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.