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FPP Pharmacology > Drug Metabolism > Flashcards

Drug Metabolism Flashcards

1
Q

Drug metabolism/Biotransformation is the __________ modification of drugs in the body which transforms relatively _________ agents into produce more ______, hydrophilic products which can easily be excreted.

A

Chemical
Lipophilic
Polar

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2
Q

What is the main pathway to remove drugs from the body

A

Drug metabolism

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3
Q

Examples of drugs that are activated by metabolism is

A

Enalapril to enalaprilat

Codeine to morphine

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4
Q

What are the 3 outcomes of drug metabolism

A

Active metabolite
Active drug
Inactivation

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5
Q

Drugs are mainly __________ and are easily transported across the cell membrane into the cells where they undergo biotransformation.

A

Lipophilic

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6
Q

Common sites of metabolism are

A

LIVER
lungs
Kidney
Git
Skin

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7
Q

Drug metabolism occurs in almost all organs of the body T/F

A

True

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8
Q

Drug metabolism involves 2 types of enzymes these are

A

Microsomal
Non microsomal

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9
Q

Drug metabolism is categorized MAINLY into 2 main reactions

A

Phase 1
Phase 2

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10
Q

Must phase 1 occurs before phase 2

A

No

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11
Q

Phase 3 rxns have been described what is it mainly involved in

A

the removal of drugs that have undergone phase 1 and or 2 reactions by transporters (P-glycoprotein)

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12
Q

Phase 1 rxns are also known as ________ &__________

A

Functionalization rxns
Synthetic rxns

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13
Q

Phase 1 rxns convert parent compound into a more polar (=hydrophilic) metabolite by

A

adding or unmasking functional groups

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14
Q

These functional groups include

A

-OH
-SH
-NH2
-COOH

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15
Q

5 types of phase 1 rxns

A

Oxidation
Reduction
Hydrolytic rxn
Cyclization
Decyclization

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16
Q

Phase 2 rxn is __________ with __________ substrate to FURTHER __________aqueous __________

A

Conjugation
Endogenous
Increase
Solubility

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17
Q

The endogenous substrates of phase 2 include

GAGAS

A

glucoronide
sulfate
acetate
amino acid
glycine

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18
Q

What is the true detoxification step in metabolism

A

Phase 2

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19
Q

Microsomal enzymes are located on what cellular organelle? And in what organs

A

Smooth endoplasmic reticulum

In Liver,
Kidney
Lungs
Intestinal mucosa

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20
Q

Examples of microsomal enzymes are

A

Monooxygynases

Cytochrome P450

UGT (Uridine 5’-diphospho-glucuronosyltransferas)

Epoxide hydroxylases

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21
Q

Microsomal enzymes are only involved in Phase 2 rxns
T/F

A

False
Phase 1&2

22
Q

Non Microsomal enzymes are found in

A

Cytoplasm
Mitochondria
Plasma

23
Q

Examples of non Microsomal enzymes are

A

Esterases
Amidases

24
Q

Microsomal cytochrome P450 monooxygenase family of enzymes, which ________ drugs

A

Oxidize

25
Q

Characteristics of cytochrome p450

A

Act on structurally unrelated drugs

Metabolize the widest range of drugs

membrane-bound, heme-containing protein.

26
Q

The human CYP family consists of ____ genes, with ____ families and ___ subfamilies.

A

57
18
44

27
Q

CYP3A4
3:
A:
4:

A

Family
Subfamily
Gene

28
Q

Modufication of CYP ACTION can occur in 3 ways

A

• Induction of drug metabolizing enzymes
• Inhibition of drug metabolizing enzymes
• Biological Factors

29
Q

Biological factors include

A

Species/Strain differences - fast acetylators vs slow acetylators
Disease state
Sex differences(M F )
Circadian rhythm
Age
Diet
Pregnancy
Inter specie and intra specie differences – rats/mice versus humans
•Genetic differences –
(fast metabolizing – depolarizing muscle blockers, fast acetylators vs slow acetylators )

30
Q

Testosterone an enzyme inducer t/f

A

T

31
Q

Inhibition of CYP enzymes causes 3

A
  • Decreased degradation of co-medicated drugs
    Increased drug plasma concentrations
    Risk of severe adverse events.
32
Q

Examples of inhibitors

A

cimetidine,
Isoniazid,
MAO Inhibitor (Phenelzine)
Grapefruit juice

33
Q

Induction of CYP enzymes causes

A

Increased degradation of co-medicated drugs

Decreased drug plasma concentrations

Loss of pharmacological effect

Risk of therapeutic failure.

34
Q

Examples of cyp inducers are

A

barbiturates,
carbamazepine,
rifampicin,
cyclophosphamide
St John wort
Glucocorticoids

35
Q

Gray baby syndrome is

And the deficient enzyme is

A

an adverse reaction to chloramphenicol

The UDP-glucuronyl transferase enzyme system in infants,
(especially premature infants, is not fully developed and incapable of metabolizing the excessive drug load needed to excrete chloramphenicol)

36
Q

Testosterone induces the drug metabolizing system T/F

A

T

37
Q

First pass effect aka

A

Presystemic metabolism

38
Q

First pass is the metabolism of drug during its passage from _______________ into _____________ _________ and it occurs with _______, ______ & _______administration

A

Absorption site

Systemic circulation

Oral drugs, skin, lungs

39
Q

In the GIT drugs are metabolized by __________________ & ______

A

the intestinal and gut wall enzymes

liver

40
Q

Drugs given __________ bypasses the first pass metabolism

A

Intravenously

41
Q

First pass effect is a determinant of

A

Bioavailability

42
Q

4 drugs with extensive first pass effect
LMNP

A

Lidocaine
Nitroglycerin
Propranolol
Morphine

43
Q

To combat first pass drugs are given
___________ or ________

A

as high oral dose

via other routes of administration

44
Q

Other factors may also affect first pass effect are 3

A

•- increased bioavailability in liver disease
•- effects of other drugs
•- individual variation in oral drug absorption

45
Q

Phase 1 drug and enzyme enzyme is

A

Alcohol

Cytochrome p450 oxidase

Dehydrogenase

46
Q

Reduction drug& enzymes

A

Eg Levodopa

Cytochrome p450 reductase

Decarboxylase

47
Q

Hydrolysis drug and example

A

Lidocaine : local anesthetic agents

Esterase
Amidase

48
Q

What do we add in phase 1

A

Functional group

49
Q

What do we add in phase 2

A

Endogenous substance

50
Q

Glucoronidation
Acetylation
Sulphation
Glycine conjugation
Methylation
Gluthathione conjugation

A

Glucoronide
Acetate
Sulphate
Glycine
Methyl group
Gluthatione

FPP Pharmacology (11 decks)

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