HS503
HS301 Clinical Pharmacology
Specific Course Learning Objectives
Introduction to Pharmacology (quizlet #1) https://quizlet.com/_63fyri
1. List the most important properties of an ideal drug
a. Effectiveness
b. Safety
c. Selectivity
2. Discuss the landmark drug legislation as far as drug purity, safety, and effectiveness
a. Pure Food and Drug Act of 1906
i. Tells what was in the drug but did not say if it was useful
ii. Set standards for drug quality and PURITY
b. Federal Food, Drug, and Cosmetic Act of 1938
i. Regulated drug SAFETY and development of the FDA
ii. Made this law so people would know that their drugs were safe
c. Kefauver-Harris Amendment of 1962
i. Increased the safety requirements to prove that the drugs were safe and
PROVEN to be EFFECTIVE (babies born with birth defects).
d. Controlled Substance Act (1970)
i. Established rules concerning drugs that have potential for abuse
3. List the three types of drug names (I will use Tylenol)
a. Chemical Name: indicates the chemical make of the drug
i. N-acetyl-p-animo-phenol
b. Generic Name: Derived from the chemical name
i. Acetaminophen
c. Brand or Trade Name: name created by the manufacturer
i. Tylenol
4. List and define the FDA Pregnancy Categories
a. A
i. Human studies show no fetal risk
b. B
i. Animal studies show no fetal risk
c. C
i. Limbo area, either animal studies do show fetal effects or no studies exist. Drugs
should only be given if potential benefits justify potential risks
d. D
i. Evidence of human fetal harm exists
e. X
i. Contraindicated! Risk to fetus clearly outweighs any possible benefit
5. Define therapeutic class, mechanism of action, indication, and contraindication.
a. Therapeutic Class
i. A way to categorize the drug. Usually based on either its chemical structure, its
mechanism of action, or generally just what is does
b. Mechanism of Action
i. How does it work? What does it do?
c. Indication
i. What is it used for? What does it treat?
d. Contraindication
i. Who should not use the product? Allergy precautions/warnings
,Principles of Pharmacokinetics & Pharmacodynamic
1. Define and apply concepts of potency, efficacy, affinity, selectivity, protein binding, first-pass
metabolism, prodrug, chelation, enzyme induction, and enzyme inhibition, onset of action, duration
of action.
a. Potency
i. Measure of the amount of drug (dose.mg) required to produce a given degree of
effect
b. Efficacy
i. The ability of a drug to produce a desired therapeutic effect
c. Potency Vs. Efficacy
i. Potency is rarely of clinical importance
d. Affinity
i. Measure of the strength of attraction between a drug and its receptor
e. Selectivity
i. Refers to the degree to which drugs act upon one site relative to all possible sites
f. Protein Binding
i. Some drugs are bound to plasma proteins, mostly albumin. Drugs bound to these
proteins are pharmacologically inactive while bound
g. First-Pass
i. Drugs absorbed in the small intestine are first exposed to the liver and may be
extensively metabolized before reaching systemic circulation
h. Metabolism
i. Chemical alteration of the parent compound usually resulting in enhanced excretion,
inactivation, or sometimes active metabolites
1. First pass metabolism: Drugs absorbed in the small intestine are first
exposed to the liver and may be extensively metabolized before reaching
systemic circulation
i. Prodrug
i. Inactive compound that must be metabolized in order to become active
j. Chelation
i. Chemical bonding that prevents absorption
k. Enzyme Induction
i. Metabolism = lower drug level = loss of efficacy
ii. Caused by one drug inducing (speeding up) the shared metabolic pathway
l. Enzyme Inhibition
i. Metabolism = higher level = increased effects, adverse reaction, and toxicity
ii. Caused by competition for the same metabolic pathway
m. Onset of action
i. The amount of time it takes to reach the minimum effective concentration
n. Duration of action
i. Length of time a drug can be expected to exhibit its pharmacological effects
2. Define and apply concepts of ADME (absorption, distribution, metabolism, and excretion), half-
life, bioavailability, and therapeutic window.
a. Absorption
i. Movement of drug from its site of administration into the systemic circulation
b. Distribution
i. Movement of the drug into the various body fluids and tissues
, ii. Volume of distribution: Mathematical concept describing the amount of drug in the
body in relation to the concentration in the plasma
c. Metabolism
i. Chemical alteration of the parent compound usually resulting in enhanced excretion,
inactivation, or sometimes active metabolites
d. Excretion
i. Process by which the drug is eliminated from the body
ii. Some drugs are excreted after metabolism
iii. Some drugs are excreted “unchanged”
e. Half-life
i. Time required for the drug’s plasma concentration to be reduced by one-half
ii. T1/2 does not depend on dose
1. Specifically refers to plasma concentrations only, while duration of effect
refers to the pharmacological action
f. Bioavailability
i. Fraction (%) of drug available in bloodstream after administration as compared to
the IV route
ii. IV route is 100% bioavailable
g. Therapeutic window
i. Minimal effective concentration: Levels lower than the minimum effective
concentration will not be affective
ii. Toxic concentration: levels near this dose may cause dramatic, unusual adverse
effects, even death
iii. Therapeutic index: is a measure of the drug’s safety. The relationship between
beneficial and adverse effects of medication
3. Discuss various patient specific variables that may influence ADME.
a.
4. Describe the blood brain barrier.
a. A filtering mechanism of the capillaries that carry blood to the brain and spinal cord tissue,
blocking the passage of certain substances
b. Only lipid soluble drugs can cross the BBB and reach the CNS
5. Discuss how various routes of administration may differ in bioavailability.
a. IV route is 100% bioavailability
b. IM and SC 100% bioavailability
c. Explains why some drugs are not effective if given by different routes
d. Sometimes normal IV doses are the same as the oral dose, but sometime they differ
6. Distinguish between an allergy and an intolerance or side effect.
a. Intolerance vs. Allergy
i. Side effect of a drug that limits its usefulness or acceptance in a patient
ii. Immune system meditated response, unpredictable (Allergy)
7. Discuss the general mechanisms of drug interaction and strategies to avoid them.
a. Direct chemical interaction
i. (inactivation, precipitation)
b. Pharmacokinetic interactions
i.
c. Pharmacodynamic Interactions
i. Synergisitc Effects and Antagonisitc Effects
d. Combined Toxicity
8. Discuss the characteristics of high-risk patients and high-risk drugs.
, a. High risk drugs
i. Ate those with a narrow therapeutic index, high incidence of adverse effects, or high
incidence of allergic reactions
b. High risk patients
i. Are those that would be least likely to tolerate adverse effects or loss of efficacy
1. Very young, the elderly, brittle diabetics
HS301 Clinical Pharmacology
Specific Course Learning Objectives
Introduction to Pharmacology (quizlet #1) https://quizlet.com/_63fyri
1. List the most important properties of an ideal drug
a. Effectiveness
b. Safety
c. Selectivity
2. Discuss the landmark drug legislation as far as drug purity, safety, and effectiveness
a. Pure Food and Drug Act of 1906
i. Tells what was in the drug but did not say if it was useful
ii. Set standards for drug quality and PURITY
b. Federal Food, Drug, and Cosmetic Act of 1938
i. Regulated drug SAFETY and development of the FDA
ii. Made this law so people would know that their drugs were safe
c. Kefauver-Harris Amendment of 1962
i. Increased the safety requirements to prove that the drugs were safe and
PROVEN to be EFFECTIVE (babies born with birth defects).
d. Controlled Substance Act (1970)
i. Established rules concerning drugs that have potential for abuse
3. List the three types of drug names (I will use Tylenol)
a. Chemical Name: indicates the chemical make of the drug
i. N-acetyl-p-animo-phenol
b. Generic Name: Derived from the chemical name
i. Acetaminophen
c. Brand or Trade Name: name created by the manufacturer
i. Tylenol
4. List and define the FDA Pregnancy Categories
a. A
i. Human studies show no fetal risk
b. B
i. Animal studies show no fetal risk
c. C
i. Limbo area, either animal studies do show fetal effects or no studies exist. Drugs
should only be given if potential benefits justify potential risks
d. D
i. Evidence of human fetal harm exists
e. X
i. Contraindicated! Risk to fetus clearly outweighs any possible benefit
5. Define therapeutic class, mechanism of action, indication, and contraindication.
a. Therapeutic Class
i. A way to categorize the drug. Usually based on either its chemical structure, its
mechanism of action, or generally just what is does
b. Mechanism of Action
i. How does it work? What does it do?
c. Indication
i. What is it used for? What does it treat?
d. Contraindication
i. Who should not use the product? Allergy precautions/warnings
,Principles of Pharmacokinetics & Pharmacodynamic
1. Define and apply concepts of potency, efficacy, affinity, selectivity, protein binding, first-pass
metabolism, prodrug, chelation, enzyme induction, and enzyme inhibition, onset of action, duration
of action.
a. Potency
i. Measure of the amount of drug (dose.mg) required to produce a given degree of
effect
b. Efficacy
i. The ability of a drug to produce a desired therapeutic effect
c. Potency Vs. Efficacy
i. Potency is rarely of clinical importance
d. Affinity
i. Measure of the strength of attraction between a drug and its receptor
e. Selectivity
i. Refers to the degree to which drugs act upon one site relative to all possible sites
f. Protein Binding
i. Some drugs are bound to plasma proteins, mostly albumin. Drugs bound to these
proteins are pharmacologically inactive while bound
g. First-Pass
i. Drugs absorbed in the small intestine are first exposed to the liver and may be
extensively metabolized before reaching systemic circulation
h. Metabolism
i. Chemical alteration of the parent compound usually resulting in enhanced excretion,
inactivation, or sometimes active metabolites
1. First pass metabolism: Drugs absorbed in the small intestine are first
exposed to the liver and may be extensively metabolized before reaching
systemic circulation
i. Prodrug
i. Inactive compound that must be metabolized in order to become active
j. Chelation
i. Chemical bonding that prevents absorption
k. Enzyme Induction
i. Metabolism = lower drug level = loss of efficacy
ii. Caused by one drug inducing (speeding up) the shared metabolic pathway
l. Enzyme Inhibition
i. Metabolism = higher level = increased effects, adverse reaction, and toxicity
ii. Caused by competition for the same metabolic pathway
m. Onset of action
i. The amount of time it takes to reach the minimum effective concentration
n. Duration of action
i. Length of time a drug can be expected to exhibit its pharmacological effects
2. Define and apply concepts of ADME (absorption, distribution, metabolism, and excretion), half-
life, bioavailability, and therapeutic window.
a. Absorption
i. Movement of drug from its site of administration into the systemic circulation
b. Distribution
i. Movement of the drug into the various body fluids and tissues
, ii. Volume of distribution: Mathematical concept describing the amount of drug in the
body in relation to the concentration in the plasma
c. Metabolism
i. Chemical alteration of the parent compound usually resulting in enhanced excretion,
inactivation, or sometimes active metabolites
d. Excretion
i. Process by which the drug is eliminated from the body
ii. Some drugs are excreted after metabolism
iii. Some drugs are excreted “unchanged”
e. Half-life
i. Time required for the drug’s plasma concentration to be reduced by one-half
ii. T1/2 does not depend on dose
1. Specifically refers to plasma concentrations only, while duration of effect
refers to the pharmacological action
f. Bioavailability
i. Fraction (%) of drug available in bloodstream after administration as compared to
the IV route
ii. IV route is 100% bioavailable
g. Therapeutic window
i. Minimal effective concentration: Levels lower than the minimum effective
concentration will not be affective
ii. Toxic concentration: levels near this dose may cause dramatic, unusual adverse
effects, even death
iii. Therapeutic index: is a measure of the drug’s safety. The relationship between
beneficial and adverse effects of medication
3. Discuss various patient specific variables that may influence ADME.
a.
4. Describe the blood brain barrier.
a. A filtering mechanism of the capillaries that carry blood to the brain and spinal cord tissue,
blocking the passage of certain substances
b. Only lipid soluble drugs can cross the BBB and reach the CNS
5. Discuss how various routes of administration may differ in bioavailability.
a. IV route is 100% bioavailability
b. IM and SC 100% bioavailability
c. Explains why some drugs are not effective if given by different routes
d. Sometimes normal IV doses are the same as the oral dose, but sometime they differ
6. Distinguish between an allergy and an intolerance or side effect.
a. Intolerance vs. Allergy
i. Side effect of a drug that limits its usefulness or acceptance in a patient
ii. Immune system meditated response, unpredictable (Allergy)
7. Discuss the general mechanisms of drug interaction and strategies to avoid them.
a. Direct chemical interaction
i. (inactivation, precipitation)
b. Pharmacokinetic interactions
i.
c. Pharmacodynamic Interactions
i. Synergisitc Effects and Antagonisitc Effects
d. Combined Toxicity
8. Discuss the characteristics of high-risk patients and high-risk drugs.
, a. High risk drugs
i. Ate those with a narrow therapeutic index, high incidence of adverse effects, or high
incidence of allergic reactions
b. High risk patients
i. Are those that would be least likely to tolerate adverse effects or loss of efficacy
1. Very young, the elderly, brittle diabetics
