Pharmacodynamics Study: Targets for Drug Action
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Questions and Answers

Pharmacodynamics is the division of pharmacology that studies what the body does to the drug.

False

Most drugs are effective because they bind to specific target proteins like enzymes, carriers, and ion channels.

True

Cytotoxic drugs work by stimulating physiological functions.

False

Bulk laxatives exert their mechanism of action through chemical interactions.

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

Enzymes can be inhibited by both competitive and non-competitive inhibition.

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

Epinephrine acts on alpha receptors in the heart.

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

Competitive antagonism results in a curve that shifts to the left without a change in slope.

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

Non-competitive antagonism can be reversed by increasing the concentration of the agonist drug.

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

Tachyphylaxis refers to a gradual increase in responsiveness to a drug over time.

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

Irreversible antagonism is characterized by the drug binding to an allosteric site on the receptor.

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

Tolerance is a phenomenon that develops within minutes of drug administration.

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

Competitive antagonism involves drugs that exert an antagonistic effect without competing for receptor occupancy.

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

Partial agonists have low affinity and high intrinsic activity.

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

Antagonists bind to receptors and elicit tissue responses.

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

High affinity drugs bind well and remain long enough to activate receptors.

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

Antagonists have high affinity but no intrinsic activity.

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

Full agonists have low intrinsic activity and low affinity.

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

Potency refers to the intensity of the drug effect produced by a given amount or dose of the drug.

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

The process of down regulation of receptors occurs due to excessive exposure to antagonists.

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

Exhaustion of mediators can lead to an increase in essential immediate substances.

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

Increased metabolic degradation results in a progressive increase in plasma concentration of a drug.

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

Therapeutic Index (TI) is calculated as TD50 / ED50.

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

Nicotinic receptor is an example of a receptor linked to G-proteins.

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

The rate at which drugs act depends on the dose administered.

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

G-protein-coupled receptors mainly use cAMP and IP3 as their principal third messengers.

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

Adenylate cyclase catalyzes the conversion of cAMP to ATP.

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

IP3 is responsible for controlling the release of sodium ions from intracellular stores.

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

Kinase-linked receptors are mainly involved in events controlling cell death.

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

The Jak/Stat pathway is activated by many cytokines and controls the synthesis and release of many anti-inflammatory mediators.

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

The insulin receptor autophosphorylates in response to insulin.

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

Study Notes

Pharmacodynamics Overview

  • Studies how the body affects drugs and their mechanisms of action.
  • Drug efficacy primarily depends on binding to specific target proteins, including enzymes, carriers, and ion channels.

Mechanisms of Drug Action

  • Cytotoxic drugs enhance physiological functions to exert their effects.
  • Bulk laxatives operate through chemical interactions.
  • Enzymatic activity can be modulated by competitive and non-competitive inhibition.
  • Epinephrine specifically targets alpha receptors in the heart.

Types of Antagonism

  • Competitive antagonism shifts drug response curves to the left without altering slope.
  • Non-competitive antagonism can be reversed by increasing agonist concentration.
  • Irreversible antagonism involves drugs binding to allosteric sites on receptors.

Drug Response and Tolerance

  • Tachyphylaxis refers to diminished responses to a drug after repeated dosage over time.
  • Tolerance can develop quickly, sometimes within minutes of administration.

Agonists and Antagonists

  • Competitive antagonists block receptor activity without directly occupying receptors.
  • Partial agonists possess low affinity combined with high intrinsic activity.
  • Full agonists exhibit low intrinsic activity with low affinity.
  • Antagonists can bind with high affinity but lack intrinsic activity, resulting in no tissue response.

Drug Potency and Efficacy

  • Potency indicates the degree of drug effect relative to the dosage.
  • Therapeutic Index (TI) calculated as TD50 (toxic dose for 50% of the population) divided by ED50 (effective dose for 50%).

Receptor Dynamics

  • Downregulation of receptors occurs with excessive exposure to antagonists.
  • Exhaustion of mediators increases the demand for essential immediate substances.
  • Enhanced metabolic degradation leads to elevated plasma concentrations of a drug.

Receptor Types and Signaling Pathways

  • Nicotinic receptors are an example of receptors associated with G-proteins.
  • G-protein-coupled receptors predominantly use cAMP and IP3 as third messengers.
  • Adenylate cyclase catalyzes cAMP conversion to ATP.
  • IP3's role includes regulating sodium ion release from intracellular stores.
  • Kinase-linked receptors play a key role in processes linked to cell death.
  • The Jak/Stat pathway is triggered by various cytokines, controlling the synthesis of anti-inflammatory mediators.
  • The insulin receptor undergoes autophosphorylation upon insulin binding.

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Learn about Pharmacodynamics, the division of pharmacology that focuses on the effects of drugs and their mechanisms of action on the body. Explore how drugs interact with target proteins to produce their physiological effects.

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