Antimicrobials Flashcards
Which antibiotic affect cell wall synthesis? (general FAMILIES, and the “other” ones )
Beta-lactam, Bacitracin, Vancomycin, Cycloserine, isoniazid, ethambutol, ethionamide
Beta lactam antibiotics
- Mechanism of action
- Weakness? (ie: if a bacteria has this it might survive)
- Uses
- Types
- Mechanism: inhibit transpeptidation (final crosslinking step in peptidoglycan synthesis inhibited) and activate autolytic enzymes
- Weakness: beta-lactamases, anything without PBP (penicilling binding protein) and bacteria with autolysin inhibitors.
- Used in combination with beta lactamase inhibitors
- Penicillins, cephalosporins, monobactams, carbapenems, aztreonam, Imipenem
B-lactam side effects
Allergies:
- pen>ceph>mono
Toxicity:
- carba (seizures)>ceph (thrombophlebitis) >pen >mono
Natural Penicillin (G or V)
- Mechanism
- used against?
- V is stable against?
- Inhibits transpeptidase (beta-lactam antibiotic)
- gram + bacteria
- Pen V is acid resistant
Penicillins that are resistant to beta-lactamase
Nafcillin, oxacillin, cloxacillin
(Naf for Staph)
These penicillins can **work on gram(+) and gram(-) **!
- called **expanded spectrum **
- Ampicillin (amino penicillin), piperacillin, mezlocillin, tiracillin
- Tiracillin battles pseudonomas
these penicillins are acid resistant
- Amoxycillin (amino-penicillin), Pen V (natural), oxacillin
Common penicillin + beta lactamase drug combos
- **augmentin= **amoxicillin + clavulanic acid
- Ampicillin + sulbactam
- Zosyn, Tazomed= piperacillin + tazobactam
Penicillin vs cephalosporin?
Cephalosporine are less sensitive to beta-lactamases
Cephalosporins- First generation
- What kind of antibiotic is this?
- Effective against?
- Types?
- Beta-lactam
- gram+ bacteria for prophylaxis only because bacteria readily develop resistance to it
- cephalexin, cephalothin, cefazolin
Cephalosporins- Second generation
- What kind of antibiotic is this?
- Effective against?
- Types?
- beta lactam
- Gram (+), gram (-), bacteroides, NOT PSEUDOMONAS, increased resistance to b-lacatamase
- cefaclor, cefuroxime, cefoxitin
Cephalosporins- 3rd generation
- What kind of antibiotic is this?
- Effective against?
- Types?
- Why is this so special?
- beta-lactam
- gram+, gram-, pseudomonas, MRSA, VRE (vancomycin resistent enterococci)
- ceftazimid, cephotaxime, cephtriaxone, cefdinir
- broadest spectrum of activity, crosses BBB
Cephalosporins- 4th generation
- MOA
- effective against
- types?
- beta-lactam
- G+ and G-, broadest of 5 generations
- Cefepime
Cephalosporin 5th Generation
- MOA
- used against?
- types?
- beta-lactam
- MRSA, drug resistant S Pnemoniae, NOT PSEUDMONOMS
- ceftaroline
Monobactams
- mechanism?
- Effective against?
- types?
- Resistant to?
- Beta lactam (inhibits transpeptidase and activates autolytic enzymes)
- Gram (-) ONLY (not against G+ or anaerobes)
- aztreoname
- Fully resistant to b-lactamases
Carbaoenems
- Mechanism of action
- Effective against
- types
- Down-side?
- beta-lactam
- broad spectrum G+ and G-
- imipenem, ertapenem, meropenem (less toxic)
- toxic
pen=pan= broad spectrum
penem= “pen him!” = kill him = it’s toxic —-I’m trying :-/
Bacitracin
- Mechanism of action
- Used on?
- Side effects
- structural feature we should know?
- blocks bactoprenol dephosphorylation
- topical on G+ with other drugs
- poorly absorbed, renal toxicity
- LARGE!!! cannot cross G- membrane, poorly absorbed
Glycopeptides Antibiotics
- MOA
- Weak against
- Used for?
- Types
- What should be know about shape?
- binds the end of the aa chain to block transglycosylation and transpeptidation
- VanA plasmid and VanB chromosome-use ala-lactate instead of ala-ala
- resistant staph, staphylococci, enterococci, NOT G- BACTERIA
- Vancomycin, Telavancin,
- Large- given via IV because can’t be absorbed by GI tract. Also won’t go into gram- bacteria
Cycloserine
- MOA
- Uses
- What else should we know?
- D-ala analog- inhibits alanine racemase
- sometimes for UTI, 2nd line drug for TB.
- neurtoxic, use carefully
We kill the cell membrane.
Polymyxins (colistin) and daptomycin (cubcin)
THIS MEANS THEY CAN AFFECT OUR HUMAN MEMBRANES TOO!
Polymyxin
- MOA
- Uses
- Type
- dissolves PE in G- membranes. We have PE too.
- Toxic. Used topically or as last resort for resistant bugs
- Colistin
Daptomycin
- MOA
- Uses
- Types
- cyclic lipopeptide that dissolves in the membrane and disrupts membrane potential
- G+ cocci, MRSA- given IV with B-lactams
- Cubicin
Antimetabolites
- MOA
- Weak against
- Used agaonst
- types
- inhibit PABA, DHF, THF, Pyrimidines =inhibition of protein/nucelic acid synthesis. I guess PABA gets incorporated into DHP?
- Things that make tons of PABA
- Nocardia. Synergistic with TMP and SMX for UTI, salmonella, shigella.
Trimethoprin
- MOA
- part of what group of antibiotics?
- Inhibits dihydrofolate reductase= no folic acid
- part of the antimetbolics antibiotics
Sulfoamides
- MOA
- types
- anything else?
- Inhibits PABA into dihydropteroic acid= inhibition of folic acid synthesis
- sulfmethaxozole, dapsone
- most common drug that causes erythema multiforme
Nucleic acid inhibitors- families?
- Fluoroquinolones
- Fidaxomycin
- Rifamycin
- Metronidazole
(Fluoro)quinolones
- MOA
- Weak against
- Why is “fluoro” there?
- Used for
- side effects
- Types
- inhibits DNA gyrase (this prevents the supercoiling; our cells use topoisomerase).
- anything with altered DNA gyrase
- its not very soluble, fluorunated Qs
- UTIs, G- and G+ infections, mycobacteria (2nd line) and pseudomonas
- prolonged QT interval
- Ciprofloxacin, moxifloxacin
FLO-XACIN- flow- will help with your flow if you have a UTI from some nasty gyrating. FLO= FLOROquinolones.
Fidaxomycin
- MOA
- Uses
- Types
- targets “switch region” loading clamp of RNA polymerase and prevents RNA polymerase and DNA interaction
- against C-dif instead of vanco, or vanco-resistant c-dif.
- Dificid
**Dificid for difficult c-dificile **
Rifamycin
- MOA
- Weak against
- Uses (x3)
- Side effects
- blocks RNA polymerase elongation subunit
- anything with altered RNA polymerase ß subunit
- Uses: a) with isoniazid (inhibits synth of mycolic acid) in mycobacteria b)meningitis (crosses CNS) c) Blocks assembly of poxviruses
- orange sweat and urine
This is what they gave me once for a bad UTI. Or it was something else that makes your pee neon orange.
Metronidazole
- MOA
- Uses
- Reduced complex with ferredoxin interacts with DNA and breaks DNA strands (makes free radicals).–DAMAGES DNA
- Giardia (protozoa), anaerobic bacteria (clostridium, bacteriodes)
All those are gut problems. If you eat off the METRO floor you’re probably gonna get the squirts.
Also-Ferredoxin–remember Farrah’s uncle took this for his giardia (somehow he got c.dif?).
Families that inhibit protein synthesis
aminoglycosides, tetracyclines, macrolides, lincosamides
Aminoglycosides
- MOA
- Weak against
- Used for?
- Types?
- bind 30s subunit, block initiation by binding tRNAfmet
- altered p12 ribosomal protein, aminoglycosidases, altered permeability (ie: streptococci)
- G- enterics, with cephalosproins or penicillin in surgery
- streptomycin, neomycin, gentamycin, tobramycin, amikacin
Almost all A/O-MYCINS are aminoglycosylides. if -THROMYCIN then it isn’t.
Tetracyclines
- MOA
- Weak against
- used for
- side effects
- types
- inhibits binding of charged tRNA to A-site of 30s subunit
- efflux pumps
- Rickettsia, chlamydia, mycoplasms
- Toxicity, diziness, ringing in ears, flyorescen teeth and puss (WTF), bone damage to newborns CLASS D PREGNANCY RISK (IE DO NOT USE)
- doxycycline, tigecycline
Cyclines will PSYCH you out. Super toxic. Apparently make glow in the dark teeth and puss. (he wrote poss, i’m realizing he could have meant piss, too?)
Chloramphenicol
- MOA
- Resistance
- Uses
- translocation reaction inhibited (peptidyl transferase 50S)
- chloramphenical acetyl transferase (CAT)
- no longer used, resistant and toxic
Macrolides
- MOA
- weak to
- uses
- side effects (what else has this side effect?)
- types
- binds rRNA and inhibits translocation
- methylated RNA
- G+, some G-
- long QT (remember fluoroquinolones?), increase CV death
- erythromycin, carithromycin, azithromycin, telithromycin
Azithromycin= z-pack
If you’re a MACRO-LYER then THRO-MY-CIN away? Also, you have to MACRO-LIE to me to get me to take something thatll fuck my QT interval up.
Lincosamides
- MOA (what else does this?)
- Uses
- Side effects
- types
- bind rRNA and inhibit translocation (macrolides)
- anaerobes, antimalarial. Does not cross CNS
- Can disrupt native fluora
- Clindamycin
- This is one MYCIN that isn’t an aminoglycoside
- use of clindamycin= c. diff colonization
- Lincosamides are LINKed with Macrolides via mechanism.
- Clinda-clean dat colon- kill some native flora.
Nitrofurantoid
- mechanism
- use
- inhibits 30S
- used for UTIs
Mupirosin
- MOA
- Use
- Inhibits synthesis of isoleucyl-tRNA
- topical for G+ bacteria
Methenamine
- MOA
- Uses
- release formaldehyde in acidic urine
- UTI
Streptogramins
- MOA
- Used for
- type
- inhibit 50S
- treat VRE (vancomycin resistent enterococci) and VRSA (vancomycin resistent staph aureus)
- synercid = quinupristin + dalfopristin
GRAMINS (dunno if this is anywhere else…but) GRANs (grams) are pretty tight, even when shit is vanco resistant.
Oxazolidinones
- MOA
- uses
- type
- inhibit 50S subunit
- treat VRE and MRSA
- Linezolid