NR 668 CERTIFICATION EVALUATION
COMPLETE QUESTIONS AND SOLUTIONS
GRADED APLUS
●● 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
COMPLETE QUESTIONS AND SOLUTIONS
GRADED APLUS
●● 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
