autonomic, and central nervous systems as well as effects on circulating blood glucose and the acute inflammatory response were examined. Nizatidine was generally inactive in the tests conducted in mice, rats, guinea pigs, rabbits, and dogs. Nizatidine and the reference H2-antagonist, cimetidine, both produced effects upon the cardiovascular and respiratory systems by intravenous administration in anesthetized dogs at doses in excess of the intended clinical exposure. In summary, these studies confirm the selective pharmacologic activity of nizatidine and indicate a low potential for secondary pharmacologic side effects to be encountered clinically.
Bemis
K
K
Lilly Research Laboratories, Indianapolis, IN.
Bendele
A
A
Clemens
J
J
Deldar
A
A
Gidda
J
J
Hamelink
J
J
Holland
D
D
Lamishaw
B
B
McGrath
J
J
Shannon
H
H
D000818:Animals; D000927:Anticonvulsants; D001341:Autonomic Nervous System / Q000187:drug effects; D001522:Behavior, Animal / Q000187:drug effects; D001786:Blood Glucose / Q000378:metabolism; D002490:Central Nervous System / Q000187:drug effects; D004064:Digestive System / Q000187:drug effects; D004285:Dogs; D005260:Female; D006168:Guinea Pigs; D006439:Hemodynamics / Q000187:drug effects; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D008111:Liver Function Tests; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D016567:Nizatidine; D011597:Psychomotor Performance / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D012119:Respiration / Q000187:drug effects; D013844:Thiazoles / Q000494:pharmacology*
D000927:Anticonvulsants; D001786:Blood Glucose; D006635:Histamine H2 Antagonists; D013844:Thiazoles; D016567:Nizatidine