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CARBAPENEMS

CARBAPENEMS. e.g. Imipenem / Cilastatin MeropenemImipenem / Cilastatin, i.vMechanism of actionSimilar to other B. lactamsAntibacterial spectrumAerobic

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CARBAPENEMS

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    4. 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

    5. 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

    6. 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

    7. 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

    9. MONOBACTAMS AZTREONAM Mechanism of action 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

    10. AZTREONAM ( CONT. ) Pharmacokinetics 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

    11. 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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