Muscarinic agonist direct and indirect
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Questions and Answers

Which enzyme is involved in the synthesis of acetylcholine?

  • Cholinergic Receptors
  • Acetylcholinesterase
  • Choline Acetyltransferase (correct)
  • Acetyl CoA

    • What is the term used for drugs that mimic the action of acetylcholine in the autonomic nervous system?

  • Muscarinic agonists
  • Parasympathomimetic drugs
  • Cholinergic neurotransmitters
  • Cholinomimetics (correct)

    • Which type of receptor is always stimulatory and is involved in the release of acetylcholine?

  • Muscarinic receptor
  • Nicotinic receptor (correct)
  • Autoreceptor
  • Alpha-2 receptor

    • Which receptor subtype is responsible for the excitatory negative chronotropic effect in the cardiovascular system?

    <p>M2</p> Signup and view all the answers

    Which receptor subtype is responsible for bronchoconstriction in the respiratory tract?

    <p>M3</p> Signup and view all the answers

    Which receptor subtype is responsible for bladder contraction in the urinary tract?

    <p>M3</p> Signup and view all the answers

    Which receptor subtype is responsible for miosis in the eye?

    <p>M3</p> Signup and view all the answers

    Which of the following is a therapeutic application of Pilocarpine?

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

    What is the most important and only modifiable risk factor for glaucoma?

    <p>Raised intraocular pressure</p> Signup and view all the answers

    Which of the following is a potential adverse effect of Pilocarpine?

    <p>Increased salivation</p> Signup and view all the answers

    Which of the following drugs is hydrolyzed by acetylcholinesterases at a relatively slow rate?

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

    What is the mechanism of action of Pilocarpine when applied locally to the cornea?

    <p>Produces rapid miosis</p> Signup and view all the answers

    Which drug has both muscarinic as well as nicotinic actions?

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

    Which drug is structurally related to acetylcholine, in which the acetate is replaced by carbamate?

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

    Which drug is used for urologic treatment and directly stimulates muscarinic receptors in smooth musculature of the bladder and gastrointestinal tract?

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

    Which enzyme is involved in the synthesis of acetylcholine?

    <p>Choline Acetyltransferase</p> Signup and view all the answers

    What is the term used for drugs that mimic the action of acetylcholine in the autonomic nervous system?

    <p>Cholinergic agonists</p> Signup and view all the answers

    What is the mechanism of action of Pilocarpine when applied locally to the cornea?

    <p>It stimulates muscarinic receptors</p> Signup and view all the answers

    Which of the following is a therapeutic use of methacholine?

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

    Which of the following drugs is rarely used therapeutically due to its high potency and non-selectivity of receptors?

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

    Which receptor subtype is responsible for vasodilation in the cardiovascular system?

    <p>M3</p> Signup and view all the answers

    Which drug is used for the treatment of neurogenic urinary retention and postoperative atony?

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

    Which drug is an irreversible anticholinesterase that phosphorylates acetylcholinesterase, leading to permanent enzyme inactivation?

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

    Which drug is used topically in the eye to produce miosis and spasm of accommodation, and is also used to treat glaucoma?

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

    Which drug is an indirect-acting cholinergic agonist that enhances cognitive function in patients with Alzheimer's Disease?

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

    Which drug is a K+ channel antagonist that prolongs excitability and slows down repolarization, leading to increased VCa2+ activation?

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

    Which of the following is a contraindication for the use of choline esters?

    <p>Gastric ulcers</p> Signup and view all the answers

    What is the therapeutic application of Pilocarpine in patients with Sjogren's syndrome?

    <p>Increase tear production</p> Signup and view all the answers

    What is the primary effect of acetylcholinesterase (AChE) inhibitors?

    <p>Prolongation of acetylcholine action</p> Signup and view all the answers

    Which enzyme is responsible for hydrolyzing acetylcholine at cholinergic synapses?

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

    Which organophosphate is more dangerous to humans and livestock compared to malathion?

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

    What is the main purpose of pralidoxime in reactivating acetylcholinesterase?

    <p>To approach an anionic site on the enzyme and displace the phosphate group of the organophosphate</p> Signup and view all the answers

    What is the limitation of using pralidoxime as a reactivator for acetylcholinesterase?

    <p>It is ineffective against newer nerve agents that produce fast aging of the enzyme</p> Signup and view all the answers

    Which of the following AChE inhibitors is reversible and forms a covalent bond with the enzyme?

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

    Which of the following AChE inhibitors is irreversible and has an extremely stable phosphorus-enzyme bond?

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

    Which of the following AChE inhibitors is used as a cholinesterase regenerator and can break the phosphorus-enzyme bond?

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

    Which of the following effects can be produced by anti-AChE agents?

    <p>All of the above effects</p> Signup and view all the answers

    ¿Cuál es el paso limitante de la síntesis de ACh en la neurotransmisión colinérgica?

    <p>Transporte de colina hacia la neurona presináptica</p> Signup and view all the answers

    ¿Qué tipo de receptores se activan directamente por los agonistas colinérgicos?

    <p>Receptores muscarínicos y nicotínicos</p> Signup and view all the answers

    ¿Cuál de los siguientes fármacos se utiliza en el diagnóstico de la miastenia gravis al aumentar rápidamente la fuerza muscular?

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

    ¿Cuál de los siguientes fármacos se utiliza para revertir los efectos de los bloqueadores neuromusculares no despolarizantes después de la cirugía?

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

    ¿Cuál de los siguientes fármacos se utiliza para el manejo crónico de la miastenia gravis debido a su acción prolongada?

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

    ¿Cuál es el subtipo predominante de receptor colinérgico en el control del músculo liso, las glándulas secretoras y el ojo?

    <p>M3</p> Signup and view all the answers

    ¿Cuál es el efecto de la acetilcolina (ACh) en el tracto respiratorio?

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

    ¿Cuál es el efecto de la acetilcolina (ACh) en el tracto urinario?

    <p>Aumento de la secreción de orina</p> Signup and view all the answers

    ¿Cuál es el tipo de receptor involucrado en la contracción de la vejiga en el tracto urinario?

    <p>Receptores M3</p> Signup and view all the answers

    ¿Cuál es el factor de riesgo más importante y el único modificable para el glaucoma?

    <p>Presión intraocular elevada</p> Signup and view all the answers

    ¿Cuál es el porcentaje de pacientes sin tratamiento que desarrollarán ceguera bilateral?

    <p>80%</p> Signup and view all the answers

    ¿Qué tipo de colinesterasa se encuentra presente en las sinapsis colinérgicas?

    <p>Acetilcolinesterasa (AChE)</p> Signup and view all the answers

    ¿Cuál de los siguientes inhibidores de AChE forma un enlace covalente irreversible con la enzima?

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

    ¿Cuál de los siguientes efectos adversos puede producir la metacolina en el sistema cardiovascular?

    <p>Bradicardia e hipotensión</p> Signup and view all the answers

    ¿Cuál de los siguientes fármacos es un agonista parcial que se utiliza para promover las secreciones glandulares?

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

    ¿Cuál de los siguientes fármacos se utiliza como fármaco de elección en emergencias de disminución de presión intraocular?

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

    ¿Cuál de las siguientes afirmaciones es correcta sobre la pilocarpina?

    <p>Es un agonista parcial de los receptores muscarínicos</p> Signup and view all the answers

    ¿Cuál de los siguientes receptores muscarínicos está involucrado en la modulación de la transmisión colinérgica en los ganglios autónomos?

    <p>M1</p> Signup and view all the answers

    ¿Cuál es el efecto observado al inyectar ACh intravenosa?

    <p>Disminución de la presión sanguínea</p> Signup and view all the answers

    ¿Qué efecto tiene la atropina en la presión sanguínea y la frecuencia cardíaca cuando se administra junto con ACh?

    <p>Aumenta la presión sanguínea y disminuye la frecuencia cardíaca</p> Signup and view all the answers

    ¿Cuál es el efecto de los receptores M3 en el endotelio del vaso sanguíneo?

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

    ¿Cuál es el mecanismo de acción de los inhibidores de la acetilcolinesterasa?

    <p>Inhiben la degradación de acetilcolina en las sinapsis colinérgicas.</p> Signup and view all the answers

    ¿Cuál es el efecto más prominente de los agentes anti-AChE en el sistema cardiovascular?

    <p>Estimulación de los ganglios parasimpáticos.</p> Signup and view all the answers

    ¿Cuál es la principal diferencia entre los agentes anti-AChE y los agonistas colinomiméticos de acción directa?

    <p>Los agentes anti-AChE tienen una acción más prolongada.</p> Signup and view all the answers

    ¿Cuál es la función principal de la pralidoxima en la reactivación de la acetilcolinesterasa?

    <p>Romper el enlace fósforo-enzima en los organofosfatos.</p> Signup and view all the answers

    Which Muscarinic agonist?

    Bladder Contraction

    Signup and view all the answers

    Which Muscarinic agonist? Stimulate secreciones

    Signup and view all the answers

    Which Muscarinic agonist? Negative chronotropic effect

    Signup and view all the answers

    Which Muscarinic agonist? Vasodilatacion

    Signup and view all the answers

    Which Muscarinic agonist? Urine Formation

    Signup and view all the answers

    Which Muscarinic agonist? Miosis

    Signup and view all the answers

    Study Notes

    Acetylcholine Synthesis and Function

    • Choline acetyltransferase is the enzyme involved in the synthesis of acetylcholine.

    Cholinergic Agonists

    • Cholinomimetics are drugs that mimic the action of acetylcholine in the autonomic nervous system.
    • Pilocarpine is a cholinomimetic used to treat glaucoma and dry mouth in patients with Sjogren's syndrome.

    Muscarinic Receptors

    • M1 receptors are involved in bladder contraction in the urinary tract.
    • M2 receptors are responsible for the negative chronotropic effect in the cardiovascular system.
    • M3 receptors are responsible for bronchoconstriction in the respiratory tract and vasodilation in the cardiovascular system.
    • M4 receptors are involved in miosis in the eye.

    Cholinesterase Inhibitors

    • Acetylcholinesterase (AChE) is the enzyme responsible for hydrolyzing acetylcholine at cholinergic synapses.
    • Neurotoxins like organophosphates can inhibit AChE, leading to accumulation of acetylcholine.
    • Pralidoxime is used to reactivate AChE inhibited by organophosphates.

    Therapeutic Applications

    • Methacholine is used to diagnose myasthenia gravis and to treat urinary retention and postoperative atony.
    • Pilocarpine is used to treat glaucoma and dry mouth in patients with Sjogren's syndrome.
    • Cholinesterase inhibitors like donepezil are used to treat Alzheimer's disease.

    Pharmacology

    • Bethanechol is a cholinergic agonist used to stimulate gastrointestinal motility and bladder contraction.
    • Carbachol is a cholinergic agonist used to treat glaucoma and induce miosis.
    • Neostigmine is a cholinesterase inhibitor used to treat myasthenia gravis and reverse the effects of non-depolarizing neuromuscular blockers.

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    Related Documents

    Direct Agonists PDF
    Cholinergic System Muscarinic Agonists PDF
    Sistema Colinérgico -Agonistas Muscarínicos- PDF

    Description

    Test your knowledge on synthetic compounds and their effects on nicotinic receptors. This quiz explores the affinity of synthetic compounds for specific receptors and their impact on cardiac function.

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