Pharmacology

Question 1

Specificity

Answer 1

Ability of a drug to act thru a single mechanism of action

Question 2

Selectivity

Answer 2

Ability of a drug to induce one effect in preference to another

Question 3

Standard Safety Margin

Answer 3

LD1-ED99/ED99 X 100

What kind of number would you want to have?

Question 4

Tachyphylaxis

Answer 4

Acute form of drug tolerance induced by rapid, repeated administration of a drug

Question 5

Potentiation

Answer 5

One drug used in combination with another does not have any effect but potentiates the effect of the other

Question 6

Isoniazid Toxicity

Answer 6

Prevalent in Scandinavians, Jews, and White North Africans; is due to slow hepatic arylamine N-acetyltransferase Type II

Question 7

Response Theory

Answer 7

The theory that the magnitude of a response is dependent upon the rate of formation of a D-R interaction

Question 8

Polymorphism effects on Biotransformation (Pharmacokinetic)

Answer 8

Can change the Vm or Kmax; CYP3A5*1 allows people of African descent to metabolize some drugs faster

Question 9

CYP2B6 polymorphism

Answer 9

Causes cyclophosphamide failure

Question 10

CYP2C9

Answer 10

Causes increased risk of bleeding and faster metabolizing of Warfarin

Question 11

Efficacy

Answer 11

The maximal effect produced by a drug

Question 12

Phase I & II enzymes

Answer 12

I => Breaking down (hydrolysis, oxidation)

II=> Addition (Conjugation)

Question 13

Pharmacokinetic Polymorphisms

Answer 13

Lead to changes in Km or Vmax

Question 14

Gilbert’s Syndrome

Answer 14

Polymorphism in UDP-glycosyltransferase (Phase II enzyme)

Causes Irinotecan toxicity

Question 15

Polymorphisms

Answer 15

Alter drug receptors in diseased states

E.g. - Methemoglobinemia in G6PD deficiency due to faulty Dapsone

Question 16

Signal 3

Answer 16

Promotes the differentiation of effector T-cells and is transmitted via cytokines

Question 17

IL-6

Answer 17

Forms Th17 cells that secrete IL-6 and IL-17

Question 18

IL-4

Answer 18

Forms Th2 cells that secrete IL-4 and IL 5

*Mediates changes via GATA-3

Question 19

INF-y

Answer 19

Promotes Th1 cells that secrete INF-y and IL-2

Also secrete IL-1, IL-12 and TNF-a

*Mediated by T-bet

Question 20

IgM to IgE

Answer 20

IL-4

Question 21

IgM to IgG

Answer 21

INF-y

Question 22

IgG to IgA

Answer 22

TNF-B

Question 23

Alcohol and Aspirin kinetics

Answer 23

Zero Order (Chronic Aspirin use only)

Question 24

Bioavailability

Answer 24

F= AUC(oral)/ AUC(iv)

Studies on this determine effects of food on drugs

Question 25

Drug Half Life

Answer 25

t^1/2= .693/ke ke= elimination constant

Question 26

How long does it take to eliminate a drug from the body?

Answer 26

4 half lives -by this point, only 6.25% remains

Question 27

Volume of Distribution

Answer 27

Vd= Dose(iv)/Co Volume of a drug distributed in the body once an EQUILIBRIUM has been established If Vd>TBW, drug has been deposited somewhere and is highly lipophilic

Question 28

Clearance Equation

Answer 28

CL= Ke X Vd CL= 0.693 X Vd / (t^1/2)

Question 29

How long does it take to achieve Css?

Answer 29

4 half lives

Question 30

Maintenance Dose

Answer 30

MD= Dose X F/ Dosing interval (t)

Question 31

Css using Maintenance Interval

Answer 31

Css= MD/CL

Question 32

Loading Dose

Answer 32

A single large dose achieves Css and MD are reapplied in the future Css= Loading Dose X F / Vd What formula is this a rearrangement of?

Question 33

First Pass Elimination Effect

Answer 33

When a drug passes thru the hepatic circulation from the GI tract and is mostly metabolized

Question 34

If you have an orally labile drug, what might be a better alternative for administration?

Answer 34

Intramuscular

Question 35

When is intraarterial administration primarily used?

Answer 35

Cancer chemotherapy

Question 36

Microsomal Enzymes

Answer 36

Consist of mostly Phase I enzymes; includes CYP enzymes and their substrates must have lipophilic character * Activity is INDUCIBLE (smoking, drinking, exercise) * Located primarily in the smooth ER

Question 37

CYP1A2

Answer 37

Includes Warfarin; smoking increases the metabolism of Warfarin via this pathway *Can be inhibited by GRAPEFRUIT JUICE

Question 38

CYP2E1

Answer 38

Microsomal enzyme whose Activity is induced by ethanol and increases the metabolism of Acetaminophen by the liver

Question 39

Non-microsomal enzymes

Answer 39

Mostly phase II enzymes that are Phase II enzymes (acetylation, sulfation, methylation) *Activity generally is not inducible; enzymes are found in the cytosol

Question 40

Enterohepatic cycling

Answer 40

Process by which a drug or metabolite is excreted thru the biliary ducts but is reabsorbed by the distal SI; leads to an increased half-life

Question 41

Freely filtered drugs at the glomerulus

Answer 41

Drugs w/ a MW that is

Question 42

VKORC1

Answer 42

Activates Vitamin-K; inhibited by Warfarin