ASSESSMENT FULLY DETAILED WITH THE
ONLY CORRECT ANSWERS
How the drug effects the body
-therapeutic vs. side effects
• Is it stimulating?
• Is it depressing?
• Does it block something?
-Onset of action
• Route, Dosage
-Duration of action
• Redistribution rate, metabolism rate and excretion rate
-Mechanism of action
• Drugs simply speed up or slow down what is already occurring in the body
-Efficacy
• (Intrinsic activity) After binding, the drugs capacity to cause an effect
-Potency
• The amount of a drug needed to produce a given effect - answer ✔✔-Pharmacodynamics
-Agonist (Efficacy = 100)
-Partial Agonist (Efficacy = > 0 < 100)
-Antagonist (Efficacy = 0.0)
-Inverse Agonist (Efficacy = < 0) - answer ✔✔-efficacy examples
Compounds which give maximal response after receptor occupation and activation.
,-Example: Oxycodone - answer ✔✔-Agonist:
Compounds which activate the receptor but not at the maximal response.
-Example Buprenorphine (Suboxone) or Buspirone - answer ✔✔-Partial Agonists:
Blocks the action of an agonist.
-Example: Neuroleptics, Naloxone - answer ✔✔-Antagonist:
Binds to receptor and has the opposite action of an agonist and below baselinesignal transduction -
answer ✔✔-Inverse Agonist:
How the body effects the drug
-Absorption, distribution, metabolism and elimination (ADME)
-Metabolizing the drug via CYP450 through the gut & liver - answer ✔✔-Pharmacokinetics
Absorption: Drugs cross a barrier.
-Involves bioavailability or Quantity of drug reaching circulation/quantityof the drug administered.
• Our own barriers such as skin and mucous membranes as well as food, molecular weight, chemical,
biological barriers, etc. reduce how much drug is actually absorbed and available. IV route has 100%
bioavailability. All other routes <100% - answer ✔✔-Bioavailability
-reduces the concentration of a drug
• travels through digestive system & entering the liver.
• reducing the bioavailability of the drug - answer ✔✔-First pass metabolism
-Route (IV, PO, Rectum, etc.)
-Dosage (Concentration)
-Lipid Solubility - answer ✔✔-rate is reduced by:
fat soluble - answer ✔✔-Drugs that cross the BBB are _____________
, amount of drug/concentration
• large Volume of distribution may indicate the drug distributes extensively into the body
• Vd is a theoretical fluid volume necessary to contain the total amount of a drug at the same
concentration observed in the plasma - answer ✔✔-Vd: Volume of distribution = ________
Increased because of fluid retention - answer ✔✔-A patient who is in renal failure would have a
increased or decreased Vd?
-cannot leave the circulation easily
-Free (unbound) crosses membranes
-Two drugs that are both highly protein bound will compete with each other
• The unbound fraction goes through metabolism and is responsible for the pharmacologic effects
-rapid weight loss may result in drugs being released from fat cells - answer ✔✔-plasma protein binding
margin of error between therapeutic and toxic is narrow - answer ✔✔-Drugs that are highly protein
bound and have a narrow therapeutic index can be dangerous because:
-Mostly in the liver
-Biotransformation or change it to inactive form or make it more water soluble to facilitate excretion
• transformed substance is called the metabolite. - answer ✔✔-Metabolism
-age, liver & drug tolerance
• Body may produce more enzymes & the liver becomes faster at breaking that particular drug down -
answer ✔✔-The rate of metabolism is affected by:
this is the time it takes the peak level to fall by ½ - answer ✔✔-half life
-When the rate of drug administration & elimination are equal