Pharmacological action The urea derivative of this product has the effect of killing African trypanosomiasis and onchocerciasis adults, but it is ineffective against microfilaria. The mechanism of killing microfilaria may be that its negative ion charge combines with the anode of worm protein to form a solid complex. In addition, it can inhibit the sugar metabolism of insects.
Pharmacokinetics is a polyanionic compound, which has poor intestinal absorption after oral administration and must be injected intravenously. This product cannot penetrate the blood-brain barrier. It is mainly excreted in urine, and the original drug that has not been metabolized can be measured in urine 3 months after the last administration.
Indications are mainly used to treat trypanosomiasis in Gambia and Rhodesia in early Africa. It can also be used to treat onchocerciasis, preferably with ethambutol to kill microfilaria. This product is ineffective against Bancroft and Malayan filariasis.
The usage and dosage of trypanosomiasis treatment are: 5 mg/kg, 1, 3,5, 1 1,17,23,30 days respectively. In the treatment of onchocerciasis, it is best to use ethambutol for a course of treatment to reduce microfilaria, and slowly inject 3.3 mg/kg, 6.3 mg/kg, 1 0/3.3 mg/kg, and 65.3 mg/kg at/kloc-0, 2, 3, 4, 5 and 6 weeks respectively.
Common adverse reactions include fatigue, fatigue, nausea, vomiting, polyuria, oral drinking, itching, urticaria, tenderness of palms and soles, etc. , this is mild. Serious adverse reactions include collapse, gastric ulcer, exfoliative dermatitis, severe diarrhea, long-term high fever and failure, proteinuria, agranulocytosis, hemolytic anemia and so on. Allergic reactions after killing parasites include swelling and pain in parasitic parts of adults, rash and abscess formation.
Precautions do not apply to people who are allergic to this product, people with liver or renal insufficiency, pregnant women, children under 10 and the elderly and infirm. Be very careful with the first injection. If there is moderate or mild proteinuria, the dosage must be reduced, and those with severe proteinuria and cast must stop treatment immediately. People with mild or moderate onchocerciasis who have no symptoms or eyes are not threatened do not need to use this product.
Specification of powder injection:1g. Sealed and refrigerated, and prepared into 10% water solution for intravenous injection.