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CARBAPENEMS e.g. Imipenem / Cilastatin Meropenem
Imipenem / Cilastatin, i.v Mechanism of action Similar to other B. lactams Antibacterial spectrum Aerobic & anaerobic G+ & G- bacteria, including pseudomonads and most enterobacter. MRSA is less sucebtible
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IMIPENEM / CILASTATIN ( CONT. )
Pharmacokinetics Not absorbed orally ( i.v infusion ) Partly broken down by dehydropeptidase in the proximal tubule- given with cilastatin ( dihydropeptidase inhibitor ) Excreted primarily by the kidney Doses must be reduced in renal failure Half- life about 1 hr
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Clinical uses of imipenem / cilastatin
Infections require multiple antibiotics ( useful in nosocomial infections ) Not used alone for serious pseud.infections Not used for MRSA infections
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Side effects Similar to those seen with B- lactams
Nausea & vomiting are frequent Excessive levels with renal failure may lead to seizures Pts allergic to penicillins may be allergic to imipenem
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Disadvantages of Imipenem / cilastatin vs Meropenem
High incidence of seizures, whereas meropenem is not. A 1g of imip./cilas require 200 ml saline to dissolve, whereas A 1g of meropenem dissolves in only 20 ml saline. Hence, meropenem can be given either by i.v bolus or i.v infusion Whereas, Imip./cilas should be given only by i.v infusion, so: Less suitable for fluid restricted pts Not suitable for outpatients- need hospitalization
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MONOBACTAMS AZTREONAM Mechanism of action Antibacterial spectrum
Similar to other B- lactams Antibacterial spectrum Active only against G- aerobic bacteria (pseudomonads, N. gonorrhea, N. meningitidis, H. influenzae and enterobacteriaceae ) Inactive against G+ and anaerobic bacteria
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AZTREONAM ( CONT. ) Pharmacokinetics Side effects
Poorly absorbed orally( i.v / 8 hr ) Limited penetration into the CSF Excreted primarily by the kidney Half- life 2 hr Side effects Similar to other B- lactams. Pts allergic to penicillins and cephalosporins can receive aztreonam
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Clinical uses of aztreonam
Active against G- aerobes only Alternative for penicillins ( piperacillin ) and cephalosporins ( ceftazidime ) allergic pts for G- infections Safe alternative to aminoglycosides, esp. in elderly and pts with renal impairements
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