PMOC DRUGS DEVELOPMENT PROCESS AND PHASE 1 AND 2

Question 1

including a clinical condition and treated with the test drug

Answer 1

In vivo

Question 2

drug activity is tested on isolated tissues or cells

Answer 2

In vitro

Question 3

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

Answer 3

Lead compound

Question 4

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

Answer 4

Pharmacology

Question 5

the study of the interaction of drugs with cells

Answer 5

Pharmacodynamics

Question 6

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

Answer 6

Pharmacokinetics

Question 7

in vitro and in vivo testing , determination of LD 50

Answer 7

Toxicity testing

Question 8

the general area of study concerned with the

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

Answer 8

Pharmaceutics

Question 9

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.

Answer 9

Pre clinical studies

Question 10

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

Answer 10

IND

Question 11

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

Answer 11

NDA

Question 12

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

Answer 12

Metabolism / Biotransformation

Question 13

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

Answer 13

Metabolism / Biotransformation

Question 14

main site of metabolism and detoxification of

endo/exogenous compounds

Answer 14

Liver

Question 15

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

Answer 15

First-Pass Effect

Question 16

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

Answer 16

Phase 1

Question 17

Pathways to attach polar,ionizable

endogenous compounds

Answer 17

• Glucuronidation
• Sulfation
• Glycine conjugation

Question 18

Pathways to terminateorattenuate biological activity

Answer 18

Methylation

Acetylation

Question 19

Protectbodyagainst

chemically reactive compounds

Answer 19

GSH conjugation

Question 20

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

Answer 20

Oxidation, Reduction and Hydrolysis

Question 21

Pathway for direct functionalization group

Answer 21

Aliphatic and Aromatic hydroxylation

Question 22

modifying or “unmasking” existing functionalities

Answer 22

⚫ 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).

Question 23

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

Answer 23

Oxidation

Question 24

What oxidation reaction is oxygen is incorporated into the drug molecule

Answer 24

Hydroxylation

Question 25

What oxidation reaction causes the loss of part of | the drug molecule

Answer 25

oxidative deamination, dealkylation

Question 26

form in vitro after cell homogenization and fractionation of ER

Answer 26

Microsomes

Question 27

primarily associated with protein synthesis

Answer 27

Rough microsomes

Question 28

contain a class of oxidative enzymes called MFOs

Answer 28

Smooth microsomes

Question 29

MFO reducing agents

Answer 29

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

Question 30

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

Answer 30

Flavoprotein

Question 31

Molecular oxygen is also known as

Answer 31

Monooxygenases

Question 32

Flavoprotient is a electron

Answer 32

transporter

Question 33

It is cytochrome P450 reductase

Answer 33

NADPH

Question 34

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

Answer 34

Cytochrome P450

Question 35

Cytochrome P450 is a electron

Answer 35

Acceptor

Question 36

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

Answer 36

Aromatic hydroxylation

Question 37

Epoxide intermediate aromatic hydroxylation

Answer 37

Arene oxide

Question 38

NIH shift leads to the formation of

Answer 38

arenols

Question 39

Enzyme use for formation of trans dihydrodiols

Answer 39

Epoxide hydrases

Question 40

Major route of metabolism for phenyl containing drugs

Answer 40

Aromatic hydroxylation

Question 41

Hydroxylation occurs at what position

Answer 41

Para

Question 42

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

Answer 42

Oxirane

Question 43

The epoxide is cleaved by epoxide hydrases to form

Answer 43

trans diol

Question 44

more stable than the arene oxides formed from aromatic compounds

Answer 44

Epoxide

Question 45

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

Answer 45

– Aflatoxin – DES – Stilbene – Vinylchloride

Question 46

These are abnormal heme derivative and N-alkylatedprotoporphyrins

Answer 46

Green pigments

Question 47

Olefinic hydroxylation final metabolite

Answer 47

Transdihydroxylation

Question 48

Diazepam belongs to

Answer 48

2-ketobenzo

Question 49

2-ketobenzo common metabolite

Answer 49

Oxazepam

Question 50

Oxazepam prototype

Answer 50

3 hydroxybenzo

Question 51

Naturally occurinf carcinogenic agent

Answer 51

Aflatoxin

Question 52

Other name for alkene

Answer 52

Olefin

Question 53

Intermediate metabolite formed in drug that undergo N-dealkylation

Answer 53

Carbinolamine

Question 54

N-hydroxylation intermediate metabolite

Answer 54

N-hydroxylamine

Question 55

Parent drug of acetaminophen

Answer 55

Phenacitin

Question 56

Addition of hydrogen or gain electrons

Answer 56

Reductions

Question 57

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

Answer 57

Reduction

Question 58

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

Answer 58

Acetohexamide

Question 59

Azo reduction intermediate metabolite

Answer 59

Hydrazo

Question 60

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

Answer 60

Hydrolysis

Question 61

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

Answer 61

Ester hydrolysis

Question 62

mediatedbyliver | microsomal amidases. Esterases and deacylases

Answer 62

Amide hydrolysis

Question 63

This is the active metabolite of acetohexamide.

Answer 63

Hydroxyhexamide

Question 64

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

Answer 64

Amides

Question 65

endogenous compounds that undergo conjugation reactions

Answer 65

1. Bilirubin 2. Steroids 3. Catecholamines 4. Histamine

Question 66

Glucuronidation enzyme

Answer 66

Glucuronyltransferase

Question 67

Phase 1 aka

Answer 67

Functionalization

Question 68

Phase 2 aka

Answer 68

Conjugation

Question 69

Addition to structure for glucuronidation

Answer 69

Glucuronic acid

Question 70

Glucuronidation co enzyme

Answer 70

UDPGA

Question 71

Chlorampenical in neonates can produce

Answer 71

Gray baby syndrome

Question 72

leadstowater-solubleandinactive metabolite

Answer 72

Sulfation

Question 73

endogenouscompoundsthatunderogo sulfate conjugation

Answer 73

steroids,heparin,chondroitin, catecholamines, and thyroxine

Question 74

Sulfation coenzyme

Answer 74

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

Question 75

important pathway for detoxifying chemically reactive electrophilic compounds

Answer 75

GSH conjugation

Question 76

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

Answer 76

N acetyl coA

Question 77

Rapid acetylator more likely to develop

Answer 77

isoniazid-associated hepatitis

Question 78

Rapid acetylator

Answer 78

Eskimos and Asian

Question 79

Terminate pharmacological activity and detoxification

Answer 79

Acetylation

Question 80

play an important role in the biosynthesis of many endogenous compounds

Answer 80

Methylation

Question 81

Methylation 2 compings

Answer 81

epinephrine and melatonin

Question 82

Metylation cozenzyme

Answer 82

S-adenosylmethionine(SAM)