伊維菌素ivermectin（伊維菌素ivermectin）

1、伊維菌素ivermectin（伊維菌素ivermectin）Ivermectinmedical aircraftIvermectin ivermectin is a new broad-spectrum, high efficiency and low toxicity of antibiotics and antiparasitic drugs, especially in vivo of parasite nematode and arthropod animal has good killing effect. But it is invalid for tapeworm, fluke

2、and protozoa. Macrolide antiparasitic drugs on nematode and arthropod animal killing effect is to increase the inhibitory neurotransmitter gamma aminobutyric acid GABA worm) release, and open the Cl ion channel glutamate control, enhance the permeability of nerve membrane to Cl, thereby blocking the

3、 transmission of nerve signals, eventually paralysis, make muscle cells lose their contractile ability, and lead to the parasite.CatalogEnglish namebrief introductionCharacterPharmacology and pharmacodynamicsPharmacokineticspurposeDrug interactionFunction indicationsclinical researchusage and dosage

4、Adverse reactionNote English namebrief introductionCharacterPharmacology and pharmacodynamicsPharmacokineticspurposeDrug interactionFunction indicationsclinical researchUse, dosage, adverse reactions, notes, edit the English name of this paragraphIvermectin IvermectinEdit this paragraph introduction

5、IvermectinBy Streptomyces avermitilis (Streptomyces avermitilis) semi synthetic macrolide antibiotics produced by fermentation of multicomponent. The main content of ivermectin B1 (Bla+B1b) is not less than 93%, which shall not be less than 85% Bla. B1 22,23- dihydro ivermectin avermectin B1Edit par

6、agraph characterThis product is white crystalline powder, tasteless. This product is soluble in methanol, ethanol, acetone and ethyl acetate, almost insoluble in water.Edit this paragraph of PharmacologyPharmacodynamicsBecause the fluke and tapeworm do not use GABA as a transmitter, they lack Cl cha

7、nnels controlled by glutamate. Therefore, this kind of medicine is invalid. Although the peripheral neurotransmitter of mammalian is acetylcholine, although GABA is distributed in the central nervous system, it is very safe because it is not easy to penetrate the blood-brain barrier. The mechanism o

8、f parasite reproductive of this drug class effect is not too clear, but can reduce tick eggs, ruminants nematode eggs and the abnormal morphology of filamentous nematodes (male and female) infertility.PharmacokineticsThe pharmacokinetics of ivermectin for livestock, dosage form and route of administ

9、ration was different. Taking plasma half-life as an example, intravenous injection of 300 g/kg of t1/2 was given to cattle and sheep, although the difference was small (2.8 days and 2.7 days), but the lower plasma concentration was due to the apparent volume of distribution greater than that of catt

10、le. Ivermectin in dogs rapid excretion (t1/2=1.6 1.8 days). The pig has a half-life of 4 days. The United States dedicated to commercial preparations with leather injection (200 g/kg), because of the injection of local slow absorption, while the half-life (t1/2=8 days),.48h blood reached the peak, a

11、ccording to the observation of the clinical efficacy of anthelmintic effect, can maintain 2 weeks. The half-life of sheep after oral administration was 35 days, and the peak value of serum was reached after 24h. The dogs were taken orally (100 g/kg) tablets, and the peak value of blood was reached a

12、t 2 4H (40ng/mL). Time to peak drug pig, oral (0.5 days) than subcutaneous injection (2 days), but subcutaneous bioavailability than oral administration is much higher, usually oral bioavailability when only 41% injection. Two different formulations (paste and aqueous micelles special formulations)

13、of ivermectin orally to the horse, the plasma peak time, not only the aqueous micelle formulation (4 5H) than paste (15h) much faster, but also high bioavailability. (paste is only 20% of aqueous micelles). After the absorption of ivermectin is widely distributed in the body tissue, and the concentr

14、ation of liver and adipose tissue in the highest. Ivermectin is usually in liver oxidized metabolites. Ivermectin in 5 6 days after fecal excretion accounted for more than 90%, the urinary excretion accounted for only 0.5% to 2%.Edit this paragraph for useIvermectin is widely used in cattle, sheep,

15、horse, pig gastrointestinal nematodes, parasitic nematode and arthropod animal lung, canine intestinal nematode,Ear mites, scabies mites, heartworm and microfilariae, and gastrointestinal nematodes and poultry parasites in vitro. (L) 0.2mg/kg according to the amount of ivermectin of cattle and sheep

16、 cattle and sheep to oral or subcutaneous injection of Haemonchus, Ostertagia, Cooper, nematode Trichostrongylus (including Ehrlich trichostrongyle), circular, Bunostomum nematode, nematode Nematodirus, Trichuris, Oesophagostomum, Dictyocaulus and chabertia ovina adult and 4 stage larvae, insect rep

17、ellent rate of 97% 100%. The dose is also very effective on the arthropod animal, such as: maggot flies, cowhide leather fly, fly), sheep (cattle, sheep scabies mite Psoroptes) and lice (cattle, cattle and sheep louse lice palatal palatal lice) etc. Ivermectin for chewing louse (Mao Shishu) and shee

18、p ked efficacy is slightly difference. Ivermectin for ticks and flies breeding in feces is also very effective, agent does not immediately make ticks death or dismemberment, but can affect the feeding, spawning and molting, thereby reducing the reproductive capacity. The above phenomenon was most ob

19、vious at 5 days after subcutaneous injection of 0.2mg/kg or low concentration (0. 01mg/kg) of drugs per day. According to a 0.2mg/kg dose subcutaneous injection has certain influence on reproduction in feces flies, development of adult flies, Musca larvae cannot face cow dung after 9 days of treatme

20、nt, after 5 days, the pupa and adult deformity maturation is blocked the flies breeding is greatly reduced and the blood of flies (haematobia irritans) with the similar dose after 4 weeks. (2) oral ivermectin on adults and 0.2mg/kg were the following genera of large and small round nematode 4 stage

21、larvae (95% 100%) were high; such as large round nematode (common round nematode, nematode, toothless horse round round, ascarid nematodes) (parascaris equorum), pinworm (horse tail nematode), stomach worms (mouth nematodes, soft line de Tracy spp.), intestinal nematodes (Ehrlich trichostrongyle, We

22、bster stercoralis), lung nematode (class Dictyocaulus) etc. On the shift of three bots or gastric residence time, skin damage caused by Onchocerca volvulus microfilariae and stomach worms third stage larvae, although a 0. 2mg/kg volume is also very limited, but the best solution is a month later by

23、the amount of medication once again. Particular significance is the recommended dose of ivermectin (0.2mg/kg) on the early common circular nematodes and fourth stage larvae, the effective rate of the transitional period of the mesenteric artery damage caused by treatment is about 99%, usually after

24、2 days of treatment, the symptoms were relieved, about 28 days of injury symptoms all disappeared. (3) pigs 0.3mg/kg intramuscular injection of ivermectin with broad-spectrum insecticide activity of swine. Such as pig roundworm, red pig cantonensis, Strongyloides ransomI, Salsola first, nematode Oes

25、ophagostomum, C. elegans, crown tail nematodes and immature worms from the rate of 94% 100%, Trichinella spiralis on intestinal (intramuscular invalid) is also very effective. The drug law have good control effect on pig lice and scabies in pigs. (4) dogs and cats have special dosage forms (612 g/kg

26、 g/kg) for the prevention and treatment of the infection of the canine heart worm, which can be treated with 50 mu of oral administration. Clinical trials have shown that high doses of ivermectin on canine parasites efficiently, such as a subcutaneous injection of 50 g/kg of Ancylostoma caninum, Bra

27、zil, European hookworm Ancylostoma caninum, 100 g/kg of canine whipworm, 200 g/kg of Toxocara canis larvae and four adults were very good. Only effect. The efficacy of subcutaneous injection of g/kg was only 69% and 95% for oral administration in 200 cases. This product is a subcutaneous injection,

28、parasitic in the lungs of dogs Capillaria aerophila (200 g/kg), Austria olster nematodes (400 g/kg) also has excellent repellent effect. Oral or subcutaneous injection of 200 g/kg, once again after two weeks, the intestinal fecal nematodes (except third stage larvae), the efficiency of 95% to 100%.

29、Ivermectin for dogs and cats, some arthropod animal infection effectively, dogs and cats, subcutaneous injection of 200 g/kg dose,After two weeks and one time to get rid of ear mites, mites, mites canine lung infection thorn. By 300 g/kg, two times (interval 2 weeks) are effective for the infection

30、of m. According to the best treatment of canine Demodicosis 600 g/kg subcutaneous injection, 7 days interval for 5 times. (5) birds are highly effective in poultry nematodes such as chicken, roundworm and closed insects and poultry parasitic arthropods such as knee mites (mutated knee mites), which

31、are taken orally or subcutaneously at the rate of 200300 g/kg. However, this product is ineffective against the chicken. (6) reindeer reindeer leather maggot (Oedemagena tarandi) infection, according to the amount of cattle (200 g/kg) subcutaneous injection can be.Edit this episode of drug interacti

32、onDifferent adjuvants can affect drug containing ivermectin in commercial preparations, such as oral preparations containing -80 sheep Twain adjuvant, ivermectin dosage was 4000 g / kg, is still very safe, but if the propylene glycol adjuvants do so that when the sheep for 3 days of ataxia and blood

33、 red urine protein. The United States -80 Twain do adjuvant Ivermectin Injection is a special commodity animal preparation, but not for the dog, or is also extremely unsafe.Edit this paragraphThis product is a derivative of avermectin, which is a semi synthetic broad-spectrum anti parasitic agent. T

34、his product acts on most nematode species (but not all nematodes) in all life cycles, but is effective in the treatment of adult worms, but not for adults, and for intestinal nematodes only in the gut. This product has a selective inhibitory effect, combined with non neural cells and spinal glutamat

35、e animal muscle cells to high affinity chloride channel of the valve, resulting in an increase of chloride ion permeability of cell membrane, causes the nerve cells or muscle cell hyperpolarization, the parasite paralysis or death. This product can also interact with other ligand valves (such as neu

36、rotransmitter g-, aminobutyric acid (GABA) and chloride channels. The selectivity of this product is because some mammals do not have glutamate chloride channels, and avermectin has only low affinity for mammalian ligand chloride channels. This product can not penetrate the blood-brain barrier. Onch

37、ocerciasis and strongyloidiasis, Ascaris lumbricoides, hookworm and pinworm infection.Edit this section of clinical researchindications for onchocerciasis and strongyloidiasis, Ascaris lumbricoides, hookworm and pinworm infection. chemical composition this product is the main component of ivermectin

38、 B1a and ivermectin B1b, B1a chemical called ivermectin (5-O- to methyl -22, 23- dihydro avermectin A1a; B1b) a chemical called ivermectin (5-O- to methyl -25- (1- methyl propyl) to -22, 23- double hydrogen. pharmacological effects 1, pharmacological action, this product is a derivative of avermecti

39、n, oral semi synthetic broad-spectrum anti parasitic drugs. This product acts on most nematode species (but not all nematodes) in all life cycles. It is effective for adults, but not for adults, and for nematodes that are only in the intestines. This product has a selective inhibitory effect, combin

40、ed with non neural cells and spinal glutamate animal muscle cells to high affinity chloride channel of the valve, resulting in an increase of chloride ion permeability of cell membrane, causes the nerve cells or muscle cell hyperpolarization, the parasite paralysis or death. This product can also in

41、teract with other ligands, valves (such as neurotransmitter gamma aminobutyric acid (GABA), chloride channels. The selectivity of this product is because some mammals do not have glutamate chloride channels, and avermectin has only low affinity for mammalian ligand chloride channels. This product ca

42、n not penetrate the blood-brain barrier. 2 、 toxicology study genotoxicity: only in vitro mutagenicity test, the results have not found that this product has genetic toxicity. Reproductive toxicity: no significant effect on animal fertility was found at 3 times the maximum recommended dose in rats.

43、The doses of mice, rats and rabbits were 0.2, 8.1 and 4. of the maximum recommended dose, respectively5 times (with body surface area meter), show that this product has teratogenic effect. There are two kinds of animal palate, rabbit also appeared clubbing paws. These effects occur when close to the

44、 maternal toxicity dose. Therefore, this product is clearly not selective fetal toxicity, however, there is insufficient and rigorous data on maternal studies to confirm the safety of this product in pregnancy and should not be used during pregnancy. drug interactions is not yet clear. ADR systemic

45、response: include weakness, weakness, abdominal pain and fever; gastrointestinal reactions include: anorexia, constipation, diarrhea, nausea and vomiting; nervous system effects include dizziness, drowsiness, dizziness, tremor; skin itching, including: rash, papules, pustules, rubella; Ophthalmology

46、: adverse reactions the eye is caused by the disease itself, but has also been reported after treatment with ivermectin. Some adverse events include visual abnormalities, eyelid edema, anterior uveitis, conjunctivitis, Limbitis, keratitis, retinitis, or choroid. The above symptoms are usually mild s

47、ymptoms, and do not lead to blindness, and generally do not relieve themselves by corticosteroids. Other: including joint pain, synovitis, axillary lymph node enlargement and tenderness, cervical lymph node enlargement and tenderness, inguinal lymph node enlargement and tenderness, other parts of ly

48、mph node enlargement and tenderness, facial edema, peripheral edema, orthostatic hypotension, tachycardia, headache, muscle pain medicine laboratory check exception: including ALT and / or AST increased, leukopenia, eosinophilia and increased hemoglobin. contraindications severe hepatic, renal and c

49、ardiac dysfunction, allergies to this product and psychiatric disorders are prohibited.Edit the usage of this paragraphThe recommended dosage is 200 g/kg for a single dose of water. Usually there is no need for additional doses, but follow-up is needed to ensure radical treatment. The commonly used

50、dose as follows: 15-24 kg, a dose of half (about 3 mg); 25-34 kg, the dose is 1 tablets (about 6 mg); 35-50 kg, at a dose of 1 and a half (about 9 mg); 51-65 kg, the dose is 2 tablets (about 12 mg); 66-79 kg that dose is 2 and a half (about 15 mg); more than 80 kg, 200 g/kg. The recommended dose of

51、filariasis is 150 g/kg per dose of oral water. The commonly used dose as follows: 15-24 g, a dose of half (about 3 mg); 25-44 kg, the dose is 1 tablets (about 6 mg); 45-64 kg, at a dose of 1 and a half (about 9 mg); 65-84 kg, the dose is 2 tablets (about 12 mg); more than 80 kg 150, g/kg. Hookworm i

52、nfections in people over the age of 14 single oral 12 mg (equivalent to 0.2 mg/kg); under 14 years of age, 6 mg orally. Ascaris infected with people over the age of 14 single oral 6 mg (equivalent to 0.1 mg/kg), under 14 years of age, 3 mg orally. Whipworm infection over the age of 14 a single oral

53、dose of 12 mg (0.2 mg/kg); 14 years following a single oral dose of 6 mg. Pinworm infection over the age of 14 a single oral dose of 12 mg (0.2 mg/kg); 14 years following a single oral dose of 6 mg. Overdose: the symptoms should be used according to the prescribed dosage. Excessive use may result in ataxia, slow breathing, tremors, drooping eyelids, decreased activity, vomiting, and mydriasis. Treatment such as drug overdose, should as soon as possible and emetic gastric lavage, if necessary,