Supriya Ghosh (Editor)

Meropenem

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Trade names
  
Merrem

Routes ofadministration
  
Intravenous

Molar mass
  
383.464 g/mol

CAS ID
  
119478-56-7

AHFS/Drugs.com
  
Monograph

ATC code
  
J01DH02 (WHO)

Bioavailability
  
100%

Meropenem

Pregnancycategory
  
US: B (No risk in non-human studies)

Legal status
  
UK: POM (Prescription only)US: ℞-only

Preparation administration of meropenem captioned


Meropenem is an ultra-broad-spectrum antibiotic used to treat a wide variety of infections. It is a β-lactam and belongs to the subgroup of carbapenems, similar to imipenem and ertapenem.

Contents

Meropenem was developed by Dainippon Sumitomo Pharma and patented in 1983. It gained US FDA approval in July 1996. It penetrates well into many tissues and body fluids, including cerebrospinal fluid, bile, heart valve, lung, and peritoneal fluid. It was initially marketed by AstraZeneca under the trade name Merrem.

Meropenem animation


Medical uses

The spectrum of action includes many Gram-positive and Gram-negative bacteria (including Pseudomonas) and anaerobic bacteria. The overall spectrum is similar to that of imipenem, although meropenem is more active against Enterobacteriaceae and less active against Gram-positive bacteria. It works against extended-spectrum β-lactamases, but may be more susceptible to metallo-β-lactamases. Meropenem is frequently given in the treatment of febrile neutropenia. This condition frequently occurs in patients with hematological malignancies and cancer patients receiving anticancer drugs that suppress bone marrow formation. It is approved for complicated skin and skin structure infections, complicated intra-abdominal infections and bacterial meningitis.

Administration

Meropenem is administered intravenously as a white crystalline powder to be dissolved in 5% monobasic potassium phosphate solution. Dosing must be adjusted for altered kidney function and for haemofiltration.

Side effects

The most common adverse effects are diarrhea (4.8%), nausea and vomiting (3.6%), injection-site inflammation (2.4%), headache (2.3%), rash (1.9%) and thrombophlebitis (0.9%). Many of these adverse effects were observed in severely ill individuals already taking many medications including vancomycin. One study showed Clostridium difficile-associated diarrhea happened in 3.6% of meropenem patients. Meropenem has a reduced potential for seizures in comparison with imipenem. Several cases of severe hypokalemia have been reported. Meropenem, like other carbopenems, is a potent inducer of multidrug resistance in bacteria.

Mechanism of action

Meropenem is bactericidal except against Listeria monocytogenes, where it is bacteriostatic. It inhibits bacterial wall synthesis like other β-lactam antibiotics. In contrast to other beta-lactams, it is highly resistant to degradation by β-lactamases or cephalosporinases. In general, resistance arises due to mutations in penicillin-binding proteins, production of metallo-β-lactamases, or resistance to diffusion across the bacterial outer membrane. Unlike imipenem, it is stable to dehydropeptidase-1, so can be given without cilastatin.

In 2016 a synthetic peptide-conjugated PMO (PPMO) was found to inhibit the expression of New Delhi Metallo-beta-lactamase, an enzyme that many drug-resistant bacteria use to destroy carbapenems.

References

Meropenem Wikipedia