Drug Metabolism-phase 1 And 2

Question 1

What are the functional groups that are added or unmasked in during phase 1 of drug metabolism

Answer 1

OH, SH, COOH, NH2

Question 2

The reactions that occur during phase 1 reaction of drug metabolism are ?
Key(5 reactions)

Answer 2

Oxidative, reductive, hydrolytic, cyclisation and decyclisation

Question 3

The endogenous substrate groups that are conjugated to the drug during phase 2 of drug metabolism are?
Key(5 groups)

Answer 3

Glucoronide, amino acid, acetate, sulfate, glycine

Question 4

The microsomal enzymes in drug metabolism are?
Key(4 of them in the slide)

Answer 4

Epoxide hydroxylases, cytochrome p450, ugt, monooxygenases

Question 5

5 drugs that induce microsomal enzymes activity

Answer 5

Rifampicin, phenytoin, phenobarbital, ethanol, carbamazepine

Question 6

Microsomal enzymes are found in?

Answer 6

The smooth endoplasmic reticulum of liver, lungs, kidney and GI mucosa

Question 7

Non microsomal enzymes are found in?

Answer 7

The cytoplasm and mitochondria of hepatic cells and other tissues like blood

Question 8

Two groups of non microsomal enzymes

Answer 8

Esterases, amidases

Question 9

What does the enzymes of the cytochrome p450 system contain?
And where in the cell are they found ?

Answer 9

Heme containing protein
Bound to the membrane

Question 10

The CYP has how many families?
Subfamilies?
Genes?

Answer 10

18
44
57

Question 11

What CYP is involved in a larger number of drug metabolism compared to other enzymes ?

Answer 11

CYP3A4

Question 12

MAOI means?

Answer 12

Monoamine oxidase inhibitors

Question 13

CYP inhibitors examples

Answer 13

Monoamine oxidase inhibitors, cimetidine, isoniazid

Question 14

High level of a certain drug causes grey baby syndrome. What is this drug ?

Answer 14

Chloramphenicol

Question 15

Grape juice inhibits what drug ?

Answer 15

Felodipine

Question 16

First pass effects lead to ?

Answer 16

The amount of drug absorbed being lesser than the amount of drug reaching the systemic circulation

Question 17

Which method of drug administration provides the highest bioavailability for drugs ?

Answer 17

Intravenous administration

Question 18

Four drugs with very high first pass effect ?

Answer 18

Lidocaine, morphine, propranolol, nitroglycerin

Question 19

CYP inducers
Key (4 in the slide)

Answer 19

Carbamazepine, barbiturates, rifampin, cyclophosphamide

Question 20

The major and most important organ in the excretion of drugs is ?

Answer 20

Kidney

Question 21

The two drugs excreted via the bile/large intestine according to the slide are ?

Answer 21

Vancomycin and vincristine

Question 22

Drugs excreted via the saliva
Key (5+1)

Answer 22

Diazepam, lithium, caffeine,theophylline, phenytoin
Alcohol is also an honorary mention

Question 23

For drugs to be excreted via the eyes, three conditions must be met. What are they ?

Answer 23

Non protein bound, unionised and lipophilic

Question 24

The skin excretes what drugs
Key( 7 of them)

Answer 24

Cocaine, alcohol, lead, mercury, salicylic acid, benzoic acid and antipyrine

Question 25

Drugs excreted via the breasts?

Answer 25

Most drugs like aspirin

Question 26

Drugs excreted via the hair
Key (3 of them)

Answer 26

Methamphetamine, phenobarbital and methoxyphenamine

Question 27

Tubular secretion is independent of ?

Answer 27

Size and protein binding

Question 28

Drugs with very short half-life
(2 in note)

Answer 28

Noradrenaline
Cyclopa (taken 4-5 times daily)

Question 29

The half-life of methodone plus the amount of times it’s administered?

Answer 29

15 hours (long) and administered once a day

Question 30

Half-life of fluoxetine and the amount of times it’s administered

Answer 30

6 days and administered once a week

Question 31

Three substances used for alkalisation of urine

Answer 31

Acetazolamide, sodium bicarbonate and potassium citrate

Question 32

Three substances used for acidification of urine

Answer 32

Potassium phosphate, sodium phosphate and ammonium chloride

Question 33

Acidic drugs
Key (6 in the note)

Answer 33

Aspirin, penicillin, indomethacin, furosemide, methotrexate and thiazid diuretics

Question 34

Alkaline drugs
Key (7 in the note)

Answer 34

Quinine, morphine, histamine, dopamine, serotonin, prebenecid and pethidine

Question 35

What is the potency of meperidine?

Answer 35

Low potency

Question 36

What is the potency of fentanyl?

Answer 36

High potency

Question 37

What kind of antagonism exists when you mix dimercaprol and mercuric ion?

Answer 37

Chemical antagonism

Question 38

What type of antagonism exists between histamine and adrenaline?

Answer 38

Physiological antagonism