Cholinergic Drugs: Agonists, Antagonists, and Inhibitors
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Questions and Answers

What is the primary action of bethanechol on the heart?

  • No effect on heart rate
  • Causing irregular heartbeats
  • Speeding it up
  • Slowing it down (correct)

Why is bethanechol described as a quaternary ammonium compound?

  • Because it rapidly crosses cell membranes
  • Because it readily reaches the central nervous system
  • Because it has a positive charge (correct)
  • Because it easily enters the bloodstream

In which system does bethanechol increase tone and motility?

  • Gastrointestinal system (correct)
  • Nervous system
  • Urinary system
  • Respiratory system

What is the primary effect of bethanechol on the smooth muscle in the lung?

<p>Constriction of bronchi (A)</p> Signup and view all the answers

What is the onset of action for bethanechol when administered orally?

<p>30-60 minutes (D)</p> Signup and view all the answers

What is the duration of action for bethanechol?

<p>~1 hour (A)</p> Signup and view all the answers

Why are cholinergic drugs not recommended in the elderly population?

<p>They can worsen existing health conditions in the elderly (A)</p> Signup and view all the answers

What is the role of cholinesterase inhibitors in preventing acetylcholine breakdown?

<p>They prevent acetylcholine breakdown (D)</p> Signup and view all the answers

What is the primary effect of muscarinic antagonists?

<p>Blocking acetylcholine effects (C)</p> Signup and view all the answers

Why should cholinergic drugs be used with caution in pregnant females?

<p>They can affect fetal development (B)</p> Signup and view all the answers

Why should cholinergic drugs not be used in lactating females?

<p>They decrease milk production due to anticholinergic side effects (D)</p> Signup and view all the answers

Which of the following is a therapeutic use of bethanechol?

<p>Treatment of urinary retention (B)</p> Signup and view all the answers

What are the adverse effects of bethanechol?

<p>Hypotension, abdominal cramps, and diarrhea (A)</p> Signup and view all the answers

What are the symptoms of muscarinic poisoning?

<p>Profuse salivation, visual disturbances, and bradycardia (B)</p> Signup and view all the answers

What is the main therapeutic use of pilocarpine?

<p>Treatment of glaucoma (D)</p> Signup and view all the answers

What are the alternative names for muscarinic antagonists?

<p>Parasympatholytic drugs and anticholinergic drugs (B)</p> Signup and view all the answers

What is the mnemonic used to remember the side effects of muscarinic poisoning?

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

Why do certain drugs like anti-histamines need to be used with caution in patients receiving muscarinic antagonists?

<p>They may exacerbate the adverse effects of muscarinic antagonists (C)</p> Signup and view all the answers

What is the primary effect of cevimeline?

<p>Treatment of dry mouth in Sjogren's syndrome (D)</p> Signup and view all the answers

Acetylcholine is used for rapid miosis after delivery in which procedure?

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

What is the effect of direct-acting muscarinic agonists on cholinesterase inhibitors?

<p>They potentiate the effects of cholinesterase inhibitors (C)</p> Signup and view all the answers

Why is pilocarpine an exception among muscarinic agonists?

<p>It can cross cell membranes easily. (B)</p> Signup and view all the answers

What effect does atropine have on muscarinic receptors?

<p>It desensitizes them. (D)</p> Signup and view all the answers

Why should bethanechol be used with caution in lactating females?

<p>It decreases milk production due to anticholinergic side effects (B)</p> Signup and view all the answers

What is the primary effect of atropine on muscarinic receptors?

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

How does bethanechol affect the heart?

<p>It slows it down (C)</p> Signup and view all the answers

What is the primary therapeutic use of muscarinic antagonists?

<p>Dilating the bronchi in the lung (B)</p> Signup and view all the answers

What is the duration of action for bethanechol when administered orally?

<p>30-60 minutes (D)</p> Signup and view all the answers

Why are cholinergic drugs not recommended for the elderly population?

<p>They affect receptors causing unwanted side effects (A)</p> Signup and view all the answers

What is the main effect of bethanechol on smooth muscle in the lung?

<p>Constriction of bronchi (C)</p> Signup and view all the answers

What is the primary therapeutic use of bethanechol?

<p>Treating urinary retention (D)</p> Signup and view all the answers

What is the adverse effect of bethanechol that can result in exacerbation of asthma?

<p>Increased motility of GI tract (B)</p> Signup and view all the answers

Which structure is mentioned as an exception among muscarinic agonists due to its ability to cross membranes easily?

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

What is the mnemonic used to remember the side effects of muscarinic poisoning?

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

What are the symptoms of muscarinic poisoning?

<p>Visual disturbances, bronchospasm, and hypotension (C)</p> Signup and view all the answers

What is the role of cholinesterase inhibitors in muscarinic poisoning?

<p>Exacerbating muscarinic symptoms (C)</p> Signup and view all the answers

Why should certain drugs like anti-histamines be used with caution in patients receiving muscarinic antagonists?

<p>They may have prominent anti-muscarinic actions (C)</p> Signup and view all the answers

What is the primary effect of cevimeline?

<p>Treating dry mouth in Sjogren's syndrome (D)</p> Signup and view all the answers

What are the pharmacologic effects of muscarinic receptor blockade caused by atropine?

<p>Increases heart rate, decreases secretions in exocrine glands, relaxes smooth muscle in the bronchi, and decreases the tone of the urinary bladder detrusor (D)</p> Signup and view all the answers

Which adverse effect is NOT associated with atropine use?

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

In which conditions can atropine be used therapeutically?

<p>Asthma and peptic ulcer disease (C)</p> Signup and view all the answers

What is the primary use of AtroPen?

<p>Cholinesterase inhibitor poisoning (A)</p> Signup and view all the answers

What is the alternative term for overactive bladder?

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

Which symptom is NOT associated with overactive bladder?

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

What is the primary effect of atropine on the eyes?

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

What is the route of administration for Atropine drops used in ophthalmology?

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

What effect does atropine have on the tone and motility of the GI tract?

<p><strong>Decreases</strong> tone and motility (B)</p> Signup and view all the answers

What is an example of a therapeutic use of atropine?

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

What adverse effect can result from atropine use?

<p>Elevation of interocular pressure (D)</p> Signup and view all the answers

Which formulation of oxybutynin provides the longest duration of action?

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

What is the main reason for the high incidence of dry mouth associated with oxybutynin use?

<p>Blockade by oxybutynin itself (B)</p> Signup and view all the answers

What is the unique feature of darifenacin that makes it well-tolerated?

<p>M3 selectivity (B)</p> Signup and view all the answers

Which drug interaction can alter oxybutynin blood levels?

<p>Inhibition of CYP3A4 (B)</p> Signup and view all the answers

What is a prominent side effect of darifenacin and oxybutynin in the pediatric and geriatric populations?

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

Which side effect is NOT associated with oxybutynin use?

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

What is the most common side effect associated with darifenacin use?

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

Which condition can be exacerbated by the side effects of oxybutynin and darifenacin?

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

What can intensify the anticholinergic side effects when used in combination with oxybutynin?

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

What is the primary effect of darifenacin on muscarinic receptors?

<p>M3 selectivity (B)</p> Signup and view all the answers

Which muscarinic antagonist is a CYP2D6 and CYP3A4 substrate?

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

What is the mechanism of action of Mirabegron?

<p>Activates adenylyl cyclase and forms cyclic adenosine monophosphate (C)</p> Signup and view all the answers

Which muscarinic antagonist is a moderate inhibitor of CYP2D6 and a minor inhibitor of CYP3A4?

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

Which muscarinic antagonist can cause QT prolongation and an increase in blood pressure?

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

What is the main adverse effect associated with Trospium?

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

What distinguishes Mirabegron from other drug classes in terms of producing a therapeutic effect?

<p>It activates beta-3-adrenoreceptors by norepinephrine. (B)</p> Signup and view all the answers

Which drugs have been evaluated as non-traditional therapies for overactive bladder?

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

What is the primary role of scopolamine?

<p>Production of cycloplegia (D)</p> Signup and view all the answers

Ipratropium bromide is used to treat which conditions?

<p>Asthma, COPD, and rhinitis caused by allergies or the common cold. (C)</p> Signup and view all the answers

What are the therapeutic uses of mydriatic-cycloplegics?

<p>To produce mydriasis and cycloplegia for ophthalmic procedures. (A)</p> Signup and view all the answers

What is the specific antidote to poisoning by the irreversible cholinesterase inhibitors?

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

What autoimmune process characterizes myasthenia gravis?

<p>Antibodies attack the nicotinic m receptors on the skeletal muscle (A)</p> Signup and view all the answers

Which drug does not cross the blood-brain barrier and will not reduce CNS effects?

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

What is the primary effect of neostigmine during myasthenic crisis?

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

What is the distinguishing factor between a cholinergic crisis and a myasthenic crisis when challenged with edrophonium?

<p>Increased muscle strength (B)</p> Signup and view all the answers

What is the initial treatment for a cholinergic crisis?

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

What is the role of benzodiazepine in a cholinergic crisis?

<p>Suppresses convulsions (B)</p> Signup and view all the answers

What can atropine be used for if muscarinic responses become excessive due to cholinesterase inhibitors?

<p>Suppress them (B)</p> Signup and view all the answers

What differentiates neostigmine and atropine in terms of their specific effects?

<p>Atropine reduces muscarinic stimulation, while neostigmine reverses inhibition of cholinesterase. (D)</p> Signup and view all the answers

What is the effect of pralidoxime in cholinergic crisis?

<p>Dissociating inhibitors from the active center of cholinesterase (B)</p> Signup and view all the answers

What is the specific antidote to poisoning by irreversible cholinesterase inhibitors?

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

Which drug does not readily cross membranes, has minimal effects on the brain and fetus, and is a poor substrate for cholinesterase?

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

What is the primary clinical application of irreversible cholinesterase inhibitors?

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

Which drug is viewed as an indirect acting cholinergic agonist, lacks muscarinic ganglionic and neuromuscular selectivity, and has limited therapeutic applications?

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

What are the symptoms of muscarinic poisoning?

<p>Dry mouth, blurred vision, photophobia, and hot, dry flush skin (D)</p> Signup and view all the answers

What is the role of atropine in the treatment of muscarine antagonist poisoning?

<p>Blocks muscarinic receptors (C)</p> Signup and view all the answers

What is the main adverse effect associated with trospium?

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

Which structure among muscarinic antagonists can cause QT prolongation and an increase in blood pressure?

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

What effect does atropine have on the eyes?

<p>Causes dilation of the pupils (D)</p> Signup and view all the answers

What is the primary effect of atropine on the ciliary muscle in the eyes?

<p>Relaxes the ciliary muscle (C)</p> Signup and view all the answers

Which of the following best describes the effect of atropine on the accommodation reflex in the eyes?

<p>Inhibits the accommodation reflex (B)</p> Signup and view all the answers

Which side effect is NOT commonly associated with oxybutynin use?

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

What can intensify the anticholinergic effects of oxybutynin when used in combination?

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

Which population is more likely to experience hallucinations and agitation as side effects of oxybutynin?

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

What is the primary difference in the metabolism of noncatecholamines compared to catecholamines?

<p>Noncatecholamines are not substrates for COMT and metabolize slowly by MAO. (C)</p> Signup and view all the answers

What is the therapeutic effect of activating alpha-1 receptors?

<p>Vasoconstriction in blood vessels of the skin, viscera, and mucous membranes (D)</p> Signup and view all the answers

What is the primary use of B2 receptor agonists?

<p>Treatment of asthma (C)</p> Signup and view all the answers

Which receptor activation is associated with the risk of angina in patients with compromised coronary circulation?

<p>Beta-1 receptors (B)</p> Signup and view all the answers

What effect does activation of B2 receptors have on the uterus?

<p>Relaxation of uterine smooth muscle (B)</p> Signup and view all the answers

Which receptor subtype does epinephrine act on?

<p>A1, A2, B1, B2 (C)</p> Signup and view all the answers

What is a potential adverse effect of B1 receptor activation?

<p><strong>Tachycardia</strong> (B)</p> Signup and view all the answers

Isoproterenol is less selective than albuterol because it acts at which receptors?

<p>B1 and B2 (A)</p> Signup and view all the answers

What is the effect of activating alpha-2 receptors in the central nervous system?

<p>Inhibition of NE release (B)</p> Signup and view all the answers

What is a potential adverse effect of oxybutynin due to its action on muscarinic receptors?

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

Activation of Dopamine receptors can improve perfusion to which organ?

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

Which group of adrenergic agonists cannot be used orally, has a brief duration of action, and cannot cross the blood-brain barrier?

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

What is the primary mechanism by which indirect adrenergic agonists work?

<p>Promotion of norepinephrine release (A)</p> Signup and view all the answers

Which enzyme is responsible for the quick metabolism of catecholamines?

<p>Monoamine oxidase [MAO] (B)</p> Signup and view all the answers

Which adrenergic agonist is known for its inability to be used orally, short duration of action, and inability to cross the blood-brain barrier?

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

Which major class of adrenergic agonists includes dopamine, epinephrine, isoproterenol, and ephedrine?

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

What distinguishes catecholamines from noncatecholamines in terms of their availability for oral use and duration of action?

<p>Availability for oral use and duration of action (A)</p> Signup and view all the answers

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