The study of how the body processes drugs, including absorption, distribution, metabolism, and excretion.
2
What is pharmacodynamics?
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The study of how drugs affect the body and the body's response to them.
3
What is pharmacotherapeutics?
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The application of pharmacokinetics and pharmacodynamics to the selection and use of drugs for the treatment of diseases.
4
What is the first phase of pharmacokinetics?
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Drug Absorption
5
What is the second phase of pharmacokinetics?
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Drug Distribution
6
What is the third phase of pharmacokinetics?
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Drug Metabolism
7
What is the fourth phase of pharmacokinetics?
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Drug Elimination
8
What is bioavailability?
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The fraction of the administered dose that reaches the systemic circulation and is available to exert its pharmacological effect.
9
List the factors affecting absorption.
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Dosage form and route of administration, first-pass metabolism, transport across membrane, blood supply to the biological compartment, physical and chemical properties, disease state.
10
What is the rate of transport for unionized drugs across a membrane?
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Drugs diffuse passively according to the concentration gradient.
11
How does the ionization degree of a drug affect its transport across a membrane?
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Only the unionized form of a drug can diffuse across biologic membranes.
12
What is the Henderson-Hasselbalch equation used for?
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It relates the dissociation of a weak acid or base and the pH of a biological medium.
13
What does pKa represent in the context of the Henderson-Hasselbalch equation?
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It is the acid dissociation constant of a drug.
14
How does the ionization status of a drug affect its absorption and excretion?
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The ionization status affects the drug's ability to cross biological membranes and be excreted.
15
What is the relationship between pH and the predominant forms of a weak acid HA and its conjugate base A-?
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When pH is less than pKa, HA and BH+ predominate. When pH is greater than pKa, A- and B predominate.
16
What is the significance of pH = pKa in the context of a weak acid HA and its conjugate base A-?
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At pH = pKa, the concentrations of HA and A- are equal.
17
What is the ionization behavior of a weak base in acidic pH?
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A weak base is ionized in acidic pH.
18
In what pH environment is a weak acid ionized?
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A weak acid is ionized in basic pH.
19
How does the ionized form of a drug affect its excretion?
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The ionized form (B-, H+) is more hydrophilic and thus more excreted.
20
What is drug distribution in pharmacology?
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The dissemination of the drug from the blood to the extracellular fluids and tissues.
21
How does the distribution rate of drugs vary among different tissues?
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The distribution rate depends on blood flow to organs, with brain, liver, and kidney having higher blood flow compared to muscle, skin, fat, and bone.
22
What is the formula for Volume of Distribution (Vd)?
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Vd = Amount of drug in the body tissue (mg) / C0 (mg/L)
23
How does a low Vd value relate to plasma protein binding?
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A low Vd may indicate extensive plasma protein binding.
24
What factors can influence Vd?
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Vd can be influenced by age, sex, weight, and disease processes such as edema and ascites.
25
What factors influence the distribution of a drug in the body?
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Cardiac output, capillary permeability, binding to plasma proteins or tissue proteins, relative lipophilicity of a drug, and biological barriers like the blood-brain barrier (BBB) and placenta.
26
What is the term for the initial rapid increase in plasma concentration after an IV bolus injection?
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Distribution phase
27
What is the importance of albumin in drug binding?
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Albumin is an important plasma protein for drug binding.
28
Which drugs are bound by serum albumin?
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Serum albumin binds many acidic drugs such as ibuprofen.
29
What is the term for the process where drugs are actively transported into tissues?
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Sequestration
30
What is the significance of 'free' drug in pharmacology?
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Pharmacologically active drug
31
How do tissue reservoirs affect drug action?
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They serve as a source of the drug and prolong its actions, which can cause local drug toxicity.
32
What is the main site for drug metabolism?
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Liver
33
What enzymes are involved in drug metabolism?
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Hepatic microsomal enzymes, including the cytochrome P450 family
34
What should be considered for patients with decompensated livers regarding drug dosage?
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Dosage adjustment may be required, and consultation with a primary care physician (PCP) is recommended
35
What is the role of the Cytochrome P-450 (CYP) enzyme group?
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The CYP enzyme group is responsible for most drug oxidation reactions (70%).
36
Where are the CYP enzymes located?
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The CYP enzymes are located in the liver, specifically in the endoplasmic reticulum.
37
Which CYP enzymes are primarily responsible for the metabolism of most drugs?
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CYP2C, CYP2D, and CYP3A are the primary CYP enzymes responsible for the metabolism of most drugs.
38
What are CYP 450 inducers and what effect do they have on drug metabolism?
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CYP 450 inducers are substances that increase the activity of the cytochrome P450 enzymes, leading to increased drug metabolism and a decrease in plasma concentrations of drugs, potentially resulting in suboptimal therapeutic effects.
39
List some examples of CYP 450 inhibitors and explain their effect on drug concentrations.
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Examples of CYP 450 inhibitors include omeprazole, cimetidine, macrolide antibiotics, azole antifungals, and grapefruit juice. These substances can significantly increase plasma drug concentrations, leading to adverse effects or drug toxicity.
40
What are the two metabolic phases of drug metabolism?
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Phase I and Phase II
41
What are the main reactions involved in Phase I metabolism?
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Oxidation, reduction, and/or hydrolysis
42
What is the typical fate of a drug after Phase I metabolism?
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Activated, unchanged, or inactivated
43
What are Phase I metabolic reactions?
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Phase I metabolic reactions are non-synthetic reactions catalyzed by hepatic microsomal enzymes, primarily involving oxidation, reduction, and hydrolysis to produce more hydrophilic compounds.
44
Which enzymes are mainly involved in Phase I reactions?
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Phase I reactions are mainly catalyzed by hepatic microsomal enzymes, particularly the cytochrome P450 enzyme family.
45
What are the main outcomes of Phase I reactions?
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Phase I reactions result in the inactivation of drugs, conversion of inactive drugs into active metabolites, and conversion of drugs into toxic compounds.
46
What are Phase II metabolic reactions?
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Synthetic reactions involving conjugation of the parent compound or its metabolite with glucuronic acid, acetic acid, or glycine.
47
How do Phase II reactions typically affect drug activity?
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They usually lead to drug inactivation.
48
What is portal circulation in the context of drug metabolism?
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The rate of blood flow to the liver and plasma protein binding.
49
How does liver function affect drug metabolism?
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Patients with decompensated livers will have lower metabolic activity.
50
What role do genetic factors play in drug metabolism?
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Individuals vary in their inherited ability to metabolize drugs.
51
What is the main organ for drug excretion?
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The kidney
52
What is renal clearance of drugs?
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It measures the volume of plasma that is cleared from the drug per minute.
53
What is the formula for calculating renal clearance (CL)?
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CL (ml/min) = Rate of drug elimination / plasma drug concentration
54
What are the three mechanisms by which renal excretion occurs?
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Glomerular filtration, active transport, and tubular reabsorption.
55
How does glomerular filtration contribute to renal excretion?
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Most chemicals and drugs with low molecular weight are excreted by glomerular filtration.
56
What factors influence renal clearance?
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Age, urine pH, and disease conditions such as heart failure, kidney, or liver disease.
57
What is first-order elimination in drug kinetics?
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A constant fraction of drug is eliminated per unit time, depending on the plasma drug concentration.
58
What is zero-order elimination in drug kinetics?
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A constant amount of the drug is eliminated per unit time regardless of the plasma concentration.
59
What is the definition of half-life (t Ā½)?
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The time needed for the plasma drug concentration to be reduced by 50%
60
Which type of drug kinetics does elimination half-life apply to?
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First order kinetics
61
How long does it take for most drugs to be cleared from the body?
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After 4-5 half-lives
62
What is the formula for calculating half-life (tĀ½)?
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tĀ½ = 0.693 Vd/CL
63
How does obesity affect the volume of distribution (Vd) and half-life (tĀ½)?
Show answer
Obesity increases Vd and tĀ½.
64
What is the effect of a CYP inducer on clearance (CL) and half-life (tĀ½)?
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A CYP inducer increases CL and decreases tĀ½.
65
What is the significance of the elimination half-life in drug kinetics?
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The elimination half-life is crucial for determining the dosing schedule to achieve a steady-state concentration and optimal therapeutic effect.
66
How many half-lives are typically required to reach a steady state in drug kinetics?
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Usually, 4 half-lives are required to reach a steady state.
67
What is pharmacodynamics?
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The study of how drugs interact with the body to produce a pharmacological effect.
68
What is a drug-receptor interaction?
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The binding of a drug to a specific receptor on a cell, which leads to a biological response.
69
What is a graded dose-response curve?
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A graph that shows the relationship between the dose of a drug and the intensity of its pharmacological effect.
70
What are the main categories of drug targets mentioned in the slide?
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Proteins and Others
71
What percentage of drug targets are receptors according to the pie chart?
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47%
72
What is a ligand in pharmacodynamics?
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A ligand is a substance that binds to a receptor.
73
How do drug-receptor interactions typically occur?
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Drug-receptor interactions are usually reversible.
74
What is the relationship between the number of receptors and the magnitude of a pharmacologic response?
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The magnitude of a pharmacologic response is proportional to the number of receptors available for drug.
75
What are the three stages of signal transduction?
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Reception, Transduction, Cell Response
76
What happens during the Reception stage of signal transduction?
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Receptors bind to ligands
77
What occurs during the Transduction stage of signal transduction?
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Receptor protein changes activate intracellular molecules (2nd messengers)
78
What are Ligand-gated ion channels and how do they function?
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Ligand-gated ion channels are cell surface receptors that open in response to ligand binding, allowing ion exchange which initiates cell signaling.
79
Provide an example of a Ligand-gated ion channel and its ligand.
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Cholinergic nicotinic receptors are an example of Ligand-gated ion channels, activated by acetylcholine.
80
What are G protein-coupled receptors?
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Seven-transmembrane receptors that are common drug targets for hydrophilic molecules.
81
What happens after G protein-coupled receptors are activated?
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G proteins bind secondary messengers leading to signal amplification.
82
What are some effector molecules activated by G protein-coupled receptors?
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Adenyl cyclase (cAMP) and phospholipase C (increase calcium concentration).
83
What are enzyme-linked receptors and how do they function?
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Enzyme-linked receptors are cell surface receptors that undergo conformational changes upon ligand binding, leading to increased intracellular enzyme activity. Some receptors have tyrosine kinase activity, which induces a phosphorylation chain.
84
Provide an example of an enzyme-linked receptor and its function.
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Insulin receptors are an example of enzyme-linked receptors. Upon ligand-induced activation, they undergo conformational changes, leading to increased intracellular enzyme activity and the induction of a phosphorylation chain.
85
What are intracellular receptors and how do they work?
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Intracellular receptors are receptors that can diffuse through the plasma membrane. They bind to hydrophobic ligands, such as cortisol, and interact with specific DNA sequences to activate or deactivate transcription of target genes.
86
What is the role of receptor-ligand binding in intracellular receptors?
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Receptor-ligand binding promotes interaction with specific DNA sequences, leading to the activation or deactivation of transcription of target genes.
87
What is receptor-mediated drug action?
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The process by which drugs interact with specific receptors on or within cells to produce a biological effect.
88
What are the two main types of receptors involved in drug action?
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G-protein coupled receptors (GPCRs) and ion channel-linked receptors.
89
What is the definition of intrinsic activity in the context of agonists?
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Intrinsic activity is a measure of the drug's ability to activate a receptor after binding.
90
What are full agonists and how do they differ from partial agonists?
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Full agonists are drugs capable of binding to receptors causing maximal activation, with intrinsic activity equal to 1. Partial agonists can occupy all receptors without producing a maximal response, with intrinsic activity less than 1.
91
What is an antagonist in pharmacology?
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A drug that binds to the receptor without activation or initiating a response, blocking the action of an agonist or any endogenous substance that activates that receptor.
92
What is a competitive antagonist?
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A competitive antagonist binds to the receptor in the same site for the agonist without causing receptor activation.
93
What is a noncompetitive antagonist?
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A noncompetitive antagonist does not bind to the same site as an agonist.
94
What is a competitive antagonist?
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A medication that reversibly binds to the same receptor site where an agonist binds but does not activate it.
95
How does a noncompetitive antagonist differ from a competitive antagonist?
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A noncompetitive antagonist does not bind to the same site as an agonist and its binding to the receptor is irreversible or dissociates very slowly.
96
What is receptor downregulation?
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The process where repeated exposure to agonists leads to a diminished response of the cell.
97
What is the term for the diminished response to repeated exposure to agonists?
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Tolerance or tachyphylaxis.
98
What is desensitization or tachyphylaxis?
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A rapid decrease in the body's responsiveness to a drug, often occurring with the initial dose.
99
How does tolerance differ from desensitization or tachyphylaxis?
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Tolerance happens more gradually and typically occurs with repeated doses, whereas desensitization or tachyphylaxis can occur with the initial dose.
100
What does EC50 stand for and what does it represent?
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EC50 stands for Effective Concentration 50, which is the concentration of a drug that produces 50% of its maximum response.
101
What is the maximal efficacy of a drug (Emax) and how is it defined?
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The maximal efficacy of a drug (Emax) is defined as the drug occupying all receptors, yielding the maximum response.
102
What is the definition of potency in pharmacology?
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The concentration (EC50) of a drug required to produce 50% of its maximal response.
103
How is potency used in comparing drugs?
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Potency is used to compare drugs within the same group.
104
What is efficacy in pharmacology?
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The ability of a drug to elicit the maximal pharmacologic response.
105
How does efficacy differ from potency?
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Efficacy is the maximal response, while potency is the dose required to achieve that response.
106
What is the therapeutic goal in understanding drug dose changes?
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To understand how changes in drug dose alter the patientās response.
107
What is the significance of comparing pharmacologic potency and efficacy for different medications?
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To choose the suitable medication according to clinical needs.
108
What is the treatment for opioid overdose?
Show answer
Naloxone
109
What is pharmacotherapeutics?
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The study of the use of drugs in the treatment of diseases.
110
What is the date of the slide?
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11/4/2025
111
What is pharmacotherapeutics?
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Application of pharmacological principles on a population level to achieve a therapeutic outcome.
112
What does pharmacotherapeutics monitor?
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It monitors drug efficacy (therapeutic index), safety margin, tolerance/dependence, interactions, and side/adverse effects.
113
What does the quantal dose-response relationship record?
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It records the population response to a given drug.
114
What is the definition of Effective dose 50 % (ED 50)?
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The minimal drug concentration that induces the specified therapeutic effect in 50 % of subjects' pool.
115
What is the definition of Toxic dose 50 % (TD 50)?
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The drug concentration sufficient to induce adverse effects in 50 % of the subjects' pool.
116
What is the definition of Lethal dose 50 (LD 50)?
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The drug concentration that induces death in 50% of the recipient pool.
117
How is the Therapeutic index (TI) calculated?
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TI = LD50/ED50 or TD50/ED50.
118
What is the definition of the margin of safety in pharmacology?
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The margin of safety is the dose range between the minimum therapeutic dose and the toxic dose.
119
How does a larger therapeutic index relate to the safety of a drug?
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A larger therapeutic index indicates a safer administered drug.
120
Which drug has a higher therapeutic index and larger margin of safety than warfarin?
Show answer
Penicillin
121
What is Pharmacogenetics?
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The study of how genetic differences influence drug response.
122
What is Cytochrome P450?
Show answer
A family of enzymes involved in drug metabolism.
123
What does SNP stand for?
Show answer
Single Nucleotide Polymorphism
124
What is the threshold for drug-induced liver injury in the context of the slide?
Show answer
The threshold is indicated by the dashed line on the graph.
125
What percentage of adverse drug reactions (ADRs) are involved in Phase I enzyme metabolisms?
Show answer
60%
126
Which enzymes are primarily involved in Phase I enzyme metabolisms?
Show answer
CYP2D6 and CYP3A4
127
What is the significance of the CYP2D6 gene being highly polymorphic?
Show answer
Genetic variations can affect the rate of drug metabolism by CYP2D6 enzymes, impacting patient response to medication.
128
What is the definition of an ultrarapid metabolizer?
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An ultrarapid metabolizer has an accelerated drug metabolism with a higher rate of drug elimination and possibly lower efficacy.
129
What is the definition of a poor metabolizer?
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A poor metabolizer has slower drug metabolism leading to drug accumulation, higher potential for adverse events, drug-drug interactions, and lower efficacy.
130
What is the prevalence of ultra-rapid metabolizers in Whites (European, North American) per 100 people?
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1-10
131
What is the prevalence of ultra-rapid metabolizers in Blacks (African Americans) per 100 people?
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3-4
132
What is the prevalence of ultra-rapid metabolizers in East Asian (Chinese, Japanese, Korean) per 100 people?
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1-2
133
What is a patient profile in the context of dental medicine?
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A detailed record of a patient's medical history, dental health, and treatment plan.
134
What institution is mentioned in the slide?
Show answer
California Northstate University College of Dental Medicine.
135
What are the key factors that influence drug metabolism and efficacy?
Show answer
Age, smoking and drinking habits, pregnancy status, liver or kidney disease, pharmacogenetics, drug-drug interaction, and psychosocial factors.
136
What are the effects of smoking and drinking on drug metabolism?
Show answer
Smoking and drinking can induce the cytochrome 450 enzymes.
137
What was the classification system for drugs during pregnancy before 2016?
Show answer
A five-letter risk category system
138
What does Category A indicate about the potential risk to the fetus in the first trimester of pregnancy?
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No potential risk
139
What does Category D indicate about the potential risk to the fetus based on human studies?
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Positive evidence of human fetal risk
140
What year did the FDA replace the prescription drug categories with a new labeling system?
Show answer
2016
141
What is the new labeling system for prescription drugs called?
Show answer
Pregnancy and lactation labeling final rule
142
What information is provided in the pregnancy section of the new labeling system?
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Information relevant to the use of the drug in pregnant women (like dosing, fetal risks)
143
What is pharmacokinetic drug interaction?
Show answer
A drug alters the absorption, distribution, metabolism, or excretion of another drug, changing the amount available to produce the desired effect.
144
What is pharmacodynamic drug interaction?
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Drugs influence each other's effects directly, such as two drugs increasing blood pressure.
145
What is synergistic effect?
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Two drugs increase the effect of each other, such as two drugs increasing blood pressure.
146
What does CYP450 refer to in the context of drug metabolism?
Show answer
CYP450 is a family of enzymes involved in the metabolism of drugs and other xenobiotics in the liver.
147
Which enzyme is responsible for metabolizing Asenapine?
Show answer
CYP1A2 is responsible for metabolizing Asenapine.
148
What is the color coding in the legend used to indicate the strength of inhibition?
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The legend uses yellow for weak, orange for moderate, and red for strong inhibition.
149
What is the title of the book on the left?
Show answer
Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy