Neurotransmission and Drugs

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Questions and Answers

What is the primary focus of the lectures based on the information provided?

  • Detailing surgical procedures involving the nervous system.
  • Listing all known neurotransmitters and their exact functions.
  • Explaining neurotransmission and how drugs can modify it. (correct)
  • Describing the anatomy of the brain.

Neurotransmission is not a target for therapeutic drugs.

False (B)

Which of the following is a primary component of a neuron?

  • Cell body (correct)
  • Salivary gland
  • Bronchi
  • Abdominal blood vessel

Local anesthetics inhibit nerve conduction by blocking ______ channels.

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

Match the following neurotransmitters with their associated nervous system component:

<p>Noradrenaline = Sympathetic terminals Acetylcholine = Parasympathetic terminals, ganglia, &amp; NMJ Dopamine = Parts of CNS Serotonin = Parts of CNS</p> Signup and view all the answers

Which neurotransmitter is primarily associated with the sympathetic nervous system?

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

The ganglia of the parasympathetic nervous system are typically located far from the target tissues.

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

The sympathetic nervous system emanates from the ______ segments of the spinal cord.

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

Which outflow is associated with the parasympathetic nervous system?

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

The sympathetic ganglia are typically close to the spinal cord in the paravertebral chain.

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

What triggers the release of neurotransmitters at the neuroeffector junction?

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

What ion influx directly triggers exocytosis of neurotransmitters at the nerve terminal?

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

L-DOPA is used therapeutically to increase ______ levels in the brains of patients with Parkinson's disease.

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

Inhibiting the termination of neurotransmission generally decreases the effect of the neurotransmitter.

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

Match these drugs with their primary mechanism of action on neurotransmitters:

<p>Cocaine = Inhibits reuptake of noradrenaline Fluoxetine = Inhibits reuptake of serotonin Neostigmine = Inhibits the enzyme acetylcholinesterase</p> Signup and view all the answers

What is the primary action of an agonist on a receptor?

<p>Stimulates the receptor. (B)</p> Signup and view all the answers

An antagonist has affinity and efficacy at a receptor.

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

What are the two main characteristics of an agonist?

<p>Affinity and efficacy</p> Signup and view all the answers

The drug ______ acts on a site different from the GABA binding site to enhance the effects of GABA.

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

Match the following receptor agonists with their therapeutic uses:

<p>Salbutamol = Asthma Phenylephrine = Decongestant Bromocriptine = Parkinson's Disease Morphine = Pain relief</p> Signup and view all the answers

Which of the following drugs is a receptor antagonist used as a pre-medication?

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

Sildenafil (Viagra) directly enhances the production of nitric oxide in erectile tissue.

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

Which of the following is NOT a typical site of drug action in neurotransmission?

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

What is the function of the enzyme acetylcholinesterase?

<p>Breaks down acetylcholine</p> Signup and view all the answers

The use of guanethidine can ______ the terminal depolarization.

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

Which of the following drugs inhibits vesicle fusion?

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

Clonidine is an α₂ antagonist that increases noradrenaline release.

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

Match the following site of drug action in neurotransmission with the drug or process:

<p>Inhibitory Effect on Precursor Uptake = Hemicholinium Inhibitory Effect on Enzyme Cascade = AMPT Inhibitory Effect on Storage = Reserpine</p> Signup and view all the answers

Which of the following is the direct result of the action potential at the neuroeffector junction?

<p>Opening of voltage-operated calcium channels (A)</p> Signup and view all the answers

The effect of a neurotransmitter is solely determined by its concentration in the synaptic cleft.

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

What geometry allows the diffusion of the neurotransmitter?

<p>Geometry of the cleft</p> Signup and view all the answers

[Blank] is used to reverse relaxation in surgery.

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

What is the function of benzodiazepine tranquillisers?

<p>Enhance channel opening and potentiate inhibitory effects of GABA. (D)</p> Signup and view all the answers

Receptors are not an important consideration in developing drugs with reduced side effects.

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

What effect does AMPT have on NA?

<p>Inhibitory effect on enzyme cascade</p> Signup and view all the answers

Botulinum inhibits ______ fusion.

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

Match the following sites of drug action with their corresponding effect:

<p>Synthesis = Inhibition of transmitter production Storage = Prevents neurotransmitter storage Release = Blocks calcium channels Receptors = Blocks receptor activation Cessation = Blocks reuptake</p> Signup and view all the answers

Which of the following is the primary reason why the synapse is an important target for drug action?

<p>It is the site of neurotransmission. (C)</p> Signup and view all the answers

Drugs that affect neurotransmitter synthesis always increase neurotransmitter concentrations.

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

Name three main routes of the sympathetic nerves.

<p>Tissue, Ganglion and parasympathetic nerves and Spinal Cord</p> Signup and view all the answers

An inhibitory effect on ____ _______ inhibits dopamine

<p>Enzyme Cascade</p> Signup and view all the answers

Which of the following best describes the aim of the lectures?

<p>To describe neurotransmission and how it can be modified by drugs. (B)</p> Signup and view all the answers

Local anesthetics inhibit nerve conduction by blocking potassium channels.

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

Which neurotransmitter is primarily associated with sympathetic terminals?

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

Where are the ganglia typically located in the sympathetic nervous system?

<p>Close to the spinal cord in the paravertebral chain (C)</p> Signup and view all the answers

In the parasympathetic nervous system, the _ outflow consists of cranial and sacral components.

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

Which of the following directly triggers the release of neurotransmitters at the neuroeffector junction?

<p>Depolarization leading to calcium influx. (B)</p> Signup and view all the answers

How does L-DOPA act therapeutically in Parkinson's disease?

<p>By increasing dopamine levels in the brain. (D)</p> Signup and view all the answers

Guanethidine inhibits action potential in nerve terminals. True or False?

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

______ such as fluoxetine, inhibit 5-HT uptake.

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

What is the key difference between an agonist and an antagonist in terms of receptor action?

<p>affinity and efficacy</p> Signup and view all the answers

Flashcards

Neurotransmission

The process by which neurons communicate with each other or with target tissues.

Neuron

A nerve cell that transmits electrical impulses.

Dendrites

Branchlike extensions of a neuron that receive signals from other neurons.

Axon

The long, slender projection of a neuron that conducts electrical impulses away from the cell body.

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Nerve terminal

The terminal portion of a neuron's axon that releases neurotransmitters.

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Neurotransmitter (NT)

A chemical substance released by a neuron to transmit signals to another neuron or target tissue.

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Ganglion

A cluster of nerve cell bodies outside the central nervous system.

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Sympathetic Nerves

Nerves originating from the thoracic and lumbar segments of the spinal cord, responsible for 'fight or flight'.

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Parasympathetic Nerves

Nerves originating from the cranial and sacral regions, promoting 'rest and digest' functions.

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Neuromuscular Junction (NMJ)

The point where a motor neuron communicates with a skeletal muscle cell.

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Neurotransmitters (examples)

Includes noradrenaline, acetylcholine, dopamine, serotonin, and nitric oxide.

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Craniosacral outflow

The outflow of parasympathetic nerves originating from the cranial and sacral regions of the central nervous system.

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Neuroeffector Junction

The junction where a neuron communicates with its target organ or tissue.

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Action Potential

An electrical signal that propagates along a neuron's axon.

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Depolarization

A reduction in the membrane potential of a cell, making it more likely to fire an action potential.

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Voltage-Operated Calcium Channel

Ion channels that open in response to changes in membrane potential.

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Exocytosis

The process by which neurotransmitters are released from a neuron.

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Agonist

A substance that binds to a receptor and activates it, producing a response.

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Presynaptic Autoinhibitory Receptors

Receptors on the presynaptic neuron that inhibit further release of neurotransmitter.

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Antagonist

A substance that binds to a receptor but does not activate it, blocking the action of an agonist.

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Reuptake

The uptake of neurotransmitters from the synaptic cleft back into the presynaptic neuron.

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Sites of Drug Action

Drugs affect neurotransmission by acting on synthesis, storage, release, receptors and cessation.

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Study Notes

  • The lectures aim to describe neurotransmission and its modification by drugs.
  • Students should understand why neurotransmission is a target for therapeutic drug development.

The Neuron

  • The neuron is a nerve cell that transmits electrical signals.
  • NT stands for neurotransmitter.
  • The neuron consists of the cell body, axon, and dendrites.
  • The cell body contains the nucleus and other organelles.
  • The axon is a long, slender projection that conducts electrical impulses away from the cell body.
  • Dendrites are branched extensions that receive signals from other neurons.
  • The nerve terminal is the end of the axon, where neurotransmitters are released.
  • Local anesthetics inhibit nerve conduction by blocking sodium channels.

Sympathetic and Parasympathetic Nerves

  • Sympathetic nerves originate from the brain and spinal cord, and connect to tissue via a ganglion.
  • Parasympathetic nerves also originate from the brain and spinal cord, connecting to tissue via a ganglion.
  • Motor nerves connect the spinal cord directly to the neuromuscular junction (NMJ) in skeletal muscle.

Neurotransmitters

  • Noradrenaline (NA) is found at sympathetic terminals.
  • Acetylcholine (ACh) is located at parasympathetic terminals, ganglia, and the NMJ.
  • Dopamine (DA) and Serotonin (5-HT) are found in parts of the CNS.
  • Nitric oxide (NO) can be found in less common places.

Anatomy of the Sympathetic Nervous System

  • The sympathetic nervous system emanates from the thoracolumbar segments of the spinal cord.
  • Ganglia are typically close to the spinal cord in the paravertebral chain.

Anatomy of the Parasympathetic Nervous System

  • Craniosacral outflow includes cranial nerves (oculomotor, facial, glossopharyngeal, vagal) and sacral nerves (nervi erigentes).
  • Ganglia are located close to or inside target tissues.

The Neuroeffector Junction (Terminal Region)

  • Action potential arrives at the nerve terminal.
  • Depolarization occurs.
  • Voltage-operated calcium channels open, allowing calcium ions (Ca) to enter.
  • NT is released via Exocytosis.
  • Neurotransmitters (NT) are released.
  • Presynaptic autoinhibitory agonism occurs
  • Postsynaptic agonism occurs.

Synthesis and Storage of Transmitter

  • Precursor uptake is inhibited by hemicholinium for Acetylcholine (ACh).
  • L-DOPA increases dopamine levels in Parkinson's patients.
  • The enzyme cascade is inhibited by AMPT for Noradrenaline (NA).
  • Storage is inhibited by reserpine for Noradrenaline (NA).

Release of Transmitter

  • Terminal depolarization is inhibited by guanethidine with Noradrenaline (NA).
  • Conotoxin inhibits calcium channels.
  • Vesicle fusion is inhibited by Botulinum for Acetylcholine (ACh).
  • Amphetamine and guanethidine displace Noradrenaline.
  • Clonidine, an α2 agonist, inhibits the release of Noradrenaline via presynaptic receptors.

Termination of Neurotransmission

  • Diffusion occurs at the geometry of the cleft.
  • Reuptake is inhibited by cocaine for Noradrenaline (NA) and fluoxetine for Serotonin (5-HT).
  • Tricyclic antidepressants inhibit NA uptake, while fluoxetine (Prozac) inhibits 5-HT uptake.
  • The breakdown of neurotransmitters is modified by inhibiting enzymes such as neostigmine/ACh.
  • Anticholinesterases reverse muscle relaxation in surgery.

Agonist and Antagonist Action on Receptors

  • Agonists have affinity and efficacy, stimulate receptors, and mimic transmitters.
  • Antagonists have affinity but no efficacy, block the binding site, and inhibit agonist action.

Receptor Agonists with Major Therapeutic Applications

  • Salbutamol is a beta 2 noradrenaline receptor agonist used for asthma.
  • Phenylephrine is an alpha-1 noradrenaline receptor agonist used as a decongestant.
  • Bromocriptine is a dopamine D2 receptor agonist used for Parkinson's disease.
  • Morphine is an enkephalin receptor agonist used for pain relief.
  • Diazepam is a GABA/A receptor agonist used for anxiety.
    • Diazepam enhances the effects of GABA by acting on a site different from the GABA binding site.

Receptor Antagonists with Major Therapeutic Applications

  • Prazosin is an alpha-1 noradrenaline receptor antagonist used to reduce blood pressure.
  • Propranolol is a beta noradrenaline receptor antagonist used to reduce blood pressure.
  • Atracurium is an acetylcholine nicotinic receptor antagonist used as a muscle relaxant.
  • Atropine is an acetylcholine muscarinic receptor antagonist used as a pre-medication.
  • Trifluoperazine is a dopamine D2, receptor antagonist used as an antipsychotic.

Drugs Affecting the Neuroeffector Response

  • Benzodiazepine tranquilizers bind to the GABA receptor/Cl ion channel complex
    • This enhances channel opening and potentiates the inhibitory effects of GABA.
  • Sildenafil (Viagra) inhibits the breakdown of cyclic GMP, a second messenger substance produced by nitric oxide in erectile tissue.

Summary of Drug Action Sites

  • Synthesis
  • Storage
  • Release
  • Receptors
  • Cessation: Reuptake, Enzyme, Autoinhibition

Conclusion

  • The synapse is an important site for drug action.
    • Because it’s the site of neurotransmission
    • It’s the site where the transmitter is synthesised, stored, and released
    • It’s a major location for receptors and target for agonists or antagonists
    • Receptors offer the best chance of producing drugs with a high degree of selectivity and reduced side effect profile

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