B-Lactams Antibiotics with other B-lactamase inhibitors Flashcards
CLASS I 𝝱-lactamase Inhibitors
- Clavam (Clavulanic acid)
-> Amoxicillin and Clavulanic acid (Co-
amoxiclav) - Penams (Sulbactam, Tazobactam)
-> Ampicillin and Sulbactam
(Sultamicillin)
-> Piperacillin and Tazobactam
(Tazocin®, Piptaz®)
-> Ceftolozane and Tazobactam - Diazobicyclocarbamoyl sulfate (Avibactam)
-> Ceftazidime and Avibactam
CLASS II 𝝱-lactamase Inhibitors
Carbapems
Narrow spectrum antibiotics and resistant to β-lactamases.
monobactams
monobactams are active against gram negative rods primarily through _____ but not against gram-positive bacteria or anaerobes
binding to PBP3
first clinically useful monobactam
aztreonam
monobactams are limited only to _______(including Pseudomonas aeruginosa), and no activity against gram positive and anaerobes
aerobic gram negative rods
are monobactams cross reactive with penicillins?
no
toxicity levels of monobactams?
relatively non-toxic
Widest spectrum among the β-lactam antibiotics.
carbapenems
what is carbapenems used for?
for empiric therapy associated with wide variety of microorganisms
clinically useful carbapenems
- Imipenem
- Meropenem
- Ertapenem
- Doripenem
clinically useful carbapenems
- Imipenem
- Meropenem
- Ertapenem
- Doripenem
what are carbapenems active against?
- gram negative rods (including Pseudomonas aeruginosa)
- gram positive bacteria
-anaerobes
list some carbapenems
- Imipenem (IV)
- Doripenem
- Ertapenem
- Metropenem
list some carbapenems
- Imipenem (IV)
- Doripenem
- Ertapenem
- Metropenem
what inactivates by renal dehydropeptidase (add cilastatin) and may cause seizures in patients with renal failure
Imipenem (IV)
irritating and formulated with (1% lidocaine)
Ertapenem (IM/IV)
are carbapenems cross reactive with penicillins?
yes
mechanism of action of vancomycin
- Directly bind to the d-alanyl-d-alanine portion of the pentapeptide, which blocks the transpeptidation.
- It also inhibits a second enzyme,
transglycosylase.
clinical uses of vancomycin
- Effective agent against Pseudomembranous colitis
- Drug of choice for resistant infections such as MRSA and MRSE
adverse effect of vancomycin where redness and rashes appear on the skin
red man syndrome
bloodstream infections and endocarditis caused by (MRSA)
methicillin-resistant staphylococci
combined with vancomycin for mengitidis caused by a penicillin-resistant strain of pneumococcus
combination with cefotaxime, ceftriaxone,
or rifampin
adverse reaction of vancomycin that results in swelling or inflammation of the large intestine
pseudomembranous colitis (PO)
another adverse reaction of vancomycin
red man syndrome
mechanism of action of bacitacin
Prevent the dephosphorylation of the
phospholipid that carries the peptidoglycan subunit across the cell membrane. This blocks the regeneration of the lipid carrier and inhibits cell wall synthesis.
clinical use for bacitracin
for topical application to skin, wounds or mucous membranes
mechanism of action for cycloserine
Inhibit cell wall synthesis by inhibiting the
activity of alanine racemase and d-alanyl-d-alanine ligase.
clinical uses of cycloserine
used as a second-line drug in the treatment of tuberculosis
mechanism of action for polymyxins
Bind to cell membranes rich in
phosphatidylethanolamine and destroying
membrane functions of active transport and permeability barrier
clinical use of polymyxins
were used primarily topically and rarely for systemic infections because of their toxicity and poor distribution to tissues
clinically useful members of polymyxins
- Polymyxin E (colistin)
- Polymyxin B
act as cationic detergents (attach to and disrupt bacterial cell membranes); against gram (-) bacteria
Polymyxin B and E
for multidrugresistant bacteria INHIBITOR OF PROTEIN SYNTHESIS
Colistin (polymyxin E)
