Podcast
Questions and Answers
Which of the following best describes medical pharmacology?
Which of the following best describes medical pharmacology?
- The study of the mechanisms by which drugs alter normal body processes.
- The science of substances used to prevent, diagnose, and treat disease. (correct)
- The study of substances used to induce toxic effects on pathogens.
- The branch of pharmacology dealing with the undesirable effects of chemicals.
What distinguishes toxicology from pharmacology?
What distinguishes toxicology from pharmacology?
- Toxicology focuses on the adverse effects of chemicals, while pharmacology studies their therapeutic uses. (correct)
- Toxicology is concerned with drug discovery, while pharmacology deals with drug development.
- Toxicology examines drug interactions, while pharmacology studies drug metabolism.
- Toxicology studies only natural substances, while pharmacology studies synthetic drugs.
An insecticide is administered to selectively eliminate an undesirable insect population. Under which branch of toxicology would this fall?
An insecticide is administered to selectively eliminate an undesirable insect population. Under which branch of toxicology would this fall?
- Economic Toxicology (correct)
- Medical Toxicology
- Environmental Toxicology
- Forensic Toxicology
In the context of pharmacology, what does the term 'pharmakon' refer to?
In the context of pharmacology, what does the term 'pharmakon' refer to?
Which of the following is a key characteristic of chemotherapeutic agents?
Which of the following is a key characteristic of chemotherapeutic agents?
What is a significant concern associated with chemotherapeutic agents, particularly antibiotics and antivirals in modern medicine?
What is a significant concern associated with chemotherapeutic agents, particularly antibiotics and antivirals in modern medicine?
A drug is designed to selectively increase heart rate in patients with bradycardia. Under which category would this therapeutic agent be classified?
A drug is designed to selectively increase heart rate in patients with bradycardia. Under which category would this therapeutic agent be classified?
How do pharmacotherapeutic agents primarily exert their effects?
How do pharmacotherapeutic agents primarily exert their effects?
What distinguishes a 'prototype' drug within its class?
What distinguishes a 'prototype' drug within its class?
What is the 'pharmacophore' of a drug responsible for?
What is the 'pharmacophore' of a drug responsible for?
Lidocaine, a local anesthetic, inhibits sodium channels in neurons; the patient reports a loss of sensation in the injected area. This is best described as its:
Lidocaine, a local anesthetic, inhibits sodium channels in neurons; the patient reports a loss of sensation in the injected area. This is best described as its:
A drug's effect on an organ and how its function is changed is best described as its:
A drug's effect on an organ and how its function is changed is best described as its:
How does a drug's 'mechanism of action' transition into being characterized as a drug 'effect'?
How does a drug's 'mechanism of action' transition into being characterized as a drug 'effect'?
What primarily defines a drug as an 'agonist'?
What primarily defines a drug as an 'agonist'?
Which characteristic defines a 'specific' drug in pharmacology?
Which characteristic defines a 'specific' drug in pharmacology?
What is the primary factor controlling the selective distribution of drugs to organs?
What is the primary factor controlling the selective distribution of drugs to organs?
What is the role of specialized transporters at the blood-brain barrier (BBB)?
What is the role of specialized transporters at the blood-brain barrier (BBB)?
How do ATP-binding cassette (ABC) transporters affect the plasma concentrations of drugs?
How do ATP-binding cassette (ABC) transporters affect the plasma concentrations of drugs?
What is the primary function of MDR1 (P-glycoprotein), an ABC transporter, in drug disposition?
What is the primary function of MDR1 (P-glycoprotein), an ABC transporter, in drug disposition?
What role do solute carrier transporters (SLC) play in drug transport?
What role do solute carrier transporters (SLC) play in drug transport?
Which of the following describes how receptors for endogenous substances mediate effects?
Which of the following describes how receptors for endogenous substances mediate effects?
What factor contributes significantly to the selective action of drugs on specific organs?
What factor contributes significantly to the selective action of drugs on specific organs?
Which statement best describes the relationship between receptor activation and drug effect?
Which statement best describes the relationship between receptor activation and drug effect?
Hydrophilic ligands interact with which part of the cell?
Hydrophilic ligands interact with which part of the cell?
Which of the following is NOT a type of bond involved in drug-receptor binding?
Which of the following is NOT a type of bond involved in drug-receptor binding?
In drug-receptor interactions, when do covalent bonds typically occur, and what is the usual consequence?
In drug-receptor interactions, when do covalent bonds typically occur, and what is the usual consequence?
Why are ionic bonds important in drug-receptor interactions and when do they occur?
Why are ionic bonds important in drug-receptor interactions and when do they occur?
Which force is crucial for distinguishing between stereoisomers of a drug interacting with a receptor?
Which force is crucial for distinguishing between stereoisomers of a drug interacting with a receptor?
What is the primary role of hydrophobic interactions in drug-receptor binding?
What is the primary role of hydrophobic interactions in drug-receptor binding?
How do ionic and cationic-Ï€ interactions contribute to the binding of a drug to its receptor?
How do ionic and cationic-Ï€ interactions contribute to the binding of a drug to its receptor?
What is the consequence of a drug not fitting a receptor well enough to cause a conformational change?
What is the consequence of a drug not fitting a receptor well enough to cause a conformational change?
What is the main characteristic of 'geometric (cis-trans) isomers' in the context of drug-receptor interactions?
What is the main characteristic of 'geometric (cis-trans) isomers' in the context of drug-receptor interactions?
In allostery, what is the role of a modulator binding to an allosteric site?
In allostery, what is the role of a modulator binding to an allosteric site?
How do allosteric site ligands differ from drugs acting on the orthosteric site of a receptor?
How do allosteric site ligands differ from drugs acting on the orthosteric site of a receptor?
What distinguishes 'cooperativity' in drug-receptor interactions?
What distinguishes 'cooperativity' in drug-receptor interactions?
A drug decreases gastric acidity. How would it be categorized based on mechanism of action?
A drug decreases gastric acidity. How would it be categorized based on mechanism of action?
Which of the following would be a non-receptor target?
Which of the following would be a non-receptor target?
Why is drug delivery and pharmacokinetics important?
Why is drug delivery and pharmacokinetics important?
Chemotherapeutic agents are primarily characterized by:
Chemotherapeutic agents are primarily characterized by:
What is a key consideration when classifying a drug as a 'specific' agent?
What is a key consideration when classifying a drug as a 'specific' agent?
How does manipulating blood flow contribute to a drug's selective action on specific organs?
How does manipulating blood flow contribute to a drug's selective action on specific organs?
How do solute carrier transporters (SLC) facilitate drug transport across cell membranes?
How do solute carrier transporters (SLC) facilitate drug transport across cell membranes?
Which of the following best describes how receptors for endogenous substances mediate their effects?
Which of the following best describes how receptors for endogenous substances mediate their effects?
How do Van der Waals forces contribute to the specificity of drug-receptor interactions?
How do Van der Waals forces contribute to the specificity of drug-receptor interactions?
In the context of drug-receptor interactions, what is the primary role of cooperativity?
In the context of drug-receptor interactions, what is the primary role of cooperativity?
Which statement accurately describes the function of ATP-binding cassette (ABC) transporters in drug disposition?
Which statement accurately describes the function of ATP-binding cassette (ABC) transporters in drug disposition?
How does allosteric modulation refine cellular processes compared to drugs acting on the orthosteric site?
How does allosteric modulation refine cellular processes compared to drugs acting on the orthosteric site?
Antacids neutralize gastric acid through physical and chemical processes. How would this categorise the drugs based on mechanism of action?
Antacids neutralize gastric acid through physical and chemical processes. How would this categorise the drugs based on mechanism of action?
How does environmental toxicology primarily differ from medical pharmacology?
How does environmental toxicology primarily differ from medical pharmacology?
What is the primary goal of chemotherapeutic agents concerning their interaction with target organisms?
What is the primary goal of chemotherapeutic agents concerning their interaction with target organisms?
In pharmacology, what does the term 'prototype drug' signify?
In pharmacology, what does the term 'prototype drug' signify?
Which statement accurately describes the function of a drug classified as an 'antagonist'?
Which statement accurately describes the function of a drug classified as an 'antagonist'?
If a drug is described as 'specific,' what does this indicate about its mechanism of action?
If a drug is described as 'specific,' what does this indicate about its mechanism of action?
How does blood flow primarily influence the selectivity of a drug's action within the body?
How does blood flow primarily influence the selectivity of a drug's action within the body?
Which characteristic of the blood-brain barrier (BBB) affects drug delivery to the central nervous system?
Which characteristic of the blood-brain barrier (BBB) affects drug delivery to the central nervous system?
What role do ATP-binding cassette (ABC) transporters play in determining drug concentrations in the body?
What role do ATP-binding cassette (ABC) transporters play in determining drug concentrations in the body?
What is the functional role of MDR1 (P-glycoprotein) in the context of drug disposition?
What is the functional role of MDR1 (P-glycoprotein) in the context of drug disposition?
How do solute carrier transporters (SLC) differ from ATP-binding cassette (ABC) transporters in their mechanism of action?
How do solute carrier transporters (SLC) differ from ATP-binding cassette (ABC) transporters in their mechanism of action?
Which of the following best describes how receptors for endogenous substances influence drug action?
Which of the following best describes how receptors for endogenous substances influence drug action?
What role does receptor expression play in the selective action of drugs on specific organs?
What role does receptor expression play in the selective action of drugs on specific organs?
How does the interaction of a drug with a receptor correlate to the resulting drug effect?
How does the interaction of a drug with a receptor correlate to the resulting drug effect?
Where do hydrophilic ligands typically interact with cell receptors?
Where do hydrophilic ligands typically interact with cell receptors?
Among the types of bonds involved in drug-receptor binding, which one typically results in irreversible drug action?
Among the types of bonds involved in drug-receptor binding, which one typically results in irreversible drug action?
Why are ionic bonds important in initial drug-receptor interactions, despite their relatively weak nature in an aqueous environment?
Why are ionic bonds important in initial drug-receptor interactions, despite their relatively weak nature in an aqueous environment?
What characterizes the role of hydrophobic interactions in stabilizing drug-receptor binding?
What characterizes the role of hydrophobic interactions in stabilizing drug-receptor binding?
How do ionic and cationic-Ï€ interactions enhance a drug's binding affinity to its receptor?
How do ionic and cationic-Ï€ interactions enhance a drug's binding affinity to its receptor?
What is the consequence if a drug does not fit a receptor well enough to induce a conformational change?
What is the consequence if a drug does not fit a receptor well enough to induce a conformational change?
How do geometric (cis-trans) isomers affect drug-receptor interactions?
How do geometric (cis-trans) isomers affect drug-receptor interactions?
What is the primary effect of a modulator binding to an allosteric site on a receptor?
What is the primary effect of a modulator binding to an allosteric site on a receptor?
How do ligands that bind to allosteric sites differ in their action compared to drugs that bind to the orthosteric site of a receptor?
How do ligands that bind to allosteric sites differ in their action compared to drugs that bind to the orthosteric site of a receptor?
What characterizes 'cooperativity' in the context of drug-receptor interactions?
What characterizes 'cooperativity' in the context of drug-receptor interactions?
When a drug acts through a physical or chemical process, such as neutralizing gastric acid, how is it categorized based on its mechanism of action?
When a drug acts through a physical or chemical process, such as neutralizing gastric acid, how is it categorized based on its mechanism of action?
Which of the following is classified as a non-receptor target for drug action?
Which of the following is classified as a non-receptor target for drug action?
Why are drug delivery and pharmacokinetics crucial in pharmacotherapy?
Why are drug delivery and pharmacokinetics crucial in pharmacotherapy?
What is the primary distinguishing factor for chemotherapeutic agents compared to pharmacotherapeutic agents?
What is the primary distinguishing factor for chemotherapeutic agents compared to pharmacotherapeutic agents?
Which criterion is most important when classifying a drug as a 'specific' agent?
Which criterion is most important when classifying a drug as a 'specific' agent?
How can adjusting blood flow to an organ contribute to the selective action of a drug?
How can adjusting blood flow to an organ contribute to the selective action of a drug?
Which of the following statements best describes how receptors for endogenous substances mediate their effects?
Which of the following statements best describes how receptors for endogenous substances mediate their effects?
How do Van der Waals forces enhance the specificity of drug-receptor interactions?
How do Van der Waals forces enhance the specificity of drug-receptor interactions?
What distinguishes chemotherapeutic agents from pharmacotherapeutic agents based on their primary mode of action?
What distinguishes chemotherapeutic agents from pharmacotherapeutic agents based on their primary mode of action?
A drug that binds to a receptor and produces a biologic response is best described as a(n):
A drug that binds to a receptor and produces a biologic response is best described as a(n):
A drug is designed to exclusively prevent sodium ions from entering neurons. What type of drug action is this?
A drug is designed to exclusively prevent sodium ions from entering neurons. What type of drug action is this?
Isoproterenol is an example of prototype drug for?
Isoproterenol is an example of prototype drug for?
Which of the following best illustrates the concept of a drug's 'pharmacophore'?
Which of the following best illustrates the concept of a drug's 'pharmacophore'?
A drug that binds to a receptor but does not activate it, instead preventing the binding of an endogenous agonist, is best described as a(n):
A drug that binds to a receptor but does not activate it, instead preventing the binding of an endogenous agonist, is best described as a(n):
A new antibiotic is developed that targets a bacterial enzyme not found in humans. This antibiotic is best described as a:
A new antibiotic is developed that targets a bacterial enzyme not found in humans. This antibiotic is best described as a:
Which of the following factors most significantly influences the ability of a drug to selectively target specific organs?
Which of the following factors most significantly influences the ability of a drug to selectively target specific organs?
What distinguishes solute carrier transporters (SLCs) from ATP-binding cassette (ABC) transporters in drug transport?
What distinguishes solute carrier transporters (SLCs) from ATP-binding cassette (ABC) transporters in drug transport?
How do receptors for endogenous substances, such as hormones and neurotransmitters, influence drug action?
How do receptors for endogenous substances, such as hormones and neurotransmitters, influence drug action?
Which of the following scenarios best illustrates the concept of 'cooperativity' in drug-receptor interactions?
Which of the following scenarios best illustrates the concept of 'cooperativity' in drug-receptor interactions?
A drug that reduces gastric acidity by directly neutralizing stomach acid acts through a:
A drug that reduces gastric acidity by directly neutralizing stomach acid acts through a:
Why are drug delivery and pharmacokinetics crucial for pharmacotherapeutic agents?
Why are drug delivery and pharmacokinetics crucial for pharmacotherapeutic agents?
In the context of drug-receptor interactions, what is the primary significance of Van der Waals forces?
In the context of drug-receptor interactions, what is the primary significance of Van der Waals forces?
How does the study of pharmacology primarily contribute to advancements in medical treatments?
How does the study of pharmacology primarily contribute to advancements in medical treatments?
What distinguishes 'economic toxicology' from other areas within toxicology?
What distinguishes 'economic toxicology' from other areas within toxicology?
What is the critical factor that dictates whether a drug is classified as chemotherapeutic rather than pharmacotherapeutic?
What is the critical factor that dictates whether a drug is classified as chemotherapeutic rather than pharmacotherapeutic?
When designing a chemotherapeutic agent, what cellular component would offer the most selective target to minimize harm to the host?
When designing a chemotherapeutic agent, what cellular component would offer the most selective target to minimize harm to the host?
Why has the development of new chemotherapeutic agents, especially antibiotics and antivirals, become less profitable for the pharmaceutical industry?
Why has the development of new chemotherapeutic agents, especially antibiotics and antivirals, become less profitable for the pharmaceutical industry?
A drug selectively inhibits a specific organ function to alleviate symptoms but does not address the underlying cause of the disease. How would this drug be classified?
A drug selectively inhibits a specific organ function to alleviate symptoms but does not address the underlying cause of the disease. How would this drug be classified?
A drug is designed to restore normal hormonal balance in patients with endocrine disorders. How would this pharmacotherapeutic agent primarily exert its effects?
A drug is designed to restore normal hormonal balance in patients with endocrine disorders. How would this pharmacotherapeutic agent primarily exert its effects?
What is the key role of the 'pharmacophore' in a drug molecule?
What is the key role of the 'pharmacophore' in a drug molecule?
Why is it important to describe a drug's action at different levels (symptomatic, physiological, cellular, and molecular)?
Why is it important to describe a drug's action at different levels (symptomatic, physiological, cellular, and molecular)?
How does the development of new measurement techniques refine the characterization of a drug's effects?
How does the development of new measurement techniques refine the characterization of a drug's effects?
What classifies a drug as an 'antagonist' based on receptor activity?
What classifies a drug as an 'antagonist' based on receptor activity?
What is a key factor in determining the selective distribution of a drug to specific organs?
What is a key factor in determining the selective distribution of a drug to specific organs?
How do specialized transporters at the blood-brain barrier (BBB) ensure drug selectivity?
How do specialized transporters at the blood-brain barrier (BBB) ensure drug selectivity?
What is the principal function of ATP-binding cassette (ABC) transporters in drug disposition?
What is the principal function of ATP-binding cassette (ABC) transporters in drug disposition?
What role do solute carrier transporters (SLCs) play in modulating drug concentrations within the human body?
What role do solute carrier transporters (SLCs) play in modulating drug concentrations within the human body?
How do receptors, as structural components of cells, influence the selectivity of drug action?
How do receptors, as structural components of cells, influence the selectivity of drug action?
How does receptor expression in different organs contribute to variations in drug effects?
How does receptor expression in different organs contribute to variations in drug effects?
What is the fundamental relationship between a drug's binding to a receptor and the resulting drug effect?
What is the fundamental relationship between a drug's binding to a receptor and the resulting drug effect?
What general property do ligands that interact with intracellular receptors have?
What general property do ligands that interact with intracellular receptors have?
Why are covalent bonds generally less common in drug-receptor interactions compared to other types of bonds?
Why are covalent bonds generally less common in drug-receptor interactions compared to other types of bonds?
Although relatively weak in aqueous environments, how do ionic bonds facilitate initial drug-receptor interactions?
Although relatively weak in aqueous environments, how do ionic bonds facilitate initial drug-receptor interactions?
How do multiple hydrogen bonds contribute to drug-receptor interactions compared to a single ionic bond?
How do multiple hydrogen bonds contribute to drug-receptor interactions compared to a single ionic bond?
Why are Van der Waals forces important for drug specificity towards its receptor?
Why are Van der Waals forces important for drug specificity towards its receptor?
How do ionic and cationic-Ï€ interactions work together to enhance drug's binding affinity to its receptor?
How do ionic and cationic-Ï€ interactions work together to enhance drug's binding affinity to its receptor?
What is the immediate consequence if a drug does not fit a receptor well enough to cause a conformational change?
What is the immediate consequence if a drug does not fit a receptor well enough to cause a conformational change?
How do geometric (cis-trans) isomers typically affect drug-receptor interactions?
How do geometric (cis-trans) isomers typically affect drug-receptor interactions?
In the context of allostery, how does a modulator binding to an allosteric site influence receptor activity?
In the context of allostery, how does a modulator binding to an allosteric site influence receptor activity?
How do allosteric site ligands refine cellular processes when compared to drugs binding on the orthosteric site of a receptor?
How do allosteric site ligands refine cellular processes when compared to drugs binding on the orthosteric site of a receptor?
How is 'cooperativity' best described in the context of drug-receptor interactions?
How is 'cooperativity' best described in the context of drug-receptor interactions?
What characterizes a receptor-independent mechanism of drug action?
What characterizes a receptor-independent mechanism of drug action?
Which cellular structure is NOT a receptor target?
Which cellular structure is NOT a receptor target?
What is the relevance of understanding a drug's effects at a molecular level?
What is the relevance of understanding a drug's effects at a molecular level?
How does adjusting blood flow to a specific organ contribute to a drug's selective action?
How does adjusting blood flow to a specific organ contribute to a drug's selective action?
A drug is found to bind to a receptor and initiate a biological response. How would this drug be categorized?
A drug is found to bind to a receptor and initiate a biological response. How would this drug be categorized?
If a drug is designed specifically to prevent sodium ions from entering neurons, what type of drug action is this considered?
If a drug is designed specifically to prevent sodium ions from entering neurons, what type of drug action is this considered?
Which statement illustrates the concept of 'cooperativity' in drug-receptor interactions?
Which statement illustrates the concept of 'cooperativity' in drug-receptor interactions?
A drug reduces gastric acidity by directly neutralizing stomach acid. Through what mechanism does this drug act?
A drug reduces gastric acidity by directly neutralizing stomach acid. Through what mechanism does this drug act?
A drug that selectively targets bacterial ribosomes, which differ structurally from human ribosomes, would be classified as which type of agent, and why?
A drug that selectively targets bacterial ribosomes, which differ structurally from human ribosomes, would be classified as which type of agent, and why?
A drug that binds to a receptor and prevents the binding of an endogenous ligand, without initiating a biological response itself, is best described as a(n):
A drug that binds to a receptor and prevents the binding of an endogenous ligand, without initiating a biological response itself, is best described as a(n):
How do specialized transporters at the blood-brain barrier (BBB) contribute to drug selectivity?
How do specialized transporters at the blood-brain barrier (BBB) contribute to drug selectivity?
Which statement best describes the function of ATP-binding cassette (ABC) transporters in drug disposition?
Which statement best describes the function of ATP-binding cassette (ABC) transporters in drug disposition?
In the context of drug-receptor interactions, what role do geometric (cis-trans) isomers play?
In the context of drug-receptor interactions, what role do geometric (cis-trans) isomers play?
How can adjusting blood flow to an organ contribute to a drug's selective action?
How can adjusting blood flow to an organ contribute to a drug's selective action?
Flashcards
Pharmacology
Pharmacology
The study of substances interacting with living systems through chemical processes, especially by binding to regulatory or structural molecules.
Toxicology
Toxicology
The branch of pharmacology dealing with the undesirable side effects of chemicals on living systems.
Prototype Drug
Prototype Drug
A representative agent for a drug class, setting the standard.
Pharmacophore
Pharmacophore
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Agonist
Agonist
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Antagonist
Antagonist
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Chemotherapeutic Agents
Chemotherapeutic Agents
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Pharmacotherapeutic Agents
Pharmacotherapeutic Agents
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Specific Drug Action
Specific Drug Action
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Non-specific Drug Action
Non-specific Drug Action
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ABC Transporters
ABC Transporters
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SLC Transporters
SLC Transporters
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Receptors
Receptors
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Covalent Bonds
Covalent Bonds
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Ionic Bonds
Ionic Bonds
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Cation-Ï€ Interactions
Cation-Ï€ Interactions
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Hydrogen Bonds
Hydrogen Bonds
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Van der Waals Forces
Van der Waals Forces
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Hydrophobic Interactions
Hydrophobic Interactions
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Allosteric Site
Allosteric Site
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Receptor-Independent Drug Action
Receptor-Independent Drug Action
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Toxicology Definition
Toxicology Definition
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Medical Pharmacology
Medical Pharmacology
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Environmental Toxicology
Environmental Toxicology
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Forensic Toxicology
Forensic Toxicology
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Drug Selectivity
Drug Selectivity
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Blood-Brain Barrier (BBB)
Blood-Brain Barrier (BBB)
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Pharmacotherapeutic Effect
Pharmacotherapeutic Effect
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Symptomatic Drug Action
Symptomatic Drug Action
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Physiological Drug Action
Physiological Drug Action
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Cellular Drug Action
Cellular Drug Action
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Molecular Drug Action
Molecular Drug Action
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Drug Action Classification
Drug Action Classification
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MDR proteins
MDR proteins
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Drug Action Selectivity
Drug Action Selectivity
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Widespread Drug Effects
Widespread Drug Effects
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SNPs impact on drugs
SNPs impact on drugs
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Drug-Receptor Complex
Drug-Receptor Complex
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Geometric Isomers
Geometric Isomers
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Allostery
Allostery
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Cooperativity
Cooperativity
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Importance of Drug Delivery
Importance of Drug Delivery
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Orientation in space with drugs
Orientation in space with drugs
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Pharmakon
Pharmakon
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Logos
Logos
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Drogue
Drogue
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Chemicals as Drugs
Chemicals as Drugs
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Antibiotics as Chemicals
Antibiotics as Chemicals
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Chemotherapeutic Specificity
Chemotherapeutic Specificity
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Drug Specificity
Drug Specificity
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Pharmacotherapeutic Impact
Pharmacotherapeutic Impact
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Drug Action Level
Drug Action Level
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Selective Drug Exclusion
Selective Drug Exclusion
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Drug Binding Portion
Drug Binding Portion
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Prolonged Drug Action
Prolonged Drug Action
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Van der Waals Role
Van der Waals Role
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Ionic/Cationic Attractions
Ionic/Cationic Attractions
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Study Notes
Key Definitions
- Pharmacology involves studying substances that interact with living systems through chemical processes.
- Substances can be chemicals or naturally found in the body like hormones and neurotransmitters.
- Substances can be administered for therapeutic effects, like antihypertensive agents.
- Substances can be administered for toxic effects on pathogens, like antibiotics.
- Medical pharmacology uses substances to prevent, diagnose, and treat diseases.
- Toxicology studies the undesirable side effects of chemicals on living systems including molecular and cellular mechanisms.
- Hazardous effects through molecular and cellular mechanisms include tissue injury, reproductive failure, teratogenicity, carcinogenicity, and immunosuppression.
- Understanding toxicity mechanisms can help lower health risks from exposures.
- Toxicology includes environmental, economic, and forensic aspects.
- Environmental toxicology concerns chemicals that become incidental or occupational hazards as contaminants of air, water, or food.
- Economic toxicology covers human/veterinary drugs, food additives/cosmetics, and agents to eliminate undesired species like insecticides and herbicides.
- Forensic toxicology focuses on diagnosis and treatment of poisonings, alongside legal issues related to chemical exposures.
- Pharmakon refers to drug/medicine/poison/magic/charm.
- Logos means study or rational discussion.
- Drogue refers to herb or plant.
- Toxicum means poison.
- Toxon refers to bow and arrow.
- Toxikon means arrow poison.
Chemotherapeutic vs. Pharmacotherapeutic Agents
- Chemotherapeutic agents eradicate bacteria, fungi, parasites, viruses, or cancer cells.
- Chemotherapeutic agents display selective toxicity between the invader and the host.
- Chemotherapeutic agents are most effective when lethal to the invading organism, but can also be suppressive.
- Chemotherapeutic agents account for 10% of available agents.
- Selective toxicity is based on cell wall structure, metabolites like folic acid, enzymes (folic acid reductase, tyrosine kinase, polymerases, proteases), or growth rate differences in cancer cells.
- If a chemotherapeutic drug isn't lethal, it relies on the host's immune system to destroy invading cells.
- A Major concern is resistant microorganisms due to overuse leading to multidrug-resistant pathogens.
- Very few new chemotherapeutic drugs are being developed because it is not seen as profitable.
- Pharmacotherapeutic agents act on specific binding sites on cells to increase or decrease organ function, like heart rate.
- Pharmacotherapeutic responses are usually dose-dependent, but can have an all-or-none effect.
- Pharmacotherapeutic agents are selective for organs, but the same receptor in different organs may cause adverse effects referring to pain medications.
- Toxicity is often an extension of the therapeutic action and may be associated with irreversible action of the drug as seen in stroke medications.
- 90% of therapeutic agents are pharmacotherapeutic.
- These agents replace dysfunctional endogenous substances like hormone replacements for thyroid hormones.
- Pharmacotherapeutic agents change the regulation of body functions to treat symptoms through antihypertensives, anti-angina drugs, diuretics, analgesics, and anticonvulsants.
- These agents alter mood and behavior and change perception with anti-anxiety and antidepressant drugs.
Prototypes and Pharmacophores
- A prototype is a representative agent for a drug class.
- Isoproterenol is an example for β2-adrenoceptor agonists.
- Ibuprofen is a prototype for non-steroidal anti-inflammatory drugs (NSAIDs).
- A pharmacophore is the portion of a drug responsible for its biological action.
- A single drug may have multiple pharmacophores, meaning multiple actions.
- Drugs are classified based on their pharmacophore, like beta-lactam antibiotics.
Drug Action vs. Drug Effect
- The effects or action of a drug can be described in the following ways:
- Symptomatic: How the drug makes you feel.
- Physiological: Which organ is affected and how its function changes.
- Cellular: Which gross cellular functions are affected.
- Molecular: Which changes in intracellular function are observed.
- Lidocaine inhibits sodium channels in neurons, which can be described in the following ways:
- Symptomatic: Pain vs no pain
- Physiological: Nerve impulses are not conducted. Pain is blocked by blocking sodium channels
- Cellular: Membrane potential stabilized and there is no depolarization in neurons.
- Molecular: Inhibit sodium channels and prevent sodium from going in the cells
- Mechanism of action becomes effect with new methods for measurement at more refined levels.
- Drug action is classified based on receptor activity.
- Agonists bind to a receptor and produce a biologic response, acting as receptor activators.
- Agonists' response can be similar to or different from that of endogenous ligands, mimicking endogenous ligands.
- Antagonists diminish or oppose the action of another drug or endogenous ligand.
- Antagonists have no effect on their own and must be in the presence of an agonist.
Specific vs. Non-Specific Drugs
- A "specific" drug addresses the main underlying cause of a disease or syndrome.
- A "non-specific" drug addresses a symptom rather than the source or cause of the disease.
Factors Affecting Drug Selectivity
- Selective distribution to organs is mainly controlled by blood flow.
- Selective exclusion from an organ can occur via the blood-brain barrier (BBB).
- Small molecules can cross the BBB, but specific transporters are required for specific molecules to enter.
Membrane Transporters
- Membrane transporters do not mediate drug action, but are involved with establishing plasma concentrations.
- ATP-binding cassette (ABC) transporters are primary active transporters for one way efflux from cells.
- ABC transporters are located in the liver, kidney, intestine, and blood-brain barrier.
- Some ABC transporters are multidrug resistant proteins (MDR) and pump the drug out of the cells.
- MDR1 (P-glycoprotein) pumps drugs out of cells into blood stream or gut lumen.
- Breast cancer resistance protein (BCRP) and bile salt excretory protein (BSEP) are ABC transporters.
- Solute carrier transporters (SLC) are facilitated or ion-coupled secondary active transporters.
- SLC transporters transport organic anions (OAT) and cations (OCT).
- OATs are important for transport in the liver.
- OCTs are important for transport in the kidney.
Drug Interactions with Cellular Components
- Selective interaction of pharmacotherapeutic agents occurs with structural components of cells.
- These structural components of cells include receptors, skeletal proteins, and enzymes.
- Receptors for endogenous substances mediate the effects of endogenous compounds, including hormones and neurotransmitters.
- Receptors refers to proteins
- Selective actions of drugs on organs varies substantially.
- Receptor expression in multiple organs causes widespread effects.
- The location of receptor expression on one or two organs leads to selective effect.
- Single nucleotide polymorphisms (SNPs) are polymorphisms that are genetically-determined forms.
Major Receptor Families
- Major receptor families include ligand-gated ion channels, G protein-coupled receptors, enzyme-linked receptors, and intracellular receptors.
- Hydrophilic ligands interact with receptors on the cell surface via extracellular domains.
- Hydrophobic ligands interact with intracellular receptors by crossing lipid bilayer membranes.
- Receptors refers to proteins on cell surfaces, or within cells.
- Drug + Receptor results in Drug-receptor complex, which leads to a biologic effect/response.
- Specific binding causes conformational change in the receptor (R ⇄ R*).
- R ⇄ R* triggers a series of events known as signal transduction, resulting in biochemical events and a physiologic/biologic response.
- Receptors are often named after specific ligands, like histamine receptors.
- Drug action is not always mediated by receptors.
Drug-Receptor Relationships and Binding Forces
- Types of bonds include covalent, ionic, cation-Ï€ interactions, hydrogen, Van der Waals forces, and hydrophobic interactions.
- Cooperation of binding forces ensures the correct 3D fit between the ligand and the binding pocket in the receptor.
- Covalent bonds involve sharing electrons between atoms, are not common, and are irreversible.
- Duration of action depends on targeted cells’ turnover, resulting in responses lasting days to weeks.
- Ionic bonds involve electrostatic attraction between ions of opposite charge.
- Ionic bonds are relatively weak in an aqueous environment.
- Ionic bonds are likely to initiate drug-receptor complexes because they operate across greater distances.
- Cation-Ï€ interactions involve an electron cloud of aromatic compounds binding +ve ions and are common in receptors.
- Interactions with multiple aromatic amino acids strengthens the drug-receptor interaction.
- Hydrogen bonds exist between polar molecules. Hydrogen is bound to an electronegative atom.
- They are Weaker than ionic bonds, but are common in drug-receptor interactions.
- Multiple hydrogen bonds can stabilize forces as strong as a single ionic bond.
- Van der Waals forces are weak interactions developing when atoms are in close proximity.
- Van der Waals forces are important for specificity of drugs to receptors and differentiate drug stereoisomers.
- Hydrophobic interactions stabilize drug-receptor binding,
- Water forms hydrogen bonds with itself and many solutes
- A drug binds a receptor by hydrophobic interaction to increase binding and decrease binding to aqueous environment.
- Many receptors have hydrophobic pockets.
- Ionic attractions drive and partially orient drug for optimal binding.
- Intermolecular interactions reduce ligand solution and generate hydrophobic, hydrogen bonds, and van der Waals forces.
- Without the right fit, drugs will not be bound to the receptor long enough to cause a conformational change plus a response.
- Structural complementation has the best induced fit
- Orientation in space has stereo-selectivity (chirality).
- Enantiomers are mirror images that possess markedly actions or toxicities.
- Geometric or cis-trans isomers are not mirror images, contain different binding properties, and are easily isolated.
Allostery and Cooperativity
- Allostery involves a modulator binding to an allosteric site influencing ligand binding at the orthosteric site.
- The modulators can facilitate positive or negative cooperativity (depending of the direction of change in the observed response).
- Allosteric site ligands finely tune processes distinct from typical agonist/antagonist drugs.
- Cooperativity occurs when some receptors require binding of two ligand molecules.
- This results in first molecule binding which facilitates the binding of the second molecule to the receptor.
Receptor-Independent Mechanisms
- Receptor-independent drug action occurs through known physical or chemical processes.
- Examples of receptor-independent drug action include using antacids to decrease gastric acidity, and the effect on pH.
- Additional examples of receptor-independent drug action are using protamine to decrease excessive amounts of heparin, and protamine having a positive charge.
- Drugs can act through known enzymatic mechanisms or binding to intracellular structural proteins.
- Non-receptor targets include structural proteins, enzymes, ribosomes, and gases (like NO).
- Paclitaxel targets tubulin, an example of a structural protein.
- Trimethoprim targets DHF reductase, an example of an enzyme.
- Erythromycin targets the bacterial 50S subunit, an example of a ribosome.
- Hydralazine increases the release of nitric oxide.
Importance of Drug Delivery and Pharmacokinetics
- Pharmacophore effects result in action.
- Delivering to the site of action requires formulation and ADME (absorption, distribution, metabolism, excretion).
- Maintain effective concentration for the correct duration of time using ADME.
- Right drug, right place in the right amount for the right duration of time.
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