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MPharm 2 - PH2114 > metabolism > Flashcards

metabolism Flashcards

1
Q

What type of reactions are carried out during phase 1 metabolism?

A

Oxidation
Reduction
Hydrolysis

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2
Q

What is phase 1 metabolism?

A

Chemically diverse small molecules are converted (transformed) generally to more polar compounds

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3
Q

Give some examples of oxidation reactions carried out in phase 1 metabolism?

A 
Oxidation
Dehalogenation
Deamination
Dealkylation
Epoxide formation
Hydroxylation
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4
Q

Which enzymes are responsible for aromatic hydroxylation reactions in phase 1 metabolism?

A

CYP450

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5
Q

How can aromatic hydroxylation be slowed down or blocked?

A

Substitute the phenyl ring with a para-fluorine or para-chlorine
- deactivates the ring

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6
Q

How does the half life change for drugs that have had halogens substituted on to their phenyl ring?

A

Diclofenac - half life = 1 hour

Fenclofenac - half life = > 20 hours ( has para chlorine)

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7
Q

Which enzymes are responsible for aliphatic hydroxylation reactions in phase 1 metabolism?

A

CYP450

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8
Q

How is diazepam metabolised to temazepam?

A

Aliphatic hydroxylation

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9
Q

How is carbemazepine metabolised to carbamazepine 10,11-epoxide?

A

Epoxide formation

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10
Q

How is diazepam metabolised to nor-diazepam?

A

Oxidative N-dealkylation

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11
Q

How is codeine metabolised to morphine?

A

Oxidative O-dealkylation

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12
Q

How is amphetamine metabolised to phenylacetone?

A

Deamination

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13
Q

Which enzymes are responsible for deamination reactions in phase 1 metabolism?

A

CYP450

Amine oxidases

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14
Q

How is imipramine metabolised to imipramine N-oxide?

A

N-oxidation

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15
Q

Which enzymes are responsible for N-oxidation reactions in phase 1 metabolism?

A

Microsomal amine oxidase

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16
Q

Which enzymes are responsible for S-oxidation reactions in phase 1 metabolism?

A

CYP450

Flavoprotein oxidase

17
Q

How is omeprazole metabolised to omeprazole sulphone?

A

S-oxidation

18
Q

What proportion of ingested ethanol is metabolised by alcohol dehydrogenase?

A

Two thirds

19
Q

What proportion of ingested ethanol is metabolised by CYP2E1?

A

One third

20
Q

How is ethanol metabolised to acetaldehyde?

A

Alcohol oxidation

21
Q

What causes hepatotoxicity after excessive alcohol consumption?

A

Excessive amounts of acetaldehyde generated from ethanol metabolism

22
Q

How is chloramphenicol metabolised?

A

Aliphatic dehalogenation

23
Q

Give some examples of reduction reactions that take place in phase 1 metabolism

A

Azo reduction
N-oxide reduction
NO2 reduction
Ketone reduction

24
Q

Which enzymes are responsible for NO2 reduction reactions in phase 1 metabolism?

A

Gut microflora

  • anaerobic
  • NOT OXIDATIVE!!
25
Q

How is nitrazepam converted to 7-amino-nitrazepam in phase 1 metabolism?

A

NO2 reduction

26
Q

Which enzymes are responsible for azo reduction reactions in phase 1 metabolism?

A

Gut microflora

  • anaerobic
  • NOT OXIDATIVE!!
27
Q

why are aliphatic halides not often used in drugs ?

A

they are too reactive

MPharm 2 - PH2114 (32 decks)

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