Neostigmine (Prostigmine) -|- Pharmacology Mnemonics - Flash Cards

Neostigmine (Prostigmine)

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Name: Neostigmine (Prostigmine)

Class: Anticholinesterase Agent: Carbamate (Quaternary Amine)

Mech.: Substrate for AChE. Competitive inhib. of interaction btwn ACh and AChE. Stim. postjxnl nicotinic (i.e., muscular) receptors.

Absorption: Oral adequate.

Dist.: No CNS. Acts mostly at neuromusc sites. Some autonomic action.

Metab.: Slowly hydrolyzed by AChE

Excretion, : Slowly hydrolyzed by AChE

Toxicity/S.E.s: Toxic doses first stim. then depress autonomic ganglia, neuromusc. jxns, and central sites. Dose too large ® skeletal muscle weakness = cholinergic crisis. Dose too small ® skeletal muscle weakness = myasthenic weakness. Avoid in cases of asthma, coronary insufficiency, peptic ulcers.

Utility: Treat myasthenia gravis. Treat post-op paralytic ileus and urinary bladder atony. Antag. NM blockade of curare-like agents.

Special Features: IV ® Non-selective. Stim. cholinergic receptors throughout CNS and PNS. Inhib. AChE and BuChE. Musc. effects prevented by pretreatment w/atropine.