Cholinergic Anticholinergic

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  1. muscarinic in low dose
    ganglionic stim in overdose (CV)
    1st agent used in dentistry
    • Pilocarpine
    • 5-10mg 30 min b4 meal
    • peak 1 hr
    • duration 3-5 hr
    • SE: sweating
    • Contradindication: angle-closure glaucoma, iritis, uncontrolled asthma
  2. mushroom poison
    emesis, diarrhea, urination, cramps salivation, bradycardia, hypotention, bronchospasm, miosis
  3. direct cholinomimetic
    structurally unique
    pharm action similar to pilocarpine
  4. —Increased secretions ¢Watery Saliva
    —Direct cardiac slowing
    —Increased GI propulsive activity
    —Increased micturition (urination)
    —Pupillary constriction
    muscarinics (Parasympathetic agonists)
  5. miosis
    iris sphincter muscle contraction
  6. parasympathetic ocular physiology
    miosis, ciliary muscle contration (near vision), intraocular pressure reduced
  7. What else other than pure parasympathetic actions do muscarinic agonists affect?
    • hypotention: local vasodilation
    • sweating: sympathetic muscarinic receptors
    • metabolic inactivation: not ACHesterase
    • Receptor selectivity
  8. rx for (open-angle) glaucoma
    • pilocarpine
    • carbachol
    • pupil constrict->increased aqueous flow out of anterior chamber-> decrease intraocular pressure
  9. rx for Sjogrens xerostomia
    • cevimeline
    • 30mg TID
    • 1.5 hr peak
    • SE: sweating
    • Contraindications: angle-closure glaucoma, acute iritis, uncontrolled asthma
  10. Reversible AchE Inhibitors
    • ->parasymp actions via increased Ach on muscarinic
    • differences: prolonged, nicotinic activation (skeletal, CNS, symp)
    • Edrophonium: reversible, short
    • Physostigmine: lipid, central acting
    • Neostigmine, pyridostigmine: reversible, slowly hydrolized
    • Donepezil, galatamine, rivastigme: central, Alzheimers, dimentia
  11. Irreversible AchE inhibitors
    • Organophosphates
    • Nerve gas: sarin, tabun
    • Insecticides: malathion, parathion
    • Therapeutic: echotiophate, isoflurophate (glaucoma eyedrops)
  12. AchE inhibitor toxic rxns
    • Muscarinic
    • Ocular: miosis, blurred vision, headache
    • Secretions: lacrimal, salivary, bronchial...
    • Smooth muscle contraction: bronchial, visceral
    • Cardiovascular: bradycardia, hypotension
    • Nicotinic
    • Skeletal muscle: fasciculation, weakness
    • Cardiovascular: tachycardia, blood pressure instability
    • CNS
    • Mixed excitatory and depressant effects
    • Respiratory and circulatory collapse
  13. AchE Inhibitor rx for glaucoma
  14. AchE Inhibitor rx for Alzheimer's
  15. AchE Inhibitor rx for myasthenia gravis
  16. AchE Inhibitor rx for atropine poisoning and central anicholinergic syndrome
  17. AchE Inhibitor rx for paralysis (neuromuscular block)
    edrophonium, neostigmine
  18. muscarinic blocker
  19. organophosphate reversal agent
    • pralidoxime
    • binds to peripheral AchE to displace organophosphates
  20. Which receptor aids erection?
    M2: activates NO-> GTP cGMP vasodilation
  21. PDE5 inhibitor
    • -AFIL
    • phosphodiesterase 5
    • PDE5 degrades cGMP(vasodilates)
    • Siladenafil
    • Vardenafil
    • Tadalafil
    • SE: CYP3A4(erythromicin)
    • potentiates nitroglycerine->profound hypotension
  22. antimuscarinics (antisialogogues)
    • Natural alkaloids (and derivatives)
    • Atropine
    • l-Hyoscyamine (Anaspaz)
    • Scopolamine (Scopace, Transderm-Scop): CNS effects
    • Synthetic quaternary ammonium drugs
    • *Glycopyrrolate (Robinul)
    • Propantheline (Pro-Banthine)
    • Ipratropium (Atrovent)

    *Glycopyrrolate is antisialogogue drug of choice (minimal CV effects)
  23. drugs with anticholinergic effects
    • Sedating Antihistamines
    • e.g., diphenydramine (Benadryl)
    • Tricyclic Antidepressants
    • e.g., amitriptyline (Elavil), doxepin (Sinequan)
    • Antipsychotics
    • e.g, haloperidiol (Haldol), risperidone (Risperdal)
    • Many Others
  24. antimuscarinic for bronchospasm
  25. antimuscarinic for bradycardia
  26. antimuscarinic for meinere's disease and motion sickness
  27. antimuscarinic therapeutics
    • Bronchospasm: ipratropium
    • Bradycardia: atropine
    • GI, GU hyperactivity: numerous antimuscarinics
    • Hyperhydrosis: numerous antimuscarinics
    • Meniere’s disease: scopolamine
    • Motion sickness: scopolamine
    • Ophthalmology: numerous antimuscarinics
    • Parkinson’s disease: several antimuscarinics
    • Anticholinesterase poisoning: atropine
  28. antimuscarinic contraindications
    • —Closed angle (angle-closure) glaucoma
    • —Acute iritis
    • —Obstructive or paralytic GI or GU disease
    • —Myasthenia gravis
  29. antimuscarinic side effects
    • Xerostomia
    • Hyperthermia in children
    • Tachycardia with atropine
    • Sedation/confusion with scopolamine
    • Mydriasis, cycloplegia
Card Set:
Cholinergic Anticholinergic
2013-03-17 05:25:07
Cholinergic Anticholinergic OSD6

Cholinergic Anticholinergic
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