Exam -2 Cholinergic and Adrenergic drugs Flashcards
What is the drug that targets the antiporter enzyme for Acetylcholine? What deficit does it cause?
Vesamicol: it results in a deficit of Ach storage and subsequent release.
What does Hexamethonium do?
Selective blockade of the modulatory presynaptic cholinergic receptors by antagonism. It prevents facilitation and causes rapid tetanic fade to occur in muscles.
Atropine
Antimuscarinic agent. Can be use to block vagal slowing of the sinoatrial node, and hece in relative tachycardia occurs.
Methacholine
It is a muscarinic receptor agonist.
This drug attaches to M-1 muscarinic receptors (located in autonomic ganglia) with higer affinity than M-2 and M-3 receptors (located in parasympathetic end organs).
What’s the drug? and what’s the outcome?
Pirenzepine
The drug’s predominant effect at clinically used does is ganglionic blockae.
What drug we will use in the case of an anticholinergic overdose?
what kind of property makes it a good drug?
Physostigmine, it is a lipophilic agent which has excellent CNS penetration.
What kind of drug is Hemicholinium-3?
ACh inhibitor, this drug is used in research setting.
Blocks the high affinity transporter for choline and thus prevents the uptake of choline required for ACh sysntehsis.
This drug degraded SNAP-25and thus prevent synaptic vesicle fusion with the axon terminal (presynaptic) membrane.
Botulinum Toxin A. Made by Clostridium Botulinum.
Which AChE inhibitor has a direct action, and activates nAChRs at the neuromuscular junction?
Neostigmine
What drug is an AChE inhibitor that binds rapidly (2-10 min) , resulting in a complete rapid and reversible block?
Edrophonium. Often used clinically to diagnosed Myasthenia Gravis.
Properties of Diisopropyl Fluorophosphate , and Isoflurophate?
Possible drug administer to reverse effect?
It is an organophosphate. These irreversible bind to AChE, and act as an inhibitor (this is due to Aging) New AChE molecules need to be synthesize in order to restore activity. f
Pralidoxime is administered before aging has occurred, it is possible to recover enzymatic function from the inhibited AChE.
Tubocurare?
What can be used to improve conditions that mimic this drug?
Anticholinergic drug, cause weakness or paralysis by acting as competitive antagonist at the nAChR, preventing ACh from binding to the receptor and causing nondepolarizing blockade of cholinergic transmission.
An AChE inhibitor in order to increase ACh, that would be Physostigmine.
If we give a patient Edrophonium and muscle weakness decreases even further, what can we deduce? what drug must be in action?
It means that there is an agonist of AChR, there is a depolarizing blockade. The receptors are being stimulated so much, the go into blockade, the drug that can cause this is succinylcholine.
What are the drug indicated for the treatment of mild and moderate Alzheimer’s disease (AD)?
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Donepezil
Tacrine
Rivastigmine
Galantamine
These are AChE inhibitors
What drug is indicated to treat AD and Parkinson’s disease?
Rivastigmine is a pseudo-irreversible cholinesterase inhibitor.
Muscarinic recptor agonist?
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Pilocarpine Bethanechol Muscarine Carbachol Acetylcholine Methacholine
What drug is used for diagnosis of asthma?
Methacoline: the bronchial hyperreactivity that is characteristic of asthma causes an exaggeraed bronchoconstriciton response to parasympathomimetics.
