Acarbose in Pregnancy and Breastfeeding
Fetal Risk Summary
Acarbose is an oral a-glucosidase inhibitor that delays the digestion of ingested carbohydrates within the gastrointestinal tract, thereby reducing the rise in blood glucose after meals (1). It is used in the management of non-insulin-dependent diabetes mellitus (type II). Less than 2% of a dose is absorbed as active drug in adults, but the systemic absorption of metabolites is much higher (about 34% of the dose) (1).
Reproductive studies in rats found no evidence of impaired fertility or reproductive performance (1). Doses of acarbose up to 9 and 32 times the human dose in pregnant rats and rabbits, respectively, were not teratogenic in either species nor, at 10 times the human dose, not embryotoxic in rabbits (1).
A 1998 non-interventional observational cohort study described the outcomes of pregnancies in women who had been prescribed one or more of 34 newly marketed drugs by general practitioners in England (2). Data were obtained by questionnaires sent to the prescribing physicians one month after the expected or possible date of delivery. In 831 (78%) of the pregnancies, a newly marketed drug was thought to have been taken during the 1st trimester with birth defects noted in 14 (2.5%) singleton births of the 557 newborns (10 sets of twins). In addition, two birth defects were observed in aborted fetuses. However, few of the aborted fetuses were examined. Acarbose was taken during the 1st trimester in five pregnancies. The outcomes of these pregnancies included two spontaneous abortions and three normal newborns (one premature) (2).
No other reports describing the use of acarbose during human pregnancy have been located. Less than 2% of a dose is absorbed systemically, but several metabolites are absorbed in much greater proportions, and the embryo or fetal risk from any of these is unknown. Acarbose is normally used in combination with oral hypoglycemic agents, and these hypoglycemic drugs are not indicated for the pregnant diabetic as they may not provide good control in patients who cannot be controlled by diet alone (3). Carefully prescribed insulin therapy will provide better control of the mother's blood glucose, thereby preventing the fetal and neonatal complications that occur with this disease. High maternal glucose levels, as may occur in diabetes mellitus, are closely associated with a number of maternal and fetal effects, including fetal structural anomalies, if the hyperglycemia occurs early in gestation. To prevent this toxicity, most experts, including the American College of Obstetricians and Gynecologists, recommend that insulin be used for types I and II diabetes occurring during pregnancy and, if diet therapy alone is not successful, for gestational diabetes (4,5).
Breast Feeding Summary
Small amounts of acarbose, or its metabolites, are excreted in the milk of lactating rats (1). No studies describing the use of acarbose during human lactation, or measuring the amount of the drug or its metabolites in milk, have been located. Because the drug acts within the gastrointestinal tract to slow the absorption of ingested carbohydrates, and less than 2% of a dose is absorbed systemically, the amount of unmetabolized drug in the mother's circulation available for transfer to the milk is probably clinically insignificant. As with all drugs, however, the safest course while taking acarbose is not to breast feed until data on its safety during lactation are available.
- Product information. Precose. Bayer Corporation, 1997.
- Wilton LV, Pearce GL, Martin RM, Mackay FJ, Mann RD. The outcomes of pregnancy in women exposed to newly marketed drugs in general practice in England. Br J Obstet Gynaecol 1998;105:8829.
- Friend JR. Diabetes. Clin Obstet Gynecol 1981;8:35382.
- American College of Obstetricians and Gynecologists. Diabetes and pregnancy. Technical Bulletin. No. 200. December 1994.
Coustan DR. Management of gestational diabetes. Clin Obstet Gynecol 1991;34:55864.
Questions and Answers
Can I use acarbose to loss weight ?, I have heard that acarbose can prevent starch being absorbed.Can I use acarbose to loss weight?how much should I take a day?
Acarbose as an aid to Weight Loss
Animal studies with acarbose have consistently shown that acarbose has a body weight-lowering action. Balfour and McTavish (1993) reported that acarbose caused a dose-dependent reduction in body weight gain of genetically obese and hyperinsulinemic rats. In higher doses, acarbose even caused a loss in weight (Fig. 7). Although some studies have reported a beneficial effect of alpha glucosidase inhibitors on body weight in humans (Coniff, et al, 1995; Calle-Pascual, et al, 1996; Johnston, et al, 1997; Hoffman and Spengler, 1997 Goto, et al, 1989), the effect was usually small to moderate. In view of the salutary effect that acarbose has on blood sugar, insulin, lipids, and HbA1c, I was at first surprised at the modest weight loss reported by participants in the studies. However, upon reflection, I believe the potential of acarbose as a weight loss agent may have been overlooked, and this apparent paradox can be explained. First, weight loss was a usual finding in the animal studies. There is no good animal model for diabetes with which to test anti-diabetic drugs - so most studies are done on normal (non-diabetic) or obese animals. However, the human studies were quite different, as the overwhelming majority of subjects were diabetic. Diabetics characteristically gain weight, even when under treatment (the major exception is when Metformin, is used, which usually results in loss of body fat). Acarbose, as we have noted above, prevents weight gain, and actually results in modest weight loss. The anti-obesity effect of acarbose becomes apparent when we add the modest amount of weight generally lost, with the amount that patients not on acarbose would have been expected to gain. Another indicator of acarbose's efficacy in weight control is its demonstrated ability to retard "relapse weight gain" in overweight patients who had lost weight before beginning treatment with acarbose (William Olsson, 1985; William-Olsson, et al, 1985). Consequently, although acarbose helps overt diabetics maintain a stable weight, I believe that people who are not overtly diabetic will derive even greater weight loss benefits than diabetics - paralleling those of the non-diabetic experimental animals.
Adverse Effects and Safety
Acarbose is a very safe drug. Only about 1-2% is absorbed systemically. The most frequent side effects are all due to the unabsorbed carbohydrates, which ferment and can cause excessive and sometimes embarrassing increased gas production, abdominal cramps, bloating and even diarrhea (Fig. 8). These effects can be minimized by taking the lowest effective dose, which is usually just below that which causes the gastrointestinal distress. Continued use usually results in a reduction or resolution of these symptoms. As some tolerance seems to develop, dosages can be increased to my maximum recommended dosage of 300 mg daily (1/2 of the manufacturer's recommended maximum of 600 mg/day). In 1988, Clissold and Edwards reported that "from the large clinical studies reported to date, acarbose - even after treatment for up to 5 years-does not produce any clinically significant adverse effects on biochemical and haematological parameters". Balfour and McTavish (1993) reviewed clinical laboratory tests in 6354 patients, and did not find any consistent trend with regard to liver enzyme abnormalities. However, they did find that the liver enzymes SGOT and SGPT were elevated to almost double the upper limit of normal in almost 4% of the patients. Notwithstanding, these enzyme changes were not associated with changes in other hepatic function tests, and the enzyme abnormalities resolved after discontinuation of acarbose. In another large placebo controlled study, 354 patients were evaluated. Doses of acarbose as large as 200 mg three times daily had no toxic effect according to the results of hematologic and biochemical profiles, including liver function tests (Chiasson, et al, 1994). Acarbose is contraindicated in people with inflammatory bowel disease, colonic ulceration or partial intestinal obstruction, predisposition to intestinal obstruction, chronic intestinal disease associated with marked disorders of absorption or digestion, conditions which might be exacerbated by increased intestinal gas formation (like hernias), or impaired hepatic function. People taking the maximum dose (200 mg three times daily) should be "monitored closely, preferably at monthly intervals, for the first six months."
Exercise and low glycemic diet works the best!
How could you synthesis Acarbose ?,
Acarbose is an anti-diabetic drug used to treat type 2 diabetes mellitus. It is sold in the USA from Bayer as PRECOSE®.
Originally extracted from fungi or plants, the synthesis of these kinds of drugs are covered by US Patents. There are several analogs made synthetically.
If your interest is for study, the most details can be found in the US Patent for Precose. I could not find this on-line, but did find an article about the synthesis of analogs (see below) and references to professional journals.
This is not easy bathtub or kitchen chemistry.
My doctor has given me Acarbose tablets.?, My doctor is trying to sort out my medical problems,im a complicated case! Anyway he has given me Acarbose tablets,just wondered if anyone took these?Will i lose weight?
These are tablets only licenced for diabetes. They do not promote weight loss.
I am Diabetic taking Acarbose to help with my blood sugar levels. It is great, except for the flatulence. HELP,
The passage of undigested carbs into the bowel give the bacteria there a feast which, alas, results in the production of copious amounts of gas. Mylicon or Gas-X may help some. Probiotics may also be of some benefit. Reducing the intake of starchy foods may have to be considered. Tablets or capsules of activated charcoal may also do some good. Search 'Acarbose' on the internet also, and see if you can find any links to sites that can offer other suggestions for help with this problem. Good luck.