News Update on Atorvastatin Research: Dec – 2019

Comparison of One-Year Efficacy and Safety of Atorvastatin Versus Lovastatin in Primary Hypercholesterolemia

This double-blind procedure to guage semipermanent effectiveness Associate in Nursingd safety of lipid-lowering medication was performed in thirty one community- and university-based analysis centers within the USA to directly compare a replacement 3-hydroxy-3-methylglutaryl-coenzyme A enzyme substance (reductase inhibitor) to an accepted drug of this category in patients with moderate hypercholesteremia. Participants remained on a cholesterol-lowering diet throughout the study. One thousand 49 patients were irregular to receive lipid-lowering medication ten mg, lipid-lowering medicine twenty mg, or placebo. At sixteen weeks the placebo cluster was irregular to either lipid-lowering medication or lipid-lowering medicine treatment. At twenty two weeks, patients United Nations agency had not met beta-lipoprotein (LDL) cholesterin target levels doubled the dose of enzyme substance. effectiveness analysis was mean p.c amendment from baseline in cholesterol, triglycerides, total cholesterin, high-density-lipoprotein cholesterin, and apolipoprotein B (apoB). [1]

Clinical Pharmacokinetics of Atorvastatin

Hypercholesterolaemia may be a risk issue for the event of illness} disease. lipid-lowering medicine lowers plasma LDL (LDL) cholesterin levels by inhibition of reductase. The mean dose-response relationship has been shown to be log-linear for lipid-lowering medicine, however plasma concentrations of lipid-lowering medicine acid and its metabolites don’t correlate with LDL-cholesterol reduction at a given dose. [2]

High-Dose Atorvastatin after Stroke or Transient Ischemic Attack

BACKGROUND: Statins cut back the incidence of strokes among patients at inflated risk for vessel disease; whether or not they reduce the chance of stroke when a recent stroke or transient anemia attack (TIA) remains to be established.

METHODS: we have a tendency to arbitrarily allotted 4731 patients WHO had had a stroke or ischemia inside one to 6 months before study entry, had lipoprotein (LDL) sterol levels of one hundred to one hundred ninety mg per metric capacity unit (2.6 to 4.9 mmol per liter), and had no celebrated coronary heart condition to double-blind treatment with eighty mg of lipid-lowering medication per day or placebo. the first finish purpose was a primary nonfatal  or fatal stroke. [3]

Surface stabilized atorvastatin nanocrystals with improved bioavailability, safety and antihyperlipidemic potential

Atorvastatin, a well-liked possibility for hyperlipoidemia exhibits the matter of poor stomachal solubility and low absolute bioavailability (12%) together with higher pre-systemic clearance (>80%). Therefore, to avoid these limitations, statin drug nanocrystals were ready exploitation poloxamer-188 as stabilizer via high homogenisation technique followed by freeze-drying. numerous variables like drug to poloxamer-188 magnitude relation, homogenisation cycle, homogenisation pressure, sort and concentration of cryoprotectant were optimized to attain uniform nanosized crystals with sensible dispersibility. Solid state characterization by ATR-FTIR and DSC discovered no incompatible chemistry interaction between drug and excipients in formulation whereas DSC and PXRD conjointly verified the reduced crystallinity of drug in nanocrystals. [4]

Biochemical and Toxicological Evaluation of Atorvastatin and Riboflavin in Diethylnitrosamine Induced Hepatocellular Carcinoma

Background: statin drug, a usually prescribed drug for the management of lipidemia, acts as competitive inhibitors of HMG-CoA reductase—a rate-limiting catalyst in cholesterin synthesis. On the opposite hand, B vitamin is additionally a well-studied substance well-known for its anti-proliferative, anti-metastatic and inhibitor properties. However, the synergistic or antagonistic result of each medication once administered along isn’t studied nonetheless.

Method: This study was an endeavor to guage the toxicity/efficacy of statin drug (30 mg/kg) together with B vitamin in hepatocarcinogenic rats once challenged by one diethylnitrosamine DENA (160 mg/kg; I.P). Serum ALT, AST, amino acid enzyme, urea, uric acid, creatinine, bilirubin, albumin, LDL, FT3, FT4, calcium, phosphorus, and glyceride levels were calculable. Histopathology was conjointly performed to review the alterations within the cellular design of viscus and viscus cells. [5]

Reference

[1] Group, A.S., Davidson, M., McKenney, J., Stein, E., Schrott, H., Bakker-Arkena, R., Fayyad, R. and Black, D., 1997. Comparison of one-year efficacy and safety of atorvastatin versus lovastatin in primary hypercholesterolemia. The American journal of cardiology, 79(11), (Web Link)

[2] Lennernäs, H., 2003. Clinical pharmacokinetics of atorvastatin. Clinical pharmacokinetics, 42(13), (Web Link)

[3] Stroke Prevention by Aggressive Reduction in Cholesterol Levels (SPARCL) Investigators, 2006. High-dose atorvastatin after stroke or transient ischemic attack. New England Journal of Medicine, 355(6), (Web Link)

[4] Surface stabilized atorvastatin nanocrystals with improved bioavailability, safety and antihyperlipidemic potential
Manu Sharma & Isha Mehta
Scientific Reports volume 9, Article number: 16105 (2019) (Web Link)

[5] Mohammed, K., Sadath, S., Jamal, T., Razvi, S., Al-Orabi, A., Aseeri, A. H., Al-Abbasi, F. A. and Anwar, F. (2018) “Biochemical and Toxicological Evaluation of Atorvastatin and Riboflavin in Diethylnitrosamine Induced Hepatocellular Carcinoma”, Journal of Pharmaceutical Research International, 22(1), (Web Link)

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