Trimethoprim is a lipophilic weakly basic pyrimethamine bacteriostat, also known as sulfonamide synergist, trimethoprim, antibacterial synergist, trimethoprim, trimethoprim Oxybenzamine, trimethoprim, white or off-white crystalline powder at room temperature, odorless, bitter, slightly soluble in chloroform, slightly soluble in ethanol or acetone, almost insoluble in water, easy in glacial acetic acid Dissolve. The antibacterial spectrum is similar to sulfa drugs, but the antibacterial effect is strong. It is effective against Escherichia coli, Proteus mirabilis, Pneumoniae, Staphylococcus saprophyticus, various Gram-positive and negative bacteria, but it is ineffective against Pseudomonas aeruginosa infection, and the minimum inhibitory concentration Usually less than 10mg/L, it is easy to cause bacterial resistance when used alone, so it is generally not used alone. It is mainly composed of sulfa drugs to form a compound preparation. It is used clinically to treat urinary tract infections, intestinal infections, respiratory tract infections, dysentery, and enteritis , Typhoid fever, meningitis, otitis media, meningitis, sepsis, and soft tissue infections. The efficacy of typhoid fever and paratyphoid fever is not less than that of ampicillin, and it can also be used in combination with long-acting sulfonamides for the prevention and treatment of drug-resistant falciparum malaria. The antibacterial principle of trimethoprim is to interfere with the folate metabolism of bacteria. The main mechanism of action is to selectively inhibit the activity of bacterial dihydrofolate reductase, so that dihydrofolate cannot be reduced to tetrahydrofolate, and the synthesis of folic acid is the main component of nucleic acid biosynthesis, so this product prevents bacterial nucleic acid and protein Synthesized, and the combination of methoxycarbidine (TMP) and bacterial dihydrofolate reductase is 50,000 to 60,000 times tighter than that of mammalian enzymes. The combined use with sulfonamides can double the bacterial folic acid anabolism and have a synergistic effect to enhance the antibacterial activity of the sulfonamides, and can turn the bacteriostatic effect into a bactericidal effect and reduce resistant strains. In addition, this product can also enhance the antibacterial effect of various antibiotics (such as tetracycline, gentamicin, etc.).
New oral broad-spectrum antibacterial drugs. The antibacterial spectrum is similar to that of sulfa drugs and has stronger potency. It is effective against a variety of Gram-positive and negative bacteria. Because bacteria will easily develop resistance to this product, it should not be used alone as an antibacterial drug. The combined use of trimethoprim and sulfa drugs can increase the antibacterial effect several times to dozens of times. This product is mainly used as a synergist of sulfonamides. Generally used at a ratio of 1:5. It can also be used as a veterinary medicine to treat sepsis caused by Escherichia coli, chicken dysentery, avian typhoid, cholera, and secondary bacterial infections of the respiratory system. It can also be used for the treatment of coccidiosis.
Post time: Jun-17-2020