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PMOC PDF 1 PART 1 > PMOC DRUGS DEVELOPMENT PROCESS AND PHASE 1 AND 2 > Flashcards

PMOC DRUGS DEVELOPMENT PROCESS AND PHASE 1 AND 2 Flashcards

1
Q

including a clinical condition and treated with the test drug

A

In vivo

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2
Q

drug activity is tested on isolated tissues or cells

A

In vitro

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3
Q

compound showing a desired pharmacological property which can be used to initiate a medicinal chemistry project

A

Lead compound

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4
Q

the science of the properties of the drugs and its effects in the body

A

Pharmacology

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5
Q

the study of the interaction of drugs with cells

A

Pharmacodynamics

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6
Q

the handling of a drug within the body, it includes the ADME processes

A

Pharmacokinetics

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7
Q

in vitro and in vivo testing , determination of LD 50

A

Toxicity testing

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8
Q

the general area of study concerned with the

formulation, manufacturing, stability and effectiveness of a pharmaceutical dosage form

A

Pharmaceutics

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9
Q

Genotoxicity screening is performed, as well as investigations on drug absorption and metabolism, the toxicity of the drug’s metabolites, and the speed with which the drug and its metabolites are excreted from the body.

A

Pre clinical studies

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10
Q

Filed before drug may be given to human (clinical trials)

A

IND

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11
Q

submitted for review and approval after the
completion of the clinical trials and requirements have
been met.

A

NDA

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12
Q

plays a central role in the elimination of drugs and other foreign compounds (xenobiotics) from the body

A

Metabolism / Biotransformation

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13
Q

an essential tool for
pharmacists in their role of
selecting and monitoring Pare appropriate drug therapy for nt their patients

A

Metabolism / Biotransformation

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14
Q

main site of metabolism and detoxification of

endo/exogenous compounds

A

Liver

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15
Q

– Metabolism before reaching systemic circulation – Limit the BA of orally administered drugs

A

First-Pass Effect

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16
Q

– Produceamorewater-
soluble compound
– Produce a molecule that can undergo subsequent
phase II reactions

A

Phase 1

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17
Q

Pathways to attach polar,ionizable

endogenous compounds

A
  • Glucuronidation
  • Sulfation
  • Glycine conjugation
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18
Q

Pathways to terminateorattenuate biological activity

A

Methylation

Acetylation

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19
Q

Protectbodyagainst

chemically reactive compounds

A

GSH conjugation

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20
Q

Funtionalization phase polar functional groups are introduced into the molecule or unmasked by:

A

Oxidation, Reduction and Hydrolysis

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21
Q

Pathway for direct functionalization group

A

Aliphatic and Aromatic hydroxylation

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22
Q

modifying or “unmasking” existing functionalities

A

⚫ reduction of ketones and aldehydes to
alcohols
⚫ oxidation of alcohols to acids
⚫ hydrolysis of ester and amides to yield
COOH, NH2 and OH groups; reduction of azo and nitro compounds to give NH2 moieties; oxidative N-, O- And S- dealkylation to give NH2. OH and SH groups).

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23
Q

Most are mediated by microsomes. and may refer to the change in
oxidation state of the substrate.

A

Oxidation

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24
Q

What oxidation reaction is oxygen is incorporated into the drug molecule

A

Hydroxylation

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25
Q

What oxidation reaction causes the loss of part of

the drug molecule

A

oxidative deamination, dealkylation

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26
Q

form in vitro after cell homogenization and fractionation of ER

A

Microsomes

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27
Q

primarily associated with protein synthesis

A

Rough microsomes

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28
Q

contain a class of oxidative enzymes called MFOs

A

Smooth microsomes

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29
Q

MFO reducing agents

A
  1. NADPH (Nicotinamide Adenine
    Dinucleotide Phosphate)
  2. Molecular Oxygen
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30
Q

One mole of this enzyme contains one mole each of flavin mononucleotide (FMN) and
flavin adenine dinucleotide • (FAD)

A

Flavoprotein

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31
Q

Molecular oxygen is also known as

A

Monooxygenases

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32
Q

Flavoprotient is a electron

A

transporter

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33
Q

It is cytochrome P450 reductase

A

NADPH

34
Q

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

A

Cytochrome P450

35
Q

Cytochrome P450 is a electron

A

Acceptor

36
Q

Refers to the mixed-function oxidation of aromatic compounds (arenes) to their corresponding phenolic metabolites (arenols)

A

Aromatic hydroxylation

37
Q

Epoxide intermediate aromatic hydroxylation

A

Arene oxide

38
Q

NIH shift leads to the formation of

A

arenols

39
Q

Enzyme use for formation of trans dihydrodiols

A

Epoxide hydrases

40
Q

Major route of metabolism for phenyl containing drugs

A

Aromatic hydroxylation

41
Q

Hydroxylation occurs at what position

A

Para

42
Q

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

A

Oxirane

43
Q

The epoxide is cleaved by epoxide hydrases to form

A

trans diol

44
Q

more stable than the arene oxides formed from aromatic compounds

A

Epoxide

45
Q

Toxicity of olefinic compounds may result from their metabolic conversion to chemically reactive epoxide

A

– Aflatoxin
– DES
– Stilbene
– Vinylchloride

46
Q

These are abnormal heme derivative and N-alkylatedprotoporphyrins

A

Green pigments

47
Q

Olefinic hydroxylation final metabolite

A

Transdihydroxylation

48
Q

Diazepam belongs to

A

2-ketobenzo

49
Q

2-ketobenzo common metabolite

A

Oxazepam

50
Q

Oxazepam prototype

A

3 hydroxybenzo

51
Q

Naturally occurinf carcinogenic agent

A

Aflatoxin

52
Q

Other name for alkene

A

Olefin

53
Q

Intermediate metabolite formed in drug that undergo N-dealkylation

A

Carbinolamine

54
Q

N-hydroxylation intermediate metabolite

A

N-hydroxylamine

55
Q

Parent drug of acetaminophen

A

Phenacitin

56
Q

Addition of hydrogen or gain electrons

A

Reductions

57
Q

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

A

Reduction

58
Q

It is recommended in diabetic patients with renal failure, because of the possible accumulation of its active metabolite hydroxyhexamide

A

Acetohexamide

59
Q

Azo reduction intermediate metabolite

A

Hydrazo

60
Q

reaction of water with substrate resulting in breaking scissile carbon- heteroatom bonds)

A

Hydrolysis

61
Q

mediatedbynonspecific

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

A

Ester hydrolysis

62
Q

mediatedbyliver

microsomal amidases. Esterases and deacylases

A

Amide hydrolysis

63
Q

This is the active metabolite of acetohexamide.

A

Hydroxyhexamide

64
Q

These are susceptible to either a-carbon hydroxylation or N-

oxidation

A

Amides

65
Q

endogenous compounds that undergo conjugation reactions

A
  1. Bilirubin
  2. Steroids
  3. Catecholamines
  4. Histamine
66
Q

Glucuronidation enzyme

A

Glucuronyltransferase

67
Q

Phase 1 aka

A

Functionalization

68
Q

Phase 2 aka

A

Conjugation

69
Q

Addition to structure for glucuronidation

A

Glucuronic acid

70
Q

Glucuronidation co enzyme

A

UDPGA

71
Q

Chlorampenical in neonates can produce

A

Gray baby syndrome

72
Q

leadstowater-solubleandinactive metabolite

A

Sulfation

73
Q

endogenouscompoundsthatunderogo sulfate conjugation

A

steroids,heparin,chondroitin, catecholamines, and thyroxine

74
Q

Sulfation coenzyme

A

3’-phosphoadenosine- 5’.phosphosulfate (PAPS).

75
Q

important pathway for detoxifying chemically reactive electrophilic compounds

A

GSH conjugation

76
Q

The acetyl group used in N- acetylation of xenobiotics is supplied by

A

N acetyl coA

77
Q

Rapid acetylator more likely to develop

A

isoniazid-associated hepatitis

78
Q

Rapid acetylator

A

Eskimos and Asian

79
Q

Terminate pharmacological activity and detoxification

A

Acetylation

80
Q

play an important role in the biosynthesis of many endogenous compounds

A

Methylation

81
Q

Methylation 2 compings

A

epinephrine and melatonin

82
Q

Metylation cozenzyme

A

S-adenosylmethionine(SAM)

PMOC PDF 1 PART 1 (5 decks)

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