PHARM 5663 – EXAM 1: WEEKS 1 & 2
Differentiate pharmacodynamics (PD) from pharmacokinetics (PK).
● Pharmacology – The
● Pharmacodynamics – The study of the biochemical and physiologic effects of drugs on the body and the molecular mechanisms
by which those effects are produced. To participate rationally in achieving the therapeutic objective, an understanding of
pharmacodynamics is essential
● Pharmacokinetics – What the body does to the drug. “The study of drug movement throughout the body.” Think: kinetics, as is
body movement. ADME: absorption, distribution, metabolism, excretion
What happens with pharmacology drug-receptor interactions on a molecular level?
Drugs produce their effects by interacting with other chemicals. Receptors are the special chemical sites in the body that most
drugs interact with to produce effects. We can define a receptor as any functional macromolecule in a cell to which a drug binds
to produce its effects.
Explain the various types of agonists and antagonists.
● Agonists – Are molecules that activate receptors. Because neurotransmitters, hormones, and other endogenous regulators
activate the receptors to which they bind, all these compounds are considered agonists. When drugs act as agonists, they simply
bind to receptors and mimic the actions of the body's own regulatory molecules. For example, dobutamine is a drug that mimics
the actions of NE at receptors on the heart, thereby causing heart rate and force of contraction to increase.
● Antagonists – Antagonists produce their effects by preventing receptor activation by endogenous regulatory molecules and
drugs. Antagonists have virtually no effects of their own on receptor function. In terms of a receptor but with no intrinsic activity.
Affinity allows the antagonist to bind the receipts, but lack of intrinsic activity prevents the bound antagonist from causing
receptor activation. Although antagonists do not cause receptor activation they most certainly do prevent the activation of
receptors by endogenous regulatory molecules. The response to an antagonist is determined by how much agonist is present.
What are the four basic concepts of pharmacokinetics?
1. Absorption: into blood
2. Distribution: movement from blood to interstitial space of tissues
3. Metabolism:(biotransformation)
4. excretion
How would I use these when prescribing?
What are the physicochemical properties for drug transfer?
Chemical properties such as solubility, the types of bonds formed, polarity, protein binding effect a medication’s ability to enter
the body and exert therapeutic effect.
What factors modify drug distribution and what is the relationship to elimination?
??“Movement of drugs from the systemic circulation to the site of drug action”
1. Blood flow to tissues
2. Ability of a drug to exit the vascular system
3. Ability of a drug to enter the cells
What factors affect metabolism?
,What is the difference between Phase I and Phase II metabolism?
• Goal is to increase water solubility of medications.
• Phase I metabolism
o oxidation (via cytochrome P450), reduction, and hydrolysis reactions
o phase I reactions convert a parent drug to more polar (water soluble) active metabolites by unmasking or inserting a polar
functional group (-OH, -SH, -NH2)
o geriatric patients have decreased phase I metabolism
drugs metabolized via phase I reactions have longer half-lives
geriatric patients metabolism drugs by phase II reactions
• Phase II metabolism
o glucuronidation, acetylation, and sulfation reactions
o "conjugation reactions" that increase water solubility of drug with a polar moiety
glucuronate, acetate, and sulfate, respectively
phase II reactions convert a parent drug to more polar (water soluble) inactive metabolites by conjugation of
subgroups to -OH, -SH, -NH2 functional groups on drug
drugs metabolized via phase II reactions are renally excreted (increased water = to the kidneys)
patients deficient in acetylation capacity (slow acetylators) may have prolonged or toxic responses to normal doses of
certain drugs because of decreased rates of metabolism
• Phase I – Phase I reactions usually convert the parent drug to a more polar metabolite by introducing or unmasking a
functional group (–OH, –NH2, –SH). Three subcategories are oxidation, reduction or hydrolysis. These type of reactions serve
to convert lipophilic drugs into more polar molecules. Often these metabolites are inactive, although in some instances, activity
is only modified or even enhanced. If phase I metabolites are sufficiently polar, they may be readily excreted. However, many
phase I products are not eliminated rapidly and undergo a subsequent reaction in which an endogenous substrate such as
glucuronic acid, sulfuric acid, acetic acid, or an amino acid combines with the newly incorporated functional group to form a
highly polar conjugate.
• Phase II – Such conjugation or synthetic reactions (secondary reactions from Phase I that form highly polar substances) are the
hallmarks of phase II metabolism.
What are the basic parameters of clearance pharmacokinetics?
How does pharmacokinetics impact therapeutic dosing?
Pharmacokinetic processes determine how much drug will be at its sites of action at any given time. In most cases the time course
of drug action bears a direct relationship to the concentration of a drug in the blood. Monitoring plasma drug levels is important
to measure drug responses. Single dose time course shows how plasma drug levels change over time after a single dose of an oral
medication. Important to stay within therapeutic range. Drug half-life means the time required for the amount of drug in the body
to decrease by 50%.
What are mechanisms of drug toxicity?
Altered pharmacokinetic process, namely hepatic enzyme activity.
Decreased renal excretion
, First ingredient is the _____ ingredient. - active.
(ingredients after that are either less potent, less active, and/or less amount)
Inactive constituents are made up of _____, _____ and _____ & _____. - fillers, vehicles, flavoring, & dyes (makes the drug
edible)
Fillers are used to make the pill _____ - larger (larger pills can sometimes be easier for pts to swallow and easier to handle)
Vehicles are the _____ to get the drug into the system – solvents (make the drug digestible/break down, so pt's body can
use/absorb)
teratogen - a substance that causes malformation of an embryo. (birth defects)
_____ is a well known teratogen that used to be used to treat _____. It caused _____. – Thalidomide, morning sickness in
expectant mothers, limb defects
The _____ came up with the schedules for controlled substances/drugs. Schedule I is the _____ addictive and Schedule V is the
_____ addictive. - Controlled Substance Act of 1970, most, least
Know Schedule for each drug that we need to memorize, esp if "surprising" info. (eg. a drug that is very addictive but only SIII) -
Study Schedules for drugs if listed on Drug Table!
Gold standard for drug development? - randomized controlled trial
Know the general process of drug approval* very basic overview "where the drug goes in each stage of development" - Phase 1 -
Humans (a few healthy humans) testing starts (before that is animal testing)
Phase 2 - 100s humans with the disease
Phase 3 - 1000s humans
If a drug is a Pregnancy Category X, it has a _____ of _____. - high risk, fetal abnormality (risk outweighs the benefit. most
teratogens)
The 3 most important properties of an ideal drug are _____, _____ and _____. – effectiveness, safety (risk vs benefit), selectivity
- doing what it's exactly supposed to do (fever med - lower fever)
ADOPIE - Nursing Process, Assessment, Diagnosis, Outcomes, Planning, Implementation, Evaluation
Pharmacodynamics cover _____ and _____ - how a drug works physiologically, what it does to or for the body
Antagonist vs Agonist. An antagonist _____ - Antagonist prevents the agonist from binding with the receptor or inactivates the
receptor
Competitive - competes with agonist for receptor sites, is reversible/not permanent
Noncompetitive - A(n) _____ inhibitor binds to a site on the enzyme that is not the active site (different site/inactivated site)
irreversible
Affinity is how well a drug can _____. – bind, (either can or cannot bind)
Efficacy is _____. - the relationship between receptor and ability to initiate a response, (eg. competitive relationship - affinity, but
no efficacy)
contraindication - any reason that you shouldn't give someone a drug, allergy, category X drug to a pregnant woman, side effects -
expected (or not surprising) effects, any effects of a medication other than the desired ones, adverse effects - not expected effects
(and should stop taking drug)
A general term for any undesirable effects that are a direct response to one or more drugs.
Drug Allergy Type 1 - IgE antibodies, anaphylactic (throat closing/difficulty breathing)
Differentiate pharmacodynamics (PD) from pharmacokinetics (PK).
● Pharmacology – The
● Pharmacodynamics – The study of the biochemical and physiologic effects of drugs on the body and the molecular mechanisms
by which those effects are produced. To participate rationally in achieving the therapeutic objective, an understanding of
pharmacodynamics is essential
● Pharmacokinetics – What the body does to the drug. “The study of drug movement throughout the body.” Think: kinetics, as is
body movement. ADME: absorption, distribution, metabolism, excretion
What happens with pharmacology drug-receptor interactions on a molecular level?
Drugs produce their effects by interacting with other chemicals. Receptors are the special chemical sites in the body that most
drugs interact with to produce effects. We can define a receptor as any functional macromolecule in a cell to which a drug binds
to produce its effects.
Explain the various types of agonists and antagonists.
● Agonists – Are molecules that activate receptors. Because neurotransmitters, hormones, and other endogenous regulators
activate the receptors to which they bind, all these compounds are considered agonists. When drugs act as agonists, they simply
bind to receptors and mimic the actions of the body's own regulatory molecules. For example, dobutamine is a drug that mimics
the actions of NE at receptors on the heart, thereby causing heart rate and force of contraction to increase.
● Antagonists – Antagonists produce their effects by preventing receptor activation by endogenous regulatory molecules and
drugs. Antagonists have virtually no effects of their own on receptor function. In terms of a receptor but with no intrinsic activity.
Affinity allows the antagonist to bind the receipts, but lack of intrinsic activity prevents the bound antagonist from causing
receptor activation. Although antagonists do not cause receptor activation they most certainly do prevent the activation of
receptors by endogenous regulatory molecules. The response to an antagonist is determined by how much agonist is present.
What are the four basic concepts of pharmacokinetics?
1. Absorption: into blood
2. Distribution: movement from blood to interstitial space of tissues
3. Metabolism:(biotransformation)
4. excretion
How would I use these when prescribing?
What are the physicochemical properties for drug transfer?
Chemical properties such as solubility, the types of bonds formed, polarity, protein binding effect a medication’s ability to enter
the body and exert therapeutic effect.
What factors modify drug distribution and what is the relationship to elimination?
??“Movement of drugs from the systemic circulation to the site of drug action”
1. Blood flow to tissues
2. Ability of a drug to exit the vascular system
3. Ability of a drug to enter the cells
What factors affect metabolism?
,What is the difference between Phase I and Phase II metabolism?
• Goal is to increase water solubility of medications.
• Phase I metabolism
o oxidation (via cytochrome P450), reduction, and hydrolysis reactions
o phase I reactions convert a parent drug to more polar (water soluble) active metabolites by unmasking or inserting a polar
functional group (-OH, -SH, -NH2)
o geriatric patients have decreased phase I metabolism
drugs metabolized via phase I reactions have longer half-lives
geriatric patients metabolism drugs by phase II reactions
• Phase II metabolism
o glucuronidation, acetylation, and sulfation reactions
o "conjugation reactions" that increase water solubility of drug with a polar moiety
glucuronate, acetate, and sulfate, respectively
phase II reactions convert a parent drug to more polar (water soluble) inactive metabolites by conjugation of
subgroups to -OH, -SH, -NH2 functional groups on drug
drugs metabolized via phase II reactions are renally excreted (increased water = to the kidneys)
patients deficient in acetylation capacity (slow acetylators) may have prolonged or toxic responses to normal doses of
certain drugs because of decreased rates of metabolism
• Phase I – Phase I reactions usually convert the parent drug to a more polar metabolite by introducing or unmasking a
functional group (–OH, –NH2, –SH). Three subcategories are oxidation, reduction or hydrolysis. These type of reactions serve
to convert lipophilic drugs into more polar molecules. Often these metabolites are inactive, although in some instances, activity
is only modified or even enhanced. If phase I metabolites are sufficiently polar, they may be readily excreted. However, many
phase I products are not eliminated rapidly and undergo a subsequent reaction in which an endogenous substrate such as
glucuronic acid, sulfuric acid, acetic acid, or an amino acid combines with the newly incorporated functional group to form a
highly polar conjugate.
• Phase II – Such conjugation or synthetic reactions (secondary reactions from Phase I that form highly polar substances) are the
hallmarks of phase II metabolism.
What are the basic parameters of clearance pharmacokinetics?
How does pharmacokinetics impact therapeutic dosing?
Pharmacokinetic processes determine how much drug will be at its sites of action at any given time. In most cases the time course
of drug action bears a direct relationship to the concentration of a drug in the blood. Monitoring plasma drug levels is important
to measure drug responses. Single dose time course shows how plasma drug levels change over time after a single dose of an oral
medication. Important to stay within therapeutic range. Drug half-life means the time required for the amount of drug in the body
to decrease by 50%.
What are mechanisms of drug toxicity?
Altered pharmacokinetic process, namely hepatic enzyme activity.
Decreased renal excretion
, First ingredient is the _____ ingredient. - active.
(ingredients after that are either less potent, less active, and/or less amount)
Inactive constituents are made up of _____, _____ and _____ & _____. - fillers, vehicles, flavoring, & dyes (makes the drug
edible)
Fillers are used to make the pill _____ - larger (larger pills can sometimes be easier for pts to swallow and easier to handle)
Vehicles are the _____ to get the drug into the system – solvents (make the drug digestible/break down, so pt's body can
use/absorb)
teratogen - a substance that causes malformation of an embryo. (birth defects)
_____ is a well known teratogen that used to be used to treat _____. It caused _____. – Thalidomide, morning sickness in
expectant mothers, limb defects
The _____ came up with the schedules for controlled substances/drugs. Schedule I is the _____ addictive and Schedule V is the
_____ addictive. - Controlled Substance Act of 1970, most, least
Know Schedule for each drug that we need to memorize, esp if "surprising" info. (eg. a drug that is very addictive but only SIII) -
Study Schedules for drugs if listed on Drug Table!
Gold standard for drug development? - randomized controlled trial
Know the general process of drug approval* very basic overview "where the drug goes in each stage of development" - Phase 1 -
Humans (a few healthy humans) testing starts (before that is animal testing)
Phase 2 - 100s humans with the disease
Phase 3 - 1000s humans
If a drug is a Pregnancy Category X, it has a _____ of _____. - high risk, fetal abnormality (risk outweighs the benefit. most
teratogens)
The 3 most important properties of an ideal drug are _____, _____ and _____. – effectiveness, safety (risk vs benefit), selectivity
- doing what it's exactly supposed to do (fever med - lower fever)
ADOPIE - Nursing Process, Assessment, Diagnosis, Outcomes, Planning, Implementation, Evaluation
Pharmacodynamics cover _____ and _____ - how a drug works physiologically, what it does to or for the body
Antagonist vs Agonist. An antagonist _____ - Antagonist prevents the agonist from binding with the receptor or inactivates the
receptor
Competitive - competes with agonist for receptor sites, is reversible/not permanent
Noncompetitive - A(n) _____ inhibitor binds to a site on the enzyme that is not the active site (different site/inactivated site)
irreversible
Affinity is how well a drug can _____. – bind, (either can or cannot bind)
Efficacy is _____. - the relationship between receptor and ability to initiate a response, (eg. competitive relationship - affinity, but
no efficacy)
contraindication - any reason that you shouldn't give someone a drug, allergy, category X drug to a pregnant woman, side effects -
expected (or not surprising) effects, any effects of a medication other than the desired ones, adverse effects - not expected effects
(and should stop taking drug)
A general term for any undesirable effects that are a direct response to one or more drugs.
Drug Allergy Type 1 - IgE antibodies, anaphylactic (throat closing/difficulty breathing)
