Albhimazole_Kain Industrial Additives

Albendazolecommonly known as albendazole, is an efficient, safe, broad-spectrum imidazole fungicide, effective against a variety of It has significant control effect on plant diseases and can prevent and cure mosaic diseases of various plants in the seedling stage. It can also prevent and control black shank, powdery mildew, brown spot, anthracnose, bacterial wilt on tobacco, rice blast and sheath blight, wheat powdery mildew, scab, rust, and frost on leafy vegetables such as rape and cabbage. Mildew, powdery mildew, leaf spot, soft rot, sclerotinia, anthracnose, powdery mildew, damping-off and blight of melons and beans, root rot of peanuts, passionflower, onions and ginger, Bacterial wilt, blight, leaf spot, powdery mildew, anthracnose, canker of tomatoes, grapes, bananas, citrus, etc., cotton anthracnose, damping off, blight, and various boll-stage diseases, leaves of mulberry and tea trees Spot, anthracnose, cataplexy, star disease. It can block the parasite's absorption of various nutrients and glucose, causing the glycogen depletion of the parasite, making the parasite unable to survive and reproduce. It is suitable for getting rid of roundworms, pinworms, hookworms, and whipworms, and treating various types of cysticercosis. It can also be used to deworm livestock.

Chinese alias

Albendazole; 5-propylthio-1H-benzimidazol-2-ylcarbamate; methyl ester; albendazole; albendazole; anti-peristaltic; alkylimidazole

Treatment of swine cysticercosis

Albendazole is a derivative of benzimidazole. It was launched in the United States in 1976 and was successfully imitated by the China Veterinary Drug Supervision Institute in 1979. It is a new type of high-efficiency, broad-spectrum, and low-toxic benzimidazole antihelminthic drug. In recent years, in-depth research has been conducted on albendazole from the aspects of drug metabolism, animal mechanics, toxicity, and clinical efficacy. The results show that its anthelmintic spectrum, efficacy and toxicity are superior to other antihelmintic drugs currently in production, and the drug has now become one of the main drugs for the treatment of swine cysticercosis.

Pharmacokinetics in pigs

Albhimazole is quickly metabolized by microsomal enzymes in the microsomes of pig liver cells after being absorbed, and its metabolic intermediates are It is albendazole sulfone and albendazole sulfoxide, and the final metabolite is diaminosulfone. The drug's activity against pig cysticercosis is likely to be borne by sulfoxides and sulfones. After oral administration to pigs, albendazole is absent or only present in trace amounts in plasma. This result is consistent with the fact that the prototype drug of albendazole was not found in blood concentration studies of horses, cattle, sheep, dogs, rabbits and other animals and humans after oral administration. Albhimazole is only a "prodrug", and its intermediate metabolites (sulfoxide and sulfone) can be distributed to various tissues and organs in the pig body with blood circulation, thereby effectively killing pig cysticercosis.
Albhimidazole can diffuse through the parasite capsule tissue (such as echinococcosis), and the drug concentration in the cyst fluid reaches 22% of the drug concentration in the patient's plasma, and the metabolites of the drug last longer in the cyst fluid than in the plasma. In the long run, the concentration of the drug in the cyst fluid depends on the dose administered.

Toxicity to pigs

Taking it once at a dose of 120-155mg/kg has no obvious effect on the pig's spirit, body temperature, appetite, stool, white blood cell count and other indicators. However, long-distance transportation and other stress factors can affect the drug resistance of pigs. Often the critical therapeutic dose becomes a toxic dose. After oral poisoning of pigs, the main clinical manifestations are loss of appetite, repeated vomiting, small amount of vomiting, yellow viscous liquid, and even death. The metabolic intermediate product of albendazole, sulfoxide, is embryotoxic to rats. Therefore, for safety reasons, pregnant women should avoid eating pork when taking albendazole.

Although the drug has obvious therapeutic effects on porcine cysticercosis, due to the inconsistent administration routes, methods and dosages, the therapeutic effects vary greatly. Poisoning, death and poor treatment effects have also occurred in some places. Both oral and intramuscular injection methods are effective in treating pigs with cysticercosis using albendazole. Generally, for pigs under 75kg, albendazole oil suspension can be injected intramuscularly once at 80mg per kilogram of body weight. It saves time and effort, has few side effects, is safe and reliable, and albendazole oil suspension is slowly absorbed and can be used for a long time. Maintain a certain concentration for a long time to exert its insecticidal effect. However, the treatment effect of injection method for large pigs weighing more than 75kg is unsatisfactory due to the large dosage and poor absorption. Therefore, it should be taken orally. The drug is quickly absorbed after oral administration, and the sulfoxide and sulfone in the blood can be maintained for at least 90 hours. Therefore, it is advisable to take the oral medication once every 2 days and divide the total dose into 3-4 doses. The use of this medicinal method not only has few side effects, but also has a good therapeutic effect on pig cysticercosis.

Preparation

Albendazole is prepared by substitution of o-nitroaniline and thiocyanate, propylation with propyl bromide, and reduction and cyclization.

Adverse reactions and side effects

Nausea, dizziness, insomnia, dry mouth, fatigue, chills, stomach discomfort, mild abdominal pain, loss of appetite, etc., mostly occur 2-3 days after taking the medicine , in mild cases, it disappears within a few hours, and dizziness and fatigue can last for 2-3 days, with an incidence rate of 6-14.9%.
When treating ascariasis, 2% of cases develop a reaction of spitting out roundworms at the mouth
Treatment of cysticercosis, especiallyCerebral cysticercosis is mainly related to the release of heterosexual proteins after the death of cysticercosis. It usually occurs 2 to 7 days after taking the medicine. Headache (53.7%), low-grade fever (22.7%), rash, muscle aches, visual impairment (4.3%), Epileptic seizures (13.3%), etc., corresponding measures must be taken (adrenocortical hormone application, intracranial pressure reduction, anti-epileptic treatment, etc.). There have been reports of death due to brain herniation during treatment in China.
In the treatment of cysticercosis and hydatid disease, due to the larger dosage and longer course of treatment, alanine aminotransferase may increase, which will gradually return to normal after drug withdrawal.

Production Unit

Guizhou Daoyuan Technology Co., Ltd.; Hangzhou Pharmaceutical Factory; Rongchang Veterinary Drug Raw Materials Co., Ltd.; Jiangsu Jintan Experimental Chemical Factory.

Keywords: Albendazole, Albendazole, Treatment of swine cysticercosis