Ribavirin glucose injection

【Drug name】

 Common Name：Ribavirin glucose injection

 English name：Ribavirin and Glucose Injection

 Pinyin in Chinese：Libaweilin Putaotang Zhusheye

【Ingredients】

 The main component of this product is ribavirin, and its chemical name is: 1-β-D-ribofuranosyl-1H-1, 2, 4-triazole-3-carboxamide.

Molecular formula：C₈H₁₂N₄O₅

 Molecular weight：244.21

 Excipient name: glucose and water for injection.

【Sexual】This product is a colorless and clear liquid.

【Indications】

 Antiviral drugs. Used for viral pneumonia and bronchitis caused by respiratory syncytial virus.

【Specification】100ml: Ribavirin 0.5g and glucose 5g

【Adverse reactions】

The most important toxicity of ribavirin is hemolytic anemia, which shows a decrease in hemoglobin, red blood cells, and white blood cells within the first 1-2 weeks after oral treatment. About 10% of patients may be accompanied by cardiopulmonary side effects. Hemoglobin should be monitored frequently before and after treatment and during treatment. This product is not recommended for patients with thalassemia and sickle cell anemia. This product should not be used in patients with symptoms of pancreatitis or have clear pancreatitis. It has been reported that using this product can cause fatal or non-fatal myocardial damage in patients with anemia, so patients with a history of heart disease or obvious symptoms of heart disease should not use this product. If any symptoms of heart disease worsening occurs when using this product, the medication should be stopped immediately and given corresponding treatment.

General systemic adverse reactions observed in clinical trials using ribavirin (including oral preparations) include: fatigue, headache, weakness, fatigue, chest pain, fever, chills, flu symptoms, etc. Neurological symptoms: dizziness; digestive system symptoms include loss of appetite, stomach discomfort, nausea and vomiting, mild diarrhea, constipation, indigestion, etc.; musculoskeletal system symptoms include muscle pain and joint pain; mental system symptoms include insomnia, mood, irritability, depression, attention disorder, neuroticism, etc.; respiratory symptoms include dyspnea, rhinitis, etc.; hair loss, rhinitis, etc. in the skin attachment system; abnormal taste and abnormal hearing were also observed.

In general doses, the side effects of this product are rare, mainly reversible anemia, which can recover slowly after stopping the medication; a few patients experience thirst, loose stool, stomach pain, insomnia, and dryness; in large doses, it can inhibit hemoglobin synthesis, hemolysis, reticulocyte growth, pneumothorax, asphyxia, hypotension, etc. Occasionally, there are loss of appetite, mild gastrointestinal reactions, dizziness, headaches and rashes.

【Forbidden Taboo】

 1、It is prohibited for those who are allergic to any ingredient in this product.

 2、It is forbidden for pregnant women.

 3、Contraindicated for patients with autoimmune hepatitis.

 4、Active tuberculosis should not be used.

【Pharmacology and Toxicology】

 Pharmacological effects     

Ribavirin is a synthetic nucleoside antiviral drug. In vitro cell culture assays show that this product has a selective inhibitory effect on respiratory syncytial virus (RSV). The mechanism of action of this product is not clear, but the results of its in vitro antiviral activity being reversed by guanine nucleosides and oxalinine nucleosides suggest that this product may act as a metabolic analog of these cells.

Toxicological research

Repeated dosage toxicity: When the dosage of this product is 30, 36 and 120 mg/kg orally, and the dosage time is 4 weeks or longer, it can cause heart damage.

 Genotoxicity:

 The concentrations of this product are 0.015 and 0.03-5.0 mg/ml, respectively. Under the condition of no metabolic activators, cell transformation and mutation of mouse Balb/c3T3 (fibroblasts) L5178Y (lymphoma) can be increased. The concentration range is 3.75-10.0 mg/ml. Under the condition of adding metabolic activators, the mutation rate of L5178Y cells has a certain increase (3-4) times. The results of the mouse micronucleus test show that when the dose range of this product is 20-200mg/kg intravenously, it has a cleavage-induced effect. In the dominant lethal test, the dose range of this product intraperitoneal injection of rats was 50-200 mg/kg, and there was no mutagenic effect for 5 consecutive days.

Reproductive toxicity：

When the dose range of male mice is 35-150 mg/kg, it can lead to significant verb atrophy, a decrease in sperm concentration and an abnormal morphology increase in sperm count. After quitting the medicine, the sperm production ability is partially restored. Several other toxicity tests also suggest that when the dosage of this product is less than 16 mg/kg orally given to adult rats, it can cause testicular damage (vasculogenic atrophy), and no lower dose studies were conducted. The reproductive capacity of male animals has not been studied yet. Animal studies of different species have confirmed that this product has obvious teratogenic and/or embryo killing potential toxicity. The dose of this product was 2.5 mg/kg or greater in a single dose of hamsters, and the doses of rabbits and rats were 0.3 and 1.0 mg/kg respectively. The results have been confirmed to have teratogenic effects. Deformities mainly occur in the skull, palate, eyes, limbs, jaw, bones and gastrointestinal tract, and their incidence and severity increase with the increase in dose. The survival rate of fetus and offspring is reduced. The dose of this product that causes embryo lethality in rabbits and rats is 1 mg/kg, and the doses without teratogenicity are 0.1 and 0.3 mg/kg, respectively (calculated based on body surface area, it is equivalent to the human equivalent doses 0.015 and 0.04 mg/kg, respectively).

 Carcinogenicity: Long-term study results of rats administered with doses of 16-200 mg/kg suggest that this product may induce benign breast, pancreatic duct, pituitary gland and adrenal tumors. The 18-24-month preliminary carcinogenic trials in mice and rats were not the final result, but these trials confirmed that the doses given to this product were 20-75 and 10-40 mg/kg, respectively. The vascular damage and retinal reductase degeneration in mice and rats were related to long-term administration of this product.

【Pharmacokinetics】800 mg of ribavirin was intravenously intravenously intravenously. After 5 minutes, the plasma concentration (μg/ml) was 17.8±5.5, and 42.3±10.4 in 30 minutes. Ribavirin enters the body and is quickly distributed to various parts of the body. The concentration in respiratory secretions is mostly higher than the blood drug concentration. It can also pass through the blood-brain barrier. After long-term medication, the drug concentration in the cerebrospinal fluid can reach 67% of the blood drug concentration during the same period. This product can accumulate in red blood cells for several weeks, and can enter the milk through the placenta. It has little binding to plasma proteins. Metabolism in the liver is mainly excreted through the kidneys. Intravenous administration within 0-48 hours, 16.7%±10.3% of the drugs were excreted from the urine as the original drug, and 6.2%±1.7% were excreted as metabolites. The elimination in the body was slow, and the medication was stopped for 4 weeks and it could not be completely removed from the body.

【Storage】 Shade, seal, and store in a cool place.

【Package】 Glass infusion bottle    100ml×100 bottles/box

【Valid period】24 months

【Implementation standards】Chinese Pharmacopoeia 2020 Edition Part Two

【Approval number】 National drug approvalH20063255

【Drug marketing authorization holder】/【Manufacturing enterprises】

name：Guizhou Tiandi Pharmaceutical Co., Ltd.

address：No. 6 Baokang Road, Hongxing Pharmaceutical Industrial Park, Dingxiao Town, Xingyi City, Qiannan Buyi and Miao Autonomous Prefecture, Guizhou Province

 postal code：562400

 tel：0859-3119928

 fax：0859-3118152

 website：www.gztiandi.com