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Disease and Defense- Pharm > Drug Metabolism Factors > Flashcards

Drug Metabolism Factors Flashcards

1
Q

After about _____ of life, both phase I and phase II enzymes begin to mature but at variable rates.

A

2 weeks

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1
Q

_____ of p-glycoproteins will increase plasma levels of drug substrates.

A

Inhibitors

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2
Q

The inhibitor can be an inhibitor without being a substrate (important determinant: _______).

A

relative concentrations and affinities of the inhibitor and the substrate whose metabolism is inhibited

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3
Q

What is production of pharmacokinetic tolerance?

A

induction by a drug of its own metabolism

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3
Q

A high protein:carbohydrate ratio in the diet stimulates ______.

A

mixed function oxidase (CYP)

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3
Q

Deficient glucuronidation in neonates can lead to “______” after chloramphenicol administration.

A

gray baby syndrome

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4
Q

______ are able to metabolize along most pathways but at somewhat lower rates than adults.

A

Neonates

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4
Q

When P-Glycoproteins move molecules out of the cell at sites of _____ into the body (_____), they would decrease absorption.

A

entry, (GI tract)

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5
Q

What is Carbamazepine?

A

an anticonvulsant and mood-stabilizing drug- treats epilepsy and bipolar disorder- aka Tegretol, Equetro

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6
Q

Induction may be accompanied by marked morphological and biochemical changes, including: _____, ______, and ______.

A

(1) Increase in liver weight (2) Marked proliferation of SER (3) Increases in NADPH and cytochrome P-450

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7
Q

A compound can inhibit the synthesis of ____.

A

enzyme

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9
Q

The mechanism of induction in many cases is ______.

A

the increased synthesis of enzyme protein

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9
Q

What is Cimetidine?

A

is a histamine H2-receptor antagonist- inhibits stomach acid production- treats heartburn and peptic ulcers- aka Tagamet

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10
Q

Stimulation of the CYP450 system, resulting in increased drug metabolizing activity, is called ______.

A

induction

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11
Q

Malnutrition generally _____ drug metabolism.

A

decreases

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12
Q

When ______ move molecules out of the cell at sites of exit (liver-kidney) they would enhance elimination.

A

P-Glycoproteins

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14
Q

What is induction?

A

the stimulation of the CYP450 system, resulting in increased drug metabolizing activity

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14
Q

Transporters located on membranes of intestinal, renal, and hepatic epithelial cells also play a role in elimination of _______.

A

xenobiotics

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15
Q

Maximal effects of enzyme induction is usually seen in _____ and require similar time to dissipate.

A

7-10 days

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16
Q

What are Azoles?

A

antifungals, hyperthyroidism drugs, anti-psychotropics

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17
Q

Some decrease in drug metabolism (mainly ____) with old age has been observed.

A

CYP

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18
Q

Deficient glucuronidation in neonates can lead to “gray baby syndrome” after _______ administration.

A

chloramphenicol

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18
Q

Transporters located on membranes of ______, _____, and _____ epithelial cells also play a role in elimination of xenobiotics.

A

intestinal, renal, and hepatic

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19
Q

______ are a member of a superfamily of transporters known as ABC (ATP binding cassette – active pumps fueled by ATP).

A

P-glycoproteins

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20
Q

The inhibition can be the result of formation of a metabolite that (1) covalently binds to the enzyme (suicide inhibition) resulting in destruction of the enzyme, or (2)_______.

A

forms a tight complex with the enzyme inhibiting its further activity

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21
Q

A compound that causes induction is called an ______.

A

inducer

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22
Q

When ______ move molecules out of the cell at sites of entry into the body (GI tract), they would decrease absorption; at sites of exit (liver-kidney) they would enhance elimination.

A

P-Glycoproteins

23
Q

______ of p-glycoproteins will decrease plasma levels of drug substrates.

A

Inducers

24
Q

What is Erythromycin/Clarithromycin?

A

an antibiotic

25
Q

The _____ in many cases is the increased synthesis of enzyme protein.

A

mechanism of induction

26
Q

P-glycoproteins are a member of a superfamily of transporters known as _____ (active pumps fueled by ATP).

A

ABC

27
Q

The inhibitor can be a ______ (important determinant: relative concentrations and affinities of the two substrates).

A

substrate competing for the enzyme

28
Q

Deficient ______ in neonates can lead to “gray baby syndrome” after chloramphenicol administration.

A

glucuronidation

30
Q

What is induction by a drug of its own metabolism called?

A

production of pharmacokinetic tolerance

31
Q

Name 7 clinically relevant inhibitors.

A

1) Cimetidine 2) Erythromycin / Clarithromycin 3) Ketoconazole / Azole antifungals 4) Fluoxetine (and other SSRIs) 5) Grapefruit juice 6) HIV protease inhibitors 7) Omeprazole

33
Q

Name 3 drugs that produce pharmacokinetic tolerance.

A

phenobarbital, meprobamate, carbamazepine

35
Q

Maximal effects of ______ is usually seen in 7-10 days and require similar time to dissipate.

A

enzyme induction

35
Q

Acute alcohol exposure competitively inhibits a variety of ______.

A

biotransformations

36
Q

What is Phenytoin?

A

a hydantoin-derivative anticonvulsant- treats seizures and arrhythmias- aka Dilantin

37
Q

What is Rifampin?

A

a bactericidal antibiotic- inhibits RNA polymerase- treats TB- aka Rifadin

38
Q

_______ competitively inhibits a variety of biotransformations.

A

Acute alcohol exposure

39
Q

Inducers of p-glycoproteins will _____ plasma levels of drug substrates.

A

decrease

41
Q

______, especially CYP enzymes, are more prone to inhibition than phase II enzymes.

A

Phase I enzymes

41
Q

Cimetidine, Phenobarbital, Phenytoin, Carbamazepine, Rifampin, Ethanol, St. John’s Wort, and Tobacco smoke are all _______.

A

inducers

42
Q

The inhibition can be the result of formation of a metabolite that (1) _______, or (2) forms a tight complex with the enzyme inhibiting its further activity.

A

covalently binds to the enzyme (suicide inhibition) resulting in destruction of the enzyme

43
Q

A compound that ______ is called an inducer.

A

causes induction

43
Q

Where are P-gylocoproteins found?

A

in renal brush border membranes, bile canaliculi, astrocyte foot processes in brain microvessels, and in the GI tract

44
Q

When P-Glycoproteins move molecules out of the cell at sites of exit (liver-kidney) they would enhance ______.

A

elimination

45
Q

What is Fluoxetine?

A

SSRI antidepressant- aka Prozac, Serafem

46
Q

The inhibitor can be a substrate competing for the enzyme (important determinant: _______).

A

relative concentrations and affinities of the two substrates

47
Q

When P-Glycoproteins move molecules out of the cell at sites of ______, they would enhance elimination.

A

exit (liver-kidney)

49
Q

What is Omeprazole?

A

a proton pump inhibitor- treats of dyspepsia, peptic ulcer disease, GERD, laryngopharyngeal reflux, and Zollinger–Ellison syndrome- aka Prilosec

50
Q

When P-Glycoproteins move molecules out of the cell at sites of entry into the body (GI tract), they would ______ absorption.

A

decrease

52
Q

What is Ketoconazole?

A

an antifungal- treats tinea, cutaneous candidiasis- aka Nizoral

53
Q

Why does drug metabolism decrease in old age?

A

decreased liver mass; decreased blood flow to the liver

54
Q

The inhibitor can be an ______ without being a ______(important determinant: relative concentrations and affinities of the inhibitor and the substrate whose metabolism is inhibited).

A

inhibitor; substrate

55
Q

Another name for P-glycoproteins is _____.

A

MDR1

57
Q

Phase I enzymes, especially______, are more prone to inhibition than phase II enzymes.

A

CYP enzymes

58
Q

A high ______ ratio in the diet stimulates mixed function oxidase (CYP).

A

protein:carbohydrate

59
Q

What is Phenobarbital?

A

a barbiturate- treats seizures and is a sedative- aka Luminal

61
Q

Induction generally takes _____ to see onset of effect.

A

48-72 hours

62
Q

Name 4 major biological factors influencing drug metabolism.

A

1) diet 2) sex 3) age 4) disease states

63
Q

______ may be accompanied by marked morphological and biochemical changes, including: (1) Increase in liver weight (2) Marked proliferation of SER (3) Increases in NADPH and cytochrome P-450

A

Induction

64
Q

Inhibitors of p-glycoproteins will _____ plasma levels of drug substrates.

A

increase

65
Q

Name 7 clinically relevant inducers.

A

1) Phenobarbital 2) Phenytoin 3) Carbamazepine 4) Rifampin 5) Ethanol 6) St. John’s Wort 7) Tobacco smoke

66
Q

Cimetidine, Erythromycin / Clarithromycin, Ketoconazole / Azole antifungals, Fluoxetine (and other SSRIs), Grapefruit juice , HIV protease inhibitors, and omeprazole and are all _______.

A

inhibitors

67
Q

A compound can _____ the synthesis of enzyme.

A

inhibit

Disease and Defense- Pharm (12 decks)

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