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Questions and Answers
What is the most direct way to administer a drug to the central nervous system (CNS)?
What is the most direct way to administer a drug to the central nervous system (CNS)?
Which of these routes of administration is most likely to result in a significant first-pass effect?
Which of these routes of administration is most likely to result in a significant first-pass effect?
What is the term for the movement of a drug from the site of administration to the circulatory system?
What is the term for the movement of a drug from the site of administration to the circulatory system?
Which of the following factors can affect the rate of drug absorption?
Which of the following factors can affect the rate of drug absorption?
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Which of these is NOT a benefit of using a transdermal drug delivery method?
Which of these is NOT a benefit of using a transdermal drug delivery method?
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What is the primary advantage of intravenous (IV) administration?
What is the primary advantage of intravenous (IV) administration?
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Which of these are examples of efflux transporters?
Which of these are examples of efflux transporters?
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Which route of administration is most likely to cause irritation of the nasal passages?
Which route of administration is most likely to cause irritation of the nasal passages?
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What is the name of the area in the medulla that allows direct detection of toxins in the blood?
What is the name of the area in the medulla that allows direct detection of toxins in the blood?
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Which type of molecule is most likely to freely diffuse across cell membranes?
Which type of molecule is most likely to freely diffuse across cell membranes?
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Which route of administration bypasses the first-pass effect and the blood-brain barrier?
Which route of administration bypasses the first-pass effect and the blood-brain barrier?
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Which of the following tissues can act as drug depots?
Which of the following tissues can act as drug depots?
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Which of these is NOT a factor affecting drug concentration?
Which of these is NOT a factor affecting drug concentration?
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What is a consequence of rapid drug binding to depots?
What is a consequence of rapid drug binding to depots?
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Which of these scenarios would lead to a person requiring a higher dose of a drug?
Which of these scenarios would lead to a person requiring a higher dose of a drug?
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What is the term for a molecule that is 'fears water' and 'loves fat'?
What is the term for a molecule that is 'fears water' and 'loves fat'?
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Which of the following is the most convenient route for drug administration?
Which of the following is the most convenient route for drug administration?
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Which of these is a potential disadvantage of administering a drug via inhalation?
Which of these is a potential disadvantage of administering a drug via inhalation?
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Which route of administration is NOT suitable for administering drugs that need to be delivered quickly to the brain?
Which route of administration is NOT suitable for administering drugs that need to be delivered quickly to the brain?
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Which of these is a disadvantage of using a sublingual route of administration?
Which of these is a disadvantage of using a sublingual route of administration?
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Which of these is a potential advantage of administering a drug transdermally?
Which of these is a potential advantage of administering a drug transdermally?
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What is the primary means of drug excretion?
What is the primary means of drug excretion?
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What is the term for a drug that reduces the activity of an enzyme?
What is the term for a drug that reduces the activity of an enzyme?
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What type of enzyme activity is associated with genetic polymorphism?
What type of enzyme activity is associated with genetic polymorphism?
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What is the primary factor that contributes to drug tolerance?
What is the primary factor that contributes to drug tolerance?
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Which of the following factors is NOT a major factor in drug metabolism?
Which of the following factors is NOT a major factor in drug metabolism?
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What is the process known as when two drugs compete for the same enzyme?
What is the process known as when two drugs compete for the same enzyme?
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What is the term used to describe the time it takes for half of a drug to be eliminated from the body?
What is the term used to describe the time it takes for half of a drug to be eliminated from the body?
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Which of the following is NOT a route of drug excretion?
Which of the following is NOT a route of drug excretion?
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What is the primary effect of metabolism on a drug?
What is the primary effect of metabolism on a drug?
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What is a key factor affecting the rate of drug absorption?
What is a key factor affecting the rate of drug absorption?
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How do lipophilic molecules affect drug absorption?
How do lipophilic molecules affect drug absorption?
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What is the primary function of depot binding?
What is the primary function of depot binding?
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Which of the following is the most likely consequence of a drug interaction?
Which of the following is the most likely consequence of a drug interaction?
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What is the primary role of the kidneys in drug excretion?
What is the primary role of the kidneys in drug excretion?
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What characteristic of a molecule is most likely to facilitate its excretion through the kidneys?
What characteristic of a molecule is most likely to facilitate its excretion through the kidneys?
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What is the significance of the term 'first-order kinetics' in regards to drug excretion?
What is the significance of the term 'first-order kinetics' in regards to drug excretion?
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What are the four principal components of pharmacokinetics?
What are the four principal components of pharmacokinetics?
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What is the meaning of 'Depot binding' in the context of pharmacokinetics?
What is the meaning of 'Depot binding' in the context of pharmacokinetics?
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What is the primary goal of 'metabolism' in pharmacokinetics?
What is the primary goal of 'metabolism' in pharmacokinetics?
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What is the difference between 'drug actions' and 'drug effects'?
What is the difference between 'drug actions' and 'drug effects'?
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Which of the following is NOT a component of pharmacokinetics?
Which of the following is NOT a component of pharmacokinetics?
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How does pharmacokinetics contribute to the clinical use of drugs?
How does pharmacokinetics contribute to the clinical use of drugs?
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What is the difference between an agonist and an antagonist?
What is the difference between an agonist and an antagonist?
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What is the primary focus of 'neuro-psychopharmacology'?
What is the primary focus of 'neuro-psychopharmacology'?
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What is the primary factor determining a drug's ability to cross cell membranes?
What is the primary factor determining a drug's ability to cross cell membranes?
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Which of the following body compartments has a relatively small surface area, resulting in slower drug absorption?
Which of the following body compartments has a relatively small surface area, resulting in slower drug absorption?
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What happens to the solubility of aspirin in the blood compared to the stomach?
What happens to the solubility of aspirin in the blood compared to the stomach?
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What is the primary reason for the blood-brain barrier's (BBB) resistance to large molecule drugs?
What is the primary reason for the blood-brain barrier's (BBB) resistance to large molecule drugs?
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Which of the following drugs is more likely to readily cross the BBB?
Which of the following drugs is more likely to readily cross the BBB?
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What is the significance of the pKa value of a drug in terms of its absorption?
What is the significance of the pKa value of a drug in terms of its absorption?
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Which of the following statements is TRUE regarding drug distribution?
Which of the following statements is TRUE regarding drug distribution?
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What is TRUE about the permeability of peripheral capillaries compared to brain capillaries?
What is TRUE about the permeability of peripheral capillaries compared to brain capillaries?
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What is the main reason behind the limited access of most small molecule pharmaceuticals to the brain?
What is the main reason behind the limited access of most small molecule pharmaceuticals to the brain?
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Which of the following accurately describes the role of transporters in drug distribution?
Which of the following accurately describes the role of transporters in drug distribution?
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Flashcards
Pharmacokinetics
Pharmacokinetics
The study of how drugs are absorbed, distributed, metabolized, and excreted in the body.
ADME
ADME
An acronym for Absorption, Distribution, Metabolism, and Excretion of drugs.
Absorption
Absorption
The process of a drug entering the body fluids after administration.
Distribution
Distribution
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Metabolism
Metabolism
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Drug Actions
Drug Actions
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Drug Effects
Drug Effects
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Receptor-Ligand Interaction
Receptor-Ligand Interaction
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Efflux Transporters
Efflux Transporters
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Blood-Brain Barrier (BBB)
Blood-Brain Barrier (BBB)
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Depot Binding
Depot Binding
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Therapeutic Outcome
Therapeutic Outcome
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Individual Drug Efficacy
Individual Drug Efficacy
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Excretion
Excretion
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Routes of administration
Routes of administration
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Oral administration (PO)
Oral administration (PO)
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Intravenous (IV)
Intravenous (IV)
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First-pass metabolism
First-pass metabolism
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Drug Polarity
Drug Polarity
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Inhalation route
Inhalation route
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Transdermal route
Transdermal route
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Passive Diffusion
Passive Diffusion
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Lipid Soluble Drugs
Lipid Soluble Drugs
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Intramuscular (IM)
Intramuscular (IM)
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pKa Value
pKa Value
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Subcutaneous (SC)
Subcutaneous (SC)
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Topical administration
Topical administration
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Ionized vs. Non-Ionized
Ionized vs. Non-Ionized
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Solubility
Solubility
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Polarity of molecules
Polarity of molecules
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Absorption Factors
Absorption Factors
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Intestinal Absorption
Intestinal Absorption
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Drug absorption
Drug absorption
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Drug Distribution
Drug Distribution
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Polar molecules
Polar molecules
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Biotransformation
Biotransformation
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CyP450 enzymes
CyP450 enzymes
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First Order Kinetics
First Order Kinetics
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Lipophilic Molecules
Lipophilic Molecules
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Hydrophilic Molecules
Hydrophilic Molecules
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Drug Competition
Drug Competition
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Enzyme Induction
Enzyme Induction
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Enzyme Inhibition
Enzyme Inhibition
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Genetic Polymorphisms
Genetic Polymorphisms
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Poor Metabolizers (PM)
Poor Metabolizers (PM)
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Extensive Metabolizers (EM)
Extensive Metabolizers (EM)
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Half-Life (t½)
Half-Life (t½)
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Study Notes
Pharmacology - Pharmacokinetics and Pharmacodynamics
- Pharmacology is the study of how drugs affect the body
- Neuropharmacology focuses on the effects of drugs on the brain and subsequent actions on behavior
- Drug actions refer to specific molecular changes resulting from drug binding to a receptor
- Drug effects involve widespread alterations in physiology or psychology arising from drug actions
- Pharmacokinetics examines the factors influencing drug bioavailability and efficacy within the human body—everything besides the actions of the drug
Learning Objectives
- Understanding and applying pharmacokinetic principles, focusing on drugs impacting the brain.
- Examining drug administration and absorption mechanisms, distribution, metabolism, and excretion pathways
- Reviewing receptor-ligand interactions and distinguishing among ligand-receptor, drug-receptor, and enzyme-substrate interactions.
- Differentiating between drug-receptor interactions, resulting effects, agonists versus antagonists, competitive and non-competitive binding, allosteric effects, and partial/inverse agonists.
- Describing long-term drug use effects such as drug tolerance, sensitization, and dependence.
Neuro-Psychopharmacology
- Neuro-psychopharmacology studies drug effects on the central nervous system and the resultant impact on human behavior.
Principal Components (ADME)
- Absorption: Drug administration and absorption into body fluids (e.g., bloodstream)
- Distribution: Drug dispersal throughout body fluids to target tissues
- Metabolism: Biotransformation or inactivation of drugs into metabolites.
- Excretion: Removal of substances or metabolites from the body
Routes of Administration
- Oral (PO): Preferred for clinical use; drugs are absorbed through the gastrointestinal tract.
- Intravenous (IV): Most rapid; drugs are directly injected into the bloodstream.
- Intramuscular (IM): Used for slow, even distribution; drugs are injected into muscle tissue.
- Subcutaneous (SC): Drugs are injected into the fatty tissue beneath the skin.
- Inhalation: Drugs are inhaled and absorbed by the lungs; this method is frequently used for rapid effects
- Intranasal: Drugs are administered through the nasal passages/membranes.
- Sublingual: Drugs are placed under the tongue for rapid absorption.
- Transdermal: Drugs are absorbed through the skin..
- Intraperitoneal: Used in animals for direct access to the abdominal cavity
- Intracranial: Used to deliver drugs directly into the cerebrospinal fluid (CSF), but mostly for experiments due to difficulty in humans
- Intracerebroventricular, intracisternal, intrathecal: Used for delivery to CSF, but mostly for experiments on animals.
Pharmacokinetic Factors
- First-pass metabolism: Drug breaks down in the liver prior to reaching the systemic circulation, decreasing its bioavailability.
- Blood-brain barrier (BBB): Limits passage of many drugs to the brain; only lipophilic substances cross easily.
- Depot binding: Drugs bind to inactive sites; this reduces the amount of free drug and can impact the efficacy and duration of action
- Competition among drugs: Different drugs compete for binding to the same receptor or metabolizing enzymes, affecting efficacy.
- Drug polarity: Nonpolar, lipid-soluble drugs readily diffuse across cell membranes; polar, charged drugs face greater barriers.
- Factors affecting absorption: Drug concentration, physiological factors (e.g., body size, age, pH), metabolic or digestive breakdown, and drug solubility. -Factors affecting absorption:** Intrinsic drug properties (especially polarity and solubility), pH of body compartments, and surface area of absorption sites (e.g., stomach versus intestines).
- Other Factors that Influence Metabolism:
- Enzyme induction: Repeated use of a drug can lead to increased levels of liver enzymes, which may lead to increased metabolism of other drugs.
- Enzyme inhibition: Certain drugs can inhibit enzymes involved in metabolism, which can lead to increased levels of other drugs in the blood.
- Drug Competition: Competition for enzymes may prevent some drugs from being metabolized efficiently.
- Individual differences: Different individuals have different rates of metabolism due to factors like age, sex, and genetics.
Drug Metabolism
- Biotransformation and elimination affect bioavailability
- Primarily occurs in the liver under control of microsomal enzymes (e.g., cytochrome P450 (CYP) system).
- Metabolism often involves two phases; Phase I often involves altering the drug structure while Phase II often involves conjugation of the altered drug with other substances.
- Factors influencing metabolism: enzyme induction/inhibition, drug competition, individual variability.
Drug Excretion
- Primary means of drug excretion is through urine after filtration by the kidneys.
- Drugs are typically eliminated via first-order kinetics (exponential elimination).
- Important physiological factors: rates, and potential for individual variation
Key Points of Pharmacokinetics
- Administration and absorption are critical
- Distribution affects drug actions, depot binding is a factor
- Drug metabolism changes drug structure and efficacy
- Excretion removes drugs through various pathways.
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Description
Test your knowledge on drug administration routes and absorption in pharmacology with this quiz. Explore key concepts such as first-pass effect, intravenous administration advantages, and the factors affecting drug absorption. This quiz is essential for understanding drug delivery methods to the central nervous system.