Imipenemimipenem antibiotics, imipenem cilastatin
Imipenem Primaxin is an intravenous β-lactam antibiotic discovered by Merck scientists Burton Christensen, William Leanza, and Kenneth Wildonger in the mid-1970s Carbapenems are highly resistant to the β-lactamase enzymes produced by many multiple drug-resistant Gram-negative bacteria, thus play a key role in the treatment of infections not readily treated with other antibiotics
Imipenem was patented in 1975 It was discovered via a lengthy trial-and-error search for a more stable version of the natural product thienamycin, which is produced by the bacterium Streptomyces cattleya Thienamycin has antibacterial activity, but is unstable in aqueous solution, so impractical to administer to patients Imipenem has a broad spectrum of activity against aerobic and anaerobic, Gram-positive and Gram-negative bacteria It is particularly important for its activity against Pseudomonas aeruginosa and the Enterococcus species It is not active against MRSA, however
- 1 Mechanism of action
- 2 Spectrum of bacterial susceptibility and resistance
- 3 Coadministration with cilastatin
- 4 Adverse effects
- 5 References
- 6 Further reading
- 7 External links
Mechanism of action
Imipenem acts as an antimicrobial through inhibiting cell wall synthesis of various Gram-positive and Gram-negative bacteria It remains very stable in the presence of β-lactamase both penicillinase and cephalosporinase produced by some bacteria, and is a strong inhibitor of β-lactamases from some Gram-negative bacteria that are resistant to most β-lactam antibiotics
Spectrum of bacterial susceptibility and resistance
Acinetobacter anitratus, Acinetobacter calcoaceticus, Actinomyces odontolyticus, Aeromonas hydrophila, Bacteroides distasonis, Bacteroides uniformis, and Clostridium perfringens are generally susceptible to imipenem, while Acinetobacter baumannii, some Acinetobacter spp, Bacteroides fragilis, and Enterococcus faecalis have developed resistance to imipenem to varying degrees Not many species are resistant to imipenem except Pseudomonas aeruginosa Oman and Stenotrophomonas maltophilia
Coadministration with cilastatinMain article: Imipenem/cilastatin
Imipenem is rapidly degraded by the renal enzyme dehydropeptidase 1 when administered alone, and is almost always coadministered with cilastatin to prevent this inactivation
Common adverse drug reactions are nausea and vomiting People who are allergic to penicillin and other β-lactam antibiotics should take caution if taking imipenem, as cross-reactivity rates are low At high doses, imipenem is seizurogenic
- ^ US Patent 4,194,047
- ^ Clissold, SP; Todd, PA; Campoli-Richards, DM Mar 1987 "Imipenem/cilastatin A review of its antibacterial activity, pharmacokinetic properties and therapeutic efficacy" Drugs 33 3: 183–241 doi:102165/00003495-198733030-00001 PMID 3552595
- ^ Vardakas, KZ; Tansarli, GS; Rafailidis, PI; Falagas, ME Dec 2012 "Carbapenems versus alternative antibiotics for the treatment of bacteraemia due to Enterobacteriaceae producing extended-spectrum β-lactamases: a systematic review and meta-analysis" The Journal of antimicrobial chemotherapy 67 12: 2793–803 doi:101093/jac/dks301 PMID 22915465
- ^ Fischer, Janos; Ganellin, C Robin 2006 Analogue-based Drug Discovery John Wiley & Sons p 490 ISBN 9783527607495
- ^ Kahan, FM; Kropp, H; Sundelof, JG; Birnbaum, J Dec 1983 "Thienamycin: development of imipenen-cilastatin" The Journal of antimicrobial chemotherapy 12 Suppl D: 1–35 doi:101093/jac/12suppl_d1 PMID 6365872
- ^ Kesado, Tadataka; Hashizume, Terutaka; Asahi, Yoshinari 1980 "Antibacterial activities of a new stabilized thienamycin, N-formimidoyl thienamycin, in comparison with other antibiotics" Antimicrobial Agents and Chemotherapy 17 6: 912–7 doi:101128/aac176912 PMC 283902 PMID 6931548
- ^ "Imipenem spectrum of bacterial susceptibility and Resistance" PDF Retrieved 4 May 2012
- Clissold, SP; Todd, PA; Campoli-Richards, DM 1987 "Imipenem/cilastatin A review of its antibacterial activity, pharmacokinetic properties and therapeutic efficacy" Drugs 33 3: 183–241 doi:102165/00003495-198733030-00001 PMID 3552595
- Buckley, MM; Brogden, RN; Barradell, LB; Goa, KL 1992 "Imipenem/cilastatin A reappraisal of its antibacterial activity, pharmacokinetic properties and therapeutic efficacy" Drugs 44 3: 408–44 doi:102165/00003495-199244030-00008 PMID 1382937
- Imipenem bound to proteins in the PDB
|See also Receptor/signaling modulators GABAA receptor positive modulators GABA metabolism/transport modulators|
imipenem, imipenem antibiotics, imipenem brand name, imipenem cilastatin, imipenem classification, imipenem dosage, imipenem dosing, imipenem package insert, imipenem side effects, imipenem structure
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