4th Flashcards

1
Q

Where does drug metabolism occur

A

Liver,intestinal lumen,lung,plasma,skin,kidney

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2
Q

The most important reaction in metabolism phase 1

A

Oxidation by cytochrome p450

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3
Q

Most important conjure reaction

A

Glucuronide conjunction

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4
Q

Cytochrome p450 oxidases

A

Hepatic microsomal enzymes

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5
Q

Phase 1 oxidation reaction&raquo_space;xanthine oxidase

A

Converts xanthine >uric acid

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6
Q

Phase 1 oxidation reaction monoamine oxidase

A

Oxidizes catecholamines & serotonin

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7
Q

Phase 1 reduction nitroreductase

A

> > chloramphenicol

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8
Q

Phase 1 reduction carbonyl reductase

A

> > naloxone

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9
Q

Phase 1 hydrolysis cholinestrase

A

Ach

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10
Q

Phase 1 hydrolysis peptidase

A

> > insulin

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11
Q

What consequence of phase 1 occurs with most drugs

A

Active drugs»>inactive drugs

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12
Q

E.g on converting inactive drug(prodrugs)»active drug

A

Cortisone&raquo_space;cortisol (hydrocortisone)

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13
Q

Eg on converting active drug»another active drug

A

Codeine»morphine

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14
Q

E.g on converting active drug&raquo_space;toxic metabolite

A

Methanol&raquo_space;formaldehyde&raquo_space;retinotoxic
Paracetamol&raquo_space;NAPQI»hepatotoxic

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15
Q

Glucuronide conjunction:Drugs that enter the enterohepatic circulation

A

Estrogen (contraceptive pills are taken once daily)

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16
Q

Non-glucuronide conjunction: sulphate formation

A

Steroids

17
Q

Non-glucuronide conjunction: glycine conjunction

A

Salicylic acid

18
Q

Non-glucuronide conjunction : Glutathione conjunction

A

Ethacrynic acid

19
Q

Non-glucuronide conjunction : acetyl conjugation (slow & rapid acetylation)

A

Isoniazid

20
Q

Consequence of phase 2 is inactivation of most drugs except for

A

Morphine is partially&raquo_space;Morphine-6-glucuronide(active)

21
Q

E.g on drugs metabolized by phase 2 then by phase 1

A

Isoniazid