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House Pharmacology > Drug Metabolism > Flashcards

Drug Metabolism Flashcards

1
Q

Drug metabolism/Biotransformation is the (physical or chemical?) modification of drugs in the body which transforms relatively lipo___ agents into products more ____, hydro_____ products which can easily be excreted.

A

Chemical

philic; polar

philic

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2
Q

Drug metabolism can Sometimes lead to chemical activation of inactive drugs to their active substrates

T/F
With examples

A

T
Enalapril to enalaprilat, Codeine to morphine

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3
Q

Inactive to active

Enalapril to _______, Codeine to _____

A

enalaprilat

morphine

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4
Q

Drug metabolism occurs Mainly in the _____, involves both ________ and ________ enzymes.

A

liver

microsomal and non microsomal

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5
Q

Drug metabolism Occur in almost all organs of the body

T/F

A

T

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6
Q

other relatively common sites for drug metabolism besides liver include the ____,_____,_____, and _____

A

lungs, kidney, GIT and the skin

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7
Q

Drug metabolism is categorized MAINLY into 2 main reactions - ______ and ______ metabolism.

A

Phase I and Phase II

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8
Q

Phase 1 of drug metabolism must occur before phase 2 of drug metabolism

T/F

A

F

Could occur in any order.

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9
Q

Phase 3 reaction has also been described – Mainly involved in the removal of drugs that _________________ by _______ (_________)

A

have undergone phase 1 and or 2 reactions

transporters

P-glycoprotein

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10
Q

Phase I Reactions/__________ reaction / ________ reaction

A

functionalization

nonsynthetic

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11
Q

Phase 1 reaction

Convert parent compound into a more __________ metabolite by adding or unmasking ________ (-OH, -SH, -NH2, -COOH, etc.) eg._____

A

polar (=hydrophilic)

functional groups

oxidation

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12
Q

Phase 1 reactions include _____,________, and _________ reactions. Others ________,______

A

Oxidative, reductive and hydrolytic

cyclization and decyclization

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13
Q

Main function of phase I reactions is to prepare chemicals for ________ and _____

A

phase II metabolism and subsequent excretion.

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14
Q

The drug May be sufficiently polar after phase 1 to be excreted readily
T/F

A

T

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15
Q

phase 2 metabolism involves,

________ with ________ to further increase aqueous solubility

Include ____,_____,_______,______,_____etc

A

Conjugation

endogenous substrate

glucoronide, sulfate, acetate, amino acid, glycine

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16
Q

Phase ____ is the true “detoxification” step in the metabolism process

A

II

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17
Q

Microsomal enzymes

Located on ____ in the ____,_____,_____,_____

A

sER

liver, kidney, lungs , intestinal mucosa

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18
Q

Example of microsomal enzymes include

____,________,______,_______

A

Monooxygynases, cytochrome P450, UGT, epoxide hydroxylases

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19
Q

Microsomal enzymes are only involved in phase 2 reactions

T/F

A

F

Involved in phase 1 and 2 reactions

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20
Q

Non-microsomal enzymes

Can be found in _______,______,______

examples include ____,______

A

Cytoplasm, mitochondria, plasma

Esterases, amidases,

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21
Q

Microsomal cytochrome P450

Act on only structurally related drugs
T/F

A

F

They act on structurally unrelated drugs

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22
Q

Microsomal cytochrome P450
which _____ drugs

A

oxidize

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23
Q

Microsomal cytochrome P450 ,__________ family of enzymes

A

monooxygenase

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24
Q

_______ enzyme Metabolizes the widest range of drugs.

A

Microsomal cytochrome P450

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25
Q

_______ enzyme metabolizes the widest range of drugs

A

Microsomal cytochrome P450

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26
Q

Cytochrome P450 system

These enzymes are _____-bound, _______-containing protein.

A

membrane; heme

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27
Q

The human CYP family consists of ___ genes, with ___ families and _____ subfamilies.

A

57

18

44

28
Q

Examples of human CYP enzymes include
_____,____,____,_____,_______

A

CYP2D6,CYP2C19,CYP2C9,CYP3A4andCYP3A5.

29
Q

The enzymes are named based on the _____ -

Eg

CYP3A4 belongs to ______ — , ______ —, and ________ —-

A

family

family 3

subfamily A

gene number 4.

30
Q

CYP ______ is involved in a significantly higher number of drug metabolism compared to the other enzymes.

A

CYP3A4

31
Q

Inhibition of CYP enzymes - ___eased degradation of co-medicated drugs, ____eased drug plasma concentrations,

Risk of ___________. Inhibitors: _______,______, MAO Inhibitor (_________)

A

Decr
Incre

severe adverse events

cimetidine

Isoniazid

Phenelzine

32
Q

Induction of CYP enzymes - ___eased degradation of co-medicated drugs , ____eased drug plasma concentrations , Loss of ________ , Risk of _________.

Inducers: _______,________,______, cyclophosphamide

A

Incr

Decr

pharmacological effect

therapeutic failure

barbiturates; rifampicin, carbamazepine

33
Q

Who is a more efficient metabolized between human and rats?

A

Rats

34
Q

Diseases affecting the liver will (reduce or increase ?) rate of drug metabolism.

A

reduce

35
Q

Testosterone is an enzyme (inducer or inhibitor?)

A

inducer

36
Q

felodipine inhibited by _____

A

grape juice

37
Q

Progesterone in an enzyme (inducer or inhibitor ?) .

A

inducer

38
Q

Placenta contains metabolizing enzymes

T/F

A

T

39
Q

Drugs with extensive first pass effect include – _______,______,______,______

A

lidocaine, propranolol, nitroglycerin, morphine

40
Q

Puritane (hinders or enhances?) sleep

A

Enhances

41
Q

List all the inhibitors of cyp450

A

Cimetidine
Isoniazid
Grapejuice fruit
Phenelzine
Omeprazole
Ketoconazole
Erythromycin
Refonavir

42
Q

List the inducers of cyp450

A

Carbamazepine
Rifampicin
Barbiturates
Cyclophosphamide
St John’s wort

43
Q

Diazapam (hinders or enhances?) sleep

A

Enhances

44
Q

Diazepam taken with ______ would make you sleep longer

Why?

A

Cimetidine

Cimetidine inhibits cyp450 that would metabolize diazepam

45
Q

Why don’t you give insulin orally?

A

Because of the first pass effect

46
Q

First pass effect is _____ proportional to bioavailability

A

Inversely

47
Q

L-dopa is given orally

T/F

With reason

A

F
Sue to the presence of dopa decarboxylase

48
Q

Propranolol has (high or low?) bioavailability

A

Low

49
Q

Determining bioavailability is important for calculating ________ for nonintravenous routes of administration.

A

drug dosages

50
Q

Bioavailability is the rate and extent to which an ___________.

For example, if 100 mg of a drug
is administered orally and 70 mg is absorbed unchanged, the bioavailability is _____ or ____%%

A

administered drug reaches the systemic circulation

0.7 or 70

51
Q

Bioavailability of a drug given
orally is the ratio of the __________ to the
__________________

A

AUC following oral administration

AUC following IV administration

52
Q

First-pass hepatic metabolism:

When a drug is absorbed
from the _______, it enters the ______ before entering the ______.

If the drug is rapidly metabolized in the _______ or ______ during this initial
passage, the amount of unchanged drug entering the systemic circulation is ____eased.

A

GI tract; portal circulation; systemic circulation

liver or gut wall

Decr

53
Q

First-pass metabolism by the ______ or ______ limits the _______ of many oral medications.

A

intestine or liver

efficacy

54
Q

For example, more than __% of nitroglycerin is cleared during
first-pass metabolism. Hence, it is primarily administered via the _______ or _______ route.

A

90

sublingual or transdermal

55
Q

Drugs with high first-pass metabolism should be given in doses sufficient to
ensure that enough active drug reaches the desired site of action.

T/F

A

T

56
Q

Very hydrophilic drugs are (poorly or well?) absorbed

Why?

drugs that are extremely lipophilic are
(poorly or well?) absorbed

Why?

A

Poorly

because of their inability to cross lipid-rich cell membranes.

Poorly

because they are totally insoluble in
aqueous body fluids and, therefore, cannot gain access to the
surface of cells.

57
Q

For a drug to be readily absorbed, it must be largely _____, yet have some solubility in ______
This is one reason why many drugs are either _______ or ______

A

lipophilic

aqueous solutions.

weak acids or weak bases.

58
Q

penicillin G, are stable in the pH of the gastric contents.

T/F

A

F

unstable

59
Q

insulin, are destroyed in the ______ by degradative enzymes.

A

GI tract

60
Q

Two drug formulations are bioequivalent if they show comparable _____ and similar times to __________

A

bioavailability

achieve peak blood concentrations.

61
Q

UGT-_____________

A

Uridine diphosphate-glucuronyltransferase (UGT)

62
Q

UGT converts the (toxic or non-toxic?) form of ____ ( ___________ ) to its (toxic or nontoxic?) form (________), making it able to be dissolved and removed from the body.

A

Toxic ; bilirubin

unconjugated bilirubin
Non toxic; conjugated bilirubin

63
Q

List 4 microsomal enzymes

A

Monooxygynases, cytochrome P450, UGT, epoxide hydroxylases

64
Q

List 2 Non microsomal enzymes

A

Esterases, amidases,

65
Q

Progesterone in an enzyme ( inducer or inhibitors?)

A

Inducer

66
Q

Drugs with extensive first pass effect include – ________,________,______,______

A

lidocaine, propranolol, nitroglycerin, morphine

House Pharmacology (50 decks)

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