Alain 1

Question 1

Slide 1: What is medicine?

Answer 1

A drug or preparation (To treat or prevent desease or to have greater welfare)

Question 2

Slide1: Is there any good Med?

Answer 2

No

Question 3

S1: Med is gd if wt?

Answer 3

1. Do what it is meant
2. No S-EFs
3. Tot Saf
4. Easy to take

Question 4

S1: Act of Morphine

Answer 4

1. Analgesic (pain reducer)
2. Tolerance (dug luog)
3. respiratory depression
4. addiction.

Question 5

S1: Wt are the dif bet Medicine,Poison, Drug

Answer 5

Medicine could be Poison or drug relate to DOSE

Question 6

S1: Wt is therapeutic index?

Answer 6

TI = (Toxic ED50)/(Benificial ED50)
The larger the better
The larger the TI the larger the safety margin.

Question 7

S1: Wt is selective toxicity?

Answer 7

Toxicity against foreign or abnormal cells

Not effect on normal cells.

Question 8

S1: How to classify drugs?

Answer 8

\+ Dif t-books have dif clas. Each has dis-adv and adv.
\+ According to:
- Pharmacological effects
- chem struc
-Target system (Tar Sys)
- Side of action

Question 9

Where do drug work?

Answer 9

Drug act on cell

Question 10

Wt are the Tar of Drug?

Answer 10

1. Macromolecules
2. Protein (Enzymes, Receptors, Transport Proteins)
3. Nucleic acids (DNA, RNA)

Question 11

Wt is binding?

Answer 11

Drug binding to the binding site of macromolecule through intermolecular bonding forces.

Question 12

Wt is pharmacodynamics?

Answer 12

The study of how drug interact with their target through binding interactions.

1. Effects (Biochemical and physiological)
2. Mechanism (correlation and chemical structure)

Question 13

Wt is pharmacokinetics?

Answer 13

To study the action of drug in the body over a period of time (ADME)

1. Absorption;
2. Distribution;
3. metabolism;
4. Excretion.

Question 14

Type of intermolecular bonding force (IBF)?

Answer 14

1. Electrostatic or ionic bond;
2. Hyd bonds;
3. Dipole-dipole or ion-dipole interactions;
4. Van der Waals;
5. Repulsive interaction;
6. Water and hydrophobic interaction

Question 15

In which case repulsive interaction occur?

Answer 15

1. Steric contact;

2. The same kind of charge

Question 16

Some bad news about Drug Dis?

Answer 16

1. Long, complex, costly, highly risky, few peer;
2. Need 12-24 years;
3. Long term research fail.
4. Not only org chem.

Question 17

Stages of Drug R&D?

Answer 17

1. Research team/objective
2. Synthesis
3. In vitro and in vivo test
4. Formulation/ Scale up Syn
5. FDA (IND)
6. Phase I/II/III
7. FDA (NDA)
8. Marketing

Question 18

Wt’re the benefit for preclinical researchers?

Answer 18

I don’t know yet.

Question 19

Hit confirmation stages

Answer 19

1. re-testing (= screening)
2. Dose response curve generation (IC50/EC50)
3. Orthogonal testing (dif essay or tech)
4. Secondaty Screening (cellular envir.)
5. Chem amenability (Easy to Syn?)
6. Intellectual property evaluation

Question 20

Hit expansion characteristics

Answer 20

1. High affinity towards the target
2. chem tractability
3. Free of Int. Pro.
4. P-450 E, P-glycoproteins
5. Not bind to Serum
6. > 100 microM
7. Permeability
8. act. in cellular assay
9. x cytotoxicity
10. x metabolized
11. Selectivity

Question 21

Wt Scie. do after Hit expantion?

Answer 21

1. Select 3-6 compound for further res.
2. Test analogous compounds.
3. QSAR.

Question 22

Hit and lead?

Answer 22

Hit > lead

* Af. confirmation and expansion, QSAR. Selected Hit will be modification to produce Lead.