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Neuro Cholinergic Pharmacology
Neuro block Spring 2008, Cholinergic Pharmacology
17
Medical
Professional
03/02/2008

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Cards

Term
Bethanechol
Definition
  • Muscarinic Agonist
  • Resistant to AchE, no nicotinic R activity,
  • Use: GI: incr contractile force in smooth muscle (M3), Incr smooth m. contraction in bladder
  • Tox: don't use with an obstruction bc rupture can occur
Term
Pilocarpine
Definition
  • Muscarinic agonist, PNS--contracts ciliary m-->accomodation for near objects, relax suspensory ligs-->convex lens, drain aq. humor, decr intraocular P.
  • res to AchE, lim nicotinic R activity,
  • Use: Xerostomia--facilitates lacrimal and salivary secretions. Narrow angle glaucoma.  Reverses mydriasis from atropine
  • Tox: in athsma incr bronchial constriction/secretion.  Incr acid secretion in peptic ulcer, abd cramps, can't focus on far objects, salivation, sweating.
Term
Carbachol
Definition
  • Muscarinic agonist
  • res to AchE, great activity at Muscarinic R, increases nicotinic R activity
  • Toxicity: blurred vision, dry mouth, constipation, indigestion, Abd pain
Term

Atropine

Definition
  • Muscarinic antagonist--get anti PNS effects
  • plant alkaloid, blocks PNS-like stuff, so blocks Ach action on muscarinic
  • Use: Irrit. bowel syndrome-reduces GI tone and motility, mydriasis, retina exam
  • Tox: mydriasis-->cyclopegia since vision is locked at distance and can't focus close
Term
Scopolamine
Definition
  • Muscarinic antagonist, deriv of atropine
  • Use: motion sickness prophylactically
  • Tox: dry mouth, amnesia
Term
Pirenzepine
Definition
  • Muscarinic antagonist--deriv of atropine
  • has M1 selectivity
  • Use: peptic ulcers, preferred over Atropine bc of selectivity
Term
Ipratropium
Definition
  • Muscarinic antagonist--derived from atropine
  • Use: COPD, athsma caused by cigarette smoke
  • Tox: dry mouth with inhalation
Term
Hexamothonium
Definition
  • Nicotinic antagonist (ganglionic blocking)
  • Use: limited, chronic hypertension, CV regulation
Term
d-Tubocurarine
Definition
  • Non depolarizing drug, competitive nicotinic antagonist (NMJ), competes with Ach for binding at nicotinc R, motor weakness giving way to flaccid paralysis(sm rapid muscles first)
  • Use: immobilize/paralyze wild animals, long duration of action, relaxation of skel m to facilitate operative manipulations (esp abdom)
Term

Succinylcholine

Definition

Depolarization blocker(NMJ)--init opens Ach channels, but bc res to ACh, it lasts longer in clerft-->long depolarization.  Brief repetitive excitation--transient m fasciculations, block NMJ transmission, flaccid paralysis.

Use: office procedures bc reversed quickly, intubation, brochoscopy, esophagoscopy

Term
Botulinum toxin
Definition
  • Ach release blocker
  • Use: focal dystonia in dermatology
Term
Pyridostigmine
Definition
  • Ach Inhibitor
  • MOA: Carbamate ester, covalent, longer lived (6hr)
  • Use: MG-incr response of myasthenic m. to repetitive n. impulses, preserves endog Ach, prophylactic for AChE inhib toxicity
Term
Neostigmine
Definition
  • AChE inhibitor
  • MOA: Carbamate ester, covalent bonds--Hydration step can take 6 hrs, so good for keeping Ach in cleft.
  • Use: MG--incr response of myasthenic m to repetitive n impulses, preserve endogenous ACh, stepwise incr in dose to find optimal
Term
Edrophonium
Definition
  • AchE Inhibitor
  • MOA:4nary alcohol, binds electrostaticly so rapidly diffuses off (2-10 min)
  • Uses: Tensilon test for MG (if muscle strength improves with test then MG diagnosis made)
Term
Physostigmine
Definition
  • AchE inhibitor
  • MOA: Carbamate ester, covalent, long lived (6hr)
  • Use: MG
Term
Malathion, Parathion, Echothiophate
Definition
  • AChE inhibitors
  • organophosphates, Extremely stable, 100s of hours, Aging, irreversible.
  • Tox: too irreversible and can't adjust the dose
Term
Pralidoxime
Definition
  • Regenerator of AchE
  • MOA: can reverse the organophosphate binding, modifies binding and reactivates AChE
  • Use: can be used prophylactically
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