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Nafcillin, Methicillin, Oxacillin
Penicillinase resistant penicillins
Active against penicillinase producing Staph. Drug of choice for Staphylococcal dz.
Worthless for garm neg bac, and MRSA
Stable in acid: absorbed in GI tract
Severe infection requires injection
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Penicillin V, Potassium
Natural Penicillin
Good oral abosrption. Treats group AB hemolytic Strep gram pos and neg cocci.
Anaerobes are susceptible
Watch renal fxn in neonates/infants
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Penicillin G
Natural Penicillins
- Used for: Group AB hemolytic strep.
- Gram neg and gram pos cocci
Anaerobes are susceptible
Unstable in gastric acid: poor oral absorption
Special considerations: neonates/infants: renal fxn
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Ampicillin
Ampicillin/sulbactam
Amoxicillin
Amoxicillin/clavulanate
- Aminopenicillins
- Broad spectrum
- used for URI, L. monocytogenes in immunocompromised. Gram negh
Resisitant: H. influenzae, N. Gonorrhoeae, enterobacteriaceae
Interferes w/ oral contraceptives
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Piperacillin
Piperacillin/tazobactum
Ticarcillin
Ticarcillin/clavulante
- Antipseudomonal PUN
- Up activity against pseudomonal, enterobacter and proteus. Activfe against Klebsiella
- Up gram neg coverage
Resistance to PCNG impries resistance to these drugs
Serious, pseudomonal require additional aminoglycoside.
Reserved for severe, hospital acquired gam neg bacteria
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All Penicillins
Adverse rxn: maculopapular rash
Uticarial rash, stevens-johnson syndrome
Serum sickness, bronchospasm angioedema
Toxicity: rare. Watch for bone
Marrow depression granupocytopenia, hepatitis, impaired pt fxn, lethargy, confusion, seizures superinfections
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Cephalexin
Cefadroxil
1st gen cephalosporin
Gram pos coverage w/ gram pos cocci, less gram neg coverage; oral anaerobes are covered
Not active against enterococcus, MRSA, MRSA or VRE
Cefadroxil- better PO absorption, BID
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Cefuroxime
- 2nd gen cephalosporin
- low gram pos coverage
- hih gram neg coveragers (e. coli, klebsiella)
- Resistant to Beta lactamases
- useful for H. influenzae, N. meningitidis and pneumococcal meningitis
Injection
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Cefotoxin
2nd gen cephalosporin/ bacteroides
Better anaerobic coverage including B. fragilis
Injectable
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Cefuroxime axefil
Cefador
2nd gen cephalosporins
More active against H. Influenzae and M. Catarrhalis
are given PO
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Ceftriaxone
3rd gen cephalosporin
Decreased gram pos, much better gam neg, esp Beta lactamase
Penetrates CSF
Enterobacteriaceae
Not for: Listeria mono, MRsA, VRE, injected, once daily, good for penicillinase- gonococcus also empiric for meningitis in noncompromised due to H. influenza, S. pneum, N. meningitis, gram neg bacilli
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Ceftazidime
Injectable 3rd gen cephalosporin
more active against pseudomonas
Penetrates CSF
DOC w/ aminoglycoside for meningitidis by pseudomonas
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cefdinir
oral 3rd gen cephalosporin
More active against enterobacteriaceae and B-lactamase producing H. influ and N. gonorrhea
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Cefixime
oral 3rd gen cephalosporin
BID dose
Enterobacteriaceae, B-lactamase, H. influenzae, and N. gon
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Cefepime
4th gen injected cephalosporin
Enterobacteriaceae resistant to other cephalos
Good antipseudomonal
Excellent CSF
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Ceftobiprole
4th gen injected cephalosporin
Designed for MRSA penicillin binding protein, active against MRSA
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Imipenem/ cilastin
IV or IM
Carbapenems
Cilastin inhgibits renal tubular dipeptidase (degrades imipenem)
Imipenem: ery broad gram pos cocci-not MRSA
Enterobacteriaseae, pseudomonas, B. fragilis, acinetobacter
For severe UTI, lower RTI, intraabol, gynecologic, skin, bone, joint, severe mixed nosocomial
N/V, hypersensitive- cross w/ pen and up LFT
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Meropenem
Similar to imipenem- not sensitive to renal tubular dipeptidase
Less active against gram pos cocci
Limited use
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Ertapenem
Same as Meropenem
Less gram pos cocci than imipenem
Limited use
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Doripenem
Same as meropenem and entapenem but w/ resistance by pseudomonas
Limited use
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Aztreonam
IV/IM
Monobactams- similar to aminoglycosides
Mostly gram neg- aerobic
gram pos/anerbobes resist
Great for enterobacteriaceae, also pseudomonas, H. flu, N. gon
OK in Penicillin allergy, phlebitis, eosinophilia
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Teicoplanin
Like vanc
T1/2 is 100hrs
Van A enterococci resist
Hypersensitivity, ototoxicity
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Vancomycin
Ototoxicity, nephrotox-caution w/ aminoglycosides: anaphylaxis, red neck flush w/ rapid....
Glycopeptide
Binds d-alanyl-d-dlanine terminus of peptidoglycan precursors
Inhibits earlier strep than B-lactams
Rapid bactericidal in growing cells
Bacteriostatin for enterococci
Resist: modified enzyme modifies peotidoglycan-plasmid
For gram pos, MRSA, 2nd line C. Dif,
Most enterobacci, bas S. pyogenesw, S. pneumo (?)
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Macrolides
Binds 5OS ribo
Gram pos= 100x etter acumulate
inhibits peptide bond formation by inhibiding translocation from A to P site
Bacteriostatic
Resist: plasmid-down permeability, efflux pump, methylate enzymes 50S, esterase hydroxyzes drug
For: gram pos cocci, not staph, enterococcus gram pos bacillus, mycoplasma=DOC
Gram neg bacilli= H. influ, H. Ducreyi, C. jejuni, J. pylori
DOC= legionella, B. pertussis
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Erythromycin
Macrolide
Poorly absorbed, worse w/ food, destroyed by acid
No Bb cross, and metab by liver
DOC: M. pneumo, C. diptheriae, C. pneumo, B. pertussis, H. ducreyi
Also- clamydiae, C. Trachomatis for strep, C. tetani, T. pallidum preggo w/ PCN allergy
GI:
Prolong QT, transient auditory
Inhibit P455, CYP 3A4= Up benzao, cyclosporine, carbametepine, steroids
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Clarithromycin
Macrolide
rapid absorb, big first pass
DOC Myco avium intracellular complex
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Azithromycin
Macrolide
rapid absorb, stable in acid
Take on empty stomach
T1/2= 68rh
Single lg dose for C. trachomatis
Also best macrolide for H. influ URI
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Telithromycin
Ketolide
Slight better spectrum, no food interfere, Major 3A4 metabolizer
No in kids less than 12
GI, NV, Diarrhea, Up LFT, prolong QT
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Clindamycin
Oral lincosamide
Binds 50S, bacteriostatin similar to macrolides
Gram pos cocci Strep and non-MRSA Staph
Better anerobe coverage than macrolides
- C. Perfingen, peptostrepto, peptococcus, propionbac, Bacteroides
- Also-protozoal
For: anaerobic infect fecal spill, pelvic abscess topical acne, bact vaginosis perotinitis gram pos cocci
GI, superinfection, rash common, STI's
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Chloramphenicol
binds 50S prevents amino-acid containing end of aminoacyl tRNA binding to A site
Bacteriostatic
resist: chloramphenicol acetyltransferase, Down perm, mutate 50S
- For: gastroenteritis- Salmonella and syph
- Meningitidis- H. influ, N. men, S. pneumoRickettsial dz if TCN sensitive, Brucellosis 2nd to TCN
Heme tox- anemia, leukopenia, thrombo, N/V common, inhibits P450 and Pheny, anaplastic anemia, gray baby syndrome, inhibit mitochondrial respiration
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Quinupristin (30) and Dalfopristin (70)
- Quinupristin: conformational change=Up quin effect
- Bacteriostatic= E. faecium, others killed
- For: gram pos cocci, MRSA, VRE, E. faecium, MDR Pneumococci
Atypicals- M. pneumo, C. pneumo, Legionella
CYP3A4 metab- inhibits
Infusion site pain, arthralgias, myalgias,, and up LFT
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Linezolid
Oxalidinone- bind 50S
- Bacteriostatic- Staph and Enterococci
- Kills-Strep
- For: gram pos staph, strep, MRsa, VRE, E. faecium, S. pyogenes, bind skin infect.
- Oral
- Not CYP metab,=-MAO
- GI, HA, N/V, diarrhea, myelosuppress thrombocytopenia, anemia
- Interacts w/ MAO inhibitors and adrenergic agonists
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Mupirocin
Bactroban
From pseudomonas fluorescens
Binds bac Bolencyl-tRNA synth
Highly active aghainst Staph, MRSA, most strep.
Usually topically for MRsa carrier in Strep
Ant. Nares(?)
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Tigecycline
Better activity against MRSA and VRE
Used empirically for complicatd skin infxns caused by MRSA and intrabol(?) infxns
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Minocycline
propionibacterium acnes
Metabolized by liver
vestibular tox
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Doxicycline
Tetracycline
DOC: borrelia, mycoplasma, ureaplasma, urealyticum, chlamydiae, rickettsiae
Metabolism induced by barbituates/phenytoin
photosensitivity, Not preggo, not less than 8yrs
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Tetracycline
Tetracycline binds 30S
DOC: rickettsiae, chlamydiae, borellia, mycoplasma, ureaplasma
Gi UPSET, PHOTOSENSITIVITY, NEPHROTOX, TEETH AND BONE
Not- preggo, less than 8yo
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Tobramycin
Better than gent for pseudomonas
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Gentamycin
Aminoglycoside
Nosocomial pneumonia- empiric for hospital acquired mulit-resist gram neg aerobes, some kleb and pseudomonas are resistant
- Pseudomonal sepsis
- enterococcal infections
- topical-ocular
- Nephrotox-renal prox tubule
- Ototox: cochlear=25% Starts high then goes low. Tinnitus, vestibular tox=HA leading to vertigo
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Aminoglycosides
Diffused through aq pore in outer membrane grm neg acive transport across cytoplasmic membrane
Binds 30S ribo of polysomes
Interfere w/ initiation and synth, block furtyher translation, premature term, misread RNA and destruction of cytoplasmic memb and death
Resist: fail permeation, low affinity for ribo, enzyme inactivation
For: gram neg aerobic bacilli, very little gram pos
w/ b lactam or vanc for sneitive strep
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Prophylaxis w/ isoniazid
6 months
300 mg adults
900 my 2X week
10mg/kg for kids
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TB w/ Upped level resist, or Disseminating TB, or TB meningitis, or TB w/ AIDS
Isoniazid, rifampin, pyrazinamide, ethambutol
9-12 months or more
At least 2 drugs continue once done susceptibility testing
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Treat TB in Urea, w/ low drug resist, or elderly
Isoniazid and rifampin 6 months and pyrazinamide first 2 months
Or, Iso, rifam, streptomycin for 9 months
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Clofazimine
Alt. to sulfones if dapsone resistant strains or pt is intolerant
M. Leprae
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Dapsone
Similar to sulfonamides most likely inhibits folate synth
Static
For: M. leprae, several years w/ rifampin, must monitor and much support
Bad, hemolysis, methemeglobinemia, GI, allergic
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Rifampin
Binds to DNA dependent RNA poly and inhibits RNA synth in Mycobacteria
Cidal
Also: M. leprae w/ dapsone
Urine and body fluids= orange rash, thrombocytopenia, nephritis, down liver fxn w/ isoniazid
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Streptomycin
- Mostly for extracellular tubercle forms.
- poor cell penetration, crosses BBB
For: iv DRUG W/ LIFE THREATENING meningitis tuberculosis and disseminating Dz
Ototox, nephrotox, CAUTION
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Pyrazinamide
Inactive at neutral pH
Bactericidal at slightly acidic pH
Resist alone but not w/ isoniazid
Impair liver fxn
Used only in combos
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Ethambutol
- Good oral, good CSf
- Fast resistane if alone
Fen adverse
Good for TB, Kansasii, and many atypicals
W/ isoniazid
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Isoniazid
primary for TB
Inhibits synth of mycolic acid
Hits cell wall
Cidal for active growers, static at low dose
Not for atypical Mycos
Good for tuberculosis and Kansasii
Fast and slow acetylator in liver
CNS/PNS- pyridoxal phos deficiency inhibits metab of diphenylhydantoin
Allergic
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Sulfadoxine and pyrinethamine
Sulfadoxine= long acting
Pyrimethamine= parasite dihydrofolate reductase inhibition
For: P. falciparum
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Sulfamethoxazole and Trimethorprim
Gram pos/neg
- Sulfamethoxazole- PABA anolog
- Inhibits dihydropteric acid synth. prevents folic acid
Trimethorprim- inhibits dihydrofolate reductase
Bacteriocidal
For: AIDS pneumocystis, jirovecii in up dose UTI
Parasitic if the combo abose is given
Anemias
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Moxifloxacin
For: low RTI only
May prolong QT, less photo, no inhibit theophylline
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Gemifloxacin
3rd gen once daily
For: community acquired pneumo and bronchitis, PCN-resist Strep pneumo
Rash, inhibits theophylline
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Levofloxacin
3rd gen
Levo or ofloxacin- once daily
For: low RTI, skin, bone, joint, gastroenteritis, GUTI, pen resist strep pneum
Less CNS, no theophylline inhibit
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Lomefloxacin
2nd gen
For: low RTI, skin, bone, joint, gastroenteritis, GUTI
Photosensitivity, NOT inhibit theophylline, CNS, NSAIDS
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Oflxacin
Racemic 2nd gen
for: low RTI, skin, bonde, joint, gastroenteritis, GUTI
CNS stim- anxiety hallucinate,
Theophylline, NSAIDS, insomnia
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Ciprofloxacin
2nd gen fluoroquinolone
More potent gram neg
Better gram pos strep faecalis, staph aureus MRSA
Intracellular
For: low RTI, skin, bone, joint, gastroenteritis, GUTI
Interact w/ theophylline and NSAIDS
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Norfloxacin
oral 1st gen
- For: GUTI, UTI, STD, gonococcus, prostatic-ecoli
- Pseudomonas=resist
inhibits theophylline metab CYP1A2
Crystalluria
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Fluoroquinolones
inhibits DNA gyrase- Topoiso IV and II
Resist: mutate gyrase, down perm,
Quinolones: gram neg only
Flouroquinolones: great gram neg, gram pos, strep paecalis, staph w/ MRSA, intracellular-chlamydia, mycoplasmin, legionella, brucella, mycobacterium
Poor against anaerobes and S. pneumo
Good oral but not w/ Ca2+ and MG2+
GI, photo, CNS, seizure, Connective tiss, endocrine
Not- preggo or young child: Not-antacids, NSAIDS, inhibit theophylline metab
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Misoprostol
Synth. analog of PGE,
PG down acid secreation and Up mucus and up bicarb
ASA down PG synth= ulcer
For: NSAID ulcers
Not: preggo= uterine contract
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Metronidazole
H. pylori w. resistance
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Clarithromycin and amoxicillin
PPI + clarith and amox
or
PPI + bismuth and tetraycline and metronidazole (for resistance)
10-14 days, ulcer cure
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Bismuth subsalycilate
up mucosal secreation
Coats ulcer
Causes H. pylori detachment and lysis
No antacid effect
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Aluminum compounds
Storage issues
Up mucus secreation
Phosphate epletion
bad: binds to tetracycline and constipate
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Calcium carbonate
Potent, good for women (Tums)
CA2+ may produce intense and long HCl rebound
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