NR565 Complete Advanced Pharmacology Fundamentals | Complete Study
Guide Review of Key Concepts with Practice Questions & Detailed Rationales
Brand New Version 2026 | Chamberlain University | Graded A+
Exam Structure:
- Non-cumulative exam
- Multiple choice format
- Covers Weeks 1-4 content
SECTION 1: PHARMACOKINETICS & PHARMACODYNAMICS
## 1.1 Pharmacokinetics (ADME)
**Pharmacokinetics** describes what the body does to the drug – the
movement of drugs through the body over time.
### A. Absorption
- **Definition:** Movement of drug from administration site into systemic
circulation
- **Route affects rate:** IV (100% bioavailability) > IM > SubQ > PO
- **Factors affecting oral absorption:**
- Gastric pH and gastric emptying
- Food intake
- Gastrointestinal motility
, - First-pass metabolism
### B. Distribution
- **Definition:** Movement of drug from bloodstream into body tissues
- **Factors affecting distribution:**
- Blood flow to tissues
- **Protein binding** – only unbound (free) fraction is pharmacologically
active
- Tissue permeability
- **Volume of distribution (Vd)** – theoretical volume required to contain
total drug at plasma concentration
### C. Metabolism (Biotransformation)
- **Primary site:** Liver
- **Phase 1 reactions:** Oxidation, reduction, hydrolysis (primarily via
**Cytochrome P450** enzymes)
- **Phase 2 reactions:** Conjugation (glucuronidation, sulfation, acetylation)
- **First-pass effect:** Drug metabolized in liver before reaching systemic
circulation
- **CYP450 inhibitors** increase drug levels (e.g., amiodarone, cimetidine,
grapefruit juice)
- **CYP450 inducers** decrease drug levels (e.g., rifampin, phenytoin,
carbamazepine)
### D. Excretion
- **Primary routes:** Renal (kidneys), biliary, pulmonary
,- **Renal excretion** affected by kidney function, urine pH
- **Half-life (t½):** Time required for drug concentration to decrease by 50%
- Determines dosing interval
- **Steady state** reached after 4-5 half-lives
---
## 1.2 Pharmacodynamics
**Pharmacodynamics** describes what the drug does to the body – the
biochemical and physiologic effects of drugs.
### A. Receptors
- **Definition:** Proteins that transduce extracellular signals to intracellular
responses
- **Receptor states:** Active and inactive (equilibrium favors inactive state)
- **Four major receptor families:**
1. Ligand-gated ion channels
2. G protein-coupled receptors
3. Enzyme-linked receptors
4. Intracellular receptors
### B. Drug-Receptor Interactions
| Type | Definition | Example |
, |------|------------|---------|
| **Agonist** | Activates receptor, produces response | Morphine (opioid
receptor) |
| **Partial Agonist** | Produces less than maximal response | Buprenorphine
|
| **Antagonist** | Blocks receptor, no intrinsic activity | Naloxone (opioid
antagonist) |
| **Inverse Agonist** | Stabilizes inactive receptor state | Some
antihistamines |
### C. Dose-Response Relationships
- **Graded response:** Continuous, measurable effect (e.g., blood pressure,
pain scale)
- **Quantal response:** All-or-none effect (e.g., seizure, death, pregnancy)
- **Potency:** Dose required to produce effect – lower dose = higher potency
- **Efficacy:** Maximum effect a drug can produce (not the same as potency)
### D. Therapeutic Index (TI)
- **Definition:** Ratio of toxic dose (TD50) to therapeutic dose (ED50)
- **Wide TI:** Safer drug (e.g., penicillin)
- **Narrow TI:** Small margin between therapeutic and toxic doses
- **Requires therapeutic drug monitoring**
- Examples: Warfarin, Digoxin, Lithium, Phenytoin
---
Guide Review of Key Concepts with Practice Questions & Detailed Rationales
Brand New Version 2026 | Chamberlain University | Graded A+
Exam Structure:
- Non-cumulative exam
- Multiple choice format
- Covers Weeks 1-4 content
SECTION 1: PHARMACOKINETICS & PHARMACODYNAMICS
## 1.1 Pharmacokinetics (ADME)
**Pharmacokinetics** describes what the body does to the drug – the
movement of drugs through the body over time.
### A. Absorption
- **Definition:** Movement of drug from administration site into systemic
circulation
- **Route affects rate:** IV (100% bioavailability) > IM > SubQ > PO
- **Factors affecting oral absorption:**
- Gastric pH and gastric emptying
- Food intake
- Gastrointestinal motility
, - First-pass metabolism
### B. Distribution
- **Definition:** Movement of drug from bloodstream into body tissues
- **Factors affecting distribution:**
- Blood flow to tissues
- **Protein binding** – only unbound (free) fraction is pharmacologically
active
- Tissue permeability
- **Volume of distribution (Vd)** – theoretical volume required to contain
total drug at plasma concentration
### C. Metabolism (Biotransformation)
- **Primary site:** Liver
- **Phase 1 reactions:** Oxidation, reduction, hydrolysis (primarily via
**Cytochrome P450** enzymes)
- **Phase 2 reactions:** Conjugation (glucuronidation, sulfation, acetylation)
- **First-pass effect:** Drug metabolized in liver before reaching systemic
circulation
- **CYP450 inhibitors** increase drug levels (e.g., amiodarone, cimetidine,
grapefruit juice)
- **CYP450 inducers** decrease drug levels (e.g., rifampin, phenytoin,
carbamazepine)
### D. Excretion
- **Primary routes:** Renal (kidneys), biliary, pulmonary
,- **Renal excretion** affected by kidney function, urine pH
- **Half-life (t½):** Time required for drug concentration to decrease by 50%
- Determines dosing interval
- **Steady state** reached after 4-5 half-lives
---
## 1.2 Pharmacodynamics
**Pharmacodynamics** describes what the drug does to the body – the
biochemical and physiologic effects of drugs.
### A. Receptors
- **Definition:** Proteins that transduce extracellular signals to intracellular
responses
- **Receptor states:** Active and inactive (equilibrium favors inactive state)
- **Four major receptor families:**
1. Ligand-gated ion channels
2. G protein-coupled receptors
3. Enzyme-linked receptors
4. Intracellular receptors
### B. Drug-Receptor Interactions
| Type | Definition | Example |
, |------|------------|---------|
| **Agonist** | Activates receptor, produces response | Morphine (opioid
receptor) |
| **Partial Agonist** | Produces less than maximal response | Buprenorphine
|
| **Antagonist** | Blocks receptor, no intrinsic activity | Naloxone (opioid
antagonist) |
| **Inverse Agonist** | Stabilizes inactive receptor state | Some
antihistamines |
### C. Dose-Response Relationships
- **Graded response:** Continuous, measurable effect (e.g., blood pressure,
pain scale)
- **Quantal response:** All-or-none effect (e.g., seizure, death, pregnancy)
- **Potency:** Dose required to produce effect – lower dose = higher potency
- **Efficacy:** Maximum effect a drug can produce (not the same as potency)
### D. Therapeutic Index (TI)
- **Definition:** Ratio of toxic dose (TD50) to therapeutic dose (ED50)
- **Wide TI:** Safer drug (e.g., penicillin)
- **Narrow TI:** Small margin between therapeutic and toxic doses
- **Requires therapeutic drug monitoring**
- Examples: Warfarin, Digoxin, Lithium, Phenytoin
---
