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Pharmacology > Exam 1: PharmacoDynamics > Flashcards

Exam 1: PharmacoDynamics Flashcards

1
Q

_________ 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

A

PharmacoDynamics

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2
Q

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

A

SAME….BLOCK

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3
Q

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

A

cellular

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4
Q

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

A

enzymes….glycoproteins..nucleic acids

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5
Q

A single cell may have _______ of receptor sites.

A

Hundreds

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6
Q

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

A

Hydrogen…ionic

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7
Q

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

A

chemical structure

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8
Q

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

A

multiple sites

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9
Q

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.

A

conformational

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10
Q

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”.

A

tertiary…“induced fit”

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11
Q

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

A

“lock and key”

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12
Q

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

A

part

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13
Q

Proteins that ______ the cell membrane act as drug receptors.

A

SPAN

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14
Q

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

A

ligand

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15
Q

What are the 4 possible types of ligands?

A
  1. hormones 2. neurotransmitters 3.growth factors 4.drug molecules
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16
Q

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.

A

conformational change

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17
Q

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

A

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

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18
Q

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

A

excitable

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19
Q

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

A

receptor

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20
Q

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

A

ligand-gated….voltage-gated

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21
Q

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

A

OPEN

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22
Q

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

A

sodium & potassium..depolarization…firing

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23
Q

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

A

second

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24
Q

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

A

organ…interesting!

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25
Q

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

A

hormone…neurotransmitter

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26
Q

What are 2 examples of receptors that generate second messengers?

A

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

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27
Q

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

A

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

28
Q

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

A

cyclic AMP (cAMP)

29
Q

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

A

phosphorylation of proteins

30
Q

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

A

ionic

31
Q

Where are tyrosine kinase receptors are located?

A

on the plasma membrane

32
Q

_______ receptors are CRITICAL to cell growth and differentiation.

A

Tyrosine Kinase

33
Q

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

A

growth…oncogenes

34
Q

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

A

Steroid

35
Q

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

A

RNA polymerase

36
Q

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

A

GENE EXPRESSION!!!

37
Q

Receptor Specificity!! A drug will have a higher _____ for a

particular type of receptor.

A

affinity

38
Q

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

A

agonist

39
Q

_______ drugs produce similar effects as endogenous chemicals.

A

Agonist

40
Q

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

A

think “LIGANDS”!!

41
Q

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

A

ANT-agoinist

42
Q

An _______ drug produces NO EFFECT!

A

antagonist

43
Q

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

A

inhibiting

44
Q

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

A

Antagonist

45
Q

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

A

antagonist

46
Q

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

A

reversible

47
Q

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

A

agonist….antagonist…agonist

48
Q

A good example of a noncompetitive antagonist is ______!

A

POISON!

49
Q

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

A

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

50
Q

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)

A

antagoinist…Na

51
Q

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

A

Physiologic

52
Q

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

A

independently on 2 (less desirable in medicine)

53
Q

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

A

quantified

54
Q

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

A

Drug Dose and Effect

55
Q

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

A

Potency…think “dose”

56
Q

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

A

Efficacy….effect…occupancy

57
Q

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).

A

ceiling

58
Q

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

A

potency and efficacy

59
Q

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

A

efficacy…potency

60
Q

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

A

Therapeutic Window

61
Q

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.

A

SMALL

62
Q

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

A

Toxic..effective…TD50 / ED50

63
Q

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)

A

therapeutic index

64
Q

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

A

therapeutic index

65
Q

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

A

monitoring

Pharmacology (23 decks)

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