|Company Name:||J & K SCIENTIFIC LTD. |
|Ivermectin Chemical Properties|
|Ivermectin Usage And Synthesis|
|Ivermectin poisoning||Ivermectin also called Ivomec, is a kind of medicine that has a good effect on mite disease treatment.It will cause poisoning if were overcommit ted. The symptoms of ivermectin poisoning are as follows: vomiting, accelerated breathing ,weakness and paralysis in arms and legs, and congestive heart failure that would cause death.|
Rescue : Just take orally mung bean licorice drink detoxification with 10% of glucose and inject dexamethasone when necessary.
|Effects of ivermectin||Ivermectin is white or light yellow crystalline powder and soluble in methyl alcohol, ester and aromatic hydrocarbon but water. Ivermectin is a kind of antibiotic medicine which has a driving and killing effect on nematodes, insects and mites. Injection and troche which are made from ivermectin are mainly used in the treatments of livestock’s gastrointestinal nematode, bovine hypodermosis, calf fly maggot, sheep nasal fly maggot, and scabies of sheep and pigs. Besides, ivermectin can also be available for the treatment of plant-parasitic nematodes(ascarid, lungworm) in poultry. In addition, it can also be made into agricultural insecticide to kill mite, plutella xylostella, cabbage caterpillar, leaf miner, phylloxera and nematode which are widely parasitic in plants. The most outstanding feature of this insecticide is that it has little side effects and can drive and kill many kinds of parasites both internally and externally at a time.|
The above information is edited by the Chemicalbook Bai Linlin.
|Botanical pesticide of ivermectin||Ivermectin is a kind of botanical pesticide which is made of cynanchum komarovii, sophora alopecuroides and many other plants and Chinese herbal pieces through grinding, dissolving, adding promoters and penetrant and processing the mixtures. Its action mechanism is mainly based on contact poisoning with stomach toxicity as an complementary, which has a promoting effect on plant growth. It can be used to prevent and kill all kinds of aphids and defoliators. If diluted with water to 1000～2000 times and spayed, its control effect can reach above 98%. Ivermectin is a new generation of botanical pesticide that is low toxicity, low residual and has no hazard to people, livestock and environment.|
The insecticidal mechanism of ivermectin is to inhibit the synthesis of chitin of insect epicutile. The main component of chlorbenzuron is stomach poison, but it can also intrude into insect epicutile and take effect. The prevention and treatment of defoliator has many advantages such as special action mechanism, good effect, long residual period, low cost, tolerant to rain shower, not easy to generate insecticide resistance and safe for plants, human, livestock and environment.
|Instruction of ivermectin||[Pharmacologic action] Ivermectin has killing effects on microfilaria, but its exact mechanism is not clear. It can be used as agonist for neurotransmitter γ-tyrosine(GABA) to break the transfer process of synapses in the central nervous system neurons mediated by GABA, which can lead to death of polypide by paralyzing its nervous system. As for adult insects, ivermectin doesn’t work, but it can affect the normal development of microfilariae of onchocerca volvulus in the female uterus, and can inhibit the release from the pregnant worm palace. Ivermectin has slow and persistent effect on microfilaria compared with diethylcarbamazine. It can quickly reduce the number of microfilariae of patients with the skin. However, it has a relatively slow effect on the larva of patients’ cornea and anterior chamber of eyes, therefore the number of larva in this area declines rather slow.|
[Pharmacokinetics]After taking the medicine orally, blood concentration will reach the peak in 4 hours and T1/2 in 10 hours. Animal experiments showed only l ~ 2% of oral doses appears in the urine in the form of original drug and the others is excreted with excrement. The drug concentration in the liver and adipose is very high, but cannot penetrate the blood brain barrier, while in the nerve cells including GABA the concentration is rather low, hence we rarely see the response of central nervous system after taking medicine.
[Adaptation disease]the main medicine of treating onchocercosis.
[Usage and dosage] Take the medicine orally one hour before the meal. The usual dose of onchocercosis treatment: 0.15- 0.2mg/kg according to the weight, every 6-12 month at a time, depending on the symptoms and the reappear time of microfilaria. It can prevent the further development of ocular disorders(mostly caused by microfilaria), but this can’t be a radical treatment, because it’s inability to kill adult insects.
[Preparation and specification] Ivermectin tablet 6mg
[Untoward effects] Non-infected people and other Mammalian species are well tolerant towards this product. Symptoms like drowsiness, ataxia, mydriasis, tremble and even death will appear when given mega dose of this product to animals. The patients who suffer from onchocercosis may have transience and slight side effect after taking this medicine, most of which are rash and pruritus(caused by the death of microfilaria in the skin), lymphadenopathy(gall, seen in the neck, armpit, and inguen). It is rare to see the symptoms such as swirl, postural hypotension(faint), radiation, headache, joint sore, weakness and so on. There is not much change in ocular lesions. Occasionally, we can see the change of electrocardiogram but the significance is unclear. This product has no carcinogenic and teratogenic effect.
|Chemical properties||Ivermectin contains at least 80% of 22，23-dihydroavermectin B1a and less than 20%22，23-dihydroavermectin B1b. It is white powder. [α]D+71.5°±3°(C=0.755，chloroform). Maximum absorption(methyl alcohol) of UV is 238，245 nm(ε27100，30100). The water solubility is about 4μg/ml and it is easily soluble in methyl ethyl ketone, propylene glycol or polypropylene glycol, but not in saturated hydrocarbon, for example cyclohexane.|
B1a：[71827-03-7]. Ethyl alcohol-water crystallization, melting point: 155～157℃.
|Application||1. Ivermectin is available for controlling and treating onchocerca volvulus, and its untoward effect is lower than that of carbamazine.|
2. Ivermectin can be used as a kind of antiphrastic drug and has an anthelmintic activity towards nematode, hookworm, roundworm, worm, insect and mite.
|Production methods||Under normal pressure and at room temperature, ivermectin can be obtained through the corresponding compounds (I) in benzene hydrogenated and catalyzed by the three (triphenylphosphine) rhodium chloride.
|Chemical Properties||Crystalline Solid|
|Usage||beta-lactamase inhibitor; antibiotic|
|Usage||Semi-synthetic derivative of Abamectin; consists of a mixture of not less than 80% component B1a and not more than 20% component B1b. Antihelmintic (Onchocerca)|
|Biological Activity||Positive allosteric modulator of the α 7 neuronal nicotinic acetylcholine receptor and the purinergic P2X 4 receptor. Antihelmintic. Also modulates glutamate- and GABA-activated chloride channels. Potentiates glycine-gated currents at low concentrations (30 nM).|
|Ivermectin Preparation Products And Raw materials|