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Trimethoprim Tablets

Function and Efficacy

Trimethoprim (TMP) is an antibacterial agent, a lipophilic weak base, and its chemical structure belongs to the pyrimethamine class. It has antibacterial activity against Escherichia coli, Klebsiella, Proteus mirabilis, Salmonella, and Shigella, but has no obvious antibacterial effect on Streptococcus pneumoniae, Neisseria gonorrhoeae, and Neisseria meningitidis, and has no effect on Pseudomonas aeruginosa. The mechanism of action of this product is to interfere with bacterial folic acid metabolism. It mainly selectively inhibits the activity of bacterial dihydrofolate reductase, so that dihydrofolate cannot be reduced to tetrahydrofolate, and synthetic folic acid is the main component of nucleic acid biosynthesis. Therefore, this product prevents the synthesis of bacterial nucleic acids and proteins, and the binding of this product to bacterial dihydrofolate reductase is 50,000 to 60,000 times tighter than that to mammalian enzymes. The combination of this product and sulfonamides can double block the bacterial folic acid synthesis metabolism, have a synergistic effect, enhance the antibacterial activity of sulfonamides, and convert the antibacterial effect into a bactericidal effect, reducing the production of drug-resistant strains.

Ingredients

Trimethoprim

Name Description Content CAS NO. Manufacturer
TrimethoprimIngredients

Trimethoprim (TMP) is an antibacterial agent, a lipophilic weak base, and its chemical structure belongs to the pyrimethamine class. It has antibacterial activity against Escherichia coli, Klebsiella, Proteus mirabilis, Salmonella, and Shigella, but has no obvious antibacterial effect on Streptococcus pneumoniae, Neisseria gonorrhoeae, and Neisseria meningitidis, and has no effect on Pseudomonas aeruginosa. The mechanism of action of this product is to interfere with bacterial folic acid metabolism. It mainly selectively inhibits the activity of bacterial dihydrofolate reductase, so that dihydrofolate cannot be reduced to tetrahydrofolate, and synthetic folic acid is the main component of nucleic acid biosynthesis. Therefore, this product prevents the synthesis of bacterial nucleic acids and proteins, and the binding of this product to bacterial dihydrofolate reductase is 50,000 to 60,000 times tighter than that to mammalian enzymes. The combination of this product and sulfonamides can double block the bacterial folic acid synthesis metabolism, have a synergistic effect, enhance the antibacterial activity of sulfonamides, and convert the antibacterial effect into a bactericidal effect, reducing the production of drug-resistant strains.

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738-70-5 44

Appearance

This product is white tablets.

Indication

This product can be used for initial cases of acute simple lower urinary tract infection caused by bacteria such as Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae, certain Enterobacteriaceae and saprophytic Staphylococcus aureus that are sensitive to it.

Usage and Dosage

The usual dosage for treating acute simple urinary tract infection in adults is 0.1g orally once every 12 hours or 0.2g once a day, for 7 to 10 days. Adult patients with renal impairment need to reduce the dosage. When the creatinine clearance rate is 30ml/min (0.5ml/s), the usual dosage for adults should still be used; when the creatinine clearance rate is 15-30ml/min (0.25-0.5ml/s), take 50mg every 12 hours; when the creatinine clearance rate is <15ml/min (0.25ml/s), this product should not be used.

Adverse Reactions

1. Due to the interference of this product with folic acid metabolism, adverse reactions in the blood system may occur, such as leukopenia, thrombocytopenia or methemoglobin anemia. Generally, leukopenia and thrombocytopenia are mild, and recovery is expected if the drug is discontinued in time. Folic acid preparations can also be added. 2. Allergic reactions: itching and rash may occur, and occasionally severe exudative erythema multiforme may occur. 3. Gastrointestinal reactions such as nausea, vomiting, and diarrhea, generally with mild symptoms. 4. Aseptic meningitis may occasionally occur, with symptoms such as headache, stiff neck, and nausea.

Precautions

This product can be used for the initial onset of acute simple lower urinary tract infection caused by Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae, certain Enterobacteriaceae and saprophytic Staphylococcus, etc., which are sensitive to it. This product is ineffective against Pseudomonas aeruginosa infection. At present, this product is rarely used alone, and is generally used in combination with sulfonamides, such as sulfamethoxazole or sulfadiazine.

Special Population Medication

Precautions for children: This product should not be used for infants under 2 months old. Precautions for pregnancy and lactation: 1. This product can cross the blood-placental barrier. Although it has not been confirmed to have teratogenic effects in human applications, it has teratogenic effects on rats and rabbits. Its mechanism of action is to interfere with folic acid metabolism. The drug concentration in the fetal circulation and amniotic fluid is close to the maternal blood drug concentration. Therefore, the use of this product during pregnancy must be decided after weighing the pros and cons. 2. This product can be secreted into breast milk with a high concentration, and the drug may interfere with the folic acid metabolism of breastfeeding infants. Therefore, although the problem has not been confirmed in humans, the use of this product in nursing mothers must be decided after weighing the pros and cons. Precautions for the elderly: Elderly patients are prone to folic acid deficiency when using this product, and the dosage should be reduced as appropriate.

Drug Interactions

1. When bone marrow suppressants are used in combination with this product, the chance of leukopenia and thrombocytopenia increases. 2. When dapsone is used in combination with this product, the blood concentrations of both drugs can increase. The increase in dapsone concentration can increase and aggravate adverse reactions, especially the occurrence of methemoglobinemia. 3. This product should not be used simultaneously with anti-tumor drugs and 2,4-diaminopyrimidine drugs, nor should it be used between courses of treatment with other folic acid antagonists, because it may cause bone marrow aplasia or megaloblastic anemia. 4. When used in combination with rifampicin, the clearance of this product can be significantly increased and the serum half-life can be shortened. 5. When used in combination with cyclosporine, renal toxicity can be increased. 6. This product can interfere with the hepatic metabolism of phenytoin, increase the T1/2 of phenytoin by 50%, and reduce its clearance by 30%. 7. When used in combination with procainamide, the renal clearance of procainamide can be reduced, resulting in an increase in the blood concentration of procainamide and its metabolite NAPA. 8 When used in combination with warfarin, it can inhibit the metabolism of the drug and enhance its anticoagulant effect.

Storage

Keep away from light and store in sealed container.

Packaging Specification

0.1g

Validity Period

36 months

Manufacturer

Jiaozuo Furuitang Pharmaceutical Co., Ltd.

  • Founded in:

    2010-07-13
  • Address:

    No. 168, Jianshe East Road, Jiaozuo City
  • Tax NO.:

    91410800558338035U
  • Registered Funds:

    30 million yuan
  • Website:

  • Email:

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