Cholinergic Pharmacolgy II Flashcards
What nicotinic antagonist historically was used extensively for chronic hypertension largely supplanted by adrenergic receptor-selective agents, some limited specific uses in CV regulation?
Hexamethonium
What drug blocks ANS functioning by deducing which branch SNS or PNS exercises dominant control of various organs?
Hexamethonium
What nicotinic antagonist was used for centuries along the amazon and Orinoco rivers to immobilize and paralyze wild animals and cause death from paralysis of skeletal muscle? (Not well absorbed through GI tract so possible to use it for hunting and then eat animal)
Curare
What nicotinic receptor antagonist blocks function at the NMJ, active components of curare extracts, and has a very long duration of action?
D-tubocurarine
What nicotinic antagonist causes motor weakness giving way to total flaccid paralysis, effects small rapidly moving muscles first (eyes, jaws, larynx), then limbs and trunk and then intercostal muscles and diaphragm, after drug removal recovery goes in reverse order?
D-Tubocurarine
What depolarizing blocking agent is essentially to ACh molecules linked together, actively excites receptor but has no way of turning signal off so results in flaccid paralysis, not degraded by AChE but is rapidly degraded by BChE?
Succinylcholine
What drugs can be used in surgery for relaxation of skeletal muscle to facilitate operative manipulations particularly abdominal and short duration blockers for intubation, bronchoscopy, esophagoscopy?
Tubocurarine derivatives and succinylcholine
What drug us used to treat focal dystonia by persistent inhibition of ACh release from neurons supplying skeletal muscle?
Botulinum toxin (Botox)
What is an example of a quaternary alcohol AChE inhibitor that uses electrostatic binding, short lived for 2-10min and used in the diagnoses of MG?
Edrophonium
What are the 3 groups of AChE inhibitors?
Quaternary alcohol, carbamate esters, organophosphates
What are 3 examples of carbamate ester AChE inhibitors that use covalent bonding and are long lived up to 6hr?
Neostigmine, physostigmine, pyridostigmine
What are 3 examples of organophosphate AChE inhibitor, that are extremely stable and can bind as long as 100hrs and are irreversible after aging?
Malathion, parathion, echothiophate
What agent can push and organophosphate AChE inhibitor off the binding cleft before aging?
Pralidoxime
What are some therapeutic uses of AChE inhibitors?
MG, atony or urinary bladder, paralytic ileus, glaucoma, muscarinic antagonist poisoning
What is used to differentiate between MG and cholinergic crisis?
Endrophonium
Skeletal muscle weakness due to depolarization of motor end plate by high concentrations of ACh (ex: ChE inhibitor overdose) describes what?
Cholinergic crisis
If edrophonium causes further weakness then what is the prognosis?
Cholinergic crisis
If edrophonium improves muscle strength than what is the prognosis?
MG
What two drugs can be used to treat MG and increase response to myasthenic muscle to repetitive nerve impulses, preservation of endogenous ACh and step wise increase of dosage to find optimal dosage?
Neostigmine, pyridostigmine
What are 3 possible ways to be exposed to AChE inhibitor toxicity?
Side effect of ChE inhibitor therapy, accidental exposure (insecticide spraying), warfare agents
What are 3 AChE inhibitor warfare agents?
Sarin, Vx, Soman
What warfare agent is volatile and mainly has inhalation exposure?
Sarin
What warfare agent is very persistent can remain on the body, terrain for extended periods of time, mainly has skin exposure but also through inhalation?
Vx
What warfare agent is moderately volatile inhalation or skin contact very rapid “aging” occurs in minutes?
Soman
In general what kind of effects do AChE inhibitors amplify?
PNS
What drug helps alleviate symptoms of AChE inhibitor toxicity by binding reversibly to AChE molecules and releasing them when it’s effects wear off, protects from irreversible binding of nerve gas agents (used extensively as prophylactic agents during 1990-1991 gulf war)?
Pyridostigmine
What are 4 treatments of AChE inhibitor toxicity?
Pyridostigmine, heroic doses of atropine, pralidoxime, artificial respiration and anticonvulsants
What drug is effective for PNS effects induced by nerve gas agents but is ineffective against skeletal muscle neuromuscular effects?
Atropine
What drug will effectively reverse all symptoms by regenerating AChE has been used as prophylactic agent for agricultural workers however must be applied before aging or organophosphate inhibitors?
Pralidoxime
What can be used incase of several AChE inhibitor intoxication?
Artificial respiration and anticonvulsants