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DD Unit I > DD Frech metabolism excretion > Flashcards

DD Frech metabolism excretion Flashcards

1
Q

In general, what are the Phases of metabolism and what occurs during these phases?

A

Phase I - drug is made more hydrophilic. Phase II - drug is made very water soluble.

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2
Q

Where does Phase I metabolism take place.

A

Liver smooth endoplasmic reticulum

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3
Q

What type of reactions take place in Phase I metabolism?

A

Oxidations, reductions, hydrolysis

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4
Q

What types of enzymes participate in Phase I

A

CYP450, reductases, esterases-amidases

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5
Q

Which phase of metabolism is more susceptible to drug-drug interactions?

A

Phase I

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6
Q

Which phase of metabolism is more likely to be saturated?

A

Phase II

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7
Q

Which phase of metabolism is more susceptible to age related changes?

A

Phase I

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8
Q

What type of reactions take place in Phase II metabolism?

A

Conjugations

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9
Q

What types of enzymes participate in Phase II

A

Transferases

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10
Q

What are the 4 things that can happen to a drug during metabolism?

A

Detoxify, active drug to more active compound, inactive drug to an active compound, make a toxic metabolite

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11
Q

Which phase of metabolism can be induced or inhibited?

A

Phase I

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12
Q

T or F: Hydrophilic drugs can be metabolized by Phase I reactions.

A

FALSE. They must be lipid soluble otherwise they will have low specificity.

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13
Q

What does an Amplichip test tell you?

A

Detects polymorphisms in metabolism - ultrarapid metabolizers and poor metabolizers

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14
Q

Name the 3 highlighted CYP450 dependent drug modifications. (probably want to know these)

A

Aromatic hydroxylation, aliphatic hydroxylation, oxidative dealkylation

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15
Q

Name the 3 highlighted CYP450 independent drug modifications. (probably want to know these)

A

Amine oxidation (monoamine oxidase), alcohol dehydration, aldehyde dehydration

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16
Q

Name the 3 highlighted Phase I reduction drug modifications. (probably want to know these)

A

Azo reduction, nitro reduction, carbonyl reduction

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17
Q

T or F: Phase I esterases are commonly used in the design of pro-drugs.

A

TRUE

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18
Q

T or F: Phase II metabolism is mature at birth.

A

FALSE. Generally takes longer to mature than Phase I metabolism

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19
Q

Describe enterohepatic recirculation.

A

Absorption in intestines?> goes into circulation?> eventually makes it back to liver ?> into bile ?> resealed back into intestines ?> reabsorbed from intestines

20
Q

What do inducers do?

A

Produce a qualitative and/or quantitative change/increase in enzyme activity. Generally this is due to an increase in enzyme synthesis, but sometimes induces will also decrease enzyme turnover.

21
Q

Generally, how long do inducers take to affect metabolism?

A

48-72 hrs. Remember, most inducers cause increased enzyme synthesis, so they act as transcription factors, which means they will take a little more time to have effect.

22
Q

Do inducers affect Phase I or Phase II metabolism?

A

They can affect both, but most are known to affect CYP450 (Phase I)

23
Q

What do inhibiters do?

A

Produce a qualitative and/or quantitative decrease in enzyme activity.

24
Q

Generally, how long do inhibitors take to affect metabolism?

A

Within hours

25
Q

Name the mechanism by which metabolism inhibitor can work (4 things).

A

1.) Inhibit enzyme synthesis 2.) Compete for enzyme active site 3.) Allosterically inhibit enzyme 4.) Destroy or permanently disable enzyme

26
Q

Do inducers affect Phase I or Phase II metabolism?

A

They can affect both, but most are known to affect Phase I

27
Q

What is pharmacokinetic tolerance?

A

Induction of a drug by its own metabolite.

28
Q

Diseases of ______ (organ) may have a profound affect on metabolism.

A

the liver

29
Q

What type of proteins move molecules out of cells?

A

P-glycoproteins

30
Q

Which drug from this unit inhibits p-glycoproteins?

A

Erythomycin (resulting in prolonged Lipitor levels in circulation)

31
Q

Which drug from this unit induce p-glycoproteins?

A

Rifampin and St. John?s Wort (rifampin increases elimination of oral contraceptives)

32
Q

T or F: Death of bacteria flora can affect hepatoenteric recycling.

A

Yes, especially if drug absorption is dependent on gut bacterial enzymes.

33
Q

T or F: Most drugs cross into breast milk.

A

TRUE. Usually at low levels.

34
Q

T or F: Milk is more basic than plasma.

A

FALSE. Milk is usually more acidic

35
Q

T or F: When choosing a drug during breastfeeding, pick one that is more lipid soluble.

A

FALSE

36
Q

T or F: When choosing a drug during breastfeeding, pick one that has higher protein binding.

A

TRUE. It will stay in the plasma rather than go into your mommy fountains

37
Q

T or F: If a highly soluble drug is eliminated via lungs, increasing your respiration rate will increase elimination.

A

TRUE

38
Q

T or F: If a poorly soluble drug is eliminated via lungs, increasing your respiration rate will increase elimination.

A

FALSE. Increasing blood flow to lungs increases the elimination of this drug.

39
Q

Define first order kinetics.

A

The rate of elimination is proportional to the concentration of drug in the plasma.

40
Q

How many half lives does it take to be reasonably sure that a drug is out of the body.

A

4-5

41
Q

What is steady state?

A

The state in which plasma concentration is constant. Amount in = amount out. Steady state is generally reached in 4-5 half lives.

42
Q

Does drug dose change the time it takes to reach steady state?

A

No. Time to steady state is independent to drug dose. However, drug concentration does influence the plasma concentration (Cp) when steady state is reached.

43
Q

What factor does change the time to steady state?

A

Drug half life

44
Q

If a drug?s half life is 2 hrs, what will be the change in plasma concentration if the drug is not given for 6 hrs?

A

8 fold fluctuation (2^3) in concentration

45
Q

Define zero order kinetics.

A

The amount of drug eliminated per unit time is constant and not dependent on drug concentration.

DD Unit I (10 decks)

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