Micro Pharm Flashcards
Binds PBPs, inhibit transpeptidation, activate autolytic enzymes
Penicillins (G and V) mechanism of action?
Gram positive bacteria
Penicillins (general) uses?
Hypersensitivity, dose adjustment in renal impairment
Penicillins (general) side effects?
Beta lactamase sensitive. Narrow spectrum (g+), Treponema pallidum.
Penicillin V uses?
Hypersensitivity, dose adjustment in renal impairment. Jarisch-Herxheimer reaction (fervers, chills, rigor hypotension) with syphillis treatment.
Penicillin V side effects?
Bactericidal. Binds PBPs, inhibit transpeptidation, activate autolytic enzymes.
Methicillin, Nafcillin, Dicloxacillin, Amoxicillin, Ampicillin, Ticarcillin, Pipercillin, Azlocillin, Carbenicillin
Beta lactamase RESISTANT. Very narrow spectrum, methicillin SENSITIVE S. aureus (MSSA).
Methicillin, Nafcillin, Dicloxacillin uses?
Hypersensitivity, dose adjustment in renal impairment. Interstitial nephritis.
Methicillin, Amoxicillin
Hypersensitivity, dose adjustment in LIVER impairment.
Nafcillin, Dicloxacillin side effects?
Hypersensitivity, dose adjustment in LIVER impairment.
Dicloxacillin side effects?
Beta lactamase sensitive. Broad spectrum, Haemophilus, E.coli, Listeria, Proteus, Salmonella, Shigella
Amoxicillin, Ampicillin uses?
Hypersensitivity, dose adjustment in renal impairment. Rash with viral infection, pseudomembranous colitis
Ampicillin side effects?
Beta lactamase sensitive. Extended spectrum, Pseudomonas aeruginosa. Gram negative anaerobes (Bacteriodes fragilis).
Ticarcillin, Piperacillin, Azlocillin, Carbenicillin
Hypersensitivity, dose adjustment in renal impairment.
Ticarcillin, Piperacillin, Azlocillin, Carbenicillin side effects?
Inhibits beta-lactamase/penicillinase
Clavulanic acid, Tazobactam, Sulbactam mechanism of action?
Combine with ampicillin/amoxicillin or antipseudomonals to protect the antibiotic from destruction by Beta-lactamase (penicillinase)
Clavulanic acid, Tazobactam, Sulbactam uses?
Beta-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases. Bactericidal.
Cephalosporins (general)
- Hypersensitivity, dose adjustment in renal impairment, vitamin K deficiency.
- Low reactivity with penicillins and increased nephrotoxicity of amino glycosides.
Cephalosporins (general) side effects?
Used for: Gram Positive Cocci, PEcK (Proteus mirabilis, E. coli, Klebsiella pneumoniae.)
- One of these was used prior to surgery to precent S. Aureus wound infections.
1st Gen: Cefazolin, cephalexin
- Cefazolin
Used for: Gram positive Cocci HEN PEcKS (Haemophilus influenzae, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E. coli, Klebsiella pneumoniae, Serratia marascens.)
- Greater Spectrum of Gram pos
2nd Gen: Cefoxitin, cefaclor, cefuroxime
Used for: Serious Gram negative infections resistant to other Beta-lactams. Sepsis and meningitis (crosses BBB.)
3rd gen: Ceftriaxone, cefotaxime, ceftazidime
Used for: increased activity against Pseudomonas and gram positive organisms.
4th gen: Cefepime
2nd gen: HEN PEcKS (Haemophilus influenzae, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E. coli, Klebsiella pneumoniae, Serratia marascens.)
Cefamandole, cefotetan uses?
Disulfiram like effects, hypersensitivity, dose adjustment in renal impairment.
Cefamandole, cefotetan side effects?
3rd gen that doesn’t cross BBB (too lipid soluble)
Cefoperazone uses?
Disulfiram like effects, hypersensitivity, dose adjustment in LIVER impairment.
Cefoperazone
A Monobactam resistant to Beta-lactamases that prevents peptidoglycan cross-linking by binding to PBP3.
- Synergistic with aminoglycosides and no cross allergenicity with penicillins.
Aztreonam mechanism of action?
Used For: Gram negative rods only: Klebsiella, Pseudomonas, Serratia.
- For penicillin-allergic pts and those with renal insufficiency who cannot tolerate amino glycosides.
- Usually nontoxic, occasional GI upset.
Aztreonam
Broad-spectrum, Beta-lactamase-resistant carbapenem. Always used with cilastatin (inhibitor of renal dehydropeptidase I) to decrease inactivation of drug in renal tubules..
Imipenem
MUST BE USED WITH CILASTATIN. Broad spectrum G+ cocci and G- rods and anaerobes. Wide spectrum but limited use due to life-threatening infections.
Imipenem uses?
SE: GI distress, skin rash, and SEIZURES. Dose reduction in renal failure.
Imipenem side effects?
Broad-spectrum, Beta-lactamase-resistant carbapenem other than Imipenem.
Meropenem mechanism of action?
Used for: Doesn’t need cilastatin. Broad spectrum G+ cocci and G- rods.
Meropenem uses?
SE: GI distress, skin rash, and less risk of seizures versus imipinem. Dose reduction in renal failure.
Meropenem side effects?
Inhibits renal dihydropeptidase I (used with Imipenem.)
Cilastatin mechanism of action?
Required for imipenem use.
Cilastatin uses?
Bactericidal. Inhibits cell wall peptidoglycan formation by binding D-ala D-ala portion of cell wall precursors (transglycosylation.)
Vancomycin mechanism of action?
Used for: Serious G+ infections. MRSA, Enterococcus, and Clostridium difficile (pseudomembranous colitis).
Vancomycin uses?
SE: Nephrotoxicity, Ototoxicity, Thrombophlebitis, diffuse flushing- “red man syndrome” (can largely prevent by pretreatment with antihistamines and slow infusion rate).
Vancomycin
Bactericidal. Inhibit formation of initiation complex and cause misreading of mRNA (30s subunit.) Requires O2 for uptake therefore ineffective against anaerobes.
Amikacin, gentamicin, streptomycin, tobramycin, neomycin
- A “initiates” the Alphabet.
Severe gram-negative rod infections. Synergistic with beta-lactam antibiotics. NOT ANAEROBES.
- Which one for bowel surgery and which one for M. tuberculosis?
Amikacin, gentamicin, streptomycin, tobramycin, neomycin uses?
- Neomycin for bowel surgery and Streptomycin for M. tuberculosis.
Nephrotoxicity (especially when used with cephalosporins), ototoxicity (especially when used with loop diuretics), teratogenic, neuromuscular blockade (like botulism.)
- Which one for Contact dermatitis?
Amikacin, gentamicin, streptomycin, tobramycin, neomycin
- Neomycin
Bacteriostatic. Inhibits attachment of aminoacyl tRNA to acceptor site (30S). Limited CNS penetration.
- Which one for renal failure because it is fecally eliminated?
Tetracycline, doxycycline, demeclocycline, minocycline mechanism of action?
- Doxycyline
Vibrio cholerae, Acne, Chlamydia, Ureaplasma urealyticum, Mycoplasma pneumoniae, Tularemia, H. pylori, Borrelia burgdorferi, Rickettsia*.
- Effective because of it’s ability to accumulate intracellularly.
Tetracycline, doxycycline, demeclocycline, minocycline uses?
GI distress, discoloration of teeth and inhibition of bone growth in children, photosensitivity. Contraindicated in children, pregnancy, and ingestion with milk (chelates calcium.) Fanconi’s syndrome (expired tetracyclines).
Tetracycline, doxycycline, demeclocycline, minocycline side effects?
Bacteriostatic. Inhibits 50S peptidyltransferase activity.
Chloramphenicol mechanism of action?
Meningitis (Haemophilus influenzae, Neisseria meningitidis, Streptococcus pneumoniae).
Chloramphenicol uses?
Anemia (dose dependent), aplastic anemia (dose independent), gray baby syndrome (in premature infants because they lack liver UDP-glucuronyl transferase). Inhibits CYP-450s.
Chloramphenicol side effects?
Bacteriostatic. Inhibit protein synthesis by blocking translocation (transpeptidation) at 50S subunit.
Clindamycin mechanism of action?
Anaerobic infections (e.g., Bacteroides fragilis, Clostridium perfringens). S. aureus osteomyelitis (enters bone.) - Treat anaerobes above the diaphragm vs metronidazole (anaerobic infections below the diaphragm).
Clindamycin uses?
Pseudomembranous colitis (C. difficile overgrowth), fever, diarrhea.
Clindamycin side effects?
Bacteriostatic. Inhibit protein synthesis by blocking translocation via 50S subunit.
Erythromycin, azithromycin, clarithromycin mechanism of action?
URIs, pneumonias, STDs, gram-positive cocci (streptococcal infections in patients allergic to penicillin), Mycoplasma, Legionella, Chlamydia, Neisseria.
- Which one for M. avium-intracellulare?
Erythromycin, azithromycin, clarithromycin uses?
- Azithromycin
Prolonged QT interval (especially erythromycin), GI discomfort (stimulates motilin receptors), acute cholestatic hepatitis, eosinophilia, skin rashes, deafness. Increases serum concentration of theophyllines, oral anticoagulants by inhibiting CYP-450s (exception: azithromycin.)
Erythromycin, azithromycin, clarithromycin side effects?
KETOLIDE. Bacteriostatic. Inhibit protein synthesis by blocking translocation via 50S subunit.
Telithromycin mechanism of action?
Macrolide-resistant S. pneumonia.
Telithromycin uses?
Bacteriostatic. Inhibits attachment of aminoacyl tRNA to acceptor site (50S) and block extrusion of completed peptide from ribosome.
Dalfopristin/quinupristin mechanism of action?
VREF/VRSA
Dalfopristin/quinupristin uses?
Bacteriostatic. Inhibits formation of initiation complex via 50S ribosomal subunit.
Linezolid mechanism of action?
VREF/VRSA
Linezolid uses?
Myelosuppression.
Linezolid side effects?
PABA antimetabolites inhibit dihydropteroate synthetase. Bacteriostatic.
Sulfamethoxazole, sulfisoxazole, sulfadiazine mechanism of action?
Gram-positive, gram-negative, Nocardia, Chlamydia, Pneumocystis, Toxoplasma (sulfadiazine). Triple sulfas or SMX for simple UTI.
Sulfamethoxazole, sulfisoxazole, sulfadiazine uses?
Photosensitivity, hypersensitivity reactions, hemolysis if G6PD deficient, nephrotoxicity (crystaluria), photosensitivity, kernicterus in infants, displace other drugs from albumin (e.g., warfarin).
Sulfamethoxazole, sulfisoxazole, sulfadiazine side effects?
Inhibits bacterial dihydrofolate reductase. Bacteriostatic.
Trimethoprim, pyrimethamine mechanism of action?
Recurrent UTIs, Shigella, Salmonella, Pneumocystis jiroveci, Toxoplasma (pyrimethamine.)
Trimethoprim, pyrimethamine uses?
Megaloblastic anemia, myelosuppression. May alleviate with supplemental folinic acid.
Trimethoprim, pyrimethamine side effects?
Inhibit DNA gyrase (topoisomerase II and IV). Bactericidal.
- Must not be taken with antacids.
Fluoroquinolones mechanism of action?
Gram-negative rods of urinary, GI tracts, and osteomyelitis (including Pseudomonas.) Neisseria, some gram positive organisms like macrolide-resistant S. pneumonia.
Fluoroquinolones uses?
GI upset, superinfections, phototoxicity (skin rashes), headache, dizziness, increase QT interval. Damage cartilage in children. Tendonitis and tendon rupture in adults; leg cramps and myalgias in kids. Contraindicate with antacids/calcium, children, and pregnancy.
Fluoroquinolones side effects?
Forms free radical toxic metabolites in the bacterial cell that damage DNA. Bactericidal, antiprotozoal.
Metronidazole mechanism of action?
Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, anaerobes (Bacteroides, Clostridium.) Used with bismuth and amoxicillin (or tetracycline) for “triple therapy” against H. Pylori.
Metronidazole
- GET GAP on the Metro with metronidazole!
Disulfiram-like reaction with alcohol; headache, metallic taste.
Metronidazole side effects?
Disrupts cell membrane.
Polymyxin mechanism of action?
Gram negative organisms.
Polymyxin uses?
Neurotoxicity, acute renal tubular necrosis.
Polymyxin side effects?
Inhibits synthesis of mycolic acids. Prodrug activated by mycobacterium’s catalase (KatG).
Isoniazid mechanism of action?
Mycobacterium tuberculosis. The only agent used as solo prophylaxis against TB .
Isoniazid uses?
Neurotoxicity, hepatotoxicity, and sideroblastic anemia. Treat with pyridoxine (vitamin B6.) Induces hemolytic anemia in G6PD deficient patients. Drug induced SLE.
Isoniazid side effects?
Inhibits DNA-dependent RNA polymerase (transcription.)
Rifampin mechanism of action?
Mycobacterium tuberculosis; delays resistance to dapsone when used for leprosy. Used for meningococcal prophylaxis and chemoprophylaxis in contacts of children with Haemophilus influenzae type B.
Rifampin uses?
Minor hepatotoxicity and drug interactions (indces CYP-450); orange body fluids (nonhazardous side effect.)
Rifampin side effects?
Effective in acidic pH of phagolysosomes where TB engulfed by macrophages is found.
Pyrazinamide mechanism of action?