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Pharmacology - Exam 1 > Unit 3 > Flashcards

Unit 3 Flashcards

1
Q

Theories of Drug Action

A

Drugs DO increase/diminish normal fx of tissues or organs

Drugs DO NOT cause diff fx to occur

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2
Q

structurally specific drug

A

work by receptor theory

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3
Q

structurally non-specific drugs

A

work by simple physical or chemical action

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4
Q

receptor theory

A

drug fits the shape of the active site of the receptor

complex is formed which causes altered cell activity

key…lock…complex

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5
Q

receptor

A

macromolecule w/ which a drug interacts to produce a response

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6
Q

drug-receptor complex causes…

A
  • transport of ions or molecules
  • enzyme activation or deactivation
  • protein synthesis
  • release of hormones/transmitter
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7
Q

receptors located?

A
  • cell membrane
  • cell components (DNA, enzymes)
  • for most drugs, we don’t actually know
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8
Q

stimulate or inhibit normal receptor activity?

A

BOTH…depends on drug

  • stimulate- agonists
  • inhibit- antagonists
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9
Q

agonist

A

compound which increases or intensifies activity of a receptor

-stimulator

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10
Q

antagonist

A

compound which decreases the activity of the receptor or prevents an agonist from acting on a receptor

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11
Q

competitive antagonist

A

binds to the same site on a receptor as an agonist

effects are reversible by competition w/ agonist

advantage - can use agonist and competitive antagonist to control exact degree of response

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12
Q

noncompetitive antagonist (allosteric)

A

bind to a DIFF part of a receptor than agonist but still prevents normal agonist action.

cannot be displaced by competition from agonist

advantage - can block an effect no matter what the concentration of agonist

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13
Q

partial agonist

A

compound which increases activity of a receptor

less effective than other agonists

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14
Q

structurally nonspecific drugs

A

drug actions NOT mediated by receptors

examples:
antacids
emollients
some laxatives
complexes to remove ions or copounds
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15
Q

membrane structure

A

“3 layers” lipid bilayer w/ small amounts of protein floating in it and on either side

  • lipids pass thru main membrane
  • pores for small water soluble substances
  • complexes for carrier mediated transport
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16
Q

what most influences drug passage thru membrane proper?

A

lipid solubility

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17
Q

drug passage thru pores is influenced by?

A

size and shape of the molecule

degree of ionization

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18
Q

degree of ionization

A

influence by pH

acids (barbiturates)
> ionized, low enviro pH
ionized, high enviro pH

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19
Q

Acid in Acid

Base in Base

A

in SIMILAR environments drugs are LESS ionized

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20
Q

Acide in Base

Base in Acid

A

in OPPOSITE environments drugs are MORE ionized

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21
Q

which form of drug moves thru membranes more readability?

A

not ionized

ionized particles are “trapped” by membranes

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22
Q

ionization influences

A

reabsorption

ability to return to blood after entering milk

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23
Q

intensity of repose to a drug, depend on:

A

[drug] at active site

  • absorption
  • distribution
  • metabolism
  • excretion

ability of active site to respond

learn to treat each pt

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24
Q

absorption

A

transfer of drug molecules from place deposited to circulating fluids

  • route of admin (oral, subQ, intramuscular, IV)
  • local conditions at site of admin (circa, pH, food)
  • chem properties of drug
  • form of medication
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25
Q

distribution

A
  • relative perfusion and permeability of area

- binding to non-receptor sites like plasma proteins

26
Q

blood brain barrier (distribution)

A

glial cells plus capillary pores

pores themselves are smaller

interstitial space minimal - packed glial cells

27
Q

placental barrier (distribution)

A

almost no barrier at all

  • low perfusion
  • some proteins and viruses cross
  • lipid soluble drugs pass readily
28
Q

binding to non-receptor sites like plasma proteins

A
  • can affect onset, intensity, and duration
  • usually weak binding so effect not severe
  • sometimes uses priming dose then smaller maintenance
29
Q

other storage sites (fat, muscle, liver, kidneys, bone)

distribution

A

often requires more drug

may redistribute to and from storage

30
Q

body weight (distribution)

A

dose per Kg body weight

31
Q

sex (distribution)

A

related to both size and fat distribution

32
Q

metabolism (biotransformation)

A

chemical alterations of a drug by the body

  • usually liver
  • usually changed to less active chem
  • more ionized so more readily eliminated
33
Q

Cytochrome P450 System

A

most common group of enzymes found in liver microsomal fraction (aka CYP)

  • inducible
  • inhibition
  • FDA suggests in vitro testing to predict interactions
34
Q

special pt considerations (metabolism)

A

pathology
age
genetic
drug exposure

35
Q

excretion

A

drug elimination from the body

  • routes
  • excretion RATE important - avoid cumulative effects
36
Q

routes (excretion)

A 
kidneys
liver - bile to feces
sweat glands
saliva
lungs
mothers milk
37
Q

kidney (nephron) rate depends upon:

A

filtration

  • circulation - GFR
  • [drug] not bound by plasma protein

secretion

  • drug characteristics
  • active transport (infants and elderly)

reabsorption

  • fat VS water soluble
  • size and shape of water soluble molecules
  • pH and ionization
38
Q

clearance = ml/min or L/hr

calculated volume

A

volume of fluid that would be completely cleared of a drug in a min if all we removed from that volume and non was removed from remaining fluid in body

39
Q

physiologists and clinicians refers to “renal” clearance

A

to est individual pt renal fx (test creatinine clearance)

40
Q

research pharmacologist refers to “total” drug clearance

A

includes metabolism and excretion by all routes

incorporated into the concept of a drug’s effective 1/2 life in the body

41
Q

intensity of response to given dose of a drug

A

-concentration at active site (pharmacokinetics)

ability of active site to respond

  • receptor number may change
  • internal responses may change
42
Q

individual pt differences

A
  • age (enzymes, blood brain barrier)
  • weight (surface area)
  • sex (body comp, pregnancy, nursing)

environment

  • physical (temp, attitude)
  • psychosocial (sensory distraction, placebo, compliance)
43
Q

Genetic (pt differences)

A
  • metabolism - deficiencies or excesses in enzymes

- receptors - insulin receptors defective in some type II diabetics

44
Q

Assess pre-drug status of the individual - baseline state

A

monitor effectiveness and toxicities

45
Q

adverse responses to drugs

A

those specific to drug

  • blood abnormalities
  • liver or kidney damage
  • teratogenic effects
  • dermatologic effects

drug idiosyncrasy
- non-allergic abnormal response

drug allergy
- response to histamine (local? systemic?)

46
Q

drug interactions due to simultaneous admin of 2+ Rx

A

may INCREASE therapeutic or toxic effect

  • additive
  • synergistic
  • potentiation

may DECREASE therapeutic or toxic effect
-antagonism

47
Q

alter pharmacodynamics (mechanism of drug interactions)

A
  • binding to receptor site modified (other antagonists or agonists)
  • increase or decrease rate of difference portions of pathway
48
Q

alter pharmacokinetics

A
  • absorption (antacids in GI, vasoconstriction, physical incompatibility at site of admin)
  • distribution (competition for plasma proteins or other storage)
  • metabolism (stimulate or depress liver enzymes, binding to plasma protein)
  • excretion (diuretics)
49
Q

competition for plasma proteins

A

given - drug A is bound to plasma protein in same position that drug B binds

what will happen when B is added:

  • if B binds more tightly than A? receptor receives drug A not drug B
  • if A binds more tightly than B? receptor gets more of B than expected, will not be as much need for a priming dose
50
Q

An alkaline drug is ______ ionized in a acidic enviroment.

A

more

51
Q

Administration of an antacid can directly alter the way a second orally administered drug is:

A

absorbed only

52
Q

A drug is most likely to pass through a membrane is it is:

A

lipid soluble

53
Q

What is a teratongenic drug?…It is a drug that:

A

causes birth defects in fetuses.

54
Q

What type of compound binds a receptor and “turns it on”.

A

agonist

55
Q

If a drug is highly plasma protein bound, what kind of effect can you expect to see in regards to free drug available to interact with drug receptors.

A

we would expect to have LESS free drug available to bind receptors.

56
Q

Which of the following terms describes a compound which increases or intensifies the activity of a receptor but is less effective than other active compounds? This compound can, therefore, decrease the effectiveness of more active compounds when in competition with them for the same receptor sites.

A

partial agonist

57
Q

Certain chemical cause the liver to make more drug metabolizing enzymes. What is this process referred to as?

A

induction

58
Q

What type of compound has effects that are reversible especially in the presence of more agonist?

A

competitive antagonist

59
Q

A gaseous anesthetic dissolves in the respiratory membrane and it _______ dependent upon receptors to mediate its action.

A

is not

60
Q

Drug idiosyncracy

A

Non- allergic abnormal response - genetic?

61
Q

Drug allergy

A

Responses to histamine

Pharmacology - Exam 1 (3 decks)

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