Science Quiz / Dr. Smith's Final Drugs

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

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

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