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Dose-Effect Curve
Intensity changes as dose changes. Intensity changes with
time. Desired theraputic effect and adverse effects are
related to dose.
TERM 2
Potency
DEFINITION 2
related to the amount of drug needed to produce effect
TERM 3
ED
DEFINITION 3
Effective dose (50% produced desired effect)
TERM 4
efficacy
DEFINITION 4
related to the maximum effect regardless of dose
TERM 5
potency and efficacy are
DEFINITION 5
unrelated
efficacy vs
potency
"more" descriptive
TERM 7
LD
DEFINITION 7
Lethal Dose (50% of subjects died)
TERM 8
an impulse travels along the nerve and
produces
DEFINITION 8
an action potential
TERM 9
The action potential is triggered by the
DEFINITION 9
neurotransmitter released at the previous synapse
TERM 10
The neurotransmitter interacts with
the
DEFINITION 10
receptor
drug agonists have
an affinity for a receptor
TERM 17
competitive
antagonists
DEFINITION 17
combine with receptor, but then produce no effect
TERM 18
noncompetitive
antagonists
DEFINITION 18
bind to a receptor site different from the agonist, minimizing
the agonist's effects
TERM 19
physiologic
antagonists
DEFINITION 19
bind to different receptor sites and produce an effect
opposite to that of the agonist
TERM 20
enteral
DEFINITION 20
placed in the GI tract (orally or rectally)
parenteral
bypasses GI tract (injection, inhalation, or topical application)
TERM 22
oral drug absorption
area
DEFINITION 22
small intestines
TERM 23
oral route may have
DEFINITION 23
GI adverse effects
TERM 24
oral routes blood levels are
DEFINITION 24
less predictable
TERM 25
rectal routes are good for
DEFINITION 25
pt.s vomiting or unconscious
active parent compounds are converted to
inactive compounds, or a second active compund and then
an inactive compound
TERM 32
inactive parent compounds are transformed
into
DEFINITION 32
active compounds
TERM 33
factors that affect
pharmacokinetics
DEFINITION 33
pt compliance age and weight sex pathologic state genetic
variations placebo effect time or route of administration
other drugs
TERM 34
drugs ellicit a pharmacologic effect at their
site of action via
DEFINITION 34
modulation in the function
TERM 35
drugs can produce the same effect
or
DEFINITION 35
block the action of an endogeous agent
examples of local chemical signaling
prostaglandins and histamines
TERM 37
examples of hormones
DEFINITION 37
insulin, thyroid, steroids
TERM 38
neurotransmitters
DEFINITION 38
move electrical impulses thru synapses
TERM 39
examples of neurotransmitters
DEFINITION 39
norepi/epi and acetylcholine
TERM 40
ADME
DEFINITION 40
absorption distribution metabolism excretion
passive transport
lipid soluble substances move across membranes by simple
diffusion (related to concentration gradient and lipid
solubility)
TERM 47
filtration
DEFINITION 47
some small water-soluble molecules pass through membrane
pores by bulk flow of water
TERM 48
specialized transport
DEFINITION 48
active transport
TERM 49
active transport
DEFINITION 49
moves against conc. gradient or electrochemical gradient,
requires energy, may be blocked by metabolic inhibitors
TERM 50
facilitated diffusion
DEFINITION 50
does not move against concentration gradient may transport
glucose into some cells may involve pinocytosis
absorption factors
physiochemical factors site of absorption (route) drug's
solubility (in solution are more readily absorbed)
TERM 52
drugs in solution come in two forms
DEFINITION 52
ionized or nonionized (influenced by the pKa of drug and pH
of tissues)
TERM 53
if pKa is equal to
pH
DEFINITION 53
drug will exist in 50/50 ratio
TERM 54
Weak Acid formula
DEFINITION 54
HAH+A-
TERM 55
(Weak Acid) When pH increases
DEFINITION 55
the H ion concentration falls ionized form (A-) increases
cannot easily penetrate tissues
weak bases are better absorbed
when
the pH is greater than the pKa
TERM 62
in the prescence of
infection
DEFINITION 62
the pH of the tissues is higher, making the tissues less able
to be penetrated and the effect of local anesthetics reduced
TERM 63
all drugs exist in the blood in two forms
DEFINITION 63
free drug protein bound drug
TERM 64
free drug
DEFINITION 64
the active form and amount depends on the %protein binding
(specific for each drug)
TERM 65
free form
DEFINITION 65
form of drug passed across membranes
free drugs distributed thru
various body fluids
TERM 67
drug distribution factors
DEFINITION 67
size of organ, blood flow, solubility of drug, protein binding
and certain barriers
TERM 68
redistribution can affect
DEFINITION 68
a drug's duration of action
TERM 69
In plasma drugs may compete for
DEFINITION 69
binding to proteins
TERM 70
half life (t 1/2)
DEFINITION 70
the amount of time that passes for the concentration of the
drug to fall to one half of its blood level at any time
metabolism AKA
biotransformation
TERM 77
metabolic process
DEFINITION 77
produces compounds that are more polar (ionized) and less
lipid soluble, therefore more easily excreted (and less liekly
to be absorbed) mainly enzyme dependent
TERM 78
three mechanisms of metabolism
DEFINITION 78
active-inactive inactive-active active to active
TERM 79
First-pass effect
DEFINITION 79
if a drug has no functional groups it goes thru nonsynthetic
(phase 1) first, afterwards it can undergo conjugation or
synthetic (phase 2) metabolism
TERM 80
phase 1 is _ difficult and is affected by _ and _
_.
DEFINITION 80
more; age; drug interactions
oxidation is metabolized in
liver, kidney, nervous tissue (phase 1 metabolism)
TERM 82
hydrolysis is metabolized in
DEFINITION 82
plasma/tissues (phase 1 metabolism)
TERM 83
reduction is metabolized in
DEFINITION 83
liver (phase 1 metabolism)
TERM 84
other drugs and environmental substances
can affect phase 1 metabolism by
DEFINITION 84
altering microsomal enzymes thru induction or inhibition
TERM 85
some drug develop _ thru _ via their own
action
DEFINITION 85
tolerance; induction
renal routes
glomerular filtration active tubular secretion passive tubular
diffusion
TERM 92
glomerular filtration
DEFINITION 92
unchanged drug or its metabolites filtered thru glomeruli and
concentrated in renal tubular fluid.
TERM 93
glomerular filtration depends on
DEFINITION 93
protein binding and the glomerular filtration rate
TERM 94
bound drugs cannot
DEFINITION 94
be filtered and remain in system circulation
TERM 95
active tubular secretion
DEFINITION 95
transports drug from bloodstream across renal tubular
epithelial cells into the renal tubular fluid
glomerular filtration and active tubular
secretion are
relatively nonselective, several compounds, both exogenous
and endogenous (naturally occuring), can compete for
transport
TERM 97
passive tubular diffusion AKA
DEFINITION 97
passive reabsorbtion
TERM 98
passive tubular diffusion
DEFINITION 98
helps regulate the amount of drug in the tubular fluid
TERM 99
passive tubular diffusion favors
DEFINITION 99
resorption of nonionized, lipid-soluble compounds
TERM 100
passive tubular diffusion is influenced by
DEFINITION 100
the urinary pH, affecting the amounts of ionized and
unionized drug in tubular fluid
