Indications

Glibenclamide is used in the treatment of non insulin dependent diabetes melitus (NIDDM). It is ineffective in completely pancreatectomized patients and in juvenile-onset type of diabetes, in which the pancreas has lost all or nearly all of its capacity to secrete insulin. Such patients require insulin and attempts to control them with oral therapy are dangerous and doomed to failure.

Therapeutic Class

Sulfonylureas

Pharmacology

Glibenclamide is an orally effective hypoglycaemic agent that reduces blood sugar concentration by stimulating secretion of endogenous insulin from the pancreatic β-cells. It stimulates the mobilization of endogenous insulin with a lower dosage and with few incidence of side effects that any available anti-diabetic. Hypoglycaemic action associated with short-term therapy appears to include reduction of basal hepatic glucose production and enhancement of peripheral insulin action at target sites.

Dosage & Administration

Initially stabilization dosage: Glibenclamide half tablet (2.5 mg) should be taken initially during or immediately after breakfast. 3-5 days after initiation of the drug, the blood sugar level and urine sugar level should be checked. Daily dose of ½ tablet (2.5 mg) may be continued as maintenance therapy if good control has been achieved. If the result is not good, increment of daily dose in steps of ½ tablet (2.5 mg) is necessary at intervals of 3-5 days up to a maximum of 3 tablets. Daily doses in excess of 10 mg may be taken in 2 divided doses. Patients should be given ½ to 1 tablet of Glibenclamide in changing over from other oral anti-diabetics with a similar action.

Change over from insulin to Glibenclamide: The mildly diabetic patient whose insulin requirement is fewer than 20 units daily, can be started on the initial dosage of Glibenclamide with immediate discontinuation of insulin. If the insulin requirement is moderate or high, the changeover should be made gradually by giving insulin and Glibenclamide simultaneously and slowly cutting down the dose of insulin.

When insulin requirements are increased as in fever, surgical interventions or trauma, the Glibenclamide alone is inadequate and the patient must be given insulin to carry him or her through such critical situation.

This changeover from insulin to Glibenclamide is strictly for NIDDM of fairly recent onset which is being controlled on small doses of insulin. This should preferably be done in hospital or with daily medical supervision.

Interaction

Alcohol, cyclophosphamide, dicoumarol, monoamino oxidase inhibitors, phenylbutazone, propranolol and other beta-adrenergic blocking agents and certain long-acting sulphonamides may enhance the hypoglycemic effect of Glibenclamide

Contraindications

Severe metabolic de-compensation with acidosis, pre-comatose states and diabetic coma, severe renal or hepatic dysfunction or serious impairment of typhoid or adrenal function; pregnancy, diabetes mellitus complicated by fever, trauma or gangrene.

Side Effects

Glibenclamide is well tolerated. Few side effects that may arise include nausea, vomiting, epigastric pain, dizziness, weakness, paraesthesia and headache. Allergic skin reactions and haemopoietic reactions (leukopenia, thrombocytopenia, etc.) are occasionally observed.

Pregnancy & Lactation

There is no information on the use of Glibenclamide in human pregnancy but it has been in wide, general use for many years without apparent ill consequence. Animal studies have shown no hazard. It has not yet been established whether Glibenclamide is transferred to human milk. However, other sulphonylureas have been found in milk and there is no evidence to suggest that Glibenclamide differs from the group in this respect.

Precautions & Warnings

Weight reduction is of the greatest importance in the treatment of diabetes. A vigorous effort must be made by the patient and the physician to reduce the patient’s weight as an integral part of diabetic treatment, irrespective of the drug chosen.

Overdose Effects

Symptoms: Hypoglycaemia.

Management: Mild hypoglycaemic symptoms without loss of consciousness or neurologic findings may be treated with oral glucose and adjust drug dosage and/or meal patterns.

Storage Conditions

Should be stored in a dry place below 30˚ C.