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    Antimicrobial Drugs: Prepared By: Stephanie Lois R. Sanchez, RPH, MSPH

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    NERA AYON
    The document discusses the history and development of antimicrobial drugs including antibiotics, antifungals, antivirals, antiprotozoals, and antihelminthics. It describes the sources and mechanisms of action of these drugs as well as the development of drug resistance.

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    Antimicrobial Drugs: Prepared By: Stephanie Lois R. Sanchez, RPH, MSPH

    Uploaded by

    NERA AYON
    47 views38 pages
    The document discusses the history and development of antimicrobial drugs including antibiotics, antifungals, antivirals, antiprotozoals, and antihelminthics. It describes the sources and mechanisms of action of these drugs as well as the development of drug resistance.

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    Antimicrobial-Drugs

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    The document discusses the history and development of antimicrobial drugs including antibiotics, antifungals, antivirals, antiprotozoals, and antihelminthics. It describes the sources and mechanisms of action of these drugs as well as the development of drug resistance.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    47 views38 pages

    Antimicrobial Drugs: Prepared By: Stephanie Lois R. Sanchez, RPH, MSPH

    Uploaded by

    NERA AYON
    The document discusses the history and development of antimicrobial drugs including antibiotics, antifungals, antivirals, antiprotozoals, and antihelminthics. It describes the sources and mechanisms of action of these drugs as well as the development of drug resistance.

    Copyright:

    © All Rights Reserved
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    Download as pdf or txt
    of 38

    Antimicrobial Drugs

    Prepared by:
    Stephanie Lois R. Sanchez, RPh,
    MSPh
    The History of Chemotherapy
    • Paul Ehrlich in Germany during early part of
    20th century
    – He speculated about some “magic bullet” that
    would selectively find and destroy pathogens but
    not harm the host.
    • In 1928, Alexander Fleming
    – Observed that the growth of the bacterium S.
    aureus was inhibited by Penicillium notatum.
    The History of Chemotherapy
    • Antibiosis → Antibiotic → a substance
    produced by microorganisms that in small
    amounts inhibits another microorganism.
    • In 1940, Howard Florey and Ernst Chain
    – Succeeded in first clinical trials of penicillin

    • Sources of Antibiotics: Streptomyces sp.,


    genus Bacillus, genera Penicillium and
    Cephalosporium
    Representative Sources of Antibiotics
    MICROORGANISMS
    Gram-Positive Rods
    Bacillus subtilis
    Bacillus polymyxa
    Actinomycetes
    Streptomyces nodosus
    Streptomyces venezuelae
    Streptomyces aureofaciens
    Streptomyces erythraeus
    Streptomyces fradiae
    Streptomyces griseus
    Micromonospora purpureae
    Representative Sources of Antibiotics

    MICROORGANISMS

    Fungi

    Cephalosporium spp.

    Penicillium grisofulvum

    Penicillium notatum
    The Spectrum of Antimicrobial Activity
    • Narrow spectrum
    • Broad-spectrum
    • Superinfection

    • Action: bactericidal and bacteriostatic


    The Action of Antibacterial Drugs
    • Inhibitors of Cell Wall Synthesis

    • 1. PENICILLINS
    • Scientists develop these penicillin's in two
    ways:
    – 1. they can interrupt synthesis of the
    molecule by Penicillium and obtain only the
    common penicillin nucleus for use.
    – 2. They can remove the side chains that
    make them more resistant to penicillinase, or
    give them an extended spectrum
    The Action of Antibacterial Drugs
    • Inhibitors of Cell Wall Synthesis
    • 1. PENICILLINS
    • Natural Penicillins
    • Penicillin G (Benzylpenicillin) – against gram-
    positive bacteria, requires injection
    – Procaine/Benzocaine penicillin (IM)
    – Benzathine penicillin (IM)
    • Penicillin V (Phenoxymethylpenicillin) – against
    gram-positive bacteria, oral administration
    The Action of Antibacterial Drugs
    • Inhibitors of Cell Wall Synthesis
    • 1. PENICILLINS
    • Semisynthetic Penicillins
    • A. Penicillinase-resistant/Narrow spectrum
    – Methicilin
    – Nafcillin
    – Isoxazoyl Penicillins (Oxacillin, Cloxacillin, Dicloxaciliin)
    • B. Aminopenicillins/Antistaphylococcal Penicillin/Broad
    Spectrum
    – Ampicillin (Parenteral)
    • Prodrugs: Hetacillin, Bacampicillin, Cyclacillin
    • Combined with sulbactam
    – Amoxicillin (PO)
    • combined with clavulanic acid
    The Action of Antibacterial Drugs
    • Inhibitors of Cell Wall Synthesis
    • 1. PENICILLINS
    • Semisynthetic Penicillins
    • C. Extended Spectrum/Anti-Pseudomonal Penicillin
    – Carboxypenicillin (Carbenicillin and ticarcillin)
    – Ureidopenecillin (Piperacillin, Azlocillin, Mezlocilllin)
    • 2. MONOBACTAM
    – Aztreonam – effective for gram-negative bacteria only,
    including Pseudomonas spp, E. coli. And Neisseria
    • 3. CARBAPENEMS
    – Thienamycin, Meropenem, Imipenem –very broad spectrum
    • Combined with cilastatin
    The Action of Antibacterial Drugs
    • Inhibitors of Cell Wall Synthesis
    • 4. CEPHALOSPORINS
    1st gen.
    • Cephalexin
    • Cephapirin
    • Cephradine
    • Cefazolin
    • Cefadroxil

    2nd gen.
    • Cefaclor
    • Cefoxitin
    • Loracarbef
    • Cefotetan
    • Cefprozil
    • Cefmetazole
    • Cefamandole
    • Cefuroxime
    • Cefonicid
    • Cefpodoxime
    • Ceforanide
    3rd gen.
    • Cefixime • Ceftizoxime
    • Cefoperazone • Ceftriaxone
    • Cefotaxime • Ceftazidime
    • Ceftibuten • Moxolactam

    4th gen. 5th gen.


    • Cefepime • Ceftaroline
    • Cefpirome • Ceftobipole
    The Action of Antibacterial Drugs
    • Inhibitors of Cell Wall Synthesis
    • 4. CEPHALOSPORINS
    Gram (+) Gram (-)
    1st gen +++ +
    2nd gen +++ ++
    3rd gen + +++
    4th gen ++ ++++
    5th gen ++++ ++++
    The Action of Antibacterial Drugs
    • Inhibitors of Cell Wall Synthesis
    • 5. POLYPEPTIDE ANTIBIOTICS
    • A. Bacitracin
    • B. Vancomycin
    – A glycopeptide type
    – Causes Redman’s syndrome
    The Action of Antibacterial Drugs
    • Inhibitors of Protein Synthesis
    • Binds to 30s Ribosomes
    • 1. AMINOGLYCOSIDES (Streptomycin,
    Amikacin, Gentamicin, Netilmicin, Neomycin,
    Tobramycin)
    – Streptomycin
    – Neomycin
    – Gentamicin
    – Tobramycin .
    The Action of Antibacterial Drugs
    • Inhibitors of Protein Synthesis
    • Binds to 30s Ribosomes
    • 2. TETRACYCLINES
    – Tetracycline, oxytetracycline, chlortetracycline,
    demeclocycline
    – Semisynthetic: doxycycline and minocycline
    • AE: Gastric discomfort, deposition in the bones
    and primary dentition causing discoloration and
    hypoplasia of the teeth and a temporary stunting
    of growth, hepatotoxicity, phototoxicity
    (demeclocycline), vestibular problems
    (minocycline)
    The Action of Antibacterial Drugs
    • Inhibitors of Protein Synthesis
    • Binds to 50s Ribosomes
    • 1. CHLORAMPHENICOL
    – Serious AE: suppression of bone marrow activity,
    aplastic anemia, gray baby syndrome
    The Action of Antibacterial Drugs
    • Inhibitors of Protein Synthesis
    • Binds to 50s Ribosomes
    • 2. MACROLIDES
    – Erythromycin
    – Clarithromycin
    – Azithromycin
    – Telithromycin
    • AE: epigastric distress, cholestatic jaundice (estolate form of
    erythromycin)
    The Action of Antibacterial Drugs
    • Inhibitors of Protein Synthesis
    • Binds to 50s Ribosomes
    • 3. LINCOSAMIDES
    – Clindamycin
    • AE: Pseudomembranous colitis and rash
    • 4. STREPTOGRAMINS
    – Quinupristin and dalfopristin (Synercid)
    • 5. Oxazolidinones
    – Linezolid
    The Action of Antibacterial Drugs
    • Injury to the Plasma Membrane
    • 1. POLYMYXIN B
    The Action of Antibacterial Drugs
    • Inhibitors of Nucleic Acid Synthesis
    • QUINOLONES AND FLUOROQUIONOLONES
    – Nalidixic acid
    – Norfloxacin, Ciprofloxacin
    – Moaxifloxacin and gatifloxacin
    • AE: development of cartilage, Diarrhea, nausea,
    headache, dizziness, nephrotoxicity, phototoxicity
    The Action of Antibacterial Drugs
    • Competitive Inhibitors of the Synthesis of essential
    Metabolites
    • 1. SULFONAMIDES
    • Trimethoprim-sulfamethoxazole
    – Effective against Pneumocystic pneumonia
    – Very effective in penetrating the brain and
    cerebrospinal fluid
    The Action of Antibacterial Drugs
    • Competitive Inhibitors of the Synthesis of essential
    Metabolites
    • 1. SULFONAMIDES
    – Silver sulfadiazine and Mafenide (Flammazine®)
    – Sodium sulfacetamide
    – Quinine + pyrimethamine + sulfadoxime
    (Fansidar®)
    The Action of Antibacterial Drugs
    • Antimycobacterial antibiotics
    • 1. Rifampin
    – AE: red-orange coloration of body fluids
    • 2. Isoniazid
    – AE: hepatoxicty, peripheral neuropathy
    • 3. Ethambutol
    – AE: optic neuritis
    The Action of Antibacterial Drugs
    • Antimycobacterial antibiotics
    • 4. Pyrazinamide
    – AE: hyperuricemia and hepatotoxicity
    • 5. Ethionamide
    – AE: Hepatotoxicity, Peripheral neuritis
    • 6. Streptomycin
    – AE: Ototoxicity, nephrotoxicity
    Antifungal Drugs
    • Agents affecting Fungal Sterols
    • 1. POLYENES
    – Amphotericin B
    • Can cause kidney toxicity → drugs are
    encapsulated in lipids (liposome)
    – Nystatin and Natamycin
    Antifungal Drugs
    • Agents affecting Fungal Sterols
    • 2. AZOLES
    – Imidazole (Clotrimoxazole, miconazole)
    – Ketoconazole
    – Voriconazole (Fluconazole and itraconazole)
    • 3. ALLYAMINES
    – Terbinafine, naftifine
    Antifungal Drugs
    • Agents affecting Fungal Cell wall
    • 1. ECHINOCANDINS
    – Caspofungin (Cancidas)

    • Agents Inhibiting Nucleic acids


    • 1. FLUCYTOCINE
    – Cruptococcus neoformans and Candida
    – AE: kidney and bone marrow toxicity
    Antifungal Drugs
    • Other fungal Drugs
    • 1. GRISEOFULVIN
    • 2. TOLNAFTATE
    • 3. PENTAMIDINE ISETHIONATE
    Antiviral Drugs
    • Nucleoside and Nucleotide Analog
    • 1. Acyclovir, famiclovir, ganciclovir, ribavirin
    • 2. Lamivudine
    • 3. Cidofovir

    • Other enzyme Inhibitor


    • 1. Zanamivir and oseltamivir phosphate
    • 2. Amantadine and Zimantadine
    Antiviral Drugs
    • Interferons
    • 1. Alpha-interferon
    • 2. Imiquimod
    Antiviral Drugs
    • ANTIRETROVIRALS
    • Nucleoside Reverse Transcriptase inhibitors
    • Abacavir, didanosine, lamivudine, stavudine,
    zalcitabine, zidovudine
    • Nucleotide Reverse Transcriptase Inhibitor
    • Tenofovir
    • Non-nucleoside Reverse Transcriptase Inhibitors
    • Delavirdine, elvirenz, nevirapine
    • Protease inhibitors
    • Amprenavir, nelfinavir, ritonavir, saquinavir,
    lopinavir, indinavir, saquinavir
    Antiprozoan drugs

    • 1. Quinine
    • Chloroquine, mefloquine, primaquine
    • 2. Quinacrine
    • 3. Diiodohydroxyquin (iodoquinol)
    • 4. Metronidazole
    Antihelminthic drugs

    • 1. Niclosamide
    • 2. Praziquantel
    • 3. Mebendazole and albendazole
    • 4. Ivermectin
    Drug resistance
    • Resistance may due to enzymatic destruction
    of a drug, prevention of penetration of the
    drug to its target site, or cellular or metabolic
    changes at target sites.
    • Rapid efflux (ejection)
    • Hereditary drug resistance factors are carried
    by plasmids and transposons.

    • ..\..\..\..\..\Downloads\Animation of
    Antimicrobial Resistance.mp4
    • Antibiotic safety
    • The risk versus the benefit must be
    evaluated prior to use of antibiotics

    • Effects of combinations of drugs


    • Synergistic or antagonistics
    • The future of chemotherapeutic Agents
    • Many bacterial diseases, previously treatable
    with antibiotics, have become resistant to
    antibiotics.
    • Chemicals produced by plants and animals are
    providing new antimicrobial agents called
    antimicrobial peptides.
    • New antimicrobial drugs include DNA that is
    complementary to specific genes in a pathogen;
    the DNA will bind to the pathogen’s DNA or
    mRNA and inhibit protein synthesis.

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