Antimicrobials

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Author:
sdespins
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260203
Filename:
Antimicrobials
Updated:
2014-02-06 22:46:47
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Drugs
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Pharmacology
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Drugs
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  1. Inhibitor of murein polymer synthesis

    Blocks Transglycosidase


    Active against MRSA


    First Choice for treating skin and soft tissue infections

    Effective for treating pseudomembraneous colitis

    Mutation at the D-Ala-D-Ala binding site leads to resistance against this drug
    • Vancomycin
    • Teicoplanin
    • Tanclopenin
  2. Natural penicillin

    Treat infections caused by spirochetes (Treponema pallidum)

    Used to treat syphilis

    Most staphylococci and gonococci and some strains of pneumococci are now resistant to this drug
    Penicillin G
  3. Treat penicillin-resistant strains of staphylococci that elaborate penicillinase (B-lactamase)

    They are not effective against MRSA
    Penicillinase-resistant penicillins:

    • Cloxacillin
    • Dicloxacillin
    • Nafcillin
    • Oxacillin
  4. Combined with a B-lactamase inhibitor

    Active against Listeria monocytogenes and is used to treat meningitis

    Can be combined with an aminoglycoside for the treatment of serious enterococall infections, such as enterococcal endocarditis
    Ampicillin: an Aminopenicillin
  5. Combined with a B-lactamase inhibitor

    This drug specifically is used for prophylaxis of bacterial endocarditis in persons with heart valve defects.
    Amoxicillin: an Aminopenicillin
  6. Used to treat some strains of Pseudomonas aeruginosa

    This drug can be combined with a B-lactamase inhibitor for the treatment of patients with intra-abdominal, skin and soft tissue, lower respiratory tract, complicated urinary tract, and gynecologic infections as well as febrile neutropenia
    Antiseudomonal penicillins:

    • Piperacillin
    • Ticarcillin
  7. Enter CNS and are agents used in the treatment of meningitis

    Used as a single-dose treatment for gonorrhea
    3rd Generation Cephalosporins:

    • Cefotaxime: renal tubular excretion
    • Ceftriaxone (excreted in bile): used in patients with renal insufficiency
  8. Advanced generation of Cephalosporin

    Effective against MRSA
    High affinity to PBPa2, a MRSA-specific PBP that has low affinity for other beta-lactam
    drugs

    Used for treating skin and soft tissue infection and community-acquired pneumonia
    Ceftaroline
  9. It is active against many aerobic G- bacteria
    It lacks activity against G+ organism and anaerobes

    Rarely shows cross-sensitivity with penicillins and cephalosporins and can usually be used in person allergic to other B-lactam antibiotics
    Aztreonam
  10. Used to treat a wide range of systemic infections, including endocarditis, pneumonia, urinary tract, pelvic, skin and soft tissue, and intra-abdominal infections
    Carbapenems:

    • Doripenem
    • Ertapenem
    • Imipenem/Cilastatin
    • Meropenem
  11. B-lactam drugs that inhibit molecular class A B-lactamases

    These drugs have no antimicrobial activity by themselves but serve as surrogate substrates for B-lactamases when given with a penicillin antibiotic
    Beta-lactamase inhibitors:

    • Clavulanate
    • Sulbactam
    • Tazobactam
  12. Drugs used in the inhibition of bacterial cell-wall synthesis
    • Penicillins
    • Cephalosporins
    • Imipenem/Meropenem
    • Aztreonam
    • Vancomycin
  13. Drugs used in the inhibition of bacterial protein synthesis
    • Aminoglycosides
    • Chloramphenicol
    • Macrolides
    • Tetracyclines
    • Streptogramins
    • Linezolid
  14. Drugs used to inhibit nucleic synthesis
    • Fluoroquinolones
    • Rifampin
  15. Drugs that inhibit folic acid synthesis
    • Sulfonamides
    • Trimethoprim
    • Pyrimethamine
  16. Penicillin used to treat Listeria monocytogenes
    Ampicillin
  17. Penicillin used to treat Borrelia burgdorferi
    Amoxicillin
  18. Penicillin used to treat H. pylori
    Amoxicillin
  19. Cephalosporins act very similar to Penicillins but they do not cover which organisms?
    LAME

    • Listeria monocytogenes
    • Atypicals (Chlamydia, Mycoplasma)
    • MRSA
    • Enterococci
  20. What is given with cilastatin, a renal dehydropeptidase inhibitor?
    Imipenem
  21. Which Aminoglycoside is used to treat tubercolosis?
    Streptomycin
  22. Which antibacterial agents should not be used during pregnancy?
    • Aminoglycosides
    • Fluoroquinolones
    • Sulfonamides
    • Tetracyclines
  23. What folic acid inhibitor is generally used to treat urinary tract infections?
    Sulfonamides
  24. Antibacterial agent that is a direct inhibitor of nucleic acid synthesis?
    Quinolones inhibit topoisomerase II (DNA gyrase)
  25. What are the primary anti-tubercular drugs?
    • Isoniazid
    • Rifampin
    • Ethambutol
    • Pyrazinamide
  26. Inhibitors of polymer synthesis
    • Vancomycin
    • Teicoplanin
    • Tanclopenin
  27. Penicillins
    • Penicillin G
    • Cloxacillin, Dicloxacillin, Nafcillin, Oxacillin
    • Amoxicillin, Ampicillin, Piperacillin, Ticarcillin
  28. Beta-lactamase inhibitors
    • Clavulanate
    • Sulbactam
    • Tazobactam
  29. Cephalosporins
    • 3rd Generation: Cefotaxime, Ceftriaxone
    • Advanced Generation: Ceftaroline
  30. Monobactam
    Aztreonam
  31. Carbapenems
    End in "penem"

    • Doripenem
    • Ertapenem
    • Imipenem/Cilastatin
    • Meropenem
  32. Antibacterials that are highly ionized and poorly absorbed

    Poor penetration of the meninges

    Must be administered parenterally for the treatment of systemic infections
    Aminoglycosides: end in "mycin"
  33. Most commonly used antibacterial agent used in the treatment of gram-negative bacterial infections?
    Aminoglycosides: end in "mycin"
  34. Aminoglycoside used to treat tuberculosis
    Streptomycin
  35. Most active aminoglycoside against strains of P. aeruginosa
    Tobramycin
  36. Antibacterial agent used in ointments and creams to prevent infections after minor skin trauma
    Neomycin
  37. Adverse effect of aminoglycosides?
    Nephrotoxicity and ototoxicity (problem with hearing)
  38. Class of antibacterials taht bind divalent and trivalent cations

    These drugs do not work as effectively when taken with food?
    Tetracyclines: end in "cycline"
  39. Drugs of choice to treat Rocky Mountain spotted fever?
    Tetracyclines
  40. Broad-spectrum of drugs that inhibit the growth of many gram-positive and gram-negative organisms, rickettsia, spirochetes, mycoplasmas, and chlamydiae
    Tetracylines
  41. Tetracylines used to treat skin and soft tissue infections caused by MRSA
    Doxycyline and minocycline
  42. Tetracycline used for treating syphilis and malaria
    Doxycycline
  43. Adverse effects of Tetracyclines?
    Nephrotoxicity and Hepatotoxicity

    Aminoglycosides and other nephrotoxic drugs should be avoided in patients having treatment with these drugs
  44. Tetracycline that can be used with patients with renal insufficiency?
    Doxycycline
  45. The prototype of macrolides
    Erythromycin
  46. Semisynthentic macrolides
    Azithromycin and Clarithromycin
  47. Class of antibacterials active against many gram-positive and gram-negative bacteria that cause upper respiratory tract infections and pneumonia
    Macrolides
  48. Most active macrolide against H.pylori
    Clarithromycin
  49. Adverse effects of macrolides
    Jaundice and ototoxicity
  50. Active against gram-positive cocci and anaerobic organism such as Bacteroides fragilis and Clostridium perfringens

    Effective against MRSA

    Used for prophylaxis of bacterial endocardiits if allergic to penicillins
    Clindamycin
  51. Side effect of Clindamycin?
    Gastrointestinal super-infections caused by Clostridium difficile
  52. Prevents formation of the 70s initiation complex

    Cross-resistance with other class of antibiotics is unlikely
    Linezoid
  53. Linezolid is indicated for what?
    Vancomycin-resistant E. faecium, Pneumonia caused by MRSA and MSSA
  54. 30s Protein Inhibitors
    Aminoglycosides: End in "mycin"

    • Amikacin
    • Gentamicin
    • Kanamycin
    • Neomycin
    • Streptomycin
    • Tobramycin

    Tetracyclines: End in "cycline"

    • Chloretetracycline
    • Demeclocycline
    • Doxycycline
    • Methacycline
    • Minocycline
    • Oxytetracycline
    • Tetracycline
  55. 50s Protein Synthesis inhibitors
    Macrolides: End in "mycin"

    • Azithromycin
    • Clarithromycin
    • Dirithromycin
    • Erythromycin
  56. Most common compounds for treating human infections include?
    Sulfisoxazole and Sulfamethoxazole
  57. What is Sulfamethoxazole administer with to prevent urinary tract infections?
    Trimethoprim
  58. Adverse effect of sulfonamides?
    Hemolytic anemia
  59. The drug of choice to treat for pulmonary infections caused by Pneumocystis jiroveci?
    Trimethoprim-Sulfamethoxazole
  60. Quinolone indicated for urinary tract infections?
    Norfloxacin
  61. Most frequently used fluorquinolones used in the USA?
    Ciprofloxacin
  62. Drug class used to treat bacterial diarrhea and is effective in treating traveler's diarrhea?
    Quinolones
  63. Used to treat anthrax?
    Ciprofloxacin
  64. Adverse effects of fluoroquinolones?
    Tendonitis and tendon rupture

    Should not be prescribed to adolescents, young children, nursing mothers, and pregnant women

    Some fluoroquinolones inhibit P450 which leads to drug to drug interactions
  65. Inhibits the cell membrane of bacteria

    Active against some strains of MRSA and VRE

    Approved for treatment of MRSA skin and skin-structure infections that are a complication of surgery, diabetic foot ulcers, and burns
    Daptomycin
  66. Adverse effect of Daptomycin?
    Muscle toxicity

    Creatine phosphokinase levels should be monitored
  67. Antifolate drugs
    • Sulfamethoxazole
    • Trimethoprim
    • Trimethoprim-Sulfamethoxazole
  68. Quinolones
    End in "oaxcin"

    • Ciprofloxacin
    • Enoxacin
    • Gemifloxacin
    • Levofloxacin
    • Moxifloxacin
    • Norfloxacin
    • Ofloxacin
  69. Tuberculosis drug that is activated by mycobacterial catalase-peroxidase, an enzyme encoded by the katG gene

    Drug inhibits fatty acid synthetase 2 (FAS2)
    Isoniazid
  70. Drug used to treat latent tuberculosis

    It is also given to prevent TB in neonates and children who have had close contact with persons in who active TB was recently diagnosed
    Isoniazid
  71. Penetrates inflamed meninges and can be used in the treatment of tubercular meningitis?
    Rifampin
  72. Tuberculosis drug used to prevent meningococcal disease in individuals who have had close contact with Neisseria meningitidis
    Rifampin
  73. Tuberculosis drug that inhibits arabinosyltransferase, an enzyme involved in the synthesis of arabinogalactan
    Ethambutol
  74. Adverse effects of ethambutol
    Optic neuritis and impaired red-green color discrimination
  75. Most toxic anti-fungal

    It is effective against a wide range of fungi

    In spite of its toxic potential, this drug is the choice for the treatment of life-threatening systemic mycoses
    Amphotericin
  76. Antifungal for the treatment of Candida species?
    Nystatin
  77. Used to treat fungal blepharitis
    Natamycin (topical use only)
  78. Triazole used to treat fungal meningitis?
    Fluconazole
  79. What class of drugs inhibit CYP3A4 which leads to drug interactions.
    Azoles especially Ketoconazole
  80. Used in many systemic fungal infections especially meningitis.

    This anti-fungal drug is combined with Amphotericin B because drug resistance develops rapidly when it is administered alone
    Flucytosine
  81. How do the Polyenes, an antifungal agent work?
    Polyenes bind to ergosterol in the plasma membrane of fungal cells and form pores which leads to cell death.
  82. Anti-viral used against HSV and VZV

    A guanosine analog that lacks a true sugar moiety, is monophosphorylated in the cell by the herpes virus, encoded enzyme, thymidine kinase

    Causes premature DNA-chain termination
    Acyclovir
  83. The prototypic antiherpetic therapeutic agent

    In the IV form it is the most effective treatment for serious herpesvirus infections, including herpetic encephalitis and severe HSV and VZV infections in immunocompromised patients.
    Acyclovir
  84. The prodrug form of acyclovir
    Valacyclovir
  85. Anti-viral used against CMV diseases, including retinitis, esophagitis and colitis
    Ganciclovir
  86. Pro-drug form of ganciclovir
    Valganciclovir
  87. What types of Anti-HIV drugs have been approved?
    Drugs that target:

    • Viral attachment
    • Fusion
    • Reverse transcription
    • Integration
    • Maturation
  88. What type of drugs are the foundation of chemotherapy for HIV infection?
    NRTIs:

    • Abacavir
    • Didanosine
    • Emtricitabine
    • Lamivudine
    • Stavudine
    • Tenofovir
    • Zidovudine
  89. Directly inhibit reverse transcriptase

    They do not require metabolic activation and they are not incorporated into viral DNA
    NNRTIs:

    • Delaviridine
    • Efavirenz
    • Etravirine
    • Nevirapine
  90. Antiviral that inhibits the metabolism of other PIs and is often combined with other PIs to increase their plasma levels and duration which is also known as boosted therapy
    Ritonavir
  91. P450 enzymes (CYP3A4) are inhibited by what anti-HIV drugs?
    PIs: end in "navir"

    • Amprenavir
    • Atazanavir
    • Darunavir
    • Fosamprenavir
    • Indinavir
    • Lopinavir
    • Nelfinavir
    • Ritonavir
    • Saquinavir
    • Tipranavir
  92. The attachment and fusion inhibitors

    They are approved for treatment of HIV infection caused by drug-resistant strains
    • Enfuvirtide
    • Maraviroc
  93. Binds to HIV glycoprotein 41 and blocks the fusion process of HIV-1
    Enfuvirtide
  94. Antagonist of chemokine co-receptor 5 (CCR5).

    Binds to CCR5 and prevents interaction with HIV-1 glycoprotein 120 that is necessary for CCR5-tropic HIV-1 to enter cells
    Maraviroc
  95. First integrase inhibitor

    Approved for the treatment of HIV-1 infection in adult patients who have HIV-1 strains that are resistant to multiple anti-retroviral agents and who show evidence of increased viral replication
    Raltegravir
  96. Drug of choice to treat Hepatitis B
    Tenofovir
  97. How does Interferon work?
    May involve the induction of host cell enzymes that inhibit viral RNA translation, ultimately leading to the degradation of viral mRNA and tRNA
  98. Adverse effect of Interferon
    Flu-like symptoms
  99. Hepatitis B drugs
    • Tenofovir
    • Adefovir
    • Entecavir
    • Lamivudine
    • Telbivudine
  100. In combination with Interferon-alpha-2b it is effective in chronic hepatitis C
    Ribavirin
  101. What compound is ribavirin converted which blocks RNA-dependent RNA polymerase?
    Ribavirin-triphosphate
  102. Newly approved hepatitis C virus (HCV) NS3/4A protease inhibitors

    These drugs cannot be used alone

    These drugs are combined with interferon and ribvirin

    Indicated, in combination with peginterferon alfa  and ribavirin, for the treatment of genotype chronic hepatitis C (CHC) in adult patients with compensated
    liver disease, including cirrhosis, who are treatment-naïve or who have been previously treated with interferon-based treatment, including prior null responders, partial responders, and relapsers.
    Both end in "previr"

    • Boceprevir
    • Telaprevir
  103. Tricyclic amine compounds that block M2 proton-selective ion channel and prevent acidification of influenza type A virus and the fusion of viral membranes and endosomes required for uncoating and transfer of viral nucleic acid into the host cell cytoplasm

    They are not currently recommended for prophylaxis and treatment of influenza in the United States
    Adamantanes: end in "mantadine"

    • Amantadine
    • Rimantadine
  104. Inhibit the enzyme neuraminidase in influenza A and B viruses

    These drugs block the release of the influenza drug from the cell

    Are active against essentially all strains of influenza A and B viruses, and they are active against most current strains including influenza A 2009 H1N1, 2009 H3N2, and the H5N1 avian influenza strain
    Neuraminidase inhibitors: end in "mivir"

    • Oseltamivir
    • Zanmivir
  105. Drugs for Herpesvirus infections
    • Acyclovir and Valacyclovir
    • Grancivlovir and Valganciclovir
    • Penciclovir and Famiciclovir
    • Cidofovir
  106. Drugs for treating hepatitis C
    • Interferon
    • Ribavirin
    • Boceprevir
    • Telaprevir
  107. Drugs for influenza
    • Amantadine
    • Rimantadine
    • Oseltamivir
    • Zanamivir
  108. Antiparasitic active against several anaerobic protozoa

    Drug of choice for amebiasis, giardiasis, and trichomniasis
    Metronidazole
  109. Anti-malaria drug that block exoerythrocytic schizogony
    Primaquine
  110. Treatment of choice for the prevention of all types of malaria

    It must be used with primaquine to eradicate Vivax or Ovale Malaria
    Chloroquine
  111. Anti-malarial drugs that interfere with heme polymerization
    • Quinine 
    • Quinidine
  112. Anti-malarial drug used to prevent the treatment of chloroquine-resistant malaria
    Mefloquine
  113. Used to treat falciparum malaria
    Artermisinin and its derivatives:

    • Artermether 
    • Artesunate

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