ARBIDOL HYDROCHLORIDE

Product information

English Name：Arbidol hydrochloride

English Alias：6-Bromo-4-[(dimethylamino)methyl]-5-hydroxy-1-methyl-2-[(phenylthio)methyl]-1H-indole-3-carboxylic acid ethyl ester monohydrochloride

Chinese Name：盐酸阿比多尔

Chinese Alias： 盐酸阿比朵尔；6-溴-4-(二甲氨甲基)-5-羟基-1-甲基-2-(苯硫甲基)-1H-吲哚-3-羧酸乙酯盐酸盐

CAS号：131707-23-8

Formula：C22H26BrClN2O3S

Molecular weight：513.88

Appearance：Off-white or light yellow crystalline power, bitter taste

Purity：98.0%102.0%

Use&Pharmacology

The chemical name of Arbidol Hydrochloride (AH) is 6-bromo-4- (dimethylaminomethyl)-5-hydroxy-1-methyl-2- (phenylthiomethyl) -1H-indole- Ethyl 3-carboxylate hydrochloride, of which hydrochloric acid is used as a stabilizer for Arbidol, mainly used for the prevention and treatment of influenza A and B and other respiratory virus infections. It has convenient oral administration, high safety and compliance. Good, no cytotoxicity and other advantages, it has a wide range of application prospects, and it has also become a research focus of domestic and foreign scholars in recent years.

Arbidol is suitable for adults and children with influenza A, influenza B, acute viral respiratory infections, severe acute respiratory disease syndrome, including the prevention and treatment of complicated bronchitis and pneumonia. Early use of Arbidol hydrochloride after the onset of influenza can significantly shorten the duration of the disease and reduce the severity of symptoms. It is useful for improving cough, headache, fever, chills, sweating, sore throat, muscle aches and fatigue, etc. The symptoms have obvious effects, and the safety is good, suitable for clinical promotion and use. Usage and dosage: 100 mg/capsule, orally, 2 capsules each time for children over 13 years old and adults, 1 capsule each time for children 6-12 years old, and 50 mg orally for 2-6 years old. Treatment: 3 times a day for 3 to 5 days. Prevention: Take it once every 3 days during the flu epidemic period for 3 weeks; take it once a day for high-risk people who come into contact with the patient for 2 weeks.

Arbidol hydrochloride has a carboxylic acid ester structure, so it may be a carrier prodrug. The structure of this drug is mostly lipophilic. As a hydrolyzed substrate, the carrier is removed by simple hydrolysis in the body to form active compounds and accumulate in the cell, and finally play a pharmacological effect. The mechanism of action of Arbidol hydrochloride is through activation 2,5-oligoadenylic acid synthase specifically prevents the contact, adhesion and fusion between the influenza virus envelope and the cell membrane of the host cell, thereby blocking the replication of the influenza virus, and can penetrate the nucleus to directly inhibit the viral RNA and DNA Synthetic; on the other hand, it has the properties of immune regulation, interference induction and anti-oxidation, induces host cells to produce interferon, stimulates humoral response and phagocytosis of macrophages, causes cellular immunity and humoral immunity, and speculates its antiviral effect It is closely related to improving immune function. Anti-infective mechanism: acidic environment (pH 5.0) is a necessary condition for influenza virus to mediate fusion. A slight increase in pH will prevent the fusion process. Water-soluble Arbidol is a weakly alkaline drug. It can increase the pH of the endosome in the host cell, so that the virus cannot complete the process of membrane fusion to release the viral genome, and effectively inhibits HCV that also belongs to the Orthomyxoviridae family. Acute and chronic infections

Arbidol hydrochloride is less toxic. Foreign literature reports that a single oral dose of 2000 mg/kg in rats and guinea pigs is well tolerated, with LD50>3000 mg/kg. The oral LD50 of mice is 340mg/kg. Chronic toxicity test: 100～125mg/kg for rats and 25 mg/kg for dogs. Oral administration for 6 months, no pathological changes occurred. Long-term medication is safe for rabbits and guinea pigs. Both in vivo and in vitro experiments show that it has no mutagenic effect. Reproductive toxicity studies in rats indicate that this product has no teratogenic effects. LD50>4g/kg, according to the recommended dosage, it will not cause any adverse effects on the human body.

Adverse reactions

The incidence of adverse events was about 6.2%, mainly manifested as nausea, diarrhea, dizziness and increased serum transaminase. Chen Qiyou and others conducted pharmacological studies on the safety of Arbidol, and the results showed that Arbidol hydrochloride is clinically used to prevent and treat influenza, severe respiratory infections, complicated bronchitis and pneumonia. The clinical dosage is: the preventive dosage is 100-200mg/d; the therapeutic dosage is 800mg/d. The experimental results showed that the mice taking Arbidol hydrochloride 10, 50, 250 mg/kg orally, except for 250 mg/kg (20 times the clinical dosage) has a synergistic sleep effect with pentobarbital sodium, it has a general effect on mice. There were no obvious effects on behavior, righting reflex, autonomous activities, sensory and memory functions. The intragastric administration of Arbidol hydrochloride at 10, 30, and 90 mg/kg has no significant effect on the body temperature of rabbits; the intragastric administration of Arbidol hydrochloride at 20 mg/kg and 80 mg/kg affects the respiratory frequency and amplitude, systolic blood pressure and Diastolic blood pressure, heart rate, heart rhythm, QRS wave, T wave, ST segment and PR interval of ECG have no obvious effect; Arbidol hydrochloride has no effect on the central nervous system, respiratory system and cardiovascular system.

Package&Storage

Package：1kg/bag, 10kg/drum, 25kg/drum (on request)

Storage&Validity：Cool, shading, dry and sealed/2years