MODULE 6 PART 3: DRUG METABOLISM BIOTRANSFORMATION OF DRUGS

Question 1

Polar H2O soluble must be first metabolized to be excreted. True or False?

Answer 1

False

Question 2

Polar H2O soluble can be excreted via ?

Answer 2

Kidneys –> urine

Question 3

Non-polar lipid soluble must be first metabolized. True or False?

Answer 3

True –> to more polar and H2O soluble form before excretion thru urine or bile

Question 4

What are the 5 consequences of Biotransformation ?

Answer 4

1. Inactivation
2. Activation
3. Modification of activity
4. Conjugation (detoxification)
5. Lethal synthesis

Question 5

Identify the consequence of biotransformation with the given data:

• Drug which an active drug is converted to an inactivate metabolite

Answer 5

Inactivation

Question 6

Identify the consequence of biotransformation with the given data:

• When an active drug (pro-drug) is converted to a pharmacologically active 1st metabolite

Answer 6

Activation

Question 7

Identify the consequence of biotransformation with the given data:

• Following conversion of an active drug to a metabolite that also possess pharmacologic activity

Answer 7

Modification of activity

Question 8

Identify the consequence of biotransformation with the given data:

• When a molecule that is more polar is attach to apparent compound or to its metabolite with marked inc. in overall H2O solubility & complete loss of a pharma activity.

Answer 8

Conjugation (detoxification)

Question 9

Identify the consequence of biotransformation with the given data:

• When drug is incorporated into a normal cellular metabolic pathway that leads to failure of the reaction sequence & cellular death will then occur

Answer 9

Lethal synthesis (intoxication)

Question 10

Identify the active-inactive resulting drug with the given data:

• Pentobarbital

Answer 10

Pentobarbital alcohol

Question 11

Identify the active-inactive resulting drug with the given data:

• Phenobarbital

Answer 11

P-hydroxyphenobarbital

Question 12

Identify the active-inactive resulting drug with the given data:

• Phenytoin

Answer 12

P-hydroxyphenyl derivative

Question 13

Identify the active-inactive resulting drug with the given data:

• Amphetamine

Answer 13

Phenylacetone

Question 14

Identify the active-inactive resulting drug with the given data:

• Phenothiazine

Answer 14

Phenothiazine sulfoxide

Question 15

Identify the active-inactive resulting drug with the given data:

• Procaine

Answer 15

PABA (paraaminobenzoic acid)

Question 16

Identify the active-active resulting drug with the given data:

• Phenylbutazone

Answer 16

Oxyphenbutazone

Question 17

Identify the active-active resulting drug with the given data:

• Aspirin

Answer 17

Salicylic acid

Question 18

Identify the active-active resulting drug with the given data:

• Propanolol

Answer 18

4-hydroxypropanolol

Question 19

Identify the active-active resulting drug with the given data:

• Diazepam

Answer 19

N-desmethyldiazepam

Question 20

Identify the active-active resulting drug with the given data:

• Primidone

Answer 20

Phenobarbital

Question 21

Identify the active-active resulting drug with the given data:

• Spironolactone

Answer 21

Canrenone

Question 22

Identify the inactive-active resulting drug with the given data:

• Protozil

Answer 22

Sulfanilamide

Question 23

Identify the inactive-active resulting drug with the given data:

• Hetacillin

Answer 23

Ampicillin

Question 24

Identify the inactive-active resulting drug with the given data:

• Parathion

Answer 24

Paraoxon