Fa- Pharmacology

Front 1

Km

Back 1

affinity of enzyme for its substrate

Front 2

Vmax

Back 2

proportional to enzyme concentration

Front 3

decreasing Km will do what to the affinity

Back 3

decrease affinity

Front 4

enzyme kinetics graph
1. x intercept
2. y intercept
3. slope

Back 4

1. 1/-Km
2. 1/Vmax
3. Km/Vmax

Front 5

EK graph
1. increasing y-intercept, does what to Vmax?
2. further right the x-intercept is, how is Km?

Back 5

1. decrease Vmax
2. greater the Km

Front 6

competitive vs. noncompetitive inhibitors on graph

Back 6

competitive inhibitors cross each other

Front 7

Vd=

Back 7

amount of drug in body/plasma drug concentration

Front 8

low Vd (4-8 L) distribute where?

Back 8

in blood

Front 9

medium Vd distribute where

Back 9

extracellular space or body water

Front 10

high Vd (greater than body weight) distribute where

Back 10

in tissues

Front 11

CL=

Back 11

rate of elimination of drug/ plama drug concentration
OR
Vd * Ke

Front 12

t1/2=

Back 12

0.7 *Vd/ CL

Front 13

competitive inhibitors
1. resemble substrate
2. overcome by increase in substrate concentration
3. bind active site
4. effect on Vmax
5. effect on Km

Back 13

1. yes
2. yes
3. yes
4. unchanged
5. increase

Front 14

noncompetitive inhibitors
1. resemble substrate
2. overcome by increase in substrate concentration
3. bind active site
4. effect on Vmax
5. effect on Km

Back 14

1. no
2. no
3. no
4. increase
5. unchanged

Front 15

calculate loading dose

Back 15

LD= Cp x Vd/F

Front 16

calculate maintenance dose

Back 16

MD= Cp x CL/F where Cp= target plasma concentration and F= bioavailability

Front 17

in patient with impaired renal and hepativ function how is loading dose

Back 17

remains unchanged although maintenance dose is decreased

Front 18

zero-order elimination
1. what is it?
2. examples of drugs?

Back 18

1. -rate of elimination is constant regardless of C (constant AMOUNT of drug eliminated per unit time)
-Cp decrease linearly with time
2. PEA (round)
Phenytoin, Ethanol, Aspirin

Front 19

First-order elimination
1. what is it?

Back 19

1. rate of elimination is proportional to drug concentration (constant FRACTION of drug eliminated per unit time)
-Cp decrease exponentially with time

Front 20

Weak acids
1. Examples
2. trapped where
3. treat overdose with what?

Back 20

1. phenobarbital, methotrexate, TCas, aspirin
2. in basic environments
3. bicarbonate

Front 21

Weak bases
1. Examples
2. trapped where
3. treat overdose with what?

Back 21

1. amphetamines
2. in acidic environments
3. ammonium chloride

Front 22

Phase I metabolism

Back 22

-cytochrome P450
-reduction, oxidation, hydrolysis
-usually yields slightly polar, water-soluble metabolites

Front 23

Phase II metabolism

Back 23

-conjugation
-acetylayion, glucuronidation, sulfation
-usually yields very polar, inactive metabolites
-renally excreted

Front 24

Efficacy

Back 24

maximal effect a drug can produce

Front 25

potency

Back 25

amount of drug needed for a given effect

Front 26

competitive anatagonist shifts curve how? does what?

Back 26

to the right
-decreasing potency
-increasing EC50

Front 27

noncompetitve anatagonist shifts curve how? does what?

Back 27

downward
-decreasing efficacy

Front 28

partial agonist acts where?
does what?
how is potency?

Back 28

-acts on smae receptor system as full agonist
-lower maximal efficacy regardless of dose
-is an independent factor

Front 29

therapeutic index is measurement of what?

Back 29

drug safety

Front 30

TI=

Back 30

LD50/ED50 or median toxic dose/ median effective dose
TILE (TI= L/E)

Front 31

TI of safer drugs

Back 31

safer drugs have higher TI values

Front 32

Phase I biotransformation classification

Back 32

-modification of drug molecule via oxidation, reduction, or hydrolysis******
-CYP450
-require for molecular oxygen and NADPH

Front 33

CYP450 IA2
1. substrate example
2. inducers
3. inhibitors
4. genetic polymorphism

Back 33

1. theophylline, acetaminophen
2. aromatic hydrocarbons (smoke), cruciferous veggies
3. quinolones, macrolides
4. no

Front 34

smoker w/ theophylline

Back 34

-if quit smoking, need to lower dose b/c toxicity
-in current smoker, plasma levels lower so need to increase dose

Front 35

CYP 450 2C9
1. substrate example
2. inducers
3. inhibitors
4. genetic polymorphism

Back 35

1. phenytoin, warfarin
2. general inducers
3.--
4. yes

Front 36

CYP 450 2D6
1. substrate example
2. inducers
3. inhibitors
4. genetic polymorphism

Back 36

1. many cardio and CNS drugs
2. none known
3. haloperidol, quinidine
4. yes

Front 37

CYP 450 3A4
1. substrate example
2. inducers
3. inhibitors
4. genetic polymorphism

Back 37

1. 60% of drugs in PDR
2. general inducers
3. general inhibitors, grapefruit juice
4. no

Front 38

grape fruit juice

Back 38

-high cholesterol and on statin and drink GF juice-- increase risk of statin toxicity
-active component- furanocoumarins
-Ex. alprazolam, midazolam, atorvastin*****, and cyclosporine

Front 39

cimetidine

Back 39

-for ulcers
-inhibit metabolism of drug and plasma level increase

Front 40

general inducers

Back 40

Smoking PCP on a RAG
-smoking
-PCP
-rifampin
-anticonvulsants (barbs, phenytoin, carbamazepine)
-glucocorticoids,
-alcohol
---stimulate liver to make more enzymes
-lowers plasma level of substrate and makes less effective

Front 41

general inhibitors

Back 41

-Grapefuit juice and COKE with your PIe
-pi= protease inhibitor- ritovir
-cimetidine, omeprazole, ketoconazole
-chloramphenical
-macrolides
-acute alcohol
-raises plasma level of substrate and make more effective

Front 42

pt. given on theophylline and has chronic broncitis is given macrolides

Back 42

-want to bronchodilate
-macrolides- for resp. infection
-increase plasma level of theophylline
-increase risk of toxicity

Front 43

what is elimination

Back 43

termination of drug action

Front 44

2 major ways to get rid of drugs

Back 44

biotransformation
-excretion

Front 45

zero-order elimination rate

Back 45

-constant AMOUNT of drug is eliminated per unit of time
-no half-life
-rate of elimination is indepent of plasma concentration
= high dose (saturation, working at max capacity)

Front 46

3 drugs with zero-order elimination

Back 46

1. ethanol
2. phentoin
3. aspirin
-at high doese

Front 47

zero-order graphs
1. x- time and y-units of drug
2. x- time and y-log units of drug

Back 47

1. down linear
2. upside-down- U but decreasing

Front 48

first-order elimination

Back 48

-constant fraction of drug is eliminated per unit time
-half-life applies

Front 49

Phase II biotransformation

Back 49

-conjugation with endogenous compounds via activity of TRANSFERASES
-conjugation--glucoronidation, acetylation, glutathione conjugation

Front 50

Glucoronosyl transferase*****

Back 50

-involved in glucoronidation

Front 51

acetylation

Back 51

phase II
-drug induced SLE by slow acetylators-- (hydralazine*****> procainamine> isoniazid
"It's HIP to have lupus"

Front 52

-CV: chloramphenicol toxicity

Back 52

-Grey-Baby syndrome
-mech of toxicity- b/c neonates have lower lvels of GT and can't metabolize

Front 53

CV: GT deficiency

Back 53

Gilbert or Crigler-Najjar
-can't conjugate bilirubin
-get jaundice

Front 54

CV: butterfly malar rash; +ANA

Back 54

-antihistones antibodies= drug-induced
-stop drug and SLE goes away