BIOPHARMACEUTICS AND PHARMACOKINETICS

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1. Metabolism The enzymatic or biochemical transformation of

the drug substance to usually less toxic metabolic
products, which may be eliminated more readily
from the body

2. Xenobiotics chemical substances that are foreign to the biolog-

ical system

3. Liver principal site of metabolism

4. liver lobule basic functional unit of the liver

5. parenchymal cells a network of interconnected lymph and blood ves-

sels

6. large right lobe of liver region of the liver that is responsible for food me-
tabolism

7. Small left lobe of liver region of the liver that is responsible for drug me-
tabolism

8. Teres ligament separates the two lobes of the liver

9. Hepatic artery perfuses blood and carries oxygen to to liver

10. Hepatic portal vein collects blood from the GI tract that perfuse in the
liver and carries nutrient to the liver

11. sinusoids large vascular capillaries which facilitates drug and

nutrient removal before the blood enters the gen-
eral circulation

12. Kupffer cells endothelial lining of the sinusoids which is also

known as the liver macrophages

13. bile acids synthesized in the gall bladder, secreted by the

liver and emulsify fats

14. hepatic metabolism metabolism happens in the liver

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15. Extrahepatic metabo- The drug biotransformation that takes place in tis-
lism sues other than the liver

16. p-aminobenzoic acid Determine the metabolite and its type

Inactive metabolite
Procaine

17. 6-mercaptopuric acid Determine the metabolite and its type

Inactive metabolite
6-mercaptopurine

18. phenylacetone Determine the metabolite and its type

Inactive metabolite
amphetamine

19. hydroxyphenobarbital Determine the metabolite and its type

Inactive metabolite
phenobarbital

20. desipramine Determine the metabolite and its type

Metabolites that retain
similar activity Imipramine

21. L-hydroxyhexamide Determine the metabolite and its type

Metabolites that retain
similar activity Acetohexamide

22. Morphine Determine the metabolite and its type

Metabolites that retain
similar activity Codeine

23. N-acetylprocainamide Determine the metabolite and its type

Metabolites that retain
similar activity Procainamide

24. Oxyphenbutazone Determine the metabolite and its type

Metabolites that retain
similar activity Phenylbutazone

25.
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Iproniazid Determine the metabolite and its type
Metabolites with al-
tered activity Isoniazid

26. Enalaprilat Determine the metabolite and its type

Bioactivated metabolite
Enalapril

27. Active sulfide Determine the metabolite and its type

Bioactivated metabolite
Sulindac

28. Dopamine Determine the metabolite and its type

Bioactivated metabolite
Levodopa

29. Sulfanilamide Determine the metabolite and its type

Bioactivated metabolite
Prontosil

30. Prontosil first discovered prodrug

31. Ampicillin Determine the metabolite and its type

Bioactivated metabolite
Hetacillin

32. Sulfapyridine + Determine the metabolite and its type

Aminosalicylic acid
Bioactivated metabolite Sulfasalazine

33. NAPQI (N-acetyl-p-ben- Determine the metabolite and its type

zoquinone imine)
Reactive metabolite Acetaminophen

34. Reactive Benzopyrene Determine the metabolite and its type

Reactive metabolite
Benzopyrene

35. Phase 1

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Phase 1 or Phase 2

functionalization reaction

36. Phase 2 Phase 1 or Phase 2

conjugation reaction

37. Phase 1 Phase 1 or Phase 2

non-synthetic

38. Phase 2 Phase 1 or Phase 2

Synthetic

39. Phase 1 Phase 1 or Phase 2

with small chemical changes occur in one or more

functional groups of drug

40. Phase 2 Phase 1 or Phase 2

A molecule provided by the body is added to the

drug

41. Oxidation most dominant pathway in phase 1 reaction

42. Glucoronidation Most common phase II reaction

43. Monooxygenase en- Mixed function oxidases is also known as (2)

zyme
CYP 450

44. CYP 2D6 mixed function oxidase that causes genetic poly-
morphism

45. glucoronyl transferase enzyme responsible for glucoronic acid conjuga-

tion

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46. true true/false

Glucoronidation is reduced during pregnancy

47. Gray baby syndrome inability to conjugate chloramphenicol by new-

borns results to what condition?

48. Kernicterus High levels of bilirubin in the bloodstream of

neonates, leading to brain damage

49. methyl transferase enzyme responsible for methylation pathway

50. methylation and acety- minor conjugation pathways

lation

51. N-acetyl transferase enzyme responsible for acetylation pathway

52. glutathione conjuga- detoxification of reactive oxygen

tion

53. Glutathione S-trans- Enzyme in glutathione conjugation

ferase

54. Glycine and glutamine amino acid conjugation (2)

conjugation

55. Coenzyme A enzyme for glycine conjugation

56. Glycine conjugation benzoic acid is metabolized to hippuric acid by

what pathway?

57. sulfation major metabolic pathway for newborns

58. Reduction, Oxidation these metabolic pathways become present in in-

fants in their first week (2)

59. acetylation this metabolic pathway becomes present in infants

in their first month

60. glucoronidation

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this metabolic pathway becomes present in infants
in their second month

61. Glycine conjugation, these metabolic pathways become present in in-

Glutathione conjuga- fants in their third month
tion, Cysteine conjuga-
tion

62. sixth month infants have complete enzyme by this month

63. auto-induction a drug that stimulates its own metabolism

64. foreign-induction one enzyme inducer stimulate the rate of metabo-

lism of another drug

65. Enzyme Inducer Enzyme Inducer/Inhibitor

Phenytoin

66. Enzyme Inducer Enzyme Inducer/Inhibitor

Phenobarbital

67. Enzyme Inducer Enzyme Inducer/Inhibitor

Rifampicin

68. Enzyme Inducer Enzyme Inducer/Inhibitor

Carbamazepine

69. Enzyme Inducer Enzyme Inducer/Inhibitor

Cigarette smoking

70. Enzyme Inducer Enzyme Inducer/Inhibitor

Chronic alcoholism

71. Enzyme Inhibitor

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Enzyme Inducer/Inhibitor

Metronidazole

72. Enzyme Inhibitor Enzyme Inducer/Inhibitor

Erythromycin

73. Enzyme Inhibitor Enzyme Inducer/Inhibitor

Disulfiram

74. Enzyme Inhibitor Enzyme Inducer/Inhibitor

Isoniazid

75. Enzyme Inhibitor Enzyme Inducer/Inhibitor

Cimetidine

76. Enzyme Inhibitor Enzyme Inducer/Inhibitor

Ketoconazole

77. Enzyme Inhibitor Enzyme Inducer/Inhibitor

Valproic acid

78. Enzyme Inhibitor Enzyme Inducer/Inhibitor

Grapefruit juice

79. Enzyme Inhibitor Enzyme Inducer/Inhibitor

Acute alcoholism

80. first pass effect presystemic metabolism

81. first pass effect initial biotransformation of an active drug before

reaching the systemic circulation
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82. Excretion the final loss of the drug substance or its metabo-
lites from the body such as through the kidney,
intestines, skin, saliva, and/or milk

83. Biliary excretion excretion pathway for anions, cations, nonionized

molecules with lipophilic polar groups, those with
MW of >500 and drugs poorly absorbed in the
intestines

84. Gentamicin drugs with extremely narrow therapeutic range that

Kanamycin are excreted via mammary glands

85. Sweat excretion pathway where passive diffusion of the

non-ionized moiety occurs

86. intestinal excretion excretion pathway that is verified by the presence

of drugs in the gut lumen after IV administration

87. renal drug excretion major route of elimination for drugs and drug
metabolites either by glomerular filtration or tubu-
lar secretion

88. Drug elimination irreversible removal of drug from the body by all
routes of elimination

89. nonvolatile drugs are excreted mainly by renal excretion, into the
urine

90. volatile drugs gaseous anesthetics, or drugs with high volatility,

are excreted via the lungs into expired air

91. clearance/drug clear- the process of drug elimination from the body or
ance from a single organ without identifying the individ-
ual processes involved

92. kidney most important organ for excretion

93. nephrons Functional units of the kidneys

94. aldosterone
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"salt-retaining hormone" which promotes the re-
tention of Na+ by the kidneys. na+ retention pro-
motes water retention, which promotes a higher
blood volume and pressure

95. proximal convoluted tubular part for active secretion; emulsifies sub-
tubule stances

96. distal convoluted tubular part for tubular reabsorption; reabsorbs

tubule blood

97. glomerulus filters blood

98. Glomerular Filtration filtration of low MW molecules which tells how

Rate (GFR) healthy the kidney is

99. 125 mL/min or 180 normal GFR

L/day

100. Inulin the standard reference for GFR measurement, ful-

fills most of the criteria needed but is time-consum-
ing

101. Creatinine used most extensively as a measurement of GFR

102. creatinine By-product of muscle metabolism

103. active tubular secretion occurs in proximal convoluted tubule in which wa-
ter is reabsorbed and active secretion of some
weak electrolytes especially weak acids

104. tubular reabsorption reabsorption of water and passive excretion of

lipid-soluble drugs based on Hendersson-Hassel-
balch equation

105. clearance/drug clear- pharmacokinetic term for describing drug elimina-

ance tion from the body without identifying the mecha-
nism of the process

106. renal clearance

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volume of plasma cleared of a particular sub-
stance per unit time through the kidney

107. hepatic clearance volume of plasma cleared of drug per unit time
through the liver

108. creatinine clearance ratio of creatinine in the urine and creatinine in the
plasma

109. response refers to the therapeutic effect, sub-therapeutic ef-

fect, side effect and toxic effect

110. zero-order reaction a constant amount of drug is metabolized per unit

time

111. first-order reaction constant fraction of drug is metabolized per unit

time

112. zero-order reaction zero/first- order kinetics

rate does not increase as drug concentration in-

creases

113. first-order reaction zero/first- order kinetics

rate increase as drug concentration increases

114. zero-order reaction zero/first- order kinetics

followed by suspension, alcohol

115. first-order reaction zero/first- order kinetics

followed by most drugs

116. zero-order reaction zero/first- order kinetics

drug concentration change is constant w/ time

117. first-order reaction

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zero/first- order kinetics

drug concentration change is decreasing depend-

ing on remaining concentration

118. open one compartment simplest way to describe the distribution and elim-
model ination in the body

119. Open two compartment if the drug entering the body does not instantly
model distribute between the blood and other body fluids
or tissues

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