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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
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)\_\_\_\_\_\_\_.
forms a tight complex with the enzyme inhibiting its further activity
21
A compound that causes induction is called an \_\_\_\_\_\_.
inducer
22
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.
P-Glycoproteins
23
\_\_\_\_\_\_ of p-glycoproteins will decrease plasma levels of drug substrates.
Inducers
24
What is Erythromycin/Clarithromycin?
an antibiotic
25
The _____ in many cases is the increased synthesis of enzyme protein.
mechanism of induction
26
P-glycoproteins are a member of a superfamily of transporters known as _____ (active pumps fueled by ATP).
ABC
27
The inhibitor can be a ______ (important determinant: relative concentrations and affinities of the two substrates).
substrate competing for the enzyme
28
Deficient ______ in neonates can lead to “gray baby syndrome” after chloramphenicol administration.
glucuronidation
30
What is induction by a drug of its own metabolism called?
production of pharmacokinetic tolerance
31
Name 7 clinically relevant inhibitors.
1) Cimetidine 2) Erythromycin / Clarithromycin 3) Ketoconazole / Azole antifungals 4) Fluoxetine (and other SSRIs) 5) Grapefruit juice 6) HIV protease inhibitors 7) Omeprazole
33
Name 3 drugs that produce pharmacokinetic tolerance.
phenobarbital, meprobamate, carbamazepine
35
Maximal effects of ______ is usually seen in 7-10 days and require similar time to dissipate.
enzyme induction
35
Acute alcohol exposure competitively inhibits a variety of \_\_\_\_\_\_.
biotransformations
36
What is Phenytoin?
a hydantoin-derivative anticonvulsant- treats seizures and arrhythmias- aka Dilantin
37
What is Rifampin?
a bactericidal antibiotic- inhibits RNA polymerase- treats TB- aka Rifadin
38
\_\_\_\_\_\_\_ competitively inhibits a variety of biotransformations.
Acute alcohol exposure
39
Inducers of p-glycoproteins will _____ plasma levels of drug substrates.
decrease
41
\_\_\_\_\_\_, especially CYP enzymes, are more prone to inhibition than phase II enzymes.
Phase I enzymes
41
Cimetidine, Phenobarbital, Phenytoin, Carbamazepine, Rifampin, Ethanol, St. John’s Wort, and Tobacco smoke are all \_\_\_\_\_\_\_.
inducers
42
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.
covalently binds to the enzyme (suicide inhibition) resulting in destruction of the enzyme
43
A compound that ______ is called an inducer.
causes induction
43
Where are P-gylocoproteins found?
in renal brush border membranes, bile canaliculi, astrocyte foot processes in brain microvessels, and in the GI tract
44
When P-Glycoproteins move molecules out of the cell at sites of exit (liver-kidney) they would enhance \_\_\_\_\_\_.
elimination
45
What is Fluoxetine?
SSRI antidepressant- aka Prozac, Serafem
46
The inhibitor can be a substrate competing for the enzyme (important determinant: \_\_\_\_\_\_\_).
relative concentrations and affinities of the two substrates
47
When P-Glycoproteins move molecules out of the cell at sites of \_\_\_\_\_\_, they would enhance elimination.
exit (liver-kidney)
49
What is Omeprazole?
a proton pump inhibitor- treats of dyspepsia, peptic ulcer disease, GERD, laryngopharyngeal reflux, and Zollinger–Ellison syndrome- aka Prilosec
50
When P-Glycoproteins move molecules out of the cell at sites of entry into the body (GI tract), they would ______ absorption.
decrease
52
What is Ketoconazole?
an antifungal- treats tinea, cutaneous candidiasis- aka Nizoral
53
Why does drug metabolism decrease in old age?
decreased liver mass; decreased blood flow to the liver
54
The inhibitor can be an ______ without being a \_\_\_\_\_\_(important determinant: relative concentrations and affinities of the inhibitor and the substrate whose metabolism is inhibited).
inhibitor; substrate
55
Another name for P-glycoproteins is \_\_\_\_\_.
MDR1
57
Phase I enzymes, especially\_\_\_\_\_\_, are more prone to inhibition than phase II enzymes.
CYP enzymes
58
A high ______ ratio in the diet stimulates mixed function oxidase (CYP).
protein:carbohydrate
59
What is Phenobarbital?
a barbiturate- treats seizures and is a sedative- aka Luminal
61
Induction generally takes _____ to see onset of effect.
48-72 hours
62
Name 4 major biological factors influencing drug metabolism.
1) diet 2) sex 3) age 4) disease states
63
\_\_\_\_\_\_ 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
Induction
64
Inhibitors of p-glycoproteins will _____ plasma levels of drug substrates.
increase
65
Name 7 clinically relevant inducers.
1) Phenobarbital 2) Phenytoin 3) Carbamazepine 4) Rifampin 5) Ethanol 6) St. John’s Wort 7) Tobacco smoke
66
Cimetidine, Erythromycin / Clarithromycin, Ketoconazole / Azole antifungals, Fluoxetine (and other SSRIs), Grapefruit juice , HIV protease inhibitors, and omeprazole and are all \_\_\_\_\_\_\_.
inhibitors
67
A compound can _____ the synthesis of enzyme.
inhibit

Disease and Defense- Pharm (12 decks)

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