NSG 531 Advanced Pharmacology Exam
1
A 23 year-old male presents to the ED with an overdose of phencyclidine (PCP), a basic
drug. How might we enhance urinary excretion of the drug? - correct answer-The Law of
Mass Action predicts that decreasing the pH favors ionization of basic drugs. We'd reduce
the pH of urine by administering ammonium chloride.
A drug is ________ . - correct answer-an agent that affects biological processes and is given
to prevent or treat diease; most are weak acids or bases
A higher Ka (association constant) means that the reaction is favored to the ______ , and
the drug is ______ . - correct answer-right; primarily bound to plasma proteins (we'd need to
sample a large volume of plasma to get one mole of free drug)
A higher Kd (dissociation constant) means that the reaction is favored to the _____ , and
there are ______ . - correct answer-left; more moles of free drug
A non-protonated acid is ______ . - correct answer-ionized and water soluble
A non-protonated base is _____ . - correct answer-non-ionized and lipid soluble
A protonated acid is _____ . - correct answer-non-ionized and lipid soluble
A protonated base is _____ . - correct answer-ionized and water soluble
Acetaminophen (APAP) toxicity is mediated by _________ . - correct answer-saturated
normal liver conjugation pathways followed by insufficient glutathione to conjugate the
metabolite NAPQI, which binds to hepatocellular proteins causing oxidative damange,
mitochondrial dysfunction, and hepatocellular death
Acidic drugs are _____ in the upper GI tract, but giving an antacid or H2 antagonist will
_____ the absorption. - correct answer-easily absorbed; slow
Acidifying urine using ammonium chloride will increase the excretion of _____ drugs -
correct answer-base
Alkalinizing urine with sodium bicarbonate will increase the excretion of _____ drugs. -
correct answer-acid
Association constant - correct answer-K1/K2 = Ka (liters/mole), or the volume needed to get
one mole of free drug when 50% of the receptors are occupied.
Bioavailability calculation - correct answer-area under the curve (oral) / area under the curve
(IV); expressed as a %
, Bioavailability is _____ for intravenous drugs. - correct answer-100%
Biotransformation - correct answer-Reactions in the liver that make drugs more water
solubule to be readily eliminated in urine or bile
Calculate the volume of distribution (VD) of a drug if the plasma concentration is 2 mg/L one
minute after you give 50mg IV. - correct answer-25L
Clearance - correct answer-the volume of plasma cleared of drug per unit time; not a weight
CYP450 inducers ______ the elimination of concurrently administered drugs. - correct
answer-increase
CYP450 inhibitors _____ plasma concentrations of concurrently administered drugs - correct
answer-increase
Decreased free drug in the plasma is associated with _____ in plasma albumin
concentration. - correct answer-increases
Dissociation constant - correct answer-K2/K1 = Kd (moles/liter), or the drug concentration
needed to occupy 50% of the receptors.
Drugs are largely eliminated by the ______ following biotransformation in the _______. -
correct answer-kidneys; liver (major), sweat and saliva (minor)
Drugs that are polar will act like _____ drugs. - correct answer-ionized, water soluble
Equation for the amount of drug in the body - correct answer-VxC (volume of distribution x
plasma concentration)
Extraction ratio - correct answer-the % of a drug that is lost in the first pass effect through
the liver
First Pass Effect - correct answer-Drugs cross intestinal epithelial cells and are delivered to
the liver via the hepatic portal vein. Then go through Phase 1 and 2 biotransformation and
become a metabolite before entering systemic circulation.
First-order kinetic effects - correct answer-have a constant half-life; elimination routes are
not saturated
Glutathione's role in acetaminophen biotransformation - correct answer-Conjugates the
hepatotoxic reactive metabolite N-acetyl-p -benzoquinoneimine (NAPQI), which can then be
renally excreted
Half-life - correct answer-the time required for the plasma concentration of a drug to be
reduced by 50% (takes several half-lives for the drug to be completely eliminated from the
body)
1
A 23 year-old male presents to the ED with an overdose of phencyclidine (PCP), a basic
drug. How might we enhance urinary excretion of the drug? - correct answer-The Law of
Mass Action predicts that decreasing the pH favors ionization of basic drugs. We'd reduce
the pH of urine by administering ammonium chloride.
A drug is ________ . - correct answer-an agent that affects biological processes and is given
to prevent or treat diease; most are weak acids or bases
A higher Ka (association constant) means that the reaction is favored to the ______ , and
the drug is ______ . - correct answer-right; primarily bound to plasma proteins (we'd need to
sample a large volume of plasma to get one mole of free drug)
A higher Kd (dissociation constant) means that the reaction is favored to the _____ , and
there are ______ . - correct answer-left; more moles of free drug
A non-protonated acid is ______ . - correct answer-ionized and water soluble
A non-protonated base is _____ . - correct answer-non-ionized and lipid soluble
A protonated acid is _____ . - correct answer-non-ionized and lipid soluble
A protonated base is _____ . - correct answer-ionized and water soluble
Acetaminophen (APAP) toxicity is mediated by _________ . - correct answer-saturated
normal liver conjugation pathways followed by insufficient glutathione to conjugate the
metabolite NAPQI, which binds to hepatocellular proteins causing oxidative damange,
mitochondrial dysfunction, and hepatocellular death
Acidic drugs are _____ in the upper GI tract, but giving an antacid or H2 antagonist will
_____ the absorption. - correct answer-easily absorbed; slow
Acidifying urine using ammonium chloride will increase the excretion of _____ drugs -
correct answer-base
Alkalinizing urine with sodium bicarbonate will increase the excretion of _____ drugs. -
correct answer-acid
Association constant - correct answer-K1/K2 = Ka (liters/mole), or the volume needed to get
one mole of free drug when 50% of the receptors are occupied.
Bioavailability calculation - correct answer-area under the curve (oral) / area under the curve
(IV); expressed as a %
, Bioavailability is _____ for intravenous drugs. - correct answer-100%
Biotransformation - correct answer-Reactions in the liver that make drugs more water
solubule to be readily eliminated in urine or bile
Calculate the volume of distribution (VD) of a drug if the plasma concentration is 2 mg/L one
minute after you give 50mg IV. - correct answer-25L
Clearance - correct answer-the volume of plasma cleared of drug per unit time; not a weight
CYP450 inducers ______ the elimination of concurrently administered drugs. - correct
answer-increase
CYP450 inhibitors _____ plasma concentrations of concurrently administered drugs - correct
answer-increase
Decreased free drug in the plasma is associated with _____ in plasma albumin
concentration. - correct answer-increases
Dissociation constant - correct answer-K2/K1 = Kd (moles/liter), or the drug concentration
needed to occupy 50% of the receptors.
Drugs are largely eliminated by the ______ following biotransformation in the _______. -
correct answer-kidneys; liver (major), sweat and saliva (minor)
Drugs that are polar will act like _____ drugs. - correct answer-ionized, water soluble
Equation for the amount of drug in the body - correct answer-VxC (volume of distribution x
plasma concentration)
Extraction ratio - correct answer-the % of a drug that is lost in the first pass effect through
the liver
First Pass Effect - correct answer-Drugs cross intestinal epithelial cells and are delivered to
the liver via the hepatic portal vein. Then go through Phase 1 and 2 biotransformation and
become a metabolite before entering systemic circulation.
First-order kinetic effects - correct answer-have a constant half-life; elimination routes are
not saturated
Glutathione's role in acetaminophen biotransformation - correct answer-Conjugates the
hepatotoxic reactive metabolite N-acetyl-p -benzoquinoneimine (NAPQI), which can then be
renally excreted
Half-life - correct answer-the time required for the plasma concentration of a drug to be
reduced by 50% (takes several half-lives for the drug to be completely eliminated from the
body)
