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Genomics > Intro to Drug Metabolism > Flashcards

Intro to Drug Metabolism Flashcards

1
Q

Which principle describes: what does the drug do to the body

A

Pharmacodynamics

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2
Q

What is the goal behind the minimum effective concentration (MEC)?

A

To keep concentration above it

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3
Q

When does onset occur in terms of the therapeutic window?

A

The moment concentration reaches MEC

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4
Q

When does termination occur in terms of the therapeutic window?

A

After concentration goes down and just dips below MEC

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5
Q

What is the therapeutic window?

A

Area between toxicity and MEC

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6
Q

Which principle describes: what does the body do to the drug?

A

Pharmacokinetics

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7
Q

Which occurs first, pharmacokinetics or pharmacodynamics?

A

Pharmacokinetics

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8
Q

Which principle describes: How the body absorbs, distributes, and eliminates the drug

A

Pharmacokinetics

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9
Q

Which principle describes: Plasma concentration (dose) needed to produce effect-

A

Pharmacodynamics

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10
Q

What are some other terms used interchangeably with metabolism?

A

Biotransformation & Inactivation

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11
Q

Do all drugs undergoing metabolism inactivate the drug itself?

A

No, not all

Some actually get activated like L-Dopa to dopamine

Some stay active and transform to another active form like diazepam to oxazepam

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12
Q

Metabolism of drugs make it more (hydrophilic/hydrophobic)

A

Hydrophilic

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13
Q

Metabolism of drugs make it more (hydrophobic/hydrophilic)

A

Hydrophilic

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14
Q

Once a drug is metabolized, where is it eliminated?

A

Kidneys & GI tract

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15
Q

Where is the primary location of metabolism?

A

Liver (hepatic)

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16
Q

What is found in phase I rxns?

A

p450

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17
Q

Which rxn requires energy?

A

Phase II

18
Q

What is found in phase II rxns?

A

Conjugation rxns

19
Q

Which rxn does NOT require energy?

A

Phase I

20
Q

Once metabolized, what exactly is being removed?

A
  1. Parent (starting) compound

2. Metabolites

21
Q

Which phase makes the compound more hydrophilic?

A

Both phase I & II

22
Q

What specific rxns occur in phase I?

A
  1. Hydroxylation
  2. Dealkylation
  3. N-oxidation
23
Q

What specifically do phase II rxns add to the compound?

A

Endogenous substrates (glucuronides, sulfates & acetates)

24
Q

What is a pro-drug? How does it cycled through?

A

Inactive form; bioactivated via enzymatic action

25
Q

Can a drug go thru phase II then phase I?

A

Yes

26
Q

Can a conjugated form of a drug be more active than the parent drug?

A

Yes (example = morphine glucuronide)

27
Q

What is the first pass effect?

A

Metabolism of RX before absorption

Concentration of RX is greatly reduced before it reaches systemic circulation

28
Q

What is bioavailability?

A

Signifies how much intact drug reaches general circulation

29
Q

When does decreased bioavailability occur?

A
  1. Drug isnt absorbed
  2. Drug is inactivated by enzymes, acid, bacteria
  3. Drug is inactivated by p450 as it passes thru liver
30
Q

Describe the Entero-hepatic recycling

A
  1. Conjugated drug is secreted in bile
  2. Hydrolysis occurs (makes drug more lipophilic)
  3. Drug is reabsorbed from GI tract
  4. Drug duration is prolonged
31
Q

What rxn occurs in the entero-hepatic recycling to make drug more lipophilic?

A

Hydrolysis

32
Q

Hydrolysis rxns in the entero-hepatic recycling makes the drug more….

A

lipophilic

33
Q

Where exactly is cytochrome P450 found?

A

ER of liver (GI tract and other tissues as well)

34
Q

What rxns do the P450 enzymes participate in?

A

Oxidation

35
Q

Nomenclature example: CYP3A4

What is the 3?

A

Enzyme family

36
Q

Nomenclature example: CYP3A4

What is the A?

A

Enzyme sub-family

37
Q

Nomenclature example: CYP3A4

What is the 4?

A

Individual enzyme/family member

38
Q

How many different families are there of P450 in humans? Different isoforms?

A

At least 18 different families

About 50 different isoforms

39
Q

What are some examples of inhibitors of biotransforming enzymes?

A
  1. Grapefruit
  2. Cimetidine
  3. Ketoconazole
40
Q

Which age group has slower metabolism?

A

Very young and very old

41
Q

Which gender has faster metabolism?

A

Males

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