Pharmacology

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Author:
jknell
ID:
113249
Filename:
Pharmacology
Updated:
2011-10-30 19:53:30
Tags:
Cholinergic
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Description:
Cholinergic Drug lists
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  1. Botulinum toxin (botox)
    Mechanism: Inhibits exocytosis of ACh

    Indications: (cervical sytonia, strabismus, blepharospasm, spasticity, glabellar frown lines) (lower esophageal spasms) (hyperhidrosis)

    Adverse Effects: Injection site reaction, weakness of injected muscle and adjacent muscles

    Other: lasts 3-4 months
  2. Nicotine
    nAChR agonist

    Mechanism: stimulates nAChRs

    Indications: drug of abuse

    Adverse Effects: increase BP, HR, CNS effects
  3. NM-selective antagonists
    • 1. D-tubocurarine
    • 2. Succinylcholine
  4. D-tubocurarine
    Mechanism: blocks NM receptors at NMJ (SKM paralysis)

    Indications: during surgery (SKM relaxation)

    Adverse Effects: produces significant NN blockade, allergic reactions (histamine release)

    Other: paralysis produced by competitive agents and can be reversed by anti-ChE, seldom used clinically
  5. Succinylcholine
    Mechanism: NM receptor agonist, but produces persistent depolarization --> SKM paralysis

    Indications: surgery (SKM relaxation)

    Other: rapidly hydrolyzed by BuChE (short duration of action)
  6. NN-selective antagonists
    (no names)
    Competitive and non-competitive

    Adverse Effects: postural hypotension, constipation, urinary retention, xerostomia

    Other: formerly used to tx HTN
  7. mAChR agonsists
    • 1. Choline Esters (bethanechol)
    • 2. Natural (muscarine)
    • 3. Alkaloids (Pilocarpine)
  8. Bethanechol (choline ester)
    Mechanism: stimulate mAChRs

    Indications: postoperative ileus, urinary retention

    Adverse Effects: GI side effects (cramps, diarrhea, nausea), diaphoresis, hypersalivation, lacrimation
  9. Pilocarpine
    Mechanism: stimulate mAChR

    Indications: Xerostomia due to damage to salivary glands, glaucoma

    Adverse Effects: Adverse Effects: GI side effects (cramps, diarrhea, nausea), diaphoresis, hypersalivation, lacrimation
  10. mAChR antagonists
    • 1. Atropine
    • 2. Scopolamine
    • 3. Oxybutynin
    • 4. Tolterodine
    • 5. Ipratropium
  11. Atropine
    Mechanism: blocks mAChRs

    Indications: bradycardia, AV block

    Side Effects: xerostomia, constipation, urinary retention, confusion
  12. Scopolamine
    Mechanism: block mAChRs

    Indications: motion sickness

    Side Effects: xerostomia, constipation, urinary retention, confusion

    Other: prominant CNS effects
  13. Oxybutynin/Tolterodine
    Mechanism: block mAChRs

    Indications: overactive bladder, enuresis, neurogenic bladder

    Side Effects: xerostomia, constipation, urinary retention, confusion
  14. Ipratropium
    Mechanism: block mAChRs

    Indications: COPD

    Side Effects: xerostomia, constipation, urinary retention, confusion
  15. anti-AChEs
    • 1. noncovalent (Donepezil)
    • 2. Carbamoylating (Physostigmine)
    • 3. Phosphorylating (Echothiophate, Malathion)
  16. Donepezil
    Mechanism: interacts noncovalently with active site of AChE

    Indications: Alzheimer's

    Side Effects: GI (cramps, diarrhea, nausea), diaphoresis, hypersalivation, lacrimation
  17. Physostigmine
    Mechanism: carbamoylates the active site of AChE, blocking enzyme activity

    Indications: Glaucoma, Toxicology

    Side Effects: GI (cramps, diarrhea, nausea), diaphoresis, hypersalivation, lacrimation (minimized by topical application)
  18. Echothiophate
    Mechanism: phosphorylates the active site of AChE, blokcing enzyme activity

    Indications: Glaucoma

    Side Effects: GI (cramps, diarrhea, nausea), diaphoresis, hypersalivation, lacrimation

    Other: only used for Pts who have not responded to other therapies
  19. Malathion
    Mechanism: phosphorylates the active site of AChE, blocking activity of the enzyme

    Indications: insecticides

    Side Effects: GI (cramps, diarrhea, nausea), diaphoresis, hypersalivation, lacrimation
  20. AChE reactivators
    Pralidoxime
  21. Pralidoxime
    Mechanism: Nucleophilic attack on AChE (phosphorylated), regenerates active enzyme

    Indications: toxicology

    Other: not effective if phosphorylated AChE has aged

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