Cholinergic Drugs (Parasympathetic)
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Questions and Answers

What is the primary action of Isoproterenol on the heart?

  • Increase diastolic blood pressure
  • No effect on heart rate
  • Decrease heart rate and contractility
  • Increase heart rate and contractility (correct)

    • Which receptor does Phenylephrine selectively act upon?

  • B2 receptor
  • a2 receptor
  • a1 receptor (correct)
  • B1 receptor

    • What is a caution associated with the use of Phenylephrine in elderly patients?

  • Increased risk of hypertension (correct)
  • Increased risk of hypotension
  • Increased risk of arrhythmias
  • Lowered effectiveness as a nasal decongestant

    • What effect does stimulation of B2 receptors have on total peripheral resistance (TPR)?

    <p>Decreases total peripheral resistance (C)</p> Signup and view all the answers

    Which of the following statements about selective drugs is accurate at high concentrations?

    <p>They lose selectivity and affect other receptors (C)</p> Signup and view all the answers

    What is the primary effect of MAO inhibitors in treating Parkinson's disease?

    <p>Block metabolism of dopamine (B)</p> Signup and view all the answers

    What condition may result from consuming foods high in tyramine while on MAO inhibitors?

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

    What kind of adrenergic receptors does Ephedrine primarily act on?

    <p>Non-selective alpha and beta (B)</p> Signup and view all the answers

    Which effect is NOT associated with the use of alpha blockers?

    <p>Increase in heart rate (C)</p> Signup and view all the answers

    Which side effect is most commonly associated with the use of non-selective alpha antagonists?

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

    What is the main therapeutic use of non-selective alpha antagonists like Phentolamine?

    <p>For the management of hypertension during surgery (C)</p> Signup and view all the answers

    How do COMT inhibitors function in regards to catecholamines?

    <p>Block degradation of catecholamines (D)</p> Signup and view all the answers

    Which of the following is an effect of mixed acting sympathomimetics like Ephedrine?

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

    What is a potential adverse effect of phenoxybenzamine due to its irreversible action?

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

    What mechanism does Selegiline utilize in treating depression?

    <p>Blocking MAO-A metabolism (B)</p> Signup and view all the answers

    What is the primary mechanism of action of artemisinin compounds in treating malaria?

    <p>Generating highly reactive free radicals (C)</p> Signup and view all the answers

    Which condition can result from the use of sulfadoxine in Fansidar?

    <p>Steven Johnson’s syndrome (C)</p> Signup and view all the answers

    Which antibiotic is commonly used in combination with quinine for treating malaria?

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

    What is the primary effectiveness of primaquine in malaria treatment?

    <p>Radical cure and prevention of relapse (B)</p> Signup and view all the answers

    What is a notable side effect of atovaquone?

    <p>GI adverse effects (D)</p> Signup and view all the answers

    Which drug combination is the recommended first line treatment for multidrug-resistant falciparum malaria?

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

    Which of the following statements about proguanil is true?

    <p>Inhibits the enzyme dihydrofolate reductase (A)</p> Signup and view all the answers

    Why is doxycycline not recommended for children?

    <p>Bone and teeth deformities (A)</p> Signup and view all the answers

    What stage of malaria does primaquine specifically target?

    <p>Primary and latent hepatic stages (C)</p> Signup and view all the answers

    Which statement about Fansidar is correct?

    <p>Acts as a slow-acting blood schizonticide. (C)</p> Signup and view all the answers

    What is the primary mechanism of action of Dantrolene?

    <p>Interferes with calcium release from the SR (C)</p> Signup and view all the answers

    Which of the following is a significant side effect of Tizanidine?

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

    Which adrenergic receptor subtype primarily results in bronchial dilation when stimulated?

    <p>b2 (C)</p> Signup and view all the answers

    In which clinical situation is adrenaline primarily utilized?

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

    What effect does Noradrenaline have on heart rate?

    <p>Causes reflex bradycardia (A)</p> Signup and view all the answers

    What is the function of b3 adrenergic receptors?

    <p>Lipolysis in adipose tissue (A)</p> Signup and view all the answers

    What condition is associated with the use of Dopamine at low concentrations?

    <p>Increased renal blood flow (D)</p> Signup and view all the answers

    What adverse effect can be anticipated from using Dantrolene?

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

    Which of the following effects is associated with alpha 1 adrenergic receptors?

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

    Which neurotransmitter is responsible for activating b1 receptors to stimulate the heart?

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

    What is the primary clinical use of Dopamine?

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

    What effect does stimulation of b2 receptors have on the uterus?

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

    Which drug binds non-selectively to all adrenergic receptors?

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

    In addition to treating shock, what is a common use of Noradrenaline?

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

    Which of the following pharmacological effects is primarily associated with M2 muscarinic receptors?

    <p>Inhibit neurotransmitter release (C)</p> Signup and view all the answers

    What is the main therapeutic use of Methacholine?

    <p>Diagnosis of bronchial hyperreactivity (C)</p> Signup and view all the answers

    Which adverse effect is associated with the use of Pilocarpine?

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

    What is the mechanism of action of cholinesterase inhibitors?

    <p>Block AChE, causing ACh accumulation (B)</p> Signup and view all the answers

    Which receptor type is targeted by Nicotine as a nicotinic agonist?

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

    What is a significant pharmacological effect of M3 receptor activation?

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

    Which of the following is an example of a reversible acetylcholinesterase inhibitor?

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

    What is a primary clinical use of Acetylcholine as a drug?

    <p>Surgery requiring miosis (C)</p> Signup and view all the answers

    What is a characteristic of the pharmacokinetics of Acetylcholine?

    <p>Rapid inactivation by cholinesterase (B)</p> Signup and view all the answers

    Which type of muscarinic receptors facilitate increased gastric secretions and motility?

    <p>M1 receptors (D)</p> Signup and view all the answers

    What adverse effect is commonly associated with excessive stimulation of M3 receptors?

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

    Which of the following drugs is an example of a nicotinic agonist used for skeletal muscle contraction?

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

    What mechanism causes the decrease in intraocular pressure (IOP) when using Pilocarpine?

    <p>Increased drainage of aqueous humor (D)</p> Signup and view all the answers

    Why is Acetylcholine not frequently used clinically despite its effects?

    <p>Rapid inactivation and short duration (B)</p> Signup and view all the answers

    What is the primary clinical use of Prazosin?

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

    Which drug is preferred for the treatment of benign prostatic hyperplasia (BPH)?

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

    What effect do beta blockers primarily have on the heart?

    <p>Decrease heart rate (A)</p> Signup and view all the answers

    Which of the following is an adverse effect of Propranolol?

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

    What is an effect of beta-3 adrenergic receptor activation?

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

    Which medication is known to have intrinsic sympathomimetic activity (ISA)?

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

    What action can Labetalol have during pregnancy?

    <p>Decrease systemic arterial BP (C)</p> Signup and view all the answers

    Which drug is specifically indicated for treating hypertension in diabetic patients?

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

    What condition can Chloroquine be used to treat?

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

    Yohimbine acts as a selective blocker for which adrenergic receptors?

    <p>Alpha-2 (D)</p> Signup and view all the answers

    Which drug is contraindicated in patients with asthma?

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

    Which condition is Tamsulosin primarily used to treat?

    <p>Benign prostatic hyperplasia (D)</p> Signup and view all the answers

    What is a potential adverse effect of using Atenolol?

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

    What is the mechanism of action of Chloroquine in treating malaria?

    <p>Prevents conversion of trophozoites (A)</p> Signup and view all the answers

    Study Notes

    Cholinergic Drugs (Parasympathetic)

    • Cholinergic drugs mimic the parasympathetic nervous system
    • Direct-acting muscarinic agonists:
      • Increase secretions (salivation, gastric)
      • Bronchoconstriction, miosis (pupil constriction)
      • Lower intraocular pressure
      • Myocardial suppression
    • Acetylcholine:
      • Primarily controlled by inhibitory Gi-coupled M2 and excitatory Gq-coupled M3 muscarinic acetylcholine receptors (mAChRs)
      • Short duration of action
    • Methacholine:
      • Non-selective muscarinic receptor agonist
      • Increases gastric secretions, suppresses myocardial contraction
      • Used to diagnose bronchial hyperreactivity
      • Side effects: Bradycardia, hypotension, sweating, flushing
    • Pilocarpine:
      • Applied locally to eye to induce miosis, lower intraocular pressure, increase secretions
      • Used to diagnose bronchial hyperreactivity, and in surgeries requiring miosis
      • Side effects: Local irritation, blurred vision, GIT hyperreactivity
    • Direct-acting Nicotinic agonists:
      • NM (neuromuscular junction) - skeletal muscle contraction
      • NN (autonomic ganglia) - facilitate neurotransmission
      • Examples: Nicotine, Suxamethonium chloride

    Indirect Acting: Cholinesterase Inhibitors

    • Inhibit acetylcholinesterase (AChE), causing acetylcholine accumulation
    • Reversible short acting: Edrophonium
      • Used to diagnose myasthenia gravis
      • Increases muscle strength
    • Reversible medium acting: Neostigmine
      • Treats myasthenia gravis, and paralytic ileus
      • Increases strength for hours
    • Reversible long acting: Physostigmine
      • Treats myasthenia gravis, glaucoma, anticholinergic poisoning
      • Longer duration of action
    • Irreversible:
      • Organophosphates (nerve gases):
        • Binds to AChE permanently
        • Causes accumulation of acetylcholine

    Cholinergic Blockers

    • Inhibit the effects of acetylcholine
    • Muscarinic antagonists:
      • Atropine:
        • Reduces secretions (dry mouth)
        • Pupil dilation (mydriasis)
      • Scopolamine:
        • Motion sickness
        • Anti-cholinergic toxicity
      • Ipratropium:
        • Used in COPD
        • Side Effects: Restlessness, blurred vision, increased IOP, inhibition of sweat, dry mouth
    • Ganglion blocking agent:
      • Hexamethonium:
        • Reduces secretions
        • Causes muscle weakness and paralysis (at high doses)

    Neuromuscular Blockers

    • Non-depolarizing: Tubocurarine
      • Used for endotracheal intubation and surgery
      • Competitive antagonist, preventing Ach binding
      • Blocks ACh receptors, inhibiting neuromuscular transmission
    • Depolarizing: Succinylcholine
      • Causes initial depolarization, followed by desensitization
      • Used for intubation, and muscle relaxation during surgery

    Spasmolytics

    • Baclofen:
      • GABA agonist
      • Relieves excitation, relieving muscle spasms
    • Tizanidine:
      • Acts on alpha-2 receptors to reduce spasticity
      • Reducing muscle spasms and pain from multiple sclerosis

    Adrenergic Agonists

    • a1 receptors:
      • Excitatory
      • Vasoconstriction, contraction, mydriasis
    • a2 receptors:
      • Inhibitory
      • Inhibition of transmitter release
    • b1 receptors:
      • Excitatory
      • Myocardial stimulation, renin secretion
    • b2 receptors:
      • Inhibitory
      • Muscle relaxation, vasodilation
    • b3 receptors:
      • Excitatory
      • Lipolysis

    Adrenergic Antagonists

    • Alpha antagonists:

      • Non-selective (phenoxybenzamine, phentolamine):
        • Relaxes muscles around prostate
        • Used to diagnose and treat pheochromocytoma
      • Selective (prazosin, tamsulosin):
        • Treats benign prostatic hyperplasia (BPH)
      • Selective (Yohimbine):

    • Beta antagonists:

      • Non-selective (propranolol):
        • Treats hypertension, angina, tremor
      • Cardio-selective (metoprolol, atenolol):
        • Treats hypertension, angina
      • Intrinsic sympathomimetic activity (ISA) (pindolol, acebutolol):

    Drugs for Malaria

    • Chloroquine:

      • Effective against erythrocytic stages
      • Large Vd and extensive tissue binding
      • Blocks parasite's food source

    • Quinine:

      • Treats severe and resistant P. falciparum malaria, RA
      • Higher sensitivity in CQ resistant parasites

    • Artemisinin compounds:

      • Generates highly reactive free radicals, effective against all stages

    • Sulfadoxine-pyrimethamine:

      • Effective against all stages
      • Inhibits DHPS and DHFR

    Antibiotics (for Malaria, not for general infection)

    • Group II:
      • Tetracycline/doxycycline/clindamycin
      • Inhibit protein synthesis
    • Group III
      • Primaquine (Inhibits respiratory processes, effective against primary and latent hepatic stages)
      • Proguanil (Blocks parasite reproduction)
      • Atovoquone (Interferes with parasite mitochondrial function; effective against the primary liver forms)

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    Description

    This quiz explores the functions and effects of cholinergic drugs within the parasympathetic nervous system. It covers direct-acting muscarinic agonists, their mechanisms, and specific drugs like acetylcholine, methacholine, and pilocarpine._ Test your knowledge on their uses, side effects, and therapeutic implications.

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