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(NEW) PSMA > MED ORG II > Flashcards

MED ORG II Flashcards

1
Q

Range of short-term toxicity studies

A

2 Weeks to 3 Months

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2
Q

Orphan drugs are used to treat fewer than ____ people in the US

A

200,000

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3
Q

IND is submitted to __ and reviewed for ___

A

FDA, 30 days

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4
Q

This gives permission to market drug product

A

New Drug Application (NDA)

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5
Q

Phase 4 aka

A

Postmarketing Surveillance

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6
Q

Metabolism aka

A

Biotransformation

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7
Q

Essential tool for pharmacists in their role of selecting and monitoring appropriate drug therapy for their parents

A

METABOLISM

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8
Q

polar functional groups are introduced
into the molecule or unmasked by:
Oxidation, Reduction and Hydrolysis

A

FUNCTIONALIZATION PHASE

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9
Q

form in vitro after cell homogenization
and fractionation of ER

A

MICROSOMES

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10
Q

are primarily
associated with protein synthesis

A

Rough microsomes

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11
Q

contain a
class of oxidative enzymes called
MFOs

A

Smooth microsomes

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12
Q

MFO Requirements

A
  1. NADPH ; 2. Molecular Oxygen
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13
Q

cytochrome P450 reductase

A

NADPH

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14
Q

One mole of FLAVOPROTEIN
contains one mole each of ____, ____

A

flavin
mononucleotide (FMN) and
flavin adenine dinucleotide
(FAD)

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15
Q

Name based on light abs at
450nm when complexed with
CO

A

Cytochrome P450

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16
Q

Hemoprotein containing an iron
atom which can alternate
between ferrous (Fe+2) and
ferric (Fe+3) states

A

Cytochrome P450

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17
Q

Serves as terminal oxidase

A

Cytochrome P450

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18
Q

refers to the mixed-function oxidation of aromatic
compounds to their corresponding phenolic
metabolites

A

Aromatic
Hydroxylation

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19
Q

aromatic
compounds

A

ARENES

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20
Q

phenolic
metabolites

A

ARENOLS

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21
Q

Reactive Oxygen Specie

A

ARENE OXIDE

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22
Q

AH proceed initially through an epoxide intermediate called an
______ which rearranges rapidly and spontaneously to
the arenol

A

ARENE OXIDE

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23
Q

NIH Shift leading to the formation of ____

A

ARENOLS

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24
Q

AH May also acted upon by_____ leading to the
formation of ______

A

EPOXIDE HYDRASES, TRANS-DIHYDRODIOLS

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25
Q

AH may be acted upon by _____ in GSH to yield _____

A

SULFHYDRYL GROUP IN GSH, GSH ADDUCT

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26
Q

It is important to prevent the formation of ___by arene oxides

A

ROS

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27
Q

Major route of metabolism for phenylcontaining drugs

A

Aromatic Hydroxylation

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28
Q

Hydroxylation occurs at
the ___

A

PARA POSITION

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29
Q

Microsomal aromatic
hydroxylation reactions
appear to proceed most
readily in _____

A

activated
(electron-rich) rings

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30
Q

If there are two or more phenyl rings, hydroxylation proceeds in the
_____

A

Electron Rich Ring

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31
Q

There are certain compounds which are resistant to aromatic
hydroxylation despite of the aromatic rings DUE TO presence of ___ atoms attached to the rings

A

MULTI-ELECTRONEGATIVE CHLORINE

32
Q

The metabolic oxidation of olefinic carbon—carbon double bonds leads to the
corresponding ___

A

Epoxide or Oxirane

33
Q

The epoxide is cleaved by epoxide hydrases to form

A

trans-diols

34
Q

Olefin Epoxidation: There are inhibitors such as ____ and _____

A

Cyclohexene oxide and Trichloropropene

35
Q

– more stable than the arene oxides formed from aromatic compounds

A

Epoxides

36
Q

susceptible to enzymatic hydration by epoxide hydrase to form trans-l,2-
dihydrodiols (also called 1,2-diols or 1,2-dihydroxy compounds

A

Epoxides

37
Q

Toxicity of olefinic compounds may result
from their metabolic conversion to
__________

A

chemically reactive epoxide

38
Q

toxin found in peanuts

A

Aflatoxin

39
Q

abnormal heme derivative

A

Green Pigments

40
Q

The epoxide is reasonably stable and can be measured
_____ in the plasma of patients receiving the parent
drug

A

quantitatively

41
Q

• Carbon atoms attached to aromatic
rings

A

Benzylic position

42
Q

Carbon atoms attached to aromatic
rings (benzylic position) are susceptible
to oxidation, forming the ____

A

Alcohol (or carbinol) metabolite

43
Q

______ metabolites are often
oxidized further to aldehydes and
carboxylic acids

A

1⁰ alcohol

44
Q

_______are converted to ketone.

A

2⁰ alcohol

45
Q

Primary Alcohol Metabolite

A

Alcohol

46
Q

____ generally does not lead to the generation of reactive
intermediates

A

Allylic hydroxylation

47
Q

Metabolic oxidation at the terminal carbon is referred to as

A

ω oxidation

48
Q

Oxidation of the penultimate carbon atom (i.e., next-to-the-last carbon) is called

A

ω— I oxidation

49
Q

Hydroxylation of the alpha-carbon atom attached directly to the
heteroatom (N, O, S).

A

Oxidation Involving Carbon-Hetero
Systems

50
Q

Hydroxylation AKA

A

oxidation of the heteroatom

51
Q

Primary aliphatic amines are biotransformed by oxidative deamination (through the carbinolamine pathway) or by ___

A

N-Oxidation

52
Q

Primary Aliphatic Amine | Enzyme:

A

MFO

53
Q

Endogenous Primary Amines | Enzyme:

A

MAO

54
Q

Dealkylation of secondary
amines gives rise to the
corresponding ____ metabolite

A

PRIMARY AMINE

55
Q

Major Biotransformation Pathway of Primary Aliphatic Amines

A

N-Oxidation

56
Q

N-oxidation appears to be a
major biotransformation pathway because
________ cannot occur

A

a-carbon hydroxylation

57
Q

Primary aromatic amines are oxidized to ____ then
further oxidized to ____

A

Hydroxylamines, Nitroso

58
Q

N- alkyl substituents are also dealkylated through

A

N-Dealkylation

59
Q

______also happens to the alpha carbon of the amide
or phosphamide.

A

Hydroxylation

60
Q

It involves the oxidation of the alpha carbon

A

Oxidative Odealkylation

61
Q

It also involves the alpha carbon hydroxylation

A

Oxidation Involving Carbon-Sulfur Systems
S-dealkylation

62
Q

– addition of hydrogen or
gain of electrons

A

Reduction

63
Q

play an important role in
the metabolism of many
compounds containing
carbonyl, nitro, and azo
group

A

Reduction

64
Q

____
groups are susceptible to
conjugation

A

Hydroxyl and Amino groups

65
Q

Reduction of N-oxides to __

A

Tertiary amines

66
Q

Ketones are resistant to oxidation are reduced to ______

A

Secondary Alcohol

67
Q

Aldehydes are reduced to form ____

A

Primary Alcohol

68
Q

not recommended in
diabetic patients with
renal failure, because of
the possible accumulation
of its active metabolite

A

Acetohexamide

69
Q

Active Metabolite of Acetohexamide

A

Hydroxyhexamide

70
Q

The (R)( + ) enantiomer of the oral anticoagulant warfarin undergoes extensive reduction of its side chain ____ to generate the (R,S)( +) alcohol

A

Keto Group

71
Q

Proceed via a hydrazo
intermediate that is
cleaved reductively to yield
the corresponding aromatic
amines:

A

Azo Reductions

72
Q

reaction of water with
substrate resulting in
breaking scissile carbonheteroatom bonds

A

Hydrolysis

73
Q

Hydrolysis is frequently
__________
although serum pH may
cause reaction

A

enzyme-mediated

74
Q

Major biotransformation
pathway for drugs containing
an Ester functionality.

A

Hydrolysis

75
Q

mediated by nonspecific
esterases found in the
liver, kidney, and
intestine and
pseudocholinesterases
present in plasma

A

Ester hydrolysis

76
Q

mediated by liver
microsomal amidases.
Esterases and deacylases

A

Amide hydrolysis

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