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ANTIMICROBIALS

QuestionAnswer
Folic acid synthesis inhibitors (DNA methylation) 1. Sulfonamides 2. Trimethroprim
BLOCK Cell wall synthesis by inhibiting 1. Peptidoglycan synthesis 2. Peptidoglycan cross-linking
Peptidoglycan synthesis inhibitors (BLOCK Cell wall synthesis) Glycopeptides 1. Vancomycin 2. Bacitracin
Peptidoglycan cross-linking inhibitors (BLOCK Cell wall synthesis) 1. Penicillinase-sensitive penicillins 2. Penicillinase-resistant penicillins 3. Antipseudomonals 4. Cephalosporins (I-V) 5. Carbapenems (-penem) 6. Monobactams
DNA Topoisomerases inhibitors 1. Fluoroquinolones (-xacin) 2. Quinolone (Nalidixic acid)
Damages DNA Metronidazole
BLOCKS mRNA synthesis (RNA polymerase) Rifampin
BLOCK protein synthesis at 50S SUBUNIT 1. Chloramphenicol 2. Clindamycin 3. Linezolid 4. Macrolides (-thromycin) 5. Streptogramins (-pristin)
BLOCK protein synthesis at 30S SUBUNIT 1. Aminoglycosides 2. Tetracyclines (-cycline)
Penicillinase-sensitive penicillins (BLOCK cell wall synthesis) 1. Penicillin G,V 2. Ampicillin 3. Amoxicillin
Penicillinase-sensitive penicillins MOA Bind penicillin-binding proteins (transpeptidases)
Penicillinase-sensitive penicillins; clinical use 1. Gram-positive organisms 2. Neisseria meningitidis, Treponema pallidum, and syphilis.
Penicillinase-sensitive penicillins; TOXICITY Hypersensitivity reactions, hemolytic anemia.
Penicillinase-sensitive penicillins RESISTANCE Penicillinase in bacteria (a type of beta-lactamase) cleaves beta-lactam ring.
Ampicillin, amoxicillin (aminopenicillins, Penicillinase-sensitive penicillins); CLINICAL USE HELPSS kill enterococci. 1. Haemophilus influenzae 2. E. coli 3. Listeria monocytogenes 4. Proteus mirabilis 5. Salmonella 6. Shigella
Ampicillin, amoxicillin (aminopenicillins, Penicillinase-sensitive penicillins); TOXICITY Hypersensitivity reactions; ampicillin rash; PSEUDOMEMBRANOUS COLITIS.
PSEUDOMEMBRANOUS COLITIS Ampicillin, amoxicillin
Ticarcillin, piperacillin (antipseudomonals); CLINICAL USE 1. Pseudomonas 2. Gram-negative rods; susceptible to penicillinase; use with clavulanic acid.
Beta-lactamase inhibitors CAST (-bactam) 1. Clavulanic Acid 2. Sulbactam 3. Tazobactam
Often added to penicillin antibiotics to protect the antibiotic from destruction by Beta-lactamase (penicillinase) Beta-lactamase inhibitors
Organisms typically not covered by cephalosporins LAME: 1. Listeria 2. Atypicals (Chlamydia, Mycoplasma) 3. MRSA 4. Enterococci. Exception: ceftaroline covers MRSA.
Which 5th generation cephalosporin covers MRSA Ceftaroline
1st generation (cefazolin, cephalexin); CLINICAL USE PEcK; gram-positive cocci 1. Proteus mirabilis 2. E. coli, 3. Klebsiella pneumoniae
1st generation used prior to surgery to prevent S. aureus wound infections Cefazolin
2nd generation (cefoxitin, cefaclor, cefuroxime); CLINICAL USE HEN PEcKS; gram-positive cocci 1. Haemophilus influenzae 2. Enterobacter aerogenes, 3. Neisseria 4. Proteus 5. E. coli 6. Klebsiella 7. Serratia
3rd generation (ceftriaxone, cefotaxime, ceftazidime); CLINICAL USE Serious gram-negative infections resistant to other Beta-lactams.
Ceftriaxone (3rd generation Cephalosporin); CLINICAL USE Meningitis and Gonorrhea
Ceftazimide (3rd generation Cephalosporin); CLINICAL USE Pseudomonas
What antibiotic should always be added to the empiric treatment with Ceftriaxone of Meningitis in children an immuocompromised Ampicillin (to cover for Listeria monocytogenes
4th generation (cefepime); CLINICAL USE Increased activity against Pseudomonas and gram-positive organisms
5th generation (ceftaroline);CLINICAL USE Broad gram-positive and gram-negative , including MRSA
5th generation (ceftaroline) does NOT cover Pseudomonas
Cephalosporins; TOXICITY -Hypersensitivity reactions -Vitamin K deficiency. -Increased nephrotoxicity of aminoglycosides.
Which medications increase Cephalosporins nephrotoxicity Aminoglycosides
Aztreonam (Monobactam); MOA Prevents peptidoglycan cross-linking by binding to PBP3. (Cell wall synthesis inhibitor)
Aztreonam (Monobactam); CLINICAL USE 1. Gram-negative rods only 2. For penicillin-allergic patients and those with renal insufficiency who cannot tolerate aminoglycosicles.
Antibiotic used in those patients with renal insufficiency who cannot tolerate aminoglycosicles. Aztreonam
Penicillin-allergic patients Aztreonam
Carbapenems are always administered with Cilastatin (inhibitor of renal dehydropeptidase I) to decrease inactivation of drug in renal tubules.
Carbapenems (lmipenem, meropenem, ertapenem, doripenem); CLINICAL USE 1. Gram-positive cocci 2. Gram-negative rods 3. Anaerobes
Which Carbapenem has a reduced risk of seizures and is stable to dehydropeptidase I. Meropenem
Carbapenems (lmipenem, meropenem, ertapenem, doripenem); TOXICITY GI distress, skin rash, and CNS toxicity (seizures) at high plasma levels.
Vancomycin; MOA Inhibits cell wall peptidoglycan formation by binding D-ala D-ala portion of cell wall precursors.
Binds D-ala D-ala portion Vancomycin
Vancomycin; CLINICAL USE 1. Gram positive 2. MRSA 3. Enterococci 4. Clostridium difficile (oral dose for pseudomembranous colitis).
Clostridium difficile (oral dose for pseudomembranous colitis). Vancomycin
Commonly used drugs for MRSA 1. Vancomycin 2. Daptomycin 3. Linezolid
Vancomycin; TOXICITY NOT 1. Nephrotoxicity 2. Ototoxicity 3. Thrombophlebitis, diffuse flushing-¨red man syndrome¨
Red Man Syndrome caused by Vancomycin can be largely prevented by pretreatment with Antihistamines and slow infusion rate
Vancomycin; RESISTANCE Occurs with amino acid change of D-ala D-ala to D-ala D-lac
Protein synthesis inhibitors Specifically target smaller bacterial ribosome (70S, made of 30S and 50S subunits)
50S inhibitors C = Chloramphenicol, Clindamycin E = Erythromycin (macrolides) L = Linezolid
30S inhibitors A = Aminoglycosides T = Tetracyclines
Protein synthesis inhibitors "Buy AT 30, CCEL (sell) at 50." A = Aminoglycosides T = Tetracyclines C = Chloramphenicol, Clindamycin E = Erythromycin (macrolides) L = Linezolid
Aminoglycosides (30S inhibitors) Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
Aminoglycosides (30S inhibitors); MOA inhibit formation of initiation complex and cause misreading of mRNA. Also block translocation.
Require 02 for uptake; therefore ineffective against anaerobes Aminoglycosides (30S inhibitors)
Ineffective against anaerobes Aminoglycosides (30S inhibitors)
Aminoglycosides (30S inhibitors); CLINICAL USE Severe gram-negative rod infections
Used for bowel surgery. Neomycin (Aminoglycoside; 30S inhibitor)
Aminoglycosides (30S inhibitors); TOXICITY 1.Nephrotoxicity (especially when used with cephalosporins) 2.Neuromuscular blockade 3.Ototoxicity (especially when used with loop diuretics) 4.Teratogen
Aminoglycosides produce Ototoxicity, especially when used with Loop diuretics
Aminoglycosides (30S inhibitors); RESISTANCE Transferase enzymes inactivate drug by acetylation, phosphorylation, or adenylation.
Tetracyclines (-cycline) doxycycline, demeclocycline, minocycline.
Tetracyclines; MOA bind to 30S and prevent attachment ofaminoacyl-tRNA; limited CNS penetration.
Tetracycline fecally eliminated and can be used in patients with renal failure Doxycycline
Do not take Tetracyclines with milk, antacids, or iron­ containing preparations because divalent cations inhibit its absorption in the gut.
Tetracyclines (30S inhibitors); CLINICAL USE 1. Borrelia burgdorferi 2. M. pneumnoniae 3. Rickettsia and Chlamydia
Tetracyclines (30S inhibitors); TOXICITY 1. Gl distress 2. Discoloration of teeth 3. Inhibition of bone growth in children, 4. Photosensitivity. Contraindicated in pregnancy.
PHOTOSENSITIVITY SAT for PHOTO: 1. S= Sulfonamides 2. A= Amiodarone 3. T= Tetracyclines
Discoloration of teeth and inhibition of bone growth in children Tetracyclines
Tetracyclines (30S inhibitors); RESISTANCE DECREASED uptake into cells or INCREASED efflux out of cell by plasmid-encoded transport pumps.
Macrolides (50S inhibitors) Azithromycin, clarithromycin, erythromycin.
Macrolides (50S inhibitors); MOA Inhibit protein synthesis by blocking translocation; bind to the 23S rRNA of the 50S ribosomal subunit.
Bind to the 23S rRNA of the 50S ribosomal subunit Macrolides
Macrolides (50S inhibitors); CLINICAL USE 1. Atypical pneumonias (Mycoplasma, Chlamydia, Legionella) 2. STDs (for Chlamydia) 3. Gram­ positive cocci (streptococcal infections in patients allergic to penicillin).
Macrolides (50S inhibitors); TOXICITY MACRO: 1. M= Motility issues, 2. A= Arrhythmia caused by prolonged QT, 3. C= Cholestatic hepatitis (acute) 4. R= Rash 5. eOsinophilia
Increases serum concentration oftheophyllines, oral anticoagulants Macrolides (50S inhibitors)
Macrolides (50S inhibitors); RESISTANCE Methylation of 23S rRNA binding site.
Chloramphenicol; MOA Blocks peptidyltransferase at 50S ribosomal subunit
Chloramphenicol (50S inhibitors); CLINICAL USE 1. Meningitis (Haemophilus influenzae, Neisseria meningitidis, Streptococcus pneumoniae) 2. Rocky Mountain spotted fever (Rickettsia ricketsii)
Rocky Mountain spotted fever (Rickettsia ricketsii) TREATMENT Chloramphenicol (50S inhibitors)
Chloramphenicol (50S inhibitors); TOXICITY 1. Anemia (dose dependent) 2. Aplastic anemia (dose independent) 3. Gray baby syndrome (in premature infants because they lack liver UDP-glucuronyl transferase).
50S inhibitor that causes Gray baby syndrome Chloramphenicol
50S inhibitor that causes Aplastic anemia (dose independent) Chloramphenicol
Chloramphenicol (50S inhibitors); RESISTANCE Plasmid-encoded acetyltransferase that inactivates drug by acetylation
Clindamycin; MOA Blocks peptide transfer (transpeptidation) at 50S ribosomal subunit.
Clindamycin; CLINICAL USE 1. Anaerobic infections (e.g., Bacteroides fragilis, Clostridium perfringens) in aspiration pneumonia or lung abscesses. 2. Oral infections with mouth anaerobes. 3. Invasive Group A streptococcal (GAS) infection.
Treats anaerobes ABOVE the diaphragm Clindamycin
Treats anaerobes BELOW the diaphragm Metronidazole
Clindamycin;TOXICITY Pseudomembranous colitis (C. difficile overgrowth), fever, diarrhea.
Sulfonamides 1. Sulfamethoxazole (SMX) 2. Sulfisoxazole 3. Sulfadiazine.
Acne vulgaris (topical antimicrobial) Tetracyclines (1st line) Erythromycin (2nd line)
work on Aerobes Aminoglycosides
Used in Hepatic Encephalopathy Neomycin (Aminoglycoside; 30S inhibitor)
Sulfonamides; MOA Inhibit Folate synthesis. Para-aminobenzoic acid (PABA) antimetabolites inhibit dihydropteroate synthase.
Sulfonamides; CLINICAL USE 1. Gram-positive 2. Gram-negative 3. Nocardia 4. Chlamydia
simple UTI´s Triple sulfas or Sulfamethoxazole (SMX)
Sulfonamides; TOXICITY 1. Hypersensitivity reactions 2. Hemolysis if G6PD deficient 3. Nephrotoxicity (tubulointerstitial nephritis) 4. Photosensitivity 5. Kernicterus in infants
Antimicrobial that displaces other drugs from albumin (e.g., warfarin) . Sulfonamides
Antimicrobial that produces hemolysis if G6PD deficient Sulfonamides
Sulfonamides; RESISTANCE Altered enzyme (bacterial dihydropteroate synthase), DECREASED uptake, or INCREASED PABA synthesis.
Inhibit dihydropteroate synthase Sulfonamides
Inhibits bacterial dihydrofolate reductase Trimethoprim
Trimethoprim; MOA Inhibits bacterial dihydrofolate reductase
Trimethoprim-sulfamethoxazole [TMP­ SMX]; CLINICAL USE 1. UTI´s 2. Shigella 3. Salmonella 4. Pneumocystis jirovecii pneumonia (treatment and prophylaxis).
Trimethoprim is used in combination with Sulfonamides (trimethoprim-sulfamethoxazole [TMP­ SMX]), causing sequential block of folate synthesis
Block folate synthesis Trimethoprim-sulfamethoxazole [TMP­ SMX]
Pneumocystis jirovecii pneumonia (treatment and prophylaxis) Trimethoprim-sulfamethoxazole [TMP­ SMX]
UTI´s Trimethoprim-sulfamethoxazole [TMP­ SMX]
Toxoplasmosis prophylaxis Trimethoprim-sulfamethoxazole [TMP­ SMX]
Trimethoprim; TOXICITY Megaloblastic anemia, leukopenia, granulocytopenia. (May alleviate with supplemental folinic acid [leucovorin rescue].)
Granulocytopenia caused by Trimethoprim may alleviate with supplemental folinic acid [leucovorin rescue].)
Fluoroquinolones; MOA Inhibit DNA gyrase (Topoisomerase II) and Topoisomerase IV.
Inhibit DNA gyrase Fluoroquinolones
Fluoroquinolones must NOT be taken with Antacids
Fluoroquinolones; CLINICAL USE 1. Gram-negative rods urinary and GI tracts (including Pseudomonas) 2. Neisseria 3. Some gram-positive organisms
Fluoroquinolones; TOXICITY 1. GI upset, superinfections, skin rashes, headache, dizziness. 2. Tendonitis, tendon rupture, leg cramps, myalgias. 3. Prolonged QT interval. 4. Tendon rupture in people > 60 years old and in patients taking prednisone.
Fluoroquinolones contraindicated due possible damage to cartilage. 1. Pregnant women 2. Nursing mothers 3. Children under 18
Tendon rupture in people > 60 years old and in patients taking prednisone. Fluoroquinolones
Antimicrobial that prolongs QT interval. Fluoroquinolones
Fluoroquinolones; RESISTANCE Chromosome-encoded mutation in DNA gyrase, plasmid-mediated resistance, efflux pumps.
Metronidazole; MOA Forms free radical toxic metabolites in the bacterial cell that damage DNA.
Bactericidal, antiprotozoal Metronidazole
Metronidazole; CLINICAL USE GET GAP on the Metro with metronidazole! G= Giardia E= Entamoeba T= Trichomonas G= Gardnerella vaginalis A= Anaerobes (Bacteroides, C. difficile). P= H. Pylori.
Used with a proton pump inhibitor and clarithromycin for "triple therapy" against H. Pylori. Metronidazole
"triple therapy" against H. Pylori. Proton pump inhibitor + Clarithromycin + Metronidazole
Metronidazole; TOXICITY 1. Disulfiram-like reaction (severe flushing, tachycardia, hypotension) with ALCOHOL 2. Headache 3. MetaIIic taste.
MetaIIic taste Metronidazole
Disulfiram-like reaction (severe flushing, tachycardia, hypotension) with ALCOHOL Metronidazole
M. tuberculosis; PROPHYLAXIS Isoniazid
M. avium-intracellulare; PROPHYLAXIS Azythromycin, Rifabutin
M. tuberculosis; TREATMENT RIPE R= Rifampin I= Isoniazid P= Pyrazinamide E= Ethambutol
M. avium-intracellulare; TREATMENT Azithromycin, rifampin, ethambutol, streptomycin
M. leprae; TREATMENT Tuberculoid form: dapsone and rifampin Lepromatous form: add clofazimine
Isoniazid; MOA Decreases synthesis of mycolic acid. Bacterial catalase-peroxidase (KatG) needed to convert INH to active metabolite.
ONLY agent used as SOLO prophylaxis against TB Isoniazid
Isoniazid; CLINICAL USE Mycobacterium tuberculosis
Isoniazid; TOXICITY 1. Neurotoxicity 2. Hepatotoxicity 3. Lupus
Can prevent neurotoxicity produced by Isoniazid Pyridoxine (vitamin B6)
Rifamycins (Rifampin, rifabutin); MOA Inhibits DNA-dependent R A  polymerase.
Rifampin's 4 R's 1. RNA polymerase inhibitor 2. Ramps up microsomal cytochrome P-450 3. Red/orange body fluids 4. Rapid resistance if used alone
Used for MONOTHERAPY in Meningococcal prophylaxis Rifampin
Red/orange body fluids Rifampin
Rifamycins (Rifampin, rifabutin); CLINICAL USE 1. Mycobacterium tuberculosis 2. Delays resistance to dapsone when used for leprosy. 3. Meningococcal prophylaxis 4. Chemoprophylaxis in contacts of children with Haemophilus influenzae type B.
Chemoprophylaxis in contacts of children with Haemophilus influenzae type B Rifamycins (Rifampin, rifabutin)
Rifamycin prefered in patients with HIV infection due to less cytochrome P-450 stimulation Rifabutin
Ethambutol; MOA Decreases carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltransferase
Blocks arabinosyltransferase Ethambutol
Ethambutol; CLINICAL USE M. tuberculosis; RIPE R= Rifampin I= Isoniazid P= Pyrazinamide E= Ethambutol
Ethambutol; TOXICITY Optic neuropathy (red-green color blindness)
Optic neuropathy (red-green color blindness) Ethambutol
Endocarditis with surgical or dental procedures; Antimicrobial prophylaxis Penicillins
Meningococcal infection; Antimicrobial prophylaxis Ciprofloxacin (drug of choice), rifampin for children
Gonorrhea; Antimicrobial prophylaxis Ceftriaxone (3rd generation Cephalosporin)
Syphilis; Antimicrobial prophylaxis Benzathine penicillin G (IV and IM form)
History of recurrent UTI´s; Antimicrobial prophylaxis TMP-SMX
Pregnant woman carrying group B strep; Antimicrobial prophylaxis Ampicillin
Prophylaxis of strep pharyngitis in child with prior rheumatic fever Oral penicillin
Prevention of postsurgical infection clue to S. aureus Cefazolin (1st generation Cephalosporin)
Prevention of gonococcal or chlamydial conjunctivitis in newborn Erythromycin ointment
HIV Prophylaxis 1. CD4 < 200 cells/mm3, Pneumocystis pneumonia: TMP-SMX 2. CD4 < 100 cells/mm3, Pneumocystis pneumonia + Toxoplasmosis: TMP-SMX 3. CD4 < 50 cells/mm3, MAC: Azithromycin
Treatment of Vancomycin- Resistant Enterococcus (VRE) Linezolid and Streptogramins (quinupristin/dalfopristin)
Created by: heidy39