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Pharmacology - Exam 1 > Unit 3 > Flashcards

Unit 3 Flashcards

(61 cards)

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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
distribution
- relative perfusion and permeability of area | - binding to non-receptor sites like plasma proteins
26
blood brain barrier (distribution)
glial cells plus capillary pores pores themselves are smaller interstitial space minimal - packed glial cells
27
placental barrier (distribution)
almost no barrier at all - low perfusion - some proteins and viruses cross - lipid soluble drugs pass readily
28
binding to non-receptor sites like plasma proteins
- can affect onset, intensity, and duration - usually weak binding so effect not severe - sometimes uses priming dose then smaller maintenance
29
other storage sites (fat, muscle, liver, kidneys, bone) | distribution
often requires more drug may redistribute to and from storage
30
body weight (distribution)
dose per Kg body weight
31
sex (distribution)
related to both size and fat distribution
32
metabolism (biotransformation)
chemical alterations of a drug by the body - usually liver - usually changed to less active chem - more ionized so more readily eliminated
33
Cytochrome P450 System
most common group of enzymes found in liver microsomal fraction (aka CYP) - inducible - inhibition - FDA suggests in vitro testing to predict interactions
34
special pt considerations (metabolism)
pathology age genetic drug exposure
35
excretion
drug elimination from the body - routes - excretion RATE important - avoid cumulative effects
36
routes (excretion)
``` kidneys liver - bile to feces sweat glands saliva lungs mothers milk ```
37
kidney (nephron) rate depends upon:
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
clearance = ml/min or L/hr calculated volume
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
physiologists and clinicians refers to "renal" clearance
to est individual pt renal fx (test creatinine clearance)
40
research pharmacologist refers to "total" drug clearance
includes metabolism and excretion by all routes incorporated into the concept of a drug's effective 1/2 life in the body
41
intensity of response to given dose of a drug
-concentration at active site (pharmacokinetics) ability of active site to respond - receptor number may change - internal responses may change
42
individual pt differences
- age (enzymes, blood brain barrier) - weight (surface area) - sex (body comp, pregnancy, nursing) environment - physical (temp, attitude) - psychosocial (sensory distraction, placebo, compliance)
43
Genetic (pt differences)
- metabolism - deficiencies or excesses in enzymes | - receptors - insulin receptors defective in some type II diabetics
44
Assess pre-drug status of the individual - baseline state
monitor effectiveness and toxicities
45
adverse responses to drugs
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
drug interactions due to simultaneous admin of 2+ Rx
may INCREASE therapeutic or toxic effect - additive - synergistic - potentiation may DECREASE therapeutic or toxic effect -antagonism
47
alter pharmacodynamics (mechanism of drug interactions)
- binding to receptor site modified (other antagonists or agonists) - increase or decrease rate of difference portions of pathway
48
alter pharmacokinetics
- 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
competition for plasma proteins
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
An alkaline drug is ______ ionized in a acidic enviroment.
more
51
Administration of an antacid can directly alter the way a second orally administered drug is:
absorbed only
52
A drug is most likely to pass through a membrane is it is:
lipid soluble
53
What is a teratongenic drug?...It is a drug that:
causes birth defects in fetuses.
54
What type of compound binds a receptor and "turns it on".
agonist
55
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.
we would expect to have LESS free drug available to bind receptors.
56
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.
partial agonist
57
Certain chemical cause the liver to make more drug metabolizing enzymes. What is this process referred to as?
induction
58
What type of compound has effects that are reversible especially in the presence of more agonist?
competitive antagonist
59
A gaseous anesthetic dissolves in the respiratory membrane and it _______ dependent upon receptors to mediate its action.
is not
60
Drug idiosyncracy
Non- allergic abnormal response - genetic?
61
Drug allergy
Responses to histamine

Pharmacology - Exam 1 (3 decks)

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