Module 4a: Pharmaceutically Active Components

Question 1

The study of interactions btwn drug and organism.

Answer 1

Pharmacology! :D

Question 2

The study of how a drug affects the organsim.

Answer 2

Pharmacodynamics!

Question 3

The study of how the organism affects the drug.

Answer 3

Pharmacokinetics!

Question 4

Pharmacodynamics can be affected by: (3)

Answer 4

1. Disease state or disorder
2. Age
3. drug-drug interactions (polypharm)

Question 5

Pharmacodynamics

How do drugs bind to receptors? (4)

Answer 5

1. Intermolecular forces
2. Covalent bonds
3. Hydrophobic interactions
4. Stereospecific interactions (enantiomers)

Question 6

What are properties of drugs? (3)

Answer 6

1. Affinity (binding)
2. Efficacy (desired effect)
3. Potency (compare relative affinity to competing drugs)

*drugs act as ligands that bind to the receptors

Question 7

Categories of drugs include: (4)

Answer 7

1. Agonist
2. Antagonist
3. Competitive
4. Non-competitive

Question 8

Pharmacokinetics

Answer 8

ADME

Question 9

What determines the time to maximum concentration at the receptor to produce its peak effect?

Answer 9

Absorption rate.

Question 10

What term describes how much of the drug administered that is actually absorbed?

Answer 10

Bioavailability.

*usually talking about oral admin

Question 11

What are some factors that affect bioavailability?

Answer 11

1. MW of drug
2. drug formation
3. drug stability (pH)
4. 1st pass metab
5. blood flow
6. gastric emptying (food slows process)
7. GI motility
8. Drug interactions (polypharm?)

Question 12

Distribution

What affects distribution of the drug throughout the body?

Answer 12

1. blood
2. TBW
3. extracellular fluids
4. lymph fluids
5. CSF
6. protein-binding
7. drug solubility properties

Question 13

Hydrolysis, REDOX reactions (CYP450s), activating prodrugs are all examples of _____?

Answer 13

Metabolism of drugs.

*has potential to form toxic metabolites :(

Question 14

Kidneys, feces, lungs, sweat glands are all examples of _____?

Answer 14

Excretion of drugs.

Question 15

Drug Development

What % of drugs make it out of clinical testing?

Answer 15

~10%
*90% fail

Question 16

When do most drugs fail clinical trials?

What phase?

Answer 16

Discovery.

Question 17

What is the “Lipinski Rule of 5” used for?

Answer 17

Tool to describe drug potential for a new chemical entity (NCE) & its bioavailability.

Question 18

If you violate only 1 rule of Lipinski Rule of 5, can this drug be deemed orally bioavailable?

Answer 18

NO!

Question 19

What are Lipinski Rule of 5 based upon?

Answer 19

1. H bond donors (amines, alcohols) (no more than 5)
2. H bond acceptors (F, O, N) (no more than 10)
3. MW (less than 500g/mol)
4. Calculated partition coefficient (cLogP 5 or less)

Question 20

If I develop a drug that is half lipophilic & half hydrophilic, is it safe to say it will move across cell membranes well?

Answer 20

YES! This is ideal.

*So is a LMW and low cLogP.

Question 21

What functional groups have been linked to increases in toxicity d/t their metabolite production? (5) And what is this called?

Answer 21

1. Aromatic anilines
2. nitroaromatics
3. polycyclic aromatic hydrocarbons
4. aliphatic halides (group 7)
5. thiophenes (superman ring)

STRUCTURAL ALERTS