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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