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| Acarbose |
PHARMACOLOGY Chemical Name: O-{4-Amino-4,6-dideoxy-N-[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-hydroxymethylcyclohex-2-enyl] -alpha-D-glucopyranosyl}- (1->4)-O-alpha-D-glucopyranosyl- (1->4)- D- glucopyranose. DESCRIPTION Acarbose is a relatively new drug for use in insulin-dependent diabetes mellitus (Type 1), adult-onset diabetes mellitus (AODM or Type II), and for those who suffer from "impaired glucose tolerance." As glucose tolerance declines with age, virtually everyone over the age 35 can be functionally glucose intolerant to some degree. Acarbose can enhance energy and mood levels during the day as a result of its sugar stabilizing action. This is particularly true after a meal when one may feel tired. Acarbose delays the digestion and absorption of carbohydrates, which subsequently delays and flattens post-meal rises in glucose and insulin. One of the main features of acarbose is its body weight lowering action. In overt diabetics, it helps maintain a stable weight, whereas in non-diabetic persons, it may prevent weight gain and actually result in modest weight loss. Scientific investigations have revealed other general anti-aging benefits which include reductions in fasting triglycerides, reduction in LDL-cholesterol levels, increases in HDL-cholesterol levels, decreased advanced glycosylation end product (AGE) formation in connective tissue, decreased cataract formation and potential improvements in insulin sensitivity, combating the neuroendocrine theory of aging. The modern diet is full of simple carbohydrates, (potatoes, pasta, bread, refined foods etc.) that contain nothing more than starch, (a simple sugar). These are quickly broken down by the body producing glucose, which in turn promotes the release of insulin. As a result, most humans are saturated with permanently high insulin levels which results in accelerated aging and the earlier onset of age-related disorders such as diabetes. ACTION Starches and complex sugars, are broken down in the digestive tract into simple sugars which are then absorbed into the body either to be used as energy or stored as fat. For complex sugars, enzymes are required for the breaking down process prior to absorption. One of the critical groups of enzymes in the final steps of carbohydrate digestion is known as the alpha-glucosidases. Acarbose acts as a potent inhibitor of these enzymes preventing the breakdown of starches, dextrins, maltose and sucrose to absorbable monosaccharides. As a result of the specifity of acarbose, beta glucosidases (e.g. lactases) are unaffected, and lactase and glucose are absorbed when acarbose is taken. Digestion of carbohydrates is therefore delayed, flattening post meal insulin and glucose peaks. Post-meal triglyceride levels, (believed by some scientists to be as accurate as fasting cholesterol levels in predicting the risk of coronary disease) are decreased. In numerous studies, acarbose has been shown to significantly reduce glycosylate haemoglobin, which is increasingly becoming known as a screening and diagnostic test for diabetes, and as a biomarker of aging. Recently, glycosylated hemoglobin was documented to increase with age in non-diabetic subjects. INDICATIONS
Avoid the use of intestinal absorbents (such as charcoal), and drugs used to aid digestion (i.e. digestive enzyme preparations) may also conflict. Avoid the use of the antibiotic Neomycin and the cholesterol drug Chloestyramine. Diabetics should check with their physician before use. The following persons should also avoid use: persons suffering from inflammation or ulceration of the bowel or Crohn's disease: any person who has or is susceptible to an obstruction of the intestines: persons with a large hernia or any other condition where excess gas could aggravate the condition. Persons with kidney or liver disorders should seek advice prior to use. Drugs that elevate blood glucose levels (thiazide diuretics, furosemide, corticosteroids, phenothiazines, thyroid, estrogen, oral contraceptives, isoniazid etc.,) can reduce effectiveness. SIDE EFFECTS The most common side effects are due to unabsorbed carbohydrates, which can ferment and cause excessive gas production (flatulence) and in the severest of cases, abdominal cramps, bloating and diarrhea. However, these side-effects are generally either dose related, (diabetic dosages are likely to be twice the anti-aging maximum) or may be more prevalent at the beginning of use. Lowered dosages, or a little time expired may see the reduction and disappearance of such side-effects. Other possible, less common, side effects are inflammation of the liver (hepatitis), jaundice and skin reactions such as redness, rash urticaria (hives). The tablets may also case an increase in the levels of certain proteins called enzymes in your blood. These effects go away when treatment is stopped. DOSAGE Diabetic dosages range from 50mg three times a day to 100mg 3 times a day, up to a maximum total of 600mg per day. Dosages of more than 150mg a day are more likely to cause potential side effects. Anti-aging/ weight control doses are 25mg to 50mg once, twice or three times per day (total). The tablets should be chewed with meals. Avoid swallowing whole as it impedes the effectiveness. CAUTIONS It would be advisable NOT to follow a diet that is rich in simple carbohydrates, or indeed not to follow a high carbohydrate diet in general, (this is just common sense for anti-aging anyway). Neither should a diet rich in sucrose be followed, (again common sense). This caution is here because such a diet with acarbose supplements, will exacerbate the possibilities of the side effects of flatulence as large amounts of fermenting starches/carbohydrates/sugars are slowed and blocked from intestinal release to blood entry. HOW SUPPLIED 50mg tablets. NOTES This product is most effective when taken orally, by chewing the tablets with the meal. REFERENCES
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