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Lipid-lowering drug. Can inhibit the activity of HMG-CoA reductase, thereby reducing cholesterol synthesis.
When atorvastatin is combined with oral contraceptives containing norethindrone and ethinylestradiol, it can increase the AUC of norethindrone and ethinylestradiol by 30% and 20% respectively; when combined with erythromycin, the plasma
concentrations increased by approximately 40%; when combined with digoxin, the steady-state blood concentration of digoxin increased by approximately 20% after multiple administrations, and digoxin concentrations should be monitored, and when combined with cotrimoxazole (cholestyramine), it increased the AUC of nandrolone and ethinyl estradiol by approximately 20%. When used in combination with colestipol (cholestyramine), the plasma concentration of this product is reduced by approximately 25%, but the effect of lowering LDL-C is greater than that of either this product or colestipol alone.
Uses and functions of Atorvastatin Powder.
Atorvastatin is a commonly used statin in clinical practice. In addition to treating hypercholesterolaemia, it has a better preventive effect in hypertension, coronary heart disease and cerebrovascular disease.
In terms of cardiovascular diseases, atorvastatin used in patients with atherosclerosis can protect endothelial function, delay atherosclerosis, protect target organs, and improve prognosis; atorvastatin used in patients with acute Atorvastatin in patients with acute coronary syndrome can reduce CRP and alleviate clinical symptoms; atorvastatin in patients with hypertension can reduce the expression of CD40 and CD40L, play the role of antihypertensive, and enhance the physiological comfort of patients. Atorvastatin can reduce the expression of CD40 and CD40L in hypertensive patients, play the role of antihypertensive and enhance the physiological comfort of patients.
From the aspect of cerebrovascular disease, atorvastatin is used in patients with acute cerebral infarction, which can reduce the level of ultrasensitive-CRP and improve the neurological deficit; atorvastatin is used in patients with arachnoiditis, which can reduce the expression of CD40 and CD40L and improve the physiological comfort of patients. Atorvastatin is used in patients with subarachnoid space haemorrhage, which can inhibit the expression of cysteine proteases 3 and 5, alleviate the symptoms of vasospasm and promote disease regression. Atorvastatin has anti-atherosclerosis, anti-inflammatory, blood pressure lowering and so on. Atorvastatin has multiple pharmacological effects such as anti-atherosclerosis, anti-inflammation, and blood pressure lowering, and its use in patients with hypercholesterolemia has a satisfactory effect and high safety, which is worthy of further reference and application in hospitals at all levels.
Pharmacological Effects of Atorvastatin Raw Powder.
The molecular structure of atorvastatin contains a benzene ring and an azetidine ring, which is biologically active without metabolism in the body. Its molecular weight is larger than that of other statins, and it has the advantages of fast effect, strong lipid-lowering effect and long duration.
HMG-CoA reductase is the rate-limiting enzyme for cholesterol synthesis, statins are similar in structure to HMG-CoA, and their affinity for the enzyme is 10,000 times higher than that of HMGCoA, so they can compete in the liver to inhibit HMGCoA reductase, and the hepatic synthesis of apoB-100 will be reduced, which will lead to a reduction in the synthesis of VLDL; on the other hand, through the mechanism of its own regulation, it can also increase the number of LDL receptors on the hepatic cell membrane by compensating. On the other hand, through its own regulatory mechanism, it can also compensatorily increase the number and activity of LDL receptors on the hepatocyte membrane and the affinity of LDL and its receptor, so that a large amount of LDL in the plasma is uptaken, and metabolised to bile acids by the LDL receptor pathway and excreted, causing a further decrease in plasma LDL-C, VLDL-C and TC.
In addition statins have the effect of increasing the reactivity of vascular smooth muscle to vasodilating substances, inhibiting the proliferation, migration and promoting the apoptosis of vascular smooth muscle cells (VSMCs), reducing the formation of foam cells in the arterial wall, inhibiting the adhesion and secretion function of macrophages and monocytes, and inhibiting platelet aggregation.
Production method of Atorvastatin.
Compound (I) is reduced with triethylboron and sodium borohydride in methanol, and the product is then hydrolysed to give sodium atropine. Acidification gives atropatin. While atropatin in toluene, with d-star Stark hydrazine (Dan-Stark trap) refluxed for 20min to produce atorstatin lactone.
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