Dna Synthesis Inhibitors

Front 1

anti folate drugs

Back 1

sulfonamides, trimethoprim

Front 2

dna gyrase inhibitors

Back 2

fluoroquinolones

Front 3

sulfonamides MOA

Back 3

compete with PABA, inhibit DHPS

Front 4

sulfonamides use

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broad spectrum G- and +, chlamydia trachomatis and some protozoa, bacteriostatic.

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how can sulfonamides be combined

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they become synergystic when combined with trimethoprim or pyreimethamine

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pharmacokinetics of sulfonamides

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metabolized in liver, eliminated by kidney

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clinical uses of sulfonamides

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UTI

Front 8

what is used for ulcerative colitis and IBS

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sulfasazaline

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topical use for

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trachoma, conjunctivitis

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drug of choice for pneumocystis jirovecci pneumonia and toxoplasmosis

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fixed combination of TMP-SMZ

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adverse reactions of sulfonamides

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urinary tract disturbances (crystalluria, hematuria or obstruction

Front 12

with what drugs are urinary tract disturbances less seen in

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sulfisoxazole

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crystalluria can be treated by

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administration of sodium bicarb and fluids

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adverse reactions of sulfonamides

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hematopoietic disturbances, stevens johnson syndrome

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mechanism of resistance for sulfonamides

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overproduction of PABA, DHPS, impair permeability of the drugs

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oral absorbable short acting sulfonamides

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sulfacytine, sulfisoxazole, sulfamethizole

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oral absorbable intermediate acting sulfonamides

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sulfadiazine, sulfamethoxazole

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oral absorbable long acting sulfonamides

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sulfadoxine

Front 19

oral non absorbable sulfonamides

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sulfasalazine

Front 20

topical use sulfonamides

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sodium sulfacetamide, mafenide acetate, silver sulfadiazine

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trimethoprim

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pyramidine derivitive, selectively inhibits DHFR, bacteriostatic

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trimethoprim use

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UTI

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sulfonamide + trimethoprim

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synergistic, bactericidal

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sulfonamide + trimethoprim use

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pneumocystis jirovecii pneumonia (PCP)

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trimethoprim and trimethoprim-sulfamethoxazole mechanism of resistance

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reduced cell permeability, overproduction of DHFR, altered DHFR

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primethoprim adverse reactions

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megloblastic anemia, granulocytopenia

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TMP-SMZ adverse reactions

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similar to sulfonamides (GI upset, renal damage, CNS disturbances)

Front 28

fluoroquiolones MOA and chemistry

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analog of nalidixic acid. Blocks DNA synthesis by inhibiting topoisomerase II and topoisomerase IV

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fluoroquinolones active against

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G+ and -

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DNA gyrase is

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a topoisomerase II that introduces negative supercoils into DNA

Front 31

fluoroquinolones

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norfloxacin, ciprofloxicin, enoxacin, ofloxacin, lomefloxacin, pefloxacin, levofloxacin, moxifloxacin, gemifloxacin

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active against G-

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ciprofloxacin

Front 33

superior activity against G+

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levofloxacin

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fluroquinolones pharmocokinetics

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oral absorption impaired by divalent cations, excreted by kidney

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which are eliminated by non renal mechanism

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moxifloxacin and gemifloxacin

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once daily dosing possible

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levofloxacin, gemifloxacin, moxifloxacin

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fluoroquinolones clinical uses

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UTI's and bacterial diarrhea

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drug of choice for the treatment of anthrax

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ciprofloxacin

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respiratory fluoroquinolones

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levofloxacin, gemifloxacin, moxifloxacin

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adverse reactions of fluoroquinolones

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QT prolongation, arthropathy (not routinely recommended for <18 yo, tendinitis, tendon rupture