Pharmacology Lecture 8_Cholinergic Pharm Flashcards
Which muscarinic receptors are coupled to a Gi proteins
M2, M4
Ipratropium and Tiotropium are used to do what
Treat COPD through broncodilation
Benztropine, Trihexphenidyl are used to treat what
parkinsons
How do ACh direct agonists work
ACh direct agonists bind to receptors and induce the same response as ACh
What does a Gq coupled receptor do?
It activates the IP3 pathway and increases cytosol levels of Ca
What are the clinical uses of muscarinic antagonists
They can be used to treat muscarinic poisening, motion sickness, parkinson’s disease, dialate pupiles, treat COPD, and over active bladder. They can also be used to reverse bradycardia
What functional group caused Muscarinic preference
methyl (CH3)
What are the 7 effects that cholinergic medication can have?
Salivation, lacrimation, urination, defication, diaphoresis (sweating), Bradycardia (slowed heart rate), and miosis (constriction of the pupil)
What can indirect acting elements be used to treat
Myasthenia gravis, postoperative ileus, reversal of neuromuscular blockage, treatment of lyse (pediculosis capitis), glaucoma, and urinary tract motility
What triggers the release of neuro transmitters from a neuron?
An action potential propigates down an axon until it reaches the buton. The buton contains voltage gated Ca and Na channels that open when the neuron is depolarized. The Ca binds to the vesicals of neuro transmiter and cause them to bind to the cell membrans and release their contents in to the synaptic cleft.
How do ACh indirect agonists work
ACh indirect agonists inhibit ACh esterase which keeps ACh in the synaptic cleft longer and triggers a bigger response
What are Edrophonium, Neostigmine, Pyridostigmine, Ambenonium Physostigmine?
the 5 important indirect acting elements
What is a muscarinic receptor
It is a cholinergic G-coupled receptor
What are Methacholine, Carbachol, Bethanechol
Ester cholinergic drugs
How do tertiary amines and quaternary amines differ?
Tertiary amines are uncharged and can be absorbed into the CNS. Quarternary amines are charged an do not distribute to the CNS. Quarternary amines are better for targeting the PNS
What does a Gi coupled receptor do?
it is inhibitory and down regulates adenylyl cyclase
What can direct acting cholinergic agents be used to treat
Glaucoma, Urinary tract motility, xerostomia, (can also cause sweating)
What receptor type is targeted by Methacholine Chloride. Is it susseptiable to Cholinesterase?
It targets Muscarinic receptors. It is slightly suseptable to cholinesterase.
Darifenacin and Solifenacin are used to treat what
bladder incontenance
Tropicamide is used to do what
dialate pupils
What receptor type is targeted by Carbchol Chloride. Is it susseptiable to Cholinesterase?
It targets Nicotinic receptors. It is not succeptable to cholinesterase
What is sclopolamine and what is it used to treat
It is an antimuscarininc durg (muscarinic antagonist) and it is often used to treat motion sickness and excessive salivation
What are the important direct acting elements
Acetylcholine, Methancholine, Carbachol, Bethanechol, Pilocarpine, Nicotine, Muscarine
Which muscarinic receptors are coupled to a Gq protein
M1, M3, M5
What receptor type is targeted by Bethanochol chloride. Is it susseptiable to Cholinesterase?
It targets Muscarinic receptors. It is not suseptable to cholinesterase.
What is a Nicotinic receptor
It is a cholinergic ion channel
What are two major uses of atropine
it reverses organophosphate poisoning and can be used to reverse bradycardia.
How can anti muscarinic drugs improve COPD?
the para sympathetic NS causes broncoconstriction. By inhibiting Para NS the Sym NS can take over.
