A nutraceutical approach (Armolipid Plus) to reduce total and LDL cholesterol in individuals with mild to moderate dyslipidemia: Review of the clinical evidence

Abstract

Compelling evidence supports the effectiveness of the reduction of total and LDL cholesterol (TC and LDL-C) in primarily preventing cardiovascular events, within the framework of life-long prevention programs mainly consisting in lifestyle changes. Pharmacological treatment should be introduced when lifestyle changes, including use of nutraceuticals, have failed. ESC/EAS guidelines list a number of nutraceutical compounds and functional foods which have been individually studied in randomized, controlled clinical trials (RCTs). To date only a proprietary formulation of three naturally occurring substances with putative complementary lipid-lowering properties - red yeast rice, policosanol and berberine - combined with folic acid, astaxanthin, and coenzyme Q10 (Armolipid Plus) has been extensively investigated in several RCTs, 7 of which were placebo-controlled, 2 were ezetimibe comparators and 4 were "real life" studies comparing diet and Armolipid Plus to diet alone. The trials included mostly patients with mild to moderate dyslipidemia, treated for 6-48 weeks. The trials also included special populations and patients in whom statins were contraindicated or who could not tolerate them. Armolipid Plus has proved to be able to achieve significant reductions in TC (11-21%) and in LDL-C (15-31%) levels, which is equivalent to expectations from low dose statins. In patients intolerant to statins, who do not achieve their therapeutic target with ezetimibe, Armolipid Plus can achieve a further 10% improvement in TC and LDL-C. The safety and tolerability of Armolipid Plus were excellent, thought likely due to the intentional combination of low doses of its active ingredients: low enough not to be associated with untoward effects, but high enough to exert therapeutic effects in combination with other complementary substances. Consequently, in the event of intolerance to statins, Armolipid Plus offers an effective alternative, which is devoid of the safety risks associated with synthetic pharmacological therapy. In conclusion Armolipid Plus, in addition to dietary measures, could be a rational choice for individuals with mild to moderate hyperlipidemia and for all dyslipidemic patients in whom statins are not indicated or who cannot tolerate them.

Effect of Monacolin K and COQ10 supplementation in hypertensive and hypercholesterolemic subjects with metabolic syndrome

“…Monacolin K has an affinity of about 2000 times compared to the endogenous substrate and can modulate the lipid profile by reducing TC and LDLC [19]. A recent study carried out in patients intolerant to statins reported that RYR was as effective as pravastatin in inducing a dose-dependent decrease of LDLC levels, with a superior safety and tolerability profile [20].…”

Berberine and barberry (Berberis vulgaris): A clinical review

“…Besides extensive animal studies in rabbits (Luo, He, Jin, Zhou, & Yang, ), rats (Jia et al, ; Jin, He, Zhou, & Yang, ), and mice (Chueh & Lin, ), the lipid‐lowering efficacy of berberine has been evaluated by randomized, placebo‐controlled clinical trials in patients with hypercholesterolemia who cannot tolerate statins; in patients with mild to moderate mixed hyperlipidemia, with and without concomitant type 2 diabetes mellitus; and in patients with hyperlipidemia cirrhosis or hepatitis B and C. Mean reductions in TG and LDL‐C levels have been reported at approximately 13–30% and 20–25%, respectively (Barrios et al, ).…”

“…Red yeast rice and policosanol target the HMG‐CoA reductase enzyme, but in different ways, monacolin K, the active ingredient of red yeast rice, competitively inhibits HMG‐CoA reductase activity; whereas policosanol decreases HMG‐CoA reductase synthesis. Berberine has broad effects on the lipid profile via the LDL liver uptake and TG synthesis (Barrios et al, ). Large interindividual inconsistency has been reported in the plasma LDL‐C response to Armolipid Plus supplementation and attributed to three polymorphisms in the 30 UTR region of LDLR, c.*773A > G, c.*52G > A, and c.*504G > A; and two at the 50 UTR region of PCSK9, c.−2,063A > G and c.−3,383C > G (De Castro‐Orós et al, ).…”

Evolocumab and lipoprotein apheresis combination therapy may have synergic effects to reduce low‐density lipoprotein cholesterol levels in heterozygous familial hypercholesterolemia: A case report

“…For these reasons, a nutraceutical treatment with substances characterized by complementary lipidlowering properties was started in 2003, including red yeast rice, policosanol, and berberine combined with folic acid, astaxanthin, and coenzyme Q10 (Armolipid Plus® 1 cp/die). 10 The patient came to our attention in December 2015. At the physical examination: body weight 5 68 kg, height 5 158 cm, BMI5 27.3 kg/m 2 , ambulatory blood pressure 5 120/84 mm Hg.…”

“…Unfortunately, muscle symptoms and CK elevation reappeared. For these reasons, a nutraceutical treatment with substances characterized by complementary lipid‐lowering properties was started in 2003, including red yeast rice, policosanol, and berberine combined with folic acid, astaxanthin, and coenzyme Q10 (Armolipid Plus® 1 cp/die) …”