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80 Cards in this Set

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  • Back
What are the ingredients for making ACh, and what enzyme makes it?
-Choline
-AcCoA
-Choline-Acetyl Transferase
What has to happen first for ACh synthesis? What can inhibit it?
Choline uptake by transporter
Hemocholinium inhibits it
What happens after ACh is made in the presynaptic vesicle? What inhibits this?
-Packing in secretory vesicles
-Vesamicol inhibits the transporter
What stimulates ACh NT release?
Calcium
What inhibits ACh release?
Botulinum toxin
What 2 enzymes break down ACh after its release?
-Tissue Acetylcholinesterase
-Plasma Butyrylcholinesterase (pseudo)
How DON'T we administer ACh? Why?
Parenterally - it would be broken dow instantaneously by the plasma butyrylcholinesterase
What is the first step in Norepinephrine synthesis? What inhibits it?
Uptake of Tyrosine - inhibited by alpha-methyl-tyrosine
What happens to Tyrosine? What inhibits it?
Conversion to DOPA
Inhibited by Metatyrosine
What happens after Dopa is converted to Dopamine? What inhibits this step?
Packaging into vesicles via the transmitter VMAT - Reserpine inhibits VMAT
What stimulates NE release after conversion from Dopamine in the vesicle by Dopamine B-hydroxylase?
Calcium
What inhibits release of the vesicle storage pool of NE?
Guanethidine and Bretylium
What stimulates the NONvesicular cytoplasmic storage pool of NE?
Indirect acting sympathomimetics
-Ephedrine
-Amphetamine
-Tyramine
This is NOT calcium stimulated!
What is the major mechanism for terminating NE's actions after release? What inhibits this?
Active Reuptake by Uptake-1
-Inhibited by Cocaine and TCA's (Imipramine)
What happens to NE after reuptake?
Transport into storage vesicles by another carrier system
What are 2 other ways that catecholamine action is terminated?
-Diffusion away
-Enzyme degradation
What enzymes metabolize catecholamines?
MAO-A/B - oxidative deamination
COMT - methylation
What is the metabolite of COMT breakdown of catecholamines?
VMA
What are 3 major things that modulate the release of NE from sympathetic nerve endings?
-NE itself on autoreceptors (a2)
-Ang II
-Acetylcholine
What effect does Ang II have on SNS release of NE?
Stimulatory
What effect does ACh have on NE release, and by what ACh receptor does this work?
Inhibitory - M1 receptor
What are 2 types of cholinomimetics?
-Direct agonists
-Indirect agonists
Difference btwn Direct and Indirect cholinomimetics?
Direct - mimic ACh
Indirect - inhibit AChesterase
What are the 4 DIRECT cholinomimetics?
-Bethanechol
-Carbachol
-Pilocarpine
-Methacholine
What is Bethanechol's CLINICAL APPLICATION?
Post-op or neurogenic ileus and urinary retention
How does Bethanechol act?
-Bowel and Bladder smooth muscle activation
-RESISTs AChesterase
What is Carbachol's CLINICAL APPLICATION?
-Glaucoma - open/closed angle
-Pupillary contraction
-Release IOP
-Stimulate Sweat/Tears/Saliva
How does Carbachol act?
-Contracts ciliary muscle to treat open angle glaucoma
-Contracts pupillary sphincter to treat narrow angle glaucoma
-Resists ACHesterase
What is Pilocarpine's CLINICAL APPLICATION?
Same as Carbachol!
What is the CLINICAL APPLICATION of Methacholine?
Challenge test for diagnosis of Asthma
How does Methacholine work?
Stimulates muscarinic receptors in airway when inhaled - bronchoconstriction
What are the 5 INDIRECT cholinomimetics?
EPNPE
-Edrophonium
-Pyridostigmine
-Neostigmine
-Physostigmine
-Echothiophate
What is the mechanism of all the indirect cholinomimetics?
Increase endogenous ACh by inhibiting Acetylcholinesterase
Which one does NOT cross the BBB?
Neostigmine
So what is Neostigmine used for clinically?
-Postop and Neurogenic ileus and urinary retention
-Myasthenia gravis
-Postop reversal of NMJ blockade (succinylcholine)
What is Pyridostigmine used for clinically?
Increasing strength in Myasthenia gravis - it does cross into the CNS
What is the CLINICAL APPLICATION of Edrophonium?
Diagnosis of Myasthenia gravis
Why is Edrophonium only used for M. gravis DIAGNOSIS?
Extremely short acting
What is the CLINICAL APPLICATION of Physostigmine?
-Glaucoma
-Atropine overdose
What is the CLINICAL APPLICATION of Echothiophate?
Glaucoma
What are the symptoms of ACholinesterase inhibitor POISONING? (What drugs are known for this?)
DUMBBLESS
-parathion/sarin
-organopesticides
DUMBBLESS
-Diarrhea
-Urination
-Miosis
-Bronchospasm
-Bradycardia
-Lacrimation
-Excitation of CNS/sk muscle
-Salivation
-Sweating
What are the 2 things to give to TREAT ACHe inhibitor overdose?
-Atropine to blockade
-Pralidoxime to reactivate ACHesterase
And what is given to treat an ATROPINE overdose?
Physostigmine
And what is given to reverse NMJ blockade after surgery due to Succinylcholine?
Neostigmine
What are the 5 main ANTICholinergic BLOCKERS?
-Atropine
-Scopalamine
-Ipratropium
-Benztropine
-Methscopalamine, Oxybutin, Glycopyrrolate
What are 2 Atropine analogs?
-Homatropine
-Tropicamide
What is the main organ system Atropine is used for? What does it do?
-Eye
-Reverses miosis to cause mydriasis
-Cycloplegia
And what are the 2 atropine analogs?
Homatropine
Tropicamide
Where does Benztropine act? Application?
CNS - Parkinson's (also Trihexyphenidyl)
Where does Scopolamine act? Application?
CNS - motion sickness
Where does Ipratropium work, application?
-Respiratory
-Asthma/COPD
Where do Methscopolamine, Oxybutin, and Glycopyrrolate work? Application?
-Genitourinary
-REDUCE urgency in mild cystitis, reduce bladder spasms
So what are 5 classes of drugs that treat Glaucoma?
-alpha agonists
-Beta blockers
-Cholinomimetics
-Diuretics
-Prostaglandin
What 2 alpha agonists are used for treating glaucoma and what effect does each have?
Epinephrine - increases Aq humor OUTFLOW

Brimonidine - decreases Aq humor SYNTHESIS
What are 2 side effects and a contraindication to giving EPINEPHRINE for glaucoma?
SE's: burning/stinging

DON'T give in CLOSED angle glaucoma!
What are 3 beta blockers for Glaucoma treatment?
-Timolol
-Betaxolol
-Carteolol
What is the mechanism of the B-blockers for treating Glaucoma?
Decrease Aq humor SECRETION
What cholinomimetics are given for glaucoma?
Pilocarpine (direct)
Echothiophate (indirect)
Physostigmine (indirect)
Carbachol (direct)
What are the 3 things that cholinomimetics do in their mechanism of treating glaucoma?
-Increase Aq humor OUTFLOW
-Contract ciliary muscle
-Open up Trabecular meshwork
What cholinomimetic is given in emergencies? Why?
Pilocarpine - it is VERY effective at opening the canal of schlemm!
What are 2 side effects of the cholinomimetics when given for glaucoma however?
Miosis
Cyclospasm
What diuretic is used for treating glaucoma? What is its mechanism?
ACETAZOLAMIDE
-Decreases Aq humor SECRETION due to decreasing Bicarb
What prostaglandin is used for treating glaucoma? What is it an analog of and what is its mechanism?
Latanoprost
PGF2alpha analog
Increases Aq humor OUTFLOW
What is a side effect of Latanoprost?
It colors the iris dark brown!
So what 3 drugs increase Aqueous humor OUTFLOW?
-Epinephrine
-Cholinomimetics
-Latanoprost
What 3 drugs decrease Aqueous humor SYNTHESIS/SECRETION?
Brimonidine - inhibs synthesis
B-blockers - inhibit secretion
Acetazolamide - inhib secretion
What is Atropine again?
A muscarinic ANTAGONIST
What are 5 organ systems Atropine affects and how?
Eye: mydriasis/cycloplegia
Airway: decreased secretions
Bladder: decreases urgency
Gut: decreases motility
Stomach: decreases acid secretion
So what are the 4 effects of Atropine in a nutshell?
BLOCKS SLUD
-Less salivation
-Less lacrimation
-Less urination
-Less Defecation
What are 5 side effects of Atropine TOXICITY?
-Hot as a hare
-Dry as a bone
-Mad as a hatter
-Red as a beet
-Blind as a bat
What can Atropine cause in elderly?
Acute closed angle glaucoma
What can Atropine cause in men with prostatic hypertrophy?
Urinary retention
What can Atropine cause in infants?
Hyperthermia
What is Hexamethonium?
A NICOTINIC ACh blocker!
What is Hexamethonium NOT to be confused with?
Hemicholinium, the choline uptake blocker
Where are there nicotinic ACh receptors?
-Neuroneuronal in ganglia
-Adrenal medulla
-Skeletal muscle
Where does Hexamethonium work? How?
At the Ganglia - it is a Ganglionic Blocker
What is Hexamethonium used FOR and what does it do?
Experimental models - PREVENTS vagal reflex responses to bp changes
What is a clinical application of Hexamethonium?
Prevents reflex bradycardia when you give things like Norepi to increase blood pressure!