Glycon MR

Gliclazide.

Each modified release tablet contains Gliclazide 60 mg.

Pharmacology: Pharmacodynamics: Gliclazide is a sulfonylurea antidiabetic agent. Gliclazide stimulates insulin release from the pancreatic beta cells. It reduces insulin uptake and glucose output by the liver. Insulin sensitivity is increased at peripheral target sites. Gliclazide reduces microthrombosis by decreasing platelet aggregation and adhesion, and by restoring fibrinolysis with an increase in tissue plasminogen activator (t-PA) activity.
Pharmacokinetics: Gliclazide completely absorbed from the gastrointestinal tract. The oral bioavailability of the drug is reported 97%. Peak plasma concentrations occur 6 hours. It is extensively 94 to 95% bound to plasma proteins and has duration of action of 24 hours. The volume of distribution is 20 to 40% of body weight. The half-life is about 16 hours (range 12-20 hours). Gliclazide is extensively metabolized in the liver to metabolites that have no significant hypoglycemic activity. Metabolites and a small amount of unchanged drug are excreted in the urine. Less than 1% unchanged Gliclazide is found in the urine.

Gliclazide is indicated for non insulin-dependent diabetes (type 2) in adults when dietary measures, physical exercise and weight loss alone are not sufficient to control blood glucose.

Recommended Dose: Adults: Initial Dose: The recommended starting dose is 30 mg/day.
Titration: Dosage adjustments should ordinarily be in increments of 30 mg, as determined by blood glucose response. The interval between dose increases of modified-release preparation should be at least 1 month, but the dose may be increased after just 2 weeks in those patients who have not responded.
Maximum Dose: 120 mg once daily.
Children: There are no data and clinical studies available in children.
Geriatric: Refer to adult dosing; use with caution.
Renal impairment: Mild to moderate renal impairment: The same dosing regimen can be used as in patients with normal renal function with careful patient monitoring.
Severe renal impairment: Use is contraindicated.
Mode of Administration: Gliclazide is administered orally. Modified-release tablets of the drug should be administrated with breakfast. Modified release tablets should not be crushed or chewed.
If a dose is forgotten, there must be no increase in the dose taken the next day.
The tablet can be divided into equal doses.

Overdose and Treatment: An overdose of sulfonylurea 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 a 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 a 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 closely monitored 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.

Gliclazide is contraindicated in patients with: Known hypersensitivity to Gliclazide or any component of the excipients, other sulfonylurea or sulfonamides; Type 1 diabetes mellitus; Diabetic ketoacidosis (with or without coma); Severe renal or hepatic insufficiency; Treatment with miconazole; Lactation.

(Based on the Ministry of Public Health's Announcement): 1. Gliclazide is contraindicated in patients with known hypersensitivity to this drug.
2. Gliclazide is contraindicated in Type I diabetes mellitus patients, diabetic ketoacidosis patients, severe infection patients, severe accident patients.
3. Avoid using this drug in pregnant women. And use this drug with caution in breast-feeding women.
4. The intake of alcoholic beverages should be avoided during treatment with Gliclazide tablets.
5. Use the drug with caution because hypoglycemic symptoms can occur such as hunger, palpitation, sweating.
6. If the following symptoms occur during using this drug e.g. skin rash, blisters, detachment of skin and epithelial lining in oral cavity, throat, nose, genital organ and conjunctivitis, stop using this drug and consult the doctor immediately as this may be Stevens-Johnson syndrome.
7. Use the drug with caution in patients with renal impairment.

Hypoglycemia: All sulfonylurea drugs are capable of producing severe hypoglycemia. Hypoglycemia is more likely to occur when caloric intake is deficient, after severe or prolonged exercise, when ethanol is ingested, or when more than one glucose-lowering drug is used. Hypoglycemia is also more likely in elderly or debilitated patients, malnourished patients and in patients with impaired renal or hepatic function, adrenal and/or pituitary insufficiency.
Hemolytic anemia: Sulfonylureas can cause hemolytic anemia in patients with glucose 6-phosphate dehydrogenase (G6PD) deficiency. Use with caution in patients with G6PD deficiency and consider use of nonsulfonylurea alternative.
Renal/Hepatic function impairment: Use with caution in hepatic or renal impairment as metabolism and/or excretion may be impaired. Dose reduction may be necessary.
Special Warnings and Precautions: This drug may elevate liver enzymes. Should be careful in patients who received this drug.

Pregnancy: The use of sulfonylurea in pregnancy should generally be avoided because of the risk of neonatal hypoglycemia. 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.
Lactation: It is not known whether Gliclazide or its metabolites is excreted into breast milk.
The potential for neonatal hypoglycemia in a nursing infant contraindicates use.

Hypoglycemia: Gliclazide appear to be less often associated with severe hypoglycemia, may be increased by missed or irregular meals, hepatic or renal impairment and drug interaction.
Other undesirable effects: Cardiovascular: Angina pectoris, hypertension, peripheral edema.
Central nervous system: Depression, dizziness, headache, insomnia, neuralgia.
Dermatologic: Dermatitis, dermatological disease, pruritus, rash (includes maculopapular rash, morbiliform rash).
Endocrine & metabolic: Hyperglycemia, hyperlipidemia, hypoglycemia, increased lactate dehydrogenase, lipid metabolism disorder.
Gastrointestinal: Abdominal pain, constipation, diarrhea, gastritis, gastroenteritis, nausea.
Genitourinary: Urinary tract infection.
Infection: Viral infection.
Neuromuscular & skeletal: Arthalgia, arthritis, arthropathy, back pain, myalgia, tendonitis, weakness.
Ophthalmic: Conjunctivitis.
Otic: Otitis media.
Renal: Increases serum creatinine.
Respiratory: Bronchitis, cough, pharyngitis, pneumonia, rhinitis, sinusitis, upper respiratory tract infection.
Rare but important or life-threatening: Abnormal lacrimation, acute pancreatitis, agranulocytosis, albuminuria, anal fissure, anemia, angioedema, anxiety, arteritis, asthma, auditory impairment, balanitis, bone disease (spine malformation), breast neoplasm (female; benign), bullous rash, bursitis, cardiac failure, carpal tunnel syndrome, cataract, cerebrovascular disease, chest pain, cholestatic jaundice, colitis, confusion, conjunctival hemorrhage, coronary artery disease, cystitis, dermal ulcer, diplopia, disulfiram-like reaction, DRESS syndrome, duodenal ulcer, dyspepsia, dyspnea, eczema, epigastric fullness, epistaxis, erythema, erythrocytopenia, esophagitis, fecal incontinence, fever, flatulence, fungal dermatitis, fungal infection, gastroesophageal reflux disease, gastrointestinal neoplasm (benign), glaucoma, glycosuria, gout, hemolytic anemia, hemorrhoids, hepatitis, hepatomegaly, hernia (congenital), hypercholesterolemia, hyperkeratosis, hypersensitivity reaction, hypertriglyceridemia, hypoglycemia, coma, hyponatremia, hypotension, hypothyroidism, impotence, increased appetite, increase serum alkaline phosphatase, increased serum ALT, increased serum AST, increased serum transaminase, increased thirst, infection, leg pain, leucopenia, malaise, mastitis, melena, menstrual disease, myocardial infarction, nail disease, nephrolithiasis, nervousness, neuropathy, nocturia, onychomycosis, pain, palpitations, pancytopenia, polyuria, prostatic disease, renal cyst, retinopathy, sialorrhea, skeletal pain, Stevens-Johnson syndrome, sleep disorders, tachycardia, thrombocytopenia, thrombophlebitis, tinnitus, toothache, toxic epidermal necrolysis, tracheitis, urticaria, vaginitis, vascular disease (vein disorder), visual disturbance, vitreous disorder, vomiting, weight gain, xeroderma, xerophthalmia, xerostomia.

Alcohol (Ethanol): Major potential reactions associated with ethanol use and sulfonylurea include prolonged hypoglycemia and disulfiram-like reactions.
Aminolevulinic Acid: Concurrent use of Gliclazide and aminolevulinic acid may increase the risk of phototoxic skin reaction.
Avoid concomitant use.
Antibacterials: Chloramphenicol markedly inhibits the metabolism of sulfonylureas which can result in hypoglycaemia. Sulfonamides may also enhance the hypoglycaemic effects of the sulfonylureas. There have been rare reports of hypoglycemia when fluoroquinolones (i.e. ciprofloxacin, levofloxacin, gatifloxacin) were used with sulfonylurea.
Antifungals: Concurrent use of Gliclazide and azole antifungals (i.e. fluconazole, miconazole, ketoconazole, voriconazole) may increase the effects of Gliclazide. Hypoglycemia has been reported.
Cimetidine: Concurrent use of Gliclazide and cimetidine may increase the effects of Gliclazide. Increased hypoglycemic effect may occur.
Rifampin: Concurrent use of Gliclazide and rifampin has been shown to reduce the glucose-lowering effects of Gliclazide. Increased dose of Gliclazide may be necessary.

Store below 30°C.

Antidiabetic Agents

A10BB09 - gliclazide ; Belongs to the class of sulfonylureas. Used in the treatment of diabetes.

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