Dr. Smith's Final Drugs

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

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

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