Dr. Smith's Final Drugs

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

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

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