Pharmacology Drug Study Notes
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Questions and Answers

What physiological process helps to prevent fatigue in the postsynaptic cell during neurotransmission?

  • Rapid synthesis of neurotransmitters
  • Continuous action potential generation
  • Constant receptor downregulation
  • Delay in neurotransmitter release (correct)

Which factor is associated with the downregulation of receptors in a postsynaptic cell?

  • Higher neurotransmitter levels
  • Increased receptor sensitivity
  • Reduced synaptic delay
  • Repetitive stimulation (correct)

What condition is suggested to lead to catecholamine depletion in heart failure patients?

  • Prolonged sympathetic nervous system activation (correct)
  • Temporary cessation of sympathetic stimulation
  • Increased sensitivity to norepinephrine
  • Enhanced neurotransmitter release

In which scenario might an older individual experience constant release of catecholamines?

<p>During acute or chronic illness (C)</p> Signup and view all the answers

How does depletion of neurotransmitters contribute to postsynaptic fatigue?

<p>By reducing neurotransmitter availability (D)</p> Signup and view all the answers

What might occur in the postsynaptic cell if it constantly receives high levels of neurotransmitter stimulation?

<p>Genetic changes to reduce response (D)</p> Signup and view all the answers

What is the consequence of using qualitative monitoring in patients with neuromuscular blockade?

<p>It might show zero twitches despite activity (A)</p> Signup and view all the answers

What is a possible outcome of long-term overactivation of the sympathetic nervous system in relation to receptor activity?

<p>Reduced receptor sensitivity and number (C)</p> Signup and view all the answers

What is indicated as the desired form of ketamine?

<p>S-ketamine (A), Esketamine (B)</p> Signup and view all the answers

Which term describes a mixture containing equal parts of two enantiomers?

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

What side effect is commonly associated with the non-preferred form of ketamine?

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

Which of the following correctly identifies the characteristic of levo bupivacaine compared to arbupivacaine?

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

What does the prefix 'S' in S-ketamine indicate?

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

In the context of the drug ketamine, what is the significance of the formulation 'esketaine'?

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

What is the relationship between S-ketamine and esketamine?

<p>Different names for the same drug (B)</p> Signup and view all the answers

What potential problem arises from giving too much arbupivacaine intravascularly?

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

What is a potential drawback of using non-competitive drugs in treatment?

<p>They can lead to irreversible effects. (C)</p> Signup and view all the answers

Which type of bond is typically the strongest in receptor interactions?

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

What characterizes chiral molecules?

<p>They exhibit three-dimensional asymmetry. (C)</p> Signup and view all the answers

What is the characteristic structure of a G protein-coupled receptor?

<p>Has a ribbon-like formation crossing the membrane seven times (B)</p> Signup and view all the answers

What type of interaction is generally considered significant in drug formulation?

<p>Dipole-dipole interactions (D)</p> Signup and view all the answers

Which proton pump inhibitor was mentioned as a contemporary example in drug use?

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

Which type of bond is primarily responsible for holding globular proteins like enzymes in their structure?

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

What is the weakest type of dipole interaction?

<p>Van der Waals (London) forces (D)</p> Signup and view all the answers

What characteristic of molecules does stereochemistry specifically describe?

<p>The three-dimensional arrangement of atoms. (C)</p> Signup and view all the answers

Why can larger hydrophobic drug molecules not easily diffuse across a membrane?

<p>They require a specific receptor to assist in their transport (D)</p> Signup and view all the answers

What is typically true about the enantiomers of a chiral compound?

<p>They are mirror images but not superimposable. (B)</p> Signup and view all the answers

Why is irreversible binding generally undesirable in drug interactions?

<p>It makes pharmacological management more complex. (D)</p> Signup and view all the answers

Which statement about nonpolar tails interacting with water molecules is correct?

<p>Nonpolar tails repel water molecules (B)</p> Signup and view all the answers

What happens to drug molecules that bind weakly to their receptors?

<p>They can easily dissociate from the receptor (B)</p> Signup and view all the answers

Which characteristic of drug bonding does not necessarily imply a longer duration of action?

<p>Stronger bond strength (D)</p> Signup and view all the answers

When discussing intermolecular forces, what is true about dipole-dipole interactions compared to weaker attractions?

<p>Weaker attractions are generally more common than dipole-dipole interactions (A)</p> Signup and view all the answers

What is the primary characteristic of a drug that allows it to effectively bind to a receptor?

<p>It must be lipophilic. (C)</p> Signup and view all the answers

What process occurs when a drug perfectly fits into its receptor, leading to a change in the receptor's shape?

<p>Conformational change. (C)</p> Signup and view all the answers

Which of the following is NOT considered an aceptor in pharmacology?

<p>Hormone receptors. (A)</p> Signup and view all the answers

Why are lipophilic molecules preferred for pharmacological activity?

<p>They can easily permeate cell membranes. (D)</p> Signup and view all the answers

Which type of drug receptor is commonly associated with ligand-gated channels?

<p>Membrane-bound receptors. (B)</p> Signup and view all the answers

What is the role of hydrophobic bonding in drug-receptor interaction?

<p>It stabilizes the drug-receptor complex. (A)</p> Signup and view all the answers

How does the presence of an aceptor like albumin affect a drug’s bioavailability?

<p>It reduces the drug's therapeutic effect. (D)</p> Signup and view all the answers

Which type of receptor is NOT mentioned as common for many drugs?

<p>Ion channels. (B)</p> Signup and view all the answers

What is the purpose of receptor upregulation in cells?

<p>To increase the quantity and sensitivity of receptors (B)</p> Signup and view all the answers

Which of the following describes downregulation?

<p>A decrease in receptor number and sensitivity (C)</p> Signup and view all the answers

What can trigger changes in gene expression within a cell?

<p>Continuous presence of agonists (C)</p> Signup and view all the answers

How does constant antagonism affect receptor expression?

<p>It causes upregulation as the cell seeks to compensate (C)</p> Signup and view all the answers

What might happen to a cell that does not receive its normal baseline activity?

<p>It will genetically adapt to increase receptor response (C)</p> Signup and view all the answers

What potential downstream effect can occur from the binding of a drug molecule to a cell receptor?

<p>A change in the cell's migration patterns (B)</p> Signup and view all the answers

What is one potential outcome of receptor upregulation?

<p>More frequent cellular responses to agonists (D)</p> Signup and view all the answers

Which of the following best describes cellular changes caused by receptor activity?

<p>Changes can include altered functions such as apoptosis (A)</p> Signup and view all the answers

Flashcards

Synaptic Delay

The short delay between when one neuron sends a signal and the next neuron receives it. This delay prevents the neuron from becoming overwhelmed with constant stimulation.

Synaptic Fatigue

The ability of a neuron to decrease its response to repeated stimulation over time. This helps prevent the neuron from becoming fatigued.

Downregulation of Receptors

A mechanism for reducing receptor sensitivity in response to constant stimulation. This process regulates the strength of cell signaling.

Neurotransmitter Depletion

The process of using up neurotransmitters faster than the neuron can replenish them. This can occur during periods of high stress or illness.

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Catecholamine Depletion

A state where the heart is constantly working harder to maintain blood pressure and circulation. This can lead to neurotransmitter depletion, particularly of norepinephrine and epinephrine.

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Neuromuscular Blockade Monitoring

A method used in intensive care units (ICUs) to assess the strength of neuromuscular blockade. It measures the patient's muscle response to electrical stimulation.

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Zero Out of Four Twitches

A condition in which a patient shows no muscle twitches in response to electrical stimulation during neuromuscular blockade monitoring.

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Qualitative Neuromuscular Blockade Monitoring

The use of qualitative assessment to evaluate the strength of neuromuscular blockade. Qualitative assessment focuses on the presence or absence of muscle twitches.

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G protein-coupled receptor (GPCR)

A type of transmembrane receptor characterized by its seven transmembrane domains (crossing the cell membrane seven times) that form a ribbon-like structure.

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Hydrogen bonds (in protein structure)

Weak intermolecular interactions that contribute to the overall shape and stability of proteins, particularly important in enzymes.

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Hydrophobicity and membrane permeability

Nonpolar molecules, like some drugs, generally cannot easily pass through cell membranes. They may still need a receptor to interact with.

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Van der Waals London forces

The weakest type of intermolecular force, often involving temporary fluctuations in electron distribution.

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Drug-receptor bond strength and duration of action

The interaction between a drug and its receptor is not always directly proportional to the duration of action. It's complex.

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Hydrophobic interactions

Nonpolar molecules, like the tails of fats or lipids, tend to avoid and repel water molecules. This is called hydrophobicity.

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Drug-receptor Interaction

The process of a drug molecule fitting into its designated receptor site, often involving hydrophobic bonding due to the nonpolar nature of both the drug and the receptor.

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Hydrophobic Bonding

A type of bonding that occurs between nonpolar molecules, where they avoid contact with water.

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Lipophilic

A molecule that is not attracted to water and tends to dissolve in lipids or fats.

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Conformational Change

A change in the shape or conformation of a molecule, particularly in the context of drug-receptor binding, where the binding of a drug to a receptor triggers a change in the receptor's shape.

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Aceptor

A protein that acts as an alternative binding site for a drug, preventing it from reaching its target receptor.

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Ligand-gated Receptor

A type of receptor that is activated by the binding of a specific molecule, known as a ligand.

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Voltage-gated Receptor

A type of receptor that is activated by changes in the electrical potential across a cell membrane.

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G-protein Coupled Receptor

A type of receptor that is coupled to a G-protein, which acts as an intermediary to activate intracellular signaling pathways.

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Receptor Upregulation

A cell's response to continuous exposure to a substance, increasing the number and sensitivity of its receptors on the membrane.

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Receptor Downregulation

A cell's response to continuous exposure to a substance, reducing the number and sensitivity of its receptors on the membrane.

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Genetic Expression Changes

A type of cellular response that can occur downstream of a drug binding to its receptor, leading to changes in gene expression.

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Cellular Metabolism Changes

A type of cellular response that can occur downstream of a drug binding to its receptor, leading to changes in how the cell uses energy and resources.

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Cellular Changes

A type of cellular response that can occur downstream of a drug binding to its receptor, leading to changes in the cell's location or function.

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Cell Sensitivity Increase

The ability of a cell to respond to a drug by increasing the number and sensitivity of its receptors.

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Cell Sensitivity Decrease

The ability of a cell to respond to a drug by decreasing the number and sensitivity of its receptors.

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Irreversible Drug Binding

A type of bonding that occurs when a drug binds to a receptor irreversibly, meaning the drug cannot easily detach from the receptor, potentially leading to prolonged effects.

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Reversible Drug Binding

A type of bonding where a drug binds to a receptor with weaker forces, allowing for the drug to detach more easily and providing more control over the duration of action.

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Stereochemistry

The unique 3D shape of a molecule, which can affect its ability to bind to receptors and proteins.

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Chiral Molecule

A molecule that exists in two mirror image forms that cannot be superimposed on each other.

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Enantiomers

A pair of molecules that are mirror images of each other and cannot be superimposed.

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Dipole-Dipole Interaction

A type of bond that occurs between molecules due to a difference in charge distribution, leading to weaker interactions compared to covalent bonds.

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Van Der Waals Forces

Relatively weak forces that arise from temporary fluctuations in electron distribution in a molecule.

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Covalent Bond

A type of bond that involves the sharing of electrons between atoms, creating a strong and durable interaction.

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Racemic Mixture

A 50/50 mixture of two enantiomers. Enantiomers are mirror images of each other. They have the same chemical formula but differ in their spatial arrangement.

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Isomers

Occur when drugs with the same chemical formula have different spatial arrangements (stereochemistry). This leads to variations in how they interact with the body and potentially different effects.

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S-Ketamine

The 'S' enantiomer of ketamine is the desired form. It's more potent and less likely to cause hallucinogenic side effects.

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R-Ketamine

The 'R' enantiomer of ketamine is associated with side effects like hallucinations. It's less potent than the 'S' enantiomer.

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Racemic Ketamine

A drug that's a racemic mixture of R and S enantiomers. It's often the cheaper version.

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Esketamine

The 'S' enantiomer is isolated from the 'R' enantiomer. It's the preferred formulation for its targeted effects and reduced side effects.

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Levobupivacaine & Arbupivacaine

A local anesthetic. The 'R' enantiomer (arbupivacaine) is more likely to cause cardiotoxicity if administered intravenously.

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Study Notes

Drug Study Notes

  • Drug Trials: Drug trials often involve healthy adults aged 20-40 to test effectiveness and safety. This may not reflect responses in other populations.
  • Individualization: Drug responses vary significantly between individuals. Dosing needs to be adjusted to account for these differences.
  • Dose-Response Curves: These curves plot drug concentration against the response (e.g., blood pressure, pain relief).
  • EC50: The effective concentration/dose where the drug produces 50% of its maximum effect.
  • LD50: The lethal dose (in animals) where 50% of the population dies.
  • Therapeutic Index: The ratio of LD50 to ED50. A higher ratio indicates a safer drug.
  • Receptor Upregulation/Downregulation: Changes in receptor numbers and sensitivity can occur in response to chronic drug exposure or lack of stimulation, affecting therapeutic response.
  • Agonists: Full agonists produce a maximal effect. Partial agonists produce a limited (partial) effect.
  • Antagonists: Block the effects of other drugs, by binding to the receptor without activating it.
  • Competitive Antagonist: Can be outcompeted by increasing concentrations of the agonist.
  • Non-Competitive Antagonist: Cannot be replaced/outcompeted, so the response is irreversible.
  • Chirality: Molecules with asymmetrical structures (e.g., enantiomers); these can significantly affect drug activity.
  • Racemic Mixtures: 50/50 mixtures of both enantiomers.
  • Stereochemistry: Three-dimensional arrangement of atoms in a molecule; important for drug function.
  • Pharmacologic effects: Can be influenced by several factors like receptors and other factors.

Receptor Pharmacology

  • Receptors: Proteins which bind to specific molecules (ligands), producing a response in the cell.
  • Receptors location: Inside or on the surface of the cell membrane.
  • Binding: Usually involves hydrophobic bonding (nonpolar molecules); for ion channels, ions generally flow along concentration gradients).
  • Activation: Binding triggers cellular changes, influencing cell function (e.g., opening ion channels, activating enzymes).

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Explore key concepts in pharmacology including drug trials, individualization of treatment, dose-response relationships, and the therapeutic index. This quiz covers essential information about drug responses and challenges in clinical settings. Ideal for students studying pharmacology or related fields.

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