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Medicinal Organic Chemistry Lec > Chapter 2 Metabolic Changes of Drugs and Related Organic Compounds > Flashcards

Chapter 2 Metabolic Changes of Drugs and Related Organic Compounds Flashcards

1
Q

What is the Topic Concept all about?

A

General Pathway of Drug Metabolism

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2
Q

Phase 1 is also known as ——————— ?

A

Functionalization reactions

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3
Q

Three types of Reaction in Phase 1

A

Oxidation, reduction and hydrolysis

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4
Q

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

A

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

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5
Q

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

A

Xenobiotic Molecule

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6
Q

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

A

Hydrolytic Biotransformation

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7
Q

Major site of Metabolism

A

Liver

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8
Q

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

A

Phase 1

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9
Q

Most Common Pathway for Metabolism

A

Oxidation

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10
Q

Most Common Pathway for Metabolism——-

A

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

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11
Q

Responsible for transferring an oxygen atom to the substrate

A

Cytochrome P450

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12
Q

How do we measure the wavelenth of Cytochrome P450

A

Spectrophotometer

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13
Q

Most Enzyme are made up of

A

Protein

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14
Q

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

A

Iron and copper

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15
Q

Majority of the Cytochrome P450 found in liver is called

A

CYP3A4

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16
Q

Majority of the Cytochrome P450 found in liver is called

A

CYP3A4

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17
Q

Enzyme responsible to metabolite antidepressants

A

CYP2D6

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18
Q

CYP means

A

Cytochrome P450 Enzymes
(Grouip of Enzyme

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19
Q

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

A

Must have more than 40% identical amino acid sequence

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20
Q

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

A

Arabic Number

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21
Q

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

A

Capital Letter

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22
Q

Also known as Subfamily in Nomenclature of Enzyme in CYP P450

A

Capital Letter
Ex. CYP1A, CYP2C,CYP3A

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23
Q

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

A

55% of identical amino acid sequence is required in subfamily

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24
Q

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

A

40% of identical amino acid sequence is required in family

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25
Q

Individual enzyme in a subfamily
Ex. CYP1A2, CYP2C9

A

Arabic number

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26
Q

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

A

Alcohol and nicotine

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27
Q

Oxidation of Alcohol yield to

A

Aldehyde

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28
Q

Further oxidation of aldehyde from alcohol

A

Carboxylic acid

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29
Q

Secondary Alcohol oxidation yield —

A

Ketones

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30
Q

Oxidation of Tertiary Alcohol

A

None or cannot further oxidize

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31
Q

Also known as rubbing alcohol

A

Isopropanol

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32
Q

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

A

Ethanol

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33
Q

Alcohol oxidized to — that causes blindness

A

Formic Acid

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34
Q

Methanol toxicity antidote

A

Ethanol

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35
Q

Common name of ethanal

A

Acetaldehyde

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36
Q

Common name of ethanoic acid

A

Acetic Acid

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37
Q

Causes hangover

A

Acetaldehyde

38
Q

Enzyme responsible of Alcohol oxidation

A

Alcohol dehydrogenase

39
Q

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

A

Aldehyde dehydrogenase

40
Q

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

41
Q

Carbonyl compounds converted in reduction to——

A

Alcohol derivatives

42
Q

In reduction,
Nitro and azo are converted to - -

A

Amino derivatives

43
Q

Chloral hydrate(Aldehyde) is also known as

A

Date rape drug or knockout drug

44
Q

Chroral Hydrate(Aldehyde) will reduce to —

A

Trichloroethanol(alcohol)

45
Q

General Formula of Ester

46
Q

Water that react with drug

A

Hydrolysis

47
Q

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

A

Ester functional group

48
Q

ROR is what functional Group

49
Q

What about RCOR?

50
Q

Phase II is also known as

A

Conjugated reactions

51
Q

Most drugs undergo first which is Phase I except-

A

INH or Isoniazid- drugs treat to tuberculosis

52
Q

Phase 1 reaction is called—

A

Functionalization Reaction

53
Q

Phase 1 reaction is called—

A

Functionalization Reaction

54
Q

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.

A

glucuronic acid, sulfate, glycine, and other amino acids

55
Q

Phase 1 plus Phase 2 will form

A

Water soluble conjugated product which is secretable in our body

56
Q

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

A

Conjugated Metabolites

57
Q

2 Product of Conjugated metabolites

A

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

58
Q

Terminate or attenuate biological activity

A

Methylation and acetylation

59
Q

Also known as GSH

A

Glutathione

60
Q

Protects the body againts chemically reactive compounds and metabolites

A

Glutathione Conjugation

61
Q

Glutathion is produce by our —-

62
Q

Most common in Phase II reaction is Called ——

A

Glucuronidation

63
Q

Three drugs that undergo glucuronidation

A

Morphine
Paracetamol
Chloramphenicol

64
Q

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

A

Gray Baby Syndrome

65
Q

This enzyme will attached to Glucunic acid

A

Glucuronyl transferase

66
Q

Well developed and first develop in infant

A

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

67
Q

Paracetamol is give every — hrs

68
Q

Each Paracetamol contain how may mg

69
Q

Limit of Paracetamol per Day
—-mg
—- tablet

A

4000mg
8 tablet

70
Q

1.If Paracetamol 500mg is taken every 4hrs in a day how many mg is the total consumption per day

  1. Total mg/day that will caused hepatic toxicity
A
  1. 3000mg/day
  2. 4000mg/day
71
Q

Antidote of Paracetamol Overdose

A

Fluimucil
Contains: NAC or (N-acetylcysteine)

72
Q

Used to conjugate carboxylic acids

A

Glycine & Glutamine Conjugation

73
Q

Example of Conjugated carboxylic acid is
Benzoic acid to —-

A

Benzoic acid to hippuric acid

74
Q

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

A

Glutathione / Mercapturic Acid Conjugation

75
Q

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

A

-Glutamine
-Cysteine
-Glycine

Also called glutamyl-cysteinylglycine

76
Q

Acetyl group utilized is supplied by acetyl CoA

A

Acetylation

77
Q

What drugs undergoes acetylation?

A

Primary amino group

78
Q

Example of Drugs that undergoes acetylation and its Toxicity:

A

Hydralazine - Systemic Lupus Erythematosus

79
Q

Symptoms of SLE

A

Malar Rash or Butterfly Rash”

80
Q

PIMCH means

A

Procainamide, Isoniazid, Methyldopa, Chlorpromazine, Hydralazine

81
Q

inactivation of physiologically active biogenic amines

A

METHYLATION

82
Q

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

A

METHYLATION

83
Q

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

84
Q

important site of metabolism especially for orally administered drug

A

Intestinal Mucosa

85
Q

Intestinal Mucosa

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

A

CYP3A4 isozyme and P-glycoprotein

86
Q

Three Sites of Drug Biotransformation

A

Liver
Intestinal Mucosa
First-Pass Effect

87
Q

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

A

First-Pass Effect

88
Q

Drugs Metabolized Extensively by First-Pass Effect

A

• Isoproterenol • Lidocaine
• Meperidine • Morphine
• Nitroglycerin

89
Q

Drugs Metabolized Extensively by First-Pass Effect

A

• Pentazocine
• Propoxyphene
• Propanolol
• Salicylamide

90
Q

Enzyme Induction

A

• Phenytoin
• Phenobarbital
• Rifampicin
• Chronic Alcoholism • Carbamazepine

91
Q

Enzyme Inhibitors

A

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

Medicinal Organic Chemistry Lec (5 decks)

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