WK5AssgnSloneO - Copy|Principles of Pharmacology: Pharmacokinetics and Pharmacodynamics:

Prodrug ● A compound that is inactive when administered and converts to active form via metabolism Active drug ● Administered as active and is inactivated when metabolized. 4 Phenotypes of Metabolizers ● UM: Ultrarapid responders ○ Active drugs: ineffective ○ Prodrug: toxic ● EM: Extensive Responders ○ Active drug & prodrug: possibly therapeutic ● IM: Intermediate Responders ○ Active drug & prodrug: possibly therapeutic ● PM: Poor Responders ○ Active drug: toxic ○ Prodrug: ineffective 4 phases of FDA Approval ● 1) Discovery and development ○ In the chemistry lab ● 2) Preclinical Research ○ Must be sure that drug is not toxic before testing it on people ● 3) CLinical Research/Trials (4 phases in itself) ○ Phase 1: 20-100 healthy volunteers (70% pass) ○ Phase 2: several hundred patients with disease/condition. Focuses on efficacy and side effects. 1/3 of drugs pass. ○ Phase 3: 300-3,000 patients with the disease. Takes 1-4 years. 25-30% pass. Focuses on efficacy an