Acipimox

Acipimox 속성

Acipimox C화학적 특성, 용도, 생산

개요

Acipimox is a nicotinic acid derivate that structurally related to nicotinic acid. Like nicotinic acid, lowers lipids effectively, but unlike nicotinic acid, acipimox is longer acting and therefore much less prone to produce free fatty acid rebounding. It is usually employed in man in the therapy of hypertriglyceridemia. In addition to its lipid lowering activity, it produces a beneficial elevation of the anti-atherogenic high density lipoprotein subfraction, HDL2. Acipimox is recommended as a lipid-lowering agent to treat hyperlipidemia in patients with noninsulin dependent diabetes mellitus.

화학적 성질

Yellow Solid

Characteristics

The advantages of acipimox to niacin are as follows:
Longer duration of inhibition of hormone-sensitive lipase than niacin.
A lower dose (250 mg BD or TDS) of acipimox is required to lower lipid levels and better tolerability with fewer side effects than niacin.
Acipimox increases insulin sensitivity, while niacin causes insulin resistance. Thus, acipimox has a favorable role in patients with dyslipidemia and diabetes, whereas niacin is contraindicated in diabetes.
Acipimox has adjuvant role in the management of PCOD and increases tissuesensitivity to GH, whereas niacin does not.

용도

Acipimox is a long-acting antilipemic agent and used for the treatment of hyperlipoproteinemias, in particular hypertriglyceridemias, and as adjunctive therapy for affecting cholesterol metabolism.

제조 방법

Synthesis of acipimox: Under cooling and stirring, 78 g of maleic anhydride was dissolved in a solution of 60 ml of chloroform, and 40 ml of 30% hydrogen peroxide was added. After 2 h, 4.8 g of 5-Methyl-2-pyrazinecarboxylic acid was added, and the temperature was kept at 0-5 °C for 2 d. The maleic acid was filtered off. Concentrate to a small volume, add ethyl acetate, and filter to obtain 1.1 g of acipimox, the melting point of which is 178-180 °C.

benefits

1. Act on the liver and adipose tissue, inhibit the lipolysis of adipose tissue, thereby reducing plasma total cholesterol, triglyceride, low-density lipoprotein, and very low-density lipoprotein.
2. Increase high-density lipoprotein in plasma, which is beneficial to the transport and clearance of cholesterol.
3. Increase liver glycogen synthesis and lower blood sugar levels. Asimimox can be used as the first-choice lipid-lowering drug for the treatment of various hyperlipidemias, especially for those with diabetes mellitus with hyperlipidemia.

생물학적 활성

Acipimox, also known as olbemox, is a nicotinic acid analog. It functions as an anti-lipolytic drug and vasodilator. Acipimox may be used in various metabolic studies involving insulin and ghrelin. It lowers total cholesterol and total triglycerides, which helps in the treatment of hyperlipidemia.

Clinical Use

Acipimox was introduced in Europe to treat hyperlipidemia in 1985. Acipimox is a weak agonist of GPR109A with micromolar binding and functional activity.Like niacin, acipimox raises HDL-C and triggers vasodilation in humans.However, it remains unclear whether acipimox causes mild hyperglycemia as is observed with niacin.

부작용

Adverse effects include flushing (associated with Prostaglandin D2), rash, palpitations, and GI disturbances (nausea, dyspepsia, diarrhoea and upper abdominal pain) . Flushing can be reduced by taking aspirin 20-30 min before taking Acipimox. High doses can cause disorders of liver function, impair glucose tolerance and precipitate gout.

Drug interactions

Potentially hazardous interactions with other drugs. It can be combined with powerful hypolipidemic drugs such as fenofibrate and lovastatin to enhance the efficacy and reduce the dose and side effects of the drug. Acyclolimus can improve the efficacy of hypoglycemic drugs, so it is necessary to reduce the dose of hypoglycemic drugs and adjust the dose according to the patient's blood sugar. In antioxidant therapy, it can be used in combination with probucol.

Mode of action

Acipimox is a nicotinic acid derivative (methyl-pyrazine-carboxylic-acid-oxide) that acts on the niacin receptor (GPR109A).The mechanism of action is similar to niacin (inhibition of hormone-sensitive lipase). However，the inhibition of hormone-sensitive lipase by acipimox is remarkably longer (9-12 h) than that of niacin (3 h). Similar to niacin, acipimox also lowers the levels of lp(a).

참고 문헌

[1] Ana T.M.G. Santomauro, Guenther Boden, Maria E.R. Silva, Dalva M. Rocha, Rosa F. Santos, Mileni J.M. Ursich, Paula G. Strassmann and Bernardo L. Wajchenberg, Overnight Lowering of Free Fatty Acids With Acipimox Improves Insulin Resistance and Glucose Tolerance in Obese Diabetic and Nondiabetic Subjects, Diabetes, 1999, vol. 48, 1836-1841
[2] K. C. Shih, C. F. Kwok, C. M. Hwu, L. C. Hsiao, S. H. Li, Y. F. Liu, L. T. Ho, Acipimox attenuates hypertriglyceridemia in dyslipidemic noninsulin dependent diabetes mellitus patients without perturbation of insulin sensitivity and glycemic control, Diabetes Research and Clinical Practice, 1997, vol. 36, 113-119

Acipimox 준비 용품 및 원자재

원자재

준비 용품

Acipimox 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Baoji Guokang Bio-Technology Co., Ltd.	0917-3909592 13892490616	gksales1@gk-bio.com	China	9335	58
Hebei Mojin Biotechnology Co., Ltd	+8613288715578	sales@hbmojin.com	China	12471	58
Zibo Hangyu Biotechnology Development Co., Ltd	+86-0533-2185556 +8617865335152	Mandy@hangyubiotech.com	China	11013	58
Shaanxi TNJONE Pharmaceutical Co., Ltd	+8618740459177	sarah@tnjone.com	China	1111	58
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
Jinan Shengqi pharmaceutical Co,Ltd	86+18663751872	christine@shengqipharm.com	CHINA	491	58
Xiamen AmoyChem Co., Ltd	+86-592-6051114 +8618959220845	sales@amoychem.com	China	6387	58
Alchem Pharmtech,Inc.	8485655694	sales@alchempharmtech.com	United States	63711	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	49391	58
career henan chemical co	+86-0371-86658258 15093356674;	factory@coreychem.com	China	29826	58

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