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Ribavirin (RBV, Ribavirin) is a synthetic broad-spectrum antiviral drug, is the first choice for the treatment of viral infections for many years, because of its exact effect, cheap, clinical commonly used in infants, children and adults influenza, diarrhea, and combined with interferon for the treatment of various hepatitis. Ribavirin has obvious inhibitory effect on a variety of RNA and DNA viruses, and also has a strong inhibitory effect on HIV virus. The antiviral mechanism of ribavirin has not been fully determined, and the mechanism of action on different viruses is different.
Uses of Ribavirin.
Ribavirin is widely used in medicine. It has high curative effect on hepatitis A, influenza, herpes, respiratory synsporal virus, human immunodeficiency virus, epidemic hemorrhagic fever virus infection, skin diseases and so on. Ribavirin is the only effective drug for the treatment of respiratory synsporal virus and is the first choice for the treatment of epidemic hemorrhagic fever. In recent years, its application in hepatitis B, hepatitis C has also shown better results in India, the drug was approved for the treatment of acute hepatitis, respiratory infections and herpes simplex infection, in the United Kingdom, Switzerland, Italy, the United States and other countries to approve it as AIDS prevention drugs, in 2003 was used in Canada and Hong Kong as a pre-treatment of SARS virus.
Broad-spectrum antiviral drugs, used for influenza (influenza virus A and B caused by), adenovirus pneumonia, hepatitis A, herpes, measles, etc., have prevention and control effects; It is effective against epidemic hemorrhagic fever. It is especially effective for early patients. Oral can cause diarrhea, no other obvious toxicity, but can have leukopenia, excessive dose inhibit hemoglobin and red blood cell maturation and lead to reversible anemia. Teratogenic embryo toxicity has been reported in animal experiments, and pregnant women should refrain from using it.
Pharmacological action of Ribavirin.
1. Ribavirin is phosphorylated in red blood cells to produce riboside monophosphate, diphosphate and triphosphate. Triazole riboside monophosphate is a powerful inhibitor of inosine monophosphate dehydrogenase, which can inhibit the synthesis of cellular guanylate, reduce the triphosphorylation of cellular guanylate, and block the synthesis of viral nucleic acid.
2. Riboside triazole triphosphate inhibits influenza virus RNA polymerase and interferes with viral replication.
3. Riboside triphosphate inhibits the synthesis and transcriptase of the 5 'terminal of viral MRNA, thus inhibiting DNA and RNA synthesis. It can inhibit a variety of viruses (including DNA-type viruses and RNA-type viruses). It is effective against influenza, adenovirus pneumonia, hepatitis A, herpes, measles, etc. It is also effective against epidemic hemorrhagic fever.
4, mainly excreted in the urine in its original form, there are also a small amount of desugarized triazolium riboside metabolites, a small amount of excretion from the stool.
Product Method of Bulk Ribavirin Powder.
Using nucleoside or nucleotide as raw materials, guanosine and guanosine are hydrolyzed under the action of glacial acetic acid and acetic anhydride to produce ribo-1-phosphate, and then react with triazide acetamide to form condensation under the catalysis of di-p-nitrophenol, which is obtained by ammonolysis. Guanosine (or guanylic acid) [acetic anhydride, glacial acetic acid]→[hydrolyzed] ribo-1-phosphate [bis -(p-nitrophenol) -phosphate]→[triazide carboxyamide] condensation [amolysis]→ triazole ribosidase synthesis first hydrolyzes guanosine and guanylic acid under the action of pyrimidine nucleoside phosphorylase to produce ribo-1-phosphate, Then, under the action of purine nucleoside phosphorylase, it reacts with triazide acetamide to directly produce triazolidine riboside. Guanosine (or guanylic acid) [pyrimidine nucleoside phosphorylase]→ ribo1-nucleic acid [purine nucleotide mutase]→ triazole riboside.
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