Neurotransmission & Pharmacology: Key Concepts
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Questions and Answers

Which of the following best describes the role of dendrites in a neuron?

  • Receiving signals from other neurons. (correct)
  • Facilitating drug metabolism.
  • Transmitting electrical impulses away from the cell body.
  • Regulating neuronal gene expression.

The process of a drug entering the bloodstream from its administration site is known as:

  • Drug metabolism
  • Drug distribution
  • Drug absorption (correct)
  • Drug excretion

What is the primary purpose of Phase I metabolism in the context of pharmacokinetics?

  • Binding drugs to receptors on target cells
  • Distributing drugs throughout the body.
  • Modifying drugs to increase their solubility. (correct)
  • Conjugating drugs to facilitate excretion.

How do G-linked proteins (GPCRs) contribute to cell signaling?

<p>By transmitting signals from extracellular molecules to intracellular pathways. (D)</p> Signup and view all the answers

What does the term 'steady state' refer to in the context of drug pharmacokinetics?

<p>The condition where drug intake equals drug elimination, resulting in a stable concentration. (B)</p> Signup and view all the answers

Which of the following describes the function of an ionic filter in ion channels?

<p>Selectively permitting specific ions to pass through based on size and charge. (B)</p> Signup and view all the answers

In classic synaptic neurotransmission, what is the role of the presynaptic neuron?

<p>To release neurotransmitters into the synapse. (C)</p> Signup and view all the answers

Which of the following is an example of a second messenger involved in intracellular signaling?

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

During signal transduction, what is the primary role of amplification?

<p>To enhance the signal's strength, ensuring a robust cellular response. (A)</p> Signup and view all the answers

Which mechanism directly prevents prolonged activation of a signaling pathway and maintains cellular homeostasis?

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

A drug binds to a receptor and elicits a biological response, mimicking the effect of the natural ligand. What type of drug is this?

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

A researcher observes that a specific gene is expressed differently based on whether it was inherited from the mother or the father. Which phenomenon is most likely responsible for this?

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

Which factor influencing gene expression involves the silencing of one copy of a gene in females?

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

A pharmaceutical company is developing a drug that binds to a receptor, activating it, but producing a weaker response than the natural ligand. What type of drug are they developing?

<p>A partial agonist (D)</p> Signup and view all the answers

Which of the following cellular responses is directly triggered by signal transduction?

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

A scientist is studying a signaling pathway and observes cross-talk between multiple pathways. What is the most likely outcome of this integration and modulation?

<p>Fine-tuning of the cellular response based on multiple inputs. (D)</p> Signup and view all the answers

A patient reports experiencing sleepwalking as a side effect. Which of the following medications is most likely contributing to this adverse effect?

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

A physician is considering prescribing a medication to help a patient both fall asleep and stay asleep throughout the night. Based on their half-lives, which of the following medications would be the MOST appropriate choice?

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

A patient with narcolepsy is prescribed a medication to promote wakefulness. Which mechanism of action is MOST likely associated with the prescribed drug?

<p>Stimulating dopamine, norepinephrine, and histamine release (B)</p> Signup and view all the answers

Which of the following medications is MOST likely to cause anticholinergic side effects, such as dry mouth, blurred vision, and urinary retention, especially in elderly patients?

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

A patient taking quetiapine (Seroquel) reports experiencing muscle stiffness and tremors. Which of the following side effects is the MOST likely cause of these symptoms?

<p>Extrapyramidal symptoms (EPS) (D)</p> Signup and view all the answers

A patient with depression is prescribed trazodone (Desyrel) primarily for its sedative effects to help with insomnia. Which of the following mechanisms of action is MOST responsible for this sedative effect?

<p>Serotonin (5-HT2) receptor antagonism and serotonin reuptake inhibition (A)</p> Signup and view all the answers

A patient taking clonazepam (Klonopin) for anxiety is advised about the potential risks associated with long-term use. Which of the following is the MOST significant concern regarding the chronic use of clonazepam?

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

Which of the following medications is approved for the treatment of both schizophrenia and bipolar disorder?

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

A patient with impaired kidney function is prescribed a medication that is primarily eliminated through renal excretion. Which pharmacokinetic process is most likely to be affected in this patient?

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

In which scenario might benzodiazepines paradoxically increase the risk of seizures?

<p>When combined with other central nervous system depressants like opioid pain relievers. (D)</p> Signup and view all the answers

A drug is known to have poor oral bioavailability due to significant first-pass metabolism. Which of the following strategies would likely be LEAST effective in improving its absorption?

<p>Increasing the drug's water solubility (A)</p> Signup and view all the answers

A drug has a high affinity for plasma proteins. How would this characteristic most likely affect its distribution?

<p>Decreased distribution to tissues (B)</p> Signup and view all the answers

Why are stimulants sometimes prescribed for individuals experiencing excessive daytime sleepiness (hypersomnia)?

<p>To increase wakefulness by boosting norepinephrine and dopamine activity. (B)</p> Signup and view all the answers

What is the primary focus when using pharmacological treatments for daytime sleepiness?

<p>Short-term symptom relief combined with behavioral strategies for long-term management. (B)</p> Signup and view all the answers

A patient is taking Drug A, which is metabolized by CYP3A4. If Drug B, a CYP3A4 inhibitor, is added to the patient's regimen, what is the most likely effect on Drug A?

<p>Increased plasma concentration of Drug A (A)</p> Signup and view all the answers

Which of the following is a potential long-term consequence of untreated chronic insomnia?

<p>Increased risk of heart disease. (C)</p> Signup and view all the answers

A patient is prescribed Drug X, a substrate of CYP2C9. The patient also starts taking Drug Y, a CYP2C9 inducer. How should the dose of Drug X be adjusted and why?

<p>Increase the dose of Drug X because Drug Y will increase its metabolism. (D)</p> Signup and view all the answers

How does chronic insomnia impact cognitive functions?

<p>By potentially causing cognitive impairment. (B)</p> Signup and view all the answers

A drug is administered intravenously. Which of the following pharmacokinetic phases is effectively bypassed?

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

Drug A is a substrate of CYP3A4. Grapefruit juice is a known CYP3A4 inhibitor. What effect would drinking grapefruit juice have on the plasma concentration of Drug A?

<p>Increase the plasma concentration of Drug A. (A)</p> Signup and view all the answers

Which of the following non-pharmacological strategies aims to address insomnia by modifying maladaptive thoughts and behaviors related to sleep?

<p>Cognitive Behavioral Therapy for Insomnia (CBT-I). (D)</p> Signup and view all the answers

Which non-pharmacological intervention for insomnia involves creating a sleep environment and daily routine that promotes consistent and restful sleep?

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

If a drug's half-life is 4 hours, approximately how long will it take for the drug to be almost completely eliminated from the body (assuming first-order kinetics)?

<p>20 hours (A)</p> Signup and view all the answers

What is the main goal of employing non-pharmacological strategies in the management of insomnia?

<p>To regulate sleep patterns, reduce anxiety, and improve overall sleep quality without medication. (B)</p> Signup and view all the answers

In a G-protein-linked system, what is the immediate consequence of a ligand binding to a GPCR?

<p>Exchange of GDP for GTP on the G-protein, activating it. (C)</p> Signup and view all the answers

Which of the following is the correct order of events in a typical G-protein-linked receptor pathway?

<p>Ligand binding → G-protein activation → Enzyme modulation → Second messenger production → Cellular response → GTP hydrolysis (B)</p> Signup and view all the answers

How do hormones initiate intracellular changes within hormone-linked systems?

<p>By binding to receptors and triggering cascades via second messengers or direct gene modulation. (A)</p> Signup and view all the answers

What role do neurotrophic factors play in neuronal function?

<p>They regulate neuronal survival, differentiation, and synaptic plasticity. (C)</p> Signup and view all the answers

Which type of receptor is typically activated by neurotrophic factors like BDNF or NGF?

<p>Tyrosine kinase receptors (Trk) (D)</p> Signup and view all the answers

How do ion-channel-linked systems alter cellular activity?

<p>By opening or closing in response to a signal, allowing specific ions to enter or exit the cell. (A)</p> Signup and view all the answers

What is a signal transduction cascade?

<p>A series of biochemical reactions converting an extracellular signal into a cellular response. (A)</p> Signup and view all the answers

A drug is designed to prevent the activation of G-proteins. At which step of the G-protein-linked receptor pathway would this drug primarily interfere?

<p>Exchange of GDP for GTP on the G-protein. (D)</p> Signup and view all the answers

Flashcards

Axon

A long projection of a neuron that transmits impulses from the cell body.

Dendrite

A branched extension of a neuron that receives signals from other neurons.

Neurotransmission

The release of neurotransmitters from a presynaptic neuron into a synapse to activate postsynaptic receptors.

Pharmacokinetics

The study of how drugs are absorbed, distributed, metabolized, and excreted by the body.

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Pharmacodynamics

The study of how drugs exert their effects on biological systems.

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Half-life

The time it takes for a drug’s concentration in the body to decrease by half.

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Second messengers

Intracellular signaling molecules that relay signals from receptors to cellular processes.

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G-linked proteins

G-protein-coupled receptors that transmit signals from outside the cell to inside pathways.

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Signal transduction cascade

A series of biochemical reactions converting an extracellular signal into a cellular response.

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G-protein-linked systems

Systems where GPCRs activate G-proteins to regulate second messengers, amplifying signals.

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Ion-channel-linked systems

Systems where ion channels open or close in response to signals, altering cellular activity.

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Hormone-linked systems

Hormones bind to receptors triggering cascades influencing metabolism, growth, or homeostasis.

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Transduction cascades

Pathways that relay and amplify cellular signals from receptors to intracellular targets.

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Transcription factors

Proteins that regulate gene expression by binding to specific DNA sequences.

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Volume neurotransmission

Diffusion of neurotransmitters beyond the synapse to impact multiple neurons.

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Retrograde neurotransmission

Postsynaptic neurons send signals back to presynaptic neurons to regulate neurotransmitter release.

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Absorption

The process by which a drug enters the bloodstream after administration.

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Distribution

The movement of a drug from the bloodstream into various tissues and organs.

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Metabolism

The process by which the body chemically alters a drug, typically in the liver.

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Elimination

The removal of a drug from the body, mainly through kidneys or liver.

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CYP450 System

A group of liver enzymes responsible for drug metabolism and detoxification.

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Substrate (CYP450)

A substance that is metabolized by a specific CYP450 enzyme.

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Inducer (CYP450)

A substance that increases the activity of a CYP450 enzyme, enhancing metabolism of its substrates.

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Inhibitor (CYP450)

A substance that decreases the activity of a CYP450 enzyme, slowing metabolism of its substrates.

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Transduction

Process where a receptor changes shape, activating signaling pathways.

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Amplification

The process of increasing the strength of a signal through intermediary steps.

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Cellular Response

The outcome of signaling that causes effects like gene expression or metabolism changes.

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Termination

Process to deactivate a signal to maintain homeostasis.

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Agonists

Molecules that activate receptors like natural ligands, causing a biological response.

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Partial Agonists

Molecules that activate receptors but produce a weaker response than full agonists.

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Factors Influencing Gene Expression

Elements like genetic makeup and environment that affect gene activity.

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Cross-talk in Signaling

Interaction between different signaling pathways that fine-tunes responses.

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Clonazepam

A benzodiazepine enhancing GABA effects; treats seizures and panic disorder.

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Side effects of Clonazepam

Common side effects include drowsiness, dizziness, and cognitive impairment.

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Z drugs purpose

Used primarily to induce and maintain sleep; have short half-lives.

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Modafinil mechanism

Promotes wakefulness by stimulating dopamine, norepinephrine, and histamine.

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Quetiapine

An antipsychotic approved for schizophrenia and bipolar disorder; sedative effects.

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Trazodone action

Serotonin antagonist and reuptake inhibitor; often used for sleep.

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Diphenhydramine purpose

Antihistamine for allergies; often used off-label as a sleep aid.

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Common side effects of Diphenhydramine

Can cause drowsiness, confusion, and anticholinergic side effects.

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Benzodiazepine Overuse

Excessive use of benzodiazepines can depress the CNS too much.

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Seizure Disorders and Benzodiazepines

Benzodiazepines may not control seizures effectively in those with a history of epilepsy.

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Psychotropics for Insomnia

Medications like benzodiazepines and antidepressants used to induce sleep.

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Stimulants for Daytime Sleepiness

Stimulants and some antidepressants increase wakefulness by boosting norepinephrine and dopamine.

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Long-term Effects of Insomnia

Can lead to cognitive impairment, mental health issues, and chronic diseases.

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CBT-I for Insomnia

Cognitive Behavioral Therapy for Insomnia helps regulate sleep without medication.

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Sleep Hygiene

Practices that promote regular sleep patterns and improve sleep quality.

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Non-Pharmacologic Strategies

Techniques such as relaxation, exercise, and dietary changes to improve sleep.

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Study Notes

Week 5 Quiz Study Guide

  • Assignments: 35%
  • Discussions: 10%
  • Quizzes: 30% (10% each quiz)
  • Final Exam: 25%

Key Concepts

  • Axon: A long, slender projection of a neuron that transmits electrical impulses away from the cell body.
  • Classic Synaptic Neurotransmission: Neurotransmitters released from a presynaptic neuron into a synapse to activate receptors on a postsynaptic neuron.
  • Concentration-Time Curve: A graphical representation showing how the concentration of a drug changes over time in the body.
  • Degradation: The breakdown of molecules (neurotransmitters or drugs) into inactive components.
  • Dendrite: A branched extension of a neuron that receives signals from other neurons.
  • Drug Absorption: The process of a drug entering the bloodstream from the site of administration.
  • Drug Distribution: The movement of a drug from the bloodstream into tissues and organs.
  • Excitation-Secretion Coupling: The process linking electrical excitation of a cell to the secretion of substances (e.g., neurotransmitters or hormones).
  • G-protein-coupled receptors (GPCRs): Transmit signals from extracellular molecules to intracellular pathways.
  • Half-life/Steady State: Half-life is the time it takes for a drug's concentration to decrease by half; steady state is when drug intake equals elimination, leading to a stable concentration.
  • Ionic Filter: A selective structure in ion channels that allows only specific ions to pass based on their size and charge.
  • Ion-gated channels: Proteins in the cell membrane that open or close in response to voltage changes or ligand binding, controlling ion flow.
  • Neuronal Gene Expression: The process by which neurons regulate the production of proteins based on genetic instructions.
  • Pharmacokinetics: The study of how drugs are absorbed, distributed, metabolized, and excreted by the body.
  • Pharmacodynamics: The study of how drugs exert their effects on biological systems.
  • Phase I Metabolism: Modification of drugs by enzymes to increase solubility.
  • Phase II Metabolism: Drug conjugation with molecules to facilitate excretion.
  • Second Messengers: Intracellular signaling molecules (e.g., cAMP, Ca2+) relaying signals from receptors to target cellular processes.
  • Signal Transduction Cascade: A series of biochemical reactions converting an extracellular signal into a cellular response.
  • Retrograde Neurotransmission: Postsynaptic neurons sending signals back to presynaptic neurons to regulate neurotransmitter release.
  • Transduction Cascades: Molecular pathways relaying and amplifying cellular signals from receptors to intracellular targets.
  • Transcription Factors: Proteins regulating gene expression by binding to specific DNA sequences.
  • Volume Neurotransmission: Neurotransmitter diffusion beyond the synapse to influence multiple neurons in a broader area.

Key Points (Additional Information)

  • Four main types of second messenger systems: G-protein-linked, ion-channel-linked, hormone-linked, and neurotropic systems.
  • G-protein-linked systems: G-protein-coupled receptors (GPCRs) activating intracellular signaling via G-proteins regulating second messengers like cAMP or Ca2+.
  • Ion-channel-linked systems: Ligand-gated or voltage-gated ion channels opening or closing in response to a signal, allowing specific ions (e.g., Na+, K+, Ca2+) to enter or exit the cell.
  • Hormone-linked systems: Hormones binding to receptors, triggering intracellular cascades via second messengers.
  • Neurotropic systems: Neurotrophic factors activating receptors to regulate neuronal survival, differentiation, and synaptic plasticity.

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Description

Key concepts cover aspects from neuron structure (axon, dendrite) to neurotransmission, drug absorption, distribution, and degradation. It also describes concentration-time curve and excitation-secretion coupling.

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