ACARBOSE

Posology Owing to the great individual variation of glucosidase activity in the intestinal mucosa, there is no fixed dosage regimen, and patients should be treated according to clinical response and tolerance of intestinal side effects.

Adults The recommended initial dose is 50mg three times a day. However, some patients may benefit from more gradual initial dose titration to minimise gastrointestinal side effects. This may be achieved by initiating treatment at 50mg once or twice a day, with subsequent titration to a three times a day regimen.

If after six to eight weeks' treatment patients show an inadequate clinical response, the dosage may be increased to 100mg three times a day. A further increase in dosage to a maximum of 200mg three times a day may occasionally be necessary.

Acarbose is intended for continuous long-term treatment. 8).

Elderly subjects:

No modification of the normal adult dosage regimen is necessary. Paediatric population The efficacy and safety of acarbose in children and adolescents have not been established. Acarbose is not recommended for patients under the age of 18 years.

Renal or hepatic impairment See section

The frequencies of adverse drug reactions (ADRs) reported with acarbose, based on placebo controlled studies (acarbose N = 8 595; placebo N = 7 278) are summarised in the table below. Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness.

Frequencies are defined as very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1000 to <1/100); rare (≥1/10 000 to <1/1000); very rare (<1/10 000). The ADRs identified only during post-marketing surveillance (status: 31 Dec 2005), and for which a frequency could not be estimated, are listed under “not known”.

System Organ Class (MedDRA) Very common Common Uncommo n Rare Not known Blood and lymphatic system disorders Thrombo- cytopenia Immune system disorders Drug hypersensitivit y and hypersensitivit y (rash, erythema, exanthema, urticaria) Vascular disorders Oedema System Organ Class (MedDRA) Very common Common Uncommo n Rare Not known Gastrointestinal disorders Flatulence Diarrhea Gastrointestinal and abdominal pains Nausea Vomiting Dyspepsia Subileus/Ileus Pneumatosis cystoidis intestinalis i Hepatobiliary Disorders Increase in transami- nases Jaundice Hepatitis Skin and subcutaneous tissue disorders Acute generalised exanthematous pustulosis In post-marketing, cases of liver disorder, hepatic function abnormal, and liver injury have been reported.

Individual cases of fulminant hepatitis with fatal outcome have also been reported, particularly from Japan. In patients receiving the recommended daily dose of 150 mg to 300 mg acarbose , clinically relevant abnormal liver function tests (three times above upper limits of normal ranges) were rarely observed.

4). If the prescribed diabetic diet is not observed the intestinal side effects may be intensified. If strongly distressing symptoms develop in spite of adherence to the diabetic diet prescribed, the doctor must be consulted and the dose temporarily or permanently reduced.

Hypoglycaemia:

Acarbose has an antihyperglycaemic effect, but does not itself induce hypoglycaemia. g. sulphonylureas metformin, or insulin) a fall of the blood glucose values into the hypoglycaemic range may require a dose adaption of the respective co-medication.

5). Episodes of hypoglycaemia occurring during therapy must, where appropriate, be treated by the administration of glucose, not sucrose. This is because acarbose will delay the digestion and absorption of disaccharides, but not monosaccharides.

Transaminases:

Cases of fulminant hepatitis have been reported during acarbose therapy. The mechanism is unknown, but acarbose may contribute to a multifactorial pathophysiology of liver injury. 8). If elevated transaminases are observed, withdrawal of therapy may be warranted, particularly if the elevations persist.

In such circumstances, patients should be monitored at weekly intervals until normal values are established. g. hydrotalcite, has been shown not to ameliorate the acute gastrointestinal symptoms of Acarbose in higher dosage and should, therefore, not be recommended to patients for this purpose.

3. Method of administration Acarbose tablets are taken orally and should be swallowed whole with a little liquid directly before the meal or chewed with the first mouthful of food. 1, pregnancy and in nursing mothers. Acarbose is also contraindicated in patients with inflammatory bowel disease, colonic ulceration, partial intestinal obstruction or in patients predisposed to intestinal obstruction.

g. larger hernias. -Acarbose is contraindicated in patients with hepatic impairment. 73m².