Antibiotics

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Dr. Paul Ehlrich

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Discovered Salvarsan for treatment of Syphilis

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Alexander Fleming

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Discovered Penicillin

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What yeast species makes penicillin naturally?

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Penicillium notatum

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Florey and Chain

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Did the clinical trials for Penicillin

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Penicillin

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Prevents the formation of peptide cross bridge in PTG by inhibiting the transpeptidation RXN. Inhibits targeting the PBPs in cytoplasmic membrane

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All penicillins contain

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the beta-lactam ring

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penicillanase

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will break the beta lactam ring at the bottom portion where N binds to C=O

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Penicillin G

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most active and stable natural penicillin

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Penicillin V

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acid tolerant and given orally

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Pros of Natural Penicillin

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Non-toxic unless allergic, cheap, effective against G+ and some G- organsims

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Cons Of Natural Penicillin

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Unstable in Stomach acid (except Penicillin V), mainly effective against G+, and causes allergic reactions

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Semi-Synthetic Penicillins

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B-lactam ring is formed naturally by Penicillium notatum then side chain is formed synthetically. Acid resistant, resistant to penicillinase, and have broader spectrum of activity

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Methicillin

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penicillanase resistant, sterically hinders penicillnase from binding and breaking the beta-lactam ring. Has two OCH groups attached on ring at 1 and 5 position

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Ampicillin

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Broad spectrum and acid resistant. Has amine group in side chain

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Carbenicillin

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Broad spectrum, Has COONa in side chain

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Oxacillin

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Penicillanase resistant and acid resistant

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Augmentin

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Amoxicillin and Potassium clavulanate. Blocks penicillanase by blocking its active site

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Cephalosporins

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Product of Cephalosporium. Same mechanism of action as penicillin but has broader spectrum, more resistant to penicillinase, w/ increased pharmokinetic properties. Ceftriaxone use to treat gonorrhea.

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Vancomyocin

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Reacts w/ D-ala, D-ala termini of cross bridges in PTG, causing a steric hindrance in PTG biosynthesis. Useful for treating MRSA, is poorly absorbed, given by IV

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Bacitracin

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polypeptide produced by Bacillus subtillus. Interferes with dephosphorylation of lipid carrier that moves PTG precursors through membrane to cell wall. Used topically for G+ skin infections

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Polymyxins

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Basic peptide that will act as a cationic detergent to cause lysis of cell membrane. Used topically because is toxic due to cell membranes of Pro and Euk are similar. Bacteriocidal

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Polyenes

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Antifungal drug that targets ergosterol and inserts cylindrical channels into membrane allowing leakage of small molecules. Toxic to mammalian cells, will interact w/ cholesterol in high concentration. (Fungalcidal)

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Nystatin

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Type of Polyene, a topical cream but can also be given orally for intestinal candidiasis because it is poorly absorbed

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Amphotericin B

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Type of Polyene, given parenterally to function systemically, will cause renal dysfunction, nephrotoxic. Only used in life threatening situations

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Imidazoles

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antifungal, targets ergosterol biosynthesis in fungal membrane, will alter membrane permeability. (Fungalstatic)

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Micanozole and Clotrimazole

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good for candidiasis, broad spectrum. Highly toxic, used topically

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Ketoconazole

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Less toxic, used for systemic fungal infections. Type of Imidazole

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Fluconazole

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better than ketoconazole, has broader spectrum, better CNS penetration, and is safest for systemic use. Type of Imidazole

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Aminoglycosides

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Bacteriocidal due to 2 stage active transport that is irreversible. Inhibits proteins synthesis by interfering with bacterial tRNA binding to 30s ribosomal subunit. Is toxic to kidneys, therapeutic levels are close to toxic levels. Toxic 8th cranial nerve as well, causing hearing loss and incoordination. Poorly absorbed so has to be given by IV or IM. Anything mycin in it is this

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Tetracyclines

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Block protein sythesis by binding 30s ribosomal subunit and blocking the binding of tRNA to mRNA-ribosome complex. Will chelate divalent cations resulting permanent discoloration of teeth, and will imbed in bone. May suppress normal flora leading to overgrowth and super infection. Liver and kidney damage as well

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Chloramphenicol

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binds 50s ribsomal subunit and inhbits peptidyl transferase, thus blocking peptide bond formation. Highly toxic, and may interfere with RBC formation in bone marrow leading to aplastic anemia.

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Macrolides

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React with 50s ribosome to block translocation during translation. Effective against G+ with similar spectrum to penicillin G. Given to those allergic to penicillin. Ezythromyocin and azithromycin are examples

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Rifampin

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binds DNA dependent RNA pol, blocking transcription at initiation step. Effective against TB. Drug resistance is rapid due to mutation in beta subunit in RNA pol, used in combination with another drug usually

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Quinolones

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Inhibit DNA gyrases and topoisomerases, which are required for supercoiling of bacterial DNA into the cell.

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Nalidixic Acid

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once used to treat UTI, but resistance happened

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Fluoroquinolones

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have enhanced activity against G- and some G+. May accumulate in cartilage. Examples include ciprofloxacin and norfloxacin. Type of quinolone

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Sulfa Drugs

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Analog of Para amino benzoic acid, a precursor of folic acid. Folic acid is vitamin responsible for transfer of 1 carbon fragments in biosynthetic pathways. Will competitively compete with dihydropteroate synthase (makes FAH2)

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Trimethoprim

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structural analogs of pteridine portion of folic acid. Competitively inhibits Dihydrofolate reductase. Includes Bactrim and Septra

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Para-amino Salicylic acid

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treats TB, structural analog of PABA, will competitively compete with dihydropteroate synthase, same as Sulfa drugs

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Isoniazid

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Structural analog of Vitamin B6, or pyrodoxine, and will competitively inhibit reactions that use Vitamin B6, inhibiting mycolic acid synthesis in the process. Used in combo with Rifampin to treat TB.