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Assessment 03
Pharm - Cholinergic drugs and receptors
88
Pharmacology
Professional
05/10/2010

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Cards

Term
M1 receptor
location
Definition
nerves
Term
M1 receptor
post-receptor mechanism
Definition
IP3, DAG cascade
Term
M2 receptor location
Definition
heart, nerves, smooth muscle
Term
M2 receptor
post-receptor mechanism
Definition
inhibition of cAMP production;
activation of K+ channels
Term
M3 receptor
location
Definition
glands, smooth muscle, endothelium
Term
M3 receptor
post-receptor mechanism
Definition
IP3, DAG cascade
Term
M4 receptor
post-receptor mechanism
Definition
inhibition of cAMP production
(like M2)
Term
M5 receptor
post-receptor mechanism
Definition
Na+, K+ depolarizing ion channel
Term
Botulinus Toxin
Definition
inhibits fusion of ACH vesicles at presynaptic membrane; degradation of VAMPs and SNAPs; clinical uses: facial wrinkles, strabismus, blepharospasm (abnormal movement or twitch of the eye lid), Meige's syndrome, spasmodic toricollis, other muscle spasms
Term
Hemicholinium
Definition
inhibits choline transport into neuron to inhibit ACH synthesis;
rate-limiting step
Term
Tetrodotoxin
Definition
inhibition of nerve impulses at Na+ channels
Term
Triethylcholine
Definition
inhibitor of synthesis, release of ACH;
false neurotransmitter;
Term
Acetylcholine
Definition
no tx uses;
can be used to test for miosis after surgery;
doesn't cross BBB;
small dose will lead to release of NO and decrease of BP;
large dose - direct effect on M2 dec BP, also acts at sympathetic ganglia and adrenal medulla (both N1), at NMJ contraction of skeletal muscle
Term
Bethanechol
Definition
M agonist; no N action!
no effects w/ atropine (complete block);
tx urinary retention and post-op bowel;
Term
Carbachol
Definition
M agonist; some action on N
tx urinary retention and post-op atonic bowel;
Term
Cevimeline
Definition
M agonist; no N actions!
oral admin;
tx [dry mouth] Sjogren's, Mikulicz's, and Sicca syndromes;
effects blocked by atropine;
Term
Methacholine
Definition
M agonist; some N action
DX asthma;
give with atropine to increase BP
Term
Pilocarpine
Definition
M agonist; no N action!
synthetic alkaloid;
tx closed-angle glaucoma, applied topically to increase outflow of aqueous humor
Term
Atropine
Definition
BLOCKS M RECEPTORS;
tx- dec secretions for endotrach tube, acute MI, digitalis toxicity
Term
Benztropine [Mesylate]
Definition
M antagonist;
tx parkinson's
Term
Glycopyrrolate
Definition
M antagonist;
tx dec gastric hypermotility
Term
Ipratropium
Definition
M antagonist;
tx asthma, COPD;
inhaled, won't absorb in GI;
won't cross BBB
Term
Scopolamine
Definition
M antagonist;
tx motion sickness;
lipid soluble, can cross BBB
Term
Trihexphenidyl HCL
Definition
M antagonist;
tx parkinson's
Term
Tropicamide
Definition
M antagonist;
examination of fundus;
shorter duration than atropine;
Term
Darifenacin
Definition
M antagonist
Term
Oxybutynin
Definition
M antagonist;
tx inhibit hyperactive bladder
Term
Solifenacin
Definition
M antagonist
Term
Tolterodine
Definition
M antagonist
Term
Trospium chloride
Definition
M antagonist
Term
Nicotine
Definition
Binds N1 and N2;
increase HR, then decrease (if large dose);
stimulation of skeletal m;
release ADH in CNS (plus others)
Term
Hexamethonium
Definition
N1 antagonist, not used clinically;
won't cross BBB (quat ammonium cpd)
Term
Mecamylamine
Definition
N1 antagonist, used clinically;
crosses BBB;
tx severe HTN, Tourette's Syndrome;
side effects- impotence, CNS effects
Term
Atracurium
Definition
non-depolarizing neuromuscular blocker;
short onset;
spontaneous Hoffman degradation and by plasma choliesterases;
CV effects due to histamine release
Term
D-Tubocurarine
(curare)
Definition
non-depolarizing neuromuscular blocker;
short onset, long duration;
histamine release may cause hypoT;
tx- muscle relax with gen anesthetics, convulsive disorders
Term
Mivacurium
Definition
non-depolarizing neuromuscular blocker;
short onset, short duration;
degraded by pseudocholinesterase
Term
Pancuronium
Definition
non-depolarizing neuromuscular blocker;
short onset, long duration;
tx muscle relaxant for endotrach intubation;
renal/hepatic degradation
Term
Rocuronium
Definition
non-depolarizing neuromuscular blocker;
short onset;
renal/hepatic degradation
Term
Vecuronium
Definition
non-depolarizing neuromuscular blocker;
short onset;
hepatic/renal degradation
Term
Succinylcholine
Definition
depolarizing neuromuscular blocker;
rapid onset, short duration;
histamine release, SA node M receptors and autonomic ganglia fx (=CV effects);
2 phases, first depolarizing activator, second desensitized block
Term
Edrophonium
Definition
reversible anticholinesterase inhbitor; DX MG; rapid onset, short duration; stimulation skeletal m by direct action
Term
Neostigmine
Definition
reversible anticholinesterase inhbitor; dx and tx MG; tx post-op bladder and bowel atony; can reverse non-depol NM blockers
Term
Physostigmine
Definition
reversible anticholinesterase inhbitor; tx glaucoma, atropine O.D., dimentia, and Alzheimer's; crosses BBB, CNS stim then depression
Term
Pyridostigmine
Definition
reversible anticholinesterase inhbitor; tx MG; some direct action on N2; long lasting;
Term
Echothiophate
Definition
irreversible anticholinesterase inhbitor; tx glaucoma; organophosphorous cpd; long duration; can cause cataracts
Term
Malathion
Definition
irreversible anticholinesterase inhbitor
Term
Parathion
Definition
irreversible anticholinesterase inhbitor
Term
Sarin
Definition
irreversible anticholinesterase inhbitor
Term
Tabum
Definition
irreversible anticholinesterase inhbitor
Term
Pralidoxime
Definition
reactivator of acetylcholinesterase; tx O.D. of irreversible anticholinesterase inhbitors
Term
saxitoxin
Definition
inhibition of nerve impulses at Na+ channels
Term
contraindications of M agonists (4)
Definition
asthma;
hyperthyroid - atrial fib;
coronary insufficiency - hypoT;
peptic ulcer dz
Term
Atropine
contraindications
Definition
glaucoma,
HTN,
Alzheimer's
Term
Mecamylamin contraindications (3)
Definition
renal, cerebrovscular, and coronary insufficiency
Term
Vesamicol
Definition
blocks the packaging of ACH into vesicles
Term
M receptors
Definition
stimulated by ACH/muscarine; blocked by atropine;
important locations include SM on blood vessels, and sweat glands
Term
N1 receptors locations
Definition
autonomic ganglion cells
Term
N2 receptor locations
Definition
NMJ and somatic nerves
Term
Diisopropyl flurophosphate (DFP)
Definition
irreversible anticholinesterase
Term
Paraoxon
Definition
irreversible anticholinesterase
Term
Fenthion
Definition
irreversible anticholinesterase
Term
Dimpylate
Definition
irreversible anticholinesterase
Term
Soman
Definition
irreversible anticholinesterase
Term
M actions on eye
Definition
iris sphincter m - contraction
ciliary m - contraction (near vision)
Term
M on SA node
Definition
dec rate (chronotrophy)
Term
M on atria (heart)
3 actions
Definition
dec contractile strength (iontropy)
dec absolute refractory period
inc conduction velocity
Term
M on AV node
Definition
dec conduction velocity (dromotropy)
inc relative refractory period
Term
M on ventricles
Definition
dec (small) in contractile strength
Term
M on blood vessels
Definition
arteries - dilation (NO production);
veins - dilation (NO production)
Term
M on lungs
Definition
bronchial m - contraction
bronchial glands - stim secretion
Term
M on GI tract
Definition
generally, inc motility
sphincters - relaxation
secretion - stimulation
Term
M on urinary bladder
Definition
detrussor - contraction
trigone and sphincter - relaxation
Term
M on glands
Definition
(sweat, salivary, lacrimal, nasopharyngeal)
stim secretion
Term
Ganglionic antagonist on arterioles
Definition
tone: S(A);
vasodilation
Term
Ganglionic antagonist on veins
Definition
tone: S(A);
dilation w/ dec venous return
Term
Ganglionic antagonist on heart
Definition
tone: P(C);
tachycardia
Term
Ganglionic antagonist on iris
Definition
myadriasis
Term
Ganglionic antagonist on ciliary muscle
Definition

cycloplegia

loss of accommodation

Term
Ganglionic antagonist on GI tract
Definition
dec tone and motility;
constapation
Term
Ganglionic antagonist on urinary bladder
Definition
urinary retention
Term
Ganglionic antagonist on salivary gland
Definition
xerostomia
Term
Ganglionic antagonist on sweat gland
Definition
anhidrosis
Term
Sugammadex
Definition
a cyclodextrin derivative that binds the steriodal neuromuscular blocking agent
Term
Halothane
Definition

inhalational anesthetics; curare-like action;

enhance competitive NM blockers

Term
Isoflurane
Definition
inhalational anesthetics;
curare-like action;
enhance competitive NM blockers
Term
Two drugs used in Anticholinesterase O.D.
Definition
Tremethadone
Thiopental
(+ Atropine and Pralidoxime)
Term
Diacetyl monoxime (DAM)
Definition
cholinesterase reactivator
Term
Benzoquinonium
Definition
non-depolarizing and depolarizing NM antagonist!;
also has anticholinesterase activity
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