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ANKI PHARMACODZNAMICS
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Flashcards in this deck (283)

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  • What is pharmacodynamics?

    The study of how drugs affect the body.

    pharmacology definitions

  • What factors affect drug action?

    • Drug dose
    • Route of administration
    • Onset of action
    • Duration of action
    pharmacology factors

  • Define potency in pharmacodynamics.

    The amount of drug needed to produce a desired effect.

    pharmacology potency

  • What is efficacy in drug action?

    The maximum effect a drug can produce.

    pharmacology efficacy

  • How do agonists work?

    They activate receptors to produce a biological response.

    pharmacology agonists

  • What role do antagonists play?

    They block receptors and prevent a biological response.

    pharmacology antagonists

  • What is the therapeutic index?

    The ratio between the toxic dose and effective dose of a drug.

    pharmacology therapeutic_index

  • Define bioavailability.

    The proportion of a drug that enters circulation when introduced into the body.

    pharmacology bioavailability

  • What does half-life measure?

    The time it takes for the concentration of a drug to reduce to half its initial value.

    pharmacology half_life

  • What is dose-response relationship?

    The relationship between the dose of a drug and the magnitude of its pharmacological effect.

    pharmacology dose_response

  • What can tolerance lead to in pharmacotherapy?

    Reduced response to a drug after repeated use.

    pharmacology tolerance

  • What is the significance of receptor phosphorylation?

    It can alter receptor activity and signaling potency.

    pharmacology receptors

  • What are enzyme inhibitors?

    Substances that decrease enzyme activity, affecting drug metabolism.

    pharmacology enzyme_inhibitors

  • What effect do enzyme inducers have?

    They increase enzyme activity, leading to faster drug metabolism.

    pharmacology enzyme_inducers

  • What is the importance of clinical trials in pharmacodynamics?

    They help evaluate the safety and efficacy of drug therapies.

    pharmacology clinical_trials

  • Identify a key aspect of patient variability in drug response.

    Genetic differences can affect drug metabolism and action.

    pharmacology variability

  • What is the impact of age on pharmacodynamics?

    Age affects drug absorption, distribution, metabolism, and excretion.

    pharmacology age_effect

  • How can drug interactions alter therapeutic effects?

    They can either enhance or diminish drug actions and side effects.

    pharmacology interactions

  • Define agonist-antagonist activity.

    Drugs that activate some receptors while blocking others.

    pharmacology agonist_antagonist

  • What is maximal efficacy?

    The greatest intensity of effect that a drug can produce.

    pharmacology efficacy

  • Explain the concept of selectivity in pharmacodynamics.

    The ability of a drug to preferentially elicit responses from one receptor subtype over others.

    pharmacology selectivity

  • What is the study of what the drug does to the body called?

    Pharmacodynamics

    pharmacology

  • What does pharmacokinetics study?

    What the body does to the drug.

    pharmacology

  • What processes are included in pharmacokinetics?

    • Absorption
    • Distribution
    • Metabolism
    • Excretion
    pharmacology processes

  • What are the four major questions pharmacodynamics answers?

    • How are drug effects produced?
    • What type of effects are produced?
    • How much effect at different doses?
    • How are effects modified?
    pharmacodynamics questions

  • What does 'action' refer to in pharmacodynamics?

    The initial combination of the drug with its target molecule.

    pharmacodynamics action

  • What does 'effect' refer to in pharmacodynamics?

    The measurable change in physiological function from the drug's action.

    pharmacodynamics effect

  • What is the action of Captopril?

    Inhibits angiotensin-converting enzyme (ACE).

    pharmacodynamics drugs

  • What is the effect of Captopril?

    Vasodilation, leading to a fall in blood pressure.

    pharmacodynamics effects

  • Why is it important to understand drug action?

    Different drugs can produce the same effect via different mechanisms.

    pharmacodynamics importance

  • What is the common mechanism of drug action?

    Inhibition of enzymes.

    pharmacodynamics enzymes

  • What are the main targets of drug action?

    • Enzymes
    • Transport proteins
    • Receptors
    • Other biomolecules
    pharmacodynamics targets

  • How can a drug alter biochemical reaction rates?

    By modulating enzyme activity.

    pharmacodynamics biochemistry

  • What types of proteins do most drugs target?

    Functional proteins.

    pharmacodynamics proteins

  • What are structural proteins?

    Proteins that form the body's framework, e.g., collagen.

    pharmacodynamics proteins

  • What happens when enzymes are inhibited by drugs?

    The rate of biochemical reactions is altered.

    pharmacodynamics enzymes

  • Is stimulation of enzymes common in drug action?

    No, it is rare.

    pharmacodynamics enzymes

  • What is competitive inhibition?

    It's when an inhibitor competes with the substrate for the active site. Can be reversible or irreversible.

    enzymology inhibition

  • What types can competitive inhibition be?

    • Reversible (equilibrium type)
    • Irreversible (nonequilibrium type)
    enzymology inhibition

  • What is noncompetitive inhibition?

    It's when an inhibitor binds to an enzyme, reducing its activity regardless of the substrate concentration.

    enzymology inhibition

  • What is the function of an enzyme?

    Enzymes act as catalysts to accelerate biochemical reactions.

    biochemistry enzymes

  • What is an enzyme's catalytic site?

    It's the active site where the substrate binds to undergo a reaction, similar to the blades of scissors.

    biochemistry enzymes

  • What happens when a substrate binds to an enzyme?

    The substrate undergoes a biochemical reaction to form a product.

    biochemistry enzyme_reaction

  • What is the role of inhibitors in enzyme activity?

    Inhibitors decrease enzyme activity by blocking the active site or altering enzyme shape.

    enzymology inhibition

  • How does reversible inhibition differ from irreversible inhibition?

    • Reversible: inhibitor can dissociate from enzyme
    • Irreversible: inhibitor permanently deactivates enzyme
    enzymology inhibition

  • What is one characteristic of a competitive inhibitor?

    It structurally resembles the substrate and binds to the active site of the enzyme.

    enzymology inhibition

  • What is an example of an enzyme action?

    An enzyme converting a substrate like glucose into glucose-6-phosphate.

    biochemistry enzymes

  • What does enzyme velocity depend on?

    The number of active enzyme molecules.

    biochemistry enzymes

  • What is the Michaelis constant (kM)?

    Substrate concentration at which half of the enzyme molecules are active.

    biochemistry constants

  • What does Vmax represent?

    Maximum rate of the enzyme-catalyzed reaction when fully saturated with substrate.

    biochemistry enzymes

  • What happens at low substrate concentration?

    Few enzymes are active.

    biochemistry enzymes

  • What is competitive inhibition?

    Inhibition where a drug resembles the substrate and competes for the same catalytic site.

    biochemistry inhibition

  • Effect of competitive inhibition on kM?

    kM increases because more substrate is needed for half-maximal enzyme activity.

    biochemistry inhibition

  • What is reversible competitive inhibition?

    Inhibitor binds weakly and can be displaced by substrate, Vmax remains unchanged.

    biochemistry inhibition

  • Example of reversible competitive inhibitor?

    Physostigmine inhibits cholinesterase and can be overcome by increasing acetylcholine.

    biochemistry inhibition

  • What is irreversible competitive inhibition?

    Inhibitor binds strongly and forms a covalent bond, cannot be displaced by substrate.

    biochemistry inhibition

  • Effect of irreversible competitive inhibition on Vmax?

    Vmax decreases because fewer active enzyme molecules are available.

    biochemistry inhibition

  • Example of an irreversible competitive inhibitor?

    Organophosphate compounds inhibit cholinesterase irreversibly.

    biochemistry inhibition

  • What is noncompetitive inhibition?

    Inhibitor binds to a different site on the enzyme, causing structural changes and Vmax decreases.

    biochemistry inhibition

  • Effect of noncompetitive inhibition on kM?

    kM remains unchanged.

    biochemistry inhibition

  • Example of a noncompetitive inhibitor?

    Aspirin inhibits cyclooxygenase (COX) noncompetitively.

    biochemistry inhibition

  • Summary of reversible competitive inhibition?

    • Binds weakly to the same site as substrate
    • kM increases, Vmax unchanged.
    biochemistry inhibition

  • Summary of irreversible competitive inhibition?

    • Binds strongly (covalently)
    • kM increases, Vmax decreases.
    biochemistry inhibition

  • Summary of noncompetitive inhibition?

    • Binds to a different site
    • kM unchanged, Vmax decreases.
    biochemistry inhibition

  • What do transport proteins do?

    Control the movement of ions and molecules across biological membranes.

    biology transport

  • What are the main types of transport proteins?

    • Ion pumps
    • Carrier proteins
    • Ion channels
    biology transport

  • What is the role of ion pumps?

    Move ions against concentration gradients using ATP.

    biology transport

  • What is an example of an ion pump?

    Na+/K+-ATPase pump – Maintains sodium and potassium balance.

    biology transport pumps

  • What do carrier proteins do?

    Utilize ion gradients created by pumps to transport substances.

    biology transport

  • Give an example of a carrier protein.

    Na+/Cl- cotransporter in the renal tubules.

    biology transport carrier

  • What function do ion channels serve?

    Allow passive movement of ions down their electrochemical gradient.

    biology transport

  • How do drugs affect transport proteins?

    They can inhibit or stimulate their activity.

    pharmacology transport

  • What is the effect of digoxin on Na+/K+-ATPase?

    • Inhibits Na+/K+-ATPase
    • Increases intracellular sodium
    • Enhances cardiac contractility.
    pharmacology drugs heart

  • What drug inhibits noradrenaline reuptake?

    Cocaine - Blocks noradrenaline transporter (NET).

    pharmacology drugs nervous_system

  • What do thiazide diuretics inhibit?

    Inhibit Na+/Cl- cotransporter in the distal convoluted tubule.

    pharmacology drugs kidney

  • What is the effect of omeprazole?

    Inhibits H+/K+-ATPase enzyme, reducing gastric acidity.

    pharmacology drugs digestive

  • How do SSRIs work?

    Block serotonin reuptake, enhancing serotonergic transmission.

    pharmacology drugs mood

  • What is one mechanism of drug action related to receptors?

    Modulating the activity of specialized macromolecules, usually proteins.

    pharmacology drugs receptors

  • What does a receptor bind?

    A drug or endogenous chemical messenger (e.g., hormone, neurotransmitter)

    biology receptors

  • What is the function of receptors?

    To recognize drug molecules and transduce their signals into biological effects

    biology receptors

  • What happens when a drug binds to a receptor?

    • It can activate the receptor (agonist)
    • It can block the receptor (antagonist)
    pharmacology receptors

  • What is an agonist?

    A substance that activates a receptor

    pharmacology agonists

  • What is an antagonist?

    A substance that blocks a receptor

    pharmacology antagonists

  • What type of response do receptors initiate?

    A cellular response

    biology cellular

  • What are endogenous chemical messengers?

    Substances like hormones and neurotransmitters produced within the body

    biology messengers

  • What is the role of a drug in receptor interactions?

    To modulate biological effects by binding to receptors

    pharmacology drugs

  • Can drugs act as both agonists and antagonists?

    Yes, based on their interaction with specific receptors

    pharmacology receptors

  • What determines the effect of a drug on a receptor?

    Whether it acts as an agonist or antagonist

    pharmacology effects

  • What is an agonist?

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

    pharmacology agonists

  • What is an antagonist?

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

    pharmacology antagonists

  • What do agonists mimic?

    The effect of endogenous substances.

    pharmacology agonists

  • What do antagonists block?

    The effects of agonists.

    pharmacology antagonists

  • What are ligand-gated ion channels?

    Integral membrane proteins that form ion channels, opening upon agonist binding.

    receptors ion_channels

  • What happens when an agonist binds to ligand-gated ion channels?

    The channel opens, allowing ions to cross the membrane.

    receptors ion_channels

  • Give an example of a ligand-gated ion channel.

    Nicotinic acetylcholine receptor (nAChR).

    receptors examples

  • What is the effect of acetylcholine binding to nAChR?

    Opens the channel, allowing sodium in and potassium out, leading to muscle contraction.

    physiology muscle

  • What is an example of an agonist for nAChR?

    Nicotine.

    pharmacology agonists

  • What is an example of an antagonist for nAChR?

    Tubocurarine (causes muscle relaxation).

    pharmacology antagonists

  • What are G-protein-coupled receptors?

    Receptors coupled to intracellular G-proteins that modulate enzymes or ion channels.

    receptors g-protein

  • What is the mechanism of G-protein-coupled receptors?

    Agonist binds, activating G-protein, which modulates effectors.

    receptors mechanisms

  • What are the key second messengers involved in G-protein signaling?

    • cAMP
    • IP3
    • DAG
    receptors second_messengers

  • Give an example of a G-protein-coupled receptor.

    Beta-adrenergic receptor, activated by adrenaline.

    receptors examples

  • What does the binding of adrenaline to beta receptors do?

    Stimulates adenylate cyclase, increasing cAMP levels.

    physiology beta_receptors

  • What are enzyme-linked receptors?

    Transmembrane proteins with intrinsic enzymatic activity, activating upon ligand binding.

    receptors enzyme-linked

  • What type of receptor is the insulin receptor?

    A tyrosine kinase receptor.

    receptors insulin

  • What happens when insulin binds to its receptor?

    Activates tyrosine kinase, leading to phosphorylation of intracellular proteins.

    physiology insulin

  • Give a drug example that acts as an agonist at insulin receptors.

    Recombinant human insulin.

    pharmacology agonists

  • What are intracellular receptors?

    Receptors located in the cytoplasm or nucleus that bind lipid-soluble substances.

    receptors intracellular

  • How do intracellular receptors affect cellular function?

    By interacting with DNA to regulate gene transcription.

    physiology gene_expression

  • What kind of ligands activate intracellular receptors?

    Lipid-soluble substances.

    receptors ligands

  • Give an example of an intracellular receptor ligand.

    Steroid hormones like glucocorticoids.

    hormones intracellular

  • What action does prednisolone have?

    Acts on intracellular glucocorticoid receptors to suppress inflammation.

    pharmacology prednisolone

  • What does levothyroxine regulate?

    Metabolism by acting on nuclear thyroid hormone receptors.

    pharmacology levothyroxine

  • What is the response time for G-protein-coupled receptors?

    Intermediate response (seconds), involving second messengers.

    biology receptors

  • What defines enzyme-linked receptors?

    Slow response (minutes to hours), mediated by phosphorylation cascades.

    biology receptors

  • What is the response time for intracellular receptors?

    Very slow response (hours to days).

    biology receptors

  • What is the main function of ligand-gated ion channels?

    Mediates ion fluxes for fast signaling.

    biology receptors

  • What role do G-protein-coupled receptors play in signaling?

    Involve second messengers for cellular responses.

    biology receptors

  • How do enzyme-linked receptors facilitate cellular responses?

    Through phosphorylation cascades over minutes to hours.

    biology receptors

  • What type of response do intracellular receptors provide?

    Provides very slow responses over hours to days.

    biology receptors

  • What is a Full Agonist?

    Produces the maximum possible response by fully activating receptors.

    pharmacology agonists

  • What is a Partial Agonist?

    Binds to receptors but produces a submaximal response even at full occupancy.

    pharmacology agonists

  • How does a Partial Agonist act?

    Can act as both an agonist and an antagonist depending on context.

    pharmacology agonists

  • What is an Inverse Agonist?

    Binds to the same receptor as an agonist but induces an opposite response.

    pharmacology agonists

  • What is the function of an Antagonist?

    Binds to the receptor without activating it, preventing agonist binding.

    pharmacology antagonists

  • What are the two types of Antagonists?

    • Competitive (reversible)
    • Noncompetitive (irreversible)
    pharmacology antagonists

  • How does Adrenaline function as a drug?

    Acts as an agonist on beta receptors to increase heart rate.

    pharmacology drugs

  • What is the role of Propranolol?

    Acts as a beta receptor antagonist to decrease heart rate and blood pressure.

    pharmacology drugs

  • How does Diazepam affect neurotransmission?

    Enhances GABA receptor activity, increasing chloride ion influx and causing sedation.

    pharmacology drugs

  • What effect does Atropine have on the body?

    Blocks muscarinic receptors, reducing secretions and dilating pupils.

    pharmacology drugs

  • What does Prednisolone activate?

    Activates intracellular glucocorticoid receptors to produce anti-inflammatory effects.

    pharmacology drugs

  • What is the dose-response relationship?

    It is the relationship between the dose of a drug and the magnitude of its effect.

    pharmacodynamics drug_action

  • What does the dose-response relationship help determine?

    • Minimum dose for therapeutic effect.
    • Maximum achievable effect.
    • Safety margin of the drug.
    pharmacodynamics drug_action

  • What are the two types of dose-response relationships?

    • Graded dose-response relationship
    • Quantal dose-response relationship
    pharmacodynamics types

  • Explain the graded dose-response relationship.

    Response measured continuously; increases with dose (e.g. blood pressure response).

    pharmacodynamics graded_response

  • What happens in the linear region of the sigmoid curve?

    Small dose increases result in large response increases.

    pharmacodynamics linear_region

  • What occurs in the plateau region of the dose-response curve?

    Response reaches maximum (Emax); further increases won't enhance effect.

    pharmacodynamics plateau_region

  • Define Emax.

    The greatest effect produced by the drug regardless of dose.

    pharmacodynamics emax

  • What is EC50?

    Concentration producing 50% of maximum response; indicates potency.

    pharmacodynamics ec50

  • What does a steep slope indicate on the dose-response curve?

    Small dose changes lead to large effect changes.

    pharmacodynamics slope

  • Differentiate between efficacy and potency.

    • Efficacy: maximum effect (Emax).
    • Potency: amount needed for a specific effect.
    pharmacodynamics efficacy potency

  • What is the receptor occupancy theory?

    Response is proportional to the fraction of receptors occupied.

    pharmacodynamics receptor_theory

  • Describe the quantal dose-response relationship.

    All-or-none response representing percentage of a population showing effect.

    pharmacodynamics quantal_response

  • Example of a quantal response?

    Percentage of subjects falling asleep with varying sedative doses.

    pharmacodynamics quantal_response

  • Graphing which relationship uses a logarithmic scale?

    Both graded and quantal dose-response relationships.

    pharmacodynamics graphing

  • What shape does the curve take when drug sensitivity data is plotted?

    A sigmoid (S-shaped) curve.

    pharmacology graphs

  • What does the y-axis represent when plotting drug sensitivity data?

    The distribution of sensitivity to the drug.

    pharmacology data_analysis

  • What type of curve is obtained when data is plotted?

    A frequency distribution curve.

    statistics graphs

  • What does a sigmoid curve indicate in drug sensitivity studies?

    Intermediate sensitivity levels among subjects.

    pharmacology statistics

  • What is ED50?

    The dose producing the desired effect in 50% of the population.

    pharmacology dosage

  • What does TD50 represent?

    The dose producing a toxic effect in 50% of the population.

    pharmacology toxicity

  • What is the definition of LD50?

    The dose causing death in 50% of experimental animals.

    pharmacology lethality

  • What is the Therapeutic Index (TI)?

    The ratio of TD50 to ED50; indicates drug safety.

    pharmacology safety

  • What does a high TI indicate?

    The drug is relatively safe; toxic dose is much higher than effective dose.

    pharmacology safety

  • What does a low TI signify?

    The drug is potentially dangerous; effective and toxic doses are close.

    pharmacology safety

  • Which drug has a high TI?

    Penicillin; considered very safe.

    pharmacology safety

  • Which drugs have low TIs?

    Digoxin, lithium, warfarin; require close monitoring.

    pharmacology monitoring

  • What is the therapeutic window?

    The range between minimum effective concentration (MEC) and minimum toxic concentration (MTC).

    pharmacology dosage

  • What defines narrow therapeutic windows?

    Require frequent plasma level monitoring to avoid toxicity.

    pharmacology monitoring

  • How does body weight affect drug dosage?

    Doses are calculated per kilogram; larger mass = higher doses.

    pharmacology physiology

  • How do lipophilic drugs distribute in obese individuals?

    They accumulate in adipose tissue, causing prolonged effects.

    pharmacology physiology

  • What are the drug metabolism effects in newborns?

    Reduced liver and kidney function; careful dose adjustments needed.

    pharmacology age

  • What syndrome can chloramphenicol cause in infants?

    Gray baby syndrome; due to immature metabolism.

    pharmacology toxicity

  • What age-related change affects the elderly?

    Reduced renal clearance and liver metabolism; sensitivity to drugs increases.

    pharmacology age

  • How do hormonal differences affect drug metabolism in sexes?

    Women may metabolize drugs (e.g., alcohol) slower.

    pharmacology sex

  • How does pregnancy impact pharmacokinetics?

    Increased plasma volume, renal clearance, and protein binding changes.

    pharmacology pregnancy

  • What toxicity can occur in cats with certain drugs?

    Inability to metabolize paracetamol efficiently; leads to toxicity.

    pharmacology species

  • How do genetic factors alter drug response?

    Variations in enzymes and receptors can significantly influence outcomes.

    pharmacology genetics

  • What is an example of a pharmacogenetic variation?

    Slow and fast acetylators affect isoniazid metabolism.

    pharmacology genetics

  • How can G6PD deficiency affect drug use?

    Increases risk of hemolysis with certain drugs like primaquine.

    pharmacology genetics

  • What can happen when increasing doses of a medication are required?

    May require increasing doses to maintain the same effect.

    pharmacology medications

  • Name examples of medications that may require increasing doses.

    • Opioids
    • Nitrates
    • Barbiturates
    pharmacology examples

  • What is tachyphylaxis?

    A rapid decrease in drug response after a few doses in quick succession.

    pharmacology definitions

  • Give examples of drugs that show tachyphylaxis.

    • Ephedrine
    • Tyramine
    pharmacology examples

  • What causes tachyphylaxis in ephedrine and tyramine?

    Depletion of stored noradrenaline.

    pharmacology mechanisms

  • What occurs in drug interactions?

    When two or more drugs affect each other's action.

    pharmacology interactions

  • What are pharmacodynamic interactions?

    • Occur at the site of action
    • Examples: synergism or antagonism
    pharmacology interactions

  • What are pharmacokinetic interactions?

    • Affect absorption, metabolism, or excretion
    • Examples: enzyme induction or inhibition
    pharmacology interactions

  • How does aspirin influence the effect of warfarin?

    • Enhances the effect
    • Example of pharmacodynamic synergism
    pharmacology drug_interactions

  • What effect does rifampicin have on oral contraceptives?

    • Induces hepatic enzymes
    • Reduces effectiveness
    • Example of pharmacokinetic induction
    pharmacology drug_interactions

  • What effect does erythromycin have on theophylline?

    • Inhibits metabolism
    • Increases toxicity
    • Example of pharmacokinetic inhibition
    pharmacology drug_interactions

  • What environmental factors can modify drug action?

    • Temperature
    • Altitude
    • Diet
    • Exposure to chemicals
    pharmacology environment

  • How does high environmental temperature affect drug action?

    • Enhances vasodilation
    • Can potentiate hypotensive effects
    pharmacology environment

  • What is the placebo effect?

    • Response from an inert substance
    • Due to patient's belief in treatment
    pharmacology psychology

  • Which substances can affect enzyme induction?

    • Cigarette smoke
    • Pesticides
    pharmacology environment

  • How can psychological factors influence drug responses?

    • Affects responses, especially with CNS-active drugs
    • Examples: analgesics, sedatives, antidepressants
    pharmacology psychology

  • What is drug antagonism?

    A phenomenon where the effect of one drug is inhibited by another drug.

    pharmacology drug_interaction

  • What is synergism?

    When two drugs enhance each other's effects.

    pharmacology drug_interaction

  • When can antagonism be beneficial?

    To counteract poisoning or overdose (e.g., naloxone with morphine).

    pharmacology benefits

  • When can antagonism be harmful?

    When an essential therapeutic effect is blocked (e.g., beta-blockers with beta-agonists).

    pharmacology dangers

  • What are the types of drug antagonism?

    • Physical antagonism
    • Chemical antagonism
    • Physiological antagonism
    • Pharmacological antagonism
    pharmacology types

  • What is physical antagonism?

    When two drugs physically oppose each other's actions without chemical reaction.

    pharmacology physical

  • Give an example of physical antagonism.

    • Activated charcoal adsorbs toxins.
    • Milk coats mucous membranes.
    • Liquid paraffin lubricates.
    pharmacology examples

  • What is chemical antagonism?

    When two substances chemically react to form an inactive product.

    pharmacology chemical

  • Give an example of chemical antagonism.

    • EDTA chelates heavy metals.
    • Protamine sulfate neutralizes heparin.
    • Sodium bicarbonate neutralizes gastric acid.
    pharmacology examples

  • What is physiological antagonism?

    When drugs act on different receptors but produce opposite effects.

    pharmacology physiological

  • Give an example of physiological antagonism.

    • Histamine vs. adrenaline (bronchoconstriction vs. bronchodilation).
    • Insulin vs. glucagon (blood glucose levels).
    pharmacology examples

  • What is pharmacological antagonism?

    Occurs when two drugs act on the same receptor system; antagonists block agonists.

    pharmacology pharmacological

  • What is competitive antagonism?

    Antagonist competes with agonist for the same receptor site, reversible binding.

    pharmacology competitive

  • What results from competitive antagonism?

    Maximum response remains the same; EC50 increases with higher agonist doses.

    pharmacology results

  • What is the difference between competitive and non-competitive antagonism?

    Competitive antagonism is reversible; non-competitive cannot be overcome by increasing agonist concentration.

    pharmacology types

  • What effect does a 50% increase in dose have on the dose-response curve?

    Shifts to the right.

    pharmacology dose-response

  • What does atropine do at muscarinic receptors?

    • Blocks acetylcholine
    • Reversible interaction
    pharmacology antagonists muscarinic

  • What is the effect of propranolol at β-adrenergic receptors?

    • Blocks adrenaline
    • Reversible antagonist
    pharmacology adrenergic propranolol

  • How does mepyramine affect H1-receptors?

    • Blocks histamine
    • Reversible antagonist
    pharmacology antagonists h1-receptors

  • What characterizes irreversible antagonism?

    • Antagonist binds permanently
    • Lasting effect
    pharmacology irreversible antagonism

  • What binds irreversibly to receptors?

    • Covalent binding
    • Agonist concentration cannot overcome the block
    • Receptor remains unavailable until new receptors are synthesized
    pharmacology receptors

  • What happens to Emax in irreversible binding?

    • Emax decreases
    • Fewer receptors are available
    pharmacology responses

  • What happens to EC50 in irreversible binding?

    • EC50 remains unchanged
    • Affinity for remaining receptors is unaffected
    pharmacology responses

  • What is an example of an irreversible antagonist?

    • Phenoxybenzamine
    • Omeprazole
    • Aspirin
    drugs antagonists

  • What characterizes non-competitive antagonism?

    • Antagonist binds to a different site
    • Agonist and antagonist do not compete for the same site
    pharmacology receptors

  • What is the result of non-competitive antagonism?

    • Emax decreases
    • EC50 may remain unchanged
    pharmacology responses

  • What is an example of a non-competitive antagonist?

    • Ketamine
    • Picrotoxin
    • Allosteric inhibitors
    drugs antagonists

  • What is a partial agonist?

    • Affinity for the receptor
    • Low intrinsic activity compared to full agonists
    pharmacology receptors

  • What happens when a partial agonist is administered with a full agonist?

    • Antagonizes full agonist's effect
    • Occupies receptor sites
    pharmacology receptors

  • What is an example of a partial agonist?

    • Pindolol
    • Buprenorphine
    drugs agonists

  • What is an inverse agonist?

    • Binds to the same receptor as an agonist
    • Induces an opposite effect
    pharmacology receptors

  • What do inverse agonists stabilize?

    • The inactive form of the receptor
    • Reduces baseline activity
    pharmacology receptors

  • What are examples of inverse agonists?

    • Propranolol
    • Clozapine
    drugs agonists

  • What is drug synergism?

    • Enhancement of drug effects when two drugs act together
    pharmacology interactions

  • What is additive synergism?

    • Combined effect equals the sum of individual effects
    • E.g., Alcohol + benzodiazepines
    synergism examples

  • What is supra-additive synergism?

    • Combined effect is greater than the sum
    • E.g., Sulfonamides + trimethoprim
    synergism examples

  • What is a clinical use of antagonism?

    • Treatment of poisoning
    • E.g., Naloxone for morphine overdose
    clinical antagonism

  • What are beta-blockers used for?

    • Control excess sympathetic activity
    • E.g., Propranolol
    clinical drugs

  • What is the significance of understanding antagonism?

    • Aids in rational therapy
    • Helps in predicting drug interactions
    clinical importance

  • What types of mechanisms can lead to antagonism?

    • Physical
    • Chemical
    • Physiological
    • Receptor-based
    pharmacology mechanisms

  • What produces effects by binding to receptors?

    Drugs

    pharmacology drugs

  • What does affinity refer to?

    The ability of a drug to bind to its receptor

    pharmacology affinity

  • What is potency a measure of?

    How much drug is required to produce a given effect

    pharmacology potency

  • What does efficacy determine?

    The maximum effect (Emax) a drug can produce

    pharmacology efficacy

  • What type of agonist has both high affinity and high efficacy?

    Full agonist

    pharmacology agonists

  • Which agonist produces a submaximal response?

    Partial agonist

    pharmacology agonists

  • What is an example of a full agonist?

    Morphine

    pharmacology full_agonist

  • What does an antagonist do?

    Binds to the receptor without activating it and blocks agonist actions

    pharmacology antagonists

  • What is the main premise of Occupation Theory?

    The response is directly proportional to the number of receptors occupied

    pharmacology theories

  • What does Rate Theory emphasize?

    The rate of drug-receptor interaction

    pharmacology theories

  • What happens when all receptors are occupied according to Occupation Theory?

    Maximum effect (Emax) occurs

    pharmacology theories

  • What are the limitations of Occupation Theory?

    • Can't explain partial agonism
    • Efficacy differences among similar binders
    pharmacology limitations

  • What happens with drugs that associate and dissociate rapidly?

    Produce stronger effects

    pharmacology effects

  • What is an example of an inverse agonist?

    Propranolol

    pharmacology inverse_agonists

  • How does a partial agonist act in the presence of a full agonist?

    Can act as an antagonist

    pharmacology partial_agonists

  • What is the term for the concentration producing 50% of maximum response?

    EC50

    pharmacology potency

  • What type of receptor activity do inverse agonists target?

    Constitutive activity

    pharmacology inverse_agonists

  • What does high affinity enable for a drug?

    Bind tightly even at low concentrations

    pharmacology affinity

  • Which phenomenon cannot be explained by Rate Theory?

    Long-lasting effects of irreversible binding drugs

    pharmacology limitations

  • What are the two states of receptors according to modern receptor theory?

    • R (inactive state)
    • R* (active state)
    biology receptors theory

  • Can receptors exist in the active state without a ligand?

    Yes, a small fraction of receptors may spontaneously exist in the active state even without a ligand.

    biology receptors ligands

  • What does 'R' represent in receptor theory?

    R represents the inactive state of a receptor.

    biology receptors theory

  • What does 'R*' represent in receptor theory?

    R* represents the active state of a receptor.

    biology receptors theory

  • What is the significance of interconvertible states of receptors?

    It allows receptors to switch between inactive and active states, affecting signaling.

    biology receptors signaling

  • What concept is highlighted by spontaneous receptor activation?

    It highlights the dynamic nature and efficiency of receptor signaling.

    biology receptors signaling

  • What shifts equilibrium toward activation in receptors?

    Agonists have higher affinity for R*.

    pharmacology receptors

  • What stabilizes the inactive state of a receptor?

    Inverse agonists have higher affinity for R.

    pharmacology receptors

  • What is the effect of neutral antagonists?

    They have equal affinity for R and R* and block both activities.

    pharmacology receptors

  • What concept explains constitutive receptor activity?

    Constitutive activity occurs with drug interactions that affect receptor states.

    pharmacology concepts

  • What defines spare receptors?

    A receptor system has spare receptors when Emax is achieved without occupying all receptors.

    pharmacology receptors

  • How does spare receptor concept relate to cardiac muscle?

    Maximal response to adrenaline can occur with only partial occupancy of ẞ1-receptors.

    pharmacology cardiac

  • What is the impact of irreversible antagonists in relation to spare receptors?

    Emax may not decrease until receptor reserve is exhausted.

    pharmacology antagonists

  • What influences receptor number and sensitivity?

    They can be upregulated or downregulated by various influences.

    pharmacology regulation

  • What leads to upregulation of receptors?

    Prolonged exposure to antagonists or deficiency of agonist.

    pharmacology upregulation

  • What is an example of upregulation effects?

    Chronic ẞ-blocker use may cause rebound tachycardia upon withdrawal.

    pharmacology clinical

  • What causes downregulation of receptors?

    Prolonged exposure to agonists results in downregulation.

    pharmacology downregulation

  • What is receptor-effector coupling?

    It describes the relationship between receptor activation and cellular response.

    pharmacology signaling

  • How does coupling efficiency affect drug response?

    Efficiently coupled drugs produce strong effects with limited activation.

    pharmacology efficacy

  • What is the cyclic AMP (cAMP) pathway?

    Activated by ẞ1- and ẞ2-adrenergic receptors, increases cAMP and activates PKA.

    pharmacology camp

  • What is the role of protein kinase A (PKA)?

    PKA phosphorylates target proteins leading to various physiological effects.

    pharmacology enzymes

  • What triggers the phosphatidylinositol pathway?

    Gq-protein-coupled receptors lead to formation of IP3 and DAG.

    pharmacology signal_transduction

  • What does DAG cause in cells?

    DAG leads to Ca²+ release and activation of protein kinase C (PKC).

    pharmacology pkc

  • What is the role of nitric oxide (NO) in signaling?

    NO activates the cyclic GMP pathway, mediating smooth muscle relaxation.

    pharmacology no

  • How is ion channel modulation achieved?

    Ligand-gated channels open/close upon ligand binding, affecting membrane potential.

    pharmacology ion_channels

  • What describes pharmacodynamics?

    Pharmacodynamics involves how drugs act on the body, including efficacy and receptor interactions.

    pharmacology pharmacodynamics

  • What is the difference between action and effect in pharmacology?

    • Action: Molecular mechanism
    • Effect: Physiological outcome
    pharmacology concepts

  • What are the types of membrane receptors?

    • Ion channel-linked
    • G-protein-linked
    • Enzyme-linked
    • Nuclear
    receptors biochemistry

  • What differentiates agonists from antagonists?

    • Affinity: Strength of binding
    • Efficacy: Ability to activate receptor
    pharmacology agonists antagonists

  • What do dose-response relationships define?

    • Potency: Amount needed for effect
    • Efficacy: Maximum effect
    • Safety Margin: Therapeutic index (TI)
    pharmacology dose-response

  • What does potency refer to?

    The amount of drug needed to produce an effect.

    pharmacology potency

  • What is efficacy in pharmacology?

    The maximum effect a drug can produce.

    pharmacology efficacy

  • What does therapeutic index (TI) indicate?

    The safety margin of a drug; a ratio comparing the effective dose to the toxic dose.

    pharmacology safety

  • What factors modify drug action?

    • Age
    • Genetics
    • Disease
    • Interactions
    pharmacology drug_action

  • What types of antagonism exist?

    • Physical
    • Chemical
    • Physiological
    • Pharmacological
    pharmacology antagonism

  • What are the theories of drug action?

    • Occupation Theory
    • Two-State Model
    • Coupling Theory
    pharmacology theories

  • What does binding translate into?

    • Response
    • Action
    pharmacology binding

  • What forms the foundation for rational pharmacotherapy?

    • Modifying drug action principles
    • Theories of drug action
    pharmacology therapeutics