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42 Cards in this Set

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  • Back
Parasympathetic Stimulation causes ...
*Constrict pupil
*Stimulates salivation
*Inhibits heart
*Constricts bronchi
*Stimulates digestive activity
*Stimulates gallbladder
*Contracts bladder
*Relaxes rectum

"Rest and digest" activities
Sympathetic Stimulation causes ...
*Dilates pupil
*Inhibits salivation
*Relaxes brochi
*Accelerates heart
*Inhibits digestive activing
*Stimulates glucose release (in liver)
*Secretion of EP and NE by kidney
*Relaxes bladder
*Contracts rectum

"Fight or flight" activites
Muscarinic Cholinoreceptors
*Smooth muscle
*Cardiac muscle
*Exocrine glands
Nicotinic Cholinoreceptors
*Ganglia
*Skeletal muscle
Alpha1 Adrenoreceptors
*Smooth muscle control
(Vascular, GI, etc)
Alpha2 Adrenoreceptors
*Adrenergic nerve terminals
*Smooth muscle (veins)
Beta1 Adrenoreceptors
*Heart
Beta2 Adrenoreceptors
*Smooth muscle (most)
Dopamine Receptor
*Renal vascular beds
Catecholamine biosynthesis
Tyrosine ---(Tyrosine hydroxylase)---> Dopa

Dopa ---(Dopa decarboxylase)---> Dopamine

Dopamine ---(Dopamine beta-hydroxylase)---> Norepinephrine

****************************
Norepinephrine ---(PNMT)---> Epinephrine

PNMT = phenylethanolamin-N-methyltransferase,
Found in some adrenergic nerves in brains, also in adrenal medulla
Acetylcholine
*Muscarinic Agonist
*Positively charged (difficulty crossing membranes)
*Rapidly degraded
*Non-specific (between N and M)
Methacholine
*Synthetic ACh derivative
*Has an added methyl group
*Decreased hydrolysis by acetylcholinesterase (still can be)
*Shift of balance towards M receptor over N
Carbachol and Bethenechol
*Synthetic ACh derivative
*Resistant to degradation by AChE

*Carbachol - replace the ester with a carbamoyl
-Has good N receptor activity, still activates M

*Bethanechol - replace ester with carbamoyl and add methyl
Muscarine and Pilocarpine
*Selective for M receptors
*Naturally occurring

*Not a substrate for AChE
Cevimeline
*Newer drug
*Very selective for M receptors
*M3 selectivity
Diagnosis for asthma
*Methacholine is a brochoconstrictor

*In asthma, hyperreactive airways will respond to a low dose of methacholine to cause bronchoconstriction

*In healthy airways a higher dose would be needed to illicit the same response
Diagnosis for CAD/endothelial malfunction
*Injected ACh

*In normal/healthy arteries it will cause vasodilation

*In CAD/endothelial malfunction is will stimulate M receptors on vascular smooth muscle to produce vasospasm
Urinary Retention treatment
Bethenachol (Muscarinic agonist)

*Stimulates M receptors to cause contraction of the detrusor muscle to induce bladder emptying
Xerostomia
Pilocarpine and Cevimeline (muscarinic agonists)

*Stimulate salivation as long as there is function tissue remaining

**this condition is caused by radiation treatment or autoimmune disease (Sjorgen's syndrome)
Glaucoma
*Muscarinic agonists induce contraction of smooth muscle in the eye (ciliary/circular) to improve drainage of aqueous humor

*AChE inhibitors increase ACh which binds receptors to stimulate contraction of of circular,/ciliary smooth muscle to incrase drainage
-Physostigmine
Contraindications for muscarinic agonists
*Asthma (will cause bronchospasm)

*Peptic ulcer disease (will increase secretions)

*Heart disease (will cause vasospasm, bradycardia, decreased force of contraction/contractility)
Cholinoreceptor Stimulants
*Direct-acting drugs:
-Muscarinic agonists
-Alkaloids and choline esters

*Indirect-acting drugs
-increase ACh by decreasing AChE
-reversible/irreversible
-available ACh can stimulate nicotinic receptors as well as muscarinic receptors
Physostigmine
Pyridostigmine
Neostigmine
*Reversible AChE inhibitor

*Physostigmine easily enters the CNS, the others are positively charged

*Intermediate DOA

*Metabolized by AChE (like ACh) but at a much slower rate, while they are being metabolized AChE can't be
Edrophonium
*Reversible AChE inhibitor

*Short acting

*Binds to the active site of AChE to compete with ACh for binding sites
Organophosphates
*Irreversible AChE inhibitor

*Phosphorylates the enzyme via an irreversible covalent bond that is difficult to break and strengthens over time

**Echotiophate, Isoflurophate are also irreversible inhibitors
Pralidoxime
*Strong nucleophile, attacks phosphate bond

*Antidote to organophosphates via breaking phosphate bond

*Must be given shortly after exposure, before aging strengthens bond

*Doesn't get into the brain very easily so it won't reverse CNS effects
Myasthenia gravis
*Autoimmune disease that targets N receptors

*AChE inhibitors will improve symptoms but won't cure the disease

*Neostigmine, pyridostigmine will increase the ACh --> increase probability the ACh will find a receptor before being degraded

*If drug dose is too high the high concentrations of ACh will desensitize the receptors
Alzheimer's disease
*Caused by decrease cholinergic transmission

*AChE inhibitors (Cognex, Aricept) are more selective for AChE in the brain
Chemical warfare (AChE inhibitors) Adverse effects
*Eye: blurry vision, miosis, tearing

*Salivary glands: increased secretion, drooling

*Heart: hypotension, decreased heart rate, bradycardia

*Lung: bronchconstriction

*GI: increased secretion, N/V, diarrhea, inreased motility

*Bladder: urination

*Skin: sweating
Atropine
"Classic" M receptor antagonist, reversible competitor

To overcome the effects, must increase the concentration of agonist (ACh)
Quarternary Amines
*Muscarinic receptor antagonist

*Limitations: poorly absorbed orally, limited access to CNS

*Propantheline
*Ipratropium (Atrovent)
*Tiotropium (Spiriva)
*Trospium (Sanctura)
Tertiary Amines
*Tropicamide
*Dicyclomide
*Oxybutinin (Ditropan XL)
*Tolteridine (Detrol LA)
Atropine
*Treat post-MI bradycardia by stimulating the vagus nerve

*Used pre-op to decrease secretions

*Used to reverse the effects (symptoms) of AChE inhibitors such as organophosphates ONLY TREAT THE SYMPTOMS
Lomotil (diphenoxylate + atropine)
*Treats diarrhea

*Diphenoxylate is the active ingredient - opiate that stimulates opioid receptors in the GI to decrease motility

*Atropine prevents abuse of the opiate
Scopalamine
Belladona alkaloid like atropine

*Transdermal patch for motion sickness

Used for its effects on the BRAIN not its effects on the periphery
Tropicamide
*Tertiary amine

*Used as an eye drop for eye exams

Short-acting pupil dilator

NOT given to glaucoma patients because or the increase in intraocular pressure that may cause an acute attack
Dicyclomide, Propantheline
Dicyclomide = Tertiary amine
Propantheline = quaternary amine

Used for hypermotility syndromes to decrease secretions and motility for symptomatic relief
Oxybutinin, Tolteridine, Trospium
Oxybutinin/Tolteridine = tertiary amines
Trospium = quaternary amine

Used for overactive bladder/incontenence

Newer agents specifically target M3 receptor in bladder
Ipratropium, Tiotropium
Quaternary amines

Used in lungs for COPD/Asthma

Because of positive charge the drug remains topical and is not systemically absorbed

Blocks the effects of ACh released by the vagus nerve thereby inhibiting bronchoconstriction

Only improves bronchoconstriction due to ACh release, not due to other mediators (inflammatory)
Anticholinergic Side Effects!!!!
Visual - cyclopegia (blurred vision), mydriasis (dilated pupil), dry eyes

Xerostomia

Constipation (decreased motility)

Urinary retention

Drowsiness (CNS EFFECTS, all others are ANS)

Tachycardia
Anticholinergic Contraindications
Glaucoma
Heart Disease
BPH
Varenicline
Partial nicotinic receptor agonist

Won't fully open the ligand-gated ion channel

Selective for the alpha-4-beta-2 nicotinic receptor in the mesolimbic area of the brain that mediates dopamine release

Binds to ligand site on the receptor/channel and prevents nicotine from binding

Adverse effects: nausea, constipation, dry mouth
Agitation, hostility, depressed mood, suicidal thoughts