Pharmacokinetics - Answers what the body does to the drug
Pharmacodynamics - Answers what the drug does to the body
Toxicology - Answers The undesirable effects of chemicals on living systems
Pharmacotherapeutics - Answers dynamic that achieves the desired therapeutic effect of the drug
without causing other undesirable effects
Legend drugs - Answers another name for prescription drugs
Pharmacogenomics - Answers the study of genetically determined variations in the response to drugs
Pharmacologic Agonist - Answers agent binds to and activates the
receptor - directly or indirectly causing an effect, full or partial agonists
Pharmacological Antagonist - Answers Agent binds to receptor-completes with other molecules and
prevents binding by other molecules-it inhibits other molecules from binding
Pro-drug - Answers An inactive percursor chemical-must be abosorbed and distributed and converted
to the active form of the drug by biologic processes.
What is ADME? - Answers Absorption
Distribution
Metabolism
Elimination
Absorption - Answers entry of pharmacologic agent into plasma
Distribution - Answers agent leaves the bloodstream and distributes to interstitial and intracellular
fluids
Metablosim - Answers chemical processes that occur to make the drug useful in the bloodstream--
done by the liver, kidney, or other tissue
Ellimination - Answers Leaving the body-via urine, bile, feces, lungs, sweat, breast milk
2 Major Administration Routes - Answers 1. Enteral -most common, easy, cheap-BUT drug absorption
pathways can be complicated
2. Parenteral-IV, fast, more expensive, once in-cannot get back
Enteral drug administration - Answers oral, sublingual, rectal
drug absorption pathways complicated
**First-pass metabolism can limit the amount of drug that enters systemic circulation
influenced by food and other drugs
What is first pass metabolism? - Answers The concentration of drug is greatly reduced BEFORE
reaching systemic circulation. This mainly involves liver enzymes, but also includes gastric enzymes,
gut wall enzymes, and bacterial enzymes. Bioavaliability is reduced.
https://www.youtube.com/watch?v=BQQns7RAUzA
Parenteral drug administration - Answers -IV, IM, SubQ
- More control over actual dose of drug
- Directly into systemic circulation-bypass first pass metabolism
- used for drugs poorly absorbed by GI
-Rapid onset of action
-Disadvantage: cannot take the drug back, infection risk
Inhalation route of administration - Answers Rapid delivery, large surface area, good for gases,
aerolsols, respiratory drugs
Rectal Route of administration - Answers 50% of circulatory drainage BYPASSES portal circulation
Meaning: Less first pass effect
Drug Transport Methods: - Answers Passive diffusion (no E needed)
Active transport (requires E)
Endocytosis
Passive diffusion (simple diffusion) - Answers no energy needed, related to concentration gradient
across membrane, HIGHER concentration goes to LOWER concentration
Active Transport - Answers requires energy (ATP), Able to move drug from LOWER to HIGHER
concentration
Endocytosis - Answers Transport large molecules
Engulfment of drug molecule by cell membrane and transport into cell
Exocytosis - Answers Process by which a cell releases large amounts of material
Drug Absorption - Answers Drugs are typically weak acids or weak bases
, Role and size of MOLECULAR WEIGHT in drug absorption
Drug Molecular Weights - Answers Most drugs weight from 100-1000
smaller sizes are easier to cross membranes
However, drugs can vary in size from MW of 7 (Lithium) to 50,000 (thrombolytic enzymes)
Solubility - Answers Hydrophilic (Lipophobic)
Lipophilic (hydrophobic)
Remember: Cell membranes tend to be LIPID filled--so LIPID based drugs tend to cross the lipid
membrane easier
What impacts drug absorption? - Answers Solubility (hydrophilic or lipophilic?), pH, pKa (how acidic
the drug is), Molecular weight, partition coefficient (ratio of concentration)
Factors that influence GI Absorption? - Answers Blood flow (intestinal blood flow is greater than
stomach blood flow)
pH-How acidic is the stomach? (is patient on PPI that decreases stomach acid?)
Intestinal surface area- (microvilli)-there are 1000x more than stomach
CONTACT TIME- Rapid vs slow GI Transport, Parasympathetic input--increases rate of gastric emptying
Sympathetic input--delayed gastric emptying
Food--delayed absorption (food is in the way)
What is the bioavailability of a drug? - Answers Fraction of chemically unchanged drug that reaches
systemic circulation
What FACTORS influence BIOAVAILABILITY? - Answers first pass hepatic metabolism, solubility of the
drug, chemical instability (ex; insulin in GI tract), nature of the drug formulation
What should you do if a drug has a HIGH first pass effect? - Answers Give drug a different way OR give
a higher dose of drug if given PO
Hydrophilic drugs - Answers Poorly absorbed, water based which means poor absorption, unable to
cross lipid-rich cell membranes
Hydro (water), Philic (likes)
Extremely Hydrophobic Drugs - Answers Hydro (water), Phobic (does not like)
these drugs are also poorly absorbed--insoluble in aqueous body fluids
What is ideal for drug absorption? - Answers Largely Hydrophobic, but with some solubility in
aqueous solution, Highly lipid soluble drugs can be transported in aqueous solutions in the body VIA
carrier proteins (ALBUMIN)
What is the relationship of the drugs MW and absorption? - Answers The smaller the drugs size-the
more easily it will move across the cell membrane and be absorbed.
Bioavailability - Answers Highest to Lowest
IV, IM, SC, PO, PR (Rectal), Inhalation, Transdermal
What is Therapeutic Equivalence? - Answers Comparable clinical effectiveness and safety between
similar drugs
Two Drugs that are Bioequivalent MAY NOT be therapeutically equivalent--we focus on therapeutic
equivalency
What is the Clinical Effectiveness of a drug? - Answers It is dependent on the serum drug
concentrations and the TIME it takes to reach PEAK drug concentrations
What is drug distribution/delivery? - Answers Process in which drug reversibly leaves the blood
stream and enters interstitium and/or cells.
What is drug delivery dependent on? - Answers blood flow, capillary permeability, albumin level
(plasma protein binding ability), drug structure, hydrophobicity
Drug Distribution--Blood Flow - Answers Wide variance r/t unequal distribution of Cardiac Output
(CO)
- Highest in organs: heart, brain, lungs, kidneys, liver, gut
-Lower in skeletal muscle
_Still lower in adipose tissue
Capillary Permeability and Drug Distribution - Answers • Capillary permeability
• capillary structure & chemical nature of the drug
• Variance in capillary structure: slit junctions between
endothelial cells (liver and pancreas have this)
• Allows passage of plasma proteins... and thus, drug molecules
• Absent in the brain- "blood-brain barrier"