NR668 2026 STUDY SHEET MASTER
QUESTIONS WITH ACCURATE ANSWERS
◉efficacy examples. Answer: -Agonist (Efficacy = 100)
-Partial Agonist (Efficacy = > 0 < 100)
-Antagonist (Efficacy = 0.0)
-Inverse Agonist (Efficacy = < 0)
◉Agonist:. Answer: Compounds which give maximal response after
receptor occupation and activation.
-Example: Oxycodone
◉Partial Agonists:. Answer: Compounds which activate the receptor
but not at the maximal response.
-Example Buprenorphine (Suboxone) or Buspirone
◉Antagonist:. Answer: Blocks the action of an agonist.
-Example: Neuroleptics, Naloxone
◉Inverse Agonist:. Answer: Binds to receptor and has the opposite
action of an agonist and below baselinesignal transduction
,◉Pharmacokinetics. Answer: How the body effects the drug
-Absorption, distribution, metabolism and elimination (ADME)
-Metabolizing the drug via CYP450 through the gut & liver
◉Bioavailability. Answer: 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%
◉First pass metabolism. Answer: -reduces the concentration of a
drug
• travels through digestive system & entering the liver.
• reducing the bioavailability of the drug
◉rate is reduced by:. Answer: -Route (IV, PO, Rectum, etc.)
-Dosage (Concentration)
-Lipid Solubility
◉Drugs that cross the BBB are _____________. Answer: fat soluble
,◉Vd: Volume of distribution = ________. Answer: 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
◉A patient who is in renal failure would have a increased or
decreased Vd?. Answer: Increased because of fluid retention
◉plasma protein binding. Answer: -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
◉Drugs that are highly protein bound and have a narrow
therapeutic index can be dangerous because:. Answer: margin of
error between therapeutic and toxic is narrow
, ◉Metabolism. Answer: -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.
◉The rate of metabolism is affected by:. Answer: -age, liver & drug
tolerance
• Body may produce more enzymes & the liver becomes faster at
breaking that particular drug down
◉half life. Answer: this is the time it takes the peak level to fall by ½
◉Steady state of a drug:. Answer: -When the rate of drug
administration & elimination are equal
-can be achieved in 4 - 5 half lives
◉Phase I reactions:. Answer: Transforms drug, CYP450 Oxidases.
Make it available for the body to use
◉Phase II reactions:. Answer: Conjugation reactions or attach drug
with something. End products tend to be less active than their
substrates
QUESTIONS WITH ACCURATE ANSWERS
◉efficacy examples. Answer: -Agonist (Efficacy = 100)
-Partial Agonist (Efficacy = > 0 < 100)
-Antagonist (Efficacy = 0.0)
-Inverse Agonist (Efficacy = < 0)
◉Agonist:. Answer: Compounds which give maximal response after
receptor occupation and activation.
-Example: Oxycodone
◉Partial Agonists:. Answer: Compounds which activate the receptor
but not at the maximal response.
-Example Buprenorphine (Suboxone) or Buspirone
◉Antagonist:. Answer: Blocks the action of an agonist.
-Example: Neuroleptics, Naloxone
◉Inverse Agonist:. Answer: Binds to receptor and has the opposite
action of an agonist and below baselinesignal transduction
,◉Pharmacokinetics. Answer: How the body effects the drug
-Absorption, distribution, metabolism and elimination (ADME)
-Metabolizing the drug via CYP450 through the gut & liver
◉Bioavailability. Answer: 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%
◉First pass metabolism. Answer: -reduces the concentration of a
drug
• travels through digestive system & entering the liver.
• reducing the bioavailability of the drug
◉rate is reduced by:. Answer: -Route (IV, PO, Rectum, etc.)
-Dosage (Concentration)
-Lipid Solubility
◉Drugs that cross the BBB are _____________. Answer: fat soluble
,◉Vd: Volume of distribution = ________. Answer: 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
◉A patient who is in renal failure would have a increased or
decreased Vd?. Answer: Increased because of fluid retention
◉plasma protein binding. Answer: -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
◉Drugs that are highly protein bound and have a narrow
therapeutic index can be dangerous because:. Answer: margin of
error between therapeutic and toxic is narrow
, ◉Metabolism. Answer: -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.
◉The rate of metabolism is affected by:. Answer: -age, liver & drug
tolerance
• Body may produce more enzymes & the liver becomes faster at
breaking that particular drug down
◉half life. Answer: this is the time it takes the peak level to fall by ½
◉Steady state of a drug:. Answer: -When the rate of drug
administration & elimination are equal
-can be achieved in 4 - 5 half lives
◉Phase I reactions:. Answer: Transforms drug, CYP450 Oxidases.
Make it available for the body to use
◉Phase II reactions:. Answer: Conjugation reactions or attach drug
with something. End products tend to be less active than their
substrates
