Molecular and Experimental Pharmacology Quiz

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Questions and Answers

What are the four main steps involved in pharmacokinetics?

  • Absorption, Distribution, Metabolism, Elimination
  • Absorption, Distribution, Elimination, Excretion
  • Absorption, Digestion, Metabolism, Excretion
  • Absorption, Distribution, Metabolism, Excretion (correct)

What is the main difference between pharmacodynamics and pharmacokinetics?

  • Pharmacodynamics focuses on the molecular targets of drugs, while pharmacokinetics focuses on the chemical properties of drugs.
  • Pharmacodynamics describes how drugs act on the body, while pharmacokinetics describes what the body does to a drug. (correct)
  • Pharmacodynamics focuses on the therapeutic effects of drugs, while pharmacokinetics focuses on the side effects of drugs.
  • Pharmacodynamics describes what the body does to a drug, while pharmacokinetics describes how drugs act on the body.

What are the two main goals of molecular pharmacology?

  • To develop personalized therapies and to predict drug resistance.
  • To improve drug bioavailability and to reduce drug-drug interactions.
  • To evaluate drug efficacy and to minimize drug side effects.
  • To understand how drugs produce their effects and to discover new drug targets. (correct)

Which of these is NOT a valid target for future drug development?

<p>Proteins that are highly abundant and ubiquitous in the body (B)</p> Signup and view all the answers

What is the main challenge in developing drugs that target protein-protein interactions?

<p>These interactions are often difficult to disrupt with small molecules. (C)</p> Signup and view all the answers

The concept of 'target validation' refers to the process of identifying new therapeutic targets.

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

What is the main difference between a 'me-too' compound and a 'true innovation' in drug development?

<p>Me-too compounds target a well-validated target, while true innovations aim to discover novel targets. (D)</p> Signup and view all the answers

Which of these is an example of a personalized treatment for a genetic disease?

<p>Use of a gene therapy to correct a specific genetic defect (D)</p> Signup and view all the answers

Which of the following is NOT a characteristic of biopharmaceuticals?

<p>Typically have a shorter half-life than small molecules (D)</p> Signup and view all the answers

What is the main factor that explains the increasing popularity of target-oriented pharmacology?

<p>The increasing understanding of the molecular mechanisms underlying disease (A)</p> Signup and view all the answers

What is the primary function of transporters?

<p>To transport molecules against their concentration gradient (A)</p> Signup and view all the answers

Which of these is NOT a characteristic of ABC (ATP binding cassette) family of transporters?

<p>They are primarily responsible for influx of molecules across the cell membrane (B)</p> Signup and view all the answers

Which of these transporters is NOT a substrate for P-glycoprotein (P-gp)?

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

What is the primary mechanism by which drugs target transporters?

<p>By binding to the active site of the transporter and blocking its function (D)</p> Signup and view all the answers

Which of these is NOT a known target for drug-mediated modulation of neurotransmitter transporters?

<p>Uric acid transporters (C)</p> Signup and view all the answers

Which of the following neurotransmitters is NOT primarily transported by an Na+/Cl- dependent transporter?

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

Which of these is NOT a known side effect of SSRIs?

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

Which of the following is a key mechanism by which antidepressants exert their therapeutic effects?

<p>By increasing the levels of norepinephrine and serotonin in the synapse (A)</p> Signup and view all the answers

The concept of 'desensitization' refers to the phenomenon where repeated exposure to a drug leads to a decrease in its effectiveness.

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

Which of the following is NOT a potential mechanism of desensitization for a G protein-coupled receptor?

<p>Increased receptor synthesis (B)</p> Signup and view all the answers

What is the primary function of RGS (regulators of G protein signaling) proteins?

<p>To enhance the intrinsic GTPase activity of G proteins, leading to faster hydrolysis of GTP (A)</p> Signup and view all the answers

What is the main difference between RAMPs and RGS proteins?

<p>RAMPs determine the specificity of ligand binding to a GPCR, while RGS proteins regulate the duration and strength of GPCR signaling (B)</p> Signup and view all the answers

What is the main role of ion channels in cellular function?

<p>To regulate the flow of ions across the cell membrane, influencing the membrane potential (C)</p> Signup and view all the answers

Which of these is NOT a mechanism of drug action for voltage-gated ion channels?

<p>Promoting the synthesis of new ion channels (C)</p> Signup and view all the answers

Which of the following is an example of a drug commonly used to target a voltage-gated sodium channel?

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

Which of the following is NOT a characteristic of the 'rotating helix' model for voltage-gated ion channel activation?

<p>The voltage sensor is located in the intracellular portion of the protein. (A)</p> Signup and view all the answers

Which of the following is NOT a mechanism by which drugs can alter the activity of voltage-gated ion channels?

<p>Direct activation of the channel protein (A)</p> Signup and view all the answers

The inactivation gate of a voltage-gated sodium channel plays a critical role in regulating the duration of the action potential by promoting rapid inactivation of the channel.

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

What is the main physiological importance of the sodium-potassium pump in the cell?

<p>To maintain the membrane potential and create an electrochemical gradient across the cell membrane (B)</p> Signup and view all the answers

Which of the following is NOT a common mechanism by which drugs can target the sodium potassium pump?

<p>Activation of the pump's signaling pathway (D)</p> Signup and view all the answers

Which of these is an example of a drug that targets the sodium potassium pump?

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

Which of these is NOT a common therapeutic indication for H+/K+ ATPase (proton pump) inhibitors?

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

What is the main advantage of using potassium-sparing diuretics?

<p>They are less likely to cause side effects such as hypokalemia. (A)</p> Signup and view all the answers

Loop diuretics can be classified among the most potent group of diuretics, and they are typically used as the first-line treatment for managing severe edema.

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

Flashcards

Molecular Pharmacology

A field of study that investigates how drugs interact with biological systems at the molecular level. It focuses on the mechanisms of action of drugs, their binding to target proteins, and the signaling pathways they activate or inhibit.

Pharmacokinetics

The study of how drugs affect the body's overall function, encompassing all stages from absorption to elimination.

Pharmacodynamics

The study of the effects of drugs on the body, including the mechanisms by which they exert their therapeutic or adverse effects. It focuses on the interaction between drugs and their target molecules.

Pharmacogenetics

A subfield of pharmacology that investigates how genetic differences between individuals influence their response to drugs.

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Pharmacogenomics

An extension of pharmacogenetics that examines the influence of the entire genome on drug response. It explores the broader genetic landscape and its impact on drug action.

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Drug Discovery

The process of identifying new drugs or biological targets that can be used to modify a specific pathway and treat a disease. It typically involves screening large libraries of compounds or genes, and then evaluating the effects of these candidates on the target under investigation.

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Functional Studies

A phenotypic screening approach that uses high-throughput techniques to identify compounds that exhibit a particular biological activity or effect. It often involves testing large libraries of compounds against cells or biological systems.

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Target-Oriented Approach

A strategy for drug discovery that begins by identifying a specific target molecule and then seeking compounds that bind to and affect the function of that target. This approach often relies on knowledge of disease mechanisms, genomics, and molecular target biology.

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Reverse Pharmacology

An approach to drug discovery that starts with an observed pharmacological effect and then seeks to identify the molecular target responsible for that effect. It's often used to discover the targets of traditional remedies or drugs whose mechanisms were previously unknown.

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Genome Project

A comprehensive study of an organism's entire genetic makeup. It involves sequencing and analyzing all the DNA present in an individual, providing insights into genetic variation, disease susceptibility, and drug response.

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Genome-wide Association Studies (GWAS)

A type of genetic research that investigates the association between specific genetic variations and the risk of developing a disease. It compares the genomes of large populations of individuals with and without a particular disease to identify genetic variations that may be linked to the disease's development.

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Loss of Function (LOF) Mutations

Genetic variants or mutations that have a protective effect against a particular disease, reducing an individual's risk of developing that condition. These variations can provide valuable insights into disease pathways and suggest potential drug targets.

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Personalized Medicine

A drug development strategy that focuses on tailoring treatment plans to the unique genetic makeup of each individual. It aims to optimize drug selection and dosage based on individual genetic variations, aiming to improve treatment efficacy and reduce side effects.

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Targeted Therapies

A type of therapeutic approach that targets specific proteins or pathways involved in the development or progression of a disease. This approach often involves using drugs that specifically bind to and modulate the function of those targets, aiming to achieve a therapeutic effect.

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Biopharmaceuticals/Biologics

A category of drugs that are large, complex molecules often derived from biological sources. Examples include antibodies, proteins, and nucleic acid-based compounds.

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ADME (Absorption, Distribution, Metabolism, Excretion)

The process by which drugs are absorbed, distributed, metabolized, and eliminated from the body. It describes the movement of drugs through the body from the time they are administered to the time they are eliminated.

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Specificity of Drugs

A drug's ability to bind selectively to its intended molecular target. It reflects the degree to which a drug preferentially interacts with its intended target, minimizing off-target effects and improving therapeutic effectiveness.

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Redundancy in Biological Systems

A property of biological systems that allows multiple pathways or molecules to contribute to a similar response. This redundancy can compensate for the loss or inhibition of individual pathways or molecules, making it difficult to target a single pathway or molecule effectively.

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Agonist

A type of drug interaction that involves the binding of a drug to a receptor molecule, triggering a response that mimics or enhances the action of the natural ligand. These drugs activate the same signaling pathways as the natural ligand.

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Antagonist

A type of drug interaction that involves the binding of a drug to a receptor molecule, blocking the action of the natural ligand and preventing its activity. These drugs prevent the natural ligand from activating its signaling pathways.

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Target Validation

The process of validating a potential drug target by demonstrating that modulating its function has a therapeutic effect in a disease model. It typically involves evaluating the effects of drugs that target the candidate target in preclinical or clinical trials.

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Druggability

The ability of a target molecule to be effectively modulated by a drug. It considers factors such as the target's accessibility, size, and suitability for binding to small molecules.

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Rare Variants

A rare genetic variation that can lead to a protective effect against a disease. These variations provide evidence that modulating the corresponding gene or protein may be a viable therapeutic strategy.

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Targeted Drug Delivery

A therapeutic approach that aims to deliver a drug directly to a specific location within the body, such as a tumor or specific tissue. This targeted delivery can improve drug efficacy and minimize side effects.

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Target Therapy

A type of drug that specifically targets a particular protein or pathway associated with a disease. These drugs are often designed to inhibit or modulate the activity of the target molecule, aiming to achieve a therapeutic effect.

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Monoclonal Antibody

A type of antibody that specifically binds to a particular target molecule, such as a protein on the surface of a cell. It can be used to block the activity of the target or deliver a therapeutic payload directly to the target cell.

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Bispecific Antibodies

A class of biopharmaceuticals that are engineered fusion proteins comprised of two or more antibodies or binding domains. They can target multiple molecules simultaneously, increasing their therapeutic potential.

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Antibody-Drug Conjugates (ADCs)

A type of antibody conjugated to a cytotoxic drug. They target specific cells or tumors and deliver the drug directly to the target cells, reducing systemic toxicity.

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Small Molecules

A category of drugs that are small, non-protein molecules. They typically interact with their target molecules through non-covalent bonds, such as hydrogen bonds or van der Waals forces.

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Drug Tolerance

A term describing the phenomenon where prolonged exposure to a drug leads to a decrease in its effectiveness. The body adapts to the drug's presence, requiring higher doses to achieve the same effect.

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Drug Addiction

A state of dependence on a drug, characterized by withdrawal symptoms when the drug is discontinued. It often occurs after repeated exposure to the drug and involves physiological and psychological dependence.

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Study Notes

Molecular and Experimental Pharmacology - Pharmacotherapy

  • Molecular pharmacology focuses on the molecular mechanisms of drug action, explaining how drugs produce their effects. It starts by identifying the target molecule and the mechanism of drug action and understanding signaling pathways.
  • Drug targets can be diverse molecular targets, structural features, or the localization of the drug.
  • Molecular target identification is increasingly important in drug discovery, with genomic studies being used to identify disease-related targets (reverse pharmacology).
  • The drug discovery process traditionally involved functional studies, but the current trend is to identify the molecular target first and then design drugs based on that target (reverse pharmacology).
  • High-throughput screening of potential drug candidates is used to identify compounds that interact with the target molecule.
  • Functional studies evaluate biological responses to identify the most effective drugs. This involves screening for compounds that affect biological response
  • After identifying the target, functional studies assess the efficacy and side effects
  • Pharmacodynamics describes the effects of drugs on the body; pharmacogenetics/pharmacogenomics examines how genetic variations affect drug response.
  • Pharmacodynamics explains how drugs affect the body.

Drug Discovery Process

  • Drug discovery is multifaceted and employs a variety of techniques. This process includes characterizing new biological activities.

Pharmacokinematics

  • Pharmacokinematics is the study of how the body processes drugs, including absorption, distribution, metabolism, and excretion (ADME).

Pharmacodynamics

  • The study of the effects of drugs on the body, including their mechanisms of action.
  • The mechanism of drug action can focus at different levels:
  • Molecular- drug's target (receptor, ion channel, enzyme, carrier)
  • Cellular- biochemical processes related to the target
  • Tissue- effects on tissue function due to signaling change
  • System-effects on systems function
  • Examples of drug targets, their mechanism of action, and related diseases

Drugs and targets with low specificity

  • Several drugs targeting multiple targets by accident producing unwanted effects
  • Unselective interactions with a particular target producing several drugs for a specific disorder

Genetic support to drug discovery

  • Studying the rare variants associated with a favorable phenotype
  • Studying gene variations associated with diseases and tumors to identify new targets
  • Genome-wide association studies (GWAS)

Drugs target

  • Drugs interact at the molecular levels on the different parts of the cell but there are few molecular targets
  • Compounds that bind to a target electively and with high affinity are suitable targets for future drug development.
  • Receptors for small endogenous ligands or enzymes (protein kinases and ATPs) are more drug-able
  • Receptors for peptides or proteins might be harder to target by small molecules

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