Cell Wall synthesis inhibs-Antimicrobials Flashcards
What are the 4 main categories of antimicrobial agents that affect cell wall synthesis?
1-Penicillins
2-Cephalosporins
3-Carbapenes
4-Monobactams
What are 3 B-lactamas inhibitors?
1-Clavulanic acid (with amoxicillin=augmentin)
2-Sulbactam (with amp=unasyn)
3-Tazobactam(with piperacillin=zosyn)
Which type of antimicrobial resembles the D-Ala-D-Ala end of the peptide that serves as a substrate for transpeptidase enzymes?
B-lactams
*are bacteriocidal
Which enzymes crosslink adjacent glycerin chains of peptidoglycan precursors to form bacterial cell walls?
Transpeptidase
*B-lactams disrupt this function by inhibiting transpeptidation.
What are five categories or B-lactam antimicrobials?
1-Natural penicillins 2-Aminopenicillins (extended spectrum) 3-Penicillinase-resistant penicillins (anti-staphylococccal) 4-Anti-pseudomonal penicillin 5-Cephalosporins
Benzathine penicillin is an example of what type of natural penicillin that is active against Gram + cocci, is narrow spectrum, and rapidly hydrolyzed by penicillinase enzymes?
Penicillin G
Which type of Natural penicillin is an acid stable analogue to Pen G, is orally active and has the same spectrum as Pen G, but less active?
Penicillin V
Ampicillin and amoxicillin are examples of what type of B-lactam?
Aminopenicillins
*have better Gram (-) coverage than Pen G or V
What are two examples of drugs that amoxicillin or ampicillin have a B-lactamase inhibitor combined?
Augmentin (amoxicillin + clavulonate)
Unasyn (Ampicillin + sublactam)
What inhibits renal tubular secretion of methotrexate and results in high serum levels of methotrexate?
Amoxicillin (drug of choice for infective endocarditis)
*Amp has higher oral absorption, Cpmax values and longer half life than Amo
Methicillin, nafcillin, oxacillin and dicloxacillin are less potent than Pen G and are used to treat S aureus, S epidermis that produce what?
Pencillinase (these are penicillinase resistant penicillins)
Which two penicillinase resistant penicillins undergo biliary, not renal, excretion?
Oxacillin and dicloxacillin
What drug is used for serious S. Aureus infections (Non-MRSA)?
Nafcillin (Use Naf for Staph)
Which drug is combined with some antibiotics to increase their serum levels and prolong half lives by inhibiting excretion of such drugs?
Probenecid
Indanyl carbenicillin and ticarcillin are carboxypenicillins that have wider coverage of Gram (-) and are part of what group of B-lactams?
Anti-pseudomonal penicillins
*Ticarcillin 2-4 x’s more active than indanyl and used for P. aeruginosa. Was replaced by Timentin (ticarcillin + clavulonate)
What are the 3 subcategories of Anti-pseudonomal penicillins?
1-Carboxypenicillins (indanyl carbenicillin, ticarcillin)
2-Ureidopenicillins (Piperacillin, broadest spectrum penicillin)
3-Monobactams (Aztreonam)
Great for patients with IgI-mediated penicillin allergy, which anti-pseudonomal penicillin is resistant to some B-lactamases?
Aztreomnam (IV)
What are the 3 types of allergic reactions to penicillins/b-lactams?
1-Immediate (within 30 minutes, anaphylaxis, IgE mediated)
2-Accelrated (30 min-48 hr)
3-Delayed onset (longer than 2 days. 80-90% of penicillins are this, rashes)
Large doses of Pen G may produce lethargy, confusion, twitching, seizures, kidney failure or coma, whereas the most common side effect of penicillin is what?
Hypersensitivity
*10% of people are allergic to Penicillin
Typically used for its resistance to many older penicillinases which b-lactam group are typically tolerated by patients with penicillin allergy and are moderate-broad spectrum?
Cephalosporins
What two things increase as the generation of cephalosporin increases?
Gram (-) activity and B-lactamase resistance
*reduced Gram (+) activity of 2-4 Gen may result in superinfection
Not the first choice for any infection, which Generation of cephalosporins are mainly prophylactic, and do not penetrate the CNS of which Cefazolin is an example?
1st generation cephalosporins
Cefaclor, cefuroxime and cefoxitin are examples of which generation of cephalosporins?
2nd generation
*Cefoxitin has enhanced anaerobe activity and extended B-lactamase resistance
Cefotaxime/ceftriaxone, ceftazimide and cefdinir are which generation of cephalosporins that are active agains Gram (-) rods, and penetrate CNS sufficient to treat meningitis?
3rd generation cephalosporins
*Cefdinir is highest selling cephalosporin
Cefepime and Ceftaroline are what generation of cephalosporin?
4th and 5th generation respectively
Imipenem is usually coadministered with cilistatin to resist renal degradation, has broadest antibacterial activity known to man and is part of what b-lactam antibiotic group?
Carbapenems
What are three examples of non-b-lactam antibacterials that inhibit cell wall synthesis?
1-Vancomycin (IV)
2-Bacitracin (Topical against Gram -)
3-Daptomycin
Which non-b-lactam is used again complicated skin infections, bloodstream, endocarditis, bone and joint infections and meningitis caused by MRSA?
Vancomycin
*not as affective against MRSA as nafcillin, is nephrotoxic and ototoxic especially around aminoglycosides
Which non-b-lactam is bactericidal agains gram (+) and is active against MRSA and vancomycin resistant enterococcus?
Daptomycin (IV)