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NUSCTX 110 Midterm 1 Questions with Detailed
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Quiz: On-Target Toxicity
Ans: Toxic effect due to the drug interacting with the intended therapeutic
target
Quiz: Off-Target Toxicity
Ans: Toxic effect due to the drug interacting with an unintended biological
target or unintended tissue
Quiz: Idiosyncratic drug reactions
Ans: drug reactions that occur rarely and unpredictably
Quiz: Idiopathic drug reactions
Ans: when the cause of toxicity in a drug is unknown
Quiz: Rosiglitazone
Ans: •It was prescribed as an insulin sensitizer for diabetics by binding to
PPAR-gamma receptors in adipocytes•First released in 1999, annual sales
peaked at 2.5 billion in 2006 and use has declined dramatically after drug
was found to increase risk of heart attacks.•Adverse effects subject to over
13,000 lawsuits and has been estimated to have caused 83,000 heart attacks
Sunday, 02 March 2025
,in the US•Rosiglitazone causes on-target edema which can put people at
risk for congestive heart failure—occurs through reduced renal excretion of
sodium and increase in sodium and water retention
Quiz: Non-Steroidal Anti-Inflammatory Drugs
Ans: Non-Steroidal Anti-Inflammatory Drugs—Aspirin, Ibuprofen, Diclofenac,
Naproxen, acetaminophen•Used for pain relief, inflammation, fever
reduction and swelling, arthritis, headache•Acetylsalicilic acid (active
ingredient of aspirin) is produced by plants including willow bark and spiraea
Quiz: Rofecoxib (Vioxx)
Ans: •COX2-selective inhibitor with very little gastrointestinal side-
effects•Prescribed to over 20 million people as a pain reliever for
arthritis•was found to be responsible for increased risk of heart attack and
stroke•Recalled in 2004; Financial damage: nearly $6 billion in
litigation•Largest drug recall in history•Merck and FDA criticized for ignoring
evidence of dangers of Vioxx before its eventual recall•140,000 people
could have suffered serious coronary heart disease from taking the drug in
just the U.S.•Studies have shown that COX2 is responsible for synthesis of
prostacyclins in the vasculature which are cardioprotective•COX2-selective
inhibition reduces the cardioprotective prostacyclin and causes cardiac
events
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,Quiz: Diphenhydramine
Ans: •Diphenhydramine also crosses the blood brain barrier where H1
histamine receptor antagonism causes sleepiness.•Modern antihistamines,
such as claritin, do not cross the blood brain barrier
Quiz: Toxicology
Ans: Toxicology is the study of adverse effects of chemicals on living
systems, including:•Mechanisms of action and exposure to chemicals as a
cause of acute and chronic illness.•Recognition, identification, quantification
of hazards from occupational exposure to chemicals. •Discovery of new
drugs and pesticides and characterizing their safety, ADME,
toxicology.•Development of standards and regulations to protect humans
and the environment from adverse effects of chemicals.
Quiz: Terfenadine
Ans: a non-sedating antihistamineformerly used for treatment of allergic
conditions by Sanofi Aventis•Was used by over 100 million patients by 1990
and made over $440 million•Replaced by fexofenadine in the 1990s due to
risk of cardiac arrhythmia
Quiz: Thalidomide
Ans: •Thalidomide was an anti-nausea and sedative drug that was
introduced in the late 1950s to be used to help with morning sickness•1950s
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, to 1960s: more than 10,000 children in 46 countries were born with deformities
such as phocomelia involving shortened limbs R-thalidomide stimulates the
GABA receptor to cause sedative effects. •S-thalidomide binds to a protein
and inactivates a protein called cereblon (CRBN), an E3 ubiquitin ligase that,
when bound to thalidomide, recruits neo-substrates to ubiquitinate and
proteasomally degrade them—including a recently identified transcription
factor called SALL4 which is involved in limb outgrowth and development
Quiz: 1.How do most small-molecule drugs that are in the clinic work
to exert their therapeutic action?
Ans: a.Most small-molecule drugs bind to a pocket in a protein and inhibits
or activates that protein, but that protein is not degraded
b.Most small-molecule drugs bind to a gene and turn on or turn off that gene
c.Most small-molecule drugs edit your genome to repair inborn errors
d.Most small-molecule drugs bind to a pocket in a protein and gets
degraded
Quiz: 2.What is involved in a typical drug discovery campaign to get
to clinical trials?
Ans: a.Target selection, screening small-molecule libraries to discover hits,
take the hit compound and file an IND to the FDA and enter Phase I clinical
trials
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