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Antibiotics White
Antibiotics for Pharmacology III Exam 4
| Question | Answer |
|---|---|
| Essential enzymes involved in cell wall synthesis | Penicillin Binding Proteins (PBPs) |
| Beta-lactam resistance | Beta-lactamase prouction, altered PBP (S. pneumoniae), novel PBP (MRSA) |
| Specific indications – any susceptible gram + infection (E.g., Strep pyogenes, N. meningitides) | Penicillin G (benzyl penicillin) |
| Significant amounts of Na or K with parenteral dosage forms | Penicillins |
| Long-acting for treatment of syphyllis | Benzathine penicillin |
| Preparation not susceptible to acid breakdown (preferred form of PO admin) | Penicillin VK |
| Aminopenicillins | Ampicillin/Sulbactam (IV) and Amoxicillin/Clavulanate (PO) |
| Spectrum of activity – most gram + organisms (excluding some Staph aureous) and E. coli (gram -) – SE is diarrhea (more than others) | Ampicillin |
| Prevents secretion of many drugs into the renal tubules | Probenecid |
| Restores some gram – and anaerobic activity to Amoxicillin | Clavulanic Acid |
| Used for bite wounds from animals | Amoxicillin/Clavulanate |
| Anti-staphylococcal PCN, semi-synthetic PCN, Penicillinase-resistant PCN | Dicloxacillin, Nafcillin or Oxacillin |
| Dicloxacillin, Nafcillin or Oxacillin | Use for Staph infections, NOT for MRSA or Strep |
| Broad spectrum but mostly used for Pseudomonas | Ticarcillin/Clavulanate, Piperacillin/Tazobactam (extended-spectrum) |
| Most potent extended-spetrum PCN | Piperacillin |
| Importance of Tazobactam | Piperacillin useful against anaerobes again |
| Combine with Zosyn | Aminoglycoside or Fluoroquinolone |
| Primarily used for empiric therapy (nosocomial infections) | Piperacillin/Tazobactam |
| GI effects (C. diff colitis), interstitial nephritis, possible seizures | Adverse effects with Penicillins |
| Activity includes MSSA and many other gram + bacteria | First generation Cephalosporins (Cefazolin, Cephalexin) |
| Activity includes MSSA, gram + orgs, NO activity against pseudomonas or enterococcus | Second generation Cephalosporins (Cefuroxime, Cefdinir) |
| Pseudomonas activity, gram - > gram +, limited anaerobic activity | Third generation Cephalosporins (Ceftazidime, Ceftriaxone) |
| Gets around Amp C resistance (Zwitterion), good Gram + and – activity, NO MRSA or enterococci activity | Fourth generation Cephalosporins (Cefepime) |
| Anti-pseudomonal and anti-pneumococcal activity | Cefepime (4th gen Ceph) |
| SE—opportunistic infections, hypersensitivity and cross-sensitivity | Cephalosporins |
| Gram – aerobic + pseudomonas activity in patients with severe PCN allergy and renal dysfunction | Aztreonam (monobactam) |
| Most potent beta-lactams | Carbapenems |
| Blocks enzyme in renal tubule that destroys Imipenem, prevents nephrotoxicity | Cilastatin |
| Cover most everthing except MRSA and MRSE, enterococcus faecium, burkholderia and S. maltophilia | Imipenem, Meropenem, Doripenem (broad) |
| Use for sickest patients with intra-abdominal sepsis, nosocomial pneumonia, febrile neutropenia | Imipenem, Meropenem, Doripenem (specific) |
| Useful for serious community-acquired infections, NOT for nosocomial-acquired infections (like cephalosporins) | Ertapenem |
| Seizures, eosinophilia, renally dosed, avoid with seizure threshold lowering drugs | Carbapenems |
| Dosed frequently (q6h), works best when max time > MIC | Penicillins, Cephalosporins, Carbapenems (esp.) |
| Inhibits regeneration of phospholipid receptors involved in peptidoglycan synthesis, more gram + | Bacitracin |
| Used topically only because of nephrotoxicity concerns | Bacitracin |
| Used for resistant gram + infections | Vancomycin, Linezolid, Daptomycin, Tigecycline, Quinupristin/Dalfopristin |
| Treats MRSA and highly resistant Strep species by preventing cross-linking of peptidoglycans | Vancomycin (activity) |
| Red man syndrome, ototoxicity, nephrotoxicity (little) | Vancomycin (SE) |
| Higher recommended trough concentrations, AUC/MIC indicator of outcomes | Vancomycin (dosing) |
| hVISA becoming a problem along with MIC “creep” with MRSA | Vancomycin (issue) |
| Inhibits initiation of protein synthesis by binding 23S peptydiltransferase | Linezolid (MoA) |
| Serotonin syndrome (BP!!!), thrombocytopenia long-term | Linezolid (SE) |
| Nosocomial pneumonia, MRSA and VRE | Linezolid (activity) |
| Low incidence of adverse effects, no significant drug interactions, bactericidal, concentration-dependent killing of gram + organisms | Daptomycin (background) |
| Calcium-dependent binding to bacterial cell membranes | Daptomycin (MoA) |
| MRSE, MRSA, S. aureus bacteremia, including right-sided endocarditis | Daptomycin (activity) |
| Monitor for muscle pain, weakness and CPK levels | Daptomycin (SE) |
| Combines cell wall effect (Vanc) with cell membrane effects (Dapto) | Televancin (MoA) |
| MRSA, works well in the lungs, not inactivated by surfactants | Televancin (activity) |
| MRSA-active cephalosporin, penicillinase resistant | Ceftobiprole |
| Gentamicin, Tobramycin, Amikacin | Most used IV aminoglycosides (protein synthesis inhibitors) |
| Lots of gram – activity, some gram +, no anaerobic activity | Aminoglycosides (activity) |
| Ototoxicity (irreversible), nephrotoxicity (reversible usually), neuromuscular blockade | Aminoglycosides (SE) |
| UTI, pneumonia (nosocomial, gram -, aspiration), bacteremia/sepsis | Aminoglycosides (Use) |
| Concentration-dependent killing, POST antibiotic effect, adaptive resistance | Aminoglycosides (PDs) |
| Strep pneumonia, LOWER respiratory tract infections, STDs, H. pylori, mycobacterium avium (MAC) in AIDs patients | Macrolides (Use) |
| Mycoplasma (atypical) – walking pneumonia | Macrolide (activity) |
| mef genes and erm genes | efflux pumps and ribosomal methylases in Macrolide resistance |
| QT interval prolongation, some hepatic injury, 3A4 inhibitors | Macrolide (SE) |
| Acid stable and overcome Macrolide resistances | Telithromycin (ketolide) |
| Inhibits DNA gyrase to form toxic complex, inhibits Topoisomerase IV | Fluoroquinolone (MoA) |
| Strep pneumoniae, NOT staph, PSEUDOMONAS, atypicals, broader gram – activity | Fluoroquinolone (Activity) |
| Higher Vd to Low Vd: Cipro, Levo, Moxi, Gemi | Cipro > Gemi > Moxi >> Levo |
| Fluoroquinolone that does not need to be renally adjusted | Moxifloxicin |
| Fluoroquinolone for UTI | Levofloxacin |
| Fluoroquinolone for Strep. Pneumoniae | Moxifloxacin, levofloxacin 750 mg |
| Photosensitivity, prolonged QTc interval, seizures, liver toxicity, arthritis/tendonitis | Fluoroquinolones (SE) |
| Complex with Zn, Ca, Mg, NSAIDs and interact with antiarrhythmics | Levofloxacin, Moxifloxacin, Gemifloxacin |
| Workhorse for gram – infections, fluoroquinolones | Ciprofloxacin, levofloxacin |
| Fluoroquinolones for respiratory infections | Levofloxacin, Gemifloxacin, Moxifloxicin |
| UTI agents | Fosfomycin, SMC/TMP, Nitrofurantoin |
| Only for UTI, urine levels used for susceptibility data | Nitrofurantoin (Use) |
| Take with food or milk, decrease dose, change microcrystals to macrocrystals | Nitrofurantoin (advice) |
| Fluid collects in lower lobes of lungs, sounds like pneumonia, possible eosinophilia | Nitrofurantoin (SE) |
| Brown urine, avoid in CrCl < 40 mL/min, G-6-P D (+) – anemia, peripheral neuropathy patients | Nitrofurantoin (Precautions) |
| SMX/TMP | 5:1 ratio |
| UTI and nocardia infections, Pneumocystis pneumonia, resistance common | SMX/TMP |
| Stevens-Johnson Syndrome | Long-acting sulfonamides |
| Give fluids to avoid crystals in urine, photosensitivity | SMX/TMP (SE) |
| Warfarin, albumin-bound drugs interact | SMX/TMP (DI) |
| 1 dose for uncomplicated UTI, avoid cations | Fosfomycin |
| Gram +, anaerobes, acne, 2nd/3rd line broad spectrum | Clindamycin |
| C. diff colitis as SE | Clindamycin (SE) |
| Treats anaerobes | Metronidazole |
| Metallic taste, seizures, peripheral neuropathy, changes urine color | Metronidazole (SE) |
| Lyme disease, H. pylori, Rocky Mountain Spotted Fever | Doxycycline, Minocycline (long-acting tetracycyline) |
| Efflux, influx decreased | Tetracycyline (resistance) |
| Lipid soluble, enterohepatic recirculation | Minocycyline |
| Adheres to teeth and bones, C/I in pregnancy, children | Tetracycylines (CI) |
| Cations, OC, Warfarin | Tetracycylines (DI) |
| Gram positive, anaerobes, gram negatives, not Pseudomonas or Acinetobacter | Tigecycline |
| Ointment at IV line sites, prevents Staph infections | Mupirocin |
| Gram negatives, especially Acinetobacter and Pseudomonas | Polymyxins |
| Gram negative—H. influenzae, Gram positive—MRSA | Rifampin (Use) |
| Reddish urine discoloration, flu-like symptoms, neutropenia | Rifampin (SE) |
| Barbie’s Car Goes Really Fast | 3A4 Inducers |
| Depolarize cell membranes of fungi, ergosterol attachment | Polyenes (Amphotericin B and Nystatin) |
| Antifungal that does NOT distribute into CSF | Amphotericin B (PK) |
| Infusion toxicity and nephrotoxicity | Amphotericin B (SE) |
| Hypokalemia, acidosis, anemia | Amphotericin B (AE) |
| Cryptococcal meningitis | Flucytosine |
| Bone marrow suppression, hepatotoxic | Flucytosine (SE) |
| Do NOT rechallenge patients with rashes | Flucytocine |
| Phenytoin concentrations greatly increased | Fluconazole (DI) |
| Candidiasis, cryptococcal meningitis | Fluconazole (Use) |
| Aspergillus activity | Voriconazole (Use) |
| Visual “events” – photopsia, 30% for 30 min | Voriconazole (SE) |
| Excipient builds up in renal dysfunction | Voriconazole (AE) |
| Oropharyngeal candidiasis | Posaconazole |
| Drug of choice for Candida | Echinocandins (fungins) |
| Phlebitis or thrombophlebitis | Caspofungin (AE) |
| Aspergillus (invasive) | Caspofungin (Use) |
| Not many drug interactions, eliminated in bile, concentration dependent anti-fungal | Micafungin |
| Esophageal candidiasis, candidemia | Anidulafungin |
| Antifungals with less drug interactions | Micafungin and Anidulafungin |
| HSV-1 > HSV-2 > VZV | Acyclovir, Famciclovir |
| Cerebro-herpes | Acyclovir |
| Anti-viral headache SE | Acyclovir (SE) |
| CMV | Gancyclovir, Cidofovir, Foscarnet, Fomivirsen |
| Anti-CMV myelosuppression SE | Ganciclovir |
| Anti-CMV nephrotoxicity SE | Cidofovir |
| Anti-CMV hyper- and hypo-Ca and PO4 SE | Foscarnet |
| Anti-CMV Increased IOP and iritis SE | Fomivirsen |
| Treats Influenza A only | Amantadine/Rimantadine (Use) |
| Anticholinergics, antihistamines, APAP and ASA interact | Amantadine/Rimantadine (DI) |
| Treats Influenza A and B | Zanamivir/Oseltamivir |
| Antiviral that may exacerbate COPD/asthma | Zanamivir |
| Anti-hepatitis that lasts longer | PEG Interferons |
| Psych consult and flu-like symptoms | PEG Interferons |
| Antiviral hemolytic anemia | Ribavirin |
| Antivirals for ophthalmic infections | Vidarabine, Idoxuridine, Trifluridine |
| Antiviral photophobia—wear sunglasses | Vidarabine |
| Treats Respiratory Syncytial Virus | Ribavirin |
| NNRTI + 2 NRTIs | Naïve HIV patient treatment |
| Boosts HIV patient treatment | Ritonavir |
| Pancreatitis in children | Lamivudine |
| Flu-like symptoms, do NOT rechallenge | Abacavir |
| Lactic acidosis as a class-wide SE | NRTIs |
| Do not combine with Didanosine or agents that cause peripheral neuropathy | Stavudine |
| Antiviral with LOTS of drug interactions | NNRTIs |
| NNRTI to use if resistance is shown to others | Efavirenz |
| Rash, Hepatotoxic, CNS side effects | NNRTIs (SE) |
| Antivirals with very low rates of resistance | Protease Inhibitors (background) |
| Fat redistribution SE | Protease Inhibitors (SE) |
| Hyperbilirubinemia, prolongs QRS interval | Atazanavir |
| Nephrolithiasis | Indinavir |
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