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Indications/Uses
Diabetes mellitus of the maturity onset type which cannot be controlled by diet alone.
Dosage/Direction for Use
Adults: The total daily dose may vary from 40 to 320 mg taken orally. The dose should be adjusted according to the individual patient's response, commencing with 40-80 mg daily (1/2-1 tablet) and increasing until adequate control is achieved. A single dose should not exceed 160 mg (2 tablets). When higher doses are required, Gliclazide (Dianorm) 80 mg Tablets should be taken twice daily and according to the main meals of the day.
In obese patients or those not showing adequate response to Gliclazide (Dianorm) 80 mg Tablets alone, additional therapy may be required.
Transferring to Gliclazide (Dianorm): Patients who have previously been treated with sulphonylureas or biguanides alone or in combination may be transferred to Gliclazide (Dianorm). When Gliclazide (Dianorm) is administered as sole therapy to patients who had previously required combination therapy (e.g. biguanides plus sulphonylureas), careful observation of the patient is essential during the transitional phase. It is recommended that insulin treated patients should not be transferred to Gliclazide (Dianorm) therapy.
Elderly: Plasma clearance of gliclazide is not altered in the elderly and steady state plasma levels can therefore be expected to be similar to those in adults under 65 years. Clinical experience in the elderly to date shows that Gliclazide (Dianorm) 80 mg Tablets is effective and well tolerated. Care should be exercised, however, when prescribing sulphonylureas in the elderly due to a possible age-related increased risk of hypoglycemia.
Children: Gliclazide (Dianorm) 80 mg Tablets as with other sulphonylureas, is not indicated for the treatment of juvenile onset diabetes mellitus.
In obese patients or those not showing adequate response to Gliclazide (Dianorm) 80 mg Tablets alone, additional therapy may be required.
Transferring to Gliclazide (Dianorm): Patients who have previously been treated with sulphonylureas or biguanides alone or in combination may be transferred to Gliclazide (Dianorm). When Gliclazide (Dianorm) is administered as sole therapy to patients who had previously required combination therapy (e.g. biguanides plus sulphonylureas), careful observation of the patient is essential during the transitional phase. It is recommended that insulin treated patients should not be transferred to Gliclazide (Dianorm) therapy.
Elderly: Plasma clearance of gliclazide is not altered in the elderly and steady state plasma levels can therefore be expected to be similar to those in adults under 65 years. Clinical experience in the elderly to date shows that Gliclazide (Dianorm) 80 mg Tablets is effective and well tolerated. Care should be exercised, however, when prescribing sulphonylureas in the elderly due to a possible age-related increased risk of hypoglycemia.
Children: Gliclazide (Dianorm) 80 mg Tablets as with other sulphonylureas, is not indicated for the treatment of juvenile onset diabetes mellitus.
Overdosage
An overdose of sulphonylureas may cause hypoglycemia.
Moderate symptoms of hypoglycemia, without any loss of consciousness or neurological signs, must be corrected by carbohydrate intake, dose adjustment and/or change of diet. Strict monitoring should be continued until the doctor is sure that the patient is out of danger.
Severe hypoglycemic reactions, with coma, convulsions or other neurological disorders are possible and must be treated as a medical emergency, requiring immediate hospitalization.
If hypoglycemic coma is diagnosed or suspected, the patient should be given a rapid I.V. injection of 50 mL of concentrated glucose solution (20 to 30%). This should be followed by continuous infusion of a more dilute glucose solution (10%) at a rate that will maintain blood glucose levels above 1 g/L. Patients should be monitored closely and, depending on the patient's condition after this time, the doctor will decide if further monitoring is necessary.
Dialysis is of no benefit to patients due to the strong binding of gliclazide to proteins.
Moderate symptoms of hypoglycemia, without any loss of consciousness or neurological signs, must be corrected by carbohydrate intake, dose adjustment and/or change of diet. Strict monitoring should be continued until the doctor is sure that the patient is out of danger.
Severe hypoglycemic reactions, with coma, convulsions or other neurological disorders are possible and must be treated as a medical emergency, requiring immediate hospitalization.
If hypoglycemic coma is diagnosed or suspected, the patient should be given a rapid I.V. injection of 50 mL of concentrated glucose solution (20 to 30%). This should be followed by continuous infusion of a more dilute glucose solution (10%) at a rate that will maintain blood glucose levels above 1 g/L. Patients should be monitored closely and, depending on the patient's condition after this time, the doctor will decide if further monitoring is necessary.
Dialysis is of no benefit to patients due to the strong binding of gliclazide to proteins.
Administration
Should be taken with food.
Contraindications
Gliclazide (Dianorm) should not be used in diabetes complicated by acidosis, ketosis or coma, or in patients with a history of repeated episodes of ketoacidosis or coma.
Juvenile onset diabetes and unstable or brittle diabetes: As sulphonylurea hypoglycemic agents are not effective in juvenile onset, unstable or brittle diabetes, Gliclazide (Dianorm) should not be used in these conditions.
Severe renal and liver disease: Gliclazide (Dianorm) is contraindicated in severe hepatic or renal insufficiency. Caution should be exercised and dosage reduction may be required when using Gliclazide (Dianorm) in patients with impaired renal or hepatic function.
Hypersensitivity: Gliclazide (Dianorm) should not be used in patients with known sensitivity to sulphonylureas.
Juvenile onset diabetes and unstable or brittle diabetes: As sulphonylurea hypoglycemic agents are not effective in juvenile onset, unstable or brittle diabetes, Gliclazide (Dianorm) should not be used in these conditions.
Severe renal and liver disease: Gliclazide (Dianorm) is contraindicated in severe hepatic or renal insufficiency. Caution should be exercised and dosage reduction may be required when using Gliclazide (Dianorm) in patients with impaired renal or hepatic function.
Hypersensitivity: Gliclazide (Dianorm) should not be used in patients with known sensitivity to sulphonylureas.
Warnings
Acute complications such as severe trauma, fever, infection or surgery: These acute complications provoke additional metabolic stress which accentuate the predisposition to hypoglycemia and ketosis. Patients presenting with such conditions may require insulin to maintain control. It is not appropriate to increase the dosage of Gliclazide (Dianorm).
Hypoglycemia: This treatment should be prescribed only if the patient is likely to have a regular food intake (including breakfast). It is important to have a regular carbohydrate intake due to the increased risk of hypoglycemia if a meal is taken late, if an inadequate amount of food is consumed or if the food is low in carbohydrate. Hypoglycemia is more likely to occur during low-calorie diets, following prolonged or strenuous exercise, alcohol intake or if a combination of hypoglycemic agents is being used.
Hypoglycemia may occur following administration of sulphonylureas. Some cases may be severe and prolonged. Hospitalization may be necessary and glucose administration may need to be continued for several days.
Careful selection of patients, of the dose used, and clear patient directions are necessary to reduce the risk of hypoglycemic episodes.
Factors which increase the risk of hypoglycemia: patient refuses or (particularly in elderly subjects) is unable to cooperate; malnutrition, irregular mealtimes, skipping meals, periods of fasting or dietary changes; imbalance between physical exercise and carbohydrate intake; renal insufficiency; severe hepatic insufficiency; overdose of Gliclazide (Dianorm) 80 mg Tablet; certain endocrine disorders: thyroid disorders, hypopituitarism and adrenal insufficiency; concomitant administration of certain other medicines.
Renal and hepatic insufficiency: The pharmacokinetics and/or pharmacodynamics of gliclazide may be altered in patients with hepatic insufficiency or severe renal failure. A hypoglycemic episode occurring in these patients may be prolonged, so appropriate management should be initiated.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Treatment of patients with G6PD-deficiency with sulphonylurea agents can lead to hemolytic anemia. Since gliclazide belongs to the class of sulphonylurea agents, caution should be used in patients with G6PD-deficiency and a non-sulphonylurea alternative should be considered.
Hypoglycemia: This treatment should be prescribed only if the patient is likely to have a regular food intake (including breakfast). It is important to have a regular carbohydrate intake due to the increased risk of hypoglycemia if a meal is taken late, if an inadequate amount of food is consumed or if the food is low in carbohydrate. Hypoglycemia is more likely to occur during low-calorie diets, following prolonged or strenuous exercise, alcohol intake or if a combination of hypoglycemic agents is being used.
Hypoglycemia may occur following administration of sulphonylureas. Some cases may be severe and prolonged. Hospitalization may be necessary and glucose administration may need to be continued for several days.
Careful selection of patients, of the dose used, and clear patient directions are necessary to reduce the risk of hypoglycemic episodes.
Factors which increase the risk of hypoglycemia: patient refuses or (particularly in elderly subjects) is unable to cooperate; malnutrition, irregular mealtimes, skipping meals, periods of fasting or dietary changes; imbalance between physical exercise and carbohydrate intake; renal insufficiency; severe hepatic insufficiency; overdose of Gliclazide (Dianorm) 80 mg Tablet; certain endocrine disorders: thyroid disorders, hypopituitarism and adrenal insufficiency; concomitant administration of certain other medicines.
Renal and hepatic insufficiency: The pharmacokinetics and/or pharmacodynamics of gliclazide may be altered in patients with hepatic insufficiency or severe renal failure. A hypoglycemic episode occurring in these patients may be prolonged, so appropriate management should be initiated.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Treatment of patients with G6PD-deficiency with sulphonylurea agents can lead to hemolytic anemia. Since gliclazide belongs to the class of sulphonylurea agents, caution should be used in patients with G6PD-deficiency and a non-sulphonylurea alternative should be considered.
Special Precautions
Monitoring of diabetic state: As with other antidiabetic therapies, patients must be under close medical supervision. Patients treated with Gliclazide (Dianorm) must be monitored regularly to ensure optimal control of the diabetic state and, where necessary, for the adjustment of dosage. Particular care must be taken during the initial period of stabilization.
Dietary restrictions: Treatment with Gliclazide (Dianorm) does not obviate the necessity for maintaining standard dietary regulations.
Patient awareness: Comprehensive instructions must be given to the patient about the nature of the disease and what must be done to detect and prevent complications.
Special Populations: Not known.
Dietary restrictions: Treatment with Gliclazide (Dianorm) does not obviate the necessity for maintaining standard dietary regulations.
Patient awareness: Comprehensive instructions must be given to the patient about the nature of the disease and what must be done to detect and prevent complications.
Special Populations: Not known.
Use In Pregnancy & Lactation
Use in Pregnancy (Risk Category: C): For gliclazide, no clinical data on exposed pregnancies are available, even though there are few data with other sulphonylureas. Control of diabetes should be obtained before the time of conception to reduce the risk of congenital abnormalities linked to uncontrolled diabetes. Oral hypoglycemic agents are not suitable; insulin is the drug of first choice for treatment of diabetes during pregnancy.
It is recommended that oral hypoglycemic therapy is changed to insulin before a pregnancy is attempted, or as soon as pregnancy is discovered.
Use in Lactation: It is not known whether gliclazide or its metabolites are excreted in breast milk. Given the risk of neonatal hypoglycemia, the product is contraindicated in breastfeeding mothers.
It is recommended that oral hypoglycemic therapy is changed to insulin before a pregnancy is attempted, or as soon as pregnancy is discovered.
Use in Lactation: It is not known whether gliclazide or its metabolites are excreted in breast milk. Given the risk of neonatal hypoglycemia, the product is contraindicated in breastfeeding mothers.
Adverse Reactions
Based on the experience with gliclazide, the following undesirable effects have been reported.
Hypoglycemia: As for other sulphonylureas, treatment with Gliclazide (Dianorm) 80 mg Tablets can cause hypoglycemia, if mealtimes are irregular and, in particular, if meals are skipped. Possible symptoms of hypoglycemia are: headache, intense hunger, nausea, vomiting, lassitude, sleep disorders, agitation, aggression, poor concentration, reduced awareness and slowed reactions, depression, confusion, visual and speech disorders, aphasia, tremor, paresis, sensory disorders, dizziness, feeling of powerlessness, loss of self-control, delirium, convulsions, shallow respiration, bradycardia, drowsiness and loss of consciousness, possibly resulting in coma and lethal outcome. In addition, signs of adrenergic counter-regulation may be observed: sweating, clammy skin, anxiety, tachycardia, hypertension, palpitations, angina pectoris and cardiac arrhythmia.
Usually, symptoms disappear after intake of carbohydrates (sugar). However, artificial sweeteners have no effect. Experience with other sulphonylureas shows that hypoglycemia can recur even when measures prove effective initially.
If a hypoglycemic episode is severe or prolonged, and even if it is temporarily controlled by intake of sugar, immediate medical treatment or even hospitalization is required.
Gastrointestinal disturbances, including abdominal pain, nausea, vomiting, dyspepsia, diarrhea, and constipation have been reported: if these should occur they can be avoided or minimized if gliclazide is taken with breakfast.
The following undesirable effects have been more rarely reported: Skin and subcutaneous tissue disorders: rash, pruritus, urticaria, angioedema, erythema, maculopapular rashes, bullous reactions (such as Stevens-Johnson syndrome and toxic epidermal necrolysis).
Blood and lymphatic system disorders: Changes in hematology are rare. They may include anemia, leucopenia, thrombocytopenia, granulocytopenia. These are in general reversible upon discontinuation of medication.
Hepatobiliary disorders: raised hepatic enzyme levels (AST, ALT, alkaline phosphatase), hepatitis (isolated reports). Discontinue treatment if cholestatic jaundice appears.
These symptoms usually disappear after discontinuation of treatment.
Eye disorders: Transient visual disturbances may occur especially on initiation of treatment, due to changes in blood glucose levels.
Class attribution effects: As for other sulphonylureas, the following adverse events have been observed: cases of erythrocytopenia, agranulocytosis, hemolytic anemia, pancytopenia, allergic vasculitis, hyponatremia, elevated liver enzyme levels and even impairment of liver function (e.g. with cholestasis and jaundice) and hepatitis which regressed after withdrawal of the sulphonylurea or led to life-threatening liver failure in isolated cases.
At first sign of any adverse drug reaction, patient must seek medical attention immediately.
Hypoglycemia: As for other sulphonylureas, treatment with Gliclazide (Dianorm) 80 mg Tablets can cause hypoglycemia, if mealtimes are irregular and, in particular, if meals are skipped. Possible symptoms of hypoglycemia are: headache, intense hunger, nausea, vomiting, lassitude, sleep disorders, agitation, aggression, poor concentration, reduced awareness and slowed reactions, depression, confusion, visual and speech disorders, aphasia, tremor, paresis, sensory disorders, dizziness, feeling of powerlessness, loss of self-control, delirium, convulsions, shallow respiration, bradycardia, drowsiness and loss of consciousness, possibly resulting in coma and lethal outcome. In addition, signs of adrenergic counter-regulation may be observed: sweating, clammy skin, anxiety, tachycardia, hypertension, palpitations, angina pectoris and cardiac arrhythmia.
Usually, symptoms disappear after intake of carbohydrates (sugar). However, artificial sweeteners have no effect. Experience with other sulphonylureas shows that hypoglycemia can recur even when measures prove effective initially.
If a hypoglycemic episode is severe or prolonged, and even if it is temporarily controlled by intake of sugar, immediate medical treatment or even hospitalization is required.
Gastrointestinal disturbances, including abdominal pain, nausea, vomiting, dyspepsia, diarrhea, and constipation have been reported: if these should occur they can be avoided or minimized if gliclazide is taken with breakfast.
The following undesirable effects have been more rarely reported: Skin and subcutaneous tissue disorders: rash, pruritus, urticaria, angioedema, erythema, maculopapular rashes, bullous reactions (such as Stevens-Johnson syndrome and toxic epidermal necrolysis).
Blood and lymphatic system disorders: Changes in hematology are rare. They may include anemia, leucopenia, thrombocytopenia, granulocytopenia. These are in general reversible upon discontinuation of medication.
Hepatobiliary disorders: raised hepatic enzyme levels (AST, ALT, alkaline phosphatase), hepatitis (isolated reports). Discontinue treatment if cholestatic jaundice appears.
These symptoms usually disappear after discontinuation of treatment.
Eye disorders: Transient visual disturbances may occur especially on initiation of treatment, due to changes in blood glucose levels.
Class attribution effects: As for other sulphonylureas, the following adverse events have been observed: cases of erythrocytopenia, agranulocytosis, hemolytic anemia, pancytopenia, allergic vasculitis, hyponatremia, elevated liver enzyme levels and even impairment of liver function (e.g. with cholestasis and jaundice) and hepatitis which regressed after withdrawal of the sulphonylurea or led to life-threatening liver failure in isolated cases.
At first sign of any adverse drug reaction, patient must seek medical attention immediately.
Drug Interactions
Disturbance of blood sugar control: As with all hypoglycemics, caution should be observed in administering thiazide diuretics to patients on Gliclazide (Dianorm) therapy, since thiazides have been reported to aggravate the diabetic state. Other drugs which may adversely affect blood sugar control with hypoglycemic agents in some patients include barbiturates, glucocorticoids and estrogens.
The following products are likely to increase the risk of hypoglycemia: Certain drugs may potentiate the effect of Gliclazide (Dianorm) and thereby increase the risk of hypoglycemia. These include insulin, biguanides, sulphonamides, oxyphenbutazone, phenylbutazone, clofibrate, salicylates, coumarin derivatives, chloramphenicol, MAOIs, β-blockers, cimetidine and ethanol.
Contraindicated combination: Miconazole (systemic route, oromucosal gel): increases the hypoglycemic effect with possible onset of hypoglycemic symptoms, or even coma.
Combinations which are not recommended: Phenylbutazone (systemic route): increases the hypoglycemic effect of sulphonylureas (displaces their binding to plasma proteins and/or reduces their elimination). It is preferable to use a different anti-inflammatory agent, or else to warn the patient and emphasize the importance of self-monitoring.
Where necessary, adjust the dose during and after treatment with the anti-inflammatory agent.
Alcohol: increases the hypoglycemic reaction (by inhibiting compensatory reactions) that can lead to the onset of hypoglycemic coma. Avoid alcohol or medicines containing alcohol.
Combinations requiring precautions for use: Potentiation of the blood glucose lowering effect and thus, in some instances, hypoglycemia may occur when one of the following drugs is taken: other antidiabetic agents (insulins, acarbose, metformin, thiazolidinediones, dipeptidyl peptidase-4 inhibitors, GLP-1 receptor agonists), betablockers, fluconazole, angiotensin converting enzyme inhibitors (captopril, enalapril), H2-receptor antagonists, MAOIs, sulphonamides, clarithromycin and nonsteroidal anti-inflammatory agents.
The following products may cause an increase in blood glucose levels: Combination which is not recommended: Danazol: diabetogenic effect of danazol. If the use of this active substance cannot be avoided, warn the patient and emphasize the importance of urine and blood glucose monitoring. It may be necessary to adjust the dose of the antidiabetic agent during and after treatment with danazol.
Combinations requiring precautions during use: Chlorpromazine (neuroleptic agent): high doses (>100 mg per day of chlorpromazine) increase blood glucose levels (reduced insulin release). Warn the patient and emphasize the importance of blood glucose monitoring. It may be necessary to adjust the dose of the antidiabetic active substance during and after treatment with the neuroleptic agent.
Glucocorticoids (systemic and local route: intra-articular, cutaneous and rectal preparations) and tetracosactrin: increase in blood glucose levels with possible ketosis (reduced tolerance to carbohydrates due to glucocorticoids). Warn the patient and emphasize the importance of blood glucose monitoring, particularly at the start of treatment. It may be necessary to adjust the dose of the antidiabetic active substance during and after treatment with glucocorticoids.
Ritodrine, salbutamol, terbutaline: (I.V.) Increased blood glucose levels due to beta-2 agonist effects. Emphasize the importance of monitoring blood glucose levels. If necessary, switch to insulin.
Combination which must be taken into account: Anticoagulant therapy (Warfarin): Sulphonylureas may lead to potentiation of anticoagulation during concurrent treatment. Adjustment of the anticoagulant may be necessary.
The following products are likely to increase the risk of hypoglycemia: Certain drugs may potentiate the effect of Gliclazide (Dianorm) and thereby increase the risk of hypoglycemia. These include insulin, biguanides, sulphonamides, oxyphenbutazone, phenylbutazone, clofibrate, salicylates, coumarin derivatives, chloramphenicol, MAOIs, β-blockers, cimetidine and ethanol.
Contraindicated combination: Miconazole (systemic route, oromucosal gel): increases the hypoglycemic effect with possible onset of hypoglycemic symptoms, or even coma.
Combinations which are not recommended: Phenylbutazone (systemic route): increases the hypoglycemic effect of sulphonylureas (displaces their binding to plasma proteins and/or reduces their elimination). It is preferable to use a different anti-inflammatory agent, or else to warn the patient and emphasize the importance of self-monitoring.
Where necessary, adjust the dose during and after treatment with the anti-inflammatory agent.
Alcohol: increases the hypoglycemic reaction (by inhibiting compensatory reactions) that can lead to the onset of hypoglycemic coma. Avoid alcohol or medicines containing alcohol.
Combinations requiring precautions for use: Potentiation of the blood glucose lowering effect and thus, in some instances, hypoglycemia may occur when one of the following drugs is taken: other antidiabetic agents (insulins, acarbose, metformin, thiazolidinediones, dipeptidyl peptidase-4 inhibitors, GLP-1 receptor agonists), betablockers, fluconazole, angiotensin converting enzyme inhibitors (captopril, enalapril), H2-receptor antagonists, MAOIs, sulphonamides, clarithromycin and nonsteroidal anti-inflammatory agents.
The following products may cause an increase in blood glucose levels: Combination which is not recommended: Danazol: diabetogenic effect of danazol. If the use of this active substance cannot be avoided, warn the patient and emphasize the importance of urine and blood glucose monitoring. It may be necessary to adjust the dose of the antidiabetic agent during and after treatment with danazol.
Combinations requiring precautions during use: Chlorpromazine (neuroleptic agent): high doses (>100 mg per day of chlorpromazine) increase blood glucose levels (reduced insulin release). Warn the patient and emphasize the importance of blood glucose monitoring. It may be necessary to adjust the dose of the antidiabetic active substance during and after treatment with the neuroleptic agent.
Glucocorticoids (systemic and local route: intra-articular, cutaneous and rectal preparations) and tetracosactrin: increase in blood glucose levels with possible ketosis (reduced tolerance to carbohydrates due to glucocorticoids). Warn the patient and emphasize the importance of blood glucose monitoring, particularly at the start of treatment. It may be necessary to adjust the dose of the antidiabetic active substance during and after treatment with glucocorticoids.
Ritodrine, salbutamol, terbutaline: (I.V.) Increased blood glucose levels due to beta-2 agonist effects. Emphasize the importance of monitoring blood glucose levels. If necessary, switch to insulin.
Combination which must be taken into account: Anticoagulant therapy (Warfarin): Sulphonylureas may lead to potentiation of anticoagulation during concurrent treatment. Adjustment of the anticoagulant may be necessary.
Storage
Store at temperatures not exceeding 30°C.
Action
Pharmacology: Gliclazide (Dianorm) is a sulphonylurea hypoglycemic agent. Gliclazide (Dianorm) stimulates insulin secretion from functional pancreatic β-cells and increases the sensitivity of the β-cells to a glucose stimulus (some residual β-cell function is therefore necessary). Gliclazide (Dianorm) restores the diminished first-phase of insulin secretion noted in non-insulin dependent diabetes mellitus.
Any long-term hypoglycemic activity of Gliclazide (Dianorm) can be attributed to an ability to maintain its effect on insulin secretion. Extrapancreatic effects may also be involved in the long-term efficacy of Gliclazide (Dianorm).
Extrapancreatic effects demonstrated for Gliclazide (Dianorm) include improvement in insulin mediated glucose utilization and potentiation of postreceptor insulin sensitive pathways.
At normal therapeutic doses in man, Gliclazide (Dianorm) reduces platelet adhesiveness and aggregation.
Pharmacokinetics: Absorption: Gliclazide (Dianorm) is absorbed in the gastrointestinal tract reaching peak serum concentrations within 4 to 6 hours. Single dose studies have demonstrated that maximal falls in blood glucose levels (23% of an 80 mg dose; 30% of a 160 mg dose) occur approximately five hours after drug administration; nine hours after a dose of 160 mg, a reduction of 20% was still in evidence.
The half-life of Gliclazide (Dianorm) is approximately 12 hours.
Distribution: Gliclazide (Dianorm) is distributed to the extracellular fluid. In animals, high concentrations of the drug were found in the liver, kidneys, skin, lungs, skeletal muscle, intestinal and cardiac tissue. Penetration of Gliclazide (Dianorm) into the CNS was negligible. It crosses the placental barrier and penetrates the fetus.
The apparent volume of distribution of Gliclazide (Dianorm) (20 to 40% expressed as a percentage of body weight) is low and probably reflects the high degree of protein binding. At a plasma concentration of approximately 8 microgram/mL, 94.2% of the drug was protein bound and 5.8% was free.
Metabolism and excretion: There is little information available in relation to the metabolism of the drug. Employing thin layer chromatography and gas-liquid chromatography, at least 8 metabolites (3 major) have been identified. Some of these were glucuronic acid conjugates. Only one of the metabolites has been identified (p-toluene sulphonamide). The liver is the probable site of metabolism.
Approximately 70% of the administered dose appears to be excreted in the urine and 11% in the feces. The urinary excretion of the drug is slow and the maximum rates do not occur until 7 to 10 hours after initial administration. The metabolic products are detectable in the urine 120 hours after oral administration. Elimination through the feces is usually completed within 144 hours of oral administration.
Any long-term hypoglycemic activity of Gliclazide (Dianorm) can be attributed to an ability to maintain its effect on insulin secretion. Extrapancreatic effects may also be involved in the long-term efficacy of Gliclazide (Dianorm).
Extrapancreatic effects demonstrated for Gliclazide (Dianorm) include improvement in insulin mediated glucose utilization and potentiation of postreceptor insulin sensitive pathways.
At normal therapeutic doses in man, Gliclazide (Dianorm) reduces platelet adhesiveness and aggregation.
Pharmacokinetics: Absorption: Gliclazide (Dianorm) is absorbed in the gastrointestinal tract reaching peak serum concentrations within 4 to 6 hours. Single dose studies have demonstrated that maximal falls in blood glucose levels (23% of an 80 mg dose; 30% of a 160 mg dose) occur approximately five hours after drug administration; nine hours after a dose of 160 mg, a reduction of 20% was still in evidence.
The half-life of Gliclazide (Dianorm) is approximately 12 hours.
Distribution: Gliclazide (Dianorm) is distributed to the extracellular fluid. In animals, high concentrations of the drug were found in the liver, kidneys, skin, lungs, skeletal muscle, intestinal and cardiac tissue. Penetration of Gliclazide (Dianorm) into the CNS was negligible. It crosses the placental barrier and penetrates the fetus.
The apparent volume of distribution of Gliclazide (Dianorm) (20 to 40% expressed as a percentage of body weight) is low and probably reflects the high degree of protein binding. At a plasma concentration of approximately 8 microgram/mL, 94.2% of the drug was protein bound and 5.8% was free.
Metabolism and excretion: There is little information available in relation to the metabolism of the drug. Employing thin layer chromatography and gas-liquid chromatography, at least 8 metabolites (3 major) have been identified. Some of these were glucuronic acid conjugates. Only one of the metabolites has been identified (p-toluene sulphonamide). The liver is the probable site of metabolism.
Approximately 70% of the administered dose appears to be excreted in the urine and 11% in the feces. The urinary excretion of the drug is slow and the maximum rates do not occur until 7 to 10 hours after initial administration. The metabolic products are detectable in the urine 120 hours after oral administration. Elimination through the feces is usually completed within 144 hours of oral administration.
MedsGo Class
Antidiabetic Agents
Features
Brand
Dianorm
Full Details
Dosage Strength
80mg
Drug Ingredients
- Gliclazide
Drug Packaging
Tablet 1's
Generic Name
Gliclazide
Dosage Form
Tablet
Registration Number
DR-XY29814
Drug Classification
Prescription Drug (RX)