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Flashcards in Pharmacodynamics Deck (14)
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1
Q

Basic Definition of Pharmacology and toxicology:

A

A. Pharmacology refers to the study of substances that interact with living systems through chemical processes
B. Toxicology is viewed as a branch of pharmacology with deals with adverse effects

2
Q

Two functions of a drug receptor:

A
  1. Recognition - the receptor binds a drug or endogenous ligand
  2. Transduction - transfer of information
3
Q

Describe Recognition, Selectivity, and Specificity of drug receptors.

A

A. The ability of a drug to bind with a receptor depends on the “goodness of fit” of drug to the receptor. This requirement for the receptor to recognize and bind a drug provides the basis for selective action at one or a small number of receptor sub-types.

B. The hundreds of different receptors types and their unique tissue localization impart specificity of drug action; that is, the ability of a drug to exert a distinctive influence on the body.

C. Proteins, which include enzymes, transporters, ion channels, structural proteins, and regulatory proteins, represent the majority of drug receptors.

4
Q

What is transduction by cell receptors?

A

The interaction of a drug with its receptor propagates a signal, i.e. it converts the “drug signal” into a tissue response.

5
Q

What are four common drug receptor mechanisms?

A
  1. G protein coupled receptors (GPCRs)
    • most common; regulate 2nd messengers like cAMP, IP3, ect.
  2. Modulate ligand-gated ion channels (both cationic & anionic)
  3. Intrinsic enzyme activity phosphorylates diverse effector proteins
  4. Regulation of gene transcription
6
Q

Two potential attributes of receptor mediated processes that can lead to durg-drug interactions:

A
  1. organization into opposing systems

2. Many receptors utilize a pool of relatively few 2nd messengers

7
Q

What is the general idea of the Occupancy Theory?

A

drug + receptor drug receptor complex –> effect

or

X + R RX, where the forward association constant is k1 and the reverse reaction dissociation constant is k2

8
Q

Define Potency.

A

a comparative term used to describe the relative positions of several agonist dose-response curves

the curve to the left (lower dose to cause effects) is more potent, it does NOT mean it has a higher maximum effect

9
Q

a drug capable of inducing a maximum response, it has full efficacy (α = 1) is called:

A

full agonist

10
Q

a drug whose maximal response is only a fraction of the maximum that can be elicited, it has partial efficacy (1 > α > 0)

A

partial agonist

11
Q

a drug which inhibits the action of an agonist is an:

A

antagonist

A “pure” antagonist is a drug that can bind to a receptor, i.e. it has affinity for the receptor, but induces no response, i.e. it has zero efficacy (α = 0).

12
Q

In the presence of a competitive antagonist, the agonist dose-response curve shifts to the_________. The slope of the curve________.

A

right, does not change

13
Q

In the presence of a noncompetitive antagonist the maximal response of an agonist is______, and the slope of the curve is________.

A

reduced, reduced

14
Q

An Inverse agonist is a drug that preferentially binds to the _______ form shifting equilibrium to the ________ form. This results in an effect _______ of that produced by an agonist.

A

inactive, inactive, opposite