Cholinergic Transmission and Parasympathomimetics

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Questions and Answers

What is the reason Acetylcholine is not therapeutically useful?

  • It only stimulates the muscarinic receptors
  • It has only nicotinic activity
  • It has a multiplicity of actions and is rapidly inactivated by cholinesterase enzyme (correct)
  • It is only found in the sympathetic nervous system

What type of receptors does Pilocarpine bind to?

  • Muscarinic acetylcholine receptors (mAChR) (correct)
  • Adrenergic receptors
  • Dopaminergic receptors
  • Nicotinic acetylcholine receptors (nAChR)

What is the effect of Acetylcholine on the heart rate?

  • Increases heart rate
  • Can either increase or decrease heart rate
  • Has no effect on heart rate
  • Decreases heart rate (correct)

Which of the following is an indirectly acting cholinergic agonist?

<p>Neostigmine (D)</p> Signup and view all the answers

What is the effect of Acetylcholine on the salivary secretion?

<p>Increases salivary secretion (B)</p> Signup and view all the answers

How do directly acting cholinergic agonists work?

<p>By binding directly to cholinoreceptors (A)</p> Signup and view all the answers

What is the effect of Acetylcholine on the tone of urinary bladder muscles?

<p>Increases the tone of urinary bladder muscles (B)</p> Signup and view all the answers

What type of receptors does Nicotine bind to?

<p>Nicotinic acetylcholine receptors (nAChR) (A)</p> Signup and view all the answers

What is the effect of atropine on the pupil?

<p>Mydriasis (C)</p> Signup and view all the answers

What is the therapeutic application of atropine in ophthalmology?

<p>To measure refractive errors of the eye (B)</p> Signup and view all the answers

What is the effect of atropine on heart rate at low doses?

<p>Bradycardia (A)</p> Signup and view all the answers

What is the use of atropine as an antidote?

<p>For overdose of cholinergic agonists (C)</p> Signup and view all the answers

What is the effect of atropine on intraocular pressure (IOP) in patients with glaucoma?

<p>Increases IOP (C)</p> Signup and view all the answers

What is the source of atropine?

<p>Atropa belladonna (B)</p> Signup and view all the answers

What is the historical use of atropine?

<p>To dilate pupils for cosmetic reasons (A)</p> Signup and view all the answers

What is the meaning of 'belladonna'?

<p>Beautiful lady (C)</p> Signup and view all the answers

What is the primary mechanism of action of anticholinesterases?

<p>Increasing the levels of acetylcholine at the neuromuscular junction (B)</p> Signup and view all the answers

What is the primary use of pilocarpine in ophthalmology?

<p>To lower intraocular pressure in emergency situations (C)</p> Signup and view all the answers

What is the primary cause of myasthenia gravis?

<p>Autoimmune disorder (D)</p> Signup and view all the answers

What is the purpose of the edrophonium test in diagnosing myasthenia gravis?

<p>To temporarily increase the levels of acetylcholine at the neuromuscular junction (B)</p> Signup and view all the answers

What is a common adverse effect of pilocarpine?

<p>Stimulation of profuse sweating and salivation (D)</p> Signup and view all the answers

What is the name of the disease characterized by fluctuating weakness and fatigability?

<p>Myasthenia gravis (D)</p> Signup and view all the answers

What is a treatment option for myasthenia gravis?

<p>Cholinesterase inhibitors (D)</p> Signup and view all the answers

What is the duration of action of pilocarpine when applied topically to the cornea?

<p>About one day (B)</p> Signup and view all the answers

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Study Notes

Cholinergic Transmission

Parasympathomimetics

  • Parasympathomimetics can be classified into directly and indirectly acting cholinergic agonists.
  • Directly acting cholinergic agonists mimic the effect of acetylcholine (ACh) by binding directly to cholinoreceptors.
  • Examples of directly acting cholinergic agonists include:
    • Acetylcholine (ACh)
    • Pilocarpine
  • ACh has both nicotinic and muscarinic activity, but it is therapeutically of no importance due to its multiplicity of actions and rapid inactivation by cholinesterase enzyme.
  • Actions of ACh:
    • Heart rate: decreased
    • Blood pressure: decreased
    • Salivary secretion: increased
    • GIT secretion and motility: increased
    • Bronchial secretion: increased
    • Tone of urinary bladder muscles: increased
    • Pupil sphincter muscle: contracted
    • Ciliary muscle: contracted

Adverse Effects of Cholinergic Drugs

  • Cholinergic drugs can cause adverse effects such as:
    • Increased salivation
    • Increased sweating
    • Nausea and vomiting
    • Abdominal cramps
    • Diarrhea

Cholinergic Antagonists

Anti-Muscarinic Agents

  • Examples of anti-muscarinic agents include:
    • Atropine
    • Scopolamine
    • Ipratropium
  • Atropine:
    • Isolated from Atropa belladonna
    • Has muscarinic activity
    • Actions:
      • Eye: mydriasis, unresponsiveness to light, cycloplegia, increased IOP in patients with glaucoma
      • CVS: bradycardia at low doses, modest tachycardia at high doses
    • Therapeutic applications:
      • Ophthalmic: mydriatic and cycloplegic effect
      • Antisecretory: blocks respiratory secretions prior to surgery
      • Antidote: for overdose of cholinergic agonists

Indirectly Acting Cholinergic Agonists (Anticholinesterases)

  • Examples of anticholinesterases include:
    • Neostigmine (Prostigmine)
    • Edrophonium
  • Uses:
    • To stimulate bladder and GIT contraction
    • To treat myasthenia gravis

Myasthenia Gravis

  • Myasthenia gravis is a neuromuscular disease characterized by fluctuating weakness and fatigability.
  • It is an autoimmune disorder caused by circulating antibodies that block acetylcholine receptors at the post-synaptic neuromuscular junction, inhibiting ACh.
  • Diagnosis: Edrophonium test
  • Treatment:
    • Cholinesterase inhibitors to directly improve muscle function
    • Immunosuppressant drugs to reduce the autoimmune process

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