shosh: ANS pharm

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  1. alpha 2 receptors
    • Gi protein
    • Decrease sympathetic outflow
    • Decrease insulin release
  2. Beta 1 receptors
    • Gs protein
    • Increase cardiac contractility and rate
    • Increase renin release
    • Increase lipolysis
  3. M1 receptors
    • Gq protein
    • Found in CNS and enteric nervous system
    • Increase acidity of stomach
  4. Where are D1 and D2 receptors found
    • D1 are found in the renal vasculature
    • D2 are found in the brain
  5. Rate limiting step in acetylcholine synthesis
    Entry of choline into cells
  6. Direct acetylcholine agonists
    • Bethanechol
    • Carbachol
    • Pilocarpine
    • Methacholine
  7. Clinical use of methacholine
    Asthma challenge test
  8. Drug used for post-op reversal of NMJ blockade
  9. Pyridostigmine
    • Acetylcholine esterase inhibitor
    • Does not cross BBB
    • Used to treat myasthenia gravis
  10. Physostigmine
    • Acetylcholine esterase inhibitor
    • Can cross BBB
    • Used to treat glaucoma and atropine overdose (does not reverse neuromuscular blockade of atropine)
  11. Pralidoxime
    Regenerates acetylcholine esterase that has been inactivated by organophosphate toxins
  12. Oxybutinin, glycopyrrolate
    • Muscarinic antagonists
    • Reduces urinary urgency and bladder spasms in patients with cystitis
  13. Methscopolamine, pirensepine, propantheline
    • Anti-muscarinics
    • Used to treat peptic ulcers
  14. Major muscarinic antagonist
  15. Selectivity of epinephrine
    • All sympathetic receptors
    • Low doses are selective for beta 1 receptors
  16. Selectivity of norepinephrine
    • Acts first on alpha receptors, than on beta 1 receptors
    • Does not act on beta 2 receptors
  17. Selectivity of isoproterenolol
    Non-selective antagonist at both beta receptors
  18. Selectivity of phenylephrine
    alpha 1 > alpha 2
  19. Selective beta 2 agonists
    • Albuterol--used for acute asthma
    • Salmeterol--used for asthma prophylaxis
    • Terbutaline--used to inhibit premature uterine contractions
    • (can all act on beta 1 receptors at high doses)
  20. Ritodrine
    • Selective beta 2 agonist
    • Used to reduce premature uterine contractions
    • Unlike the other selective beta 2 agonists, has no effect on beta 1 receptors, even at high doses
  21. Clonidine, alpha methyldopa
    • Central alpha 2 agonists
    • Decrease sympathetic tone
    • Used for hypertension, especially hypertension with renal disease
    • Effects minimized by TCAs
    • Alpha methyldopa is the drug of choice for hypertension in pregnancy
  22. Alpha antagonists
    • Phenoxybenzamine--non-competitive, irreversible inhibition
    • Phentolamine--competitive inhibition
  23. Effect of adding an alpha antagonist after infusing with phenylephrine
    Effects of phenylephrine will be reversed, blood pressure will return to baseline
  24. Effects of adding an alpha antagonist after an infusion of epinephrine
    Vasoconstrictive effects of alpha 1 receptors will be lost, vasodilatory effects of beta 2 receptors will be unopposed, resulting in decreased bood pressure
  25. Effect of NE on blood pressure and heart rate
    • Blood pressure will rise, due to preferential activation of alpha receptors
    • Heart rate will fall, due to reflex bradycardia
  26. Effect of epinephrine on blood pressure and heart rate
    • Blood pressure will stay constant
    • Heart rate will rise due to activation of beta 1 receptors
  27. Effect of isoproterenol on blood pressure and heart rate
    • Blood pressure will fall due to preferential activation of beta receptors
    • Heart rate will rise, due to activation of beta 1 receptors
  28. Non-selective alpha and beta blockers
    • Carvedilol
    • Labetalol
  29. Partial beta agonists
    • Pindolol--non-selective
    • Acebutolol--selective
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shosh: ANS pharm
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