Muscarinic/Cholinergic Antagonists Overview and Effects

Sep 13, 2024

Muscarinic Antagonists (Anti-Muscarinic Medications)

Overview

  • Muscarinic Antagonists prevent muscarinic receptors in the parasympathetic nervous system from being stimulated by acetylcholine (ACh).

Nervous System Breakdown

  • Central Nervous System (CNS): Brain and Spinal Cord.
  • Peripheral Nervous System (PNS):
    • Somatic Nervous System: Controls voluntary movement of skeletal muscles.
    • Autonomic Nervous System: Divided into sympathetic and parasympathetic nervous systems.

Parasympathetic Nervous System

  • Function: Controls involuntary actions like digestion, urination, etc.
  • Pathway:
    • Signals originate in hypothalamus and synapse in brain stem or spinal cord.
    • Preganglionic neurons target parasympathetic ganglions near target organs.
    • Postganglionic neurons release acetylcholine (ACh), stimulating muscarinic receptors for 'rest and digest' effects.

Effects of Parasympathetic Stimulation

  • Heart: Slows heart rate.
  • Gastrointestinal: Increases motility for digestion.
  • Bladder: Causes detrusor muscle contraction (urination).
  • Glands: Increases salivary/sweat/lacrimal secretions.
  • Liver: Triggers glucose storage.
  • Lungs: Causes bronchoconstriction.
  • Eyes: Causes pupil constriction (miosis) and reduces intraocular pressure.
  • Brain: Generally stimulant effects, controlling movement and preventing vomiting.

Muscarinic Antagonists

  • Mechanism: Block ACh on muscarinic receptors.
  • Atropine:
    • Uses: Treat bradycardia, nocturnal enuresis, pupil dilation, antidote for organophosphate poisoning.
    • Side Effects: Tachycardia, constipation, urinary retention, dry mouth/skin/eyes, blurry vision, hypothermia, dizziness, confusion.
    • Contraindications: Narrow-angle glaucoma.

Organ-Specific Medications

  • Oxybutynin: Targets bladder, reduces detrusor muscle spasms, treats urge incontinence.
  • Ipratropium & Tiotropium:
    • Use: Bronchodilators for COPD and asthma.
    • Characteristics: Ipratropium is short-acting; Tiotropium is long-acting.

Brain-Targeting Medications

  • Scopolamine: Prevents motion sickness by acting on the brain's vomiting center.
  • Benztropine & Trihexyphenidyl: Used in Parkinson’s disease to restore cholinergic-dopaminergic balance, reducing tremors.
    • CNS Side Effects: Sedation, mental confusion.

Mnemonics & Memory Aids

  • Atropine Mnemonic: Tropical island setting with a boy covering enuresis with a heart (bradycardia), empty water bottle (dryness), and a closed porta-potty (urinary retention).
  • Organ-Specific Mnemonics:
    • Oxybutynin: Oxygen tank inflating a bladder.
    • Ipratropium: Short palm tree with a rat (short-acting).
    • Tiotropium: Tall palm tree with ties (long-acting).
    • Parkinson’s: Parking spot with a Mercedes-Benz.
    • Scopolamine: Scallop vomiting from motion sickness.

Recap

  • Inhibition: Muscarinic antagonists inhibit ACh effects.
  • Main Drugs: Atropine, Oxybutynin, Ipratropium, Tiotropium, Scopolamine, Benztropine, Trihexyphenidyl.
  • Side Effects: Tachycardia, constipation, dry mouth/skin/eyes, blurry vision, hypothermia, confusion.
  • Contraindication: Narrow-angle glaucoma.

Stay tuned for a mind map and more mnemonics to help remember pharmacological details.