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Medicinal Chemistry > Drug Metabolism - I > Flashcards

Drug Metabolism - I Flashcards

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1
Q

Explain the basic principles of metabolism

A
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2
Q

What is pro-drug strategy

A

Metabolism could be used to activate the drug inside the body

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3
Q

What is needed for drug approval

A

The metabolites must be identified and tested

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4
Q

How many phases does the metabolism have

A

2

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5
Q

What happens in phase 1 reactions ?

A
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6
Q

Phase 1 reactions include what

A
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7
Q

What are the different examples of oxidation reaction

A
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8
Q

Give example of reduction reaction

A
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9
Q

Give example of hydrolysis reaction

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10
Q

What are the types of oxidations

A
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11
Q

What is a major route of drug metabolism

A

Hydroxylation of aromatic rings

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12
Q

Hydroxylation occurs on what

A

Activated rings that are electron rich at the ortho and para position to the substituent
Hydroxylation of deactivated ring occurs at the meta position of the substituent

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13
Q

Which position para or ortho is favored

A

Para because of steric crowdedness

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14
Q

Deactivator and Activator have what position

A

Deactivator - meta position
Activator - para and ortho position

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15
Q

What are strong activators

A
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16
Q

What are the moderate activators

A
17
Q

What are weak activator

A

Alkyl group

18
Q

What are strong and moderate Deactivator

A
19
Q

Give example of weak Deactivator

A

Halogen, the only exception that is para and ortho directing

20
Q

What are stronger activators or deactivators

A

Activators

21
Q

How does Hydroxylation occur if there is more than one substituent attached to the ring

A

Then Hydroxylation occurs most often para to the most electron donation substituent

22
Q

Aromatic Hydroxylation is catalyzed by what

A

By mixed function oxidases (MFOs)

23
Q

Mixed function oxidases are composed of what three parts

A
24
Q

Aromatic Hydroxylation reactions proceed through what

A

An epoxide intermediate called an arene oxide

25
Q
A
26
Q

Explain the detoxification of arene oxide by spontaneous rearrangement

A
27
Q

Explain the detoxification of arene oxide by hydration

A
28
Q

Explain the detoxification of arene oxide by glutathione

A
29
Q

What happens when the body gives up on detoxification of arene oxides

A

Medicinal Chemistry (11 decks)

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