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Penicillins
Class: Antibacterials, Beta Lactams Use: Gram + MOA:Bactericidal. Penicillin binding protein (PBP) aka transpeptidase inhibition, cannot crosslink peptidoglycans, no murein assembly--> weak cell wall; lysis Side Effects: Hypersensitivity, sensitization, allergy, ana shock Resistance: beta-lactamases, mycobacteria (b/c slow growing, TB and Leprosy), mycoplasma (b/c lack cell walls), inaccessible PBP Other: Food interferes so parenteral is best (except amoxicillin), no BBB cross (unless inflammed meninges), eliminated by kidney, probenecid prolongs half-life
Penecillin G
Class: Antibacterials, Beta lactams, Penicillins Use: NARROW SPECTRUM. G+, Non-lactamase producing Streptococcus, C. diptheria, Syphilis (spirocete)
Oxacillin
Class: Antibacterials, Beta lactams, Penicillins MOA: penicillinase resistant Use: penicillinase-producing Staph aureus (soft tissue and skin infections)
Amoxicillin
Class: Antibacterials, Beta lactams, Penicillins Use: Extended spectrum; E. coli and CA G(-) infections (sinusitis, otitis media, UTI); endocarditis prophylaxis for dental work Resistance: sensitive to lactamase
Ampicillin
Class: Antibacterials, Beta lactams, Penicillins Use: Extended spectrum; E. coli and CA G(-) infections (sinusitis, otitis media, UTI) Resistance: sensitive to lactamase
Ticarcillin
Class: Antibacterials, Beta lactams, Penicillins Use: NA G(-) enteric bacteria (except Klebsiella) and pseudomonas aeroginosa Resistance: sensitive to lactamase unless you add inhibitor (Clavulanate)
Piperacillin
Class: Antibacterials, Beta lactams, Penicillins Use: NA G(-) enteric bacteria (except Klebsiella) and pseudomonas aeroginosa Resistance: sensitive to lactamase unless you add inhibitor (Tazobactam)
Cephalosporins
Class: Antibacterials, B lactams (bacteriocidal) Use: Gram (+) Resistance: not effective for anaerobes Metabolism: mainly excreted by kidney, some by bile (Cefperazone, ceftriaxone); some cross BBB (cefotaxime) Side effects: Hypersensitivity; less than 5% of ppl sensitive to penicillin will react to cephalosporins - use with caution; Disulfram-like reaction (inhibits aldehyde dehyrogenase so accumulate acetaldehyde); nephrotoxicity
Cefazolin
Class: Antibacterials, B lactams, Cephalosporins, 1st generation Use: penicillinase resistant; G (+) --> Strep/Staph infections for surgical prophylaxis and skin infections (cellulitis); G (-)--> PEcK (proteus mirabilis; E. coli; Klebsiella pneumoniae)
Ceftriaxone
Class: Antibacterials, B lactams, Cephalosporins, 3rd gen Use: Broad Spectrum, esp G (-); gonorrhea, meningitis, pneumonia !!!!!Crosses BBB!!!!!
Ceftazidime
Class: Antibacterials, B lactams, Cephalosporins, 3rd gen Use: Broad Spectrum, esp G (-); Best against Pseudomonas
Cefepime
Class: Antibacterials, B lactams, Cephalosporins, 4th gen Use: Broad Spectrum; Treats multidrug resistant aerobic G (-); resistant to many B lactamases; one of \"big guns\" against opportunistic G (-) nosocomial acquired infections, only used in hospital setting
Ceftobiprole
Class: Antibacterials, B lactams, Cephalosporins, 5th gen Use: G (+) and some G (-) like pseudomonas; Broad spectrum anti-MRSA Interactions: will compete with Cefepime
Carbapenems
Class: Antibacterials, beta lactams Use: broadest spectrum; G(+); G(-) rods (pseudomonas); anaerobes; drug of choice for enterobacter
Imipenem
Class: Antibacterials, beta lactams, Carbapenems Use: BIG GUN for serious nosocomial infections, intra-abdominal infections, and mixed infections; resistant to most B-lactamases; Broad spectrum = G (+) and G(-) rods (pseudomonas); anaerobes; enterobacter Metabolism: inactivated by dehydropeptidase in renal tubule to inactive metabolite that is potentially nephrotoxic; MUST use with cilastatin (inhibits dehydropeptidase); penetrates CSF when inflamed; IV admistration Side effects: penicillin sensitive cross allergic to Imipenem; cause seizures; CI in epileptics
Meropenem
Class: Antibacterials, B lactams, Carbapenems (First carbapenem used in children) Use: BIG GUN for serious nosocomial infections, intra-abdominal infections, and mixed infections; resistant to most B-lactamases; Broad spectrum = G (+) and G(-) rods (pseudomonas); anaerobes; enterobacter Metabolism: no need for cilastatin. IV Side effects: well tolerated; low incidence of seizures
Aztreonam
Class: Antibacterial, beta lactams, Monobactam Use: narrow spectrum, Bactericidal, resistant to B-lactamase, NO G (+) coverage; Only G (-) aerobic rods, Pseudomonas aeruginosa Metabolism: excreted in urine Side effects: tolerable to penicillin sensitive patients; no cross allergic rxns; usually safe but can cause GI upset, Leucopenia or SEIZURES - CI for epileptics and pts with low WBC
Ticarcillin + clavulanate (Timentin fyi)
Class: Penicillin + B-lactamase inhibitor Use: G (-) including Pseudomonas; nosocomial acquired stenotrophomonas (acquired in plastic tubing used in hospitals)
Amoxicillin + clavulanate (Augmentin fyi)
Class: Penicillin + B-lactamase inhibitor, Use: broad spectrum for community acquired infections - upper respiratory infections; sinusitis, otitis media
Ampicillin + sulbactam (Unasyn fyi)
Class: Penicillin + B-lactamase inhibitor, Use: G + coverage - staph/strep infections causing cellulitis
Piperacillin + Tazobactam (Zosyn fyi)
Class: Penicillin + B-lactamase inhibitor, Use: nosocomial infections - used in ICU for empiric treatment; one of \"big guns\" against nosocomial infections ( G (-) multidrug resistant); G (-), G (+) and anaerobes in intra-abdominal infections, pneumonia and sepsis
Vancomycin
Class: Class: Antibacterial, Non B-lactams, Glycopeptide MOA: inhibit cell wall synthesis by binding to substrate of transpeptidase ( D-alanyl - D alanine site); bactericidal, resistant to b-lactamase Use: G (+); agent of last resort; serious and penicillin resistant nosocomial G (+) ie. MRSA from line infections, Staph and Strep Metabolism: poor oral admin but used orally to treat antibiotic associated colitis Side effects: Red man syndrome (flushing); nephrotoxicity; ototoxicity, thrombophlebitis
Sulfonamides
Class: Antibacterial, Non B-lactams MOA: bacteriostatic; p-aminobenzoic acid (PABA) analog; inhibits bacterial dihydropteroate synthase which uses PABA in Tetrahydrofolic acid (folate) synthesis (human cells obtain folate from diet) Use: G (+/-), UTI, URI Metabolism: rapidly absorbed from GI (70-100% oral dose) unless insoluble type; bound to plasma proteins; can enter CSF, placenta, mother\'s milk; acetylated in liver: this inhibits drug’s activity but it’s still toxicity; INHIBITS P450; excreted in urine Side effects: nephrotoxicity due to precipitation in urinary tract; hypersensitivity rxns (Stevens Johnson syndrome – skin sloughs off; “arthritis and lupus-like” symptoms); acute hemoylytic anemia (G6PD deficiency); agranulocytsosis (low PMN); aplastic anemia (not making WBCs) Drug Interactions: oral anticoagulants, sulfonylurea hypoglycemic agents, hydantoin anticonvulsants (binding to plasma protein by sulfa drug may result in displacement of other drugs thus increasing their plasma conc.) CI: pregnant or lactating women Resistance: alter drug, get folate from environment
Sulfamethoxazole
Class: Antibacterial, Non B-lactams, Sulfonamides Use: Uncomplicated UTIs (usually by E. coli); prevention of urinary and upper respiratory tract infections. Metabolism: Rapidly absorbed and eliminated
Trimethoprim
Class: Antibacterial, Non B-lactams, Dihydrofolate Reductase Inhibitors MOA: bacteriostatic; inhibits dihydrofolate reductase so cannot produce THF; folate needed for nucleic acid synthesis by bacteria; much higher affinity by bacterial reductase than human reductase Metabolism: Orally given along with sulfamethoxadole (TMP-SMX); rapidly absorbed and distributed; can get into CSF, placenta, milk; excreted in urine Side effects: megaloblastic anemia; leukopenia; granulocytopenia; skin rashes; GI upset, hemolysis if G9PDh deficient
Sulfamethoxazole + Trimethoprim (TMP-SMX), (Cotimoxazole fyi)
Use: first line treatment for uncomplicated UTI; bacterial respiratory tract infections (CA Bronchitis, sinusitis and acute otitis media); treat salmonella and shigella in GI; parasitic infections in AIDS patients (prophylaxis and treatment for Pneumocysis carinii pneumonia (fungus)); COMMUNITY acquired MRSA DI: These have synergy, don’t need as high of a dose of sulf, less side effects
Quinolones
Class: Antibacterial, Non B-lactams MOA: Bactericidal; enter through porins; inhibit DNA replication by interfering w/ DNA gyrase (topoisomerase II), prevents relaxation of supercoiled DNA; binds gyrase and DNA and inhibits the rejoining step following DNA cleavage. Use: BROAD SPECTRUM; virtually all G (-) community acquired pneumonia; enteric bacteria; atypical respiratory pathogens (Legionella, Chlamydia, Mycoplasma); TB and MAC, multi-drug resistant UTIs, NA opportunistic infections, gastroenteritis, STDs, mycobacterial infections Metabolism: Oral absorption (70-90% in most); ingestion of antacids or dietary iron or zinc supplements (cations) decrease absorption; excreted in urine, blocks p450 enzymes Resistance: change DNA Gyrase so drug can’t bind it Side effects: Inhibits P450, Hepatotoxicity, photosensitivity, Tachycardia; nausea, vomiting, diarrhea, headache, dizziness, insomnia, rarely seizures, delirium, hallucinations; NSAID may potentiate stimulation; skin rashes (photosensitivity)-should avoid direct sunlight; CI for children and pregnant woman; superinfection with Candida (yeast) and streptococci; arrhythmias
Ciprofloxacin
Class: Antibacterial, Non B-lactams, Quinolones, (2nd Gen) Use: G (-) Gastroenteritis (enteric pathogens) where you have Shigella and salmonella, best for Pseudomonal infections and nosocomial infection
Levofloxacin
Class: Antibacterial, Non B-lactams, Quinolones, (3rd G) Use: increased G(+) coverage, G(-) too; serious community-acquired pneumonias (S. pneumonia) ; H. influenzae, sinusitis, chronic bronchitis, URI
Moxifloxacin
Class: Antibacterial, Non B-lactams, Quinolones, (4th G) Use: G(+) coverage; Streptococcus; anaerobes Side effects: No photosensitivity or liver metabolism
Tetracyclines
Class: Antibacterial, Non B-lactams MOA: Protein synthesis inhibitor; enter bacteria’s outer membrane through porins, then actively pumped across inner membrane; binds 30s ribosomal subunit; blocks access of the amino acyl-tRNA to mRNA-ribosome complex “A” site; bacteriostatic Use: broad spectrum; G(-), we have better drugs for G(+); First line for Chlamydia and Cholera and Zoonotic infections; spirochetes; lyme disease (Borrelia -spirochete) Metabolism: Rapid absorption from GI; most are excreted in urine; enter CNS (but NOT enough to treat meningitis), placenta, milk Side effects: photosensitivity; vestibular problems; superinfection; stored in bone and teeth b/c it binds Caresult in discoloration; may stunt growth in children; CI in pregnant women, breast feeding woman, or children < 8; hepatotoxicity w parenteral administration ; renal toxicity if expired (Fanconi like syndrome); do not take with milk or Ca containing antacids Resistance: bacteria may induce efflux pump, may change porin, enzymatic inactivation
Doxycycline
Class: Antibacterial, Non B-lactams, Tetracyclins Use: Rocky Mountain Spotted Fever (Rickettsia), Lyme Disease (Borrelia - Spirochete), and Urethritis (Chlamydia trachomatis) Metabolism: bind to calcium; excreted via bile; can be used with renally impaired, lipophilic so penetrates tissue well
Tigecycline
Class: Antibacterial, Non B-lactams, Glycylcycline (similar to tetracyclines) MOA: Binds 30s Use: Expanded broad spectrum, G+, G-, anaerobic, atypical, resistant pathogens; used for DRUG RESISTANT STRAINS only; MRSA, PRSP, VRE, Complicated skin infections, Complicated intra-abdominal infections; does NOT cover Pseudomonas (pump) Metabolism: IV administration, Blocks P450 Side effects: cross sensitivity with tetracycline; CI for pregnant woman; superinfection Drug Interaction: warfarin levels increased; oral contraceptives less effective
Macrolides
Class: Antibacterials, Non B-Lactams MOA: Protein synthesis inhibitor; bacteriostatic/bacteriocidal at higher doses; irreversibly binds to 50S ribosomal subunit and inhibits translocation Use: community-acquired upper respiratory infections, like walking Pneumonia, from Legionella, mycoplasma, chlamydia; Bordetella pertussis (whooping cough) -Azithromycin (Z-pac) = Think URI; best empiric coverage, also covers Otitis media from H. influenzae, M. catarrhalis, M. avium, NOT inhibit P450 -Erythromycin = Gram (+) Corynebacterium diphtheria -Clarithromycin = M. avium, H. pylori Metabolism: Oral route; NOT distribute to CSF; can diffuse into prostatic fluid; most are metabolized in liver so interfere with p450 (except azithromycin); erythromycin and azithromycin excreted in bile; clarithromycin excreted in urine and liver Side effects: can inhibit metabolism of other drugs due to p450 inhibition (corticosteroids, digoxin, warfarin, theophylline); irritating to GI; cholestatic hepatitis Resistance: plasmids: change porin, modify 50s, efflux pump (S. pneumonia), hydrolysis of drug by esterases
Telithromycin
Class: Antibacterials, Non B-Lactams, Ketolides MOA: first ketolide; binds TWO sites on 50s subunit; prevent protein synthesis Use: most common and atypical respiratory pathogens; URIs; effective against B-lactam and macrolide resistant pathogens; Strep pneumonia, acute sinusitis and bronchitis Metabolism: inhibits p450 Side effects: vision problems; irregular heartbeat (arrythmias), dizziness, diarrhea, headache; liver toxicity; DO NOT USE with pts that have liver problems or myasthenia gravis!!!! DI: not use with pimozide and cisapride
Clindamycin
Class: Antibacterials, Non B-Lactams, Lincomycins (Lincosamides) MOA: binds 50 S subunit; protein synthesis inhibitor Use: Most G(+), and those resistant to penicillin; NOT for use with Gram (-). Treat lung abscesses; anaerobe infections ABOVE the diaphragm; anaerobic Strep, Staph or Bacteroides; good for pts allergic to B-lactam antibiotics; good against ANAEROBES (but not C. difficile) Metabolism: widely distributed, NOT in CNS; 90% bound; excreted via liver, kidney, and bile Side effects: diarrhea, nausea, rashes, superinfection (colitis) due to broad specificity
Quinopristin/Dalfopristin (synercid)
Class: Antibacterials, Non B-Lactams MOA: binds to 50s (or 23s) subunit; protein synthesis inhibitor Use: bacteriocidal to G(+); multidrug resistant strains of Staphylococci, pneumococci (Strep pneumoniae); enterococci (Strep). Use for Osteomyelitis, endocarditis, line infections, pneumonia, bacteremia and soft tissue infections if resistance or intolerance to Vancomycin Side effects: very painful injection, inflammation, edema, nausea, vomiting, rash, muscle and joint pain
Linezolid (Zyvox)
Class: Antibacterials, Non B-Lactams, oxazolidinones fyi MOA: protein synthesis inhibitor; binds 50S and prevents formation of tRNA-mRNA-30S complex Use: for severe multidrug resistant G+ bacteria; MRSA; MRSE, S. pneumoniae and VRE; NOT USED for G(-) b/c efflux pump Metabolism: oral; no cross rxn with other antibiotics Resistance: appears slowly via methylation of 50s which prevents the drug from binding it Side effects: headache, nausea, and vomiting; bone marrow suppression, decreased platelets (reversible with discontinuation)
Metronidazole
Class: Antibacterials, Non B-Lactams MOA: serves as electron acceptor and disrupts electron transport chains in anerobes and amoebae; inhibits DNA synthesis. Use: anaerobes BELOW diaphgram; Superinfections from Clostridium difficile; “GET on the metro” (Giardia, entamoeba, trichomonas) Metabolism: taken orally; can distrubute well including CSF; metabolized in liver by P450 DI: phenobarbital enhances metabolism; cimitidine prolong half life Side effects: nausea, vomiting, epigastric distress; disulfiram affect w/ alcohol
Daptomycin
Class: Antibacterials, Non B-Lactams MOA: novel cyclic lipopeptide; targets membrane; causes rapid depolarization of membrane potential, bactericidal Use: G(+); drug resistant G+ bugs of the skin; NOT for respiratory infections (can’t penetrate lung) Metabolism: excreted in urine Side effects: constipation; nausea; fever; headaches
Aminoglycosides
Class: Antibacterials, Non B-Lactams MOA: enters porin, binds to 30S; oxygen dependent active transport across inner membrane; inhibits INITIATION of protein synthesis, Causes premature termination of translation, and incorporation of incorrect AA into the membrane (causing POST-ANTIBIOTIC EFFECT… bacteria that survive initial AB will die later anyway because their membrane is messed up) Use: G(-) aerobes; Used exclusively in hospital, with penicillin or cephalosporin for synergy; Serious G- bacilli, Pseudomonas, Klebsiella, Serratia Resistance: if bacteria become anaerobic or inactivate aminoglycoside (via phosphorylation, acetylation, or adenylation); can change 30s, porin Metabolism: poorly absorbed orally; administered IV or IM; NOT enter CSF; rapidly excreted by kidney Side effects: Reserved for severe, life threatening conditions due to TOXICITY; ototoxicity (causes clumping together of hair cells); retrograde degeneration of auditory nerve; decreased type I sensory hair cells in vestibular organ (headaches, vertigo, ataxia); renal insufficiency due to degeneration of proximal tubular cells (reversible); neuromuscular blockage - inhibits internalization of calcium in presynaptic terminal so decrease ACh release; CI with myasthenia gravis pts
Amikacin
Class: Antibacterials, Non B-Lactams, Aminoglycosides Use: Used with B-lactams to increase coverage in serious G (-) nosocomial acquired infections; resistant to many enzymes that inactivate other aminoglycosides; less toxic than others
Tobramycin
Class: Antibacterials, Non B-Lactams, Aminoglycosides Use: used with B-lactams to increase coverage in serious G (-)nosocomial acquired infections
Gentamicin
Class: Antibacterials, Non B-Lactams, Aminoglycosides Use: used with B-lactams to increase coverage in serious G (-)nosocomial acquired infections
Streptomycin
Class: Antibacterials, Non B-Lactams, Aminoglycosides Use: TB; plague; limited use due to high levels of resistance
Treatment of G + Bacteria - Community Aquired
Penicillin G for non-resistant Strep

Oxacillin for non-resistant Staph

Cefazolin/Clindamycin for non-resistant Staph or Strep severe skin infection

Treatment of G + Bacteria - Nosocomial or severe CA
Vancomycin for MRSA

Ceftriaxone for S. pneumonia

Levofloxin, Moxifloxacin 

Treatment of G + Bacteria - Multi-drug Resistant
Linezolid; Synercid (Quin/Dalf); Daptomycin for VRE and Staph

Linezolid; Synercid; Telithromycin for S. pneumoniae

 
Treatment of G (-) Bacteria - CA
Azithromycin for walking pneumonia

Ampicillin, Amoxicillin for otitis media and sinusitis

Sulfamethoxazole/Trimethoprim for UTI

Doxycycline for Chlamydia, Cholerae, Zoonotic

Ciprofloxacin for gastroenteritis with Shigella and Salmonella

Treatment of G (-) Bacteria - NA or serious CA
Ceftazidime for Pseudomonas

Ceftriaxone is the "work horse"

Aztreonam for Pseudomonas

Aminnoglycosides + beta lactams

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