Intro To Drug Diacovery

Question 1

Pharmacokinetics

Answer 1

Absorption
Distribution
Metabolism
Excretion

Question 2

Drug screening

Answer 2

Aims to define the pharmacologic profile of the compound

Results in a lead conpound

Question 3

Safety and toxicity testing
Type of test:

Answer 3

Acute toxicity
Subacute toxicity
Chronic toxicity
Effect on reproductive performance
Carcinogenic potential
Mutagenic potential

Question 4

Acute toxicity

Answer 4

2 species
2 routes

Determine the No-effect & Max tolerated dose
Determine the acute dose that is lethal in approx 50% of animals

Question 5

Subacute or Subchronic toxicity

Answer 5

3 doses
2 species
2 weeks to 3 mos
Determine biochemical, physiologic effects

Question 6

Chronic toxicity

Answer 6

Rodent & atleast 1 non-rodent species for 6 mos
Required when drug is intended to be used in humans for prolonged periods
Run concurrently with clinical trials
Determine same endpoints as subacute toxicity tests

Question 7

Effect on reproductive performance

Answer 7

2 species:
1 rodent & rabbits

Question 8

Carcinogenic potential

Answer 8

2 years
2 species
Determine gross & histologic pathology

Question 9

Mutagenic potential

Answer 9

Test effects on genetic stability & mutations in bacteria
Ames test or mammalian cells in culture

Question 10

Phase 1

Answer 10

20-100 healthy subjects
Safety & pharmacokinetic profile

Question 11

Phase 2

Answer 11

100-200 subjects with target disease
Efficacy

Question 12

Phase 3

Answer 12

Thousands of subjects with target disease
Efficacy & Safety

Question 13

Phase 4

Answer 13

Post marketing surveillance
Monitoring the Safety under actual conditions