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Drug Action I > Week 2 > Flashcards

Week 2 Flashcards

1
Q

Possible consequences of biotransformation (metabolism)
Activity
Polarity
Toxicity

A

Dec in activity (detoxication)
Inc in polarity
Inc in activity or bioactivation (prodrug)
Inc in toxicity (toxication)

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2
Q

Metabolism (biotransformation) phase 1 and phase 2

A

Phase 1: oxidation, hydrolysis, reductive
adds or exposes function group
Phase II: conjugative- inc size and hydrophilicity
Goal: drug turned into an inactive, polar, water-soluble, and excretable metabolite

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3
Q

Which organs are responsible for eliminating drugs from the body?

A

Liver and kidneys

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4
Q

Which organ is responsible for metabolism of a drug?

A

Liver

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5
Q

Which organ is responsible for elimination of drugs?

A

Kidney

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6
Q

Cytochrome P450

A

Major enzyme for reduction/oxidation rxns during phase 1 of metabolism
Primarily found in endoplasmic reticulum (ER) of cell, small amounts in mitochondria
Utilizes NADPH and molecular oxygen

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7
Q

What do phase II enzymes do?

A

Inc hydrophilicity, water solubility
Promotes excretion
Typically faster rxns than phase I

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8
Q

Competitive inhibition

A

Inhibitor binds to same site on the enzyme as the substrate

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9
Q

Non-competitive inhibition

A

Inhibitor binds to both enzymes at a different site than the substrate

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10
Q

Uncompetitive inhibition

A

Inhibitor binds to the enzyme-substrate complex. Does not bind to active site

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11
Q

Irreversible inhibitor

A

Inhibitor binds chemically with residues and destroys the enzyme

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12
Q

How is felodipine impacted by grapefruit juice?

A

Grapefruit increases body absorption of felodipine into the blood by inhibiting intestinal CYP3A4 protein

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13
Q

Pharmacogenomics

A

Study of how genes affect a person’s response to drugs

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14
Q

Pharmacogenetics

A

Effect of genetic variation on drug response- such as safety, tolerability and efficacy

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15
Q

Human genome

A

Contains 3 bill base pairs
Gene size can be from 3000 to 2.4 mill bases
30,000 approx genes code for proteins

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16
Q

Polymorphism

A

Single nucleotide polymorphisms (SNPs) most common genetic variation which occurs from a diff in a single DNA building block (nucleotide)
SNPs occur q300 nucleotides on average

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17
Q

Genetic mutation

A

Permanent alteration in DNA sequence, can be hereditary or acquired

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18
Q

Chromosome mutations: deletion

A

When part of a chromosome is left out

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19
Q

Chromosome mutations: insertion

A

Part of a chromatid breaks off and attaches to sister chromatid- results in duplic. Of genes on same chromosome

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20
Q

Chromosome mutations: inversion

A

Part of chromosome breaks off and reattaches backwards

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21
Q

Chromosome mutations: translocation

A

Part of one chromosome breaks off and is added to a diff chromosome

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22
Q

Clinical importance of polymorphism

A

Mutation leads to alteration in AA seq of protein

If proteins are metabolic enzymes that can lead to alteration in PK and cause adverse drug rxns

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23
Q

How does polymorphism effect drug metabolism? (Assume same diagnosis, same prescription and how it effects patients differently)

A

Mutations in enzymatic proteins can cause major complications

  • Drug can become toxic but not beneficial due to mutation causing enzyme to convert drug to quickly to byproduct
  • Drug can be not toxic and beneficial
  • Drug can be not toxic and not beneficial- mutation prevents body from metabolizing drug
  • Drug can be toxic but beneficial
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24
Q

distribution

A

reversible xfer of drug to and from site of measurement (usually blood)

25
Q

how many liters makes up total body water “plasma+interstitial volume+intracellular volume

A

42 liters

26
Q

liters make up intracellular volume

A

28 liters

27
Q

liters make up extracellular volume

A

14 liters

28
Q

extracellular volume is consisting of what two components? how many liters?

A

interstitial volume and plasma volume. 14 liters

29
Q

liters make up interstitial volume

A

10 liters

30
Q

liters make up plasma volume

A

4 liters

31
Q

volume of distribution equation

A

volume of distribution= amount of drug administered (dose) / initial drug concentration

32
Q

define volume of distribution (Vd)

A

apparent volume into which a drug distributes in the body at equilibrium

33
Q

if the Vd volume is ~18L…

A

drug distribution is prob limited to extracellular fluid

34
Q

if the Vd volume is ~42L…

A

drug distribution is prob limited to all body water

35
Q

if the Vd volume is less than or equal to 5L…

A

drug distribution is prob limited to plasma

36
Q

if the Vd volume is greater than or equal to 42L…

A

drug distribution is into the tissue outside of plasma and interstitial fluid

37
Q

Cp is?

A

drug blood plasma concentration, used to calculate VD

38
Q

if Vd is high

A

there is low drug blood plasma (Cp) concentration which means more drug is in tissues

39
Q

if Vd is low

A

there is higher drug blood plasma (Cp) concentration which means less drug is in tissues

40
Q

two main plasma proteins that bind drugs?

A

albumin-binds to acidic drugs and few basic drugs

beta-globulin and an alpha1 acid glycoprotein also bind certain basic drugs

41
Q

What percentage of the genetic makeup in the human body is made up of our microbiome?

A

99%

42
Q

What are the microbiota organs

A 
Gut (primary location)
Oral
Lungs
Vagina
Skin
43
Q

Which part of body would you find the highest microbial density?

A

large intestine (Colon)

44
Q

Stomach and small intestine have many or few species of bacteria present?

A

Few

45
Q

Gut microbiota and their role in metabolizing drugs

A

Considered “metabolic organ”
Has a huge capacity to dominate and metabolize drugs
Varies in patients
Differences can effect drug metabolism and toxicity

46
Q

Indirect and direct interactions of microbiome and drug interaction

A

Indirect: competition between microbiome and drug (microbiota can metabolize same drug as host enzyme)
Direct: partial or complete biochemical xformation of drug by microbiome-derived enzymes. Effects body metabolization of drug and drug ability to work

47
Q

Drug excretion occurs primarily In which organ?

A

Kidney-> Nephron

48
Q

what does the Nephron do?

A

Filters blood

49
Q

Nephron turns ____________ form of drug into the more hydrophilic ______ form

A

Ionized, unionized**

50
Q

Most drugs are freely filtered at the?

A

Glomerulus

51
Q

Does filtration require a drug to be “free”

A

Yes

52
Q

Passive reabsorption is favored for ________ drugs

A

Unionized

53
Q

Probenecid

A

Prevents renal clearance of penicillin and incr circulation time in blood stream

54
Q

What is Clearance (Clp)

A

Describes removal of drug from a volume of plasma in a specific time
Does not indicate amount of drug removed, but the volume of plasma from which drug is removed in a time period

55
Q

T/F total drug clearance is defined as excretion from just the kidneys

A

False

56
Q

T/F clearance is defined as amount of drug removed in a given period of time from body

A

False

57
Q

T/F clearance is defines as volume of plasma from which all drug is removed in a given time period

A

True

58
Q

T/F the 1/2 life is not a pharmacokinetic parameter that can be used to measure clearance

A

False

59
Q

Half-life of drug

A

Time where half of drug is removed

Drug Action I (10 decks)

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