HNG 540 EXAM 1 STUDY GUIDE
Pharmaceutical phase - Answers -Disintegration of dosage form and dissolution of
active substance
Pharmacokinetic phase - Answers -Absorption, distribution, metabolism, and excretion
of drug
Pharmacodynamic phase - Answers -Drug-receptor interaction in target tissue
Advantages of oral drug delivery - Answers -- Patient acceptability and compliance,
- Large surface area,
- Rich blood supply,
- Prolonged retention,
- Zero-order release,
- Commercial advantages
Disadvantages of oral drug delivery - Answers -- Variability,
- Adverse reactions,
- Adverse environments effects,
- High metabolic activity,
- Extreme pH,
- Intestinal motility,
- Mucus barrier,
- P-glycoprotein efflux,
- Impermeable epithelium
Drug release profiles - Answers -- Immediate release,
- Delayed release,
- Repeat-action,
- Sustained release,
- Controlled release
Bioavailability - Answers -Rate and extent to which an active agent is absorbed and
available at the site of action and yields a therapeutic response
Physicochemical properties influencing drug absorption - Answers -- Lipid solubility,
- pKa,
- Molecular weight and volume,
- Aqueous solubility- dissolution rate limited?,
- Chemical stability
Lipinski's Rule of 5 - Answers -- Molecular weight < 500g/mol,
- Log K < 5,
- < 5 hydrogen bond donors,
, - < 10 hydrogen bond acceptors
Physiological factors of oral drug absorption - Answers -- Solubility,
- GI motility,
- Membrane permeability,
- Differential drug absorption,
- Gut wall metabolism,
- Blood flow,
- Luminal contents,
- Gastric/intestinal secretions
Prodrugs - Answers -A medication that is metabolized into a pharmacologically active
drug
BCS Class I - Answers -High solubility, high permeability (metoprolol)
BCS Class II - Answers -Low solubility, high permeability (carbamazepine)
BCS Class III - Answers -High solubility, low permeability (atenolol)
BCS Class IV - Answers -Low solubility, low permeability (ritonavir)
Four stages of drug development - Answers -1. Discovery,
2. Pre-clinical,
3. Clinical,
4. Post-clinical
Discovery phase - Answers -Disease state, target identification, target validation,
creation of new drug molecule, candidate selection, safety and efficacy
Pre-clinical phase - Answers -Drug substance scale up, candidate selection, pre-clinical
testing, IND application
Clinical phase - Answers -1. Dosing to 10-15 healthy individuals to assess safety and
PK,
2. Dosing to 20-100 patients with the disease assess proof of concept,
3. Testing on particular indication in > 1000 patients,
4. Post-marketing approval studies in 300-3000 volunteers
Post-clinical phase - Answers -New Drug Application (NDA), FDA review of NDA
Brand name drug requirements - Answers -1. Chemistry,
2. Manufacturing,
3. Controls,
4. Labeling,
5. Testing,
Pharmaceutical phase - Answers -Disintegration of dosage form and dissolution of
active substance
Pharmacokinetic phase - Answers -Absorption, distribution, metabolism, and excretion
of drug
Pharmacodynamic phase - Answers -Drug-receptor interaction in target tissue
Advantages of oral drug delivery - Answers -- Patient acceptability and compliance,
- Large surface area,
- Rich blood supply,
- Prolonged retention,
- Zero-order release,
- Commercial advantages
Disadvantages of oral drug delivery - Answers -- Variability,
- Adverse reactions,
- Adverse environments effects,
- High metabolic activity,
- Extreme pH,
- Intestinal motility,
- Mucus barrier,
- P-glycoprotein efflux,
- Impermeable epithelium
Drug release profiles - Answers -- Immediate release,
- Delayed release,
- Repeat-action,
- Sustained release,
- Controlled release
Bioavailability - Answers -Rate and extent to which an active agent is absorbed and
available at the site of action and yields a therapeutic response
Physicochemical properties influencing drug absorption - Answers -- Lipid solubility,
- pKa,
- Molecular weight and volume,
- Aqueous solubility- dissolution rate limited?,
- Chemical stability
Lipinski's Rule of 5 - Answers -- Molecular weight < 500g/mol,
- Log K < 5,
- < 5 hydrogen bond donors,
, - < 10 hydrogen bond acceptors
Physiological factors of oral drug absorption - Answers -- Solubility,
- GI motility,
- Membrane permeability,
- Differential drug absorption,
- Gut wall metabolism,
- Blood flow,
- Luminal contents,
- Gastric/intestinal secretions
Prodrugs - Answers -A medication that is metabolized into a pharmacologically active
drug
BCS Class I - Answers -High solubility, high permeability (metoprolol)
BCS Class II - Answers -Low solubility, high permeability (carbamazepine)
BCS Class III - Answers -High solubility, low permeability (atenolol)
BCS Class IV - Answers -Low solubility, low permeability (ritonavir)
Four stages of drug development - Answers -1. Discovery,
2. Pre-clinical,
3. Clinical,
4. Post-clinical
Discovery phase - Answers -Disease state, target identification, target validation,
creation of new drug molecule, candidate selection, safety and efficacy
Pre-clinical phase - Answers -Drug substance scale up, candidate selection, pre-clinical
testing, IND application
Clinical phase - Answers -1. Dosing to 10-15 healthy individuals to assess safety and
PK,
2. Dosing to 20-100 patients with the disease assess proof of concept,
3. Testing on particular indication in > 1000 patients,
4. Post-marketing approval studies in 300-3000 volunteers
Post-clinical phase - Answers -New Drug Application (NDA), FDA review of NDA
Brand name drug requirements - Answers -1. Chemistry,
2. Manufacturing,
3. Controls,
4. Labeling,
5. Testing,
