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WorksheetsStatins
Total questions: 70
Worksheet time: 48mins
Statins target de novo cholesterol biosynthesis in liver
true
false
Liver compensates by
increasing LDLR
clears LDL and VDLDS from blood
decrease LDLR
PJ is a 4.5 year old boy. At his checkup, the pediatrician notices cutaneous xanthomas and orders a lipid panel. Repeated measures confirm that the patient's serum cholesterol levels are high (936 mg/dL). Further testing confirms a diagnosis of homozygous familial hypercholesterolemia. Which of the following interventions will be LEAST effective in this patient?
Atorvastatin
Ezetimibe
Lomitapide
Mipomersen
Niacin
Which of the following are enzymes involved in cholesterol biosynthesis that are good targets for drugs?
HMG CoA Reductase
Squalene Synthase
PCDK9
NPC1L1
Which of the following are enzymes that serve as targets to statins?
HMG CoA Reductase
Squalene Synthase
PCDK9
NPC1L1
Inhibitors were designed based on the intermediate in cholesterol biosynthesis
true
false
3,5 dihydroxy acid in statins mimics the tetrahedral intermediate produced by
HMG CoA Reductase
Squalene Synthase
Statins are transition state inhibitors
true
false
Plasma cholesterol can be lowered by
decrease liver cholesterol biosynthesis
increase in LDL receptors leading to increase uptake in liver
decrease VLDL precursors
increase liver cholesterol biosynthesis
Stereochemistry in the pharmacophore is required in which positions?
3R
5R
3S
5S
Which of the following functional groups are present in Ring A?
two cyclohexane rings
hydroxyl group at R1
Metyl substitution at R2
5-6 member heterocyclic ring attached with floro-phenyl
R= Aryl groups/hydrocarbon chains/amides/DO2/NH2
Which of the following functional groups are present in Ring B?
two cyclohexane rings
hydroxyl group at R1
Metyl substitution at R2
5-6 member heterocyclic ring attached with floro-phenyl
R= Aryl groups/hydrocarbon chains/amides/DO2/NH2
Essential for anchoring the compound to enzyme active site
two cyclohexane rings
hydroxyl group at R1
Metyl substitution at R2
Increase hydrophilicity and may provide some cellular specificity
two cyclohexane rings
hydroxyl group at R1
Metyl substitution at R2
Increase activity
two cyclohexane rings
hydroxyl group at R1
Metyl substitution at R2
Lovastatin is more potent that Simvastatin
true
false
Which of the following have a short duration of action (2 hours)?
Lovastatin
Simvastatin
Pravastatin
Atorvastatin
Fluvastatin
Which of the following does not have to be taken at bedtime?
Lovastatin
Simvastatin
Pravastatin
Which of the following are true about Pravastatin?
neutral
lipophilic
acidic
hydrophilic
less muscle penetration
Which of the following are true about Lovastatin and Simvastatin?
neutral
lipophilic
acidic
hydrophilic
less muscle penetration
Which structure is a hydrophilic statin and most likely to have less muscle penetration?
According to these structures, which drug is more potent?
Which of the following is true about Simvastatin and Lovastatin?
active metabolite is the acid form
further metabolized in liver (CYP3A4)
excreted mainly in feces (84%)
extensive first pass metabolism
metabolized into active metabolite (less activity): CYP3A4 substrate minor
Which of the following is true about Pravastatin?
active metabolite is the acid form
further metabolized in liver (CYP3A4)
excreted mainly in feces (84%)
extensive first pass metabolism
metabolized into active metabolite (less activity): CYP3A4 substrate minor
Which of the following drugs belong to the Ring B group?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Simvastatin
This drug belongs to the Ring B group, but has a short duration of action, similar to Ring A
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Simvastatin
Which of the following have a long duration of action and can be taken any time of the day?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Simvastatin
Which of the following lipophilic statins?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Simvastatin
Which is the MOST lipophilic statin?
Atorvastatin
Fluvastatin
Which is a racemic mixture?
Atorvastatin
Fluvastatin
Which of the following are acidic statins?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Which of the following are true about Rosuvastatin?
it's amphoteric
most hydrophilic statin
less muscle pain
most potent
more muscle pain
Which of the following is 99% protein bound?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Which of the following has an extensive first pass metabolism?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Which of the following does not have an extensive first pass metabolism and is excretes unchanged in feces?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Which of the following has least first pass metabolism (high bioavailability) and is excreted in feces?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Which of the following are excreted in feces?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Which of the following is excreted in bile (less by kidneys)?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Which of the following is metabolized to an equipotent metabolite (CYP3A4) that has an increased half life of 20-30 hours?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Which of the following has a strong affinity for CYP2DC6?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Which of the following has some metabolism by CYP2C9 (~10%)?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Which of the following is majorly metabolized by UDP-glucuronosyltransferase (UGT1A3 & UGT2B7)?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Which of the following is less likely to interact with drugs metabolized by 3A4 and is good in geriatric patients?
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Which of the following require OAT?
anionic form (free acid) to be transported into hepatocytes
active from (not prodrugs) of all statins
cationic form (free acid) to be transported into hepatocytes
Which functional group is responsible for making Pravastatin the second most hydrophilic statin?
A
B
Rosuvastatin is the most hydrophilic because of
A
B
C
Atorvastatin is more potent than Rosuvastatin
true
false
Pitavastatin has the least first pass metabolism because of
A
B
C
Which structure represents a Ring B statin?
Atorvastatin and Rosuvastatin have long half lives but, Atorvastatin lasts longer
true
false
Significant interactions with drugs affecting CYP3A4, PgP and OAT1B1
Atorvastatin
Fluvastatin
Rosuvastatin
Pitavastatin
Atorvastatin causes more muscle problems because it's the most lipophilic
true
false
Not all statins can interact with OAT1B1 hepatocytes
true
false
Which statins can be taken at any time at any time of the day?
Atorvastatin
Rosuvastatin
Pitavastatin
Pravastatin
Which of the following are true about drug-drug interactions of statins with OATPB1 inhibitors?
Gemfibrozil and Cyclosporin
Fluvastatin and Rosuvastatin can be used with cyclosporin and gemfibrozil at reduced doses
Fluvastatin and Rosuvastatin can't be used with OATP1B1 inhibitors
Fluvastatin + Gemfibozil recommended dose
avoid
20mg max
Fluvastatin + Ciclosporin recommended dose
avoid
20mg max
Which of the following are true about the drug-drug interactions of statins with CYP3A4 inhibitors?
macrolide antibiotics
azole antifungals like ketoconazole
HIV protease inhibitors
interaction with Atorvastatin, Simvastatin and Lovastatin
Naproxen, Aspirin, Acetaminophen
Which of the following are metabolized by CYP3A4?
Simvstatin
Lovastatin
Atorvastatin
Pravastatin (minor)
Pitavastatin
Which of the following are metabolized by CYP2C9?
Fluvastatin
Rosuvastatin
Atorvastatin
Pitavastatin
Which of the following are metabolized by glucorination?
Fluvastatin
Rosuvastatin
Atorvastatin
Pitavastatin
Rosuvastatin + Gemfibrozil recommended dose
10mg max
5mg max
avoid
Rosuvastatin + Cyclosporine recommended dose
10mg max
5mg max
avoid
Which of the following are true about statins?
can decrease LDL cholesterol levels dramatically
effective and well tolerated
decrease risk of coronary events and mortality in patients with ischemic heart disease (IHD)
can increase LDL cholesterol levels dramatically
Which of the following are true about toxicity of statins?
mild increase of serum aminotransferases (check ALT and AST)
severe muscle pain and even rhabdomyolysis
increase creatinine kinase (CK)
CYP inhibitors increase risk for hepatotoxicity and myopathy
decrease creatinine kinase (CK)
Statins are safe to use during pregnancy
true
false
Patients taking statins should not take grapefruit juice because it increases risk for hepatotoxicity and myopathy
true
false
Fluvastatin is the most potent drug and Rosuvastatin is the least
true
false
Which statin would not be prescribed to a patient who has myopathy?
Fluvastatin
Rosuvastatin
Atorvastatin
Pitavastatin
Which of the following are lactone derivates?
Lovastatin
Simvastatin
Pravastatin
Rosuvastatin
Pitavastatin
