Anti-Cholinergics (aka Anti-Muscarinics)

on 1.2.07 with 0 comments



  • Remember, these block acetylcholine receptors and should therefore yield sympathetic effects

  • Effects include blind as a bat (mydriasis), red as a beet (flush), dry as a bone (xerostomia), mad as a hatter (psychosis), and hot as a hare (increased body temperature).

  • All competitively block muscarinic receptors (quarternaries block nicotinics as well)

Tertiary Amines

  • Cross BBB

  • Do not block nicotinic receptors

    1. Atropine – (natural) behavioral effects, biphasic cardiac response (low dose = bradycardia, high = tachycardia), relax smooth muscle, decrease secretions, etc.

    2. Scopolamine – (natural) motion sickness, vestibulation, biphasic cardiac response, relax smooth muscle, decrease secretions, etc.

    3. Homatropine, Cyclopentolate, Tropicamide – [eyes] used to examine mydriasis and measure cycloplegia

    4. Pirenzepine, Telenzepine – [GI] primarily block M1 to decrease gastric secretion in peptic ulcer

    5. Dicyclomine – [GI] use for visceral hypermotility and spasms

    6. Oxybutynin, Oxyphencyclimine – used to relieve bladder spasms following urologic surgery

    7. Benztropine, Trihexyphenidyl – [CNS] use to treat Parkinson’s

Quarternary Ammonium Compounds

      • Do not cross BBB

      • Able to block nicotinic receptors

        1. Propantheline, Methantheline, Mepenzolate, Methscopolamine – use for visceral hypermotility and spasms, as well as duodenal ulcer treatment

        2. Glycopyrrolate – use for visceral hypermotility and spasms, duodenal ulcer treatment, and cardiovascular disorders; pre-anesthetic drug of choice to reduce salivation (due to mild effect on heart in comparison to atropine)

        3. Ipratropium – key respiratory drug, use to treat bronchial asthma and COPD

Category: Pharmacology Notes

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