Science Quiz / Dr. Smith's Final Drugs

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

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

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