Antibacterial- Folic Acid Inhibitors

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    are necessary for the synthesis of Aminoacids, hence necessary for bacterialprotein synthesis

    growth of micro-organisms

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    SulfonamidesSulfadiazine

    SulfamethoxazoleSulfisoxazoleSulfamethizole

    DiaminopyrimidineTrimethoprim

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    Derivatives of sulfanilamidesFirst drug to prevent and cure human

    bacterial infection successfullybacteriostatic(stops bacteria fromreproducing)

    Structural analogs of para-aminobenzoic acid (PABA)

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    MOA: competitively inhibitdihydropteroate synthase

    SOA: broad spectrum agents; againstmany gram positive organisms(Streptococcus pyogenes,Streptococcus pneumoniae ) and certaingram negative organism ( Haemophilus

    influenzae, Escherichia coli, Proteusmirabilis ) and other strain Chlamydiatrachomatis, Nocardia, Actinomyces,Bacillus anthracis

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    Inhibited bySULFONAMIDES Dihydropteroate

    synthase

    Dihydrofolate

    reductase

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    INDICATION: Often used to treat urinary tract

    infections(E. coli) including acute andchronic cystitis, and chronic upper UTITx for nocardiosis, trachoma, inclusionconjunctivitis and dermatitis herpetiformis

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    Sulfadiazine + Pyrimethamine tx oftoxoplasmosis

    Px should take 2liters fluid to avoid UTcomplicationPyrimethamine: Ldose=75mg; 25mg

    daily& Sulfadiazine= 1g/every 6 hours; for3-6 wks

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    Cotrimoxazole*=Sulfamethoxazole +Trimethoprim

    Tx for Pneumocystis carinii pneumonia,Shigella enteritis, Serratia sepsis, UTI*,respiratory infections, gonococcalurethritisDOC for Stenotrophomonas maltophiliaIncreased frequency of Cutaneoushypersensitivity for AIDS Px

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    Sulfisoxazole + Erythromycin = AcuteOtitis Media ( H. Influenzae)

    Sulfisoxazole + Phenazopyridine =uncomplicated UTI (relief of Sx of pain,

    burning, urgency)

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    Prophylactic sulfonamide therapy toprevent Streptococcal infections andrheumatic fever recurrences

    PRECAUTIONS:May cause blood dyscrasias (HemolyticAnemia)

    For Px w/ G6PD deficiency, AplasticAnemia, Thrombocytopenia,Agranulocytosis, Eosinophilia

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    Life Threatening Hepatitis Caused by drug toxicity (rare SE) Headache, nausea, vomiting, jaundice

    Hypersensitivity (manifest in skin&mucous membranes)

    skin rashexfoliative dermatitisphotosensitivity

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    Trimethoprim

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    Substituted pyrimidineCommonly combined withsulfamethoxazole

    MOA: Inhibits dihydrofolate reductasethus blocking bacterial folic acidsynthesis

    SOA: most gram negative and grampositive microorganism

    *If used alone may develop resistance

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    SOA: Streptococcus pneumoniae,Neisseria meningitidis,

    Corynebacterium diphtheriae ; somestrains of Staphylococcus aureus,Staphylococcus epidermidis, Proteusmirabilis, Enterobacter, Salmonella,Shigella, Serratia, Klebsiella andEscherichia coli

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    Inhibited byTRIMETHOPRIM

    Dihydropteroatesynthase

    Dihydrofolate

    reductase

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    INDICATION:Tx for UTI caused by E. coli, P. mirabilis,Klebsiella and Enterobacter

    Tx for acute gonococcal urethritis, acuteexacerbation of chronic bronchitis,shigellosis, and Salmonella infections

    Prophylactic/Suppressive therapy for P.Carinii pneumoniaDOC for Stenotrophomonas maltophiliainfections

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    PRECAUTIONSSkin sensitization (rash, pruritus,exfoliative dermatitis)Blood dyscrasia(rarely)Adverse GI effect(nausea, vomiting,epigastric distress glossitis)Neonate may develop kernicterusAIDs Px may suffer from fever, rash,malaise, pancytopenia