Meropenem
Meropenem was developed by Sumitomo Pharmaceutical Company and ICI Pharmaceutical Company. 1994 was first listed in Italy, and 1999 entered the China market under the trade name "Meiping". It developed earlier in China. Zhejiang Haizheng Pharmaceutical Co., Ltd. obtained the approval of Meropenem API and powder injection on 1998 under the trade name of Haizhengmeite. Subsequently, Shenzhen Haibin Pharmaceutical Co., Ltd. obtained the approval of Meropenem bulk drug and injection on 200 1, with the trade name of "Beineng". Meropenem is one of the most widely used varieties in China.
Meropenem is the second generation of broad-spectrum carbapenem antibiotics and the first carbapenem antibiotic that can be used alone. The cell wall of bacteria is stable to most β -lactamases and has high affinity to PBPS, so meropenem has broad-spectrum antibacterial activity against aerobic and anaerobic bacteria.
Imipenem
Imipenem is produced by Merck; Co.) company (domestic name: Merck) 1979, which is also the first carbapenem antibiotic created by it. Imipenem cilastatin sodium was first listed in Germany on 1985, and was approved to be listed in the United States on1985+065438+1October 26th. The patent of imipenem compound is not binding in all countries in the world, but it has patent protection for its substance and method, and the protection period is long.
Imipenem and cilastatin sodium are compound antibiotics of carbapenems, which are mainly composed of imipenem and cilastatin sodium. Imipenem is the latest β -lactam antibiotic-imiphos, and it is also an amidine derivative. The antibacterial spectrum is wide, and it has good antibacterial activity against gram-negative bacteria and positive bacteria, aerobic bacteria and anaerobic bacteria. Cilastatin sodium is a specific enzyme inhibitor, which can block the metabolism of imipenem in kidney, thus increasing the concentration of imipenem in urinary tract.
Imipenem cilastatin sodium is mainly used for lower respiratory tract infection, abdominal infection, gynecological infection, urogenital infection, skin and soft tissue infection, bone and joint infection, sepsis, endocarditis and so on. It can also be used to prevent infection before and after operation. The main adverse reactions of imipenem cilastatin sodium are allergic reactions such as rash, itchy skin and fever, and gastrointestinal symptoms such as nausea, vomiting and diarrhea.
panipenem
Panipenem/Betamilon, alias: Kbeining. It is a carbapenem antibiotic. The antibacterial activity of methicillin-sensitive staphylococcus, streptococcus pneumoniae, streptococcus and enterococcus faecalis is similar to or slightly stronger than that of imipenem, while methicillin-resistant staphylococcus and enterococcus faecalis are resistant to this product. It has a prominent effect on Acinetobacter, and has a good effect on anaerobic bacteria such as Bacteroides fragilis and Clostridium difficile. Suitable for serious infections caused by sensitive bacteria: septicemia, infective endocarditis, lower respiratory tract infection, abdominal infection, urinary tract infection, bacterial meningitis, skin and soft tissue indications, gynecological infection.
Panipenem is a variety developed by Japan's Mitsuo * * Co., Ltd.,/KLOC-0 was listed in March, 1994. It is a variant of Japan's first pharmaceutical company, Sanxiong. In 2004, the global market of panipenem /Beta Miron was $86 million, and in 2005 it was $73 million.
The drug has the same effect as imipenem, and has strong antibacterial effect on gram-positive bacteria and negative bacteria, aerobic bacteria and anaerobic bacteria. In order to further improve the safety, panipenem/betamipron compound preparation was synthesized by using organic ion transport inhibitor betamipron 1 ∶ 1.
Itapenem
Ertapenem is a new long-acting penem for injection developed by Merck Pharmaceutical Company of the United States. It has reliable curative effect on multidrug-resistant Enterobacter but does not cover non-fermentative bacteria, and has good pharmacokinetic characteristics. The commodity name is "10,000 pieces". Graeme Bell, a Merck spokesperson, said: "This product is suitable for cases where the cause of infection is uncertain." Compared with imipenem and meropenem, ertapenem focuses on the treatment of community-acquired infections. The indications approved by ertapenem are: intra-abdominal infection; Community acquired pneumonia; Urinary tract infection with complications; Acute reproductive system infection; Skin and soft tissue infection with complications.
Ertapenem 200 1 was listed in the United States, and Merck's global sales in 2006 were $65,438+$400 million.
Faropenem
Faropenem sodium was first developed by Yamanouchi Pharmaceutical Co., Ltd. in Japan, and was approved to be listed in Japan on 1997. Faropenem is the only penem drug for oral administration, which greatly improves the oral bioavailability. Compared with other similar varieties, faropenem sodium has at least the following advantages: (1) oral absorption is good, no injection is needed, and patients' compliance is better; (2) All drugs in the market showed different degrees of nephrotoxicity, but in preclinical studies, faropenem sodium was given to dogs at a dose of 2000mg/kg for 26 weeks, and no nephrotoxicity was found. (3) The antibacterial spectrum is further expanded, and there are fewer drug-resistant strains.
Because of the optimistic prospect of faropenem sodium, domestic manufacturers have joined in. In 2006, Lunanbeite Pharmaceutical Co., Ltd. obtained the approval of Faropenem Sodium Tablets for the first time under the trade name of Di Jun. Up to now, seven manufacturers have been approved for preparation, and five manufacturers have been approved for the production of APIs. There are also Faropenem sodium dispersible tablets, Ropenem sodium for injection and Faropenem sodium enteric-coated tablets under review. Faropenem sodium entered the hospital market in China in the third quarter of 2007.
Biapenem
Biapenem is a carbapenem antibiotic for injection developed by Lederle Company of Japan and Cyanamide Company of the United States in 1989. It was listed in Japan in 2002 under the trade name "Omegaei". In 2008, Jiangsu Zheng Da Tianqing Pharmaceutical Co., Ltd. and Nanjing Xiansheng Dongyuan Pharmaceutical Co., Ltd. obtained the approval for the production of Biapenem bulk drug and powder injection. The specifications of biapenem powder for injection produced by the two manufacturers are 0.3g. The trade name of Biapenem under Zheng Da Tianqing Pharmaceutical Co., Ltd. is "Ce Tian", and the trade name of Xiansheng Dongyuan Pharmaceutical Co., Ltd. is "Anxin".
Biapenem is a new kind of penem drug, which has broad-spectrum antibacterial activity, can inhibit the synthesis of bacterial cell wall, and can tolerate the hydrolysis of various β -lactamases Biapenem is highly combined with pbps, which has good cell penetration to Gram-negative bacteria and less bacterial resistance to other β -lactam antibiotics. This product has 1 β methyl at position C 1, and is stable to human renal dihydropeptidase-1(DHP- 1), so it is unnecessary to use it with DHP- 1 inhibitor cilastatin.
Donipenem
Donipenem was developed by Shionogi Company in Japan, and was first listed in Japan in September 2005 under the trade name of "Finibax". Its injection is approved for the treatment of complex urinary tract infections and respiratory tract infections.
In the United States, this product is used to treat hospital-acquired pneumonia, including ventilator-associated pneumonia (VAP). The development of this product inhalation has been reported, which is mainly used to treat pulmonary infection in patients with cystic fibrosis. This product has broad antibacterial spectrum and strong antibacterial activity, and has strong antibacterial activity against various aerobic and anaerobic G+ and G- bacteria. In vitro activity showed that the activity of this product against G+ bacteria was stronger than meropenem and biapenem, equivalent to imipenem, and stronger than imipenem and biapenem, but slightly lower than meropenem. The mouse infection model experiment shows that this product has a good protective effect on a variety of G+ and G- bacteria infections.
Donipenem is stable to most β -lactamases including penicillinase, cephalosporinase and extended-spectrum β -lactamases. Donipenem is stable to human dehydropeptidase (DHP- 1) and can be used alone without being hydrolyzed by DHP- 1 in vivo.
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