gram neg.(semisynthetic) Bacteria Drugs that inhibit cell wall synthesis Drug Action Organisms Comments Spectrum of Action Mycobacterium

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1 Mickey Dufilho s Drugs and Bugs Revised 10/10/15 Bacteria Drugs that Inhibit Cell Wall Synthesis Drug Action Spectrum of Action Comments Spectrum of Action Bacitracin Beta-Lactam antibiotics Penicillin G (injection) Penicillin V (oral) Mono-Lactam Antibiotics semi synthetic Ampicillin(injection) Amoxicillin (oral) Methicillin (injection) Oxacillin (injection) Beta-Lactam antibiotics Cephalosporins (any drug that begins with Ceph of Cef) 4 generations Natural Cephalothin (injection) Semi-synthetic Ceftriaxone Cephalexin Interferes with Peptidoglycan Synthesis Blocks of peptidoglycan Gram + Blocks of peptidoglycan Blocks of peptidoglycan Gram positive Topical use only toxic to kidneys Gram positive Mechanism of resistance organism makes beta lactamases change outer membrane to prevent Adverse effects toxic to kidneys Gram + Mechanism of resistance Aerobic Gram neg. organism makes beta lactamases change outer membrane to prevent Adverse reactions allergic reactions Gram + (natural) Mechanism of resistance Gram + and aerobic organism makes beta lactamases gram neg.(semisynthetic) change outer membrane to prevent Adverse reactions allergic reactions Natural - narrow Semi-synthetic - Bacteria Drugs that inhibit cell wall Spectrum of Action Isoniazid (oral) Inhibits mycolic acid Mycobacterium Used with Rifampin for TB tuberculosis and M. leprae Adverse effects liver toxicity Vancomycin (IV) Blocks of peptidoglycan by preventing the formation of alaninealanine bridges Gram + -Used for Methicillin resistant organisms. Good for Staphylococcal infections that are resistant to the cillins like MRSA Adverse effects damage to ears and kidneys, and allergic reactions MDufilho 10/10/15 Page 1

2 Bacteria Drugs that inhibit Protein Synthesis Spectrum of Action Aminoglycocydes (IV) Inhibit protein at Most effective Gram Adverse effects kidney toxicity and Gentamicin neg. auditory nerves causing deafness Kanamycin Not very effective Neomycin against anaerobes Streptomycin No very effective Tobramycin against biofilms Lincosamides Clindamycin (oral, IV) Inhibit Protein at Gram + and anaerobic Gram neg Adverse effects GI distress Macrolides (oral) Inhibit Protein at Gram + and few gram neg Adverse effects GI distress Azithromycin Erythromycin Tetracyclines (oral) Inhibit Protein at Gram + and gram neg and Adverse effects GI distress, light Doxycycline Mycoplasma sensitivity Do not give to pregnant Tetracycline women or young children due to adverse affect on teeth and bones Bacteria Drugs that Alter Cytoplasmic Membranes Spectrum of Action Polymyxin (topical) some Destroys membranes Gram neg - Pseudomonas Adverse effects toxic to kidneys named Colistin and some amoebae Bacteria Drugs that are antimetabolites Sulfonamides (oral) Sulfanilamide Trimethoprim (oral) Spectrum of Action Synthetic - Inhibits folic acid * Synthetic - Inhibits folic acid Gram + and Gram neg, Chlamydia and some protozoans and fungi Gram + and Gram neg, Chlamydia and some protozoans and fungi * spectrum if given with Trimethoprim Widespread resistance Adverse effects rare not given in last trimester * spectrum if given with Sulfonamides Widespread resistance Adverse effects allergic reactions and liver damage * MDufilho 10/10/15 Page 2

3 Bacteria Drugs that inhibit nucleic acid Spectrum of Action Fluoroquinolones (oral) Synthetic inhibits enzymes Gram + and gram neg Adverse reactions rare - tendonitis Ciprofloxacin needed to replicate DNA Nitroimidazoles(oral) Damages DNA and prevents Obligate Anaerobic Metronidazole replication bacteria Rifamycin (oral) Prevents transcription of Aerobic Gram + and used Bacteriostatic for aerobic gram + and Rifampin with other drugs for bactericidal for Mycobacteria Rifaximin Mycobacteria Antiviral Drugs attachment antagonists Neuraminidase inhibitors Prevents influenza viruses Influenzavirus A and B Oseltamivir (oral) from attaching to host cells Zanamivir /Tamiflu(aerosol) and also release of viruses Antiviral Drugs Inhibit viral uncoating Amantadine (oral) It inhibits the uncoating of the virus and release of viral Influenza A virus and some other viruses Given orally to prevent infection. Use within hours of onset of symptoms to have any benefit. Rimantadine (oral, adults only) It inhibits the uncoating of the virus and release of viral Influenza A virus and some other viruses Adverse effects can be neurotoxic Given orally to adults only Adverse effects can be neurotoxic MDufilho 10/10/15 Page 3

4 Antiviral Inhibit nucleic acid Acyclovir (ACV) (oral) Stops viral DNA and DNA Virus Herpesvirus chickenpox and Does not prevent or terminate latency, so Ganciclovir shingles, Cytomegalovirus, varicella viruses infection can reemerge when treatment is Zovirax stopped. Herpes viruses are resistant Valtrex Adenosine arabinoside (IV) Inhibits DNA Herpesvirus Can cause cell death and anemia Nucleotide analogs (oral) Inhibits DNA by HIV, Hepatitis B virus Adverse effects nausea, bone marrow toxicity Adefovir incorporating into DNA Azidothymidine (AZT) especially with reverse Tenofovir transcriptase Valaciclovir Ribavirin (oral, aerosol, IV) Stops viral DNA and Respiratory syncytial virus, hepatitis C, influenza A, measles, some hemorrhagic fever viruses Not given to pregnant women. Antiviral Inhibit Protein Synthesis Antisense nucleic acids Acts like a m, binds to Cytomegalovirus May cause eye problems like glaucoma Fomiversen (injected ribosome and blocks protein into the eyes) Antiviral Inhibit Viral Proteins Protease inhibitors (oral) Blocks the active site on essential protease enzyme use with other drugs HIV Treatment of HIV requires the use of several drugs Fungi Inhibit Cell Membranes Azoles (agents that end in azole) (topical and IV) Inhibits production of ergosterol necessary for spectrum. Dermatophytes, dimorphic fungi and yeasts Possibly cancer causing Ketoconazole fungal cell membranes Polyenes Inhibits production of Fungi and some amoebae When used orally, can be toxic to kidneys. Amphotericin B (IV) ergosterol necessary for Nystatin (topical) fungal cell membranes MDufilho 10/10/15 Page 4

5 Fungi other Drugs Caspofungin (IV) Inhibits cell wall production Candida and Aspergillus Adverse effects various of fungi Griseofulvin (topical and oral) Prevents complete cell division Dermatophyte infections Protozoans Heavy Metals (topical, oral) Melarsoprol Salvarsan (Arsenic) Deactivate essential enzymes Metabolically active cells Toxic to active cells brain, kidney, liver and bone marrow Iodoquinol (oral) Unknown Intestinal amoebae Adverse effects fever, rash Sulfonamides and Damages DNA Trimethoprim (see bacteria) Metronidazole (Flagyl) (oral) Quinine Containing (end in quine) (oral) Quinine Chloroquine Derived from bark of cinchona inhibits metabolism of malaria parasites Entamoeba, Giardia, Trichomonas and others Plasmodium Has caused cancer in lab rodents Allergic reactions, visual disturbances MDufilho 10/10/15 Page 5