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POD > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Specificity

A

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

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2
Q

Selectivity

A

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

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3
Q

Standard Safety Margin

A

LD1-ED99/ED99 X 100

What kind of number would you want to have?

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4
Q

Tachyphylaxis

A

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

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5
Q

Potentiation

A

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

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6
Q

Isoniazid Toxicity

A

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

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7
Q

Response Theory

A

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

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8
Q

Polymorphism effects on Biotransformation (Pharmacokinetic)

A

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

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9
Q

CYP2B6 polymorphism

A

Causes cyclophosphamide failure

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10
Q

CYP2C9

A

Causes increased risk of bleeding and faster metabolizing of Warfarin

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11
Q

Efficacy

A

The maximal effect produced by a drug

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12
Q

Phase I & II enzymes

A

I => Breaking down (hydrolysis, oxidation)

II=> Addition (Conjugation)

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13
Q

Pharmacokinetic Polymorphisms

A

Lead to changes in Km or Vmax

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14
Q

Gilbert’s Syndrome

A

Polymorphism in UDP-glycosyltransferase (Phase II enzyme)

Causes Irinotecan toxicity

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15
Q

Polymorphisms

A

Alter drug receptors in diseased states

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

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16
Q

Signal 3

A

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

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17
Q

IL-6

A

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

18
Q

IL-4

A

Forms Th2 cells that secrete IL-4 and IL 5

*Mediates changes via GATA-3

19
Q

INF-y

A

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

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

*Mediated by T-bet

20
Q

IgM to IgE

A

IL-4

21
Q

IgM to IgG

A

INF-y

22
Q

IgG to IgA

A

TNF-B

23
Q

Alcohol and Aspirin kinetics

A

Zero Order (Chronic Aspirin use only)

24
Q

Bioavailability

A

F= AUC(oral)/ AUC(iv)

Studies on this determine effects of food on drugs

25
Q

Drug Half Life

A

t^1/2= .693/ke

ke= elimination constant

26
Q

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

A

4 half lives

-by this point, only 6.25% remains

27
Q

Volume of Distribution

A

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

28
Q

Clearance Equation

A

CL= Ke X Vd

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

29
Q

How long does it take to achieve Css?

A

4 half lives

30
Q

Maintenance Dose

A

MD= Dose X F/ Dosing interval (t)

31
Q

Css using Maintenance Interval

A

Css= MD/CL

32
Q

Loading Dose

A

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?

33
Q

First Pass Elimination Effect

A

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

34
Q

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

A

Intramuscular

35
Q

When is intraarterial administration primarily used?

A

Cancer chemotherapy

36
Q

Microsomal Enzymes

A

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
37
Q

CYP1A2

A

Includes Warfarin; smoking increases the metabolism of Warfarin via this pathway

*Can be inhibited by GRAPEFRUIT JUICE

38
Q

CYP2E1

A

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

39
Q

Non-microsomal enzymes

A

Mostly phase II enzymes that are Phase II enzymes (acetylation, sulfation, methylation)

*Activity generally is not inducible; enzymes are found in the cytosol

40
Q

Enterohepatic cycling

A

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

41
Q

Freely filtered drugs at the glomerulus

A

Drugs w/ a MW that is

42
Q

VKORC1

A

Activates Vitamin-K; inhibited by Warfarin

POD (4 decks)

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