GMP manufactured 

BP/USP Tinidazole Sodium Chloride Injection

Generic name: Tinidazole Sodium Chloride Injection

The main component of this product is tinidazole, its chemical name is: 2-methyl-1-[2-(ethylsulfonyl)ethyl]-5-nitro-1H imidazole.

Molecular formula: C8H13N3O4S

Molecular weight: 247.28

[Properties] This product is a colorless or almost colorless clear liquid.

Pharmacology and Toxicology

Pharmacological effects This product has a strong antibacterial effect on most anaerobic bacteria. The antibacterial spectrum includes Bacteroides fragilis and other Bacteroides, Fusobacterium, Peptococcus and Peptostreptococcus, Veillonella and Gardnerella. The concentration of 2~4mg/L can inhibit most anaerobic bacteria; microaerobes and Helicobacter pylori are sensitive to them; MTC to Trichomonas vaginalis is similar to metronidazole, and its metabolites are more active against Gardnerella Metronidazole is enhanced.

The sterilization mechanism of this product has not been fully elucidated. The nitroreductase of anaerobic bacteria plays an important role in the energy metabolism of sensitive strains. The nitro group of this product is reduced to a kind of cytotoxicity, which acts on the cell's DNA metabolism process and promotes the death of bacteria. Drug-resistant bacteria often lack nitroreductase and are resistant to this product. The mechanism of this product against amoeba protozoa is to inhibit its redox reaction and break the nitrogen chain of the protozoa, thereby killing the protozoa.

Toxicological research Animal tests or in vitro tests have found that this product has carcinogenic and mutagenic effects, but it has not been confirmed in humans.

[Pharmacokinetics] The peak plasma concentration of this product after intravenous infusion of 0.8g and 1.6g is 14-21mg/L and 32mg/L. Intravenous drip 1g daily, the blood concentration can be maintained above 8mg/L. Tinidazole is widely distributed in the body. It can reach high concentrations in the reproductive organs, intestines, abdominal muscles, and milk, but low in liver and fat. The concentration in bile and saliva is similar to the blood concentration of the same period. The penetration of the blood-brain barrier is higher than that of metronidazole. When the meninges are not inflamed, the concentration in the cerebrospinal fluid is 80% of the blood concentration in the same period, which is related to the fat solubility of tinidazole. Tinidazole can pass through the blood placental barrier and can reach higher concentrations in the fetus and placenta. The protein binding rate of tinidazole is 12%. Tinidazole is metabolized in the liver. After intravenous administration, 20-25% is excreted in the urine in its original form, and 12% is excreted in the form of metabolites. Elimination T1/2 was 11.6~13.3 hours, with an average of 12.6 hours. The pharmacokinetic indicators of renal insufficiency remain unchanged, but hemodialysis can quickly clear tinidazole, so it must be administered once after hemodialysis.

[Indications] 1. This product is used to confirm or may be derived from Bacteroides, Bacteroides fragilis, other Bacteroides, Clostridium, Peptococcus, Eubacterium, Streptococcus fermentum, and Veillonella The following infections caused by sensitive anaerobic bacteria: severe oral infections (such as severe pericoronitis, severe oral cavity infection); sepsis, sinusitis, pneumonia, lung bronchial infection, skin cellulitis, osteomyelitis, peritonitis, and surgery Wound infection; gastrointestinal and female reproductive system infections.

2. This product can be used for the treatment of intestinal and extraintestinal amoebiasis, vaginal trichomoniasis, giardiasis, Gardnerella vaginitis, etc.

3. This product can be used as an alternative to metronidazole for the treatment of antral gastritis and peptic ulcer caused by Helicobacter pylori.

[Usage and Dosage] Intravenous drip.

1. Infections caused by anaerobic bacteria: 0.8g, once a day, slow intravenous drip, the general course of treatment is 5 to 6 days, or according to the condition.

2. Surgical prevention of infection after surgery: total 1.6g, 1 or 2 intravenous drips, the first time is 2 to 4 hours before the operation, the second time is during the operation or within 12 to 24 hours after the operation Note.

[Adverse reactions] Adverse reactions are rare and mild. Common adverse reactions are nausea, vomiting, loss of appetite, and bad mouth odor. Dizziness, headache, dizziness, skin itching, rash, constipation and general malaise have also been reported. Angioedema, neutropenia, disulfiram reaction, and black urine may also occur. Occasionally, mild phlebitis at the drip site is seen. High doses can also cause seizures and peripheral neuropathy.

[Contraindications] 1. People who are allergic to tinidazole and nitronitrosimidazole derivatives are prohibited.

2 It is forbidden for patients with hematological diseases or with a history of hematological diseases, and for patients with active central nervous system diseases.

3 Women within three months of pregnancy and lactating women are prohibited.

4 It is forbidden or not suitable for patients under 12 years old.

Precautions

1. The dripping speed of this product should be slow, and the dripping time for each bottle should be no less than 2 hours. The drug should not be in contact with aluminum-containing needles and cannulas, and avoid dripping with other drugs.

2. If adverse reactions to the central nervous system occur during the course of treatment, the drug should be stopped in time.

3. This product can interfere with the test results of alanine aminotransferase, lactate dehydrogenase, triglyceride, hexokinase, etc., to reduce the measured value to zero.

4. Alcoholic beverages should not be consumed during medication, because it can cause accumulation of acetaldehyde in the body, interfere with the oxidation process of alcohol, and cause disulfiram-like reactions. Patients may experience abdominal cramps, nausea, vomiting, headache, facial flushing, etc.

5. The metabolism of this product slows down in patients with liver function decline, and the drug and its metabolites are easy to accumulate in the body, so the dose should be reduced and the blood drug concentration monitored.

6. This product can be continuously removed from the gastric juice. Some people who place a gastric tube for suction and decompression can cause the blood concentration to drop. During hemodialysis, this product and metabolites are quickly removed, so there is no need to reduce the dose when using this product.

7. Patients with Candida infection will have worse symptoms after using this product and need to be treated with antifungal drugs at the same time. When treating vaginal trichomoniasis, the sexual partner must be treated at the same time.

[Medicine for pregnant and lactating women]

   This product can quickly enter the fetal circulation through the placenta. Animal experiments have found that intraperitoneal administration is toxic to the fetus, while oral administration is non-toxic. The effect of this product on the fetus has not been sufficiently and closely controlled and observed. Therefore, pregnant women should only use this product when there are clear indications, but it should be disabled within the first 3 months of pregnancy. Patients who are more than three months pregnant should use it with caution or follow the doctor's advice after fully weighing the pros and cons. The concentration of this product in milk is similar to that in blood. Animal experiments show that this product has carcinogenic effects on young mice, so it is not recommended for breastfeeding women. If medication is necessary, breastfeeding should be suspended, and breastfeeding can only be resumed 3 days after the treatment.

Children's MedicationIt is forbidden for patients under 12 years old.

[Medication for elderly patients] The pharmacokinetics of the elderly patients have changed due to decreased liver function, and blood concentration needs to be monitored.

medicine interactions

1 This product can inhibit the metabolism of warfarin and other oral anticoagulants, can strengthen its effect, and cause prothrombin time to prolong.

2 At the same time, phenytoin sodium, phenytoin and other drugs that induce liver microsomal enzymes can be used to enhance the metabolism of this product and reduce the blood concentration, while the excretion of phenytoin sodium is slow.

3 Simultaneous application of cimetidine and other drugs that inhibit liver microsomal enzyme activity can slow down the metabolism and excretion of this product in the liver, and prolong the serum half-life of this product. The dosage should be adjusted according to the results of blood concentration determination.

4 This product interferes with the metabolism of disulfiram, and patients with the combination of the two may have mental symptoms after drinking. Therefore, it is not recommended to use this product again if disulfiram is applied within 2 weeks.

5 This product can interfere with the determination results of serum aminotransferase and LDH, and can reduce cholesterol and triglyceride levels.

[Drug overdose] When this product is overdose, symptomatic treatment (supportive therapy) should be given. Most of this product is excreted in urine, which can increase urine output to speed up the clearance rate.

Since 2015, NINGBO VOICE BIOCHEMIC CO. LTD. is a professional company to offer one-package service for FPP (Finished Pharmaceutical Products ); APIs (Active Pharmaceutical Ingredients); Chemicals (Pharmaceutical Intermediates ); Veterinary Pharmaceuticals.that meet requirements of Standard GMP and current BP,USP version.

We will spare no efforts to meet your demands!