Carbapenems

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Chapter: Essential pharmacology : Betalactam Antibiotics

Imipenem : It is an extremely potent and broad-spectrum βlactam antibiotic whose range of activity includes gram-positive cocci, Enterobacteriaceae, Ps. aeruginosa, Listeria as well as anaerobes like Bact. fragilis and Cl. difficile.


CARBAPENEMS

 

Imipenem

 

It is an extremely potent and broad-spectrum βlactam antibiotic whose range of activity includes gram-positive cocci, Enterobacteriaceae, Ps. aeruginosa, Listeria as well as anaerobes like Bact. fragilis and Cl. difficile. It is resistant to most βlactamases; inhibits penicillinase producing staphylococci and some MRSA.

 

A limiting feature of imipenem is its rapid hydrolysis by the enzyme dehydropeptidase I located on the brush border of renal tubular cells. An innovative solution to this problem is its combination with cilastatin, a reversible inhibitor of dehydropeptidase I, which has matched pharmacokinetics with imipenem (t½ of both is 1 hr) and protects it.

Imipenemcilastatin 0.5 g i.v. 6 hourly (max 4 g/day) has proved effective in a wide range of serious hospital-acquired infections including those in neutropenic, cancer and AIDS patients.

 

Imipenem has propensity to induce seizures at higher doses and in predisposed patients. Diarrhoea, vomiting and skin rashes are the other side effects.

 

Meropenem

 

This newer carbapenem is not hydrolysed by renal peptidase; does not need to be protected by cilastatin. Like imipenem, it is active against both gram-positive and gram-negative bacteria, aerobes as well as anaerobes; somewhat more potent on gram-negative aerobes, but less potent on gram-positive cocci.

 

Meropenem is a reserve drug for the treatment of serious nosocomial infections like septicaemia, febrile neutropenia, intraabdominal and pelvic infections, etc. caused by cephalosporin-resistant bacteria. For P. aeruginosa infections, it should be combined with an aminoglycoside. The adverse effects of meropenem are similar to imipenem, but it is less likely to cause seizures.

 

Dose: 0.5–2.0 g (10–40 mg/kg) by slow i.v. injection 8 hourly.

 

MERONAM, MENEM, UBPENEM 0.5, 1.0 g/vial inj.

 

Faropenem

 

Another carbapenem βlactam antibiotic that is orally active against many gram-positive as well as gram-negative bacteria, including some anaerobes. Strep. pneumoniae, H. influenzae, Moraxella catarrhalis are highly susceptible. It has been mainly used in respiratory, ENT and genitourinary infections. Usual side effects are diarrhoea, abdominal pain, nausea and rashes.

 

Dose: 200–300 mg oral TDS; FARONEM 100, 200 mg tab.

 

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