Study Guide Exam 1 Advanced Pharmacology
Exam Content: Units 1-3 (Foundations of Pharmacology; CV; Hematology)
For meds to be taken once/day, it must have a peak ratio of >50%
o ACEi are often BID
o ARBs are often qday
1. Understand pharmacokinetics and pharmacodynamics
● Pharmacokinetics – the study of the action of the drug in the body or what the body does with the drug as
described in ADME (Absorption, Distribution, Metabolism, Elimination).
it’s what the body does to this medication.
● Factors affecting pharmacokinetics: compliance, dosing, med errors, absorption, tissue & body fluid, mass
& volume, drug interactions, elimination, drug metabolism.
● Drug potency: how much a drug is needed to produce a biological response.
- More potent drug requires a lower dosage or concentration to produce to the same response.
- Ex: Lasix vs Bumex vs Torsemide.
● Drug efficacy: the ability of a drug to produce the mas effect at nay dosage.
● Pharmacodynamics - the study of the effect of a drug on the biochemical and physiological function in the
body or what the medication does to the body
● Factors affecting pharmacodynamics: drug receptor status, genetic factors, drug interactions, tolerance.
2. Factors that affect the volume of distribution (Vd)
a. Plasma protein binding: drugs that bind extensively to plasma proteins (e.g., albumin) tend to have a
lower volume of distribution because only the unbound drug can cross cell membranes and distribute into
tissues.
b. Body fat: individuals with higher body fat content may have a larger volume of distribution for lipophilic
drugs.
c. Tissue binding: drugs that bind to tissue components (e.g., fat, muscle) can have a larger volume of
distribution as they accumulate in these tissues.
Higher lipid solubility often correlates with better absorption in the stomach and intestines.
d. Pathophysiological conditions:
Edema fluid accumulation (e.g., heart failure, renal disease) can increase the volume of distribution for
hydrophilic drugs.
e. Can change with age, gender, and diseases (kidney and liver diseases)
Elderly individuals may have a larger volume of distribution for lipophilic drugs due to increased body fat
and decreased muscle mass. In infants, the volume of distribution for hydrophilic drugs is larger due to
higher body water content.
3. ADME
a. Absorption: how much of the drug & how fast it leaves the site of administration, “bioavailability-how
much drug actually gets to the site”
i. Bioequivalence: where 2 drugs have same active ingredients & are identical in strength or
concentration, dose form, administration, and “F” (fraction making it)
ii. Drug characteristics
● Dosage formulation (influences the rate of dissolution)
● Drug concentration
● Drug molecular weight
● Lipophilicity of drug formulations
, ● Dependance of transporters (not all meds require this)
● Ionization of the drug (acidic vs alkaloid drugs)
▪ Weak acids get trapped in basic environments
o R-COOH ↔ R-COO- + H+
o Ex. Aspirin, NSAIDS
▪ Weak bases get trapped in acidic environments
o R-NH3+ ↔R-NH2+ + H+
o Ex. Lactulose for hepac encephalopathy
b. Distribution: where the drug can be and is measured, “fluid compartments” where drug can reside
c. Metabolism
i. First-pass-contributes to bioavailability of drug by decreasing the amount delivered into general
circulation after passing through GI & liver
- Drugs that have a significant first pass effect are rapidly metabolized by the liver and may
have little if any desired action
ii. Prodrugs
iii. Oxidation/reduction primarily CYP450 enzyme system
- Found in liver (mainly), intestine, lungs, and kidneys
d. Elimination: majority occurs in kidneys via filtration, tubular secretion, or partial reabsorption
i. can also be fecal or breast milk elimination.
ii. Steady state
iii. 1⁄2 Life
4. Understand therapeutic index.
- Ratio of minimum effective concentration (MEC) to minimum toxic concentration (MTC) of a drug
The ratio between the toxic dose and effective dose of a given medication. It is used to determine the safety of
a medication.
Medications that have a low therapeutic index have a narrow margin of safety, which means that there is a thin line
between the dose needed to produce the desired effect and the toxic dose. These medications, including warfarin, lithium,
digoxin, gentamicin, phenytoin, or theophylline, require close monitoring of serum levels.
5. Phase 1 vs Phase 2 metabolism
Both of them take place in the liver, creating polar and water soluble metabolites, and are affected by genes, age,
liver disease, and interactions with medications, foods, and supplements.
Phase I
- mediated by cytochrome P450 and involves oxidation, hydrolysis, or reduction; and phase II involves
conjugation reactions.
- The enzymes convert non-polar, lipid-soluble medications into slightly more polar, water-soluble metabolites
through oxidation, hydrolysis, or reduction.