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Ivermectin is a new broad-spectrum, highly effective, low-toxicity antibiotic antiparasitic drug, which has good anthelmintic effect on both internal and external parasites, especially nematodes and arthropods.
However, it is ineffective against tapeworms, trematodes and protozoa. The anthelmintic effect of macrolides on nematodes and arthropods lies in the increase of the release of the inhibitory transmitter γ-aminobutyric acid (GABA) in worms, as well as the opening of glutamate-controlled Cl ion channels and the enhancement of the permeability of nerve membranes to Cl, thus blocking the transmission of nerve signals, and ultimately nerve paralysis, so that the muscle cells lose the ability to contract, which leads to the death of the worms.
Uses of Ivermectin.
Antiparasitic agent with anthelmintic activity against nematodes, hookworms, roundworms, helminths, insects and mites
Effective in the treatment and control of onchocerciasis, with fewer adverse effects than etanercept.
White or slightly yellow crystalline powder, soluble in methanol, esters and aromatic hydrocarbons, insoluble in water. It is an antibiotic drug with repellent activity against nematodes, insects and mites. Injections and tablets made with ivermectin are mainly used for the treatment of gastrointestinal nematodes, cowhide fly maggots, tattoo fly maggots, sheep nose fly maggots in livestock and scabies mites in pigs and sheep. In addition, ivermectin can also be used for the treatment of poultry body parasitic nematodes (such as roundworms, lung nematodes, etc.).
Can also be made into agricultural insecticides, acaricides, used to kill a wide range of parasitic mites on plants, cabbage moths, cabbage greenfly, leaf miner flies, woodlice, nematodes and so on.
The outstanding features of the drug are: light side effects, a single application of the drug at the same time to kill a variety of parasites in vivo and in vitro.
Pharmacological Effect of Ivermectin.
It has a killing effect on microfilariae, the exact mechanism of which is not known. It may act as an agonist of the neurotransmitter γ-tyrosine (GABA), disrupting the GABA-mediated synaptic transmission process in the central nervous system, leading to death by paralysis of the worm's nervous system.
Although Ivermectin has no effect on adult worms, it can affect the normal development of microfilariae of Onchocerca volvulus in the uterus of female worms and inhibit their release from the uterus of pregnant worms. The effect of Ivermectin on microfilariae is slower and more persistent than that of Ethamizine.
It can rapidly reduce the number of microfilariae in the skin of the patient, but its action on microfilariae in the cornea and anterior chamber of the eye of the patient is slower, and the number of microfilariae in this part of the body decreases rather slowly.
Production methods of Bulk Ivermectin Powder.
Obtained by hydrogenation of the corresponding compound (I) in benzene, tris(triphenylphosphine)rhodium chloride catalysed at room temperature under atmospheric pressure.
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