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PharmFour

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lunalovegood's version from 2016-10-10 23:53

Section

Acetylcholine Receptor Agonists --- Cholinomimetics --- Acetylmimetics --- Parasympamimetics --- Cholinergic Agonist
Question Answer
Muscarinepasses BBB (but quat!)
Pilocarpinepasses BBB
Nicotine passes BBB
Methacholineno pass
Bethancholno pass (quat)
Carbacholno pass (quat)
Neostigmineno pass (quat)
Edrophoniumno pass (quat)
Physostigminepasses BBB
Pyridostigmineno pass (quat)
Organophosphatespasses BBB
Tacrinepasses BBB
Propanthelineno pass (quat)
Methantelineno pass (quat)
Atropinepasses BBB
Scopolaminepasses BBB
Benztropinepasses BBB
Cyclopentolatepasses BBB
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Big Picture
Question Answer
Muscarine, Pilocarpine, Nicotine, Methacholine, Bethanechol, CarbacholCholinomimetics
Neostigmine, Edrophonium, Physostigmine, Pyridostigmine, Organophosphates, TacrineAnti-AchE
Succinylcholinedepolarizing NMJ blocker (muscle relaxer)
Tubocurarine, Pancuronium, Gallaminenon-depolarizing NMJ blockers (Nm) (muscle relaxers)
Atropine, Scopolamine, Propantheline, Methanteline, Ipatropium, Benztropine, Cyclopentolate, HomotropineAntimuscarinic
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Muscarinic &AND& Nicotinic
Question Answer
Carbacholyes
Bethanecholno (muscarinic)
Pilocarpineno (M3)
Muscarineno (muscarinic)
Nicotineno (nicotinic)
Methacholineno (M1-M5 and not really nicotinic)
Neostigmineyes (indirect)
Edrophoniumyes (indirect)
Physostigmineyes (indirect)
Pyridostigmineyes (indirect)
Antimuscarinicsno (M1-M5)
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M1-M5 Muscarinic Receptors
Question Answer
M1Gq (IP3 DAG --> Ca2+) (brain + autonomic ganglia)
M2Gi (decrease cAMP) (peripheral autonomic)
M3Gq (IP3 DAG ---> Ca2+) (peripheral autonomic)
M4Gi (decrease cAMP) (brain + autonomic ganglia)
M5Gq (IP3 DAG ---> Ca2+)
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Does acetylcholinesterase break it down?
Question Answer
Acetylcholineyes
Methacholineyes (but it's pretty resistant)
Muscarineno (potential toxicity)
Bethancholno
Carbacholnot easily
Nicotineno
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What can cause this? (acetylmimetics and Anti-AchE are pretty much the same)
Question Answer
Miosisacetylmimetics (CONSTRICT PUPIL)
Increase aqueous humor outflowacetylmimetics
Blurred visionacetylmimetics
Increased salivaacetylmimetics
Increased sweatingacetylmimetics
Lacrimationacetylmimetics
Bronchoconstrictionacetylmimetics
Bronchial secretionsacetylmimetics
Bradycardiaacetylmimetics
Abdominal crampingacetylmimetics
Increased gastric acid secretionacetylmimetics (bad for ulcer!)
Diarrhea acetylmimetics
Polyuriaacetylmimetics
Hypotensionacetylmimetics
Vasodilationacetylmimetics
Reduce intraoccular pressureacetylmimetics
Relax ciliary muscle acetylmimetics (but iris SPHINCTER contracts)
Relax vascular smooth muscleacetylmimetics (via endothelial release of NO --> Ach + M3)
Tremorsacetylmimetics
Mydriasisantimuscarinics
Increase intraoccular pressureantimuscarinics
Decrease urine flowantimuscarinics (no good for prostate hypertrophy)
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Separate things
Question Answer
Treats glaucomaCarbachol, Physostigmine, Pilocarpine
Administered topically on eyeCarbachol
Treats xerostomia****Pilocarpine, Neostigmine ***
Treats non-obstructed GI motility needsBethanechol, Physostigmine
Treats urinary retentionBethanechol
Treat Myasthenia GravisNeostigmine (& pyridostigmine)
Reverse NM cascadeNeostigmine
Post-surgery - get the GI and bladder going againNeostigmine
Can diagnose bronchial hyperreactivityMethacholine
Contraindicated in uncontrolled HTN or recent MIMethacholine
2 Nicotinic receptors -- which is responsive to lower dose?Nm
AchEsterase INHIBITORS THAT ALSO ACT DIRECTLY ON CHOLINERGIC RECEPTORSNeostigmine & pyridostigmine
AchEsterase INHIBITORS THAT INTERACT WITH BOTH CHOLINE & ESTERATIC SITESNeostigmine & Physiostigmine
Tensilon testEdrophonium (can diagnose Myasthenia Gravis)
Senile dementia (Alzheimer's)Tacrine
Endotracheal intubationssuccinylcholine
Electroconvuslive therapysuccinylcholine
T/F - ANTIMUSCARINICS AT LOW DOSES --- REDUCE SALIVA, SWEAT, and BRONCHIAL SECRETIONSTRUE
LOW DOSE OF ATROPINE IS...sedation
HIGH DOSE OF ATROPINE IS ...stimulation
Treats gastric ulcersPropantheline
Treats asthma/COPDIpatropium
Atropine has a good margin of safety?Yes
AntisialagogueGlycopyrrolate (Atropine and Scopolamine too)
Antihistamines, Isoniazids, MAOIs, TCA's, Phenothiazines -- DO NOT WORK WELL WITH ...antimuscarinics
Acute lethal dose of nicotine60mg (1 cigarette is 1-2mg)
-Bronchial, GI, and sweat gland secretions reduced- , lower BP, lower saliva, increased urine retention, mydriasis and cycloplegianon-depolarizing Nicotine receptor drugs
Prototype non-depolarizing, non-competitive blockersHexamethonium *********
Depolarizing Nm blocking agentsuccinylcholine
Inhibits Ca2+ release from sarcoplasmic reticulum - treats malignant hyperthermiaDantrolene *** (for example, malignant hyperthermia caused by succinylcholine)
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Antidotes
Question Answer
Muscarine's antidoteatropine
Atropine's antidotephysostigmine (atropine = belladonna -- atropine poisoning makes pupils dilate, which was considered beautiful, hence the term -bella-donna-)
Organophosphate's antidote#1 Atropine #2 BDZ #3 Pralidoxime
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Reversible or no?
Question Answer
Edrophoniumreversible
Neostigminereversible
Physiostigminereversible
OrganophosphatesNO! (irreversible acetylcholinesterase inhibitor)
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