Antibiotics Flashcards
Pen G and Pen V:
Route of admin
MOA
Pen G- IV and IM
Pen V- oral
D-ala D-ala analog.
Binds PBP to block transpeptidase cross-linking of peptidoglycan in cell wall. Activate autolytic enzymes.
Clinical use for PenG/PenV (5)
Bactericidal or Bacteriostatic?
Penicillinase Sensitivity?
- S. pneumo
- S. pyogenes
- Actinomyces
- N. meningitidis
- T.pallidum
Bactericidal
Penicillinase sensitive
PenG/PenV
Adverse (2)
Mech of Resistance
- Hypersensitivity (Rash/anaphylaxis)–>Type1 Hypersens
- direct Coombs hemolytic anemia (Haptan)–>Type2 Hypersens
Resistance: Penicillinase in bacteria (B-lactamase) cleaves B-lactam ring between N and C=O
Name 2 penicillinase sensitive penicillins
Aminopenicillins
- Amoxicillin
- Ampicillin
Aminopenicillins (Amoxicillin/Ampicillin)
MOA
MOResistance
Penicillinase Sensitivity?
MOA:
Same as penicillin w/ wider spectrum
Penicilinas (B-lactamase) cleaves B-lactam ring
Penicillinase sensitive–>combine w/ clavulanic acid to protect against destruction by B-lactamase
Typically: Amox w/ sulbactam, Amp w/ clavulanic acid
Aminopenicillins: Clinical Use (8*)
Broad Spectrum "Ampicillin/Amoxicillin HHELPSS kill Enterococci" H.flu H.pylori E.coli Listeria Proteus Salmonella Shigella Enterococci
Aminopenicillins (Amoxicillin/Ampicillin):
Adverse (3)
- Hypersensitivity
- Rash–>not a hypersensitivity (not IgE) but specific for amoxicillin with mononucleosis
- pseudomemb colitis
What contributes to Penicillin’s clinical use
The R group on penicillins determines
- Broad vs. Narrow
- ability of drug to cross Bacterial membrane
Name Penicillinase-resistant penicillins (4)
Why “resistant”?
- Dicloxacillin
- Nafcillin
- Oxacillin
- Methicillin
Bulky -R group blocks B-lactamase’s access to B-lactam ring
Name Penicillinase-resistant penicillins: Clinical Use(1*)
Narrow spectrum
1. S. aureus (Except MRSA-it mutates transpeptidase enzyme gene so drug can’t bind))
“use Naf for Staph”
Name Penicillinase-resistant penicillins:
Adverse (2)
- Hypersensitivity (Rash/anaphylaxis)
2. Interstitial Nephritis (remember Methicillin was taken off market for beating up too many kidneys)
Name Antipseudomonal penicillins (2)
Penicillinase Sensitivity?
- Pipercillin
- Ticarcillin
Penicillinase sensitivity–>use B-lactamase inhibitors
*classically Tazobactam w/ Pipercillin/Ticarcillin
Antipseudomonal penicillins: Clinical Use (2) Adverse (1)
- Pseudo spp.
- Gram (-) rods
* typically with Tazobactam - Hypersensitivity
Why use B-lactamase inhibs?
Name 3* B-lactamase inhibs
Added to penicillin abx to protect abx from penicillinase destruction
“CAST a net to protect Penicillins”
- Clavulanic Acid (w/ Amox)
- Sulbactam (w/ Amp)
- Tazobactam (w/ Pip or Ticar)
Cephalosporins: MOA Bactericidal or Bacteriostatic? Penicillinase Sensitivity? MOResistance
- B-lactam drugs inhib cell wall synthesis
- Bactericidal
- Less susceptible to penicillinase
- Structural change in PBP (transpeptidase)
Cephalosporins:
Organisms typically not covered by 1st-4th generation
“1st-4th Generation cephalosporins are LAME”
- Listeria
- Atypicals (chlamydia/mycoplasma)
- MRSA (covered by ceftaroline-5th gen)
- Enterococci
1st Gen Cephalosporins:
Names (2)
coverage (5)
Any special uses
- Cefazolin-used pre surgery to prevent S.aureus infection
- cephalexin
“PEcK-g”
- gram + cocci
- Proteus
- E.coli
- Klebsiella
2nd Gen Cephalosporins:
Names (3)
Coverage (8)
“FAke FOX FUR”
- CeFOXitin
- CeFAclor
- CeFURoxime
“PEcK-g HENS”
- gram + cocci
- Proteus
- E.coli
- Klebsiella
- H. flu
- Enterobacter aerogenes
- Neisseria
- Serratia marcescens
3rd Gen Cephalosporins:
Names (3)
Coverage (3,1)
Serious gram (-) infections resistant to other B-lactams
- Ceftriaxone- 1. N.meningitids 2. N.gonorrhea 3. Lyme
- Cefotaxime
- Ceftazidine- 1. Pseudo
4th Gen Cephalosporins:
Names (1)
Coverage (3)
Cefepime
- Gram (+)
- Gram (-)
- Pseudo
5th Gen Cephalosporins:
Names (1)
Coverage (3)
Ceftaroline
- Gram (+)
- Gram (-)
- MRSA
Name 2 Cephalosporins that cover Psuedomonas
- Ceftaz (3rd gen)
2. Cefepime (4th gen)
Cephasporins:
Adverse (6)
- Hypersensitivity
- Autoimmune Hemolytic anemia
- Disulfuram-like Rxn
- Vit K def (from killing off enteric bacteria)
- Cross-react w/ penicillins
- Nephrotox w/ Aminoglycosides
Name Carbapenems (4)
Special considerations per drug
- Imipenem
- Meropenem- less Seizure Risk, stable to Dehydropeptidase I
- Ertapenem-new, limited Pseudomonas coverage
- Doripenem-new
Carbapenems:
MOA
Special administration*?
Broad or Narrow
MOA: B-lactamase resistant
- Always admin w/ CILASTATIN (inhib Renal Dehydropeptidase I) to decrease inactivation of drug in Renal tubules
- Broad spectrum
“With imipenem, the kill is LASTIN’ with CILASTATIN”
Carbapenems:
Coverage(3)
When used?
- Gram + cocci
- Gram - rods
- anaerobes
- Wide spectrum but limited use to life-threatening infections or after other drugs fail b/c of significant Adverse
Carbapenems:
Adverse (3)
- Seizures/ CNS tox @ high plasma levels
- GI distress
- Skin rash
Aztreonam (a Monobactam):
MOA
Penicillinase sensitivity
Adverse
Prevents Peptidoglycan cross-linking by binding to PBP-3
- Less susceptible to B-lactamases
- usually non-toxic, occasional GI upset
Aztreonam:
Coverage (1)
3 special uses
Gram - rods
- Penicillin-allergic patients safe
- well-tolerated in renal insuff pt (who can’t use Aminoglycosides)
- Synergistic activity w/ amino glycosides
Vancomycin:
MOA
Penicillinase Sensitivity
Bactericidal or Bacteriostatic
- binds Dala Dala portion of cell wall precursors to prevent peptidoglycan formation
- Not sensitive to penicillinase
- Bactericidal against most (Bacteriostatic for C.Diff)
- bacterial A.A. mutation to Dala Dlac
“Pay back 2Dala’s (dollars) for VANdalizing”
Vancomycin:
Adverse(4)
“Vancomycin is generally well tolerated but NOT trouble free”
- Nephrotox
- Ototox
- Thrombophlebitis
- Red Man Syndrome- pretreat w/ histamines & slow infusion
Bacterial Ribosome subunits
70S (30S, 50S)
Which Abx bind 30S and which bind 50S?
Bactericidal or Bacteriostatic
” Buy AT 30, CCEL (sell) at 50”
30S:
- Aminoglycosides- bactericidal
- Tetracyclines-bacteriostatic
50S:
- Chloramphenicol-bacteriostatic
- Clindamycin-bacteriostatic
- Erythromycin (macrolides)-bacteriostatic
- Linezolid-variable
Name Aminoglycosides (5)*
“MEAN (a-min-oglycoside) GNATS caNNOT kill ANAEROBES.”
- Gentamicin
- Neomycin
- Amikacin
- Tobramycin
- Streptomycin
Aminoglycosides:
MOA(2)*
Special consideration about MOA*
“‘A’ starts the alphabet, ‘A’minoglycosides inhib INITIATION”
- Irreversible inhib initiation–>mRNA misread
- inhib translocation
Require O2 for uptake making them ineffective against anaerobes
“‘Mean’ GNATS caNNOT kill ANAEROBES”
Aminoglycosides: Clinical use (4)
1 . Severe Gram - rod (like Pseudo/E.coli)
- Synergistic w/ B-lactams–> increase response
- Bowel surgery (Neomycin)
- Neonate suspected infections (Gentamycin & Ampicillin)
Aminoglycosides:
Adverse*
“‘Mean’ GNATS caNNOT kill ANAEROBES”
- Nephrotox (worse w/ cephalosporines)
- Neuromuscular blockade
- Ototox (worse w/ Loops)
- Teratogen
Aminoglycosides:
MOResistance
Bacterial transferase enzymes inactivate drug by:
- acetylation
- phosphorylation
- adenylation
Abx’s ending in -mycin (4 groups)
- Aminoglycosides (‘GNAT’)
- Clindamycin
- Macrolides (Azithromycin, Clarithromycin, Erythromycin)
- Daptomycin
Tetracyclines: Tetracycline, Doxycycline, Minocycline
MOA
Bactericidal or Bacteriostatic
MOResistance
Binds 30S –>prevent aminoacyl-tRNA attachment
Bacteriostatic
Plasmid-encoded transport pumps decrease uptake/increase efflux
Tetracyclines: Tetracycline, Doxycycline, Minocycline
CNS penetration
D-D(3)
- limited CNS penetration
- Milk(Ca+2), antacids (Ca/Mg), Fe+-containing preparations: Divalent cations inhib gut drug absorption
Tetracyclines: Tetracycline, Doxycycline, Minocycline
Coverage (5)
Special population use
Atypicals/Intracellular:
- Lyme (borrelia burgdorferi)
- M. pneumo
- RMSF (Rickettsia)
- Clamydia
- Acne
Fecally excreted–>Good for pt w/ Renal Failure
VACUUM THe BedRoom:
Vibreo, acne, chlamydia, ureaplasma, urealyticum, mycoplasma, Tuleremia, H pylori, Borrelia burgdorferi, rickettsia
Tetracyclines: Tetracycline, Doxycycline, Minocycline
Adverse(4)
Contra(2)
- GI distress (fecally excreted)
- Discoloration of Teeth
- Inhib bone growth children (not
Chloramphenicol:
MOA
Bactericidal or Bacteriostatic
MOResistance
Blocks peptidyltransferase of 50S
Bacteriostatic
Plasmid-encoded acetyltransferase inactivates drug
Chloramphenicol: Clinical use(2)
- Meningitis (H.flu/Neisseria/S.pneumo)
2. RMSF (Rickettsia)
Chloramphenicol:
Adverse (3)
(special note)
- Microcytic Anemia (dose dependent)–>*know picture
- Aplastic Anemia (dose independent)
- Gray-Baby syndrome (premature babies lack UDP-glucuronyl transferase–>decrease renal excretion)
*Limited use in USA b/c adverse but still used in developing countries($cheap)
Clindamycin:
MOA
Bactericidal or Bacteriostatic
Block peptide transfer at 50S
Bacteriostatic
Clindamycin: Clinical Use (4)
Treats anaerobic infections above diaphragm
- aspiration pneumo
- lung abscesses
- oral infections
- invasive GAStrep
Aspiration pneumo patients (3)
- alcoholics
- seizures
- Altered mental status
Gray Baby symptoms(4)
Which drug causes this?
- Gray ash-colored skin
- V
- Limp Muscles
- CV collapse
Cloramphenicol- premies lack UDP glucuronyl transferase
Clindamycin:
Adverse (2)
- C.diff-pseudomembranous colitis
2. F/D
Abx to treat Lyme disease (2)
Vector
- Doxycycline
- Ceftriaxone
Ixodes tick
Use of Demeclocycline
MOA
treat SIADH
block V2-R in collecting duct (and bind 30s to prevent attachment of aminoacyl-tRNA)
C.diff causing Abx: (2)
potentially all Abx but the 2 big ones are:
- Clindamycin
- Ampicillin (aminopenicillin)
Linezolid (a Oxazolidinone):
MOA
Bactericidal or Bacteriostatic
MOResistance
Bind 50S and prevent initiation complex formation
Bacteriostatic
rRNA point mutations
Linezolid (a Oxazolidinone):
Clinical Use
Gram + esp. MRSA & VRE
Linezolid (a Oxazolidinone):
Adverse (3)
- BM suppression (esp. thrombocytopenia)
- peripheral neuropathy
- serotonin syndrome
treatment of pt w/ MRSA and kidney disease?
Linezolid (not Vancomycin- Nephrotox)
Macrolides:
Names (3)
- Azithromycin
- Clarithromycin
- Erythromycin
Macrolides:
MOA*
Bactericidal or Bacteriostatic
MOResistance
Bind 23S (of 50S) to block translocation ("macroSLIDES") Bacteriostatic Methylation of 23S
Macrolides: Clinical Use (4)
- Atypical pneumonia (Mycoplasma/Chlamydia/Legionella)
- STI (Chlamydia)
- Gram + Cocci (Strep in penicillin-allergic)
- B. pertussis
Macrolides:
Adverse (5)*
D-D(2)
“MACRO”
- Motility issues (GI)
- Arrhythmia (prolonged QT–>torsades de pointe)
- Cholestatic hepatitis (bile produced in liver/stored in gallbladder)
- Rash
- eOsinophilia
Clarithromycin & Erythromycin INHIB P450–>^serum concentration
- Theophylline
- oral anticoag
Serotonin Syndrome Symp (6) Causative ABx Treatment serotonin precursor molecule
Life threatening!!
- HA
- Aggitation
- Sweating
- muscle twitch
- clonus
- Hallucinations
Abx cause: Linezolid
Tx: stop med
Tryptophan–>serotonin
Sulfonamides:
Name (3)
- Sulfamethoxazole (SMX)
- Sulfisoxazole
- sulfadiazine
Sulfonamides:
MOA
Bactericidal or Bacteriostatic
MOResistance(3)
Competitive Inhib DihyDROPteroate synthase–>inhib folate synthesis
“Don’t DROP the ‘S’oap”
Bacteriostatic (bactericidal w/ Trimethoprim)
- alter dihyDROPteroate synthase
- decrease uptake
- increase PABA (substrate for RXN)
Sulfonamides: Clinical Use(5)
- Gram +
- Gram -
- Nocardia
- Clamydia
- Simple UTI
“SNAP”
Sulphonamides=Nocardia
Actinomyces = Penicillin
Sulfonamides:
Adverse(6)
- Hypersensitivity
- Hemolysis of G6PD def
- Nephrotox (Tubulointerstitial Nephritis)
- Photosensitivity
- Kernicterus (infants)
- Displace drugs from Albumin (esp. warfarin–>must decrease dose)
Drugs causing Photosensitivity(4)
“SAT For PHOTO”
- Sulfonamides
- Amidarone
- Tetracyclines
- 5-FU
Drugs causing Hemolysis in G6PD def (7)
Characteristic cells found on G6PD blood smear?
“Hemolysis IS D PAIN”
- isoniazid
- sulfonamides
- dapsone
- primaquine
- aspirin
- ibuprofen
- nitrofurantoin
Bite cells & Heinz bodies(Hb precipitation)
What is Kernicterus?
Cause in infants?
Why do sulfonamides cause kernicterus?
- Kernicterus is buildup of bilirubin in CNS
- Babies have immature BBB
-Sulfonamides outcompete bilirubin for binding albumin–>increase free bilirubin crosses the immature BBB
Dapsone:
MOA
Clinical Use(2)
Adverse
-inhib DihyDROPteroate synthase(like sulfonamides, differ structure)
- Leprosy(lepromatous/tuberculoid)
- px Pneumocystis jirovecii (PCP)
Hemolysis in G6PD def
Trimethoprim (TMP):
MOA
Bactericidal or Bacteriostatic
Inhib bacterial Dihydrofolate reductase
Bacteriostatic (bactericidal w/ Sulfamethoxazole)
Trimethoprim (TMP): Clinical Use(4 tx, 2 px in immunocompromised)
Combo with Sulfamethoxazole
- UTIs
- Shigella
- Salmonella
- PCP
- PCP
- Toxo
Fluroquinolones:
Names(7)
” -oxacin”
- Ciprofloxacin
- Norfloxacin
- Levofloxacin
- Ofloxacin
- Moxifloxacin
- Gemifloxacin
- Enoxacin
Fluroquinolones:
MOA
Bactericidal or Bacteriostatic
MOResistance(3)
Inhib prokaryotic topoisomerase-II(DNA gyrase) & topo-IV
(topoisomerases break DNA to undo supercoils)
Bactericidal
- Chromosome-encoded mutation in DNA gyrase
- plasmid-mediated resistance
- Efflux pumps
Fluroquinolones:
Clinical Use(3)
Which fluroquinolone loves the Lung?
- Gram - rods UTI & GI (including pseudomonas)
- Neisseria
- some gram +
Levofloxacin “Levo loves the lungs”
-S.pneumo/ H.flu/ Leigenella/ Mycoplasma/ Chlamydia Pneumonia
Fluroquinolones:
Adverse(6)
Contra (2, why)
- GI upset
- Superinfections
- Skin rashes
- HA/dizzy
- leg cramps/myalgias (less common)
- prolong QT interval (some)
Contra:
1. Pregnant/Nursing Moms/ Cartilage Damage
2. >60yo/ pt on prednisone–>Tendonitis or Tendon Rupture
“FluroquinoLONES hurt attachments to your BONES”
Daptomycin:
MOA
Clinical Use (4)
Lipopeptide disrupts cell membrane of Gram + cocci
Severe infections
- S.aureus skin infections (esp MRSA)
- Bacteremia
- Endocarditis
- VRE
Mnemonic for Endocarditis
"FROM JANE" Fever Roth spots Osler nodules Murmur Janeway lesions Anemia Nailbed hemorrhages Emboli
Daptomycin:
Adverse(2)
What can daptomycin not be used for?
- Myopathy
- Rhabdomyolysis (“Dapto causes Rhabdo”)
“Dapto = SurfactNO”
can’t be used for pneumonia b/c avidly binds to and is inactivated by surfactant
Metronidazole:
MOA
Bactericidal or Bacteriostatic
Other organisms Metronidazole can treat?
Forms Toxic Free Radical metabolites in the bacterial cell that damages DNA
Bactericidal
anti-protazoal
Metronidazole: Clinical Use (6- targeting 3 systems)
“GET GAP on the METRO with METRONIDAZOLE”
- GI (Giardia/Enteromoeba)
- Vaginitis (Trichomonas/ Gardnerella vaginalis)
- Entero (Anaerobes (Bacteroides, C. Diff)/h. Pylori (part of triple therapy)
What drug treats anaerobes above the diaphragm?
Below the diaphragm?
Above= Clindamycin Below= Metronidazole
What is the triple therapy for H.pylori?
- PPi
- Metronidazole / amoxicillin
- Clarithromycin
Metronidazole:
Adverse (3)
- Disulfiram-like Rxn
- HA
- Metallic taste (‘METro causes METallic taste”)
Drugs causing Disulfiram-like Rxn (5)
Symptoms
- Metronidazole
- Certain cephalosporins
- Griseofulvin
- Procarbazine
- 1st gen sulfonylureas
Symps: Flushing, Tachycardia, Hypotension
Compare Trichomonas vs. Gardnerella:
- smell
- discharge
- Micro view
- cervix appearance
- Does the partner need treated too?
Trich: Foul smell, green discharge, trich species/WBC, strawberry cervix, YES YOU TREAT PARTNER
Gardnerella:Fish smell, white discharge, Clue cells, NO NEED TO TREAT PARTNER
Compare Giardia vs. Entamoeba:
Giardia: bloating/Gas, Foul smelling fatty diarrhea, typically in campers/hikers (be able to identify species with face)
Entamoeba: BLOODY diarrhea, liver abscess, “anchovy paste exudate”, RUQ pain, flask shaped ulcer
How to treat MRSA?
“Very Dangerous Cocci Loathe Treatment”
- vancomycin (not for renal failure)
- daptomycin
- Ceftaroline
- Linezolid
- Tigecycline
How to treat VRE?
How does resistance develop?
“VRE Doesn’t Quite Like Vancomycin”
- Dalfopristin
- Quinupristin
- Linezolid
Vancomycin resistance: Dala Dala–>Dala Dlac