Cholinergic Rx

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  1. Methacholine
    • MAChR Agonist:  ^M3
    • Dx of Airway Hyperreactivity:  Methacholine Challenge with low-dose Provocholine
    • No effect on non-asthmatics
  2. Bethanachol
    • MAChR Agonist:  
    • Tx:  ^GI (postop GIatony, Congenital Megacolon), ^Detrusor (postop retention, spinal injury, non-obstructive)
    • Long t1/2:  not a substr for AChE
  3. Pilocarpine
    • MAChR Agonist:
    • Tx:  Glaucoma, Xerostomia (radiation, Sx, Sjogren's)
    • Sides:  Diaphoresis, CNS effects (tertiary amine)
  4. Carbachol
    • NAChR/MAChR Agonist:  <NAChR
    • Tx:  Glaucoma (if pilocarpine uneffective)
    • Long t1/2:  not a substr for AChE
    • Sides:  Ganglionic stim.
  5. Neostigmine
    • AChE Inh:
    • Tx:  ^SM (GIatony, Detrussor atony), Glaucoma, MG, Reverse NMJ blockers
    • Quaternary: no CNS effect
  6. Pyridostigmine
    • AChE Inh:
    • Tx:  most common Tx for MG
    • Longer t1/2 than neostigmine
    • Quaternary:  no CNS effect
  7. Physostigmine
    • AChE Inh:
    • Tx:  Anticholinergic OD (atropine, antipsychotic/depressant)
    • Tertiary:  crosses BBB 
  8. Edrophonium
    • AChE Inh:  
    • Dx of MG:  Tensilon Test
    • Rapid onset, Short Duration
  9. Tacrine (Cognex)
    • Long-Acting AChE-Inh:  (Cognex)
    • Tx:  Alzheimer's
  10. Donepezil (Aricept)
    • Long-Acting AChE-Inh:  (Aricept)
    • Tx:  Alzheimer's
  11. Rivastigmine (Exelon)
    • Long-Acting AChE-Inh:  (Exelon)
    • Tx:  Alzheimer's
  12. Galantamine (Reminyl)
    • Long-Acting AChE-Inh:  (Reminyl)
    • Tx:  Alzheimer's
  13. Echothiophate
    • Irrev. AChE-Inh:  Plates AChE, then "ages" 
    • Tx:  Glaucoma (powerful, persistent miosis)
    • Quaternary: doesn't penetrate skin
  14. OP-toxin
    Irrev. AChE-Inh:  Plates AChE, then "ages"
  15. Pralidoxime (2-PAM)
    • 2-PAM:  reverses Plation of AChE (OP-toxin, Saran)
    • Must be given before "aging"
  16. Atropine
    • Competitive MACh Antagonist:
    • Tx:  Retinal Exam (mydriasis), Resp. (bronchD, dries secretion, but inh mucociliary), Heart (trachy after slight brady, post-MI brady, AV block), IBS, OB
    • Antidote for "Cholinergic Crises":  OP-toxin, Mushroom poison, Saran, excessive stigmine in MG Tx
  17. Scopolamine
    • Competitive MAChR Antagonist:
    • Tx Systemic:  Retinal Exam (mydriasis), Resp. (bronchD, dries secretion), Heart (trachy after slight brady, post-MI brady, AV block), IBS, OB
    • Tx CNS:  Motion sickness, Parkinsonism 
    • Antidote for "Cholinergic Crises":  OP-toxin, Mushroom poison, Saran, excessive stigmine in MG Tx 
    • Sides:  depression, amnesia
  18. Ipratropium (Atrovent)
    • Competitive MAChR Antagonist:  (Atrovent)
    • Tx:  Asthma/COPD
    • Doesn't inh mucociliary clearance
  19. Tiotropium (Spiriva)
    • Competitive M3 Antagonist:  (Spiriva)
    • Tx:  COPD
    • less M2 affinity
    • doesn't inh mucociliary clearance
    • long t1/2:  once-a-day
  20. Pirenzepine
    • Competitive M1 Antagonist:
    • Tx:  Peptic Ulcers (inh M1 of parietal cells & PNS ganglia)
  21. Tolterodine (Detrol)
    • M3 Antagonist:  (Detrol)
    • Tx:  OB
  22. Oxybutynin (Ditropan)
    • M3 Antagonist:  (Ditropan)
    • Tx:  OB
  23. Darifenacin (Enablex)
    • M3 Antagonist:  (Enablex)
    • Tx:  OB
  24. Solifenacin (Vesicare)
    • M3 Antagonist:  (Vesicare)
    • Tx:  OB
  25. Varenicline (Chantix)
    • Partial CNS NAChR Agonist:  (Chantix)
    • Tx:  smoking cessation
  26. Mecamylamine
    • Nn Antagonist:  Gang blocker (PNS & SNS)
    • Tx:  AntiHT (last resort)
  27. d-Tubocurarine
    • Competitive Nm Antagonist:  Paralysis for Sx
    • Sides:  some Nn activity, Histamine release
  28. Doxacurium
    • Competitive Nm Antagonist:  Paralysis for Sx
    • less histamine
    • longer duration of action
  29. Rocuronium
    • Competitive Nm Antagonist:  Paralysis for Sx
    • least potent- high doses
    • Rapid onset
    • little histamine
  30. Atracurium
    • Competitive Nm Antagonist:  Paralysis for Sx
    • little histamine
    • intermediate duration of action
    • No Renal/Hepatic metab:  ideal for kidney/liver disease
  31. Mivacurium
    • Competitive Nm Antagonist:  Paralysis for Sx
    • Short Duration
    • substr for PseudoChE:  beware def.
    • some histamine
  32. Succinylcholine
    • Depolarizing Nm Antagonist:  Paralysis for Sx
    • Very rapid, Very short (substr for PseudoChE, not AChE)
    • Sides:  Hyperkalemia (releases Ca: burns, ^arrhythmia), Myalgia, may stim Nn
    • Malignant Hyperthermia:  in combo w/ anesthetics:  rigidity/heat prod., calcium release from SR
    • Tx:  Dantrolene (inh Ca release from SR) & ice bath
Card Set:
Cholinergic Rx
2012-08-25 15:41:08
Cholinergic Rx

Cholinergic Medications
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