Metronidazole
Function and Efficacy
This product is a nitroimidazole derivative that can inhibit the redox reaction of amoeba target=_blank and break the nitrogen chain of the protozoa. In vitro tests have shown that when the drug concentration is 1-2 g/ml, the histolytica amoeba can undergo morphological changes in 6-20 hours and all are killed within 24 hours. When the concentration is 0.2 g/ml, the histolytica amoeba can be killed within 72 hours. This product has a strong effect of killing trichomonas, and its mechanism is unknown. The antibacterial spectrum includes Bacteroides fragilis and other Bacteroides, Fusobacterium, Bacillus aerogenes, Eubacterium, Peptococcus and Peptostreptococcus. Its bactericidal concentration is slightly higher than the inhibitory concentration. Metronidazole kills cells and anaerobic microorganisms growing under hypoxic conditions. The metabolites generated when it is reduced in the human body also have anti-anaerobic effects, but have no effect on aerobic bacteria and facultative anaerobes. The nitroreductase of anaerobic bacteria plays an important role in the energy metabolism of sensitive strains. The nitro group of the drug is reduced to a cytotoxic substance, which acts on the bacterial DNA metabolism process, inhibits the synthesis of bacterial deoxyribonucleic acid, interferes with bacterial growth and reproduction, and ultimately leads to cell death. Drug-resistant bacteria often lack nitroreductase.
Ingredients
The main ingredient is metronidazole, and its chemical name is 2-methyl-5-nitroimidazole-1-target=_blank ethanol.
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| MetronidazoleIngredients |
This product is a nitroimidazole derivative that can inhibit the redox reaction of amoeba and break the nitrogen chain of the protozoa. In vitro tests have shown that when the drug concentration is 1-2μg/ml, the histolytica can undergo morphological changes in 6-20 hours and all are killed within 24 hours. When the concentration is 0.2g/ml, the histolytica can be killed within 72 hours. This product has a strong effect of killing trichomonas, and its mechanism is unknown. The antibacterial spectrum includes Bacteroides fragilis and other Bacteroides, Fusobacterium, Bacillus aerogenes, Eubacterium, Peptococcus and Peptostreptococcus. Its bactericidal concentration is slightly higher than the inhibitory concentration. Metronidazole kills cells and anaerobic microorganisms growing under hypoxic conditions. The metabolites generated when it is reduced in the human body also have anti-anaerobic effects, but have no effect on aerobic bacteria and facultative anaerobes. The nitroreductase of anaerobic bacteria plays an important role in the energy metabolism of sensitive strains. The nitro group of the drug is reduced to a cytotoxic substance, which acts on the bacterial DNA metabolism process, inhibits the synthesis of bacterial deoxyribonucleic acid, interferes with bacterial growth and reproduction, and ultimately leads to cell death. Drug-resistant bacteria often lack nitroreductase. More |
443-48-1 | 39 |
Indication
It is used to treat intestinal and extraintestinal amebiasis (such as amoebic liver abscess, pleural amebiasis, etc.). It can also be used to treat vaginal trichomoniasis, balantidiasis, cutaneous leishmaniasis, guinea worm infection, etc. It is also widely used to treat anaerobic infections.
Usage and Dosage
1. Common dosage for adults (1) Intestinal amebiasis: 0.4-0.6 g once, 3 times a day, for a course of 7 days; extraintestinal amebiasis: 0.6-0.8 g once, 3 times a day, for a course of 20 days. (2) Giardiasis: 0.4 g once, 3 times a day, for a course of 5-10 days. (3) Guinea worm disease: 0.2 g once, for a course of 7 days. (4) Balantidiasis: 0.2 g once, 2 times a day, for a course of 5 days. (5) Cutaneous leishmaniasis: 0.2 g once, 4 times a day, for a course of 10 days. Repeat the course of treatment after an interval of 10 days. (6) Trichomoniasis: 0.2 g once, 4 times a day, for a course of 7 days; suppositories can be used at the same time, 0.5 g inserted into the vagina every night, for 7-10 days. (7) For anaerobic infection, take orally 0.6-1.2g per day, divided into 3 times, for a course of 7-10 days. 2. Common dosage for children (1) For amebiasis, take orally 35-50mg/kg per day, divided into 3 times, for a course of 10 days. (2) For giardiasis, take orally 15-25mg/kg per day, divided into 3 times, for 10 consecutive days; the dosage for treating dracunculiasis, bagworm disease, and trichomoniasis is the same as that for giardiasis. (3) For anaerobic infection, take orally 20-50mg/kg per day, for a course of 10 days.
Adverse Reactions
Adverse reactions occur in 15-30% of cases, with gastrointestinal reactions being the most common, including nausea, vomiting, loss of appetite, and abdominal cramps, which generally do not affect treatment; neurological symptoms include headache, dizziness, occasional paresthesia, limb numbness, ataxia, multiple neuritis, etc., and large doses can cause convulsions. A few cases have measles, flushing, itching, cystitis, dysuria, metallic taste in the mouth, and leukopenia, all of which are reversible and recover on their own after drug discontinuation. 1. Adverse reactions to intravenous administration. The most serious are epileptic seizures and peripheral neuropathy. The latter is mainly manifested by numbness and paresthesia of the extremities. In some cases, peripheral neuropathy persists during long-term medication. Other common adverse reactions include: ① Gastrointestinal symptoms, nausea, vomiting, abdominal discomfort, diarrhea, metallic taste in the mouth; ② Reversible neutropenia; ③ Erythematous rash, urticaria; ④ Central nervous system symptoms, such as headache, dizziness, syncope, ataxia and mental confusion; ⑤ Local reactions such as thrombophlebitis; ⑥ Others include fever and dark urine, which may be caused by the metabolites of this product and seem to have no clinical significance. 2. Adverse reactions during oral administration. ① Gastrointestinal symptoms, such as nausea, anorexia, vomiting, diarrhea, upper abdominal discomfort, abdominal cramps, and constipation. ② Oral: Occasionally there is a significant metallic taste in the mouth, thick tongue coating, glossitis and gastritis, which may be related to the rapid growth of Candida. ③ Blood system: reversible neutropenia and erythrocyte reduction. ④ Cardiovascular: flat T wave on electrocardiogram. ⑤ Central nervous system: epilepsy, peripheral neuropathy, dizziness, ataxia, mental confusion, excitability, depression, fatigue and insomnia. ⑥ Allergy, urticaria, erythematous rash, flushing, nasal congestion, vaginal or vulvar dryness, fever. ⑦ Urinary system: dysuria, cystitis, polyuria, urinary incontinence, dark urine. ⑧ Others: excessive vaginal yeast growth, loss of libido, proctitis, joint pain similar to serum sickness. If you drink alcohol while using this product, you may experience abdominal discomfort, nausea, vomiting, flushing, headache, and change in the taste of alcohol; rare pancreatitis, which disappears after stopping the drug; patients with segmental ileitis who use large doses of long-term medication have an increased incidence of gastrointestinal cancer and breast cancer for unknown reasons. 3. Overdose manifestations: There are reports of oral administration of 27mg/kg of this product, 3 times a day, for a total of 20 days; or the first dose of 75mg/kg, followed by 7.5mg/kg maintenance, with no adverse reactions. An accidental dose of 15g resulted in nausea, vomiting, and ataxia. Patients with malignant tumors use this product as a radiosensitizer, and take 6 to 10.4g every other day. Neurotoxic reactions such as epilepsy and peripheral neuropathy occur 5 to 7 days later. It can cause gastrointestinal reactions such as nausea, vomiting, loss of appetite, abdominal distension, and diarrhea. In some cases, headache, insomnia, rash, leukopenia, numbness, paresthesia, movement disorders, ataxia, mood disorders, and can cause allergic temporary myopia and exfoliative dermatitis. [Cardiovascular system] 6% of patients who inject this drug may develop thrombotic phlebitis. [Respiratory system] This drug was first reported to cause pneumonia. One patient had a history of pollen allergy and had taken oral contraceptives for many years. He suffered from recurrent vaginitis. He developed high fever, cough, conjunctivitis, and maculopapular rash all over his body on the day of treatment with this drug. Chest X-ray examination showed pulmonary infiltration and bilateral pleural effusion. [Nervous system] General doses can cause headache, dizziness, ataxia, depression, and even epileptic seizures, but they are rare. Large doses or long treatment duration may cause severe central nervous system toxicity, such as convulsions, ataxia and confusion, and occasionally peripheral sensory neuropathy. Intravenous medication may cause headache, fever, dizziness and collapse. [Digestive system] Loss of appetite, metallic taste in the mouth, nausea, vomiting, abdominal pain and diarrhea may occur, and the severity of symptoms is mostly related to the dose. [Urinary system] Urethral discomfort and black urine may occur. [Hematopoietic system] There may be mild leukopenia and neutropenia. One case had bone marrow suppression after one week of medication; one case had granulocytopenia, which improved after three days of discontinuation of medication; two cases had aplastic anemia. [Skin] This drug can cause itching and rash. One case had fixed drug eruption and pityriasis rosea-like rash. One patient took 0.4g for the first time, and felt itchy skin all over the body 40 minutes after taking it, followed by the appearance of light red papules of varying sizes on the face, neck, trunk and limbs, which quickly merged into patches when scratched.
Precautions
Patients with active central nervous system diseases and blood diseases are contraindicated. (1) Pregnant women can cross the placenta and quickly enter the fetal circulation. Animal experiments have found that intraperitoneal administration is toxic to the fetus, while oral administration is not toxic. There are no sufficient and rigorous controlled studies on the effects of this product on the fetus, so pregnant women should only use this product when there is a clear indication. (2) The concentration of this product in breast milk is similar to the concentration in blood. Whether the nursing mother stops taking the drug or interrupts breastfeeding depends on the necessity of the drug. If the drug must be used, breastfeeding should be interrupted. (3) The pharmacokinetics of this product are changed when used by adults, so blood drug concentrations need to be monitored. (4) Patients with a history of allergy to this product and other imidazole drugs should not use it. (5) This product is a nitroimidazole drug and should be used with caution by patients with blood dyscrasias. (6) Pregnant and lactating women are contraindicated. (7) The dose should be reduced for patients with pre-existing liver disease. The drug should be discontinued if movement disorders or other central nervous system symptoms occur. Patients with active central nervous system diseases and blood diseases are also prohibited from using this product. Animal experiments have shown carcinogenic, teratogenic, and mutagenic effects. Lactating women, pregnant women within 3 months of pregnancy, and patients with central nervous system diseases and blood diseases are prohibited from using this product. Patients with liver diseases should reduce the dosage.
Drug Interactions
Metronidazole can slow down the metabolism of oral anticoagulants (such as warfarin), enhance their effects, and prolong the prothrombin time. Combination with oxytetracycline can interfere with the effect of metronidazole in clearing vaginal Trichomonas. It inhibits acetaldehyde dehydrogenase, thereby enhancing the effect of ethanol and causing disulfiram reaction. During medication and within 1 week after discontinuation of medication, alcoholic beverages or medicines are prohibited. Abdominal pain, vomiting, headache and other symptoms may occur after drinking. (1) This product can enhance the effects of warfarin and other oral anticoagulants, causing the prothrombin time to be prolonged. (2) Simultaneous use of drugs that induce liver microsomal enzymes such as phenytoin and phenobarbital can accelerate the excretion of this product and reduce the blood drug concentration; while the excretion of phenytoin is slowed down. (3) Simultaneous use of drugs that weaken the activity of liver microsomal enzymes such as cimetidine can slow down the clearance of drugs and prolong the half-life of this product. (4) Patients who use this product and disulfiram at the same time may experience mental symptoms if they drink alcohol, so those who have used disulfiram within two weeks should not use this product again. zhikaoy. This product can prolong the t1/2 of warfarin and enhance its efficacy. Avoid drinking alcohol during medication, otherwise, disulfiram-like effects may occur, manifested as facial flushing, rapid pulse, dyspnea, macules, followed by pale complexion, hypotension, arrhythmia, etc.
Storage
Keep away from light and store in a sealed container.
Manufacturer
Hengcheng Pharmaceutical Group Huainan Co., Ltd.
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Founded in:
1998-10-14 -
Address:
No. 1, Zhenxing Road, Economic and Technological Development Zone, Huainan City, Anhui Province -
Tax NO.:
913404007110463982 -
Registered Funds:
66 million yuan -
Website:
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Email: