Chapter 2 Metabolic Changes of Drugs and Related Organic Compounds

Question 1

What is the Topic Concept all about?

Answer 1

General Pathway of Drug Metabolism

Question 2

Phase 1 is also known as ——————— ?

Answer 2

Functionalization reactions

Question 3

Three types of Reaction in Phase 1

Answer 3

Oxidation, reduction and hydrolysis

Question 4

The Purpose of the Phase 1 is to introduce a functional polar group(s): ———— into the xenobiotic molecule to produce a more-water soluble compound
Give the following Four functional Group and their Formula

Answer 4

Alcohol = ROH,
Carboxylic Acid = RCOOH
Amine = NH2
SH = Thiol

Question 5

———- Molecule is a chemical compund that is foreign to an organism or an ecosystem

Answer 5

Xenobiotic Molecule

Question 6

Is a type of Biotransformation reaction taht involves the enzymatic hydrolysis of a molecule.

Answer 6

Hydrolytic Biotransformation

Question 7

Major site of Metabolism

Answer 7

Liver

Question 8

Majority of the Drugs in Metabolism undergo—— Phase 1 or Phase 2?

Answer 8

Phase 1

Question 9

Most Common Pathway for Metabolism

Answer 9

Oxidation

Question 10

Most Common Pathway for Metabolism——-

Answer 10

Oxidation
Explanation:because of the Enzyme called Cytochrome P450(Group of Enzyme)

Question 11

Responsible for transferring an oxygen atom to the substrate

Answer 11

Cytochrome P450

Question 12

How do we measure the wavelenth of Cytochrome P450

Answer 12

Spectrophotometer

Question 13

Most Enzyme are made up of

Answer 13

Protein

Question 14

Board Exam Question:
What metals are presence in Cytochrome P450?

Answer 14

Iron and copper

Question 15

Majority of the Cytochrome P450 found in liver is called

Answer 15

CYP3A4

Question 16

Majority of the Cytochrome P450 found in liver is called

Answer 16

CYP3A4

Question 17

Enzyme responsible to metabolite antidepressants

Answer 17

CYP2D6

Question 18

CYP means

Answer 18

Cytochrome P450 Enzymes
(Grouip of Enzyme

Question 19

In Enzyme Nomenclature what is the requirements in able to belong to the same family Ex. CYP1,CYP2

Answer 19

Must have more than 40% identical amino acid sequence

Question 20

In Cytochrome P450 enzymes Nomenclature,it is also categorize as Family Ex. CYP1, CYP2

Answer 20

Arabic Number

Question 21

Must have more than 55% identical amino acid sequence in Nomenclature Enzyme of Cytochrome P450?

Answer 21

Capital Letter

Question 22

Also known as Subfamily in Nomenclature of Enzyme in CYP P450

Answer 22

Capital Letter
Ex. CYP1A, CYP2C,CYP3A

Question 23

More than ——% of identical amino acid sequence is required in subfamily

Answer 23

55% of identical amino acid sequence is required in subfamily

Question 24

More than ——% of identical amino acid sequence is required in family

Answer 24

40% of identical amino acid sequence is required in family

Question 25

Individual enzyme in a subfamily Ex. CYP1A2, CYP2C9

Answer 25

Arabic number

Question 26

This two bad Habit can have effect in drug that we intake, whether there is a toxicity because it cannot be metabolize or there is no effect due to the drug metabolize fast

Answer 26

Alcohol and nicotine

Question 27

Oxidation of Alcohol yield to

Answer 27

Aldehyde

Question 28

Further oxidation of aldehyde from alcohol

Answer 28

Carboxylic acid

Question 29

Secondary Alcohol oxidation yield —

Answer 29

Ketones

Question 30

Oxidation of Tertiary Alcohol

Answer 30

None or cannot further oxidize

Question 31

Also known as rubbing alcohol

Answer 31

Isopropanol

Question 32

—- type of alcohol is considered safe in human consumption in moderate amounts

Answer 32

Ethanol

Question 33

Alcohol oxidized to — that causes blindness

Answer 33

Formic Acid

Question 34

Methanol toxicity antidote

Answer 34

Ethanol

Question 35

Common name of ethanal

Answer 35

Acetaldehyde

Question 36

Common name of ethanoic acid

Answer 36

Acetic Acid

Question 37

Causes hangover

Answer 37

Acetaldehyde

Question 38

Enzyme responsible of Alcohol oxidation

Answer 38

Alcohol dehydrogenase

Question 39

During drinking of Alcohol this Enzyme is lacking when the person experience Redness and Allergic Reaction

Answer 39

Aldehyde dehydrogenase

Question 40

Plays an important role in the metabolism of many compounds containing Carbonyl,nitro and azo group

Answer 40

Reduction

Question 41

Carbonyl compounds converted in reduction to——

Answer 41

Alcohol derivatives

Question 42

In reduction, Nitro and azo are converted to - -

Answer 42

Amino derivatives

Question 43

Chloral hydrate(Aldehyde) is also known as

Answer 43

Date rape drug or knockout drug

Question 44

Chroral Hydrate(Aldehyde) will reduce to —

Answer 44

Trichloroethanol(alcohol)

Question 45

General Formula of Ester

Answer 45

RCOOR

Question 46

Water that react with drug

Answer 46

Hydrolysis

Question 47

Most of the time that undergo hydrolysis are the drugs that contains —

Answer 47

Ester functional group

Question 48

ROR is what functional Group

Answer 48

Ether

Question 49

What about RCOR?

Answer 49

Ketone

Question 50

Phase II is also known as

Answer 50

Conjugated reactions

Question 51

Most drugs undergo first which is Phase I except-

Answer 51

INH or Isoniazid- drugs treat to tuberculosis

Question 52

Phase 1 reaction is called—

Answer 52

Functionalization Reaction

Question 53

Phase 1 reaction is called—

Answer 53

Functionalization Reaction

Question 54

Purpose is to attach small, polar, and ionizable endogenous compounds such as ———-to the functional handles of phase I metabolites or parent compounds that already have suitable existing functional groups to form water-soluble conjugated products.

Answer 54

glucuronic acid, sulfate, glycine, and other amino acids

Question 55

Phase 1 plus Phase 2 will form

Answer 55

Water soluble conjugated product which is secretable in our body

Question 56

Are readily excreted in the urine and are generally devoid lf pharmacological activity and toxicity in humans

Answer 56

Conjugated Metabolites

Question 57

2 Product of Conjugated metabolites

Answer 57

Devoid the 1. Pharmacologic activity 2. Toxicity of the drug

Question 58

Terminate or attenuate biological activity

Answer 58

Methylation and acetylation

Question 59

Also known as GSH

Answer 59

Glutathione

Question 60

Protects the body againts chemically reactive compounds and metabolites

Answer 60

Glutathione Conjugation

Question 61

Glutathion is produce by our —-

Answer 61

Liver

Question 62

Most common in Phase II reaction is Called ——

Answer 62

Glucuronidation

Question 63

Three drugs that undergo glucuronidation

Answer 63

Morphine Paracetamol Chloramphenicol

Question 64

Babies dont have glucoronic Acid, and when chloramphenicol(Antibiotic) is accidentally administer to the Baby, it wont metabolite the toxicity is called—-

Answer 64

Gray Baby Syndrome

Question 65

This enzyme will attached to Glucunic acid

Answer 65

Glucuronyl transferase

Question 66

Well developed and first develop in infant

Answer 66

Sulfate Conjugation Ex. Paracetamol. That is why safe siyansa infant

Question 67

Paracetamol is give every — hrs

Answer 67

4hrs

Question 68

Each Paracetamol contain how may mg

Answer 68

500mg

Question 69

Limit of Paracetamol per Day —-mg —- tablet

Answer 69

4000mg 8 tablet

Question 70

1.If Paracetamol 500mg is taken every 4hrs in a day how many mg is the total consumption per day 2. Total mg/day that will caused hepatic toxicity

Answer 70

1. 3000mg/day 2. 4000mg/day

Question 71

Antidote of Paracetamol Overdose

Answer 71

Fluimucil Contains: NAC or (N-acetylcysteine)

Question 72

Used to conjugate carboxylic acids

Answer 72

Glycine & Glutamine Conjugation

Question 73

Example of Conjugated carboxylic acid is Benzoic acid to —-

Answer 73

Benzoic acid to hippuric acid

Question 74

Important pathway by which chemically reactive electrophilic compounds are detoxified or also know as “ free radical scavenger”

Answer 74

Glutathione / Mercapturic Acid Conjugation

Question 75

Glutathione is a Tripeptide that consist or three amino acid which is

Answer 75

-Glutamine -Cysteine -Glycine Also called glutamyl-cysteinylglycine

Question 76

Acetyl group utilized is supplied by acetyl CoA

Answer 76

Acetylation

Question 77

What drugs undergoes acetylation?

Answer 77

Primary amino group

Question 78

Example of Drugs that undergoes acetylation and its Toxicity:

Answer 78

Hydralazine - Systemic Lupus Erythematosus

Question 79

Symptoms of SLE

Answer 79

Malar Rash or Butterfly Rash"

Question 80

PIMCH means

Answer 80

Procainamide, Isoniazid, Methyldopa, Chlorpromazine, Hydralazine

Question 81

inactivation of physiologically active biogenic amines

Answer 81

METHYLATION

Question 82

does not lead to polar or water-soluble metabolites but are pharmacologically inactive

Answer 82

METHYLATION

Question 83

the most important organ in drug metabolism and detoxification of endogenous and exogenous compounds.

Answer 83

Liver

Question 84

important site of metabolism especially for orally administered drug

Answer 84

Intestinal Mucosa

Question 85

Intestinal Mucosa contains—- and ——- that can capture drug and secrete it back into the intestinal tract.

Answer 85

CYP3A4 isozyme and P-glycoprotein

Question 86

Three Sites of Drug Biotransformation

Answer 86

Liver Intestinal Mucosa First-Pass Effect

Question 87

orally administered drugs pass through the liver and are susceptibe to hepatic metabolism before reaching the bloodstream

Answer 87

First-Pass Effect

Question 88

Drugs Metabolized Extensively by First-Pass Effect

Answer 88

• Isoproterenol • Lidocaine • Meperidine • Morphine • Nitroglycerin

Question 89

Drugs Metabolized Extensively by First-Pass Effect

Answer 89

• Pentazocine • Propoxyphene • Propanolol • Salicylamide

Question 90

Enzyme Induction

Answer 90

• Phenytoin • Phenobarbital • Rifampicin • Chronic Alcoholism • Carbamazepine

Question 91

Enzyme Inhibitors

Answer 91

• Metronidazole • Erythromycin • Disulfiram • Isoniazid • Cimetidine • Ketoconazole • AcuteAlcoholism • ValproicAcid