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    ANTIBIOTICS ST

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    Joram David Beltran
    Antibiotics can be categorized based on their mechanism of action. Some major categories include cell wall synthesis inhibitors like beta-lactam antibiotics such as penicillins and cephalosporins. Other categories are protein synthesis inhibitors that target the 30S or 50S ribosomal subunits, such as tetracyclines, aminoglycosides, macrolides and oxazolidinones. Nucleic acid synthesis inhibitors inhibit RNA polymerase or topoisomerases, including rifampicin and fluoroquinolones. Antitubercular drugs used as first line therapy are rifampicin, isoniazid, pyrazinamide and ethambutol. Second line drugs include aminogly

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    ANTIBIOTICS ST

    Uploaded by

    Joram David Beltran
    39 views29 pages
    Antibiotics can be categorized based on their mechanism of action. Some major categories include cell wall synthesis inhibitors like beta-lactam antibiotics such as penicillins and cephalosporins. Other categories are protein synthesis inhibitors that target the 30S or 50S ribosomal subunits, such as tetracyclines, aminoglycosides, macrolides and oxazolidinones. Nucleic acid synthesis inhibitors inhibit RNA polymerase or topoisomerases, including rifampicin and fluoroquinolones. Antitubercular drugs used as first line therapy are rifampicin, isoniazid, pyrazinamide and ethambutol. Second line drugs include aminogly

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    ANTIBIOTICS st

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    ANTIBIOTICS st

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    Antibiotics can be categorized based on their mechanism of action. Some major categories include cell wall synthesis inhibitors like beta-lactam antibiotics such as penicillins and cephalosporins. Other categories are protein synthesis inhibitors that target the 30S or 50S ribosomal subunits, such as tetracyclines, aminoglycosides, macrolides and oxazolidinones. Nucleic acid synthesis inhibitors inhibit RNA polymerase or topoisomerases, including rifampicin and fluoroquinolones. Antitubercular drugs used as first line therapy are rifampicin, isoniazid, pyrazinamide and ethambutol. Second line drugs include aminogly

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    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    39 views29 pages

    ANTIBIOTICS ST

    Uploaded by

    Joram David Beltran
    Antibiotics can be categorized based on their mechanism of action. Some major categories include cell wall synthesis inhibitors like beta-lactam antibiotics such as penicillins and cephalosporins. Other categories are protein synthesis inhibitors that target the 30S or 50S ribosomal subunits, such as tetracyclines, aminoglycosides, macrolides and oxazolidinones. Nucleic acid synthesis inhibitors inhibit RNA polymerase or topoisomerases, including rifampicin and fluoroquinolones. Antitubercular drugs used as first line therapy are rifampicin, isoniazid, pyrazinamide and ethambutol. Second line drugs include aminogly

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    of 29

    ANTIBIOTICS

    I. CELL WALL SYNTHESIS


    INHIBITORS
    A. BETA LACTAM ANTIBIOTICS
    B. GLYCOPEPTIDES
    C. CYCLOSERINE
    D. POLYPEPTIDE
    BETA LACTAM ANTIBIOTICS
    • Chemistry: beta-lactam ring
    • MOA: binds to penicillin-binding protein leading to the
    inhibition of cross-linking
    • Effective for: gram-positive infection and gram-
    negative infection
    • Ineffective for: wall-less microorganisms,
    microorganisms with atypical cell wall (mycolic acid),
    intracellular parasites, resistant microorganisms
    • ADE: hypersensitivity reactions
    • PENICILLINS, CEPHALOSPORINS, CARBAPENEMS, MONOBACTAM
    A.1. PENICILLINS
    • Example: Natural Penicillins
    • Pen G & Pen V
    • Isoxazolyl Penicillins
    • Cloxacillin, oxacillin, dicloxacillin,
    nafcillin
    • Extended Spectrum Penicillins
    • Aminopenicillins – amoxicillin,
    ampicillin, bacampicillin
    • Carboxypenicillins – carbenicillin,
    ticarcillin
    • Ureidopenicillins – piperacillin,
    azlocillin, mezlocillin
    A.2. CEPHALOSPORINS
    • 1st generation – all starts with “ceph” except Cefazolin
    & cefadroxil
    • 2nd generation – all starts with “cef”, nothing ends in
    the suffix “–one” or “–ine”, except cefuroxime and
    lovacarbef
    • 3rd generation – all starts with “cef”, all ends with “-
    one” or “-ime” except for cefdinir, ceftibuten,
    cefditoren, moxalactam
    • 4th generation – cefepime, cefpirome
    • 5th generation – ceftaroline, fosamil
    • COMMONLY USED: cefazolin, cefuroxime, cephamycin,
    ceftazidime, cefoperazone, cefixime, ceftriaxone,
    cefotaxime
    • A.3. CARBAPENEMS
    • Ex: imipenem + cilastatin, ertapenem, meropenem
    • A.4. MONOBACTAM
    • Ex: aztreonam
    B. GLYCOPEPTIDES
    • B.1. VANCOMYCIN
    • MOA: binds to D-ala-D-ala terminus of the nascent peptide
    chain
    • Clinical use: MRSA & MRSE
    • ADE: red man syndrome
    • B.2. TEICOPLAMIN
    • B.3. TELOVANCIN
    • Semi-synthetic lipopolysaccharide derived from vancomycin
    • B.4. DAIVABANCIN
    • Semi-synthetic lipopolysaccharide derived from
    teicoplamin
    • C. CYCLOSERINE
    • MOA: inhibition of two enzymes for synthesis of D-ala-D-ala

    • D. POLYPEPTIDE
    • Ex: Bacitracin
    • CHEM: mixed cyclic polypeptide
    • KINETICS: poorly absorbed systematically
    II. PROTEIN SYNTHESIS
    INHIBITORS
    A. INHIBITORS OF 30s RIBOSOMAL SUBUNIT
    B. INHIBITORS OF 50s RIBOSOMAL SUBUNIT
    INHIBITORS OF 30s RIBOSOMAL
    SUBUNIT

    A. TETRACYCLINE
    B. AMINOGLYCOSIDES
    A. TETRACYCLINES
    • CHEM: naphthacene ring
    • MOA: prevents the binding of aminoacyl tRNA to the
    ribosomal complex
    • Examples: tetracycline, doxycycline,
    demeclocycline, minocycline
    • Effective for: g (+) & g (-) bacteria, obligate
    intracellular parasites, spirochetes, protozoans,
    wall-less bacteria
    • ADE: permanent yellow staining of the teeth,
    hypoplasia of the teeth, ototoxicity,
    nephrotoxicity
    B. AMINOGLYCOSIDES

    • Mycin (Streptomyces); micin (micromonospora)


    • MOA: inhibition of the formation of initiation
    complex, misreading of mRNA, formation of
    nonfunctional polysomes
    • KINETICS: concentration-dependent killing;
    post-antibiotic effect; synergistic killing
    • ADE: ototoxicity, vestibulotoxicity,
    nephrotoxicity
    INHIBITORS OF 50s RIBOSOMAL
    SUBUNIT
    A. LINCOSAMIDES
    B. CHLORAMPHENICOL
    C. MACROLIDES
    D. OXAZOLIDINONES
    E. STREPTOGRAMINS
    A. LINCOSAMIDES
    • Examples: lincomycin, clindamycin
    • MOA: blocks the polypeptide exit tunnel leading
    to the dissociation of peptidyl tRNA from the
    ribosome
    • USE: soft tissue and skin infection
    B. CHLORAMPHENICOL
    • MOA: inhibition of peptidyltransferase
    • CHEM: nitro group
    • ADE: dose-dependent; gray-baby syndrome;
    aplastic anemia
    C. MACROLIDES
    • MOA: blocks the polypeptide exit tunnel leading
    to the dissociation of peptidyl tRNA from the
    ribosome
    • Examples: erythromycin, clarithromycin,
    azithromycin
    • ADE: abdominal cramps; jaundice; cardiotoxicity
    D. OXAZOLIDINONES
    • Example: linezolid
    • USE: treatment of VRSA/VRSE
    • ADE: thrombocytopenia
    E. STREPTOGRAMINS
    • Examples: Streptogramin A, Streptogramin B
    • USE: treatment of VRSA/VRSE
    III. NUCLEIC ACID
    SYNTHESIS INHIBITORS
    A. RIFAMYCINS
    B. QUINOLONES/FLUOROQUINOLONES
    A. RIFAMYCINS
    • Examples: rifampicin/rifampin; rifabutin
    • MOA: inhibits RNA polymerase
    • USE: 1st line agent for PTB/EPTB; 1st line agent
    for leprosy; prophylaxis for meningococcemia
    • ADE: red-orange discoloration of body fluids
    B. QUINOLONES/FLUOROQUINOLONES
    • MOA: inhibition of topoisomerase II and
    topoisomerase IV
    • GENERATIONS:
    • 1st (quinolones) – nalidixic acid, cinoxacin
    • 2nd (fluoroquinolones) – ciprofloxacin, ofloxacin,
    norfloxacin, enofloxacin, lomefloxacin
    • 3rd (fluoroquinolones) – levofloxacin, gatifloxacin,
    gemifloxacin, moxifloxacin, sparfloxacin
    • 4th (fluoroquinolone) - trovafloxacin
    • ADE:
    • abdominal discomfort, tendinitis/tendonitis,
    ototoxicity, photoxicity
    ANTITUBERCULAR
    DRUGS
    1ST LINE (HRZE)
    2ND LINE
    1ST LINE
    • RIFAMPICIN
    • ISONIAZID
    • CHEM: isonicotinic acid hydrazide
    • MOA: inhibits mycolic acid synthesis
    • ADE: hepatotoxicity, peripheral neuritis
    • KINETICS: metabolized by N-acetyltransferase
    1st LINE
    • PYRAZINAMIDE
    • Short-term management only
    • ADE: arthritis, hepatotoxicity
    • ETHAMBUTOL
    • MOA: inhibition of arabinosyl transferase
    • ADE: optic neuritis, red-green visual disturbance
    2nd LINE
    • Aminoglycosides (streptomycin)
    • Fluoroquinolones
    • Cycloserine
    • Thionamides
    • Para-aminosalicylic acid
    V. ANTIMETABOLITES
    SULFONAMIDES
    TRIMETHOPRIM AND PYRIMETHAMINE
    MISCELLANEOUS AGENTS (nitroimidazoles, urinary
    antiseptics)
    A. SULFONAMIDES
    • MOA: inhibition of dihydropteroate synthetase
    • CHEM: same structure with PABA
    • ADE: Steven-Johnson syndrome
    B. TRIMETHOPRIM AND PYRIMETHAMINE
    • MOA: inhibition of dihydrofolate reductase
    • ADE: megaloblastic anemia, pernicious anemia
    C. MISCELLANEOUS AGENTS
    • NITROIMIDAZOLES
    • Ex: metronidazole, tinidazole
    • USE: anaerobic infection below the diaphragm;
    pseudomembranous colitis, protozoan infection
    • ADE: metallic-after taste
    • URINARY ANTISEPTICS
    • Ex: nitrofurantoin
    • Prodrug: methenamine

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