Acarbose

(BAN, USAN, rINN)
Acarbose Chemical formula
Synonyms: Acarbosa; Acarbosum; Akarboosi; Akarbos; Akarbosa; Akarboz; Akarboze˙; Bay-g-5421. O-{4-Amino-4,6-dideoxyN[(1S,4R,5S,6S)4,5,6-trihydroxy-3-hydroxymethylcyclohex-2-enyl]pyranosyl}-(1→4)O
Cyrillic synonym: Акарбоза.

💊 Chemical information

Chemical formula: C25H43NO18 = 645.6.
CAS — 56180-94-0.
ATC — A10BF01.
ATC Vet — QA10BF01.

Pharmacopoeias.

In Eur. and US.

Ph. Eur. 6.2

(Acarbose). A white or yellowish, amorphous, hygroscopic powder. Very soluble in water; practically insoluble in dichloromethane; soluble in methyl alcohol. A 5% solution in water has a pH of 5.5 to 7.5. Store in airtight containers.

USP 31

(Acarbose). Produced by certain strains of Actinoplanes utahensis. Store in airtight containers.

💊 Adverse Effects

Acarbose often causes gastrointestinal disturbances, particularly flatulence due to bacterial action on nonabsorbed carbohydrate in the colon. Abdominal distension, diarrhoea, and pain may occur. Ileus has been rarely reported. A decrease in dosage and improved dietary habits may reduce these adverse effects. Hepatotoxicity may occur and may necessitate a reduction in dosage or withdrawal of the drug. Skin reactions have occurred rarely. Very rarely oedema has been reported.

Incidence of adverse effects.

The manufacturers reported that adverse effects of acarbose were rarer in a postmarketing surveillance study than in previous clinical trials;1 this was held to represent better tailoring of individual doses to patient tolerability.
1. Spengler M, Cagatay M. The use of acarbose in the primary-care setting: evaluation of efficacy and tolerability of acarbose by postmarketing surveillance study. Clin Invest Med 1995; 18: 325–31.

Effects on the liver.

Hepatocellular liver damage, with jaundice and elevated serum aminotransferases, have been reported in patients receiving acarbose.1-3 Symptoms resolved on stopping the drug.
1. Andrade RJ, et al. Hepatic injury caused by acarbose. Ann Intern Med 1996; 124: 931
2. Carrascosa M, et al. Acarbose-induced acute severe hepatotoxicity. Lancet 1997; 349: 698–9
3. Fujimoto Y, et al. Acarbose-induced hepatic injury. Lancet 1998; 351: 340.

Effects on the skin.

Generalised erythema multiforme and eosinophilia occurred in a male diabetic patient 13 days after starting acarbose.1 The hypersensitivity reaction was confirmed by rechallenge.
1. Kono T, et al. Acarbose-induced generalised erythema multiforme. Lancet 1999; 354: 396–7.

💊 Precautions

Acarbose is contra-indicated in inflammatory bowel disease, particularly where there is associated ulceration, and in gastrointestinal obstruction or patients predisposed to it. It should be avoided in patients with chronic intestinal diseases that significantly affect digestion or absorption, and in conditions which may deteriorate as a result of increased gas formation, such as hernia. Acarbose is also contra-indicated in patients with hepatic impairment and liver enzyme values should be monitored, particularly at high doses. If hypoglycaemia should develop in a patient receiving acarbose it needs to be treated with glucose, since the action of acarbose inhibits the hydrolysis of disaccharides.

Breast feeding.

In the absence of evidence, licensed product information recommends that acarbose should be avoided during breast feeding.

💊 Interactions

Acarbose may enhance the effects of other antidiabetics, including insulin, and a reduction in their dosage may be needed. Use with gastrointestinal adsorbents and digestive enzyme preparations can diminish the effects of acarbose and should be avoided. Neomycin and colestyramine may enhance the effects of acarbose and a reduction in its dosage may be required. Acarbose may inhibit the absorption of digoxin.

💊 Pharmacokinetics

After ingestion of acarbose, the majority of active unchanged drug remains in the lumen of the gastrointestinal tract to exert its pharmacological activity and is metabolised by intestinal enzymes and by the microbial flora. Ultimately about 35% of a dose is absorbed in the form of metabolites. Acarbose is excreted in the urine and faeces.

💊 Uses and Administration

Acarbose is an inhibitor of alpha glucosidases, especially sucrase. This slows the digestion and absorption of carbohydrates in the small intestine and hence reduces the increase in blood-glucose concentrations after a carbohydrate load. It is given in the treatment of type 2 diabetes mellitus either alone or with a sulfonylurea, biguanide, or insulin. Acarbose treatment may be started with a low oral dose of 25 or 50 mg daily to minimise gastrointestinal disturbance. It is then gradually increased to a usual dose of 25 or 50 mg three times daily, immediately before food. Doses up to 100 to 200 mg three times daily may be given if necessary. Some benefit has also been found when acarbose is used to supplement insulin therapy in type 1 diabetes mellitus. Acarbose has also been studied for the treatment of reactive hypoglycaemia, the dumping syndrome, and certain types of hyperlipoproteinaemia.
1. Chiasson J-L, et al. The efficacy of acarbose in the treatment of patients with non-insulin-dependent diabetes mellitus: a multicenter controlled clinical trial. Ann Intern Med 1994; 121: 928–35.
2. Coniff RF, et al. Multicenter, placebo-controlled trial comparing acarbose (BAY g 5421) with placebo, tolbutamide, and tolbutamide-plus-acarbose in non-insulin-dependent diabetes mellitus. Am J Med 1995; 98: 443–51
3. Spengler M, Cagatay M. The use of acarbose in the primarycare setting: evaluation of efficacy and tolerability of acarbose by postmarketing surveillance study. Clin Invest Med 1995; 18: 325–31
4. Salvatore T, Giugliano D. Pharmacokinetic-pharmacodynamic relationships of acarbose. Clin Pharmacokinet 1996; 30: 94–106
5. Anonymous. Acarbose for diabetes mellitus. Med Lett Drugs Ther 1996; 38: 9–10
6. Hoffman J, Spengler M. Efficacy of 24-week monotherapy with acarbose, metformin, or placebo in dietary-treated NIDDM patients: the Essen-II study. Am J Med 1997; 103: 483–90
7. Hollander P, et al. Acarbose in the treatment of type I diabetes. Diabetes Care 1997; 20: 248–53
8. Buse J, et al. The PROTECT study: final results of a large multicenter postmarketing study in patients with type 2 diabetes. Clin Ther 1998; 20: 257–69
9. Holman RR, et al. A randomized double-blind trial of acarbose in type 2 diabetes shows improved glycemic control over 3 years (UK Prospective Diabetes Study 44). Diabetes Care 1999; 22: 960–4
10. Riccardi G, et al. Efficacy and safety of acarbose in the treatment of type 1 diabetes mellitus: a placebo-controlled, doubleblind, multicentre study. Diabet Med 1999; 16: 228–32
11. Chiasson J-L, et al. Acarbose for prevention of type 2 diabetes mellitus: the STOP-NIDDM randomised trial. Lancet 2002; 359: 2072–7.

Impaired glucose tolerance.

A prospective study of patients with impaired glucose tolerance concluded that acarbose significantly reduced the incidence of cardiovascular disease and hypertension.1
1. Chiasson J-L, et al. Acarbose treatment and the risk of cardiovascular disease and hypertension in patients with impaired glucose tolerance: the STOP-NIDDM trial. JAMA 2003; 290: 486–94.

💊 Preparations

Proprietary Preparations

Arg.: Glucobay; Austral.: Glucobay; Austria: Glucobay; Belg.: Glucobay; Braz.: Aglucose; Glucobay; Canad.: Prandase; Chile: Glucobay; Cz.: Glucobay; Denm.: Glucobay; Fr.: Glucor; Ger.: Glucobay; Gr.: Glucobay; Hong Kong: Glucobay; Hung.: Glucobay; India: Acarbay; Asucrose; Glubose; Glucar; Glucobay; Indon.: Glucobay; Irl.: Glucobay; Israel: Prandase; Ital.: Glicobase; Glucobay; Malaysia: Dibose; Glucar; Glucobay; Precose; Mex.: Glucobay; Incardel; Sincrosa; Neth.: Glucobay; Norw.: Glucobay; NZ: Glucobay; Philipp.: Glucobay; Gluconase; Pol.: Glucobay; Port.: Glucobay; Rus.: Glucobay (Глюкобай); S.Afr.: Glucobay; Singapore: Glucobay; Spain: Glucobay; Glumida; Swed.: Glucobay; Switz.: Glucobay; Thai.: Glucobay; Turk.: Glucobay; Glynose; UK: Glucobay; USA: Precose; Venez.: Glucobay.
Published October 08, 2018.