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S2 Pharmacology > Intro > Flashcards

Intro Flashcards

1
Q

how do drugs impact rehab?

A 
response to exercise
patient's pain perception
participation and motivation in rehab
interactions with modalities
side effects screening
understanding of current medical management in inter-professional care
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2
Q

what is a drug

-types of drugs

A 
any non-nutrient chemical which has a physiological effect on the body
types
-natural
-semi-synthetic
-synthetic
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3
Q

what is pharmacotherapeutics

-subcategories

A

the use of specific drugs to prevent, treat, or diagnose a disease
subcategories
-pharmacokinetics
-pharmacodynamics

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4
Q

what is pharmacokinetics

-areas of interest

A 
study of how the body processes a drug
areas of interest
-administration
-absorption
-distribution
-elimination
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5
Q

what is pharmacodynamics

-types of effects

A

analysis of drug mechanism and effects
types of effects
-systemic
-cellular

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6
Q
  • azine
  • use
  • example
A

antipsychotics, neuroleptic, antiemetic

phenothiazine

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7
Q
  • azole
  • use
  • example
A

antifungal

miconazole

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8
Q
  • azapam
  • use
  • example
A

antianxiety drugs

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9
Q

barbital/-bital

  • use
  • example
A

barbiturate sedative hypnotics

phenobarbital

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10
Q
  • caine
  • use
  • example
A

local anesthetics

lidocaine

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11
Q
  • cillin
  • use
  • example
A

antibiotics

penicillin

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12
Q
  • cycline
  • use
  • example
A

antibiotic protein synthesis inhibitor

tetracycline

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13
Q
  • mycin, -micin
  • use
  • example
A

aminoglycoside inhibiting antibiotic

erythromycin

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14
Q
  • navir, -vir
  • use
  • example
A

antiviral (protease inhibitor)

saquinavir

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15
Q
  • olol
  • use
  • example
A

beta-adrenengic blocker

propanolol

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16
Q
  • oxin
  • use
  • example
A

cardiac glycosides

digoxin

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17
Q
  • ine
  • use
  • example
A

stimulants

caffeine

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18
Q
  • pril
  • use
  • example
A

ACE inhibitor

ramipril

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19
Q
  • statin
  • use
  • example
A

HMG-CoA reductace inhibitors

lovastatin

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20
Q

OTC pros and cons

A 
pros
-lower drug doses
-increased availability/access
-less expensive
cons
-possible interactions with prescription medications
-may delay use of more effective medications or treatments
-adverse effects
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21
Q

when determining the dosage of a drug, what is the overall consideration?

A

concentration must be large enough to produce a beneficial response without being toxic

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22
Q

dose-response curves: threshold dose and ceiling effects (maximal efficacy)

A

threshold dose
-where response begins and increases in magnitude until a response plateau is reached
ceiling effect
-point at which there is no further response

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23
Q

dose-response concepts: efficacy vs. potency

A

efficacy
-dosage ranges over which the drug has desired effect
-magnitude of response increases as dosage increases (up to some maximum effect)
potency
-threshold dose that produces a given response
-higher potency means less of the compound is required to produce a given response
-lower threshold dose = greater potency

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24
Q

quantal dose-response curve

A

% of the population who exhibit a specific response relative to the dose of the drug
looks at variations in drug responses due to individual differences within the clinical population

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25
Q

therapeutic index

  • what is it
  • equation
A

calculated value to indicate drug sfaety

TI = TD50/ED50

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26
Q

median effective dose

  • abbreviation
  • what is it
A

ED50

dose at which 50% of the population respond to a drug in a specified manner (response)

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27
Q

median toxic dose

  • abbreviation
  • what is it
A

TD50

dose at which 50% of the population exhibits the adverse effect/response

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28
Q

median lethal dose

  • abbreviation
  • what is it
A

LD50

dose that causes death in 50% of the animals studied

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29
Q

FDA drug approval process

-general characteristics of the process

A

clinical testing phases: 0-IV
7-9 years (about 1 billion dollars total cost)
fast track exists for life-threatening conditions or approval of a new indication for a known drug

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30
Q

clinical testing phases

A 
0: pre-clinical testing: lab animals
I: clinical testing: healthy subjects
2: limited target population
3: large target population
new drug approval
IV: monitor general population
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31
Q

a drug is placed into a category or “schedule” based on…

A

potential for abuse

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32
Q

schedule I

  • abuse potential
  • legal use
  • example
A 
potential
-highest
legal use
-restricted to approved research or therapeutic use in very limited # of patients
example
-medical marijuana
-cocaine
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33
Q

schedule II

  • abuse potential
  • legal use
  • example
A 
potential
-high
legal use
-specific therapeutic purposes w/ prescription
example
-opoids: morphine
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34
Q

schedule III

  • abuse potential
  • legal use
  • example
A

potential
-mild-moderate possible physical/psychologic dependence
legal use
-specific therapeutic purposes w/ prescription
example
-certain opoids: codeine combos; anabolic steroids

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35
Q

schedule IV

  • abuse potential
  • legal use
  • example
A

potential
-limited possible physical/psychologic dependence
legal use
-specific therapeutic purposes w/ prescription
example
-anti-anxiety drugs; other depressants and stimulants

36
Q

schedule V

  • abuse potential
  • legal use
  • example
A 
potential
-lowest relative abuse potential
legal use
-OTC
example
-cough medications; anti-diarrheal medications
37
Q

areas to look at involving pharmacodynamics

A 
potency
efficacy
therapeutic effect
side effects
receptors
38
Q

what is efficacy

A

drug’s ability to produce a desired response

39
Q

which route of administration does phonophoresis and iontophoresis

A

transdermal

40
Q

enteral

  • characteristics
  • absorbed by…
  • drug must have…
A 
usually oral
easiest for self-administration
generally safe, controlled entry to system
absorbed by small intestine
drug must have high lipid solubility
41
Q

enteral

-first pass effect

A

metabolism/destruction of drug molecule in liver before reaching its site of action

42
Q

parenteral

-characteristics

A

bypass the GI system
more direct route to target site
more predictable quantity
not subject to “first pass effect”

43
Q

bioavailability

  • what is it
  • depends on…
A

% of drug administered that reaches the bloodstream
depends on
-route of administration and the drug’s ability to cross membrane barriers
-extent of first pass metabolism

44
Q

why is the SI the primary location of drug absorption

A

surface area

45
Q

which drugs are absorbed out of the stomach

A

weak acids

46
Q

which drugs are absorbed out of the SI (duodenum)

A

weak bases

47
Q

bioavailability factors

A

body membrane structure and function
drug movement across membrane barriers
active transport

48
Q

factors that affect distribution

A

tissue permeability
blood flow
plasma protein binding
subcellular protein binding

49
Q

serum protein binding

A

drugs will sometime attach to plasma proteins
proteins allow the drug to stay in the blood, but a drug that is bound to plasma protein cannot leave the blood to distribute into tissues and is inactive
drug that is unbound (free) may distribute from blood to tissues and is active

50
Q

volume of distribution (Vd)

-what is it

A

amount of drug administered / concentration of drug in plasma

51
Q 
if Vd...
-equals total amount of body water
-greater than total amount of body water
-less than total amount of body water
slides 80-83
A

equal
-uniform body distribution
greater than
-drug is being concentrated in the tissues
less than
-drug is being retained in the bloodstream (due to plasma protein binding for example)

52
Q

when does apparent volume of distribution come into play?

A

when there is some material that absorbs the drug and prevents it from showing up when you try and check the Vd

53
Q

primary sites of drug storage

-what type of drugs are stored in each?

A 
adipose tissue
-primary site; ex: anesthetics
bone
-toxic agents; ex: lead
muscle
-long-term storage; ex: anti-malarials
organs
-often liver and kidneys; ex: anti-microbials
54
Q

other (new) drug delivery examples

A

controlled release
implanted reservoir
targeted cell and tissue delivery

55
Q

controlled release

  • benefits
  • examples
A 
decreases the number of doses/day
sustains dose throughout night
examples
-beta blockers
-analgesics
-Parkinson's drugs
56
Q

implanted reservoir

  • locations
  • examples of drugs
A 
locations
-abdomen
-spinal cord
examples
-muscle relaxers
-analgesics
-anesthetics
-hormones
57
Q

trageted cell and tissue delivery

  • function
  • examples
A

attaching antibodies to drugs
examples
-Brentuximab vedotin for Hodgkin Lymphoma

58
Q

drug elimination

-what are mechanisms for doing this?

A

biotransformation
excretion
combination
-of the above 2

59
Q

biotransformation

  • aka
  • what is it
A

aka metabolism

chemical altering of a drug to a metabolite via enzymes to deactivate that drug

60
Q

excretion

  • what is it
  • common methods
A

excreting the active form of a drug
methods
-liver to SI via bile duct
-through kidneys

61
Q

biotransformation-cellular mechanisms

A

oxidation
reduction
hydrolysis
conjugation

62
Q

drug metabolism

  • where
  • how
  • other factors
A 
where
-primary location: liver
-lungs, kidneys, GI, skin
how
-biotransformation
other factors
-tissue/organ damage
-metabolic inhibitors
-enzyme induction
63
Q

competitive inhibition of metabolism

A

inhibition of the enzyme that metabolizes drug B, by drug A, decreases the metabolism of drug B
if drug A forms a covalent bond with the enzyme, then you have to wait for the cell to make more enzymes for drug B to have effect

64
Q

induction of metabolism

A

induction of the enzyme that metabolizes drug B, by drug A, increases the metabolism of drug B by increasing the enzyme quantity

65
Q

factors affecting excretion

A 
reabsorption
polarity of metabolite
ionized=polar
polar drugs tend to be excreted
non-polar drugs tend to be reabsorbed into body versus being excreted
66
Q

drug elimination rates

-two key ideas

A

clearance

half-life

67
Q

clearance (CL)

  • what is it
  • equation
  • dependent on…
  • what is systemic CL
A

the ability of one organ or all organs to clear a drug
CL = Q x ((Ci-Co/Ci))
dependent on organ ability to extract drug from plasma and perfusion
systemic CL
-sum of individual organ CLs

68
Q

CL factors

A

blood flow to organ (Q)
extraction ratio - the fraction of drug removed from the plasma as it passes through the organ (Ci-Co)
concentration

69
Q

half-life

A

duration of activity of the compound in the body
the amount of time required for 50% of the drug remaining in the body to be eliminated
a function of both clearance and volume of distribution

70
Q

dosing schedules

-2 types

A

continuous administration

interval administration

71
Q

continuous administration

A

matching the rate of administration with the rate of drug elimination (clearance) once the desired plasma concentration in achieved
after 5 half-lives of a drug you will reach a steady state

72
Q

interval administration

A 
dosage is adjusted to provide an average plasma concentration over the dosing period
dosing interval (time in hours) will affect size of dosage need to maintain same relative plasma concentration
73
Q

what is a receptor

A

a cellular component where a drug binds and initiates a chain of biochemical events

74
Q

surface receptors

  • location
  • responsive to…
  • recognize and effect change by…
A 
located on outer cell membrane
responsive to amino acid peptides, or amine compounds
recognize and effect change by
-ion channel/membrane permeability
-enzymatic effects
-regulatory protein links
75
Q

surface mechanisms

A

receptor + ion channels
enzymes + receptors
regulatory proteins + receptors

76
Q

receptor + ion channels

A

ACh example

-ACh binds to receptor which activates opening pore in membrane allowing sodium in

77
Q

enzymes + receptors

A

protein tyrosine kinases

-outer surface stimulation activates inner surface wall enzymatic process

78
Q

regulatory proteins + receptors

A

proteins are located on inner surface of membrane
G-proteins when stimulated then activates enzymes or Ion channels
2nd messenger system

79
Q

intracellular receptors

  • location
  • examples
  • generally control…
A

located at cytoplasm and nucleus
a specific interaction mechanism for hormones
examples: thyroid hormones; steroids
generally control gene expression when activate

80
Q

drug-receptor interactions

-successful binding is affected by…

A

drug size
drug shape/fit: key-lock analogy
affinity
presence of allosteric modulators

81
Q

affinity

A

electrostatic attraction between a drug and receptor
related to the drug amount required to bind to the unoccupied receptors (if affinity is low, higher concentrations may be needed)

82
Q

what are allosteric modulators

A

local modulators that affect affinity of receptor portion of bond

83
Q

drug selectivity

A

a drug affects only one type of cell or tissue and produces a specific physiologic response

84
Q

dose response

  • what is it
  • can also be affected by
A 
response is essentially proportion to the number of receptors occupied by the drug
not always a linear relationship
can be affected by
-affinity
-receptor signal transmission
85
Q

what is an agonist

-what is a partial agonist

A

drug capable of binding to a receptor and activating change in the cell’s function
has both affinity and efficacy
partial agonists
-create a less than optimal response even though they are capable of occupying receptors

86
Q

what is an antagonist

  • example
  • competitve vs irreversible
A

drug capable of binding to a receptor but unable to create change in the receptor cell’s function
has affinity, but not activity
occupy valuable receptor site thereby “blocking” agonists from binding
example: beta blockers
competitve or irreversible
competitve antagonists can be displaced with higher concentrations of a drug agonist, but irreversible antagonists form permanent bonds that prevent agonists from binding

87
Q

receptor regulation

A

a prolonged increase in receptor stimulation will result in a decrease in receptor function (due to agonists)
a decrease in receptor stimulation will result in an increase in receptor numbers or sensitivity (due to antagonists)

S2 Pharmacology (7 decks)

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