What is Policosanol?

Policosanol refers to the general mixture of saturated alcohols of major long-chain fatty acids. This is the mixture of 8 high-molecular primary aliphatic alcohols extracted from the wax films of stems and leaves of plants such as Saccharum officinarium and dioscorea opposite. Also, it is included in the bee wax. The long-chain alcohol of policosanol is 1-octanosol with 28 carbons and the largely included alcohol is 1-triacontanol with 30 carbons. These long-chain alcohols are water-soluble solid wax.

Policosanol has been known as a natural compound which provides vital energy needed by modern people under extreme stress from busy schedules. Recently, new functionality of policosanol is becoming highlighted in medical and sitologic areas around Japan and USA. Therefore, policosanol which was once used for sexual enhancer and restorative supplement became treatment, preventive medicine or food for hypertension, arteriosclerosis, and heart disease.

Effects of Policosanol Products:

1. Lower the level of cholesterol

Policosanol is known to lower the lipid level by deactivating the HMG-CoA reductase which catalyzes the initial rate limiting step in the cholesterol synthesis. In other words, Saccharum officinarium wax alcohol lowers the total cholesterol level as well as low density lipid-cholesterol (LDL-C) level. Cholesterol is synthesized in the liver and agglomerated into the very low density lipid (VLDL) which is released into the blood stream. VLDL is a precursor of LDL. Saccharum officinarium wax alcohol does not directly attenuate the HMG-CoA reductase. Instead, it inhibits the cholesterol synthesis by controlling the activity. Many experimental data implicates that it decreases the synthesis of HMG-CoA reductase and/or stimulates the degradation. Saccharum officinarium wax alcohol also increases the number of LDL receptors on the surface of the cells to reduce the level of LDL-cholesterol while increasing the level of high density lipid-cholesterol (HDL-C) on the other hand.

The table below shows the changes in the level of cholesterol in patients with specific disease when administered of policosanol everyday.

- Change in the level of cholesterol in 84 patients with type II diabetic patients and hypercholesterolemia

Change in level of cholesterol

Daily dose

Total cholesterol

Daily dose

Total cholesterol

10mg

▼ 14.2%~28.9%

▼ 20.4%~44.4%

▲ 7.7%~12.9%



- Change in the level of cholesterol in 150 menopausal women with type II hypercholesterolemia

Change in level of cholesterol

Daily dose

Total cholesterol

Daily dose

Total cholesterol

5mg

▼ 12.6%~12.9%

▼ 17.3%~17.7%

▲ 3.6%~16.5%

10mg

▼ 16.7%~19.5%

▼ 25.2%~26.7%

▲ 7.4%~29.3%



- Change in the level of cholesterol in patients with type II hypercholesterolemia and liver function abnormality(ALT>45U/L, GGT >55 U/L)

Change in level of cholesterol

Daily dose

Total cholesterol

Daily dose

Total cholesterol

5mg

▼ 13.6%

▼ 19.0%

▲ 11.5%

10mg

▼ 15.4%

▼ 22.3%

▲ 17.9%



- Change in the level of cholesterol in patients with kidney syndromes (proteinuria and kidney disease confirmed by biopsy)

Change in level of cholesterol

Daily dose

Total cholesterol

Daily dose

Total cholesterol

10mg

▼ 34.7%

▼ 51%

▲ 24.2%

2. Decrease the occurrence of coronary artery disease

It is widely known that cholesterol is the main cause of coronary artery syndromes. By lowering the cholesterol level by drug, the risk of coronary artery disease can be decreased. Reduction of LDL-C level improves the morbidity and death rate contributed by coronary artery disease. The effects on the cholesterol level is observed after 4~6 weeks of treatment with the peak at week 8.

The table below represents the changes in the level of cholesterol in the placebo-controlled study on 309 patients with minimum of 2 risk factors for the coronary artery disease accompanied by hypercholesterolemia. Patients were divided into two groups, 5mg and 10 mg of policosanol daily.

Change in level of cholesterol

Daily dose

Total cholesterol

LDL Cholesterol

HDL Cholesterol

5mg

▼ 12.8%~13.0%

▼ 16.9%~18.2%

▲ 14.6%~15.5%

10mg

▼ 16.2%~17.4%

▼ 24.4%~25.6%

▲ 28.4%~29.1%

3. Attenuate platelet aggregation.

In the result of a study on healthy volunteers, hypercholesterolemia patients, and type II diabetic patients, policosanol has attenuated the platelet aggregation in a dose-dependent manner. The studies on both human and animals implicate that these effects are demonstrated by decreased level of thromboxane and prostaglandin-12.

4. Decrease the risk of death and concurrent disease

10 long-term, placebo-controlled studies have shown maintenance or slight increase in the level of cholesterol even after 1~3 years and it was also confirmed by 5 meta-analyses. In one randomized, double-blinded, placebo-controlled clinical trial, 1470 patients with hypercholesterolemia accompanied by at least one risk factor for the coronary artery disease in old age were followed-up for 3 years. 5mg of policosanol has decreased the total cholesterol level by 22% and LDL-cholesterol by 30% while increasing HDL-cholesterol by 15%. Also, serious risk was decreased by 71%. The reduction in the risk of serious complication and concurrent disease of cardiac vessel and cerebral vessel was approximately 80%. The risk of death was decreased by up to 81%.

5. Reduce the risk of obesity double by two times when accompanied by aerobic exercises

In middle-aged diabetic women, the effects of policosanol and aerobic exercise was investigated. As a result, the uptake of policosanol and exercise both improved the blood lipid factors as well as body composition to prevent various diseases contributed by obesity. Also, their combination doubled the effect.

Drug interaction

1. Aspirin

Administration of 20mg of policosanol daily + 100mg of aspirin daily has shown additional effects on platelet aggregation in human. While aspirin lowers the level of TxB2 and PgI2, policosanol only lowers the level of TxB2 with no influence on the level of PgI2. Also, policosanol has treated the gastric ulcer induced by aspirin in experimental animal models.

2. Antiplatelet agents

Single or repeated oral administration of policosanol had little influence on the bleeding time in mice. The increased bleeding time induced by warfarin and heparin was not expanded.

3. β-blockers

In rodents, policosanol has slightly, yet significantly increased the effect of propranolol lowering the blood pressure without influence on the pulse. Compared to the placebo, it greatly decreased the arterial blood pressure and continuously lowered the cholesterol level in patients who were administered of β-blockers without increasing any adverse event rates. Policosanol has been used in combination with β-blockers, calcium-channel blockers, diuretics, angiotensin-converter inhibitors, antiplatelet agents, vasodilators, oral antidiabetics, digitalis, anti-anxiety agents, antidepressants, neuroleptics, anticoagulants, thyroid hormones, antiulcer agents, and vitamins with no clinically adverse events.

4. Fish oil (Omega-3 fatty acids)

In an experimental study, the combination treatment of policosanol and omega-3 fatty acids have lowered both total cholesterol level and LDL-cholesterol level compared to the single treatment by omega-3 fatty acids. Also, it lowered the neutral lipid level compared to the single treatment of policosanol as well as attenuating platelet aggregation more than each of the single treatment.

In other 3 clinical trials, daily administration of 5mg and 10 mg of policosanol with  omega-3 fatty acids has decreased the total cholesterol level and LDL cholesterol level in serum compared to the treatment of placebo + omega-3 fatty acids without influencing the level of neutral lipids reduced by the treatment of placebo + omega-3 fatty acids. In a study out of these, combination treatment has shown better results on the platelet aggregation as well.

5. Vitamins

There was no study on the specific interaction between policosanol and vitamins. However, policosanol has been practically administered with all vitamins (complex vitamins of A, D, E, or B) without related adverse events in clinics and studies. Moreover, very favorable tolerance was shown in an open study on subjects with the history of stroke treated by aspirin + vitamin + 20 mg of policosanol daily with low rate of new or recurrent serious events and excellent nerve recovery.

Absorption and excretion

Policosanol is rapidly absorbed when orally administered with Cmax between 1 to 4 hours. As a result of low bioavailability, it has great first-pass effect at liver and is absorbed in general tissues rapidly. The tissue uptake of policosanol is the most in liver followed by heart, aorta, and lipid tissue. It is not much absorbed in brain and striated muscle. Alcohols included in policosanol is rapidly converted into the same length of fatty acids in liver. Octacosanoic acid and triacontanoic acid are the major metabolites of the Saccharum officinarium wax alcohol. Octacosanoic acid shows rapid pharmacologic features inhibiting the synthesis of cholesterol and decreasing the serum thromboxane B2. Policosanol and its metabolites are mostly excreted via bile acids (over 90%) with little excretion via urine (less than 2%). The excretion is slow to have 140 hours of half-life.

Cautions in administration

1. Even though policosanol has never demonstrated teratogenicity on animals, it is contraindicated to pregnant women and lactating women since cholesterol metabolites are essential for the normal growth of fetus.

2. For its antiplatelet activity, hemophiliac patients and those being administered of warfarin need to take cautions to use policosanol.

3. Supplementary use of policosanol must be withdrawn prior to undergoing surgery. 

Side effects

Side effects from relieved gastrointestinal tract, skin rash, headache, insomnia, and loss of weight have been reported in very low occurrence rate. Also, most of them were well tolerated. 

Note!

- LDL: High level of LDL-cholesterol can be cumulated in the blood vessels on the way from liver to the peripheral nerves. It induces blood circulation disorders, arteriosclerosis and hypertension. It is the bad cholesterol often mentioned of.

- HDL: In contrary to LDL, HDL-cholesterol removes the LDL-cholesterol cumulated within the arterial wall to prevent arteriosclerosis. It can be called, good cholesterol.