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Methoxybenzidine is a lipophilic and weakly basic ethylaminopyrimidine bacteriostatic agent, also known as sulfonamide synergist, methoxybenzylaminopyrimidine, antimicrobial synergist, methoxybenzylaminopyrimidine, methoxybenzylpyrimidine, trimethobenzamidopyrimidine, trimethobenzylpyrimidine, at room temperature it is a white or off-white crystalline powder, odourless and bitter in taste, slightly soluble in chloroform, slightly soluble in ethanol or acetone, virtually insoluble in water, readily soluble in glacial acetic acid
Antibacterial spectrum and sulfonamides are similar, but the antibacterial effect is stronger, effective against Escherichia coli, Proteus mirabilis, Pneumocystis pneumoniae, Staphylococcus putrefaciens, a variety of Gram-positive and negative bacteria, but ineffective against Pseudomonas aeruginosa infections, the lowest inhibitory concentration is often less than 10mg/L, the use of a single easy to cause bacterial resistance, so it is generally not used alone, mainly with sulfonamides to form a combination of preparations, clinically used in the treatment of urinary tract infections, Intestinal infections, respiratory infections, bacillary dysentery, enteritis, typhoid fever, meningitis, otitis media, otitis media, sepsis and soft tissue infections.
It is not less effective than ampicillin in typhoid fever and paratyphoid fever, and can also be used in combination with long-acting sulfonamides for the prevention and treatment of drug-resistant falciparum malaria.
Uses of Trimethoprim.
New oral broad-spectrum antibacterial drug. The antimicrobial spectrum is similar to that of sulphonamides but more potent, and it is effective against a variety of gram-positive and gram-negative bacteria.
Since bacteria will easily develop resistance to this product, it is not suitable to be used as an antibacterial drug alone.
Combined with sulfonamides, methotrexate can enhance the antibacterial effect several times to dozens of times. It is mainly used as a potentiator of sulfonamides.
It is generally used in the ratio of 1:5. It can also be used as veterinary medicine for the treatment of septicaemia caused by avian coliform hepatic bacteria, chicken dysentery, avian typhoid fever, cholera, respiratory system secondary bacterial infections and so on. It can also be used in the treatment of coccidiosis.
Preferred as an antimicrobial, prokaryotic enzyme-selective inhibitor of dihydrofolate reductase; specific dosage form inhibitor widely used in the study of dihydrofolate reductase; inhibits the synthesis of tetrahydrofolate through prokaryotic specific dihydrofolate reductase (DHFR).
Undesirable Effect of Trimethoprim.
Methotrexate (TMP for short) has low toxicity and adverse reactions are rare at commonly used doses.
As methotrexate can interfere with folic acid metabolism, patients may experience haematological reactions such as anaemia, leucopenia and thrombocytopenia, mostly in cases of excessive dosage and prolonged course of treatment.
Therefore, blood tests should be performed during the administration of the drug. The maximum daily dosage of this product should not exceed 0.5g, and the duration of continuous use of the drug should not exceed 1 week. When the adverse reactions of the blood system are obvious, oral folic acid preparations can be given to correct them.
Methotrexate should not be used concomitantly with antineoplastic drugs, antiepileptic drugs and other folic acid antagonists; TMP may occasionally cause crystalluria when combined with SMZ or SD. Other adverse reactions include skin rash and mild gastrointestinal reactions.
Production Method of Bulk Trimethoprim Powder.
Trimethoxybenzaldehyde as raw material, first condensed with methoxypropionitrile to form 3'4'5'-trimethoxy-2-cyano-3-methoxypropene, and then cyclized with guanidine nitrate in methanol/sodium methanol to obtain
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