Doramectin Veterinary Drugs Anti-parasitic Antibiotics

English name：Doramectin

CAS number：117704-25-3

Molecular formula：C50H74O14

Molecular weight 899.11

EINECS number601-490-4

Related categories: Veterinary drug raw materials; Medical raw materials; Veterinary drug raw materials; Pharmaceutical raw materials; Organochlorine pesticides; Macrolide antibiotics; Pesticides; Acaricides; Microbial metabolites; Pharmaceutical intermediates; Tetracyclines; Raw drug substance; Veterinary medicine, anti-parasitic animal; Small molecule inhibitors; Small molecule inhibitors, natural products; Veterinary antiparasitic drugs; Pharmaceutical raw materials; Antibiotics; Medical raw materials; Pharmaceutical additive; Raw materials; Raw materials for animal use; Chemical intermediates - chemical raw materials; Insect repellent; API API - veterinary drug API; Pharmaceutical Chemicalbook Chemical industry; Chemical raw materials; Veterinary drug raw materials; Organic intermediates; Pharmaceutical, pesticide and dye intermediates; Antiparasitic; Intermediates&FineChemicals; Pharmaceuticals; IMIPEM; Inhibitors; rawmaterial; API; Veterinary chemical industry; Intermediate of original drug; Chemical reagents; Chemical reagents - raw materials for animal use; 117704-25-3; Chemical raw materials

Molecular structure:

The melting point is 116-1190C

Boiling point 967.4±65.0 °C(Predicted)

Density 1.25±0.1 g/cm3(Predicted)

The vapor pressure was 0Pa at 20 ° C

Storage conditions：Sealed in dry,Store in freezer, under -20°C

Solubility soluble in methanol:

Morphological solid

Acidity coefficient (pKa)12.42±0.70(Predicted)

Color White

InChIKeyQLFZZSKTJWDQOS-YDBLARSUSA-N

LogP4.39-4.43 at 25℃

Introduction

Doramectin is a new generation of macrolide antiparasitic drugs developed by Sotten (formerly Pfizer) in the United States at the end of last century. It is an avermectin antibiotic produced by fermentation of a new strain of Streptomyces avermectins with cyclohexanecarboxylic acid as a precursor and is considered to be one of the best antiparasitic drugs in the avermectins family. Compared with other ivermectin products, doramectin has higher blood concentration in vivo, slower elimination, longer drug effect, wider anti-parasitic spectrum, and no allergic reaction. Therefore, doramectin can be used as a good alternative anti-parasitic drug of ivermectin. Doramectin is a new Chemicalbook avermectin antiparasitic drug. Its anthelmintic effect is similar to that of ivermectin, which can inhibit the transmission of nerve impulses between nerves and muscles, paralyzing the worm and leaving the host and killing it. The half-life of ivermectin was 4.2d), and the drug effect was prolonged, so the deworming effect was better, and no allergic reactions occurred, and the use was relatively safe. Clinical practice has shown that a dose of 300μg/kg (300μg/kg body weight) is recommended for mild cases, and a dose of 400μg/kg (400μg/kg body weight) is recommended for severe cases.

Chemical structure

Doramectin is a macrolide member of the avermectin family and is structurally very similar to ivermectin. As shown in the figure, doramectin C25 is cyclohexane, ivermecton is a mixture of several congener, its highly active component B1a (containing 80% Chemicalbook content) C25 is CH(CH3)C2H5, another component B1b (20%) C25 is CH(CH3)-CH3. Doramectin C22 and C23 are double bonded, while ivermectin is single bonded.

The highest plasma concentration of doramectin was twice that of ivermectin. The effective blood concentration of ivermectin was 18 days and 12 days, respectively. This is due to the non-polar six-carbon ring at the 25th carbon of Doramella chemicalbootin, which improves its pharmacokinetics. In addition, the unique oile-based adjuvant formulation of doramella chemicalbootin also makes the drug longer-acting.

Ivermectin injection is difficult to handle in large pigs because it can only be injected subcutaneously (because subcutaneous injection needs to be guaranteed), and the change of administration mode of doramectin greatly improves the efficiency of work.

Pharmacological action

[Chemical properties] Yellowish brown powder, very low solubility in water. Streptomycesavermitilis is a recombinant strain of doramectin, which is used to treat ectoparasitic diseases such as nematodiasis and acariasis in livestock. The main difference from ivermectin is a cyclohexyl substitution at C25 position. Doramectin is a new, broad-spectrum antiparasitic drug. It was highly effective against gastrointestinal nematodes, lungworms, eyeworms, lice, ticks, mites and wound maggots. It also had good repellent effect on in vivo and in vitro parasites, especially some nematodes (round worms) and arthropods. Its mechanism of action is mainly to increase the release of γ-aminobutyric acid (GABA), an inhibitory transmitter of the worm, thereby blocking the transmission of nerve signals, making the muscle cells lose the ability to contract and leading to the death of the worm. The peripheral neurotransmitter of mammals is acetylcholine, which is not affected by doramectin, which does not easily cross the blood-brain barrier, has minimal damage to the central nervous system, and is relatively safe for livestock. The main characteristics are that the plasma concentration and half-life of ivermectin are higher or two times longer than that of ivermectin. The United States has approved the injection for cattle and pigs and the pouring agent for cattle.

Effect of use

Doramicin is an internal and external parasite and insecticidal agent, which is effective against nematodes and arthropods. At present our country pig industry commonly used anthelmintic drugs are: internal parasitic drugs: albendazole, levamisole, trichrodipteron, Yue mycin, hygromycin, ivermectin, avermectin. Ectoparasitic drugs: Trichlorfon, dimethylamidine, diazinon, pyrethroids, avermectin, ivermectin. It was reported that the pigs with artificial infection and natural infection gained significantly more weight than the control at 7, 14 and 21 days after the intramuscular injection of 0.3 mg/kg of doramacin (P<0.0001). Compared with the control group, 100% of the worms were eradicated and no side effects occurred. The treatment of scabies scabies showed good results from Suckling piglets to sows. Artificial infection with scabies scabies followed by intramuscular injection at a dose of 0.3 mg/kg body weight resulted in significant elimination of Chemicalbook's dermatitis, lesions and parasitic infections in pigs after 4 weeks (P<0.05). In the treatment of kidney worms in pregnant sows, a single neck injection of 0.3 mg/kg was given, and the detection rate of urinary eggs was 0 and the expulsion rate was 100% on days 56 and 57, while the control group was 3762 eggs per ml urine. It has the same effect on pig lung worms and pig lice. On the basis that tissue drug concentrations greater than l ng/g have antiparasitic activity, the validity of the drug can be evaluated. The duration of doramectin concentrations above 1 ng/g was 26 days in skin, 38 days in lung, 38 days in gastrointestinal mucosa and 38 days in abomasum mucosa. Thus, doramectin was greater than l ng/g in the gastrointestinal mucosa, lung tissue for 38 days, 20 days longer than ivermectin. Therefore, the effect of doramectin on parasite killing was significantly stronger than that of ivermectin, and the effective time of preventing parasite reinfection was longer.

Note

1: Doramicin is not stable and rapidly decomposed and inactivated under sunlight. Its residual drug is toxic to fish and aquatic organisms, so pay attention to water source protection.

2, pouring agent: cattle after application, can not rain within 6 hours.

Use with caution in dogs.

4Chemicalbook. Keep this product out of reach of children. Operators should not eat or smoke when using this product, and wash hands after operation

5, the residual drugs are toxic to fish and aquatic organisms, and attention should be paid to the protection of water resources.

6, rest period, 35 days for cattle and 24 days for pigs.

Biological activity

Doramectin is a derivative of Ivermectin (HY-15310). Doramectin is a potent antiparasitic antibiotic. Doramectin has anti-S. mansoni activity in NMRI mouse model of infection.

In VIVO Studies

Doramectin (10 mg/kg) is active in vivo with worm burden reductions of 60.1% in worm burden reductions of S.mansoni-infected mice.

Safety Information

dangerous mark ：T,N,Xi

Dangerous category code：25-50/53-36/37/38

Safety instructions33-45-60-61-36/37-26

Dangerous goods transport number：UN28116Chemicalbook.1/PG3WGKGermany3

HS Code：29419090

Toxic material data：117704-25-3(HazardousSubstancesData)

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