Direct Acting Cholinergic Agonists Overview
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Questions and Answers

What are drugs that mimic acetylcholine (Ach) called?

Cholinomimetics

Cholinomimetics are divided into what two categories?

  • Muscarinic receptors and nicotinic receptors
  • Alkaloids and choline esters
  • Ach receptor stimulants and cholinesterase inhibitors (correct)
  • Direct-acting drugs and indirect-acting drugs
  • What is the name for the type of cholinomimetic that directly stimulates Ach receptors?

    Direct-acting cholinomimetics

    What is the name for the type of cholinomimetic that inhibits cholinesterase?

    <p>Indirect-acting cholinomimetics</p> Signup and view all the answers

    What are the two main types of Ach receptors?

    <p>Muscarinic and nicotinic receptors</p> Signup and view all the answers

    Which are examples of direct-acting cholinomimetics?

    <p>Acetylcholine, Carbachol, Methacholine, and Bethanecol</p> Signup and view all the answers

    Choline esters are relatively lipid soluble.

    <p>False</p> Signup and view all the answers

    Which of the following statements is TRUE about choline esters?

    <p>They undergo varying degrees of hydrolysis by cholinesterase.</p> Signup and view all the answers

    Which of these choline esters has negligible effects on nicotinic receptors?

    <p>Bethanechol</p> Signup and view all the answers

    What is the reason that Methacholine and Bethanechol have minimal effects on nicotinic receptors?

    <p>The presence of a beta-methyl group</p> Signup and view all the answers

    What is the main action of Bethanechol?

    <p>It acts chiefly on the bladder &amp; bowels</p> Signup and view all the answers

    Study Notes

    Direct Acting Cholinergic Agonists (Cholinomimetics)

    • Cholinergic agonists mimic acetylcholine (ACh) actions
    • Divided into direct-acting and indirect-acting
    • Direct-acting stimulate ACh receptors
    • Indirect-acting inhibit acetylcholinesterase (AChE)
    • They cause parasympathetic effects

    Parasympathetic Division Effects

    • Eye: Constricts pupil (miosis)
    • Eye: Ciliary muscle contraction for near vision, increases aqueous outflow
    • Eye: Reduces intraocular pressure
    • Salivary Glands: Stimulates saliva production
    • Lung: Constricts bronchi
    • Heart: Inhibits heart rate
    • Stomach, Pancreas, Intestines: Stimulates contractions/secretions (motility)
    • Liver: Stimulates digestive secretions
    • Bladder: Stimulates urination
    • Genitals: Causes erection

    Cholinergic Agonists Classified

    • Choline esters: Acetylcholine, Carbachol, Methacholine, Bethanechol
    • Alkaloids: Muscarine, Nicotine, Lobeline, Pilocarpine, Arecholine, Oxotremorine

    Choline Esters Properties

    • Acetylcholine: Undergoes rapid hydrolysis
    • Acetylcholine: IV bolus injection - effects last 5-20 seconds
    • Acetylcholine: IM and SC injections cause local effects
    • Methacholine: 3 times more resistant to hydrolysis than ACh, longer duration
    • Methacholine: Effective orally
    • Bethanechol: Negligible CVS effects, acts primarily on bladder and bowel
    • Bethanechol: Preferable to Carbachol due to partial selectivity
    • Carbachol: Acts on both muscarinic and nicotinic receptors
    • Choline esters are lipid-insoluble, poorly absorbed and poorly penetrate the central nervous system (CNS)

    Choline Esters- Clinical Uses

    • Bethanechol: Postoperative paralytic ileus, postoperative/postpartum urinary retention, neurogenic bladder atony, congenital megacolon, gastroesophageal reflux
    • Other uses: Dry mouth (Sjogren's syndrome with pilocarpine) and diagnosis of bronchial airway hyperreactivity (methacholine)

    Adverse Effects

    • Excessive salivation, sweating
    • Nausea, diarrhea, abdominal cramps
    • Urinary urgency
    • Cutaneous vasodilation
    • Bronchoconstriction
    • Hypotension

    Contraindications

    • Bronchial asthma
    • GI or urinary tract obstruction

    Alkaloids Notes

    • Muscarine: Occurs in poisonous mushrooms, only muscarinic actions, not used therapeutically, toxic when ingested, less well absorbed than tertiary alkaloids
    • Pilocarpine, Lobeline, and Nicotine: Tertiary alkaloids, well absorbed, nicotine derived from tobacco, lipophilic, absorb through skin

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    Description

    This quiz covers the key concepts of direct-acting cholinergic agonists and their effects on the parasympathetic division. Learn how these agonists, including choline esters and alkaloids, mimic acetylcholine and influence various bodily functions. Test your knowledge on their classification and physiological impacts.

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