Pharmacokinetics and Pharmacodynamics - Advanced Pharmacology | Lecture Notes - YNetStudyHub
Advanced Pharmacology

Pharmacokinetics and Pharmacodynamics

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Explore the principles of how drugs move through the body (pharmacokinetics) and their effects on the body (pharmacodynamics), including absorption, distribution, metabolism, and excretion.

Pharmacokinetics & Pharmacodynamics – Study Guide


1. Overview

Aspect Definition Primary Question
Pharmacokinetics (PK) What the body does to a drug. How is the drug absorbed, distributed, metabolized, and eliminated?
Pharmacodynamics (PD) What the drug does to the body. How does the drug produce its therapeutic (and toxic) effects?

Both fields are essential for dose selection, predicting drug interactions, and optimizing therapy.


2. Pharmacokinetics (ADME)

2.1 Absorption

  • Goal: Transfer of drug from site of administration into systemic circulation.
  • Key Factors
    • Physicochemical: Lipophilicity, ionization (pKa), molecular size, polarity.
    • Formulation: Salt form, particle size, excipients, controlled‑release systems.
    • Physiological: Gastric pH, gastric emptying time, intestinal surface area, perfusion, presence of food or other drugs.
  • Common Routes & Characteristics
Route Onset Bioavailability (F) Advantages Limitations
Oral (PO) 30 min – 2 h 0.1–1 (first‑pass effect) Convenient, non‑invasive Variable F, GI irritation
Intravenous (IV) Immediate 1.0 Precise control, 100 % F Invasive, requires venous access
Intramuscular (IM) 5–30 min 0.5–1 Faster than PO, depot forms Pain, variable absorption
Subcutaneous (SC) 10–30 min 0.5–1 Simple, can use pumps Limited volume, variable perfusion
Inhalation Seconds–minutes 0.1–0.9 Direct lung effect, rapid Technique dependent
Transdermal Hours 0.5–0.9 Steady plasma levels Skin irritation, limited drug types

2.2 Distribution

  • Concept: Movement of drug from plasma to tissues.
  • Determinants
    • Plasma protein binding (albumin, α1‑acid glycoprotein).
    • Tissue binding (lipid affinity, melanin binding).
    • Blood flow to organs.
    • Capillary permeability (fenestrated vs. continuous).
  • Key Parameters
    • Volume of Distribution (Vd) = (Amount of drug in body) / (Plasma concentration).
      • Low Vd (<0.1 L/kg) → confined to plasma.
      • High Vd (>0.7 L/kg) → extensive tissue sequestration.
    • Fraction unbound (fu) → pharmacologically active portion.

2.3 Metabolism (Biotransformation)

  • Purpose: Convert lipophilic parent drug into more water‑soluble metabolites for excretion.
  • Phases
Phase Main Enzymes Typical Reactions
Phase I Cytochrome P450 (CYP) isoforms, FMOs, esterases Oxidation, reduction, hydrolysis
Phase II Transferases (UGTs, SULTs, GSTs, NATs) Conjugation (glucuronidation, sulfation, glutathione
Topic Concept Map
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Unit Syllabus 10 Topics
Pharmacokinetics and Pharmacodynamics
Drug Interactions
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Pharmacogenomics
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Drug Development and Approval Process
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Drug Classes and Mechanisms of Action
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Adverse Drug Reactions and Side Effects
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Pharmacotherapy in Special Populations
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Drug Resistance
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Herbal and Alternative Medicines
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Ethical and Legal Issues in Pharmacology
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