quiz 1 MPharm PHA112 Drug Receptor Concepts Quiz

114 Questions

What is the measure of the ease with which a drug binds to its receptor?

Affinity

Which type of drug binds to its receptor, activates the receptor, and elicits a biological response?

Agonist

What is the measure of the ability of the drug-receptor complex to couple or transduce the drug binding into a biological response?

Efficacy

What type of drug binds to its receptor, activates the receptor, and is capable of eliciting the maximum possible response?

Full agonist

Which drug type binds to its receptor but fails to activate the receptor, and so fails to elicit a response?

Antagonist

What concept allows low affinity drugs to elicit the maximum possible response?

'Spare Receptor' concept

What is reflected in the location of the Dose-Response curve along the dose axis?

Potency

Which characteristic reflects the magnitude of change in response per unit change in dose?

'Slope'

What does 'efficacy (e)' express about a drug?

Ability to activate or cause a conformational change in the receptor leading to a biological response

What does 'potency' measure?

The amount of drug needed to elicit a specified response

Which characteristic reflects the maximal response or effect produced by a drug?

Maximal efficacy

What type of drug competes with the agonist drug for binding to the receptor?

Antagonist

Which of the following is not a characteristic of graded dose-response curves?

Drug-Drug Interactions

What type of antagonism occurs when the antagonist and agonist drugs compete for the same receptor binding site?

Reversible competitive antagonism

In irreversible competitive antagonism, what happens to the available receptors for the agonist?

They become permanently reduced

Which type of antagonism occurs when the antagonist drug binds directly to the agonist drug in solution, rendering it inactive?

Chemical antagonism

What type of antagonism occurs when the antagonist drug reduces the effective concentration of the agonist drug at its site of action, through mechanisms such as decreased absorption or increased metabolism?

Pharmacokinetic antagonism

When two drugs elicit opposing responses, canceling each other out, by acting on different receptors, what type of antagonism is this?

Physiological antagonism

What type of drug interaction occurs when the combined effect of two drugs is equal to the algebraic sum of their individual effects?

Summation

What type of drug interaction occurs when the combined effect of two drugs is greater than the algebraic sum of their individual effects?

Synergism

What is the term used to describe a state of progressively decreasing responsiveness to a drug due to prior or repeated exposure?

Tolerance

Which concept refers to the measure of the margin of safety of a drug based on the ratio of the median toxic dose to the median effective dose?

Therapeutic index

What area of pharmacology deals with the absorption, distribution, metabolism, and elimination of drugs from the body?

Pharmacokinetics

What type of variation refers to a state of progressively decreasing responsiveness to a drug due to prior or repeated exposure?

Acquired tolerance

Which book is recommended reading material for the lecture series on Drug Receptor Concepts?

Katzung and Trevor's: Basic & Clinical Pharmacology

Which type of drugs bind to receptors and activate a response?

Agonists

What is the study of drugs and their interactions with living organisms called?

Pharmacology

What concept provides a useful measure of the benefit to risk ratio of a drug?

Therapeutic index

What is the basic distinction between an 'Agonist' and an 'Antagonist' drug?

An agonist drug produces the same effect as the natural chemical messenger, while an antagonist drug produces no effect

Which type of drug binds to a site near the binding site for a natural chemical messenger and influences its binding?

Positive Allosteric Modulator

What type of drug may produce an opposite effect to the natural chemical messenger?

Inverse Agonist

Which type of drug interaction occurs when the combined effect of two drugs is greater than the algebraic sum of their individual effects?

Potentiation

What is reflected in the location of the Dose-Response curve along the dose axis?

Potency

Which characteristic reflects the maximal response produced by a drug?

Efficacy

What concept allows low affinity drugs to elicit the maximum possible response?

Efficacy

What type of antagonism occurs when the antagonist drug reduces the effective concentration of the agonist drug at its site of action?

Competitive antagonism

In which type of antagonism does the antagonist drug binds directly to the agonist drug in solution, rendering it inactive?

Chemical antagonism

Which type of drug interaction occurs when the combined effect of two drugs is equal to the algebraic sum of their individual effects?

Additive effect

Which branch of pharmacology involves the study of drug effects on the body?

Pharmacodynamics

What type of drug action involves interaction with specific macromolecular or cellular targets, called receptors, resulting in clear-cut structure-activity relationships?

Specific drug action

Which type of drug target involves regulatory proteins or binding sites for endogenous chemical messengers?

Classical receptors

What kind of drug-receptor interactions involve the drug's molecular structure fitting complementarily into the binding site on the receptor, forming a drug-receptor complex via a reversible chemical reaction?

Specific interactions

What is the relationship between the drug effect and the fraction of receptors occupied by the drug?

Direct relationship

What theory assumes that the drug effect is proportional to the fraction of receptors occupied and that the maximum effect occurs when all receptors are occupied?

Receptor occupancy theory

Which curve is an important tool in understanding drug-receptor interactions and drug action?

$\log$ drug concentration-receptor occupancy curve

What type of antagonism occurs when the antagonist drug binds directly to the agonist drug in solution, rendering it inactive?

Chemical antagonism

'Efficacy (e)' expresses what about a drug?

The maximal response or effect produced by a drug

What type of variation refers to a state of progressively decreasing responsiveness to a drug due to prior or repeated exposure?

Tolerance

Which type of drugs bind to receptors, activate them, and elicit a biological response?

Agonist drugs

What is the study of drugs and their interactions with living organisms called?

Pharmacology

Which element is the main constituent of a bacterial cell?

Carbon

From where do bacteria obtain their energy?

Organic molecules

What is the main inorganic cation and enzymatic cofactor in a bacterium?

Potassium

Which element is responsible for forming nucleic acids, nucleotides, and phospholipids in bacteria?

Phosphorus

What do lithotrophs use as their electron source?

H2S

What serves as the electron source for organotrophs in bacterial metabolism?

Organic molecules

What is the function of agar in solid media for microbial culture?

To serve as a gelling agent

What distinguishes defined media from undefined media in microbial culture?

Defined media contains chemically defined components

What is the main purpose of GasPak sachets in anaerobic microbial culture?

To produce CO2 and H2 for creating an anaerobic environment

In which phase of bacterial growth do nutrients become depleted and waste products build-up?

Stationary phase

What does secondary metabolism in microbial metabolism primarily involve?

Production of natural products like antibiotics

What is the time taken for a bacterial cell to reproduce by DNA binary fission called?

"Generation time"

What is the atmospheric requirement for obligate aerobes in microbial culture?

"Cannot survive without oxygen"

What is the primary function of candle extinction in creating an anaerobic environment for microbial culture?

"Uses up oxygen by burning a candle"

What are the two ways to culture microorganisms mentioned in the text?

"Liquid media and solid media"

What are the primary components of TSA agar used in microbial culture?

Tryptone, Soytone, Agar, CaCl2, dH2O

Which atmospheric requirement is associated with Camplylobacter jejuni in microbial culture?

Increased CO2 content

What distinguishes solid media from liquid media in microbial culture?

Solid media facilitates the formation of distinct colonies

What is the assumed mechanism of action of broad spectrum antimicrobials?

Alkylation of various protein functional groups

Which type of radiation requires heavy shielding and can damage some materials due to radiolysis of water?

γ-rays

What is the primary target of ionising radiation and UV light used for sterilization?

Microbial DNA

How can sterilisation be checked?

Chemical indicators based on color change

What is the microbial safety index that indicates a 1 in 10 chance of a single surviving organism?

$10^{-5}$

What method is commonly used for assessing whether a sterilized product is free from microbial contamination?

Membrane filtration

What can lead to product recall and litigation if sterilisation goes wrong?

Microbial contamination

What is the main risk associated with ionising radiation for sterilisation?

Radiolysis of water

What type of contamination can be controlled through environmental controls, clean or aseptic preparation areas, and Grades C, D, B, and A?

Bacterial contamination

What indicator is used based on a visible color change to assess steam sterilisation?

$pH$ indicator strips

Where does the air for aseptic production come from, and what filtration method is used?

Air drawn from outside aseptic area, HEPA filtration

Which characteristic reflects the magnitude of change in response per unit change in dose?

$EC_{50}$ value

Which type of water in pharmaceutical manufacturing has stricter quality guidelines than purified water and focuses on Endotoxin levels?

Purified Water for injection

What is the relationship between exposure time and the probability of a non-sterile unit?

$10^{-6}$ probability per microsecond exposure time

What is the purpose of hand washing and alcohol hand gels in reducing contamination from personnel in pharmaceutical manufacturing?

To minimize biological contamination

What does 'sterile' mean in terms of microbial populations?

No survivors in the population

What are the common methods used for product sampling and clinical samples in pharmaceuticals?

Filtration, direct inoculation, surface swabbing, air sampling

Which regulatory body sets acceptable limits for microbial contamination in non-sterile products?

British Pharmacopoeia

What are the consequences of microbial contamination in pharmaceuticals?

Chemical deterioration, inactivation of products, resistance to spoilage

What type of calculations are used to assess microbial content in pharmaceutical products?

Total microbial count calculations

What is the primary source of biological contamination in pharmaceuticals?

$Utilities used in production$

How can microbial contamination be controlled within a pharmaceutical facility?

$By implementing environmental controls$

What method is used to reduce contamination from personnel in pharmaceutical manufacturing?

$Alcohol hand gels$

Which type of contamination can be controlled through Grades C, D, B, and A areas in pharmaceutical facilities?

Viral contamination

In batch culture, what limits nutrient availability and product production?

Closed systems

What is the primary reason for scaling up production through bulk culturing?

Increased product production

What is the main goal of strain improvement in production processes?

Increase production through mutations or genetic modification

Which process involves the production of human-identical insulin through cloning and gene modification in E. coli?

Heterologous gene expression

In viral replication, what can lead to cell destruction or budding?

Host cell machinery

What is the result of bacterial evolution over time due to mutation or DNA acquisition?

Reduced effectiveness of treatments

What is the main consequence of antimicrobial resistance resulting from selective pressure from antibiotics?

Reduced effectiveness of treatments

What is a characteristic of lab-scale culture that limits its industrial applications?

'Optimization' for product production

What is a key consideration for maintaining adequate mixing, high oxygen levels, and control of pH, temperature, and foam in production processes?

Important criteria

What is a potential consequence of contamination of pharmaceutical products?

Reduced effectiveness of treatments

What is the primary goal of continuous culture in manufacturing processes?

Controlled growth with constant nutrient supply

Which process aims to remove or kill all microorganisms and infectious proteins?

Sterilization

What can result from contamination of medical products with toxic microbial metabolites?

Systemic/bloodstream infection

What is the process of separating products from production mixtures and removing unwanted components called?

Purification

Which method aims to minimize microbial contamination while minimizing product damage?

Gas sterilization

What type of infection affects the digestive system, often caused by ingestion of contaminated products?

GI infection

What is the most serious effect of contamination with toxic microbial metabolites?

General bacteraemia

What refers to a series of operations to purify and sterilize medical products, reducing the risk of contamination and side effects?

Downstream processing

What process aims to minimize microbial contamination while minimizing product damage?

Gas sterilization

What is the term for a minor infection that does not spread beyond the site of injection or contact?

Local infection

What type of infections are serious and spread throughout the body, often caused by injected products or immunocompromised patients?

Systemic/bloodstream infection

What can product contamination lead to, in terms of legal consequences?

Recalls and litigation

Study Notes

The text is from a lecture series on Drug Receptor Concepts in the MPharm program at Sunderland University, taught by Dr. Gabriel Boachie-Ansah.
The lecture series covers various topics, including pharmacology, drug-receptor interactions, variation in drug responsiveness, and clinical selectivity.
Drug responsiveness varies and can result in lack of efficacy or unexpected side effects. Variations can be inter-patient or intra-patient.
Variation in drug responsiveness can be due to pharmacokinetic or pharmacodynamic mechanisms.
Possible types of variation include qualitative and quantitative variations. Quantitative variations include hyper-responsiveness and hypo-responsiveness or tolerance.
Acquired tolerance is a state of progressively decreasing responsiveness to a drug due to prior or repeated exposure. Mechanisms include pharmacodynamic and metabolic processes.
Clinical selectivity refers to the therapeutic vs undesirable or side effects of drugs. Therapeutic index is a measure of the margin of safety of a drug based on the ratio of the median toxic dose to the median effective dose.
The therapeutic index provides a useful measure of the benefit to risk ratio of a drug.
The recommended reading materials for this lecture series include Katzung and Trevor's "Basic & Clinical Pharmacology" and Ritter's "Rang & Dale's Pharmacology."
Drug-receptor concepts are fundamental to understanding how drugs affect human health and disease.
Pharmacology is the study of drugs and their interactions with living organisms. It can be divided into pharmacodynamics, which deals with the biochemical and physiological effects of drugs, and pharmacokinetics, which deals with the absorption, distribution, metabolism, and elimination of drugs from the body.
Drugs act by binding to receptors or targets, which can be proteins or other molecules. Agonists bind to receptors and activate a response, while antagonists bind to receptors but block the effects of agonists.
Drug-receptor binding translates into a biological effect through various mechanisms, including receptor activation, ion channel modulation, and enzyme inhibition.
Therapeutic index is an important concept in drug development and therapy, as it helps determine whether the therapeutic benefits of a drug outweigh the risks.
The text emphasizes the importance of understanding drug-receptor interactions and their impact on drug responsiveness and clinical selectivity.
Pharmacology is the study of the interaction between drugs and the living body.
Pharmacology has three main branches: Pharmacodynamics (study of drug effects on the body), Pharmacokinetics (study of how the body deals with drugs), and Pharmacotherapeutics (study of drug use in disease treatment).
Drugs act on the body through two main mechanisms: non-specific drug action and specific drug action.
Non-specific drug action involves simple physical or chemical interactions with the body, such as those of antacids or osmotic diuretics, requiring large doses for effect and lacking specific structure-activity relationships.
Specific drug action involves interaction with specific macromolecular or cellular targets, called receptors, resulting in clear-cut structure-activity relationships and producing biological effects at very low doses.
Drug receptors are protein or glycoprotein entities, some of which are located on the cell membrane, while others are located inside the cell.
Multiple types of drug targets or receptors include classical receptors (regulatory protein or binding sites for endogenous chemical messengers), ion channels, enzymes, and carrier or transport proteins.
Drug-receptor interactions involve the drug's molecular structure fitting complementarily into the binding site on the receptor, forming a drug-receptor complex via a reversible chemical reaction.
The drug effect is proportional to the fraction of receptors occupied by the drug, with the maximum effect occurring when all receptors are occupied.
Drug concentration and receptor occupancy are related through the drug concentration-receptor occupancy curve, with the receptor occupancy theory assuming that the drug effect is proportional to the fraction of receptors occupied and that the maximum effect occurs when all receptors are occupied.
The drug concentration-effect curve and log drug concentration-effect curve are important tools in understanding drug-receptor interactions and drug action.
Health hazards to patients: contamination of medical products with pathogens can result in various infections
Local infection: minor infections that do not spread beyond the site of injection or contact
GI infection: infections affecting the digestive system, often caused by ingestion of contaminated products
Systemic/bloodstream infection: serious infections that spread throughout the body, often caused by injected products or immunocompromised patients
Contamination with toxic microbial metabolites: most serious effects come from contaminated injectable products, leading to general bacteraemia and even death
Product contamination can lead to recalls and litigation
Downstream processing: series of operations to purify and sterilize medical products, reducing the risk of contamination and side effects
Purification: process of separating products from production mixtures and removing unwanted components, using methods such as sedimentation, precipitation, centrifugation, adsorption, and filtration
Sterilization: process of removing or killing all microorganisms and infectious proteins, using methods such as heat, filtration, and radiation
Microbial sensitivity to sterilization: different microbes have different levels of resistance to sterilization, influencing the choice of method
Selection of sterilization method: it is important to minimize microbial contamination while minimizing product damage, as harsh methods can reduce therapeutic efficiency, stability, and patient acceptability. Recognized sterilization methods by European Pharmacopoeia(2002) include gas sterilization, steam sterilization, filtration, dry heat, and ionizing radiation.

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