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  1. Discuss the types and distribution of cholinergic receptors
    • Nicotinic:
    • N1 – skeletal muscle
    • N2 – ganglionic
    • Muscurinic G-protein linked:
    • M1 – parietal cell, CNS
    • M2 – Cardiac muscle (inhibitory)
    • M3 – Visceral SM (contraction) and Vascular smooth muscle (Relaxation)
  2. Describe muscurinic Ach receptors
    • M1 and M3: Gq linked
    • M2 – Gi linked
  3. Describe synthesis of Acetylcholine (Ach)
    • Made from acetyl CoA and choline in nerve terminals
    • Catalized by choline acetyltransferase
    • Packaged in synaptic vesciles
    • Uptake of choline is rate limiting step
  4. Describe Ach termination
    • By enzyme acetylcholinesterase
    • Splits into Acetate and choline
    • Choline taken up by nerve terminal
  5. Discuss lstructure of Acetylcholinesterase active site
    • Active site has 2 regions
    • - 1. Anionic site binds choline
    • - 2. Esteric site transferes Acetyl group to OH group
  6. Discuss drugs which affect Ach synthesis
    • Hemicholinium: competitively inhibits choline uptake
    • Vesamicol: inhibits packaging of Ach in vesicles
    • Triethycholine: inhibits choline uptake, taken up itself, converted to acetyltriethylcholine, stored as false NT
  7. Discuss drugs which affect Ach release
    • Botulinum toxin:
    • - breaks down SNARE proteins
    • - prevents release of vesicles
  8. Discuss why muscurinic agonists channot be administered. Discuss two exceptions
    • Poor absorption from GI tract
    • Many Side effects
    • Exceptions: Pilocarpine and Carbachol (Bethanachol)
    • Pilocarpine: lowers intra occular pressure, treats glaucoma
    • Carbachol (Bethanacol): Increase GI motility / bladder emptying
  9. Discuss Atropine and its effects on the following body parts:
    • Competetive Ach antagonist
    • Eye: Mydriasis, Cyclopledgia, increase intro occular pressure
    • GI: reduce motility, treats enuresis
    • CV:
    • -- low dose: slows heart rate
    • -- higher dose: speeds heart rate
    • -- Toxic dose: dilates cutaneous blood vessels
    • Secretions: blocks secretions- salivary, sweat glands, lacrimal glands, airways
  10. Discuss the mechanism of actions of anti-cholinesterases
    • Edrophonium: short term
    • Neostigmine: medium duration
    • Isoflurophate: irreversible
  11. Discuss D-tubocurarine
    • Competetive NAchR receptor antagonist at NMJ
    • Relaxes skeletal muscle
    • Motor paralysis
    • Lowers blood pressure
  12. Discuss Succinylcholine
    • Depolarizes membrane
    • Maintains depolarization above threshold
    • Muscle reverts to flaccid state
Card Set:
2011-01-03 18:01:09

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