FINAL FINAL
Chapter Outline
Pharmacokinetics
Routes of Administration
Drug Absorption
Drug Distribution
Free Versus Bound Drugs
Drug Metabolism
Drug Elimination
Elimination Example
Pharmacodynamics
Specimen Collection
Pharmacogenomics
Drug Categories
Cardioactive Drugs
Digoxin
Quinidine
Procainamide and N-acetylprocainamide
Disopyramide
Antibiotics
Aminoglycosides
Gentamicin
Tobramycin
Amikacin
Vancomycin
Antiepileptic Drugs
Primidone
Phenobarbital
Phenytoin and Free Phenytoin
Valproic Acid
Carbamazepine
Ethosuximide
Felbamate
Gabapentin
Lamotrigine
Levetiracetam
Oxcarbazepine
Tiagabine
Topiramate
Zonisamide
Psychoactive Drugs
Lithium
Tricyclic Antidepressants
Clozapine
Olanzapine
Immunosuppressive Drugs
Cyclosporine
Tacrolimus
Sirolimus
Everolimus
Mycophenolic Acid
Antineoplastics
Methotrexate
Bronchodilators
Theophylline
References
Key Terms
Bioavailability
Distribution
Drug half-life (T½)
Peak drug concentration
Pharmacodynamics
Pharmacogenomics
Pharmacokinetics
Therapeutic drug monitoring (TDM)
Therapeutic range
Trough drug concentration
Chapter Objectives
Discuss drug characteristics necessitating therapeutic drug monitoring.
Identify factors influencing absorption of orally administered drugs.
List factors influencing drug elimination rates.
Define drug distribution and discuss influencing factors.
Calculate volume of distribution, elimination constant, and drug half-life.
Correlate drug concentrations to pharmacokinetic and pharmacodynamic parameters.
State specimen collection and handling requirements for therapeutic drug monitoring.
Specify therapeutic categories or uses of drugs presented.
Describe potential toxic side effects/toxicity of the therapeutic drugs.
Apply knowledge of therapeutic drug monitoring to interpret laboratory results.
Therapeutic Drug Monitoring (TDM)
Measurement of prescribed drugs and metabolites in body fluids (mostly blood) to maintain therapeutic benefits.
Avoids ineffectiveness or toxicity due to concentrations outside the therapeutic range.
Essential for drugs with narrow therapeutic ranges or significant pharmacokinetic variability.
Pharmacokinetics
Studies the movement of drugs in the body including absorption, distribution, metabolism, and excretion.
Key factors that influence these processes:
Routes of Administration: Oral, IV, IM, SC, and their bioavailability.
Drug Absorption: Efficiency influenced by dissociation, solubility, and diffusion across membranes.
Drug Distribution: Movement between circulation and tissues.
Free Vs. Bound Drugs: Only free drugs can interact biologically.
Case Studies
Case Study 25.1
John, a man with renal failure, treated with digoxin for congestive heart failure, compliance questioned due to recent international travel.
Case Study 25.2
Thelma, an elderly woman with heart arrhythmia and potential medication adherence issues relating to procainamide.
Case Study 25.3
Adriene, having seizures after a period of severe diarrhea, leading to low serum phenytoin.
Pharmacodynamics
Study of the biochemical and physiological effects of drugs.
Focus on the relationship between drug concentrations and pharmacological responses.
Monitoring and Interaction
Accurate timing of specimen collection is crucial for TDM (trough before the next dose, peak within 1 hour after oral administration).
Patient age, gender, diet, co-administered drugs, and physiologic changes influence drug concentrations and effectiveness.