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WorksheetsMed Chem ex2
Total questions: 100
Worksheet time: 51mins
Name
Class
Date
1.
Basiliximab & Daclizumb…
a)
Used for preventing transplant rejection
b)
Prevent T-lymphocyte activation
c)
Immunosuppress
d)
Immunoactivate
2.
Herceptin (Trastuzumab)…
a)
Used for metastatic breast cancer
b)
Contains the ErB2/HER2 antigen
c)
Used for testicular cancer
d)
An antibody-drug conjugate
3.
Zevalin…
a)
Used for NHL
b)
Contains Yttrium-90
c)
Contains the CD20 antigen
d)
Selectively targets B Cells
e)
Selectively targets T Cells
4.
Kadcyla…
a)
Is Herceptin linked with mertansine
b)
Used for metastatic breast cancer
c)
Used for transplant rejection
d)
Is released in the cytosol
e)
Is released in the extracellular space
5.
Casirivimab and Imdevimab are used for…
a)
SARS-COV-2
b)
SARS-COV-1
c)
SARS-COV-19
d)
H1N1
e)
H5N1
6.
What are some issues related to protein-based drugs?
a)
Antigenicity
b)
Stability
c)
Drug Delivery
d)
Cytotoxicity
7.
What are some of the characteristics of an antigenic response in a protein-based drug?
a)
Anaphylaxis
b)
Loss of efficacy
c)
Increase in efficacy
d)
Immunosuppression
8.
What are some of the stability issues associated with protein-based drugs?
a)
Denaturation
b)
Proteolysis
c)
Covalent breakage due to temp/pH changes
d)
Enteric effects
9.
What are methods to measure protein-based drug stability?
a)
SDS Page
b)
RP-HPLC
c)
IEF
d)
Potency Determination
e)
Assays
10.
What changes is SDS Page able to detect?
a)
Fragmentation
b)
Crosslinking
c)
Oligomerization
d)
Deamidation
e)
Disulfide Scrambling
11.
What changes is RP-HPLC able to detect?
a)
Deamidation
b)
Crosslinking
c)
Methionine Oxidation
d)
Disulfide Scrambling
e)
Fragmentation
12.
What changes is IEF able to detect?
a)
Deamidation
b)
Crosslinking
c)
Methionine Oxidation
d)
Fragmentation
e)
Oligomerization
13.
What changes is potency determination able to detect?
a)
Disulfide Scrambling
b)
Crosslinking
c)
Oligomerization
d)
Methionine Oxidation
e)
Deamidation
14.
What are some methods to develop a 'biosuperior' drug?
a)
Modify/remove selected Aas
b)
Alternative source production
c)
Unessential portion deleted
d)
Disulfide bond introduction
e)
Phosphorylation
15.
What chemical modifications can be done to increase circulating half life?
a)
Make changes in glycosylation
b)
Link PEG to proteins
c)
Make the molecule unmetabolized
d)
Increase excretion
e)
Decrease absorption
16.
An antisense agent that targets at the DNA level can do so how?
a)
Forms a triplex with the target DNA
b)
Binds to ssDNA regions
c)
Binds to DNA-Polymerase I
d)
Forms a duplex with the target DNA
17.
An antisense agent that targets at the mRNA level can do so how?
a)
Bind during synthesis
b)
Bind to intron/exon junctions
c)
Alter mRNA transport
d)
Inhibit protein interaction factors
e)
Binds to DNA and form a triplex
18.
An antisense agent that targets at the Ribosomal level can do so how?
a)
Bind at the start codon
b)
Mess with the interaction between mRNA and the ribosome
c)
Alter synthesis
d)
Alter mRNA transport
e)
Inhibit protein interactions
19.
How can you test for a non-antisense mechanism?
a)
Use a scrambled control ODN
b)
Chop the ODN into parts and test those
c)
There is no test
d)
Use a different primary sequence
e)
Use a different secondary sequence
20.
What are ribozymes?
a)
RNA assembled into a tertiary structure with catalytic activity
b)
RNA assembled into a quarternary structure with catalytic activity
c)
RNA assembled into a tertiary structure with non-catalytic activity
d)
RNA assembled into a quaternary structure with non-catalytic activity
21.
What are some issues associated with antisense/RNA drugs?
a)
Charge and cellular uptake
b)
Vacuole, endosomal, liposomal trapping
c)
Endo/exonuclease degradation
d)
Specificity
e)
Affinity
22.
Kynamro…
a)
Is used to treat high cholesterol
b)
Blocks apolipoprotein B-100 synthesis
c)
Is expensive
d)
Contains phosphorothioate linkages
e)
Contains 2'OH substituted groups with methoxyethyl groups
23.
Onpattro (Patisiran)…
a)
Is the first RNAi drug approved by the FDA
b)
Is used to treat peripheral neuropathy
c)
Is LNP formulated
d)
Is used to treat high cholesterol
e)
Is an anticancer agent
24.
Milasen…
a)
Is used to treat Batton disease
b)
Targets the primary sequence in an intron involved with RNA splicing
c)
Is used for a very rare disease
d)
Took years to develop
e)
Took months to develop
25.
What's a method to increase aqueous solubility of a drug?
a)
Attach a polar group
b)
Increase lipophilicity
c)
Modify a drug for rapid metabolization
d)
Mask a drug for slower activation
26.
What's a method to increase site specificity of a drug?
a)
Add a group that is metabolized only at a certain organ
b)
Add a group that naturally decays inside the body
c)
Modify a drug for rapid metabolization
d)
Mask a drug for slower activation
27.
A bipartate prodrug is comprised of…
a)
A carrier
b)
The drug
c)
A linker
d)
Another drug
28.
A tripartate prodrug is comprised of…
a)
A carrier
b)
The drug
c)
A linker
d)
Another drug
29.
A mutual pro-drug (a co-drug) is comprised of…
a)
A carrier
b)
The drug
c)
A linker
d)
Another drug
30.
What are some advantages of an ester pro-drug?
a)
Synthesis is straightforward
b)
Various hydrophilicity can be achieved
c)
Easily modifiable for solubility
d)
Differing ester stabilities
31.
Ampicillin is an example of…
a)
A tripartate prodrug
b)
A bipartate produg
c)
A carrier-linked prodrug
d)
A mutual prodrug
32.
Sultamicillin is an example of…
a)
A tripartate prodrug
b)
A bipartate produg
c)
A carrier-linked prodrug
d)
A mutual prodrug
33.
What method of activation causes cyclophosphamides to become active?
a)
Oxidative
b)
Reductive
c)
Nucleotide
d)
Phosphorylation
e)
Decarboxylation
34.
How does the Thiamin precursor become activated?
a)
Reductive
b)
Oxidative
c)
Nucleotide
d)
Phosphorylation
e)
Decarboxylation
35.
What bioprecursor activation method does thioinosinic acid (TIMP) use?
a)
Nucleotide
b)
Oxidative
c)
Reductive
d)
Phosphorylation
e)
Decarboxylation
36.
How is acyclovir activated?
a)
Phosphorylation
b)
Nucleotide
c)
Oxidative
d)
Reductive
e)
Decarboxylation
37.
How does Remdesivir become activated?
a)
Carrier Cleavage
b)
Phosphorylation
c)
Nucleotide
d)
Reductive
e)
Decarboxylation
38.
What neurotransmitter undergoes a decarboxylation activation in the kidneys?
a)
Dopamine
b)
Norepinephrine
c)
Dopayours
d)
GABA
e)
Acetylcholine
39.
What is the bioavailability of an IV infused drug?
a)
1
b)
0.75
c)
0.5
d)
0.25
e)
<.25
40.
Which of the following factors affect solubility?
a)
pKa
b)
Local pH
c)
logP
d)
Particle Size
e)
Surface Area
41.
Compounds that form highly ordered crystals tend to have…
a)
Higher MP, Lower solubility
b)
Lower MP, Higher solubility
c)
Higher MP, Higher solubility
d)
Lower MP, Lower solubility
42.
Which of the following characteristics can lead to poor solubility?
a)
High # of H-Bond donors/acceptors
b)
Planar conformations
c)
Inflexible Conformations
d)
Low number of H-Bond donors/acceptors
43.
A compound with a logP of 4.0 would be expected to have…
a)
Poor aqueous solubility
b)
Good aqueous solubility
44.
Introduction of ionizable or polar groups is a viable method to reduce lipophilicity.
a)
true
b)
false
45.
Drug diffusion through aqueous pores between intestinal enterocytes is known as…
a)
Paracellular pathway
b)
Transcellular pathway
c)
Intracellular pathway
d)
Extracellular pathway
e)
Enterocellular pathway
46.
The use of natural products in relation to their human anatomy or mimicry of a disease state is known as…
a)
Doctrine of signatures
b)
Apothecary
c)
Alchemy
d)
Convalescence
e)
Hepatica
47.
What is the prototypical text for Ancient Egypt's pharmacopeia?
a)
Ebers Papyrus
b)
Ayurveda
c)
Humors
d)
De Materia Medica
e)
Mandrake
48.
What's the traditional medicine name for Ancient India?
a)
Ayurveda
b)
Ebers Papyrus
c)
Humors
d)
De Materia Medica
e)
Mandrake
49.
What toxic chemical(s) are found in Borage?
a)
Pyrrolizodine alkaloids
b)
cis-isoasarone
c)
NDGA
d)
Diterpenoids
e)
Triterpenoid saponins
50.
What are the touted benefits of Borage?
a)
Diuretic
b)
Expectorant
c)
Antidiarrheal
d)
Painkiller
e)
Pregnancy prevention
51.
What toxic chemical(s) are found in Sweet Flag (Calamus)?
a)
cis-isoasarone
b)
Pyrrolizodine alkaloids
c)
NDGA
d)
Diterpenoids
e)
Triterpenoid saponins
52.
What are the touted benefits of Sweet Flag (Calamus)?
a)
Digestive upsets
b)
Colic
c)
Febrifuge
d)
Antidiarrheal
e)
Expectorant
53.
What toxic chemical(s) are found in Chapparal?
a)
NDGA
b)
Pyrrolizodine alkaloids
c)
cis-isoasarone
d)
Diterpenoids
e)
Triterpenoid saponins
54.
What toxic chemical(s) are found in Coltsfoot?
a)
Pyrrolizidine alkaloids
b)
NDGA
c)
cis-isoasarone
d)
Diterpenoids
e)
Triterpenoid saponins
55.
What are the touted benefits of Coltsfoot?
a)
Coughs
b)
Bronchial congestion
c)
Colic
d)
Febrifuge
e)
Antidiarrheal
56.
What toxic chemical(s) are found in Comfrey?
a)
Pyrrolizadine alkaloids
b)
NDGA
c)
cis-isoasarone
d)
Diterpenoids
e)
Triterpenoid saponins
57.
What toxic chemical(s) are found in Germander?
a)
Diterpenoids
b)
NDGA
c)
Pyrrolizadine alkaloids
d)
Triterpenoid saponins
e)
cis-isoasarone
58.
What are the touted benefits of Germander?
a)
anorectic
b)
Bronchial congestion
c)
colic
d)
Antidiarrheal
e)
Expectorant
59.
What are the touted benefits of Licorice?
a)
Expectorant
b)
Demulcent
c)
Bronchial Congestion
d)
Febrifuge
e)
Colic
60.
What are the toxic effects of Licorice?
a)
pseudoaldosteronism
b)
hyperaldosteronism
c)
hypoaldosteronism
d)
pseudohyperaldosteronism
e)
pseudohypoaldosteronism
61.
What toxic chemical(s) are found in Poke Root?
a)
Triterpenoid saponins
b)
Pyrrolizodine alkaloids
c)
cis-isoasarone
d)
Diterpenoids
e)
NDGA
62.
What are the touted benefits of Sassafras?
a)
Blood purification
b)
Stimulant
c)
Antispasmodic
d)
Antirheumatic
e)
Colic
63.
What family of CYP enzymes are primarily responsible for Phase I metabolism?
a)
CYP3A
b)
CYP2D6
c)
CYP2C9
d)
CYP2C19
e)
CYP2E1
64.
What family of enzymes make up the bulk of Phase II metabolism?
a)
UGTs
b)
STs
c)
NATs
d)
COMT
e)
HMT
65.
Which natural product(s) has Saquinivir been proven to interact with?
a)
Garlic
b)
Rosemary
c)
Thyme
d)
Coriander
e)
Allspice
66.
Garlic has the following effects on PK profiles…
a)
CYP3A4 inducer (high doses)
b)
CYP3A4 inhibitor (low doses)
c)
CYP2C19 inducer
d)
CYP2D6 inhibitor
e)
CYP2D6 inducer
67.
Ginkgo Biloba has the following effects on PK profiles…
a)
CYP3A4 inhibitor
b)
CYP2C19 inducer
c)
CYP3A4 inducer
d)
CYP2C19 inhibitor
e)
CYP2C19 inducer
68.
Valerian has the following effects on PK profiles…
a)
CYP3A4 inhibitor
b)
CYP2D6 inhibitor
c)
CYP2C19 inducer
d)
CYP2C19 inhibitor
e)
CYP2D6 inducer
69.
Echinacea has the following effects on PK profiles…
a)
CYP3A4 inhibitor
b)
CYP3A4 inducer (long term)
c)
CYP2D6 inducer
d)
CYP2D6 inhibitor
70.
Ginseng has the following effects on PK profiles…
a)
CYP3A4 inhibitor
b)
CYP3A4 inducer
c)
CYP2D6 inducer
d)
CYP2D6 inhibitor
e)
CYP2C19 inducer
71.
Grape seeds (in high doses) have the following effects on PK profiles…
a)
CYP3A4 inducer
b)
CYP3A4 inhibitor
c)
CYP2C19 inducer
d)
CYP2C19 inhibitor
72.
Kava has the following effects on PK profiles…
a)
PXR activator
b)
CYP3A4 inducer
c)
CYP3A4 inhibitor
d)
CYP2C19 inhibitor
e)
CYP2C19 inducer
73.
St John's Wort has the following effects on PK profiles…
a)
PXR activator
b)
CYP3A4 inducer
c)
P-gp activator
d)
CYP2C19 inhibitor
e)
CYP2C19 inducer
74.
Grape seed has the following effects on PK profiles…
a)
CYP3A4 inducer
b)
CYP3A4 inhibitor
c)
P-gp activator
d)
PXR activator
e)
PXR inhibitor
75.
Black pepper has the following effects on PK profiles…
a)
CYP3A4 inhibitor
b)
P-gp inhibitor
c)
CYP3A4 inducer
d)
P-gp inducer
e)
PXR inhibitor
76.
Seville orange has the following effects on PK profiles…
a)
CYP3A4 inhibitor
b)
P-gp inhibitor
c)
OATP inhibitor
d)
OATP inducer
e)
P-gp inducer
77.
Goldenseal has the following effects on PK profiles…
a)
CYP3A4 inhibitor
b)
CYP2D6 inhibitor
c)
P-gp inhibitor
d)
PXR inhibitor
e)
PXR activator
78.
Which of the following is not an advantage of a prodrug?
a)
Affinity
b)
Site specificity
c)
Metabolic stability
d)
Solubility
e)
None of the above
79.
Which of the following is not correct?
a)
A tripartrate drug is the drug-linker-carrier
b)
Co-drugs are carrier prodrugs
c)
Carrier-linked prodrugs are typically activated through esterases
d)
Carrier prodrugs usually involve a hydroxy or carboxylic acid linkage through an ester bond
e)
None of the above
80.
Which of the following about Remdesevir is incorrect?
a)
It's a sort of bioprecursor drug
b)
It's a sort of carrier prodrug
c)
To activate, it involves phosphorylation
d)
To activate, it's oxidized by CYP450 enzymes
e)
None of the above
81.
A poorly soluble drug with a logP <3.50 can gain permeability by reducing its lipophilicity further
a)
true
b)
false
82.
Hydrophillic molecules can be transported by which of the following methods?
a)
Transporters
b)
Carrier-mediated endocytosis
c)
Paracellular pathway
d)
Diffusion
e)
P-gp
83.
Lipophillic molecules can be transported by which of the following methods?
a)
Diffusion
b)
P-gp
c)
Carrier-mediated endocytosis
d)
Paracellular pathway
e)
Transporters
84.
How does the pro-drug DHPG-CDS (Ganciclovir) gain access through the BBB?
a)
Lock-in mechanism
b)
Lock-and-key mechanism
c)
Esterases on the outside of the BBB
d)
Esterases on the inside of the BBB
e)
A direct injection into the frontal lobe
85.
What are mechanisms by which a drug can cross the BBB?
a)
Lock-in mechanism
b)
Use of the Large Amino-acid Transporter (LAT)
c)
Lock-and-key mechanism
d)
Diffusion
e)
Paracellular pathway
86.
What percentage of CNS drug candidates can actually cross the BBB?
a)
2
b)
4
c)
16
d)
32
e)
64
87.
What is/are the active ingredient(s) in Ginkgo?
a)
Flavones
b)
Lactones
c)
Phenolics
d)
Isoflavones
e)
Silymarin
88.
What is/are the active ingredient(s) in Echinacea?
a)
Phenolics
b)
Flavones
c)
Isoflavones
d)
Fatty acids
e)
Allicin
89.
What is/are the active ingredient(s) in Garlic
a)
Allicin
b)
Saponins
c)
Proanthocyanidins
d)
Fatty Acids
e)
Isoflavones
90.
What is/are the active ingredient(s) in Soy Bean?
a)
Isoflavones
b)
Saponins
c)
Flavones
d)
Silymarin
e)
Fatty Acids
91.
What is/are the active ingredient(s) in Saw Palmetto?
a)
Fatty Acids
b)
Isoflavones
c)
Saponins
d)
Phenolics
e)
Silymarin
92.
What is/are the active ingredient(s) in St. John's Wort?
a)
Hypericins
b)
Isoflavones
c)
Saponins
d)
Proanthocyanidins
e)
Silymarin
93.
What is/are the active ingredient(s) in Valerian?
a)
Valeric Acid
b)
Fatty Acids
c)
Lactones
d)
Phenolics
e)
Silymarin
94.
What is/are the active ingredient(s) in Cranberry?
a)
Proanthocyanidins
b)
Valeric Acid
c)
Fatty Acids
d)
Saponins
e)
Isoflavones
95.
What is/are the active ingredient(s) in Milk Thistle?
a)
Silymarin
b)
Proanthocyanidins
c)
Fatty Acids
d)
Valeric Acid
e)
Isoflavones
96.
Of the following, which of these factors do not affect drug solubility?
a)
local pH
b)
affinity
c)
logP
d)
pKA
e)
none of the above
97.
Which of the following is true regarding drug permeability?
a)
For small, neutrally charged molecules, paracellular diffusion is the primary mechanism
b)
For charged molecules, transcellular diffusion is the primary mechanism
c)
Influx transporters and efflux pumps negatively affect permeability
d)
Hydrophilic drugs utilize transcellular diffusion
e)
Lipophilic drugs utilize transcellular diffusion
98.
With regards to both Thalidomide and methylated Thalidomide, which is correct?
a)
The small MW of Thalidomide makes it more soluble
b)
The activated amide of Thalidomide makes it more soluble
c)
Methylated Thalidomide is more soluble due to the reduction of its crystal lattice energy
d)
Methylated Thalidomide has reduced H-Bond donors which contributes to its increase in solubility
e)
None of the above
99.
Regarding these three compounds, which of the following is true?
a)
Ganciclovir is BBB permeable
b)
DHPG-CDS is a prodrug for Ganciclovir and also BBB permeable
c)
Cpd 1 is a prodrug of DHPG-CDS
d)
Cpd 1 can be obtained by reducing DHPG-CDS
100.
Which of these two drugs is BBB permeable and why?
a)
Both, due to ionizable functional groups
b)
Gabapentin solely because it's a bioprecursor to GABA
c)
Gabapentin because it's a carrier-linked prodrug
d)
Gabapentin because it's a substrate for the LAT
e)
Gabapentin due to its high aqueous solubility
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