robbypowell's version from 2016-10-09 19:36


Question Answer
Acetylcholine is made from ____ & ______ using the enzyme _______Acetyl Co-A & Choline; choline acetyltransferase (enzyme)
Acetylcholine is stored in vesicles and released via _______ (process)Exocytosis
Acetylcholine is degraded by the enzyme ________Acetylcholine Esterase
of the 3 kinds of receptors that Ach can bind to, _____ receptors are ion channel receptors and release NaNicotinic
of the 3 kinds of receptors that Ach can bind to, _____ receptors are G-protein linkedMuscarinic
Acetycholine can bind to muscarinic, nicotinic, and/or _______ junction receptorsNeuromuscular Junction receptors
T/F: Acetylcholine is released on every ganglion, regardless of whether is is SNS or PNSTrue
T/F: Acetylcholine is only released from PNS ganglia, and not SNS ganglia of the autonomic nervous systemFalse (every ganglia)
Parasympathomimetic agents/agents that mimic Acetylcholine effects are referred to as _______Cholino-MIMETIC
T/F: Cholinomimetic drugs primarily act directly by binding to receptors for AchTrue
T/F: Cholinomimetic drugs primarily act indirectly by increasing the availability of AcetylcholineFalse (Direct; bind to Ach receptors)
3 natural sources of cholinomimeticsPilocarpus (used for eyedrops and to induce salivation), Mushrooms (source of muscarine), and Tobacco
what are the 2 "main" classes of Ach receptors?Muscarinic & Nicotinic
Of the 2 classes of cholinomimetic drugs, ____ ____ are synthetic; examples are Methacholine, carbachol & bethanecholCholine Esters
Of the 2 classes of cholinomimetic drugs, ____ ____ are from plant sources; examples are muscarine, pilocarpine & nicotineNatural Alkaloids
T/F: choline esters and muscarine cannot cross BBB because they are positively charged; therefore, they have no CNS effectTrue (Quaternary NH4/ammonium structure in both choline esters and muscarine)
If you want a cholinomimetic drug to only act peripherally, it must have a _____ ______ structure quaternary NH4 (positive charge stops it from crossing BBB)
of cholinomimetic drugs, Both ______ (orally absorbed) and _____ can cross BBBpilocarpine & nicotine (no quaternary NH4, so can cross BBB)
Choline esters (synthetic cholinomimetics), _____ and ______ all affect muscarinic receptorsPilocarpine & Muscarine
Choline esters (synthetic cholinomimetics), Pilocarpine & Muscarine all affect _______ receptorsMuscarinic
in general Cholinomimetic drugs have the pharmacological effect of _____(inc/dec) parasympathetic functionIncrease SLUD (Salivation, Lacrimation, Urination, Defecation)
Most Anticholinergic drugs act by blocking actions of _______ receptorsMuscarinic (peripheral parasymp)
Muscarine stimulating drugs affect muscarinic receptors and affect vision how? HR how? Vascular smooth muscle how?Miosis & near vision; decrease HR; relaxation of vascular smooth muscle (via endothelial cells)
Muscarine stimulating drugs affect muscarinic receptors and affect secretory exocrine glands how? urinary flow how? Peristalsis how?More exocrine secretion, more urinary flow, more peristalsis
Vasorelaxant effect of Muscarine receptor is initiated by release of _____ from endothelial cells to to muscarine receptor activationNO
Ach binds to ____ (specific receptor) on Endothelial cells, _____ converts to NO, ____ to cGMP, cGMP mediates relaxationM3 receptor; L-arginine; GTP
This Nicotinic receptor is at both SNS and PNS ganglionic sites (pre ganglion)Nn receptor (n for connects to Nerves)
This Nicotinic receptor causes activation at NMJ (skel/voluntary musc)Nm receptor (m for connects to Muscle)
Of the two Nicotinic receptors (Nn and Nm) lower doses are more effective for ____ receptorNm
Acetylcholine is hydrolyzed by both _____ and ____________ (a non-specific enzyme found in plasma in butyryl form)AchE & pseudo-Cholinesterase
Methacholine (Mch) is susceptible to _________ (enzyme) and is only slowly metabolized... creating a longer duration of effectAchE (Acetylcholine Esterase)
________ is susceptible to Acetylcholine Esterase and is SLOWLY metabolized, creating a longer duration of effectMethacholine (Mch)
List 6 adverse effects of Cholinomimetics (including SLUD as one)bronchoconstriction (contraindicated in asthma), hypotension (due to NO release), ulcer, cramps/pain, sweating*, SLUD*
T/F: Anti-cholinesterase drugs primarily act directly by binding to receptors for AchFalse (protect Ach from hydrolysis by AchE)
T/F: Anti-cholinesterase drugs primarily act indirectly by increasing the availability of AcetylcholineTrue
Endrophonium, Neostigmine & Physiostigmine are ______ (reversible/irreversible) anti-ChE'sReversible (Neostigmine does not cross BBB)
Organophosphates (such as Sarin), are mainly seen in insecticides, nerve gases, chemical warfare and have some minor uses in ophthalmology are _____ (reversible/irreversible) anti-ChE'sIrreversible
regarding the mechanism of AchE... At interacts with AchE at 2 sites: ______ binding and _______ sitesCholine binding & Esteratic sites
What 2 AchE inhibitors also have direct action on Cholinergic receptors?neostigmine and pyridostigmine (both reversible Anti-ChE's)
AchE acts by splitting Ach at its _____ bond via hydrolysisEster bond
Organophosphates (eg Sarin) interact with ______ sites on AchE and form a stable attachment, preventing it from interacting with AchEsteratic
Which reversible Anti-AchE interacts reversibly with the Catalytic site of AchE?Endrophonium
Which 2 reversible Anti-AchE's interact reversibly with at both the Choline binding and Esteratic sites?Neostigmine and Physiostigmine
What 2 Anti-AchE's do not cross BBB because of their quaternary NH4 structure?Neostigmine & Endrophonium
T/F: Physostigmine only acts peripherally as an Anti-ChEFalse (Neostigmine and Endrophonium only act peripherally bc quat NH4 won't allow BBB crossing)
T/F: Neostigmine only acts peripherally as an Anti-ChETrue (Neostigmine and Endrophonium only act peripherally bc quat NH4 won't allow BBB crossing)
T/F: Organophosphates (Sarin) are highly lipid soluble and pass BBB for CNS effectsTrue
T/F: Organophosphates (Sarin) are very hydrophilic and do not pass BBB for CNS effectsFalse (Lipophilic, do cross)
What are the 4 Adverse effects of Anti-AchE's on the CNS?Restlessness, Anxiety, Tremors, Death (resp failure)
T/F: The diaphragm is innervated by PNS and excess Anti-Che's or Cholinomimetics can cause death from respiratory failure, due to over contraction of the diaphragmTrue
T/F: The diaphragm is innervated by PNS and excess Anti-Che's or Cholinomimetics can cause death from respiratory failure, due to under contraction of the diaphragmFalse (OVER contraction; the rest is true)
Death from respiratory failure as a result of Anti-ChE's would be a _____ (muscarinic/nicotinic) effectNicotinic
Treatment of acute toxicity with organophosphates: (1) remove from site, (2) Give _____ antagonist, (3) Maintain airways, (4) Give ____ if (step 2) isn't working, (5) Administer ______ antidote to recover ChE enzymeAtropine antagonist; Benzodiazepine; Pralidoxime antidote
Pralidoxime antidote is used as a final step for acute toxicity of what drugs/agents?Organophosphate (irreversible) Anti-ChE's (e.g. Sarin)

what drugs given for these conditions?

Question Answer
Glaucoma (must dec intraocular pressure)Pilocarpine (BBB+ Ch-mimetic), Carbachol (synthetic Ch-mimetic), or Physiostigmine (reversible Anti-ChE) & Pilocarpine (BBB+ Ch-mimetic)
Xerostomia (must increase peripheral PNS function)pilocarpine** (BBB+ Ch-mimetic), neostigmine (reversible Anti-ChE, BBB-) **TEST**
Myasthenia Gravis (autoimmune disease that blocks Ach receptors)endrophonium (anti-ChE), neostigmine (Anti-ChE)
atropine poisoning (atropine poisoning = dec Ach)give Physiostigmine (Anti-ChE)
To reverse NM blockadeNeostigmine (Ach agonist in this function... but class is Ant-ChE)
paralytic ileus and bladder atonyNeostigmine (Anti-ChE) (this occurs after surgery, want to stimulate pt’s GIT and urinary system after surgery)
senile dementia (Alzheimer’s)Tacrine** (Centrally acting Anti-ChE) (we've only seen this associated with Alzheimers)
All Cholinergic agonists stimulate salivation, but _____ is primarily used in dental applications for XerostomiaPilocarpine (Cholinomimetic BBB+)
treating adverse reactions of antimuscarinic IV sedation (using atropine) (aka Atropine poisoning)Physostigmine (Anti-ChE)
Endotracheal intubationsSuccinylcholine (dp NMJ blocker)
Tetanussome NMJ blocker (didn't specify...)
Electroconvulsive therapySuccinylcholine (dp NMJ blocker)

Antimuscarinic drugs

Question Answer
Anti-cholinergics and Anti-muscarinic (synonymous) are also known as ______-like drugsAtropine
What 2 synthetic (not semi-synthetic) Antimucarinic drugs have quaternary ammonium compounds (and thus don't cross BBB)Propantheline** & Methanteline
What 2 synthetic (not semi-synthetic) Antimuscarinic drugs do not have quaternary ammonium compounds ( and thus can cross BBB)benztropine & cyclopentolate
What was the one "semi-synthetic" antimuscarinic drug we were given?Homatropine
______ _____ are a crude plant extract that have Atropine and Scopolamine, and so are used for their Antimuscarinic effectsBelladonna Alkaloids
What is the mechanism of action for Anti-muscarinics?Competitive antagonist of Ach (via M1-M5 receptors)
Anti-muscarinics block/interfere with any response mediated by Acetylcholine except those on _____ receptorsNicotinic
What is the prototype Antimuscarinic drug?Atropine
T/F: Antimuscarinics can have central or peripheral effectsTrue
How do Anti-muscarinics affect pupils?induce Mydriasis (dilated pupils)
How do anti-muscarinics affect Intra-Ocular Pressure?Increase (contra-indicated for Glaucoma)
How do anti-muscarinics affect urinary flow?dec flow, inc retention (prostate hypertrophy contraindication)
T/F: Antimuscarinic drugs at low doses decrease secretion of salivary/sweat/bronchial glandsTrue **TEST**
T/F: Antimuscarinic drugs at low doses increase secretion of salivary/sweat/bronchial glandsFalse **TEST** (decrease)
Antimuscarinic drug of choice for CNS effectsScopolamine
T/F: High dose of atropine = Stimulation, low dose of atropine = sedationTrue **TEST**
T/F: High dose of atropine = Sedation, low dose of atropine = StimulationFalse (reversed)
High dose of Atropine = ________, Low dose of atropine = _________Stimulation; Sedation
Quaternary NH4 Antimuscarinics have greater ______ effects; --> orthostatic hypotension; and greater selectivity for GITGanglionic
_______ (drug) given for gastric ulcers (bc it dec GIT secretions)propantheline (Anti-muscarinic BBB-)
_______ (drug) given for COPD, asthma, etc mainly via inhalation and it causes a localized effectIpatropium (Anti-muscarinic)
Major use of belladonna alkaloids is for Pre-________Anesthesia
Anti-muscarinics are mainly used for ______ toxicity and mushroom poisoningAnti-AchE
Atropine (large dose) good to use for ______ receptor mediated side effects from toxicity, but not for _______ receptor mediated effectsMuscarinic (good for these); Nicotinic (doesn't work on these; NMJ sites)
T/F: Atropine has a good margin of safetyTrue
T/F: Atropine has a narrow margin of safetyFalse
Ophtalmic topical use of atropine is contraindicated in patients with ______Glaucoma
Antimuscarinics can cause urinary retention and lead to _____ hypertrophyProstate
Drug interactions of Anti-Muscarinics: potentiation of anti-muscarinic effects of these 5 types of drugsAntihistamines, Isoniazids, MAOI's, TCA's & Phenothiazines (AIMTP)
Atropine antagonizes bradycardia caused by _____, vagal action of _____ ______ (used for heart failure, arrhythmia)Propranolol; Digitalis Glycosides
What does and Antisialogogue do?dec salivary flow (functional name, not drug class)
_______ and other quarternary NH4 compounds have less CNS effects and are more effective antisialagogues and drugs of choice if CNS effects aren’t desiredGlycopyrrolate

Drugs affecting Nicotinic receptors

Question Answer
Nicotine and DMPP are ________ (polarizing/depolarizing) drugsDepolarizing
Second to caffeine, this drug is one of the most abused substancesNicotine (depolarizing)
T/F: Nicotine is highly lipid solubleTrue (crosses BBB and placenta easily)
The acute lethal dose of nicotine is ____ mg60 mg (1-2 mm of nicotine is delivered per cigarette)
Of non-depolarizing nicotinic drugs with a non-competitive blockade, ______is most common, prototype of non-competitive blockers, quaternary NH4Hexamethonium **Test**
Effects of non-depolarizing Nicotine receptor drugs on EyeMydriasis and Cyclopegia
Effects of non-depolarizing Nicotine receptor drugs on Respiratory tractdec secretion and moderate relaxation
Effects of non-depolarizing Nicotine receptor drugs on Salivary functiondec salivation
Effects of non-depolarizing Nicotine receptor drugs on GITreduced activity and secretion
Effects of non-depolarizing Nicotine receptor drugs on CVSreduced bp
Effects of non-depolarizing Nicotine receptor drugs on urinary flowinc retention
Effects of non-depolarizing Nicotine receptor drugs on sweat glandsdec secretion and warm skin
Effects of non-depolarizing Nicotine receptor drugs on when they have quaternary NH4tremor, convulsion, euphoria(?)

somatic ( Nm receptors))

Question Answer
_____ (depolarizing/non-depolarizing) agents are competitive blockers of Ach at Nm receptors of NMJ endplateNon-depolarizing
List 3 non-depolarizing agents that act on Nm receptorsTubocurarine, Pancuronum (steroid compound) & Gallamine
There is some evidence for Local Anesthetic action of _______, (a non-depolarizing Nm comp blocker), at high dosesTubocurarine
Action of non-depolarizing Nm receptor blocking drugs leads to _____ _____ of skeletal muscle, most have a large margin of safetyFlaccid Paralysis
What is a commonly used Depolarizing Nm Blocking agent?Succinylcholine
NMJ blockers don't have major autonomic effects except for ____ & ____ which inc HR, and _____ which dec HRPancuronium & Gallamine (non-dp NMJ blockers); Succinylcholine (dp NMJ blocker)
_____ is the NMJ blocker associated with Histamine releaseTubocurarine (non-dp NMJ blocker)
_______ administration can cause Fasciculation (painful spasms)Succinylcholine (dp NMJ blocker)
T/F: there are additive effects when non-dp NMJ blockers are given togetherTrue
____ is another agent, that acts within skeletal muscle fiber at SR → dec Ca release and interferes with contraction **TEST**Dantroline

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