Theraputic Drug Monitoring Flashcards
What is an individualized system for drug administration and management?
Therapeutic Drug Monitoring (TDM)
What does TDM measure during therapy?
Drug concentrations
What are the goals of TDM?
Achieve therapeutic range
Determine timing and dosage
Ensure compliance
Monitor drug interactions
Assess preventive effects
When is a steady-state drug level reached?
When administration equals metabolism and excretion rates
How is the decline rate of a single drug dose expressed?
Half-life
What are the three blood concentration levels in TDM?
Subtherapeutic
Therapeutic
Toxic
What is the release of an active ingredient from a dose form called?
Liberation
What is drug uptake into systemic circulation called?
Absorption
What are the mechanisms of drug absorption?
Diffusion
Transport
Pinocytosis
What is first-pass elimination/metabolism?
Hepatic metabolism after absorption
How long does drug distribution take?
30 minutes to 2 hours
What is the term for the absorbed drug available for distribution?
Bioavailability
What is the transformation of a parent drug into water-soluble metabolites?
Metabolism
What are the routes of drug elimination?
Urine
Feces
Sweat
Saliva
What is the mathematical study of drug disposition over time?
Pharmacokinetics
What type of kinetics depends on drug concentration?
First-order kinetics
What type of kinetics has a constant elimination rate?
Zero-order kinetics
What factor determines zero-order kinetics?
Liver metabolic capacity
What specimens are used in TDM?
Serum
Plasma
Urine metabolites
Whole blood (cyclosporine, tacrolimus)
Why should serum separator tubes (SSTs) be avoided?
They interfere with drug measurement
When should drug levels be measured?
After steady state is achieved
When is trough concentration measured?
Immediately or 30 minutes before the next dose
What does trough concentration indicate?
Lowest drug level in the blood
When is peak concentration measured?
One hour after oral dose (except digoxin, measured after 8 hours)
Why is peak concentration measured?
To assess drug toxicity
When is peak concentration measured for IV infusion?
After infusion completion
What reaction detects acetaminophen in urine?
Indophenol blue formation with o-cresol
What reaction detects salicylate in the Trinder assay?
Colored complex formation with ferric nitrate
What method uses drug-specific antibodies for detection?
Immunoassay
What are two common immunoassay techniques?
EMIT (Enzyme-Multiplied Immunoassay Technique)
FPIA (Fluorescence Polarization Immunoassay)
What specimen is preferred for chromatography?
Urine
What chromatography techniques are used in TDM?
Thin-Layer Chromatography (TLC)
High-Performance Liquid Chromatography (HPLC)
Gas Chromatography-Mass Spectrometry (GC-MS, gold standard)
What substances are detected using chromatography?
Tricyclic antidepressants
Volatile drugs
What drug classifications are monitored in TDM?
Cardioactive
Antibiotics
Antiepileptics
Psychoactive
Bronchodilators
Immunosuppressives
Antineoplastics
Anti-inflammatory (Analgesics)
Neuroepileptics
What are the four classifications of cardioactive drugs and their mechanisms?
Class I: Rapid sodium channel blockers (Quinidine, Procainamide, Lidocaine)
Class II: Beta receptor blockers (Propranolol)
Class III: Potassium channel blockers (Amiodarone)
Class IV: Calcium channel blockers (Verapamil)
What are the uses of Digoxin?
Atrial arrhythmia
Congestive Heart Failure (CHF)
What is the mechanism of action of Digoxin?
Inhibits Sodium-Potassium Adenosine Triphosphatase (Na-K-ATPase)
When is the peak serum level of Digoxin reached post-oral dose?
8 hours
What is the half-life of Digoxin?
38 hours
What is the therapeutic range of Digoxin?
0.5-2 ng/mL
What are the toxic effects of Digoxin?
Nausea
Vomiting
Visual disturbances
Premature ventricular contractions
Atrioventricular (AV) node blockage
What is another name for Lidocaine?
Xylocaine
What is another name for Procainamide?
Pronestyl
What is another name for Amiodarone?
Cordarone
What are the uses of Lidocaine?
Ventricular arrhythmia
Local anesthetic
How is Lidocaine administered?
Intravenous (IV) infusion
What proteins does Lidocaine bind to?
Albumin and Alpha-1 Acid Glycoprotein (AAG)
What is the therapeutic range of Lidocaine?
1.5 – 4.0 μg/mL
What is a toxic effect of Lidocaine?
Congestive Heart Failure (CHF)
Heart block
What is the primary use of Quinidine?
Ventricular arrhythmia
When does Quinidine reach peak serum levels post-oral dose?
2-4 hours
What is the therapeutic range of Quinidine?
2.3-5.0 μg/mL
What are the toxic effects of Quinidine?
Cinchonism
Blood dyscrasias
Hepatitis
What is the primary use of Procainamide?
Ventricular arrhythmia
What is the major metabolite of Procainamide?
N-acetyl-procainamide (NAPA)
When does Procainamide reach peak serum levels?
1 hour post-dose
What is the therapeutic range of Procainamide?
4-10 μg/mL
What are the toxic effects of Procainamide?
Reversible lupus-like syndrome
Nephrotic syndrome
Urticaria
What is the primary use of Disopyramide?
Arrhythmia
What additional effect does Disopyramide have?
Anticholinergic effects
What is the therapeutic range of Disopyramide?
3-5 μg/mL
What are the toxic effects of Disopyramide?
Bradycardia
AV node blockage
What are the uses of Propranolol?
Angina pectoris
Hypertension
Coronary artery disease
Thyrotoxicosis
What is the therapeutic range of Propranolol?
50-100 ng/mL
What are the toxic effects of Propranolol?
Bradycardia
Arterial insufficiency
Platelet disorder
Pharyngitis
What are the uses of Amiodarone?
Ventricular arrhythmias
Hyperthyroidism
What is the therapeutic range of Amiodarone?
1.0 – 2.5 μg/mL
What are the uses of Verapamil?
Angina
Hypertension
Supraventricular dysfunction
What is the therapeutic range of Verapamil?
80-400 ng/mL
What are examples of aminoglycoside antibiotics?
Gentamicin
Tobramycin
Amikacin
Kanamycin
Neomycin
Streptomycin
How are aminoglycosides administered?
Intramuscular (IM) or Intravenous (IV)
How are aminoglycosides eliminated?
Renal filtration
What is a toxic effect of aminoglycosides?
Hearing loss
What is Vancomycin used to treat?
Gram-positive cocci and bacilli infections
How is Vancomycin administered?
Intravenous (IV) infusion
What are the toxic effects of Vancomycin?
Red man syndrome
Nephrotoxicity
Ototoxicity
What is the mechanism of action of Chloramphenicol?
Inhibits protein synthesis in Gram-negative bacteria
What are the toxic effects of Chloramphenicol?
Blood dyscrasia (Aplastic anemia)
Cytoplasmic vacuolation
What neurotransmitters do neuroepileptics block?
Dopamine
Serotonin
What are examples of neuroepileptics?
Phenothiazines (Chlorpromazine)
Butyrophenones (Haloperidol)
What condition do neuroepileptics treat?
Schizophrenia
What toxic effects do neuroepileptics cause?
Aplastic anemia
Muscle rigidity
What is Lithium used to treat?
Bipolar disorder
Chronic cluster headaches
What does Lithium inhibit?
Iodine uptake
What toxic effects does Lithium cause?
Seizures
Coma
What do Tricyclic Antidepressants (TCAs) treat?
Depression
Insomnia
What are examples of TCAs?
Imipramine
Amitriptyline
Doxepin
Nortriptyline
Trazodone
What is the major metabolite of TCAs?
Desipramine
What is the other name for Fluoxetine?
Prozac
What does Fluoxetine block?
Serotonin reuptake
What disorder does Fluoxetine treat?
Obsessive-compulsive disorder
What toxic effect is associated with Fluoxetine?
Attempted suicide
What condition does Theophylline treat?
Asthma
Chronic Obstructive Pulmonary Disease (COPD)
What is the function of Theophylline?
Relaxes bronchial smooth muscles
What birth defect is linked to Theophylline?
Teratogenicity
What does Cyclosporine block?
Interleukin-2 production
What does Cyclosporine have a high affinity for?
Red blood cells
What conditions does Cyclosporine prevent?
Allogenic organ transplant rejection
Graft-versus-host disease (GVHD)
What specimen is used for Cyclosporine testing?
Whole blood
What is the other name for Tacrolimus?
Prograf
How much stronger is Tacrolimus than Cyclosporine?
100 times
What class of drug is Tacrolimus?
Macrolide antibiotic
What specimen is used for Tacrolimus testing?
Whole blood
What toxic effects does Tacrolimus cause?
Thrombus formation
Nephrotoxicity
Neurotoxicity
What is the other name for Rapamycin?
Sirolimus
What side effects does Sirolimus cause?
Lipid abnormalities
Thrombocytopenia
What condition is Mycophenolate Mofetil used for?
Renal allograft rejection
What does Leflunomide inhibit?
Lymphocyte proliferation
What condition does Leflunomide treat?
Rheumatoid arthritis
What condition is Methotrexate used for?
Cancer treatment
Immunosuppression
What does Methotrexate inhibit?
DNA synthesis (Dihydrofolate reductase)
What antidote is used for Methotrexate toxicity?
Leucovorin
What toxic effect is associated with Methotrexate?
Leukopenia
What condition does Busulfan treat?
Leukemia
Lymphoma before bone marrow transplant
What is a toxic effect of Busulfan?
Hepatic occlusive disease
What is the other name for Salicylate?
Aspirin
What does Aspirin directly stimulate?
The respiratory system
What enzyme does Aspirin inhibit?
Cyclooxygenase
What fatal condition does Aspirin cause in children?
Reye’s Syndrome
What lab method detects Aspirin?
Trinder’s assay
What is the other name for Acetaminophen?
Tylenol
What does Acetaminophen inhibit?
Prostaglandin metabolism
What toxic effects does Acetaminophen overdose cause?
Hepatotoxicity
Cyanosis
What advantage does Ibuprofen have over Salicylates?
Lower toxicity
What side effects does Ibuprofen cause?
Vomiting
Abdominal pain
Nausea