1 basic introduction
The drug is mezlocillin sodium, and its chemical name is (2S, 5R, 6R)-3,3- dimethyl -6-[(R)-2[3- (methylsulfonyl) -2- oxo -1- imidazolidine formylamino ]-2- phenylacetylamino ]-7- oxo -4- thio-.
It is white or white-like powder or crystalline or loose block.
Methicillin sodium is soluble in water, methanol, dimethyl formyl, ethanol, acetone, isopropyl alcohol, ethyl ether, chloroform, ethyl acetate, etc.
2 development process
Mezloeillin Sodium was discovered in 1968 by Bayer Company in the Federal Republic of Germany when it was studying the amino phthalide derivative of amoxicillin A. It was first listed in the Federal Republic of Germany in 1977. In 1981, FDA officially approved the drug to be listed in the United States. Since 1980s, it has been listed in the United States, Japan, Italy, the Netherlands, Switzerland and other countries. As the third generation semi-synthetic penicillin, this medicine has been widely used abroad.
As a generic drug supplier in China, Feiyue Pharmaceutical can provide finished drugs such as Mezlocillin Sodium for Inection
Packaging:7ml tubular vial with filp-off, 1’s/box, 10’s/box50’s/box
10ml tubular vial with filp-off, 1’s/box, 10’s/box50’s/box
20ml mould vial with alum-cap, 1’s/box, 10’s/box, 50’s/box
FEIYUE recruits agents worldwide, we can provide complete registration documents.
3 Pharmacology and toxicology
As a semi-synthetic penicillin antibiotic, it has antibacterial effect on Pseudomonas aeruginosa, Escherichia coli, Pneumonia, Proteus, Enterobacter, Citrobacter, Serratia, Acinetobacter and Gram-positive cocci sensitive to penicillin, and has bactericidal effect in large doses. The antibacterial activity against Escherichia coli, Enterobacter, Pneumonia, Citrobacter, Serratia and Acinetobacter is stronger than that of carbenicillin and ampicillin. The antibacterial activity against indole-positive Proteus and Pseudomonas aeruginosa is stronger than that of carbenicillin and sulbenicillin. The antibacterial activity against Gram-positive bacteria such as Staphylococcus aureus is similar to that of carbenicillin, but the antibacterial activity against Streptococcus faecalis is superior to that of carbenicillin and sulbenicillin. Has good antibacterial effect on most anaerobic bacteria such as Bacteroides fragilis.
In vitro experiments show that it can inhibit the production of ß -Lactamase is unstable.
It has significant synergistic effect with aminoglycoside antibiotics such as gentamicin and kanamycin.
Mezlocillin sodium and sulbactam sodium for injection, a broad-spectrum antibiotic of Penicillium, is highly sensitive to gram-positive bacteria, gram-negative cocci and actinomycetes, such as staphylococcus, streptococcus and diplococcus. It is also sensitive to Corynebacterium diphtheriae, Bacillus anthracis, Clostridium, Actinomycetes bovis, Streptococcus candida, Listeria monocytogenes, Treponema pallidum, Leptospira, Neisseria gonorrhoeae and meningococcus. And is effective for drug-resistant staphylococcus aureus.
mechanism of action
It is a compound preparation of mezlocillin sodium and sulbactam sodium for injection mezlocillin sodium and sulbactam sodium in a ratio of 4∶1. Methicillin mainly interferes with the synthesis of mucin in bacterial cell wall, so that it can’t cross-link and cause cell wall defects. It can not only inhibit the synthesis of cell wall, but also promote the decomposition of cell wall, which leads to the death of bacteria. This process occurs during the reproductive period of bacterial cells. Bacteria have cell walls, while mammalian cells have no cell walls. Therefore, its bactericidal action is mainly aimed at cells in mitosis, and it has no effect on intracellular bacteria, latent bacteria and microorganisms without cell walls, so it has no toxic effect on human body.
5 Adaptation symptoms
It can be used to treat infections of respiratory system, urinary system, digestive system, gynecology and reproductive organs caused by sensitive strains of Gram-negative bacilli such as Escherichia coli, Enterobacter and Proteus, such as sepsis, suppurative meningitis, peritonitis, osteomyelitis, skin and soft tissue infections and eye, ear, nose and throat infections.
6 taboo of use
Those allergic to penicillin antibiotics are prohibited.
7 Adverse reactions
Adverse reactions mainly include loss of appetite, nausea, vomiting, diarrhea, local pain of intramuscular injection and rash, and most of them occur in the course of drug administration. Most of them are mild and do not affect the continued use of drugs. In severe cases, the above symptoms are quickly reduced or disappeared after drug withdrawal. In a few cases, serum aminotransferase, alkaline phosphatase and eosinophil transient increase can occur. Neutropenia and hypokalemia are extremely rare. No serious reactions such as renal function change and blood electrolyte disturbance were found. The main impacts are:
Hematological effects: A few patients can cause leukopenia, thrombocytopenia and eosinophilia after taking medicine. 2. Influence of cardiovascular system: Thrombophlebitis may occasionally occur in a few patients when intravenous administration.
Effects of mezlocillin on the central nervous system: It has been reported that the potential toxicity of mezlocillin on the central nervous system is convulsion and neuromuscular irritability. These toxic reactions are particularly likely to occur in elderly patients with decreased renal function. Occasionally, there are reports of seizures caused by medication.
Effects of endocrine/metabolic system: Hypokalemia is occasionally reported when mezlocillin is used, especially in cancer patients.
Gastrointestinal effects: After treatment with mezlocillin, a few patients may have gastrointestinal symptoms such as anorexia and diarrhea.
Influence of kidney/genitourinary system: It is reported that interstitial nephritis occasionally occurs in patients treated with mezlocillin.
Influence of liver: It is reported that patients may have abnormal liver function during mezlocillin treatment. Serum transaminase (aspartate transaminase and alanine transaminase) increased.
Skin effects: It is reported that during mezlocillin treatment, a few patients may have various skin reactions, such as generalized rash, fever, urticaria, itching, etc.
8 matters needing attention
Penicillin skin test must be done before taking medicine, and those who are positive are forbidden.
Methicillin is cross-allergic to penicillin drugs. Cross-allergic reaction: People who are allergic to one penicillin antibiotic may also be allergic to other penicillin antibiotics. It can also be allergic to penicillamine or cephalosporins. People who are allergic to mezlocillin are forbidden; Those who are allergic to any other penicillin drugs are prohibited.
Use with caution in the following situations
Use it with caution in patients with abnormal coagulation function. Use with caution in patients allergic to cephalosporins or other allergens. Use it with caution in patients with severe liver and kidney dysfunction. People with a history of allergic diseases such as asthma, eczema, hay fever and urticaria.
When mezlocillin is used, the urine glucose test (Clinitest method) can give false positive results. During mezlocillin treatment, the results of urine protein test can be positive. A few patients can have leukopenia, thrombocytopenia and eosinophilia after taking medicine. Decreased blood potassium; Serum transaminase (aspartate transaminase and alanine transaminase) increased.
Liver, kidney function and hemogram should be routinely detected during long-term medication; Blood potassium concentration should be monitored when taking large doses of drugs for a long time.
Disturbance to diagnosis: (1) During medication, false positive may appear when urine sugar is measured by copper sulfate method, but it is not affected by glucoamylase method; High-dose injection can cause hypernatremia; ⑵ It can increase serum alanine aminotransferase or aspartate aminotransferase.