Cholinergic Antagonists

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4 Terms

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Muscarinic Receptor Antagonists

  • Used for

  • Atropine

    • Cardiovascular, GI

  • Benztropin (Congentin) and Trihexyphenidyl (Artane)

    • Parkinson Disease

  • Scopolamine (Transderm cop)

    • Motion sickness, take before, causes dry mouth and sedation

  • Cyclopentolate (Cyclogyl), Tropicamide (Mydriacyl) and Tropicamide + hydroxyamphetamine (Paremyd)

    • Mydriasis EYE

  • Ipratropium (Atrovent), Ipratropium + albuterol (Combivent), Tiotropium (Spiriva), Aclidinium (Tumorza)

    • For COPD and las 2 for LAMA

  • Glycopyrrolate (Robinul)

    • GI, respiratory, peripheral

  • Dicyclomine (Bentyl) L-Hyoscyamine (Anaspaz)

    • antispasmodic for IBS

  • Oxybutynin (Ditropan XL), Tolterodine (Detrol)

    • Bladder

  • Darifenacin (Enablex), Solifenacin (Vesicare)

    • M3 selective for bladder

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Contraindications for muscarinic antagonists

  • Toxicity synmptoms

  • Narrow/closed glaucoma or prostatic hyperplasia (urinary retention)

  • Tox symptoms:

    • Blind as a bat

    • Dry as a bone

    • Red as a beet

    • Mad as a hatter

    • Hot as a hare

    • Can’t see can’t pee

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Ganglionic Blockers (Cholinergic Antagonists)

  • Define

  • Only one drug does this

  • Effects

  • Agents that block nicotinic receptors at all autonomic ganglia, pre-synaptic and post synaptic

    • Results in the Dominant tone being lost with ganglia blockage

      knowt flashcard image
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  • Mecamylamine: rarely used but can reduce bleeding by controlled hypotension

<ul><li><p>Agents that block nicotinic receptors at all autonomic ganglia, pre-synaptic and post synaptic</p><ul><li><p>Results in the Dominant tone being lost with ganglia blockage</p><img src="https://knowt-user-attachments.s3.amazonaws.com/ed88eba6-b969-4fb1-8a5d-9876df70a083.png" data-width="75%" data-align="center" alt="knowt flashcard image"></li></ul></li></ul><img src="https://knowt-user-attachments.s3.amazonaws.com/10bfbcd3-a799-4f57-9276-9cb802a35ae0.png" data-width="75%" data-align="center" alt="knowt flashcard image"><ul><li><p>Mecamylamine: rarely used but can reduce bleeding by controlled hypotension</p></li></ul><p></p>
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NMJ Blocking Agents (Cholinergic Antagonists)

  • Define

  • Types

    • Drugs

  • Produce paralysis by blocking muscle contraction

  • Non-depolarizing: block pre-junctional Na+ channels; causes muscle weakness leading to flaccid paralysis, cannot respond to pain

    All reversed by cholinesterase inhibitors such as Neostigmine and Pyridostigmine

    • Atracurium (Tracrium)

    • Cistracurium (Nimbex): more potent, no seizures and less histaminic response

    • Rocuronium (Zemuron)

      • fastest

    • Vecuronium (Norcurom)

  • Depolarizing: P1. activates and keeps channel open and does not allow muscle to recover. P2. membrane repolarizes but receptor is desensitized

    • Succinylcholine (Anectine): extremely rapid onset and ultra short acting

      • Dantrolene: use to reverse effects

        • Hyperkalemia, Arrhytmias, Bradychardia, Fasciculations, Malignant Hyperthemia