Dr. Smith's Final Drugs

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

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

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Created Dec 6, 2011ReportNominate
Tags:description, drug, final, smith