Exam 1: PharmacoDynamics Flashcards Preview

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Flashcards in Exam 1: PharmacoDynamics Deck (65):
1

_________ is the study of the biochemical and physiologic actions of drugs, and their mechanisms of drug action at the cell level and sub-cell level...AKA-What the drug does to the body

PharmacoDynamics

2

Drugs do not impart NEW functions: they either: Produce the ____ action as the body’s own chemicals OR _____ the action of the body’s own chemicals

SAME....BLOCK

3

Action at _____ level is an interaction and binding of the drug to receptor macromolecules.

cellular

4

Receptors may be: metabolic or regulatory _______; proteins or ________ associated with transport mechanism; or structural and functional components of the cell membrane or _______.

enzymes....glycoproteins..nucleic acids

5

A single cell may have _______ of receptor sites.

Hundreds

6

______ binding and _____ binding are the most common methods for a drug to bind to a receptor.

Hydrogen...ionic

7

The AFFINITY of a drug for a particular receptor and the type of binding is intimately related to the drug’s _______.

chemical structure

8

In a typical drug interaction with a protein/glycoprotein receptor, Drug binding occurs at ______ (amino acid residues) on protein structure. (INTERESTING!)

multiple sites

9

In a typical drug interaction with a protein/glycoprotein receptor, binding to one or more amino acid residues causes a ________ change in the protein molecule.

conformational

10

In a typical drug interaction with a protein/glycoprotein receptor, this results in a modification of the _______ structure to bring other amino acid residues closer to the drug = called an “______ fit”.

tertiary..."induced fit"

11

Induced fit is also known as the "________" mechanism of binding.

"lock and key"

12

For drugs that bind within the cell: Receptor protein may be a structural or enzymatic component of the cell membrane = _____ of the cell membrane.

part

13

Proteins that ______ the cell membrane act as drug receptors.

SPAN

14

The term “______” refers to the molecules that bind to the receptor protein or receptor glycoprotein.

ligand

15

What are the 4 possible types of ligands?

1. hormones 2. neurotransmitters 3.growth factors 4.drug molecules

16

When a ligand binds to a SPECIFIC area of the receptor protein on the outer surface of the cell, or within the cell membrane, a ________ occurs in the receptor-protein molecule which is transmitted to the inner surface of the cell membrane.

conformational change

17

What are the 4 well known mechanisms by which receptors induce a response? you got this dawg

1.Ligand-Gated Ion Channels 2.G-Proteins 3.Intracellular Receptors 4.tyrosine kinase receptors

18

Ligand-gated ion channels are found in ______ tissues like nerves in the CNS, neuromuscular junctions, and autonomic ganglia.

excitable

19

For Ion Channel Receptors: The ligand binding occurs directly to ______ at channel site.

receptor

20

For Ion Channel Receptors: the receptors are located on ______-gated channels and ______-gated channels.

ligand-gated....voltage-gated

21

For Ion Channel Receptors: Binding causes the channel to ______, allowing for the influx of ions.

OPEN

22

For Ion Channel Receptors: KEY POINT--->Binding increases cell membrane permeability to ______ and _______ = determines ________ or hyperpolarization of nerve = affects nerve _____.

sodium & potassium..depolarization...firing

23

In signal transduction: ligand binding causes a series of events which generate a ______ messenger.

second

24

Second messengers pass the message from the inside of the cell to the effector ______ (target site of action)

organ...interesting!

25

Some _______ receptors and _________ receptors (e.g. in the autonomic nervous system) depend on G proteins to mediate their actions on cells

hormone...neurotransmitter

26

What are 2 examples of receptors that generate second messengers?

1.Muscarinic Cholinergic Receptors (ACh) 2.Adrenergic Receptors (epi/norepi)

27

What are the 3 effectors activated in a G-Protein pathway?

1.Adenylyl Cyclase 2.Phospholipase C 3.A membrane channel

28

If the effector is adenylyl cyclase: the cell’s response is the generation of ______ (____).

cyclic AMP (cAMP)

29

If the effector is phospholipase C: the cell's response is _______ of proteins.

phosphorylation of proteins

30

If the effector is a membrane channel: the cell's response is a change in ______ conductance.

ionic

31

Where are tyrosine kinase receptors are located?

on the plasma membrane

32

_______ receptors are CRITICAL to cell growth and differentiation.

Tyrosine Kinase

33

Tyrosine Kinase: A variety of ______ factors and certain _____ (regulate cancer growth) interact with these receptors.

growth...oncogenes

34

Intracellular receptors are proteins associated with the nuclear matrix that are activated by _______ hormones.

Steroid

35

The steroid-receptor complex ultimately increases binding of _____ ________ and the expression of regulated genes.

RNA polymerase

36

KEY FREGGIN POINT: steroid hormones interact in the cell nucleus to alter ________!!!

GENE EXPRESSION!!!

37

Receptor Specificity!! A drug will have a higher _____ for a
particular type of receptor.

affinity

38

An _______ drug is a drug that is able to bind to a receptor and produce an effect.

agonist

39

_______ drugs produce similar effects as endogenous chemicals.

Agonist

40

For agonists drugs, Neurotransmitters, hormones, etc. (think "_______”)

think "LIGANDS"!!

41

An _______ drug is a drug that binds to same receptor as an agonist, but is unable to activate the receptor.

ANT-agoinist

42

An _______ drug produces NO EFFECT!

antagonist

43

Antagonist drugs oppose the actions of an agonist by reducing or _______ the effect.

inhibiting

44

_______ drugs are also known as “blocker” drugs e.g. beta blockers, calcium channel blockers

Antagonist

45

When BOTH agonist AND antagonist compete for the same receptor site the ________ BINDS FIRST! (in either a competitive or noncompetitive manner)

antagonist

46

Is binding of the antagonist in competitive inhibition reversible or irreversible?

reversible

47

DONT WORRY! In our battle of agonist vs antagonist-- Administering additional ______ will displace the _______ from the receptor, allowing _____ to produce its effect.

agonist....antagonist...agonist

48

A good example of a noncompetitive antagonist is ______!

POISON!

49

Does a noncompetitive antagonist bind reversibly or irrecversibly? Where does a noncompetitive antagonist bind?

irreversibly (CANNOT BE DISPLACED)...binds to either active site or allosteric site

50

Our dental anesthetic is a great example of a chemical _______ because it blocks ____ channels which promote depolarization of nerves. (so depolarization does not occur=no pain)

antagoinist...Na

51

A _______ antagonist activates pathways that oppose the action of the agonist.

Physiologic

52

hmm interesting: In Physiologic antagonism: the agonist and antagonist act ________ on ___ different receptors!

independently on 2 (less desirable in medicine)

53

When a drug exerts an effect on a biologic system, the effect can be ______ according to the dose given.

quantified

54

The ______ and effect: The dose (how much) of the drug is compared against the intensity (magnitude) of the effect.

Drug Dose and Effect

55

_______ refers to the amount of drug necessary to produce the effect. (think "_____")...its related to the ______ of the drug to its receptor.

Potency...think "dose"

56

_______ is the degree of maximum intensity of the effect. (think "_____" of the drug"...its related to receptor _______ by drug molecules.

Efficacy....effect...occupancy

57

In drug efficacy: Additional doses produce no additional benefit: “______ dose” occurs when all receptors are occupied (intrinsic drug activity once a drug-receptor complex is formed).

ceiling

58

An example of _______ and ______: 300+ mg of aspirin for moderate pain, while 25mg of meperidine is used for moderate pain.

potency and efficacy

59

Example of Meperidine and Morphine: 100mg meperidine for severe pain, 10mg morphine for severe pain. They are SIMILAR in ______, but DIFFER in ______.

efficacy...potency

60

________: The range of the doses (concentrations) of a drug that elicits a therapeutic response, without unacceptable side effects (toxicity) in a population of people.

Therapeutic Window

61

Blood plasma levels of a drug with a ______ therapeutic window must be monitored closely to maintain effective dosing without exceeding the level that could produce toxicity.

SMALL

62

TD50: dose that causes _____ response in 50% of the population....ED50: does that is ______ in 50% of the population.... Theraputic Index= _____ / _____

Toxic..effective...TD50 / ED50

63

The ________ provides a single number that quantifies the relative margin of safety of a drug in a population of people (this is similar to the margin of safety which is done in animals)

therapeutic index

64

A large _______ represents a large (or “wide”) therapeutic window.

therapeutic index

65

A small TI represents a small (or “narrow”) therapeutic window = requires _______.

monitoring