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3 Antibiotics
Antibiotic classes & MOA's
| Question | Answer |
|---|---|
| What is the general MOA for penicillin family antibiotics? | Penicillin beta lactam ring binds to and competitively inhibits the transpeptidase enzyme (AKA penicillin-binding protein). |
| What are the general adverse effects of penicillin family antibiotics? | Anaphylactic reactions – bronchospasm, urticaria and anaphylactic shock |
| What are the clinical uses of penicillins? | S. pneumo (wind [lungs]), S. pyogenes (fire [pyo]), N. meningitides (meningitis), L. monocytogenes (monocyte), P. multocida (lot’s of AIDS [cida sounds like SIDA – multo = lot’s[), T. pallidum (syphilis) |
| What is the general MOA of the cephalosporins? | Same as penicillin: beta lactam ring binds to and competitively inhibits the transpeptidase enzyme (AKA penicillin-binding protein). |
| What are the 2 advantages of the cephalosporins? | More resistant to β-lactamases. A new R group side chain allows for more manipulations to create variations of the drugs. |
| With each new generation of cephalosporins, they can kill an increasing spectrum of: | Gram negative bacteria |
| What are the adverse effects of cephalosporins? | Same as penicillins: Anaphylactic reactions – bronchospasm, urticaria and anaphylactic shock |
| What bacteria are resistant to ALL cephalosporins? | MRSA & Enterococci. |
| What is the general MOA of the anti-ribosomal antibiotics? | Inhibition of either the 50S or 30S ribosomal subunit => block protein synthesis |
| Which antibiotics bind 50S ribosome? | CLE (Clindamycin, Linezolid, Erythromycin)Chloramphenicol – G+’s & anerobesClindamycin – G+’s & anaerobesOxazolidinones – Linezolid – G+ resistant bugs!Macrolides (eryth) – Mac ATE Clar – old school bugs (CBC ML) |
| Which antibiotics bind the 30S ribosome? | TAg + spectinomycin (Tetracycline, Aminoglycosides) |
| Name the penicillinase-resistant penicillins. | C, D . . . M, N, O: Cloxacillin (oral), Dicloxacillin (oral), Methicillin (IV), Nafcillin (both), Oxacillin (both) |
| Which of the penicillinase-resistant penicillins can kill S. aureus? | Methicillin (IV), Nafcillin (both), Oxacillin (both) |
| What is the mnemonic for remembering the penicillinase-resistant penicillins that can be administered via IV? | I met a nasty ox w/ a β-lactamase ring around his neck: Methicillin (IV), Nafcillin (both), Oxacillin (both) |
| What kind of bacteria are penicillinase-resistant antibiotics good for? | Gram positive |
| What kind of antibiotics are good for skin infections? | Penicillinase-resistant penicillins: think S. aureus or GAS – if you treat w/ penicillin you’re not covering penicillinase-producing S. aureus. If you use a PRP, you are! |
| Name the oral penicillinase-resistant penicillins. | Cloxacillin & Dicloxacillin: The CLOX were ticking! It was only a matter of time before the oral penicillinase-resistant penicillins were discovered! |
| Why is methicillin banned in the US? | Can cause interstitial nephritis. |
| How is methicilin used? | Used in sensitivity testing - MRSA. Outside of US it's used in IV form. It's highly effective against S. aureus. |
| How is nafcillin used? | IV & oral: Drug of choice for serious S. aureus infections like cellulitis, endocarditis, & sepsis. |
| How is oxacillin used? | IV & oral |
| Name the anti-pseudomonal penicillins. | Carbenicillin, Ticarcillin, Piperacillin: James Bond’s weapons: Car, Tick, Pipebomb |
| What are the anti-pseudomonal penicillins used for? | They have extended Gm negative rod coverage, esp Pseudomonas aeruginosa (causes devastating pneumonia & sepsis). It’s crafty & sneaky so it needs James Bond to kill it. Also active against anaerobes (Bacteroides fragilis) & many Gm+’s. |
| What can you use in combination with anti-pseudomonal penicillins to increase pseudomonas killing? | Aminoglycosides; usually gentamycin. |
| What is the limitation of anti-pseudomonal penicillins? | It's not penicillinase resistant (can’t kill S. aureus). |
| Name the 3 Beta-Lactamase Inhibitors? | Clavulanate, Sulbactam, Tazobactam |
| What are Beta-Lactamase Inhibitors used against? | Broad coverage against β-lactamase producing Gm+’s (S. aureus), Gm-’s (H. flu), & anaerobes (Bacteroides fragilis). |
| What is Augmentin? | Clavulanate + Amoxicillin = Augmentin |
| What is Timentin? | Clavulanate + Ticarcillin = Timentin |
| What is Ampictam (Unasyn)? | Sulbactam + ampicillin = Ampictam or Unasyn |
| What is Zosyn? | Tazobactam + Piperacillin = Zosyn |
| How do you identify a 1st generation cephalosporin? | Almost all have PH in their name. Exceptions: ceFADroxil & ceFAZolin. But it's just a FAD so don't let it FAZe you. |
| What are 1st generation cephalosporins used for? | Better against Gm positive. Strep & Staph are more susceptible to these guys. Good for skin infections. |
| What's the mnemonic for remembering 2nd generation cephalosporins? | You FONed your FAMily & they got in the CAR & MET wearing FOX FUR to drink TEa. Cefonicid, Cefamandole (& cefaclor), Loracarbef, Cefmetazole, Cefoxitin, Cefuroxime, Ceftetan, Cefprozil (you’re a PRO if you can remember this one). |
| What is the difference between 1st & 2nd generation cephalosporins? | 2nd generation covers more Gm negative than 1st. |
| What are the mnemonics for remembering the 3rd generation cephalosporins? | T for Third – lot’s of them have T right after Cef: ceftriaxone, ceftazidime, ceftizoxime, ceftibuten.I FIXed myself a POD full of FETA then took a TAXI to the OPERAZONE: CeFIXime, CefPODoxin, CeFETAmet, CefTAXIme, cefOPERAZONE. |
| What are 3rd generation cephalosporins good for? | Even more gram negative coverage! Can penetrate CSF so good for meningitis. |
| What is the name of the only 4th generation cephalosporin? | Cefepime. |
| What is the 4th generation cephalosporin good for? | Great Gm positive & Gm negative coverage. |
| What are carbapenems? | Antibiotics that are stable to beta-lactamases. |
| Name the carbapenems. | Imipenem, meropenem, ertapenem |
| What is the general MOA of carbapenems? | Inhibit bacterial cell wall synthesis. |
| What is so special about imipenem? | Broadest antibacterial coverage known to man: It's small so can squeeze thru porin channels to periplasmic space to interact w/ transpeptidase. Some bacteria have devo'd enzymes that can hydrolyze it & some Gm-’s made their porins smaller |
| What bacteria are resistant to imipenem? | Imipenem - “I’m a pen & I’m crossing out all the bacteria that are hard to treat!”MRSA, Pseudomonas, & mycoplasma still resistant |
| What's the mnemonic for Imipenem? | Imipenem - “I’m a pen & I’m crossing out all the bacteria that are hard to treat!” |
| What is aztreonam? | Monobactam – β lactam antibiotic that only binds transpeptidases of Gm NEGATIVES to inhibit cell wall synthesis. |
| What are the advantages of aztreonam? | Magic bullet for Gm-’s – even P. aeruginosa. Okay for penicillin allergics. |
| What do you combine with aztreonam to cover Gm positives? | vanc or clindamycin |
| What is Chloramphenicol? | The “chlorine” - 50S - Chlorox – CLEan TAg |
| What does Chloramphenicol cover? | Wide spectrum but toxic! Gm+, Gm-, & anaerobes |
| What are the adverse effects of Chloramphenicol? | Bone marrow depression, gray baby syndrome. Reversible dose-related anemia, or irreversible (usually fatal) aplastic anemia. Babies can’t conjugate it – excrete thru kidney & build up toxic levels => gray! |
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