Dr. Smith's Final Drugs

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

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

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