Intensive Review
Pharmacology ANS: The study of the interaction between the body and drugs
Pharmacokinetics ANS: The movement of drugs through the body (absorption, bioavailability,
distribution, metabolism, and excretion).
Pharmacodynamics ANS: The study of the physiologic and biochemical effects of the drug
Pharmacogenomics ANS: The study of how a person's genes affect response to medications.
FDA recently recommended genotyping all asians for HLA-B*1502 before starting carbamazepine
therapy. (This allele is highly associated with fatal carbamazepine therapy induced Steven-Johnson
Syndrome and toxic epidermal necrolysis).
Half-life ANS: The amount of time in which drug concentration decreases by 50%
Area under the curve (AUC) ANS: The average amount of drug in the blood after a dose is given. It is a
measure of the bioavailability of a drug that is administered.
Minimum Inhibitory Concentration (MIC) ANS: The lowest concentration of an antibiotic that will inhibit
the growth of organisms (after overnight incubation).
Maximum Concentration ANS: The highest concentration of a drug after a dose.
Trough (Minimum concentration) ANS: the lowest dose of a drug after a dose
,First pass effect ANS: all oral drugs (except SL) must go through the first pass metabolism before they
can be released in the body.
Swallow pill > esophagus > stomach > small intestine > portal circulation > liver > (in liver, CYP450
system is responsible for metabolism) > when completed, released in it's active form into the body.
A few are also broken down in the small intestine by bacteria (for example: oral contraceptives) in
addition to being metabolized in the liver.
Clinical Pearl: Some drugs cannot be given by oral route simply because there is not enough of the active
drug left after metabolism (I.E Insulin).
Drug metabolism ANS: Main Organ: Liver
The CYP450 system is the most active. It can either be induced (increase metabolism) or inhibited
(decrease metabolism). Ex: Carbamazepine increases metabolism- resulting in numerous drug
interactions. Other organs are involved in metabolism such as the kidneys, GI tract, lungs, plasma, and
skin.
Drug excretion ANS: Renal filtration accounts for most drug excretion. Renal drug excretion is deceased
because of physiologic decline in GFR.
Drugs affected by Kidney Disease ANS: NSAIDS> Decrease renal blood flow will damage kidneys.
ACEI > Increase risk for hyperkalemia
Warfarin > increase risk of over coagulation, hemorrhagic complications.
Lithium > increase risk for kidney injury
Contrast dyes > can injure kidneys
,Potassium-sparing diuretics > increase risk for hyperkalemia
Sodium-phosphate > may cause sudden loss of kidney function as well as blood mineral disturbances.
Potent Inhibitors CYP450 system ANS: These drugs are responsible for a large number of drug-drug
interactions. Drugs that act as inhibitors slow down drug clearance which increases risk of drug overdose
and ASE.
- Macrolides (erythromycin, clarithyromycin)
- Antifungals (ketoconazole, fluconazole)
-Cimetidine (Tagamet)
-Celexa
-Protease inhibitors (saquinarvir, indinavir)
-Grapefruit juice
Narrow Therapeutic index drugs ANS: Warfarin > Monitor INR
Digoxin > Monitor Digoxin level, EKG, electrolytes
Theophylline > Monitor blood levels
Carbamazepine and Phenytoin > Monitor blood levels
Levothyroxine > Monitor TSH
Lithium > Monitor blood levels and TSH (Risk of hypothyroid).
H2 antagonist safety issues ANS: ex: famotidine, cimetidine, nizatidine
Mental status changes with kidney disease. Avoid kidney disease with creatinine clearance of < 50
ml/min.
, Proton-pump inhibitors safety issues ANS: ex: omeprazole
Increase risk of fractures (post-menopausal women), pneumonia, c-diff, decreased mag, B12 and iron
Mal-absorption, atrophic gastritis, and kidney disease.
Interacts with warfarin, diazepam, carbamazepine, phenytoin, and ketoconazole.
Vitamin K antagonist safety issues ANS: Ex: warfarin
interacts with "G" herbs such as garlic, ginger, gingko, and ginseng. other herbs/supplements: feverfew,
green tea, and fish oil.
Numerous drug interactions.
Discontinue 7 days before surgery.
Thiazides safety issues ANS: ex: Pioglitazore (DM/TZD's)
Black box warning: cause or exacerbate CHF in some patients. do not use in class III or IV.
Contraindications: history of mI, stroke, bladder cancer, T2DM, eye or liver problems.
Stop if causes dyspnea, weight gain, cough (HF).
Atypical antipsychotic safety issues ANS: ex: Risperiodone, olanzapine, quetiapine