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GMS 6504 Exam 1 Questions And Correct Answers
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GMS 6504 Exam 1 Questions And Correct AnswersPharmacology
the study of how chemical substances interact and modulate living systems
Pharmacokinetics
what the body does to the drug
Pharmacodynamics
what the drug does to the body
Pharmacogenetics
how genetics determines response to the drug
Pharmacotherapeutics
medicinal use of drugs
Toxicology
side effects, negative outcomes
Receptor
protein that drug or ligand binds to
Types include ion channels, enzymes, nuclear receptors, DNA
Primary structure
Sequence of amino acid residues
secondary structure
repeating 3-D units such as a-helices and B-sheets
tertiary structure
single folded and arranged polypeptide chain, the structure of which is determined by the
amino acids
quaternary structure
arrangement of separate chains
,ex. hemoglobin
Pharmacological Test Systems
Animal Receptors (animal tissues)
Human Receptors (surrogate cells)
Human Receptors (human target cells)
Human Receptors (Human target cells under influence of pathology)
System Independent Parameters
Affinity and Efficacy
Affinity
How likely a drug will bind to receptor and how strongly
thermokinetic propensity of drug to bind to receptor
based largely on delta G
Efficacy
Magnitude of change of receptor shape/function upon drug binding
based on atom/atom interactions
System Dependent Parameters
Number of receptors
cellular machinery
presence of other drugs (competitive, noncompetitive)
Occupancy Theory
Response is proportional to fraction of receptors that are occupied
i.e. 100% response is obtained when all receptors have ligand
Langmuir Equation
DR/Rt=r=D/D+Kd
D= drug concentration (molarity)
Rt= total # of receptors
DR= drug receptor complex
, r=occupancy (r=1=100% occupancy)
Calculates the fraction of receptors that have drug bound to them
Occupancy vs response
A + R ----> AR --> Response (effect)
Sigmoid curve
Kd=EC50 (concentration that gives 50% maximal response)
Is occupancy and response a 1:1 relationship?
No
intrinsic activity (efficacy)
ability of a drug to activate a receptor upon binding
a=intrinsic activity
multiplication factor describing ability of agonist to produce a stimulus
E=a(r)
if a=1 what type of agonist?
0<a<1?
a=0?
Full
partial
antagonist
You add an agonist to a cell that has 10 receptors and get a response of 8. if you add the
same agonist to a cell that has 100 receptors, what will your response be?
8
80
impossible to tell
impossible to tell
What is used to describe between the agonist binding and what we measure?
Cellular stimulus-response cascade
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