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Ch. 11 anticholinergic drugs. R1. 이송이. Anticholinergic Drugs. Anticholinergic drugs : group of drugs that block muscarinic receptors Commonly Used Atropine Scopolamine Glycopyrrolate. Mechanism of Action. Anticholinergics Muscarinic Rc. subgroups M1 – Neuronal M2 – Cardiac

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anticholinergic drugs
Anticholinergic Drugs
  • Anticholinergic drugs : group of drugs that block muscarinic receptors
  • Commonly Used
    • Atropine
    • Scopolamine
    • Glycopyrrolate
mechanism of action
Mechanism of Action
  • Anticholinergics
  • Muscarinic Rc. subgroups
    • M1 – Neuronal
    • M2 – Cardiac
    • M3 - Glandular

Ester Link

Organic Base

Aromatic Acid

Ester linkage is essential for effective binding of Anticholinergic s to Acetylcholine Rc.

Competitively blocks Ach & Prevents further activation

clinical pharmacology
Clinical Pharmacology
  • In clinical doses only Muscarinic Receptors are blocked

 Extent of effect depends on the degree

of baseline vagal tone

clinical pharmacology1
Clinical Pharmacology
  • Cardiovascular
    • SA node  tachycardia useful in reversing bradycardia d/t vagal reflexes (e.g. baroreceptor reflex, peritoneal stimuli, oculocardiac reflex)
    • AV node facilitation of conduction PR interval shortening
    • Ventricle, Pph. Vasculature little effect
    • Modestly enhance sympathetic activity
    • Large dose dilatation of cutaneous vessels (atropine flush)
clinical pharmacology2
Clinical Pharmacology
  • Respiratory
    • Inhibit secretions of respiratory mucosa (nose ~ bronchi)
    • Relaxation of bronchial smooth musculature
      • Reduce airway resistance
      • Increase anatomic dead space
      • Effects pronounced in COPD or Asthma pts.
clinical pharmacology3
Clinical Pharmacology
  • Cerebral
    • Cause a spectrum of CNS effects ; stimulation ~ depression
    • Depends on drug choice and dose
    • Stimulation : excitation, restlessness or hallucination
    • Depression : sedation & amnesia
    • Physostigmine : reverses these actions
clinical pharmacology4
Clinical Pharmacology
  • Gastrointestinal
    • Salivary & Gastric secretions are reduced
    • Intestinal motility and peristalsis decrease
      • Prolong gastric emptying time
    • LES is reduced
    • Risk of aspiration pneumonia increases
  • Opthalmic : Mydriasis & Cycloplegia
  • GU : Decreased ureter & bladder tone urinary retention
  • Thermoregulation : Inhibit sweat gl. rise in body temp. (atropine fever)
atropine
Atropine
  • Physical Structure
  • Dosage
    • Premedication
      • 0.001-0.02mg/kg (up to 0.4-0.6mg in adults) IV or IM
    • Treating severe bradycardia – up to 2mg
atropine1
Atropine
  • Clinical Consideration
    • Potent effect on the heart & bronchial smooth muscle
      • Treatment in bradyarrhythmias
      • CAD pts may not tolerate the increased myocardial O2 demand & decreased O2 supply
    • Ipratropium bromide (Atropine derivative) : used in the treatment of bronchospasm
    • CNS effects : minimal
    • Mild postop. memory loss
    • Toxic doses  excitatory reaction
    • Antisialagogue effect : 0.01 ~ 0.02 mg/kg IM
    • Use cautiously in 1. Narrow angle glaucoma 2. PH 3. Bladder Obx
scopolamine
Scopolamine
  • Physical Structure
  • Dosage
    • Premedication
      • 0.01-0.02mg/kg IM (up to 0.4-0.6mg in adults)
scopolamine1
Scopolamine
  • Clinical Considerations
    • More potent antisialagogue
    • Greater CNS effects
    • Causes Drowsiness & Amnesia
    • Restlessness & Delirium is possible
    • Prevents motion sickness
    • Pronounced ocular effects
      • Should be avoided in closed angle glaucoma
glycopyrrolate
Glycopyrrolate
  • Physical Structure
  • Dosage
    • Half dose of Atropine
    • Premedication
      • 0.005-0.001mg/kg (up to 0.2-0.3mg in adults)
glycopyrrolate1
Glycopyrrolate
  • Clinical Considerations
      • cannot cross the BBB Devoid of CNS & Opthalmic activity
      • Potent inhibitor of salivary gl. & respiratory tract secretion
      • HR increases after IV injection but not IM
      • Longer duration of action than Atropine

(2~4hr vs. 30 min)