Pharmacology · MU Sofia

19. Antimuscarinic drugs (M-cholinolytics).

Covers antimuscarinic drugs that block acetylcholine at muscarinic receptors, starting with a classification into natural alkaloids, semi-synthetic and synthetic analogues with their uses. It then goes through pharmacodynamic effects by organ system, pharmacokinetics, side effects, drug interactions, therapeutic uses and risks in pregnancy, ending with recap questions.

Inside: 9 sections · 2 labelled pictures · 10 flashcards · 6 min

Topic 18 of 93 in the MU Sofia syllabus for Pharmacology (Medicine, Year 3). The free AceMed note covers it in 9 sections, about 778 words (6 min of reading), with 10 flashcards.

In this note

  1. Antimuscarinic Drugs (M-cholinolytics)
  2. Classification
  3. Pharmacodynamics
  4. Pharmacokinetics
  5. Side Effects
  6. Drug Interactions
  7. Therapeutic Use
  8. Contraindications in Pregnancy
  9. Recap Questions:

Antimuscarinic Drugs (M-cholinolytics)

Anticholinergic drugs inhibit the action of acetylcholine at muscarinic receptors. They are used to treat various conditions by reducing parasympathetic nervous system activity.

Classification

  1. 1. Naturally Occurring Alkaloids:
  • Atropine: A classic muscarinic antagonist, often used to treat bradycardia and as a preoperative medication to reduce salivation.
  • Scopolamine: Used primarily for motion sickness and postoperative nausea and vomiting.
  • Belladonnae (Extract/Tinct): Derived from the belladonna plant, used for a variety of purposes, including as an antispasmodic.
  1. 2. Semi-Synthetic Analogs:
  • Homatropine: Used primarily for eye examinations to induce pupil dilation (mydriasis).
  • Buscolysin: Often used as an antispasmodic to relieve cramps in the gastrointestinal system.
  1. 3. Synthetic Analogs:
  • Oxybutynin: Primarily used to treat overactive bladder and urinary incontinence by reducing bladder contractions.
  • Tropicamide: Used in ophthalmology to dilate the pupils for diagnostic eye procedures.
  • Ipratropium: A bronchodilator used in respiratory conditions such as asthma and COPD.

Pharmacodynamics

Antimuscarinic drugs block the action of acetylcholine at muscarinic receptors, leading to a variety of effects on different organ systems.

  • Cardiovascular:
  • Tachycardia: Increased heart rate, primarily due to inhibition of the vagal tone.
  • Increased blood pressure: May occur due to tachycardia and reduced vasodilation.
  • Gastrointestinal:
  • Reduced motility: Inhibition of smooth muscle contraction leads to slowed gastric emptying and decreased peristalsis.
  • Reduced secretions: Decreased salivation and gastrointestinal secretions, which may result in dry mouth and constipation.
  • Respiratory:
  • Bronchodilation: By inhibiting muscarinic receptors in the smooth muscle of the bronchi, leading to dilation of airways.
  • Reduced bronchial secretions: Decrease in mucus production, helpful in conditions like COPD.
  • Urinary:
  • Reduced bladder contractions: Effective in reducing urgency and frequency associated with overactive bladder.
  • Ocular:
  • Mydriasis: Pupil dilation, often used for eye examinations.
  • Cycloplegia: Paralysis of the ciliary muscles, inhibiting accommodation (the ability to focus on near objects).
  • Central Nervous System (CNS):
  • Drugs that cross the blood-brain barrier (e.g., atropine, scopolamine) can have sedative effects, but may also cause confusion, memory impairment, and even hallucinations, particularly in elderly patients.

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