Dr. Smith's Final Drugs

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Can you name the Dr. Smith's Final Drugs?

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Induces hemolysis in patients with glucose 6-phosphate dehydrogenase deficiency
Converted to alloxanthine which binds tightly with xanthine oxidase, which decreases urate production and xanthine and hypoxanthine concentrations rise
Nucleotide analog of deoxcycytidine used in treatment of pancreatic cancer
decrease efficiency of fat-soluble vitamin absorption due to their effect on bile acids.
Antibiotic that directly binds to ATP synthase and inhibits both ATP synthesis and the transfer of electrons through the electron transport chain
Its mechanism is to increase glutathione levels by supplying cysteine for the synthesis of glutathione
structure similar to dihydrofolate, thus can be a competitive inhibitor of dihydrofolate reductase.
Inhibits cyclooxygenase by acetylating the serine residue that lies along the path to the active site and blocks the channel
Analog of uracil used to treat breast and colorectal cancer.
Inhibits the production of prostaglandins;irreversible inhibitor
Bind bile acids, thus decrease absorption of exogenous (dietary) cholesterol.
competitively inhibiting HMG CoA reductase to inhibit endogenous cholesterol synthesis
Increases cytochrome b5 reductase
can also inhibit folate absorption by preventing the excess glutamates from being cleaved off
inhibits cell division in a similar manner as 6-mercaptopurine and is also inactivated by thiopurine methyltranserfase
Binds bacterial/protozoal dihydrofolate reductase proteins 10^5 more tightly than human DHFR
Herpes treatment
Marketed by Roche as CellCept(R)
peroxynitrite [ONOO-] scavenging compound
Used to treat acetaminophen overdose
Inhibits oxidative phosphorylation by binding to one of the ubiquinone binding sites on Complex III
Competitively inhibits dihydrofolate reductase and prevents the regeneration of tetrahydrofolate
Inhibits inducible nitric oxide synthase
Anticoagulant, similar to warfarin, which prevents the formation to carboxyglutamate in prothrombin.
Suicide inhibitor; is converted into FdUMP and forms a covalent intermediate with thymidylate synthase that cannot be reversed
the committed step of its reaction is the inhibition of the conversion of PRPP into PR-amine
Selective COX-2 inhibitor
Carboxylation of glutamate to carboxyglutamate in prothrombin requires the enzyme ________ and cofactor _________
Binds at ubiquinone binding site that is close to cytochrome bH on the matrix side membrane
similar structure to vitamin K and competitively inhibits carboxylase.
Combined antibiotic - sulfamethoxazole and trimethoprim
inhibits IMP dehydrogenase (IMP --> XMP [de novo pathway])
prodrug of 6-mercaptopurine
Inhibits the electron flow from the Fe-S centers of Complex I to ubiquinone, thus blocking oxidative phosphorylation
Inhibitor of pancreatic lipase, side effects are GI problems
Inhibits TMP production by preventing the regeneration of methylene-THF; used as an anticancer agent and in the treatment of rheumatoid arthritis
Drug used to treat sickle cell disease
Relieves symptoms of gout
Has a modified sugar which has 2 fluorine atoms at the 2' position rather than 2 hyrdogens. Can be twice phosphorylated by deoxycytidine kinase and then dCMP kinase and acts as a s
a prodrug of mycophenolic acid (MPA)
Anti-coagulant, binds to ant-thrombin which leads to a conformation change allowing anti-thrombin to bind to thrombin, which inactivates it, inhibiting the activation of fibrinogen
Is converted to fluorodeoxyuridylate (has a similar structure to deoxyuridylate), which irreversibly inhibits thymidylate synthase - suicide inhibition.
Common treatment for methemoglobinemia
If this drug is dosed >7mg/kg, then it becomes an oxidant
converted to the deoxynucleotide, which inhibits cell division.
Inhibits alpha-amylase, alpha-dextrinase, maltase, and sucrase
Anti cancer drug, can block the synthesis of thymidylate
Side effects: gastrointestinal problems due to fermentation of carbohydrates in large intestines and water holding capacity of the disaccharides.
Blocks electron flow from cytochrome bH to ubiquinone.
Large, bulky molecules;unable to bind to COX-1
Used in treatment of inflammatory bowel disease.
Vasodilator which releases NO
An alpha-glucosidase inhibitor. It delays carbohydrate digestion in the small intestines and thus decreases blood glucose in Diabetics (type II)
Phosphorylated by viral encoded thymidine kinase but not human thymidine kinase. Only infected cells efficiently phosphorylate the drugs, which then inhibit DNA replication
Inhibits bacterial synthesis of folate
An anti-inflammatory drug metabolized in the colon by intestinal bacteria to produce 5-aminosalicylic acid
used as an immunosuppressant in organ transplants and in patients with inflammatory bowel disease
Suicide inhibitor of xanthine oxidase
Associated with inflammation, cancer, colitis, and arthritis
inhibitor of pancreatic lipase
Phosphorylated by human kinases but selectively interfere with viral replication. Both have modified sugars that lack 3; OH group and in effect terminates DNA synthesis
Covalently binds to transpeptidase thus prevents synthesis of bacterial cell walls. Suicide inhibitor.
Inactivated by xanthine oxidase and thiopurine methyltransferase (TPMT).
non-prescription form of Orlistat
cytostatic against lymphocytes which almost entirely lack purine salvage and depend on de novo pathway for purines
Anticancer and rheumatoid arthritis agent that affects both DNA synthesis and de novo purine synthesis
It binds to the toxic metabolite (forming mercapturic acid) for excretion in the urine
prevents the necessary 1,3 hydride shift to reduce the CH2 to CH3 on methylenetetrahyrdofolate
Works by increasing the blood concentration of fetal hemoglobin
It catalyzes the conversion of arachidonic acid to prostaglandins

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