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Pharmacology > Drug Metabolism > Flashcards

Drug Metabolism Flashcards

1
Q

Drug metabolism aka _______ is the chemical modification of drugs in the body which transforms ______ into produce more ____, ____ which can easily be excreted.

A

Bio transformation
Relatively lipophilic agents
Polar, hydrophilic products

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2
Q

Drug metabolism involves chemical activation of inactive drugs to their active substrates eg
____ to ____
______ to _____

A

Enalapril to enalaprilat
Codeine to morphine

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3
Q

Outcome of drug metabolism:
______
______
______

A

Inactivation
Active metabolite
Active drug

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4
Q

Drugs are mainly _____

A

Lipophilic

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5
Q

Drug metabolism occurs mainly in the ___, and involves both ____ and ___ enzymes.

A

LIVER
Microsomal and non-microsomal enzymes

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6
Q

Drug metabolism occurs in almost all organs of the body and other relatively common sites are

Mnemonic: Let’S Get Kids(sounds like let’s get this) Hint: 4 sites

A

Lungs
Kidney
Skin
GIT

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7
Q

Drug metabolism is categorized mainly into ___ main reactions, namely:

A

Two
Phase I metabolism
Phase II metabolism

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8
Q

Phase 3 reaction involves removal of drugs that have undergone phase 1 and or 2 reactions by transporters called _____

A

P-glycoprotein

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9
Q

Phase I reactions are also knows as ____/_____ reactions

A

Functionalization
Non-synthetic

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10
Q

Phase I reactions convey a parent compound into a ____ metabolite by _______

A

More polar hydrophilic
Adding/unmasking functional groups

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11
Q

Phase I reactions include:

A

Oxidative
Reductive
Hydrolytic
Cyclization
Decyclization

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12
Q

After phase I reactions, drugs must go through phase 2 to be sufficiently polar to be excreted readily. (True/False)

A

False, after phase I reactions, drugs may be sufficiently polar to be excreted readily

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13
Q

Phase 2 reactions involve conjugation with _____ to further increase aqueous solubility.

A

Endogenous substrates

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14
Q

Phase 2 reactions include:

Mnemonic: SAGGA

A

Glucuronide
Sulfate
Acetate
Amino acid
Glycine

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15
Q

Phase 2 is referred to as the ______ step in the metabolism process.

A

True detoxification step because the drug is more likely to be excreted.

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16
Q

Microsomal enzymes are located on the ______ in what organs?
Mnemonic: KILL

A

Smooth Endoplasmic Reticulum
Liver, kidney, lungs, intestinal mucosa.

17
Q

Examples of microsomal enzymes:

A

Monooxygenases
Cytochrome P450
UGT- UDP glucuronosyltransferase enzyme
Epoxide hydroxylases

18
Q

Microsomal reactions are involved in phase I and II reactions. (True/False)

A

True

19
Q

Non-microsomal enzymes are found in _____, ____ and _____ . Examples are:

A

•Cytoplasm
Mitochondria
Plasma
•Esterases , amidases

20
Q

______ metabolize the widest range of drugs and also act on structurally unrelated drugs.

A

Microsomal cytochrome P450 monooxygenases family of enzymes

21
Q

Cytochrome P450 system involves enzymes that are ______ and _____

A

Membrane bound
Heme-containing protein

22
Q

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

A

57
18
44

23
Q

CYP____ is involved in a significantly higher number of drug metabolism compared to other enzymes.

A

CYP3A4

24
Q

Example of enzymes in category of human CYP family include:

A

CYP2D6
CYP2C19
CYP2C9
CYP3A4
CYP3A5

25
Q

The cytochrome P450 system enzymes are named based on ____.

A

The family

26
Q

In CYP3A4:
3 stands for
A stands for
4 stands for

A

3-Family
A-Subfamily
4-Gene number

27
Q

Biological factors affecting drug metabolism:

(7 in number)

A

Species/Strain differences (fast acetylators vs slow acetylators)
Disease state
Sex differences
Circadian Rhythm
Age
Diet
Pregnancy

28
Q

Modification of drug metabolism involves:

A

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

29
Q

Effects of inhibition of CYP enzymes:

A

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

30
Q

Examples of CYP enzyme inhibitors:

A

Cimetidine
Isoniazid
Monoamine oxidase inhibitor-Phenelzine

31
Q

Effects of induction of CYP enzymes:

A

Increased degradation of co-medicated drugs
Decreased drug plasma concentrations
Loss of pharmalogical effects
Risk of therapeutic failure

32
Q

Examples of CYP enzymes inducers:

A

Barbiturates
Carbamazepine
Rifampicin
Cyclophosphamide

33
Q

Testosterone is an enzyme ___

A

Inducer

34
Q

Grape juice inhibits _____

A

Felodipine

35
Q

In pregnancy, there is _____ level of hormone inducer or inhibitors.

A

Increased

36
Q

Progesterone is an enzyme ____

A

Inducer

37
Q

Pertaining to pregnancy, _____ contains metabolizing enzymes

A

Placenta

38
Q

Drugs with extensive first pass effect include: (Hint: LMNP)

A

Lidocaine
Propranolol
Nitroglycerin
Morphine

39
Q

Factors affecting first pass effect:

A

Increased bioavailability in liver disease
Effects of other drugs
Individual variation in oral drug absorption

Pharmacology (6 decks)

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