Curare antidote

ACh receptors are destroyed by endocytosis via coated pits and proteolysis in lysosomes. In myasthenia gravis, the receptors are crosslinked by antireceptor antibodies, which facilitate the rate-limiting endocytosis step receptor destmction occurs in less than half the normal time, resulting in net receptor loss. The chronic disease is characterized clinically by such muscular weakness and abnormal fatigue that patients cannot even keep their eyes open. Acetylcholinesterase inhibitors increase the ACh concentration and excitation of the neuromuscular junction, resulting in increased strength and endurance. As expected, AChE inhibitors are also potent curare antidotes because the increased ACh levels displace the blocker more readily. 

The sudden absorption of postoperatively instilled kanamycin from the peritoneal cavity (3-5 g) has resulted in curare-like neuromuscular blockade and respiratory arrest. Calcium gluconate and neostigmine can act as antidotes. 

As antidotes to poisoning from curare and the tricyclic antidepressants As preanesthetic medications As mydriatics As cycloplegics... 

Neostigmine (= 3-Dimethyl-carbamoxyphenyl) trimethylammonium] (quaternary amine aryl carbamate) Synthetic - cf. Physostigmine AChE (carbamoylates - forms carbamoyl ester with active site Serine) [cholinergic, myotic, toxic (curare antidote)]... 

Use Oxidizing agent disinfectant bactericide manufacture of saccharin antidote for poisoning by morphine, curare, and phosphorus. 

Physostigmine has limited medicinal use since it has serious side-effects, and as a result it has only been used in the treatment of glaucoma. However, simpler analogues have been made and have been used in the treatment of myasthenia gravis and as an antidote to curare. These analogues retain the important features mentioned above. Miotine (Fig. 11.51) still has the necessary carbamate, aromatic, and tertiary... 

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