Autonomic Nervous System and Parasympathetic Drugs
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Questions and Answers

What type of receptors do both the sympathetic and parasympathetic nervous systems use at the synapses between preganglionic and postganglionic neurons?

  • Alpha-adrenergic receptors
  • Nicotinic ACh receptors (correct)
  • Muscarinic ACh receptors
  • Beta-adrenergic receptors

Which drug is a non-competitive antagonist of autonomic nicotinic ACh receptors?

  • Hexamethonium (correct)
  • Muscarine
  • Atropine
  • Pilocarpine

What is the primary effect of Muscarinic M2 receptors in cardiac muscle?

  • Activate phospholipase C
  • Facilitate smooth muscle contraction
  • Increase cAMP levels
  • Inhibit adenylyl cyclase (correct)

Which of the following actions is NOT associated with muscarinic agonists?

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

Which subtype of muscarinic receptors is primarily found in the stomach and salivary glands?

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

What structural characteristic differentiates nicotinic ACh receptors in the autonomic nervous system from those in skeletal muscle?

<p>Number of subunits (A)</p> Signup and view all the answers

Hexamethonium has largely fallen out of use mainly due to what reason?

<p>Significant side effects (B)</p> Signup and view all the answers

What is a potential consequence of muscarine poisoning?

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

What is the primary action of NAT inhibitors on norepinephrine (NA)?

<p>Decrease NA reabsorption, prolonging sympathetic activation (A)</p> Signup and view all the answers

Which of the following side effects is NOT associated with MAO inhibitors?

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

What potential effect can occur from consuming cheese while taking MAO inhibitors?

<p>Severe headaches and palpitations (A)</p> Signup and view all the answers

Which drug is commonly known to function as a NAT inhibitor?

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

What is a common effect of sympathetic amines on the body?

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

Which of the following best describes the role of MAO in the presence of norepinephrine?

<p>Degrades NA, maintaining normal levels (D)</p> Signup and view all the answers

Which class of drugs is structurally similar to norepinephrine and can lead to increased release of NA?

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

What could be a consequence of prolonged use of DAT and SERT inhibitors like cocaine?

<p>Withdrawal symptoms including anxiety (B)</p> Signup and view all the answers

Which of the following symptoms is NOT associated with extreme parasympathetic effects?

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

What is the primary action of atropine when used in poisoning cases?

<p>Act as a competitive antagonist for muscarine (C)</p> Signup and view all the answers

Pilocarpine is primarily used to treat which condition?

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

Which of the following is a muscarinic antagonist used to manage bradycardia?

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

The effects of which class of drugs can be countered by using muscarinic agonists?

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

Which receptor is responsible for causing vasoconstriction through Gq pathway activation?

<p>α1 (C)</p> Signup and view all the answers

What is the primary effect of beta-2 adrenoceptors?

<p>Relax smooth muscle (C)</p> Signup and view all the answers

What is the role of α2 receptors in the sympathetic nervous system?

<p>Inhibit release of noradrenaline (B)</p> Signup and view all the answers

What is the primary mechanism through which β3 adrenoceptors achieve their effects?

<p>Activation of adenylyl cyclase (A)</p> Signup and view all the answers

Which of the following is a therapeutic use of α1 adrenoceptor agonists?

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

Which drug is commonly used to treat hypertension by acting on α1 receptors?

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

What is a common use for β2 adrenoceptor agonists?

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

What physiological role does noradrenaline play in the sympathetic nervous system?

<p>Activates G-protein coupled receptors (D)</p> Signup and view all the answers

Which drug targets β1 receptors specifically to improve cardiac function?

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

Which enzyme is primarily responsible for synthesizing noradrenaline from tyrosine?

<p>Dopamine β-hydroxylase (C)</p> Signup and view all the answers

Which condition is treated by β-adrenoceptor antagonists?

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

Flashcards

Nicotinic ACh Receptor (ANS)

A type of acetylcholine receptor found in the autonomic nervous system (ANS) at synapses between preganglionic and postganglionic neurons. It is also found in skeletal muscles, but the structure is different.

Hexamethonium

A drug that blocks the effects of acetylcholine at nicotinic receptors in the ANS. It does not affect skeletal muscle.

Muscarinic ACh Receptor

A type of acetylcholine receptor found in the parasympathetic nervous system (PaNS) at synapses between postganglionic neurons and effector organs. It is a G-protein coupled receptor.

Muscarinic Agonist (Parasympathomimetic)

A drug that activates muscarinic receptors, mimicking the effects of parasympathetic stimulation.

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M1 Muscarinic Receptor

Present in the stomach and salivary glands. It is a Gq receptor, activating phospholipase C (PLC) leading to increased secretion.

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M2 Muscarinic Receptor

Present in cardiac muscle. It is a Gi receptor, inhibiting adenylyl cyclase, reducing cAMP levels and decreasing heart rate.

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M3 Muscarinic Receptor

Present in smooth muscle (e.g. eyes, bronchi) and exocrine glands. It is a Gq receptor, activating PLC, leading to smooth muscle contraction and increased secretions.

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Muscarine Poisoning

A condition caused by ingesting mushrooms containing muscarine, resulting in excessive stimulation of muscarinic receptors.

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Muscarinic receptor

A type of cholinergic receptor that is activated by acetylcholine (ACh), primarily responsible for parasympathetic nerve responses.

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Muscarinic antagonist

A drug that blocks the action of acetylcholine at muscarinic receptors, effectively reducing the effects of the parasympathetic nervous system.

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Muscarinic agonist

A medication that stimulates muscarinic receptors, mimicking the effects of acetylcholine and causing parasympathetic responses.

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ACh Esterase Inhibitors

A group of drugs that block the breakdown of acetylcholine by inhibiting the enzyme acetylcholinesterase (AChE). This leads to an increase in acetylcholine levels at synapses.

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Adrenoceptors

A family of G-protein coupled receptors that respond to the neurotransmitter norepinephrine (noradrenaline). They are found throughout the body and play a crucial role in the sympathetic nervous system.

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Alpha-1 (α1) adrenoceptor

A type of adrenoceptor that is activated by norepinephrine and causes smooth muscle contraction, such as vasoconstriction.

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Alpha-2 (α2) adrenoceptor

A type of adrenoceptor that is activated by norepinephrine and is involved in vasoconstriction, inhibition of norepinephrine release, and reducing sympathetic outflow from the central nervous system.

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Beta-1 (β1) adrenoceptor

A type of adrenoceptor that is activated by norepinephrine and is primarily responsible for increasing heart rate and contractility.

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β3 Adrenoceptor

A type of adrenergic receptor that activates adenylyl cyclase, increasing intracellular cAMP levels. It is involved in smooth muscle relaxation and lipolysis.

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Adrenergic Agonists

Adrenergic agonists are drugs that stimulate adrenergic receptors, mimicking the effects of adrenaline and noradrenaline. They can be further classified based on the specific adrenergic receptor they target.

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Adrenergic Antagonists

Adrenergic antagonists, also called blockers, inhibit the effects of adrenergic receptors by blocking the binding of adrenaline and noradrenaline. They are used to treat a variety of conditions, including hypertension and Benign Prostatic Hyperplasia (BPH).

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α-adrenoceptor agonists

A type of adrenergic receptor that causes vasoconstriction, primarily through α1 receptors. It plays a role in regulating blood pressure and has other applications in medicine, such as nasal decongestant.

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α-adrenoceptor antagonists

A type of adrenergic receptor that causes vasodilation through α1 receptors. It is used to treat conditions like hypertension and BPH by relaxing smooth muscle in blood vessels and the prostate.

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β-adrenoceptor agonists

A type of adrenergic receptor that increases heart rate and contractility, primarily through β1 receptors. It is used to treat conditions like heart failure and anaphylactic shock, where the heart needs to pump more efficiently.

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β-adrenoceptor agonists (Asthma treatment)

A type of adrenergic receptor that causes bronchodilation through β2 receptors, relaxing the smooth muscle of the bronchi. It is used to treat conditions like asthma, where the airways are constricted.

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β-adrenoceptor antagonists (Beta-blockers)

A type of adrenergic receptor that slows down the heart rate, primarily through β1 receptors. It is used to treat various conditions, including hypertension, angina, and anxiety.

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What are NAT inhibitors?

Drugs that prevent the reuptake of norepinephrine (NA) by neurons, increasing its concentration in the synaptic cleft.

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What are MAO inhibitors?

Drugs that block the enzyme monoamine oxidase (MAO), which breaks down norepinephrine (NA) in neurons, leading to increased NA levels.

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What are sympathetic amines?

Drugs that are structurally similar to norepinephrine (NA) and can displace NA from its storage vesicles, leading to increased NA release.

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What is the 'cheese reaction'?

A side effect of MAO inhibitors where consumption of tyramine-rich foods (like cheese) can cause severe increases in blood pressure due to the interaction of tyramine with MAO inhibition.

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Give examples of NAT inhibitors.

Desipramine is an antidepressant, while cocaine is a local anesthetic.

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Give examples of MAO Inhibitors.

Moclobemide is a mild MAO inhibitor, while phenelzine is a stronger one.

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Give examples of sympathetic amines.

Amphetamine is a stimulant, ephedrine is a nasal decongestant, and tyramine is found in aged cheese.

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How do drugs targeting norepinephrine (NA) affect other neurotransmitters?

NAT inhibitors can also affect dopamine and serotonin transporters, leading to side effects like euphoria and excitement. MAO inhibitors can also lead to increased dopamine and serotonin levels, causing side effects like restlessness and insomnia.

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Study Notes

Autonomic Nervous System Drugs

  • Drugs targeting the entire autonomic nervous system affect both sympathetic and parasympathetic branches.
  • Nicotinic ACh receptors are found at synapses between preganglionic and postganglionic neurons in both these branches.
  • Nicotinic ACh receptors are pentameric transmembrane ion channels. Skeletal muscle AChRs use α1 subunits while ANS receptors use α2-7 subunits.
  • Hexamethonium is a non-competitive antagonist for nicotinic ACh receptors in the autonomic nervous system. It blocks both sympathetic and parasympathetic effects, but not the effects on skeletal muscle.

Parasympathetic Nervous System Drugs

  • Postganglionic neurons of the parasympathetic nervous system (PaNS) use muscarinic ACh receptors to affect effectors.
  • Muscarinic receptors consist of 7 transmembrane domains and are G-protein-coupled.
  • M1 receptors are found in the stomach and salivary glands, using Gq and activating phospholipase C (PLC), while M2 receptors are in cardiac muscle, using Gi to inhibit adenylyl cyclase and reduce cAMP.
  • M3 receptors are in smooth muscle (eyes, bronchi) and exocrine glands, using Gq and activating PLC.
  • Muscarinic agonists (parasympathomimetics) mimic parasympathetic stimulation, causing decreased heart rate, vasodilation, smooth muscle contraction (gut, respiratory tract), salivation, lacrimation and bronchial mucous secretions.

Sympathetic Nervous System Drugs

  • Sympathetic postganglionic neurons utilize noradrenaline (NA) as a neurotransmitter.
  • Adrenoceptors are G-protein-coupled receptors. There are five types: α1, α2, β1, β2, and β3.
  • α1 receptors cause smooth muscle contraction (vasoconstriction) using Gq and activating PLC.
  • α2 receptors cause vasoconstriction, inhibit NA release, and modulate sympathetic outflow via Gi and inhibiting adenylyl cyclase.
  • β1 receptors increase heart rate and contractility using Gs and activating adenylyl cyclase and increase cAMP.
  • β2 receptors relax smooth muscle (bronchi, blood vessels, bladder) using Gs and activating adenylyl cyclase and increase cAMP.
  • β3 receptors also relax smooth muscle, especially in the bladder and stimulate lipolysis, using Gs and activating adenylyl cyclase and increase cAMP.

Catecholamine Regulation Drugs

  • Synthesis of noradrenaline (NA) proceeds from tyrosine with dopamine as an intermediate.
  • NA acts on receptors then is reabsorbed into the presynaptic bulb via NA transporter protein (NAT), to terminate its action.
  • Some NA is broken down by monoamine oxidase (MAO) enzymes.
  • NAT inhibitors prevent reuptake of NA, causing prolonged sympathetic effects.
  • MAO inhibitors block the breakdown of NA enhancing sympathetic effects and increasing NA levels in the presynaptic neurons.
  • Sympathomimetic amines are structurally similar to NA and mimic NA actions, by entering neurons and displacing NA to increase its effect.

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L17 Autonomic Pharmacology PDF

Description

Test your knowledge on the drugs influencing the autonomic nervous system, including both sympathetic and parasympathetic branches. This quiz covers key receptors such as nicotinic and muscarinic ACh receptors, their functions, and specific drug interactions.

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