INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo GLUCOBAY® 50, 100

SCHEDULING STATUS:
S4

PROPRIETARY NAME
(and dosage form):

GLUCOBAY® 50, 100
Tablets

COMPOSITION:
GLUCOBAY 50 tablets contain 50 mg acarbose
GLUCOBAY 100 tablets contain 100 mg acarbose

PHARMACOLOGICAL CLASSIFICATION:
A 21.2 Oral hypoglycaemics

PHARMACOLOGICAL ACTION:
GLUCOBAY is a competitive inhibitor of intestinal alpha-glucosidases with maximum specific inhibitory activity against sucrose. Under the influence of GLUCOBAY, the digestion of starch and sucrose into absorbable monosaccharides in the small intestine is dose-dependently delayed. In diabetic subjects, this results in a lowering of postprandial hyperglycaemia.
GLUCOBAY has no stimulatory action on the pancreas.
Treatment with GLUCOBAY also results in a reduction of fasting blood glucose and to modest changes in levels of glycosylated haemoglobin (HbA
1, HbA1c). The changes may be a reduction or reduced deterioration in HbA1 or HbA1c levels, depending upon the patient's clinical status and disease progression. These parameters are affected in a dose-dependent manner by GLUCOBAY.
Following oral administration, only 1-2% is absorbed.

INDICATIONS:
GLUCOBAY is indicated for the treatment of non-insulin dependent diabetes mellitus (NIDDM) in patients inadequately controlled on diet alone, or on diet and oral hypoglycaemic agents.

CONTRA-INDICATIONS:
Known hypersensitivity to acarbose or any of the excipients, use in children less than 12 years of age, pregnancy and in nursing mothers. GLUCOBAY is also contra-indicated in patients with inflammatory bowel disease, colonic ulceration, partial intestinal obstruction or in patients predisposed to intestinal obstruction. In addition, GLUCOBAY should not be used in patients who have chronic intestinal diseases associated with marked disorders of digestion or absorption and in patients who suffer from states which may deteriorate as a result of increased gas formation in the intestine, (e.g. Roemheld’s syndrome [an angina pectoris-like syndrome or aggravation of an angina pectoris due to the post-prandial filling of the stomach] and larger hernias). GLUCOBAY is contra-indicated in patients with hepatic and severe renal impairment (creatinine clearance <25 mL/min/ 1,73m2).

WARNINGS:
Hypoglycaemia:
When administered alone, GLUCOBAY does not cause hypoglycaemia. It may, however, act to potentiate the hypoglycaemic effects of insulin, metformin and/or sulphonylurea drugs and the dosages of these agents may need to be modified accordingly.
In the management of episodes of hypoglycaemia occurring during therapy, it is essential that glucose and not sucrose is used. This is because acarbose will delay the digestion and absorption of disaccharides, but not monosaccharides.
Transaminases:
At higher doses, GLUCOBAY may give rise to transient idiosyncratic elevations of serum hepatic transaminases.
Asymptomatic liver enzyme elevations may occur. Therefore, liver enzyme monitoring should be considered during the first 6 to 12 months of treatment. Patients titrated to the maximum recommended dose of 200 mg three times a day should be closely monitored, preferably at monthly intervals for the first six months. If elevated transaminases are observed, a reduction in dosage or 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. In evaluable cases these changes were reversible on discontinuation of Glucobay therapy.
Interactions:
Intestinal adsorbents (e.g. charcoal) and digestive enzyme preparations containing carbohydrate splitting enzymes (e.g. amylase, pancreatin) may reduce the effect of GLUCOBAY and should not therefore be taken concomitantly.
The concomitant administration of neomycin may lead to enhanced reductions of postprandial blood glucose and to an increase in the frequency and severity of gastrointestinal side-effects. If the symptoms are severe, a temporary dose reduction of GLUCOBAY may be warranted.
The concomitant administration of cholestyramine may enhance the effects of GLUCOBAY, particularly with respect to reducing postprandial insulin levels. In the rare circumstance that both acarbose and cholestyramine therapy are withdrawn simultaneously, care is needed as a rebound phenomenon has been observed with respect to insulin levels in non-diabetic subjects.
In a pilot study to investigate a possible interaction between GLUCOBAY and nifedipine, no significant or reproducible changes were observed in the plasma nifedipine profiles.
Acarbose may affect digoxin bioavailability, which may require dose adjustment of digoxin.
The concomitant administration of metformin, sulphonylureas and/or insulin may enhance the antihyperglycaemic effects of GLUCOBAY. Hypoglycaemic shock may thus occur less frequently in patients taking these combinations.

DOSAGE AND DIRECTIONS FOR USE:
GLUCOBAY tablets are taken orally and should be chewed with the first mouthful of food, or swallowed whole with a little liquid directly before the meal. 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 50 mg three times a day. If after six to eight weeks treatment patients show an inadequate clinical response, the dosage may be increased to 100 mg three times a day. A further increase in dosage to a maximum of 200 mg three times a day may occasionally be necessary. GLUCOBAY is intended for continuous long-term treatment.
Elderly patients:
No modification of the normal adult dosage regimen is necessary.

SIDE EFFECTS AND SPECIAL PRECAUTIONS:
Owing to its mode of action, GLUCOBAY results in a greater proportion of dietary carbohydrate being digested in the large bowel. This carbohydrate may also be utilised by the intestinal flora, resulting in the increased formation of intestinal gas.
Flatulence, diarrhoea, abdominal pain, nausea, borborygmi and a feeling of fullness. Subileus/ileus may occur.
If the prescribed diabetic diet is not adhered to 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.
The symptoms are both dose and dietary substrate related and may subside with continued treatment. Symptoms can be reduced by adherence to the prescribed diabetic diet and the avoidance of sucrose or foodstuffs containing sugar. If symptoms are poorly tolerated, a reduction in dosage is recommended.
Should diarrhoea persist, patients should be closely monitored and the dosage reduced, or therapy withdrawn, if necessary.
The administration of antacid preparations containing magnesium and aluminium salts has been shown not to ameliorate the acute gastrointestinal symptoms of GLUCOBAY in higher dosage and should therefore not be recommended to patients for this purpose.
In individual cases, hypersensitive skin reactions may occur e.g. rash, erythema, exanthema and urticaria. Cases of jaundice and/or hepatitis, clinically relevant abnormal liver function tests (three times above upper limit of normal range) and associated liver damage have been reported less frequently. Abnormal values may be transient under ongoing Acarbose therapy (See Warnings).
Oedema has been observed less frequently.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
No information on overdosage is available. No specific antidotes to GLUCOBAY are known.
Intake of carbohydrate-containing meals or beverages should be avoided for 4-6 hours. Diarrhoea should be treated by standard measures.

IDENTIFICATION:
GLUCOBAY 50: Round, convex white to yellow tinged tablets with G 50 on the upper side and the BAYER cross on the lower side.
GLUCOBAY 100: Round, convex, scored white to yellow tinged scored tablets with G 100 on the upper side and the BAYER cross on the lower side.

PRESENTATION:
GLUCOBAY 50: Blister packs of 90 tablets
GLUCOBAY 100: Blister packs of 90 tablets

STORAGE INSTRUCTIONS:
Store below 25°C. Protect from moisture. Keep out of reach of children.
At higher temperatures and/or higher relative humidity, discolouration can occur in tablets that are not in the packs (blisters). Tablets should therefore not be removed from the foil until immediately prior to use.

REGISTRATION NUMBER:
                                ZIMBABWE ONLY
GLUCOBAY 50:         28/21.2/0425        2000/17.7/3650
GLUCOBAY 100:         28/21.2/0426        2000/17.7/3649

NAME AND BUSINESS ADDRESS OF THE APPLICANT:
Bayer (Pty) Ltd        Wrench Road        ISANDO        1600        Reg. No. 1968/011192/07

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
02/03/2001

® = Registered Trade Mark of Bayer AG, Germany

CCDS12/SA5                02D/0301

Updated on this site: February 2003
Source: Pharmaceutical Industry

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