FA Antibiotics Flashcards
Penicillin G
IV
Penicillin V
Oral
Penicillin MOA
Bind PBPs, inhibit transpeptidase cross-linking of peptidoglycan, activate autolytic enzymes
Penicillin Clinical Use
SASS: S. pneumo, Actinomyces, S. pyogenes, Syphilis
Generally: Bactericidal for GramPos/Neg cocci, GramPos rods, spirochetes
Penicillin Toxicity
HS, hemolytic anemia
Penicillin Resistance
Beta-lactamase cleavage of beta-lactam ring
Aminopenicillin Drugs
Amoxicillin, Ampicillin
Aminopenicillin MOA
Bind PBPs, inhibit transpeptidase cross-linking of peptidoglycan, activate autolytic enzymes Wider spectrum (AMPed up penicillins)
Aminopenicillin Clinical Use
Wider spectrum –> HHELLPS kill enterococi: H. flu, H. pylori, E. coli, Listeria, Proteus, Shigella, Salmonella, enterococci
Aminopenicillin with better oral bioavailability
AmOxicillin
Aminopenicillin Toxicity
HS, Amp Rash, Pseudomembranous Colitis
Aminopenicillin Resistance
Beta-lactamase cleavage of beta-lactam ring
Penicillinase-Resistant Penicillin Drugs
Dicloxacillin, Nafcillin, Oxacillin, Methicillin
Penicillinase-Resistant Penicillin MOA
Bind PBPs, inhibit transpeptidase cross-linking of peptidoglycan, activate autolytic enzymes
Narrower-spectrum
Bulky R-group prevents beta-lactamase access to ring
Penicillinase-Resistant Penicillin Clinical Use
S. aureus (not MRSA)
Antipseudomonal Penicillin Drugs
Ticarcillin, Piperacillin (+ beta-lactamase inhibitor)
Antipseudomonal Penicillin MOA
Bind PBPs, inhibit transpeptidase cross-linking of peptidoglycan, activate autolytic enzymes
Extended spectrum
Susceptible to beta-lactamases
Antipseudomonal Penicillin Clinical Use
Pseudomonas, GramNeg Rods
Antipseudomonal Penicillin Toxicity
HS
Beta-lactamase inhibitors
Clavulanic Acid, Sulbactam, Tazobactam
Cephalosporin MOA
Bind PBPs, inhibit transpeptidase cross-linking of peptidoglycan, activate autolytic enzymes
Less susceptible to beta-lactamases
Bactericidal
Cephalosporin Toxicity
HS, autoimmune hemolytic anemia, disulfiram-like rxn w/EtOH, Vit K deficiency
Cross-reactive w/penicillins
Increase nephrotoxicity of Aminoglycosides
Cephalosporin Resistance
structural change in PBPs (transpeptidases)
These drugs can cause a disulfiram-like reaction with alcohol
Metronidazole, Cephalosporins
1st Gen Cephalosporin Drugs
Lin, Lex: Cefazolin, Cefalexin
1st Gen Cephalosporin Clinical Use
PEcK: Proteus, E. coli, Klebsiella
2nd Gen Cephalosporin Drugs
Fake Fox Fur: Cefaclor, Cefoxitin, Cefuroxime
2nd Gen Cephalosporin Clinical Use
HEN PEcKS: H. flu, Enterobacter, Neisseria, Proteus, E. coli, Klebsiella, Serratia
3rd Gen Cephalosporin Drugs
Tri, Tax, Taz: Ceftriaxone, Cefotaxime, Ceftazidime
3rd Gen Cephalosporin Clinical Use
Triax: Meningitis, Gonorrhea, disseminated Lyme
Taz: Pseudomonas
4th Gen Cephalosporin Drugs
Cefepime
4th Gen Cephalosporin Clinical Use
Pseudomonas, GramNeg, additional GramPos activity
5th Gen Cephalosporin Drugs
Ceftaroline
5th Gen Cephalosporin Clinical Use
MRSA, broad GramPos and GramNeg coverage (not Pseudomonas)
These antibiotics are relatively safe in pregnancy
Beta-lactams, Azithromycin, Clindamycin, Metronidazole
These antibiotics can be used against Pseudomonas
Aminoglycosides (GNATS), Aztreonam, Carbapenems, Cefepime, Ceftazidime, Fluoroquinolones, Ticarcillin/Piperacillin, Colistin and Ploymixin B (MDR Strains)
Carbapenem Drugs
Imipenem, Meropenem, Ertapenem, Doripenem
Carbapenem MOA
Bind PBPs, inhibit transpeptidase cross-linking of peptidoglycan, activate autolytic enzymes
Broad spectrum
Beta-lactamase resistant
Imipenem always + cilistatin to reduce inactivation by dihydropeptidase I in renal tubules
Carbapenem Clinical Use
GramPos Cocci, GramNeg Rods, Anaerobes
Imipenem always adminstered with what, and why?
Cilastatin to reduce inactivation by dihydropeptidase I in renal tubules
These drugs can be given to a pt w/penicillin allergy
Monobactams, Macrolides, Clindamycin
Carbapenem Toxicity
CNS toxicity (seizures), GI distress, skin rash
Monobactam drugs
Aztreonam
Monobactam MOA
Bind PBP3, inhibit transpeptidase cross-linking of peptidoglycan, activate autolytic enzymes
Less susceptible to beta-lactamases
Synergistic w/aminoglycosides
No cross-allergicity w/penicillins
Monobactam Clinical Use
GramNeg rods ONLY
These drugs can be used in pts w/renal insufficiency instead of aminoglycosides
Monobactams (Aztreonam)
These drugs are less susceptible to beta-lactamases
Monobactams,
These drugs are beta-lactamase resistant
Carbapenems, Vancomycin, Cephalosporins, Penicillinase-Resistant Penicillins
These drugs should be administered with beta-lactamase inhibitors
Penicillin, Aminopenicillins, Antipseudomonal Penicillins
Monobactam Toxicity
usually nontoxic; occasional GI upset
Vancomycin MOA
binds D-ala-D-ala to inhibit cell wall elongation
Bactericidal
Beta-lactamase resistant
Vancomycin Clinical Use
MRSA, Staph epi, Enterococcus, C. diff
Vancomycin Toxicity
“Red Man’s NOT in the Van”: Red Man Syndrome (antihistamines), Nephrotoxicity, Ototoxicity, Thrombophlebitis
Vancomycin Resistance
amino acid modification of D-ala-D-ala to D-ala-D-lac
This carbapenem has decreased risk of seizures and is stable to dihydropeptidase I in renal tubules
Merepenem
These bugs are NOT covered by Cephalosporins
LAME: Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA (except 5th gen), Enterococci
These drugs bind to 30S subunit to inhibit protein synthesis
“Ami has 30 Tetras”: Aminoglycosides, Tetracyclines
These drugs bind to 50S subunit to inhibit protein synthesis
“CCEL at 50”: Chloramphenicol, Clindamycin, Erythromycin (Macrolides), Linezolid
Aminoglycoside Drugs
GNATS: Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin
Aminoglycoside MOA
Bind 30S subunit –> misreading of mRNA, blockage of translocation
Bacteriocidal
Require O2 for uptake (Amin”O2”glycosides)
Aminoglycoside Clinical Use
Severe GramNeg Rod infxns (Ami”NOT”glycoside)
Synergistic w/Beta-lactams
Bowel sterilization for Sx (neomycin)
These drugs are synergistic w/Beta-lactams
Aminoglycosides
This drug is used for bowel sterilization pre-Sx
Neomycin
This aminoglycoside is hepatically excreted
Amikacin
Aminoglycoside Toxicity
“caNNOT kill anaerobes:” Nephrotoxicity, NMJ blockade, Ototoxicity (esp. w/loop diuretics), Teratogen
Aminoglycoside mnemonic
Mean GNATS caNNOT kill anaerobes
Aminoglycoside Resistance
Bacterial tranferase enzymes inactivate via APA: Adenylation, Phosphorylation, Adenylation
Tetracycline Drugs
Tetracycline, Doxycycline, Minocycline, Demeclocycline, Tygecycline
Tetracycline MOA
T’s: Bind to 30S (Thirty) subunit –> prevent tRNA attachment
Accumulate intracellularly
Limited CNS penetration
Ca2+, Mg2+, Fe2+ decrease absorption in gut
This tetracycline is hepatically eliminated
Doxycycline
This tetracycline is commonly used for acne
Minocycline
This tetracycline can be used as a diuretic in SIADH
Demeclocycline
These products inhibit tetracycline absorption
Ca2+, Mg2+, Fe2+
Tetracycline Clinical Use
Borrelia burgdorferi, M. pneumoniae, Rickettsia, Chlamydia, acne
Tetracycline Toxicity
Tummy (GI distress), can’t get Taller (inhibition of bone growth in kids), Tooth discoloration, Teratogenic
Tetracycline Resistance
decreased uptake or increased efflux via plasmid-encoded transport pumps
Chloramphenicol MOA
Blocks peptidyltransferase at 50S subunit
Bacteriostatic
Chloramphenicol Clinical Use
Meningitis (H. flu, N. meningitidis, S, pneumo), Rocky Mtn Spotted Fever (Rickettsia)
Chloramphenicol Toxicity
Dose-dependent anemia, dose-independent aplastic anemia, gray baby syndrome
What is gray baby syndrome and what causes it?
Chloramphenicol –> Vomiting, Ashen gray skin color, Limp body tone, HypOtension, Cyanosis, Hypothermia, Cardiovascular collapse
Chloramphenicol Resistance
Plasmid-encoded acetyltransferase inactivates drug
Clindamycin mnemonic
Clindamycin Cleans Up Anaerobes (anaerobic infxns above diaphragm)
Clindamycin MOA
Blocks translocation (peptide transfer) at 50S subunit Bacteriostatic
Clindamycin Clinical Use
Anaerobic infxns (Bacteroides, C. perfringens) in aspiration pneumonia, lung abscesses, oral infxns; invasive Strep pyogenes infxn
Clindamycin Toxicity
Pseudomembranous colitis from superinfxn (C. diff overgrowth) (primary cause), fever, diarrhea
Oxazolidinone Drugs
Linezolid
Linezolid MOA
Binds 50S subunit and blocks Initiation Complex formation
Linezolid Clinical Use
GramPos, incl. MRSA and VRE
Linezolid Toxicity
Bone marrow suppression (esp thrombocytopenia), peripheral neuropathy, serotonin syndrome
What is serotonin syndrome and what antibiotic causes it?
Linezolid –> excessive accumulation of serotonin –> symptoms can range from mild (shivering and diarrhea) to severe (muscle rigidity, fever and seizures)
These drugs can suppress bone marrow
Linezolid, TMP
Linezolid Resistance
rRNA point mutation
Macrolide Drugs
ACE: Azithromycin, Clarithromycin, Erythromycin
Macrolide MOA
Binds to 23S rRNA of 50S subunit –> blocks translocation (macro”slide”)
Bacteriostatic
Macrolide Clinical Use
Atypical pneumonia (Mycoplasma, Chlamydia, Legionella), STIs (Chlamydia), GramPos Cocci (Strep in pts w/penicillin allergy), B. pertussis
Macrolide Toxicity
MACRO: Increased GI Motility, Arrhythmia from prolonged QT interval, acute Cholestatic hepatitis, Rash, eOsiniphilia
Increases serum conc of theophyllines and oral anticoagulants
Erythro and Clarithro inhibit P450
Macrolide Resistance
Methylation of 23S rRNA-binding site
Trimethoprim MOA
Inhibits bacterial Dihydrofolate Reductase (folate synthesis)
Bacteriostatic
Trimethoprim Clinical Use
Used w/SMX to cause sequential block of folate synthesis (bactericidal) – UTIs, Shigella, Salmonella, Pneumo jirovecii, Pneumonia Rx and prophylaxis, toxoplasmosis prophylaxis
Trimethoprim Toxicity
Treats Marrow Poorly: Megaloblastic anemia, leukopenia, granulocytopenia (alleviate w/folinic acid)
Sulfonamide MOA
PABA metabolites inhibit dihydropterate synthase (folate synthesis)
Bacteriostatic
Sulfonamide Clinical Use
GramPos, GramNeg, Nocardia, Chlamydia, simple UTI (triple sulfas or SMX)
Sulfonamide Toxicity
HS, Hemolysis in G6PDH Def, Nephrotoxicity (tubulointerstitial nephritis), Photosensitivity, Kernicterus in infants, displaces other drugs from albumin (warfarin), Stevens-Johnson Syndrome
Sulfonamide Resistance
Altered enzyme, decreased uptake, or increased PABA synthesis
TMP-SMX Toxicity
Stevens-Johnson Syndrome (mostly SMX)
TMP-SMX MOA
Sequential inhibition of folate synthesis
TMP-SMX Clinical Use
PUSS: Pneumo jirovecii, UTIs, Shigella, Salmonella
Fluoroquinolone Drugs
Ciprofloxacin, Levofloxacin, Moxifloxacin
Fluoroquinolone MOA
inhibit DNA Topoisomerase I (DNA Gyrase) and DNA Topoisomerase IV
Bactericidal
Cannot be taken w/antacids
These antibiotics cannot be taken with antacids
Fluoroquinolones, Tetracyclines
Fluoroquinolone Clinical Use
GramNeg Rods in urinary and GI tracts; Pseudomonas, Atypical pneumonia (Levo, Moxi), Neisseria, some GramPos organisms
Fluoroquinolone Toxicity
Superinfection, Tendon Rupture, GI upset, may prolong QT interval, skin rash, headache, dizziness
C/I in pregnancy, nursing, kids under 18 (cartilage damage)
“Quinolones hurt attachments to Bones”
Fluoroquinolone Resistance
Chromosome-encoded mutation in DNA gyrase; plasmid-mediated resistance; efflux pumps
Daptomycin MOA
Lipopeptide that disrupts cell membrane of GramPos cocci
Daptomycin Clinical Use
S. aureus skin infxns (esp. MRSA), bacteremia, endocarditis, VRE – NOT used for pneumonia (inactivated by surfactant)
Daptomycin toxicity
Myopathy, rhabdomyolysis
Metronidazole MOA
Forms toxic free radical metabolites that damage bacterial DNA
Bactericidal, antiprotozoal
Metronidazole Clinical Use
GET GAP on the Underground Metro: anaerobes below diaphragm: Giardia, Entamoeba, Trichomonas, Gardenerella, Anaerobes (Bacteroides, C. diff), H. Pylori (w/PPI and Clarithromycin)
These 2 antibiotics are used in “triple therapy” w/PPI to treat H. pylori
Clarithromycin, Metronidazole
Metronidazole Toxicity
Disulfiram-like rxn w/EtOH, headache, dysgeusia
Disulfiram-like reaction
severe flushing, tachycardia, hypotension
These antibiotics should be avoided in pregnancy
SAFe Children Take Really Good Care: Sulfonamides, Aminoglycosides, Fluoroquinolones, Clarithromycin, Tetracyclines, Ribavirin (antiviral), Griseofulvin (antifungal), Chloramphenicol
post-antibiotic effect
persistent suppression of bacterial growth after a brief exposure (1 or 2 hours) of bacteria to an antibiotic even in the absence of host defense mechanisms
this antibiotic exhibits post-antibiotic effect
Azithromycin
These drugs can be used against MRSA
Vancomycin, Linezolid, Daptomycin, Tigecycline, Ceftaroline
These drugs can be used against VRE
Linezolid, Tigecycline, Daptomycin
These drugs can be used against anaerobes
Clindamycin (above diaphragm), Metronidazole (below diaphragm), Tigecycline, Cefoxitine, Zosyn (Piperacillin + Tazobactam), Respiratory Fluoroquinolones (Moxi > Levo), Carbapenems
These drugs can be used against Atypical Pneumonia (Legionella, Mycoplasma, Chlamydia)
Macrolides, Tetracyclines, Moxifloxacin, Levofloxacin
These drugs can be used for UTIs
TMP-SMX, Fluoroquinolones, Fosfomycin (if the others don’t work)
These drugs can be used for outdoor diseases (Borrelia Lyme Disease/Ricksietta Rocky Mtn/Y. pestis Plague)
Tetracyclines, Ceftriaxone (Lyme)
These drugs can be used for Chlamydia
Macrolides
These drugs can be used for Syphilis
Penicillin G
These drugs can be used for Gonorrhea
Ceftriaxone
These drugs can be used for MDR Pseudomonas
Polymixins B/E (Colistin)
These drugs can be used for Hepatic encephalopathy
Neomycin
These drugs can be used for Anthrax
Doxycycline, Fluoroquinolones
These drugs can cause pseudomembranous colitis (superinfxn)
Clindamycin, Tetracyclines, Aminopenicillins (Treat w/Vanco, Metronidazole)
These drugs can cause ototoxicity
Aminoglycosides (esp w/loop diuretics), Vancomycin
These drugs can cause myopathy
Daptomycin
These drugs can cause tendon rupture and cartilage damage
Fluoroquinolones
These drugs are motilin agonists that can cause severe diarrhea
Macrolides (ACE)
These drugs can cause NMJ blockade
Aminoglycosides (GNATS)
These drugs can cause seizures
Carbapenems, Isoniazid
This drug can cause Red Man Syndrome
Vancomycin
These drugs can cause bone marrow suppression
TMP, Linezolid
These drugs can cause kernicterus
Sulfonamides
These drugs can cause hemolysis in G6PDH deficiency
Sulfonamides
These drugs can cause Vit B6 deficiency / peripheral neuropathy
Isoniazid
These drugs can cause Vit K deficiency
Cephalosporins
These drugs can cause nephrotoxicity
Aminoglycosides, Vancomycin, Sulfonamides
These drugs can cause optic neuropathy / red-green colorblindness
Ethambutol (“Eye”-thambutol)
These drugs can cause megaloblastic anemia
Trimethoprim
These drugs can cause red-orange body fluids
Rifampin
These drugs can cause hyperuricemia
Pyrazinamide
These drugs can cause aplastic anemia
Chloramphenicol
These drugs can cause hepatotoxicity
Isoniazid, Pyrazinamide
These drugs can cause acute cholestatic hepatitis
Erythromycin
These drugs are P450 2C9 inhibitors
Sulfonamides, Metronidazole
These drugs are P450 2C9 inducers
Rifampin
These drugs are P450 inhibitors
Isoniazid, Clarithromycin and Erythromycin (NOT Azithromycin), Ciprofloxacin
Rifampin MOA
Inhibits DNA-dependent RNA Polymerase
Rifampin Clinical Use
Mycobacterium tuberculosis; delay resistance to Dapsone in leprosy; prophylaxis for close contacts of kids with HiB meningitis
Rifampin Toxicity
Minor hepatotoxicity, P450 inducer (drug interaxns), Red-Orange body fluids
Rifamycin Drugs
Rifampin, Rifabutin
Which rifamycin is preferred in HIV and why?
Rifabutin b/c less P450 stimulation
Rifampin Resistance
Mutations reduce drug binding to RNA Pol
Monotherapy rapidly leads to resistance
4 R’s of Rifampin
DNA-dependent RNA Polymerase
Ramps up P450
Red-orange body fluids
Rapid Resistance when used alone
These drugs are used for active TB
RIPE for treatment: Rifampin, INH, Pyrazinamide, Ethambutol
These drugs are used for latent TB
Rifampin, INH
Isoniazid MOA
decrease Mycolic Acid synthesis
requires bacterial KatG (catalase-peroxidase) for activation
Isoniazid Clinical Use
Mycobacterium tuberculosis – only agent used as solo prophylaxis
This drug is the only agent used as solo prophylaxis against TB
Isoniazid
Isoniazid Toxicity
Neurotoxicity (B6 deficiency – peripheral neuropathy – treat w/pyridoxine), hepatotoxicity
Isoniazid Resistance
Mutations causing underexpression of KatG
Pyrazinamide MOA
Uncertain – somehow converted to active cpd pyrazinoic acid
Pyrazinamide Clinical Use
Mycobacterium tuberculosis
Pyrazinamide Toxicity
Hyperuricemia, hepatotoxicity
Ethambutol MOA
inhibits arabinosyltransferase –> decreases carbohydrate polymerization of cell wall
Ethambutol Clinical Use
Mycobacterium tuberculosis
Ethambutol Toxicity
Optic neuropathy, Red-Green colorblindness (“Eye”-thambutol)
This drug is used as prophylaxis for endocarditis, Sx/dental procedures
Amoxicillin
This drug is used as prophylaxis for gonorrhea
Ceftriaxone
This drug is used as prophylaxis for recurrent UTIs
TMP-SMX
This drug is used as prophylaxis for meningococcal exposure
Ceftriaxone, Ciprofloxacin, or Rifampin
This drug is used as prophylaxis for pregant women w/Group B Strep
Penicillin G
This drug is used as prophylaxis for gonorrheal conjunctivitis in newborn
Erythromycin ointment
This drug is used as prophylaxis for post-Sx Staph aureus infxn
Cefazolin
This drug is used as prophylaxis for Strep pharyngitis in kids w/Hx Rheumatic Fever
Benzathine Penicillin G or Oral Penicillin V
This drug is used as prophylaxis for syphilis
Benzathine Penicillin G
What gene is implicated in MRSA strains?
MecA codes for new PBP2a
Which carbapenem has best activity against Pseudomonas?
Doripenem
What drug can be used to treat C. diff?
ORAL Vancomycin, Metronidazole
Which tetracycline is used for antibiotic-resistant infections?
Tygecycline (broad spectrum)
Antibiotic for Staph skin infxn?
Mupirocin (can also eliminate nasal carriage)
These drugs These agents may compete with penicillin for renal tubular secretion, prolonging the half-life of penicillin
Aspirin, furosemide, indomethacin, sulfonamides, thiazide diuretics