EXAM2 Flashcards by Renee W

Science of interactions of chemical compounds with biological systems

Pharmacology

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The study of the biochemical and physiological effects of drugs and the mechanisms of their actions, including the correlation of their actions and effects with their chemical structure

Pharmacodynamics

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The study of the absorption, distribution, biotransformation, and elimination of xenobiotics

Pharmacokinetics

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Which of the following statements are true:
Pharmacodynamics are a subset of pharmacokinetics
OR
Pharmacokinetics are a subset of pharmacodynamics?

FIRST: Pharmacodynamics are a subset of pharmacokinetics

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What is the “cornerstone of pharmacology” that explains how the organism interacts with a drug and initiates a chain of biochemical events which results in observed effects?

drug receptor

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Drug whose interaction with the receptor stimulates a biological response

agonist

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Orthosteric or Allosteric:
agonist, antagonist, partial agonist, and inverse agonists

Orthosteric

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Orthosteric or Allosteric:
Site where the native ligand binds

Orthosteric

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PAM is an allosteric _____, while NAME is an allosteric _____

activator, inhibitor

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What are the receptor and drug reactions to full, partial, antagonist, and inverse agonist?

Full: R active, D active
Partial: R active, D partial
Antagonist: R both, D both
Inverse agonist: R inactive, D inactive

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Orthosteric or Allosteric:
Positive (PAM) and Negative (NAM)

Allosteric

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What happens when a drug binds to SERT?

Blocking leads to more serotonin in the synapse (SSRIs)

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What happens to serotonin with an MAOI?

Increased serotonin

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How many serotonin receptors in the body?

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What inhibitor breaks down serotonin in the synapse, where in its absence serotonin increases?

MAO

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Why is Buprenorphine affective for drug addiction?

Stays on drug’s receptor longer, decreasing effect of drug from binding sites

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True or False: Drugs only modify cellular function

TRUE

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True or False: Drugs have a single effect

FALSE

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Which site of drug action is used for the following:
-Neutralization of gastric acid by antacids
-cholestyramine resin being used to reduce cholesterol absorption

Extracellular

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Which site of drug action is used for the following:
-Drugs used to treat infections
-Drugs used for cancer chemotherapy
-Hormones such as estrogen

Intracellular site

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Which site of drug action is used for the following:
Many drugs:
-Acetylcholine and muscarinic or nicotinic receptors
-Catecholamines and alpha and beta receptors
-Growth factors (EGF/FGF) and GF receptors

Surface of the cell

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Most receptors are ______

Proteins

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Receptors determine the quantitative relationship between ____ or concentration of drug and pharmacologic _____

Receptors determine the quantitative relationship between dose or concentration of drug and pharmacologic effects

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Receptors are responsible for _______ of drug action

selectivity

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Drugs that bind to a receptor and stimulate a biological response

agonists

Drugs that bind to a receptor without altering receptor function

antagonists

_____ is one of the determinants of potency

Affinity

relationship between affinity and potency

direct

The ability of the drug to interact with the receptor

affinity

The way affinity is measured

Assessing signaling event associated with receptor activity

Functional assay

As doses increase, the incremental response ______

decreases

Which part of the concentration response curve measures efficacy?

Max Response

If EC50=20nM, what are the concentrations of EC90? EC10?

EC90= 200 nM EC10= 2 nM

What are the log values of EC10 and EC90 if EC50=10^-10?

EC10= 10^-11 EC90= 10^-9

What are the ways affinity is measured?

Ki and KD

Equation for Law of Mass Action and their receptor availability

[D][R]/[DR] or k(off)/k(on) =KD

What value determines association rate? What does it measure?

Ka- how fast a drug jumps onto receptor [k(on) [D][R] ]

What value determines dissociation rate? What does it measure?

Kd- how fast drug jumps off receptor [k(off) [DR] ]

Coming off a receptor slowly on a graph shows (higher/lower) affinity

higher

At what value of [D] is unoccupied [R]=occupied [DR]?

When D occupies half of the receptors

In the Law of Mass Action, binding is (reversible/irreversible), [D] and [R] are either ____ or ____, and receptor sites have (value) affinity and are (dependent/independent)

Binding is reversible, [D] and [R] are either free or bound, and receptor sites have equal affinity and are independent

How can KD be measured from Bmax?

Half of Bmax is KD

What is the measure for number of receptors in a system?

Bmax

How to find the Bmax given a saturation binding assay?

Total-Non Specific= Specific

How test (radioactive) ligand/drugs compete for same sight as labeled ligand

Heterologous competition assays

Can you find KD with IC50?

Yes: Cheng-Prusoff equation

What is the Cheng-Prusoff equation? (NEED TO MEMORIZE)!!

Ki=IC50/[1+L/KD]

What parameter is NOT required to calculate Ki from a drug/binding curve? A. KD of radioligand B. Bmax value C. IC50 value of test compound D. Concentration of radioligand [L]

B. Bmax Reason: not in Cheng-Prusoff equation

What is the correlation on a drug/concentration plot between affinity and IC50 value?

Inverse: High affinity=low IC50 value

How do we find the most DOR/MOR/KOR selectivity? Least selective?

Most: highest selectivity ratio Least: least/closest selectivity ratio

Which of the following is NOT true? A. Pharmacology is the science of interactions of chemical compounds with biological systems B. The drug receptor is the cornerstone of pharmacology C. Drugs are defined by action (e.g. agonist or antagonist) D. Antibodies are in increasing use as drugs E. Pharmacodynamics is the study of the absorption, distribution, biotransformation, and elimination or xenobiotics

E. Pharmacokinetics definition!

Which of the following is NOT true? A. Most drugs have a single effect B. Agonist and antagonists have overlapping binding sites C. Allosteric modulators can have both positive and negative effects on agonists

Which of the following statements regarding Bmax is not true? A. Bmax is an estimated of number of receptors in a given tissue B. Bmax values are determined through saturation binding studies C. Bmax values are not regulated by drug treatment D. Bmax values are independent of the ligand E. Bmax can influence downstream signaling events

C. Bmax values are not regulated by drug treatment

Partial agonist are also ____ ______

partial antagonist

Causes response that is greater than the endogenous ligand

super agonist

On the ligand spectrum, drives response in opposite direction

partial inverse agonist

The dose of a drug required to produce a particular effect of given intensity

potency

On a graph, where is the most potency? The most efficacy?

Most potency is furthest left, most efficacious is highest

On a graph, where is the most potency? The most efficacy?

Most potency is furthest left, most efficacious is highest

The biological response resulting from the drug-receptor interaction

efficacy

A strong agonist has (low/high) affinity and (low/high) efficacy

high affinity and high efficacy

Which drug property is more important: efficacy or potency?

Efficacy

Identify constitutive and endogenous activity

Constitutive: absent Endogenous: absent

Identify constitutive and endogenous activity

Constitutive: present Endogenous: absent

Identify constitutive and endogenous activity

Constitutive: absent Endogenous: present

Identify constitutive and endogenous activity

Constitutive: present Endogenous: present

What are the three types of receptor antagonism?

Competitive, non-competitive, and irreversible

Reversible or equilibrium antagonism by increasing the dose of agonist

competitive antagonism

Competitive antagonist has _____ but lacks _____

has affinity, lacks efficacy

Plot determining affinity of agonist to a receptor through functional analysis of competitive antagonist

Schild Plot

Which assay shows specific binding %

receptor-binding assay

Which assay shows maximal release %?

Functional assay

Type of antagonist that cannot be completely reversed by increasing the concentration of agonist; produces its effect at a site of the receptor other than the site used by the agonist

Noncompetitive Antagonist

Increasing antagonist concentrations ____ the KD and ________ Emax of the agonist

increase, decrease

What happens to the curve of a competitive antagonist vs an irreversible antagonist

non-competitive shifts down on graph

Spare receptors result in EC50 being (equal, less, or greater) than KD?

EC50

When two drugs influence a physiological system but in opposite directions.

Functional (physiological) antagonism

Which of the following is NOT true regarding spare receptors? A. It is system/tissue dependent B. Allow a noncompetitive antagonist to look like a competitive antagonist C. Spare receptors are independent of effector numbers D. May differ between signaling pathways with the same receptor

C. Spare receptors are independent of effector numbers

Which of the following is NOT true regarding antagonists? A. Irreversible and allosteric antagonists have similar effects on the dose response curves of agonists B. In the absence of space receptors, a noncompetitive antagonist increases the Emax C. Irreversible antagonists typically bind the Orthosteric site D. Antagonist affinity can be estimated using a Schild plot

B. In the absence of space receptors, a noncompetitive antagonist increases the Emax

Chemical reaction occurring between an agonist and an antagonist to form an inactive product

chemical antagonism