ADME overview

Question 1

Absorption requires SOLUBILILZATION. TRUE OR FALSE?

Answer 1

TRUE

Question 2

Drugs that are more hydrophilic are more likely to be dissolved than those that are hydrophobic. TRUE OR FALSE

Answer 2

TRUE

Question 3

Ionization does not determine solubilization. TRUE OR FALSE?

Answer 3

FALSE

Question 4

Ph does not determine rate of ionization. TRUE OR FALSE?

Answer 4

FALSE

Question 5

What is thermodynamic solubility?

Answer 5

Refers to how soluble a drug is if left in solution to come to equilibrium

Question 6

What is kinetic solubility?

Answer 6

Refers to how quickly a drug dissolves in solution

Question 7

What is pinocytosis transport of drug?

Answer 7

When cell membrane invaginates the drug

Question 8

What is Paracellular transport pf drug?

Answer 8

Transport of drug between different cells

Question 9

What is Lipid diffusion transport of drug?

Answer 9

Movement of drug directly across cell membrane

Question 10

What is Aquaporin transport of drug?

Answer 10

Drugs can move across ion channels

Question 11

What is carrier transport of drug?

Answer 11

These are proteins that can transport certain drugs

Question 12

What does fick’s law describe?

Answer 12

The flux of drug across the membrane i.e how many moles of the drug is moving across the membrane per unit time

Question 13

Absorption is determined by POLARITY AND LIPOHILICITY. TRUE OR FALSE?`

Answer 13

TRUE

Question 14

What re the factors affecting GI absorption?

Answer 14

1. Anatomical factors
2. pH
3. Permeability and solubility
4. Binding to other material in GI tract
5. Gastric emptying
6. Metabolism

Question 15

What is permeability dependent on?

Answer 15

1. Solubility in membrane lipid
2. Mobility in membrane lipid
3. Molecular mass ( Reduces permeability)

Question 16

what is the pH partition hypothesis?

Answer 16

uncharged molecules preferentially cross membrane (there are exceptions to this)

Question 17

what is distribution?

Answer 17

The reversible transfer of a drug between different tissues in the body

Question 18

Many drugs exert their effect in interstitial water or intracellular water. TRUE OR FALSE?

Answer 18

TRUE

Question 19

Only unbound drug moves between compartments.TRUE OR FALSE?

Answer 19

TRUE

Question 20

Blood-brain barrier restricts access to CNS. TRUE OR FALSE?

Answer 20

TRUE

Question 21

Blood-brain barrier DOES NOT prevents
water-soluble drugs from
reaching the CNS. TRUE OR FALSE?

Answer 21

FALSE

Question 22

What are Perfusion limited drugs?

Answer 22

These are drugs where the membrane presents little permeability barrier - this is the case for lipophilic drugs

Question 23

What are permeability limited drugs?

Answer 23

Are drugs where membrane present significant permeability barrier- this is the case for polar drugs that are affected by charge

Question 24

Blood flow does not control the distribution of drug, its the permeability of the membrane to those drugs that affects their distribution. TRUE OR FALSE?

Answer 24

TRUE

Question 25

Drugs may bind to blood cells, tissue proteins and plasma protein. TRUE OR FALSE?

Answer 25

TRUE

Question 26

What does serum albumin mostly bind?

Answer 26

Acidic drugs

Question 27

What doe a1 acid glycoprotein mostly bind?

Answer 27

Basic drugs

Question 28

Only unbound drug exerts a pharmacodynamic effect. TRUE OR FALSE?

Answer 28

TRUE

Question 29

What does the one compartment model mean?

Answer 29

The drug can diffuse into all the tissues at the same time

Question 30

What does the two compartment model mean?

Answer 30

Drug can distribute into one compartment more rapidly than in another compartment

Question 31

Elimination is both metabolism and excretion. TRUE OR FALSE?

Answer 31

TRUE

Question 32

What is metabolism?

Answer 32

The conversion of drug to another chemical

Question 33

Which organ is the major site of metabolism?

Answer 33

Liver

Question 34

What occurs in Phase I in metabolism?

Answer 34

conversion to more reactive form to allow conjugation

Question 35

What occurs in Phase II in metabolism?

Answer 35

conjugation with another biomolecule to increase solubility to allow excretion

Question 36

Some drugs may be excreted unchanged Some drugs may not undergo phase II ARE THESE STATEMENTS TRUE OR FALSE?

Answer 36

TRUE

Question 37

Oxidation and reduction both occurs in phase 1 of metabolism. TRUE OR FALSE?

Answer 37

TRUE

Question 38

95% of reactions does not occur by cytochrome P450. TRUE OR FALSE?

Answer 38

FALSE

Question 39

List the different types of isoforms of cyp and describe their uses.

Answer 39

3A4 - most commonly associated with drug metabolism 2D6 - shows greatest variability between different people

Question 40

Apart from cytochromes there no other enzymes that can catalyze metabolism. TRUE OR FALSE?

Answer 40

FALSE

Question 41

``` Biotransformation can render a drug more reactive: - aids conjugation - makes more harmful TRUE OR FALSE? ```

Answer 41

TRUE

Question 42

What is Excretion?

Answer 42

the irreversible removal of drug from the | body

Question 43

List the different Routes of excretion

Answer 43

- Urine - Bile - Sweat - Milk - Exhaled breath

Question 44

What are the Processes involved in | renal excretion?

Answer 44

1. Filtration in Renal corpuscle 2. Active secretion in the tubule 3. Reabsorption in the tubule