Muscarinic Agonists and the Parasympathetic Nervous System - Hernandez Block 1
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Questions and Answers

Muscarinic Agonists target the Parasympathetic Nervous System.

True

Halt Digestion, Mydriasis, Urinary retention, Bronchodilation, and Halt salivary secretions are associated with the Parasympathetic Nervous System.

False

Which of the following is a Reversible Cholinesterase Inhibitor that does NOT cross the blood-brain barrier?

  • Donepezil
  • Galantamine
  • Neostigmine (correct)
  • Rivastigmine

    • Which of the following is a Reversible Cholinesterase Inhibitor that does cross the blood-brain barrier?

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

    An overdose of cholinergic drugs is called "Cholinergic Crisis" or "Cholinergic Toxicity".

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

    Which of the following ADR is associated with cholinergic agonists?

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

    Which of the following is the Pharm. Action of Cholinesterase Inhibitors?

    <p>Increase duration and amount of synaptic ACh</p> Signup and view all the answers

    What is the CNS pathology of Alzheimer's Disease (AD)?

    <p>Degeneration of basal forebrain pathway neurons</p> Signup and view all the answers

    What is the main symptom of Alzheimer's Disease?

    <p>Memory loss</p> Signup and view all the answers

    Which pharmacologic class is associated with Alzheimer's Disease?

    <p>Cholinesterase Inhibitors</p> Signup and view all the answers

    Irreversible, cholinesterase inhibitors that do not cross the BBB are used to treat AD.

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

    Rivastigmine is metabolized by cholinesterase.

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

    Transdermal patches are available for Donepezil and Rivastigmine

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

    Donepezil and Galantamine are substrates of which two CYPs?

    <p>CYP3A4/CYP2D6</p> Signup and view all the answers

    Irreversible cholinesterase inhibitors are used as pesticides and warfare agents?

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

    Which of the following drugs are NOT pesticides?

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

    Which of the following drugs is NOT a warfare agent?

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

    Which pharmacologic class is associated with Myasthenia Gravis (MG)?

    <p>Cholinesterase Inhibitor</p> Signup and view all the answers

    What is the Peripheral pathology of MG?

    <p>Auto-antibodies to muscle-type nicotinic receptors</p> Signup and view all the answers

    Muscle weakness and fatigue are symptoms of Myasthenia Gravis (MG).

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

    Reversible, competitive cholinesterase inhibitors that do NOT cross the BBB are used to treat MA, Cholinergic crisis from exposure to irreversible cholinesterase inhibitors and Neuromuscular blockade reversal

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

    Which cholinesterase inhibitors used for Myasthenia Gravis treatment have a long duration?

    <p>Both C and D</p> Signup and view all the answers

    What is the most common cholinesterase inhibitor used for Alzheimer's Disease?

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

    Edrophonium, used to treat Myasthenia Gravis, has a short duration (minutes)

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

    Antidote, used to treat toxic exposure to irreversible cholinesterase inhibitors (aka Cholinergic Criss or Toxicity). It is an Acetylcholinesterase Activator

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

    Parasympathetic Nervous System - Associated with Miosis, Promoting salivary secretions, Maintain steady heart rate, Promote digestion, Promote urination.

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

    Cholinergic agonist binds both nicotinic and muscarinic receptors

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

    Which of the following drugs are Cholinergic Agonists?

    <p>Both A and B</p> Signup and view all the answers

    What is the Pharm. Action of Pilocarpine?

    <p>Induce miosis and decrease intraocular pressure</p> Signup and view all the answers

    What is the MOA of Pilocarpine?

    <p>Muscarinic Agonist</p> Signup and view all the answers

    What is the clinical use of Pilocarpine?

    <p>Glaucoma, ocular hypertension, eye procedures</p> Signup and view all the answers

    What is the therapeutic class of Pilocarpine?

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

    What is the indication for Methacholine, a Muscarinic Agonist?

    <p>Bronchoprovocation Test (bronchial hyperactivity diagnostic tool)</p> Signup and view all the answers

    What is the Pharm. Action of Methacholine?

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

    What is the indication of Bethanechol, a Muscarinic Agonist?

    <p>Urinary retention (related to surgical procedure or childbirth)</p> Signup and view all the answers

    What is the Pharm. Action of Bethanechol?

    <p>Contract bladder detrusor (promote urination)</p> Signup and view all the answers

    Match the Muscarinic Agonists with their Pharm. Actions.

    <p>ADR = SLUDGE-DDUMBELS Pilocarpine = Induce miosis/lower intraocular pressure Methacholine = Bronchoconstriction Bethanechol = Promote urination</p> Signup and view all the answers

    What is the MOA of Atropine?

    <p>Muscarinic Antagonist</p> Signup and view all the answers

    Which of the following is NOT an indication for Atropine?

    <p>Motion sickness (Vertigo)</p> Signup and view all the answers

    Atropine indications are usually critical conditions.

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

    Atropine is used for Peripheral uses

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

    What is the MOA of Scopolamine?

    <p>Muscarinic Antagonist</p> Signup and view all the answers

    What is NOT an indication for Scopolamine?

    <p>GI distress disorders</p> Signup and view all the answers

    Scopolamine is indicated for usually NOT critical conditions.

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

    Scopolamine is for Central uses.

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

    Which of the following is NOT indicated for both Atropine and Scopolamine?

    <p>Increasing terminal secretions (salivation, bronchial secretions)</p> Signup and view all the answers

    ADRs associated with Atropine and Scopolamine are SLUDGE-DDUMBELS?

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

    Which drug does NOT have the "Mydriatic, Cycloplegic" therapeutic class?

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

    What is the clinical use of the Mydriatic, Cycloplegic class?

    <p>Eye procedures (Pupil dilation, Induce Cycloplegia)</p> Signup and view all the answers

    What is the Pharm. Action of the Mydriatic, Cycloplegic class?

    <p>Induce mydriasis (pupil dilation) or cycloplegia (paralyze muscles that control pupil diameter).</p> Signup and view all the answers

    The ADR for the Mydriatic, Cycloplegic class is: Minimized due to local application

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

    Which of the following is NOT an non-selective Muscarinic Antagonist for OAB?

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

    Which of the following is a M3-selective Muscarinic Antagonist for OAB?

    <p>Both A and B</p> Signup and view all the answers

    Which kind of drugs treat an overactive bladder (OAB)?

    <p>Genitourinary/Urinary Antispasmodic</p> Signup and view all the answers

    What is the MOA of Genitourinary/Urinary Antispasmodic drugs?

    <p>Muscarinic Antagonists</p> Signup and view all the answers

    What is the Non-selective OAB drug that can cross the BBB?

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

    Darifenacin is a CYP2D6 substrate.

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

    Trospium is a CYP3A4 substrate.

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

    Trospium has lipophilicity.

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

    What is the Pharm. Action of Urinary Antispasmodics?

    <p>Bladder detrusor muscle relaxation</p> Signup and view all the answers

    What is the MOA of Bronchodilators?

    <p>Muscarinic Antagonists</p> Signup and view all the answers

    What is the short-acting (6-8 hours) Bronchodilator?

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

    Which of the following is NOT a long-acting (>12 hours) Bronchodilator?

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

    What is the Pharm. Action for Bronchodilators?

    <p>Induce bronchodilation and reduce bronchial secretions</p> Signup and view all the answers

    ADR for Bronchodilators: Xerostomia but minimized due to local application - Anticholinergic Syndrome-like symptoms for systemic circulation.

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

    What is the indication for Bronchodilators?

    <p>Respiratory disorders</p> Signup and view all the answers

    Long-acting muscarinic agonists (LAMA) - Prophylactic use for daily maintenance

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

    Which of the following Bronchodilators do NOT have Dry Powder formulations?

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

    For the Dry Powder Bronchodilators, avoid use if you have a milk allergy

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

    What is the Pharmacologic Class for Nicotine?

    <p>Nicotinic Agonist</p> Signup and view all the answers

    What is the indication for Nicotine?

    <p>OTC Smoking cessation aid</p> Signup and view all the answers

    Tobacco is the unnatural source of nicotine

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

    What is the Pharm. Action of Nicotine?

    <p>Decrease nicotine craving and withdrawal symptoms</p> Signup and view all the answers

    Match the ADRs of Nicotine

    <p>CNS = Psychoactive stimulation CV = Hypertension, Tachycardia Other = Physical/Psychological dependence Binds all 3 nicotinic receptor subtypes: = Nm, Nn, Ng</p> Signup and view all the answers

    Match the Positive/Negative effects of nicotine

    <p>Positive = Anxiolytics Negative = Gastrointestinal distress Negative = Hyopthermia Positive = Cognitive enhancement</p> Signup and view all the answers

    What drug is apart of the Partial Nicotinic Agonist class?

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

    What is the indication for Varenicline?

    <p>Rx smoking cessation aid</p> Signup and view all the answers

    What is the Pharm. Action of Varenicline?

    <p>Decrease nicotine craving and withdrawal symptoms</p> Signup and view all the answers

    Which of the following is NOT an ADR to Varenicline?

    <p>Increased migraines/Light sensitivity</p> Signup and view all the answers

    What Pharmacologic class is Mecamlyamine?

    <p>Nicotinic Antagonist</p> Signup and view all the answers

    Mecamylamine is in the antihypertensive class, therefore making it indicated for malignant hypertension.

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

    What is the MOA of Mecamylamine?

    <p>Ganglionic nicotinic antagonist (blocker)</p> Signup and view all the answers

    Mecamylamine significantly decreases blood pressure

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

    ALL anticholinergics are identified to be inappropriate for any individual with dementia, cognitive impairment, delirium, lower urinary tract symptoms, and benign prostatic hypertrophy

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

    Anticholinergic drugs are known as "Antimuscarinics" and "Muscarinic Antagonists"

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

    What identifies drugs with increased incidence of anticholinergic syndrome-like adverse drug reactions?

    <p>Magellan Anticholinergic Risk Scale</p> Signup and view all the answers

    You should avoid taking more than 2 anticholinergic drugs

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

    Match the Generic/Brand names

    <p>Acetylcholine = Miochol-E Carbechol = Miostat Pilocarpine (ophthalmic) = Isopto Carpine Pilocarpine (oral) = Salagen</p> Signup and view all the answers

    Match the Generic/Brand names.

    <p>Cevimeline = Evoxac, Tarceva Bethanechol = Duvoid, Urecholine Methacholine = Provocholine Atropine = Atropen</p> Signup and view all the answers

    Match the Generic/Brand names.

    <p>Scopolamine = Transderm Scop Ipratropium = Atrovent Ipratropium w/ Albuterol = Combivent Tiotropium = Spiriva</p> Signup and view all the answers

    Match the Generic/Brand names.

    <p>Oxybutynin (oral) = Ditropan Darifenacin = Enablex Donepezil = Aricept Oxybutynin (transdermal film) = Oxytrol</p> Signup and view all the answers

    Match the Generic/Brand names.

    <p>Solifenacin = Vesicare Tiotropium = Spiriva Tolterodine = Detrol Atropine = Isopto Atropine</p> Signup and view all the answers

    Match the Generic/Brand names.

    <p>Varenicline = Chantix Mecamylamine = Inversine Nicotine = Nicotine Polacrilex Pralidoxime = 2-PAM</p> Signup and view all the answers

    Study Notes

    Parasympathetic Nervous System

    • Targets of Muscarinic Agonists
    • Associated with:
      • Halt Digestion
      • Mydriasis
      • Urinary retention
      • Bronchodilation
      • Halt salivary secretions
      • Miosis
      • Promoting salivary secretions
      • Maintaining steady heart rate
      • Promoting digestion
      • Promoting urination

    Cholinergic Crisis

    • An overdose of cholinergic drugs is also known as "Cholinergic Toxicity"
    • Associated with cholinergic agonists

    Alzheimer's Disease (AD)

    • CNS pathology:
    • Main symptom:
    • Associated pharmacologic class:
    • Irreversible, cholinesterase inhibitors that do not cross the BBB are used to treat AD
    • Rivastigmine is metabolized by cholinesterase
    • Transdermal patches are available for Donepezil and Rivastigmine
    • Donepezil and Galantamine are substrates of CYP2D6 and CYP3A4

    Myasthenia Gravis (MG)

    • Associated pharmacologic class:
    • Peripheral pathology:
    • Symptoms: muscle weakness and fatigue
    • Reversible, competitive cholinesterase inhibitors that do NOT cross the BBB are used to treat MG
    • Cholinergic crisis from exposure to irreversible cholinesterase inhibitors and Neuromuscular blockade reversal
    • Edrophonium, used to treat MG, has a short duration (minutes)

    Cholinesterase Inhibitors

    • Pharm.Action:
    • Irreversible cholinesterase inhibitors are used as pesticides and warfare agents
    • Antidote, used to treat toxic exposure to irreversible cholinesterase inhibitors (aka Cholinergic Crisis or Toxicity), is an Acetylcholinesterase Activator

    Muscarinic Agonists

    • Bind both nicotinic and muscarinic receptors
    • Examples:
    • Pharm.Action of Pilocarpine:
    • MOA of Pilocarpine:
    • Clinical use of Pilocarpine:
    • Therapeutic class of Pilocarpine:
    • Indication for Methacholine:
    • Pharm.Action of Methacholine:
    • Indication of Bethanechol:
    • Pharm.Action of Bethanechol:

    Anticholinergics

    • MOA of Atropine:
    • Indications:
    • Peripheral uses
    • MOA of Scopolamine:
    • Indications:
    • Central uses
    • ADRs associated with Atropine and Scopolamine: SLUDGE-DDUMBELS

    Urinary Antispasmodics

    • MOA:
    • Pharm.Action:
    • Treat an overactive bladder (OAB)
    • Non-selective Muscarinic Antagonist for OAB:
    • M3-selective Muscarinic Antagonist for OAB: Darifenacin
    • Darifenacin is a CYP2D6 substrate
    • Trospium is a CYP3A4 substrate
    • Trospium has lipophilicity

    Bronchodilators

    • MOA:
    • Pharm.Action:
    • Short-acting (6-8 hours):
    • Long-acting (>12 hours):
    • ADR: Xerostomia but minimized due to local application - Anticholinergic Syndrome-like symptoms for systemic circulation
    • Indication:

    Nicotine

    • Pharm.Action:
    • Indication:
    • Tobacco is the unnatural source of nicotine
    • Match the ADRs of Nicotine
    • Match the Positive/Negative effects of nicotine
    • Varenicline is a Partial Nicotinic Agonist
    • Indication for Varenicline:
    • Pharm.Action of Varenicline:
    • ADR to Varenicline:

    Miscellaneous

    • Mecamylamine is in the antihypertensive class, therefore making it indicated for malignant hypertension
    • MOA of Mecamylamine:
    • Mecamylamine significantly decreases blood pressure
    • ALL anticholinergics are identified to be inappropriate for any individual with dementia, cognitive impairment, delirium, lower urinary tract symptoms, and benign prostatic hypertrophy
    • Anticholinergic drugs are known as "Antimuscarinics" and "Muscarinic Antagonists"
    • Identify drugs with increased incidence of anticholinergic syndrome-like adverse drug reactions:
    • Avoid taking more than 2 anticholinergic drugs

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    Explore how Muscarinic Agonists affect the Parasympathetic Nervous System with this quiz. Test your knowledge on the interactions between drugs and the parasympathetic branch of the autonomic nervous system.

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