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Pharmacology
Pharmacokinetics and dynamics
49
Pharmacology
Graduate
01/17/2014

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Term
Km
Definition
reflectx affinity of the enzyme for its substrate
Term
Vmax
Definition
directly proportional to the enzyme concentration
Term
y intercept
Definition
Vmax
Term
K intercept
Definition
-1/km
Term
the further the right the x intercept what happens to Km?
Definition
greater and thus lower affinity
Term
competitive vs noncompetitive: resembles substrate
Definition
competitive
Term
competitive vs noncompetitive: doesn't resemble substrate
Definition
noncompetitive
Term
competitive vs noncompetitive: overcome by increased []
Definition
competitive
Term
competitive vs noncompetitive: not overcome by increased [S]
Definition
noncompetitive
Term
competitive vs noncompetitive: binds active side
Definition
competitive
Term
competitive vs noncompetitive: binds other site
Definition
noncompetitive
Term
competitive vs noncompetitive: no change of v max
Definition
competitive
Term
competitive vs noncompetitive: decreases Vmax
Definition
noncompetitive
Term
competitive vs noncompetitive: increases Km
Definition
competitive
Term
competitive vs noncompetitive: no change in Km
Definition
noncompetitive
Term
competitive vs noncompetitive: decreases potency
Definition
competitive
Term
competitive vs noncompetitive: decreases efficacy
Definition
noncompetitive
Term
Vd equation
Definition
amount of drug in body / plasma [drug]
Term
low vd
Definition
distribute to blood, large or charged
Term
medium vd
Definition
distribute to extracelluar space/body water, small hydrophilic and do not bind plasma proteins
Term
high vd
Definition
distribute to all tissues, small lipophilic and bind to extravascular proteins
Term
cl concentration
Definition
rate of elimination of drug / plasma [drug]
Term
half life definition
Definition
time required to change amount of drug in the body by 1/2
Term
1st or 0 order for half life?
Definition
first
Term
half lives to reach steady state
Definition
4-5
Term
half life equation
Definition
0.7 x Vd / Cl
Term
bioavailability
Definition
fraction of administered drug that reaches circulation, IV = 100%
Term
LD equation
Definition
Cp x Vd / F
Term
MD equation
Definition
Cp x Cl / F
Term
efficacy
Definition
max effect a drug can produce; Km; analgesic meds, antibiotics, antihistamines, decongestants
Term
potency
Definition
amount of drug needed for a given effect, Km; chemotherapy, antihypertensive, anti lipid drugs
Term
shift for competitive
Definition
right
Term
noncompetitive shift
Definition
downward shift
Term
partial agonis shift
Definition
down and either left or right
Term
Therapeutic index equation
Definition
LD / ED
Term
safer drugs have high or low TI?
Definition
high
Term
constant amount is eliminated
Definition
zero order
Term
examples of zero order drugs
Definition
phenytoin, ethanol and ASA
Term
rate of elimination is constant fraction
Definition
first order
Term
enviroment WA get trapped
Definition
basic
Term
WA overdose tx
Definition
sodium bicarb
Term
WB trapped in what kind of environment
Definition
acidic
Term
treat WB overdose
Definition
ammonium chloride
Term
yields slightly polar, water soluble
Definition
phase I
Term
polar inactive metabolites
Definition
phase II
Term
phase 1 vs 2: p450
Definition
1
Term
phase 1 or 2: conjugation
Definition
2
Term
phase 1 or 2: lose first in elderly
Definition
1
Term
examples of phase II
Definition
glucuronidation, acetylation and sulfation
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