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Trimethoprim-sulfamethoxazole tablets

Function and Efficacy

This product is a compound preparation of sulfamethoxazole (SMZ), sulfadiazine (SD) and trimethoprim (TMP). It has a broad antibacterial spectrum, strong antibacterial effect, and synergistic antibacterial or bactericidal effect. It has good antibacterial activity against most Gram-positive and negative bacteria, including non-enzyme-producing Staphylococcus aureus, Streptococcus pyogenes, Pneumococcus, Escherichia coli, Klebsiella, Salmonella, Proteus, Morganella, Shigella and other Enterobacteriaceae, gonococci, meningococci, Haemophilus influenzae, etc. In recent years, bacterial resistance to this product is common, especially Enterobacteriaceae such as Shigella, so it is rarely used clinically. In addition, it also has good antibacterial activity against Vibrio cholerae, Chlamydia trachomatis, etc. in vitro. Its mechanism of action is that both SMZ and SD can compete with p-aminobenzoic acid for dihydrofolate synthase, making it impossible for bacteria to synthesize dihydrofolate, while TMP inhibits the dihydrofolate reductase of bacteria, hindering the reduction of dihydrofolate to tetrahydrofolate. When the three are used together, they have a double blocking effect on the bacterial synthesis of tetrahydrofolate, so their antibacterial effect is stronger than that of a single drug, and the strains resistant to them are also reduced accordingly.

Ingredients

This product is a compound preparation, each tablet contains sulfamethoxazole, sulfadiazine and trimethoprim

Name Description Content CAS NO. Manufacturer
SulfadiazineIngredients

It competes with p-aminobenzoic acid for dihydrofolate synthase, hindering bacterial synthesis of dihydrofolate. When used in combination with trimethoprim, it can double block the bacterial tetrahydrofolate synthesis process.

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68-35-9 14
TrimethoprimIngredients

By inhibiting bacterial dihydrofolate reductase, it hinders the reduction of dihydrofolate to tetrahydrofolate. When used in combination with sulfonamides, it can double block the bacterial tetrahydrofolate synthesis process.

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738-70-5 44

Appearance

This product is white tablets.

Indication

It is mainly used for urinary tract infections, intestinal infections, acute attacks of chronic bronchitis in adults, acute otitis media, etc. caused by bacteria sensitive to this product.

Usage and Dosage

The usual oral dose for adults is: 2 tablets at a time, twice a day, and the first dose is doubled. The course of treatment for acute exacerbation of chronic bronchitis is at least 10 to 14 days; the course of treatment for urinary tract infection is 7 to 10 days; the course of treatment for bacillary dysentery is 5 to 7 days; the course of treatment for acute otitis media is 10 days

Adverse Reactions

1. Allergic reactions are relatively common. It can manifest as drug rash. In severe cases, exudative erythema multiforme, exfoliative dermatitis and bullous epidermolysis atrophic dermatitis may occur; there are also serum sickness-like reactions such as photosensitivity reaction, drug fever, joint and muscle pain, fever, etc. Anaphylactic shock is occasionally seen. 2. Neutropenia or deficiency, thrombocytopenia, and occasionally aplastic anemia. Patients may show symptoms of sore throat, fever and bleeding tendency. 3. Hemolytic anemia and hemoglobinuria. This is prone to occur in patients who lack glucose-6-phosphate dehydrogenase after using sulfonamides, and is more common in newborns and children than in adults. 4. Hyperbilirubinemia and neonatal kernicterus. Because this product competes with bilirubin for protein binding sites, it can cause an increase in free bilirubin. Newborns have imperfect liver function,

Precautions

1. Patients who are allergic to sulfonamides are contraindicated. 2. Since this product blocks the metabolism of folic acid and aggravates the folate deficiency in patients with megaloblastic anemia, patients with this disease are contraindicated to use this product. 3. Pregnant and lactating women are contraindicated to use this product. 4. Infants under 2 months old are contraindicated to use this product. 5. Patients with liver and kidney damage are contraindicated to use this product.

Special Population Medication

Precautions for children: Since sulfonamides can compete with bilirubin for binding sites on plasma proteins, and the acetyltransferase system of newborns is not fully developed, the free blood concentration of sulfonamides increases, which increases the risk of kernicterus. Therefore, the use of this type of drug in newborns and infants under 2 months old is contraindicated. Precautions for pregnancy and lactation: 1. Sulfonamides can cross the blood-placental barrier to the fetus, and animal experiments have found that they have teratogenic effects. There is a lack of sufficient data in human studies, so pregnant women should avoid using them. 2. Sulfonamides can be secreted in breast milk, and the concentration in breast milk can reach about 50% to 100% of the maternal blood concentration. The drug may affect the baby; the use of sulfonamides in newborns with glucose-6-phosphate dehydrogenase deficiency may cause hemolytic anemia. In view of the above reasons, breastfeeding women should suspend the use of this product. Precautions for the elderly: Elderly patients have an increased chance of serious adverse reactions when using sulfonamides. Such as severe rash, bone marrow suppression and thrombocytopenia. Therefore, elderly patients should avoid using them, and when there is an indication, they need to weigh the pros and cons before making a decision.

Drug Interactions

1. The combined use of urine alkalinizing drugs can increase the solubility of this product in alkaline urine and increase excretion. 2. It cannot be used in combination with para-aminobenzoic acid, which can replace this product for bacterial uptake, and the two are antagonistic to each other. 3. When the following drugs are used together with this product, this product can replace the protein binding sites of these drugs, or inhibit their metabolism, resulting in prolonged drug action time or toxic reactions. Therefore, when these drugs are used at the same time as this product, or when used after the application of this product, their dosages need to be adjusted. Such drugs include oral anticoagulants, oral hypoglycemic drugs, methotrexate, phenytoin sodium and thiopental sodium. 4. The combined use with bone marrow suppressive drugs may enhance the adverse reactions of such drugs to the hematopoietic system. For example, leukopenia and thrombocytopenia, etc. If there is an indication for the combined use of the two drugs, the possible toxic reactions should be closely observed. 5. Long-term combined use with contraceptives (estrogens) may reduce the reliability of contraception and increase the chance of extramenstrual bleeding. 6. When used in combination with thrombolytic drugs, their potential toxic effects may be increased. 7. When used in combination with hepatotoxic drugs, the incidence of hepatotoxicity may increase. Liver function should be monitored for such patients, especially those who have been taking the drug for a long time and have a history of liver disease. 8. When used in combination with photosensitive drugs, photosensitization may be additive. 9. Patients receiving this product have an increased need for vitamin K. 10. It should not be used in combination with methenamine, because methenamine can decompose in acidic urine to produce formaldehyde, which can form insoluble precipitates with this product. This increases the risk of crystalluria. 11. This product can replace the plasma protein binding site of phenylbutazone, and when the two are used together, the effect of phenylbutazone can be enhanced. 12. When sulfinpyrazone is used in combination with this product, the latter's secretion from the renal tubules can be reduced, and its blood drug concentration will increase and last, thereby producing toxic reactions. Therefore, the dose of this product may need to be adjusted during or after the use of sulfinpyrazone. When the course of sulfinpyrazone treatment is long, the blood concentration of this product should be monitored to help adjust the dosage and ensure safe use. 13. The TMP in this product can inhibit the metabolism of warfarin and enhance its anticoagulant effect. 14. The TMP in this product can increase nephrotoxicity when used in combination with cyclosporine. 15. When rifampicin is used in combination with this product, the clearance of TMP in this product can be significantly increased and the serum half-life can be shortened. 16. It is not suitable to be used in combination 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. 17. It is not suitable to be used in combination with dapsone, because the blood concentration of both dapsone and TMP in this product can be increased. The increase in dapsone concentration increases and aggravates adverse reactions, especially the occurrence of methemoglobinemia. 18. Avoid using it in combination with penicillins, because this product may interfere with the bactericidal effect of such drugs.

Storage

Keep away from light and store in sealed container.

Packaging Specification

Sulfadiazine 0.2 g, sulfadiazine 0.2 g, trimethoprim 80 mg

Validity Period

36 months

Manufacturer

Jinzhou Jiuyang Pharmaceutical Co., Ltd.

  • Founded in:

    1998-12-25
  • Address:

    No. 6, Section 3, Jingang Street, Jinzhou Economic and Technological Development Zone, Liaoning Province
  • Tax NO.:

    912107007016206591
  • Registered Funds:

    10 million yuan
  • Email:

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