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Compound sulfamethoxazole injection

Function and Efficacy

This product is a compound preparation of sulfamethoxazole (SMZ) and trimethoprim (TMP). It has good antibacterial effects on non-enzyme-producing Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Escherichia coli, Klebsiella, Salmonella, Proteus, Morganella, Shigella and other Enterobacteriaceae, Neisseria gonorrhoeae, Neisseria meningitidis, and Haemophilus influenzae. In particular, the antibacterial effects on Escherichia coli, Haemophilus influenzae, and Staphylococcus aureus are significantly enhanced compared with SMZ alone. In addition, it also has good antimicrobial activity against Chlamydia trachomatis, Nocardia asteroides, protozoa, and Toxoplasma gondii in vitro. The mechanism of action of this product is that SMZ acts on dihydrofolate synthase, interfering with the first step of folic acid synthesis, and TMP acts on the second step of folic acid anabolism, selectively inhibiting the action of dihydrofolate reductase. The combination of the two can double-block the folic acid metabolism of bacteria. The synergistic antibacterial effect of this product is enhanced compared with a single drug, and the number of strains resistant to it is reduced. However, in recent years, bacterial resistance to this drug has also been on the rise.

Ingredients

Trimethoprim, sulfamethoxazole.

Name Description Content CAS NO. Manufacturer
TrimethoprimIngredients

It acts on the second step of folic acid anabolism and selectively inhibits the action of dihydrofolate reductase. When used in combination with sulfamethoxazole, it can double-block the bacterial folic acid metabolism, enhance the synergistic antibacterial effect, and reduce drug-resistant strains.

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738-70-5 44
SulfamethoxazoleIngredients

It acts on dihydrofolate synthase, interfering with the first step of folic acid synthesis. When used in combination with trimethoprim, it can doubly block the bacterial folic acid metabolism, enhance the synergistic antibacterial effect, and reduce drug-resistant strains.

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723-46-6 33

Appearance

This product is a colorless or slightly yellow clear liquid.

Indication

In recent years, many common clinical pathogens are often resistant to this product, so it is necessary to refer to the drug sensitivity results when treating bacterial infections. The main indications of this product are the following infections caused by sensitive strains: 1. Urinary tract infections caused by sensitive strains of Escherichia coli, Klebsiella, Enterobacter, Proteus mirabilis, Proteus vulgaris and Morganella. 2. Acute otitis media in children over 2 years old caused by Streptococcus pneumoniae or Haemophilus influenzae. 3. Acute exacerbation of chronic bronchitis in adults caused by Streptococcus pneumoniae or Haemophilus influenzae. 4. Intestinal infections and Shigella infections caused by sensitive strains of Shigella flexneri or Shigella sonnei. 5. This product is the first choice for the treatment of Pneumocystis carinii pneumonia. 6. For the prevention of Pneumocystis carinii pneumonia, it can be used in patients with a history of at least one attack of Pneumocystis carinii, or H

Usage and Dosage

1 Common dosage for adults: 160 mg of trimethoprim and 800 mg of sulfamethoxazole for the treatment of bacterial infections, taken once every 12 hours. For the treatment of Pneumocystis carinii pneumonia, 3.75-5 mg/kg of trimethoprim and 18.75-25 mg/kg of sulfamethoxazole are taken once every 6 hours. Preventive medication for adults: initially give 160 mg of trimethoprim and 800 mg of sulfamethoxazole twice a day, followed by the same dose once a day, or 3 times a week. 2 Common dosage for children: contraindicated for infants under 2 months old. For the treatment of bacterial infections, infants over 2 months old and weighing less than 40 kg are given SMZ 20-30 mg/kg and TMP 4-6 mg/kg orally according to body weight, once every 12 hours; the dosage for children weighing >40 kg is the same as the common dosage for adults. For the treatment of parasitic infections such as Pneumocystis carinii pneumonia, take SMZ 18.75-25 mg/kg and TMP 3.75-5 mg/kg orally once every 6 hours according to body weight. 3 The course of treatment for acute exacerbation of chronic bronchitis is at least 10-14 days; the course of treatment for urinary tract infection is 7-10 days; the course of treatment for bacillary dysentery is 5-7 days; the course of treatment for acute otitis media in children is 10 days; the course of treatment for Pneumocystis carinii pneumonia is 14-21 days.

Adverse Reactions

1. Allergic reactions are common and may manifest as drug eruptions. 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, drug fever, joint and muscle pain, and fever. Occasionally, anaphylactic shock is seen. 2. Neutropenia or deficiency, thrombocytopenia, and aplastic anemia. Patients may present with sore throat, fever, pallor, and bleeding tendency. 3. Hemolytic anemia and hemoglobinuria. This is easy to occur in patients who lack glucose-6-phosphate dehydrogenase after taking 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 and poor bilirubin processing, so they are more likely to develop hyperbilirubinemia and neonatal jaundice, and occasionally kernicterus. 5. Liver damage. Jaundice and liver dysfunction may occur, and in severe cases, acute liver necrosis may occur. 6. Kidney damage. Crystalluria, hematuria, and tubular urine may occur; occasionally, patients may experience serious adverse reactions such as interstitial nephritis or tubular necrosis. 7. Nausea, vomiting, decreased appetite, diarrhea, headache, fatigue, etc., generally mild symptoms. Occasionally, patients may develop Clostridium difficile enteritis, and the drug should be discontinued at this time. 8. Occasionally, thyroid enlargement and hypofunction may occur. 9. Central nervous system toxicity may occasionally occur, manifested as mental confusion, disorientation, hallucinations, euphoria or depression. 10. Occasionally, aseptic meningitis may occur, with symptoms such as headache, stiff neck, and nausea. Although serious adverse reactions caused by this product are rare, they often involve various organs and can be fatal, such as exudative erythema multiforme, exfoliative dermatitis, epidermolysis bullosa atrophic dermatitis, fulminant liver necrosis, agranulocytosis, aplastic anemia and other blood system abnormalities. The above adverse reactions are more common in AIDS patients than in non-AIDS patients.

Precautions

1. Patients who are allergic to SMZ and TMP are contraindicated to use this product. 2. Since this product blocks the metabolism of folic acid and aggravates the folate deficiency in patients with megaloblastic anemia, this product is contraindicated for patients with this disease. 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 severe liver and kidney damage are contraindicated to use this product.

Special Population Medication

Precautions for children: Since this product 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 sulfonamide 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. Children are in the growth and development period, and their liver and kidney functions are not yet perfect, so the dosage should be reduced as appropriate. Precautions for pregnancy and lactation: 1. This product can cross the blood-placental barrier to the fetus, and animal experiments have found that it has teratogenic effects. There is a lack of sufficient data in human studies, and pregnant women should avoid using it. 2. This product can be secreted in breast milk, and the concentration in breast milk can reach about 50% to 100% of the maternal blood drug concentration. The drug may affect the baby. The use of this product in newborns with glucose-6-phosphate dehydrogenase deficiency may lead to hemolytic anemia. In view of the above reasons, this product should not be used by lactating women. Elderly patients are more likely to experience serious adverse reactions when using this product: such as severe skin allergic reactions such as rashes, and blood system abnormalities such as bone marrow suppression, leukopenia and thrombocytopenia. It is more likely to occur when using diuretics at the same time. Therefore, elderly patients should avoid using this product. If there is an indication, the decision should be made after weighing the pros and cons.

Drug Interactions

1. 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. 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 or 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. Combination with bone marrow suppressive drugs may enhance the adverse reactions of such drugs to the hematopoietic system. Such as leukopenia and thrombocytopenia, etc. If there is an indication for the combination of the two drugs, possible toxic reactions should be closely observed. 5. Long-term combination with contraceptives (estrogens) can 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, increasing the risk of crystalluria. 11 This product can replace the plasma protein binding site of phenylbutazone, and when the two are used together, it can enhance the effect of phenylbutazone. 12 When sulfinpyrazone is used in combination with this product, it can reduce the latter's secretion from the renal tubules, and its prolonged increase in blood concentration is prone to toxic reactions. Therefore, the dose of this product may need to be adjusted during or after the application of sulfinpyrazone. When the course of sulfinpyrazone treatment is long, the blood concentration of this product should be monitored to help adjust the dose and ensure safe medication. 13 The TMP in this product can inhibit the metabolism of warfarin and enhance its anticoagulant effect. 14 The TMP in this product can enhance 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 blood elimination half-life (t1/2b) 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 when used in combination. 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

Store in a cool, dry place.

Packaging Specification

2ml: sulfamethoxazole 0.4g and trimethoprim 80mg

Validity Period

24 months

Manufacturer

Shanghai Modern Hasen (Shangqiu) Pharmaceutical Co., Ltd.

  • Founded in:

    1999-11-12
  • Address:

    No. 166, North side of Xinxing Road, west side of Zhenxing Road, Liangyuan District, Shangqiu City
  • Tax NO.:

    91411400716735619N
  • Registered Funds:

    83.29 million yuan
  • Website:

  • Email:

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