2 English reference acipimox [Xiangya Medical Dictionary]
Summary Acipimox is a nicotinic acid derivative, which inhibits the release of free fatty acids from adipose tissue, resulting in the decrease of free fatty acids entering the liver, the obstruction of TG synthesis, the corresponding decrease of VLDLC formed with apolipoprotein Bl00 and the decrease of LDLC. Acipimox can activate lipoprotein esterase, reduce very low density lipoprotein cholesterol and LDLC, but reduce triglyceride and total cholesterol, and increase high density lipoprotein level. It is mainly used for treating hypertriglyceridemia (type IV), hypercholesterolemia, type IIA, type IIA, type III and type V hyperlipoproteinemia. It is especially effective for hyperlipidemia patients with gout and diabetes.
4 Instructions for Acipimox 4. 1 Drug Name Acipimox
4.2 English name Acipimox
4.3 Asimos alias Asimos; Le Zhiping; Pyrimidic acid; Hydroxymethyl pyrazine; Bimo acid; Methoxypyrazine; Olbemox Holbert Tan
4.4 classification of drugs in circulatory system >: lipid-regulating and anti-atherosclerosis drugs > nicotinic acid drugs.
4.5 crystalline powder, insoluble in water.
4.6 dosage form capsules: 0.25g per capsule.
4.7 Pharmacological effects of acipimox 1. Inhibit the decomposition of adipose tissue, reduce the release of free fatty acids and reduce the synthesis of triacylglycerol;
2. Inhibit the production of very low density lipoprotein and low density lipoprotein;
3. Inhibit the activity of hepatic lipase and reduce the transfer of high-density lipoprotein cholesterol;
4. The activation of lipoprotein lipase in adipose tissue accelerates the decomposition of LDL, which is beneficial to the increase of HDL cholesterol. Its hypolipidemic effect is stronger than nicotinic acid. The combination of acipimox and bile acid binding resin can enhance the lipid-lowering effect. It can improve patients' glucose tolerance and reduce fasting blood glucose by about 15%.
4.8 The pharmacokinetics of acipimox can be rapidly absorbed orally. The peak of plasma concentration can be reached about 2 hours after taking the drug, and it does not bind to plasma protein, with a half-life of 2 hours. There is no obvious metabolism in the body, and it is basically excreted from the urine in its original form.
4.9 Indications of acipimox: hyperlipoproteinemia Ⅱ a, hyperlipoproteinemia Ⅲ b, hyperlipoproteinemia Ⅲ, hyperlipoproteinemia Ⅳ and hyperlipoproteinemia Ⅴ.
4. 10 contraindications to acipimox are prohibited for those allergic to acipimox, pregnant women and lactating women, and those with severe ulcer disease and severe liver function damage are prohibited.
4. 1 1 Precautions: If renal insufficiency occurs, reduce the dosage or extend the interval.
4. The adverse reaction of12 acipimox was obviously less than that of nicotinic acid. At present, no obvious damage to liver and kidney function has been found; No obvious metabolic disorder was observed; In facial flushing, the incidence of skin itching is about 6%. Individual patients have epigastric discomfort, heartburn, nausea and diarrhea. Most of these adverse reactions gradually eased or disappeared after taking the medicine for a few days.
4. 13 usage and dosage of acipimox should be taken after meals. Type ⅳ patients, 250mg each time, three times a day; For patients with type II, III and IV, the dosage can be 250mg each time, three times a day, and the maximum dosage can be 1 200mg/ day if necessary.
4. 14 Drug Interaction No drug interaction was found when combined with oral hypoglycemic agents and oral anticoagulants.
4. 15 expert comments Clinical research shows that acipimox is a safe and effective drug for regulating blood lipid, which can reduce TC by 25%, TG by 50% and increase HDLC by 20%.
5 Acipimox poisoning Acipimox (Lezhiping, methoxypyrazine) is a nicotinic acid derivative, which inhibits the release of free fatty acids from adipose tissue, resulting in the decrease of free fatty acids entering the liver, the obstruction of TG synthesis, the corresponding decrease of VLDLC formed with apolipoprotein Bl00, and the decrease of LDLC, which can activate lipoprotein esterase and reduce VLDLC and LDLC, but reduce TG and total TC, and improve HDL level. It is mainly used for treating hypertriglyceridemia (type IV), hypercholesterolemia, type IIA, type IIA, type III and type V hyperlipoproteinemia. It is especially effective for hyperlipidemia patients with gout and diabetes. The drug is completely absorbed by oral administration, and its half-life is 2 hours. It is excreted in urine without metabolism. Rats were given oral LD50 > 4g/kg. The usual dosage was 0.25g per dose, 2-3 times a day [1].
5. 1 Less clinical manifestations, less adverse reactions, which can cause hot flashes and itching of the skin at the initial stage of treatment; Occasionally, I have heartburn, upper abdominal pain and headache. Very few patients may have urticaria, maculopapular rash, lip edema, rash, asthma, dyspnea and hypotension. [ 1]
5.2 The treatment points of acipimox poisoning are [1]: