Antibiotics Flashcards
Types of antibiotics
1 bactericidal
2. Bacteriostatic
Bactericidal antibiotics
Vancomycin Fluoroquinolones Penicillins Aminoglycosides Metronidazole
Very Finely Proficient at Murder
Bacteriostatic antibiotics
Erythromycin Clindamycin Sulfamethoxazole Trimethoprim Tetracycline Chloramphenicol
ECSTaTiC
natural penicillin
narrow spectrum
for streptococcal, pneumococcal, meningococcal infections, syphilis
SE: hypersensitivity, GI disturbances, seizures
RENAL TUBULAR REABSORPTION INHIBITED BY PROBENECID
INACTIVATED BY BETA-LACTAMASE (PENICILLINASE)
Penicillin G (parenteral) Penicillin V (oral)
isoxazolyl penicillin (anti-staphylococcal)
very narrow spectrum
for STAPHYLOCOCCAL INFECTIONS
SE: hypersensitivity, cross allergenicity with other penicillins, GI disturbances, INTERSTITIAL NEPHRITIS, NEUTROPENIA
RESISTANT TO INACTIVATION BY BETA-LACTAMASE (PENICILLINASE)
methicillin (interstitial nephritis)
nafcillin (neutropenia), oxacillin, cloxacillin, dicloxacillin
amino penicillin extended spectrum for HELPSE infections SE: PSEUDOMEMBRANOUS COLITIS, rash INACTIVATED BY BETA-LACTAMASE ENHANCED EFFECT WHEN USED WITH BETA-LACTAMASE INHIBITORS (CLAVULANIC ACID, SULBACTAM) SYNERGISTIC EFFECT WITH GLYCOSIDES
Ampicillin (IV)
Amoxicillin (oral)
anti-pseudomonal penicillin
SE: hypersensitivity, cross-allergenicity, GI disturbances,
INACTIVATED BY BETA-LACTAMASE
ENHANCED EFFECT WHEN USED WITH BETA-LACTAMASE INHIBITORS (CLAVULANIC ACID, SULBACTAM)
SYNERGISTIC EFFECT WITH GLYCOSIDES AGAINST PSEUDOMONAS
Piperacillin
Ticarcillin, Carbenicillin
Beta-Lactamase RESISTANT drugs
- 4th generation cephalosporins
- monobactam (aztreonam)
- isox. benz.
1st gen cephalosporin
gram + coverage
for SURGICAL PROPHYLAXIS, BONE INFECTIONS
SE: hypersensitivity
INCREASES nephrotoxicity of aminoglycosides
cefazolin
cefadroxil, cephalexin, cephalothin, cephapirin, cephradine
which microbes are covered by spectrum of activity of 1st gen cephalosporins?
PEcKs FIRST
Proteus mirabilis
E. Coli
Klebsiella pneumoniae
2nd gen cephalosporin
addded coverage for Haemophilus, Enterobacter, and Neisseria
SE: hypersensitivity, DISULFIRAM REACTION
INCREASES nephrotoxicity of aminoglycosides
cefaclor
cefamandole, cefmetazole, cefonicid, cefuroxime, cefprozil, ceforanide, cefoxitin, cefotetan, loracarbef
DISULFIRAM REACTION: cefamandole, cefotetan
3rd gen cephalosporin
SE: hypersensitivity
SYNERGISTIC EFFECT WITH AMINOGLYCOSIDES
cefoperazone
cefotaxime, ceftazidime, ceftizoxime, ceftriaxone, cefixime, cefpodoxime proxetil, cefdinir, cefditoren pivoxil, ceftibuten, moxalactam
4th gen cephalosporin wide coverage against gram + and gram - bacteria, MRSA SE: hypersensitvity RESISTANT TO BETA-LACTAMASE BROAD GRAM NEG ACTIVITY
cefepime
ceftaroline
carbapanem
wide coverage against gram + and gram - bacteria
SE: hypersensitvity, CNS toxicity (confusion, encephalopathy, SEIZURES)
for SERIOUS LIFE THREATENING INFECTIONS
Imipinem-Cilastatin
Ertapenem, Meropenem, Doripenem
Cilastatin inhibits renal metabolism
Hydrolysis of imipenem by dihydropeptidase
monobactam for GRAM NEG RODS RESISTANT TO BETA LACTAMASE NO CROSS-ALLERGENICITY WITH PENICILLINS NO ACTIVITY AGAINST GRAM POSITIVE BACTERIA OR ANAEROBES
aztreonam
anti-pseudomonal cephalosporins
ceftazidime
cefepime
cefoperazone
beta-lactamase inhibitor
SE: hypersensitivity
usually combined with amoxicillin, ampicillin, piperacillin
clavulanic acid
sulbactam, tazobactam
glycopeptide binds to D-Ala-D-Ala for MRSA, PSEUDOMEMBRANOUS COLITIS SE: Red Man Syndrome, Nephrotoxicity, Ototoxicity for SERIOUS LIFE-THREATENING INFECTIONS
vancomycin
teicoplanin, dalbavancin, telavancin
treatment for Red Man Syndrome
slowing rate of infusion
drugs of last resort
Imipinem Amikacin Meropenem Linezolid Streptogramins Vancomycin
peptide antibiotic
SE: nephrotoxicity
for TOPICAL USE ONLY DUE TO MARKED NEPHROTOXICITY
bacitracin
blocks incorporation of D-Ala into pentapeptide
for DRUG-RESISTANT TB (2ND LINE DRUG)
SE: NEUROTOXICITY (TREMORS, SEIZURES, PSYCHOSIS)
cycloserine
binds to cell membrane causing depolarisation and rapid cell death
for gram + infections (sepsis, endocarditis)
SE: myopathy
inactivated by pulmonary surfactants
daptomycin
inactivates enzyme UDP-acetylglycosamine-3-enolpyruvyltransferase
for uncomplicated UTI
SAFE FOR PREGNANT PATIENTS
fosfomycin
bacterial protein synthesis inhibitors
30s
Aminoglycosides
Tetracyclines
50s Chloramphenicol Erythromycin (macrolides) Linezolid Lincosamides (clindamycin) Streptogramins
broad spectrum bacterial protein synthesis inhibitor
binds 50s subunit
BACTERIOSTATIC
for MENINGITIS
SE: APLASTIC ANEMIA, GRAY BABY SYNDROME
inhibits hepatic drug-metabolising enzymes causing many drug interactions
chloramphenicol
moderate spectrum bacterial protein synthesis inhibitor
macrolide
binds 50s subunit
BACTERIOSTATIC
SE: cholestatic hepatitis, hepatotoxicity, QT prolongation, drug interactions
erythromycin (alternative for penicillin allergic patients)
azithromycin (highest Vd and slowest elimination)
clarithromycin
telithromycin (used for macrolide resistance)
ALL macrolides inhibit CYP450 enzymes EXCEPT for
azithromycin
broad spectrum bacterial protein synthesis inhibitor
tetracycline
binds 30s subunit
BACTERIOSTATIC
for atypical infections (M. pneumoniae, chlamydiae, rickettsiae, and Vibrio)
SE: tooth enamel dysplasia/discoloration, photosensitivity
tetracycline
doxycycline, minocycline (vestibulotoxicity) tigecyline (broadest spectrum and least resistance), demeclocycline
narrow spectrum bacterial protein synthesis inhibitor
lincosamide
binds 50s subunit
BACTERIOSTATIC
for ANAEROBIC INFECTIONS
SE: PSEUDOMEMBRANOUS COLITIS (C. difficile overgrowth)
clindamycin
lincomycin
cross-resistance between clindamycin and macrolides is common
narrow spectrum bacterial protein synthesis inhibitor
streptogramin
binds 50s subunit
BACTERICIDAL
for MRSA, VRSA, VRE
SE: arthralgia-myalgia syndrome
INHIBITS CYP450 ENZYMES causing multiple drug interactions
quinupristin-dalfopristin
narrow spectrum bacterial protein synthesis inhibitor oxazolidinone binds to 23s of 50s subunit BACTERIOSTATIC for MRSA, VRSA, VRE
linezolid
post-antibiotic effect of aminoglycosides
killing action continues when plasma levels have declined below measurable levels
greater efficacy when administered as single large dose
pharmacokinetics of aminoglycosides
not absorbed after oral administration
limited tissue perfusion
glomerular filtration is major mode of excretion
aminoglycoside
binds to 30s subunit
BACTERICIDAL
SE: nephrotoxicity (reversible), ototoxicity (irreversible)
synergistic effects with beta-lactam antibiotics and vancomycin
gentamicin
tobramycin
most vestibulotoxic and nephrotoxic aminoglycosides
aminoglycoside
binds to 30s subunit
BACTERICIDAL
for PSEUDOMONAS, MDR-TB (2ND LINE DRUG)
SE: nephrotoxicity (reversible), ototoxicity (irreversible)
synergistic effects with beta-lactam antibiotics
LEAST RESISTANCE BUT NARROWEST THERAPEUTIC WINDOW
amikacin
aminoglycoside binds to 30s subunit BACTERICIDAL for TB SE: nephrotoxicity (reversible), ototoxicity (irreversible), CONGENITAL DEAFNESS synergistic with beta-lactam antibiotics administered IM
streptomycin
aminoglycoside
binds to 30s subunit
BACTERICIDAL
for BOWEL PREP FOR ELECTIVE SURGERY, HEPATIC ENCEPHALOPATHY
SE: nephrotoxicity (reversible), ototoxicity (irreversible), NEUROMUSCULAR BLOCKADE
limited to TOPICAL AND ORAL USE
neomycin
kanamycin (most ototoxic), paromomycin
reverses neuromuscular blockade sec to aminoglycosides
gluconate and neostigmine
most ototoxic aminoglycosides
kanamycin, amikacin
most vestibulotoxic aminoglycosides
tobramycin, gentamicin
most nephrotoxic aminoglycosides
tobramycin, gentamicin
skin reactions common with which aminoglycosides
neomycin and streptomycin
nucleic acid synthesis inhibitors
anti-folate sulfonamide
BACTERIOSTATIC
for BURN INFECTIONS
SE: ACUTE HEMOLYSIS IN G6PD DEFICIENCY, HYPERSENSITIVITY, KERNICTERUS
displaces protein blinding of other drugs/bilirubin
silver sulfadiazine
mafenide acetate
nucleic acid synthesis inhibitors
anti-folate sulfonamide
BACTERICIDAL
seuqential BLOCKADE OF DIHYDROFOLATE SYNTHASE & REDUCTASE
for UTI, PCP
SE: ACUTE HEMOLYSIS IN G6PD DEFICIENCY, HYPERSENSITIVITY, KERNICTERUS
displaces protein blinding of other drugs/bilirubin
co-trimoxazole
antibiotic for anaerobic infections above diaphragm vs. below diaphragm
clindamycin: above diaphragm
metronidazole: below diaphragm
long-acting sulfonamide
sulfadoxine
DOC for toxoplasmosis
2nd line for malaria
sulfadoxine-pyrimethamine
co-administered with leucovorin to limit bone marrow toxicity
pyrimethamine
aminoglycoside
binds to 30s subunit
BACTERICIDAL
for DRUG RESISTANT GONORRHEA, GONORRHEA IN PENICILLIN-ALLERGIC PATIENTS
SE: nephrotoxicity (reversible), ototoxicity (Irreversibl), anemia
spectinomycin
generation of fluoroquinolones that is NOT fluorinated
1st gen: for UTI
nalidixic acid, cinoxacin, rosoxacin, oxolinic acid
2nd gen fluoroquinolone
inhibits DNA replication
BACTERICIDAL
for UTI, ATYPICAL PNEUMONIA, TB (2ND LINE DRUG)
SE: GI DISTRESS, TENDONITIS, TENDON RUPTURE
AVOID USING IN YOUNG CHILDREN & PREGNANT WOMEN (chelates Ca)
ciprofloxacin
ofloxacin, norfloxacin, lomefloxacin, enoxacin
DOC for UTI
ciprofloxacin
3rd gen fluoroquinolone
inhibits DNA replication
BACTERICIDAL
for LUNG INFECTIONS by gram + cocci, ATYPICAL PNEUMONIA
SE: GI distress, TENDINITIS, QT PROLONGATION
AVOID USING IN YOUNG CHILDREN & PREGNANT WOMEN
levofloxacin
sparfloxacin, moxifloxacin, gemifloxacin
enhances toxicity of methylxanthines (theophylline)
grepafloxacin withdrawn due to severe cardiotoxicity (arrhythmias)
gatifloxacin SE: DM
4th gen fluoroquinolone
inhibits DNA replication
BACTERICIDAL
ENHANCED ACTIVITY AGAINST ANAEROBES
SE: GI distress, TENDINITIS, QTc prolongation, hepatotoxicity
AVOID USING IN YOUNG CHILDREN & PREGNANT WOMEN
enhances toxicity of methylxanthines (theophylline)
WIDEST SPECTRUM OF ACTIVITY AMONG FLUOROQUINOLONES
trovafloxacin
alatrofloxacin
nitroimidazole, anti-protozoal
reactive reduction by ferredoxin FORMING FREE RADICALS THAT DISRUPT ETC
BACTERICIDAL
for ANAEROBIC infections, VAGINITIS, PSEUDOMEMBRANOUS COLITIS
SE: GI irritation, metallic taste, DISULFIRAM REACTION
metromidazole
tinidazole
disrupts protein, RNA, DNA synthesis
BACTERICIDAL
for UNCOMPLICATED UTI (except PROTEUS and PSEUDOMONAS)
SE: skin rashes, PULMONARY FIBROSIS & INFILTRATES
nitrofurantoin
topical anti-infective
pseudomonic acid
BACTERICIDAL
for GRAM + COCCI, minor skin infections
mupirocin
cationic detergents BACTERICIDAL for GRAM - bacteria proteus and neisseria resistant TOPICAL USE ONLY
polymyxin B
polymyxin E
macrocyclic, narrow spectrum inhibits bacterial protein synthesis BACTERIOSTATIC GRAM + bacteria ORPHAN DRUG STATUS FOR C. DIFFICILE IN CHILDREN
fidaxomicin
