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Pharmacology Exam 1 (Lauren) > L6 Pharmacokinetics III > Flashcards

L6 Pharmacokinetics III Flashcards

1
Q

What is the goal of the biotransformation and metabolism of drugs?

A

To promote their elimination from the body

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2
Q

Drugs with a MW > 350 are excreted how

A

In the bile

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3
Q

What is an example of a drug that must be metabolized to be active?

A

Codeine

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4
Q

What is an example of a drug whose metabolites are more active than the parent drug. What does this do to its half life?

A

Diazepam. Increases half life OBVIOUSLY

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5
Q

What is an example of a drug that gets metabolized to toxic metabolites?

A

Acetaminophen

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6
Q

What toxic pathway does ethanol induce for acetaminophen metabolism?

A

CYP 2E1

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7
Q

What do Phase I reaction do?

A

Convert lipid-soluble, non-ionized compounds into more ionized, hydrophilic metabolites

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8
Q

What do Phase II reactions do?

A

Add an ionized, charged particle to a phase I metabolite in order to form a more polar and hydrophilic conjugate

(Conjugation)

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9
Q

What is the most common type of phase I reaction?

A

Oxidation

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10
Q

What kind of drugs get transferred to the fetus ?

A

BASIC drugs

Fetus is acidic

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11
Q

For first order drugs, what kind of graph should we make to make it easier to interpret?

A

Semilogarithmic

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12
Q

How long does it take to eliminate most of a drug?

A

5 half lives

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13
Q

How long does it take to obtain Css plasma levels

A

5 half lives

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14
Q

How long does it take to determine Css levels?

A

5 half lives

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15
Q

Is the time it takes to reach Css related to the size of the dose?

A

No, it is related to half life

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16
Q

If you decrease “tao” what will happen to Css?

A

It will increase

You’re giving the drug more often

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17
Q

When you’re drinking alcohol, do you ever reach a Css?

A

No, it just keeps accumulating

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18
Q

How do you calculate clearance?

A

CL= Vd x (.7 / T 1/2)

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19
Q

What is CL?

A

Measure of the body’s capacity to eliminate a drug

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20
Q

What is the optimal dosing interval?

A

The same amount of time as the half life

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21
Q

WHat is the most optimal maintenance dose?

A

When it is equal to the elimination rate

22
Q

If you increase dose and the decrease the dosing interval by the same ratio, what will happen to the Css?

A

It wont change

23
Q

What kind of metabolism do CYP450’s do?

A

Phase I

24
Q

What P450 enzyme metabolizes over 50% of drugs?

A

3A4

25
Q

What P450 enzyme gets a polymorphism that impairs codeine metabolism?

A

2D6

26
Q

What enzyme metabolizes and is induced by alcohol

A

2E1

21 years of age to drink EtOH

27
Q

Are Phase I microsomal enzymes (CYP 450’s) inducible?

A

Yes

28
Q

WHat is the only Phase II enzyme that is microsomal and inducible?

A

Glucuronyl transferase

29
Q

Drugs metabolized by 3A4 have a _____ degree of interactions

A

High

30
Q

What is the only phase II enzyme that can be induced?

A

Glucuronyl transferase

31
Q

What does it mean if a drug “induces” an enzyme?

A

It means the enzyme increases in number and the drugs it metabolizes get disposed of faster
(They work less)

32
Q

Fluoxetine inhibits which enzyme?

A

2D6.

So you’ll have increased concentrations of codeine and oxycodone

33
Q

Grapefruit juice inhibits which enzyme?

A

3A4.

So you’ll have increased concentrations of APAP, diazepam, and lidocaine

34
Q

What are the OXIDATIVE Phase I reactions that are NOT CYP450’s and not microsomal and inducible?

A

Alcohol dehydrogenase

Monoamine oxidase

35
Q

What are the NON-oxidative Phase I reactions that are not CYP450 and not inducible?

A

Reductive reactions (warfarin gets a H+)

Hydrolytic reactions (esterases and amidases like succinylcholine and AChE)

36
Q

What enzyme does most Phase II reactions?

A

UDP glucuronyl transferase

37
Q

What is a drug that goers through phase II before phase I?

A

Isoniazid. It gets acetylated first and then goes through hydrolysis

38
Q

What drug is used to measure activity of CYP 2D6

A

debrisoquin

Tells you how well they will metabolize codeine

39
Q

What enzyme metabolized nortriptyline?

A

2D6

40
Q

What type of polymorphism is the alcohol flush reaction?

A

Phase I polymorphism

Deficient in alcohol dehydrogenase

41
Q

Butyrylcholinesterase and fast/slow acetylators are which type of polymorphism

A

Phase II

42
Q

If someone is a slow acetylator, according to isoniazid, what should you do to their dose?

A

Lower it

43
Q

What kinds of drugs are subject to enterohepatic circulation and “freeing” by bacteria?

A

Large drugs like estrogens

44
Q

What happens to the half life of drugs that undergo enterohepatic circulation

A

Longer half lives (bacteria remove conjugation and it re-enters circulation)

45
Q

What form are antibiotics given in?

A

Conjugated form

46
Q

Why do antibiotics affect birth control?

A

Because estrogens are given in conjugated form and if you kill the bacteria that would take that conjugate off and make it active, its not gonna be active

47
Q

What is the first organ system to mess up in old people

A

Renal

48
Q

Where do hydrolysis reactions take place

A

Plasma

49
Q

How many passes through the kidney does it take to clear penicillin

A

Just 1

50
Q

What enzyme acetylates isoniazid?

A

N-acetyltransferase

51
Q

Is n-acetyltransferase inducible?

A

NO

Pharmacology Exam 1 (Lauren) (7 decks)

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