Pharmacology and therapeutics 5

Question 1

Explain why drug metabolism is needed. Which organ is the main organ where drug metabolism is used the most.

Answer 1

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Question 2

What is ‘first pass’ metabolism(hepatic and pre-hepatic), describe why the hepatic one is so relevant, explain the consequences of having an extensive ‘first pass’ metabolism, and how this can be resolved.

Answer 2

pg1

Question 3

What other organs can metabolism also occur in

Answer 3

pg1

Question 4

What are phase I metabolic changes generally about, explain roles in drug activation , drug polarity and lipophilicity changes

Answer 4

pg 2

Question 5

Metabolic . change is split into phases. Identify the different types of metabolic change and whuch phase they belong to. Explain what eavch phase is in general.

Answer 5

pg 2

Question 6

Where do phase 1 metabolic changes primarily occur)

Answer 6

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Question 7

Describe what the cytochrome p450 enzyme system is and the range of processes it is a part of.

Answer 7

pg 3

Question 8

Some drugs can inhibit or induce CYP450 (T/F), Is this good or bad and why

Answer 8

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Question 9

Describe the process of Cytochrome P450 Mediated Oxidation

Answer 9

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Question 10

Describe four CYP450 oxidative reactions, two where the drug is activated from its prodrug form and two where the drug loses it’s pharmacological activity

Answer 10

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Question 11

Describe, and explain two non-CYP450 oxidation reactions. Explain the consequences of a deficiency in one of the enzymes. Describe the location of all the enzyme and/or enzyme systems relevant to phase 1 oxidation.

Answer 11

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Question 12

Describe and explain example reductive reaction. Where do reductive reactions usually occur, and why. Which type of enzymes them out. Describe and explain an example of a hydrolysis reaction. What is the name of the enzyme that carries out hydrolysis.

Answer 12

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Question 13

List the type of reactions in phase 2 metabolism. What happens to the activity, solubility, polarity and extractability of the conjugate formed. Describe thwe genral feature of the conjugating agent.

Answer 13

pg 7

Question 14

For the different phase 2 reactions, name the conjugating agent and the target functional group. Describe the usual attribute of the conjugating agents. Describe the most common phase 2 reaction and identify a types that is considered to be one of the most important and explain why.

Answer 14

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Question 15

Describe and explain an example of a glucuronidation reaction, include an explanation of the consequences of such a reaction.

Answer 15

pg 8

Question 16

Describe , and explain examples of acetylation, methylation and sulphation reactions, with descriptions where/ if relevant of the consequences of the reaction and/ or a description of features of the products

Answer 16

pg 9

Question 17

Describe the structure of glutathione and explain the sheer importance this structure

Answer 17

pg 10

Question 18

Explain the importance of drug metabolism

Answer 18

pg 11

Question 19

Explain in what situation you will administer enteric-coated and soluble aspirin

Answer 19

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