A second-generation sulfonylurea known as gliclazide (Diamicron) decreases blood sugar by encouraging the release of insulin from the pancreatic beta-cells and improving the sensitivity of peripheral tissue to insulin. It also has anti-oxidant properties.

Gliclazide Uses:

• Diabetes mellitus, type 2:

  • It is used in the management of noninsulin-dependent diabetes mellitus.

Gliclazide (Diamicron) Dose in Adults

Gliclazide (Diamicron) Dose in the treatment of type 2 Diabetes mellitus: Oral:

Gliclazide does not have a set dosing regimen for the treatment of diabetes mellitus. During dose titration and maintenance, the dose must be customised  based on regular blood glucose monitoring. It is interesting to notice that an 80 mg immediate-release tablet is equivalent to a 30 mg modified-release tablet.

• Immediate-release tablet:

  • It can first be administered as 80 mg twice daily. Adapt the dose based on your blood sugar levels

  • The typical dosage range is 80 to 320 mg/day with a 320 mg/day maximum.

  • For use twice day, a dose of more than 160 mg should be split into 2 equal halves.

• Modified-release tablet:

  • Start with 30 mg once day with breakfast and increase by 30 mg every two weeks depending on blood sugar levels.
  • One 120 mg dose per day is the maximum permitted.

Gliclazide (Diamicron) Conversion from insulin:

• Patients receiving less than 40 units of insulin per day may want to consider switching from insulin to gliclazide medication.
• Withdraw insulin for 48 to 72 hours prior to conversion, and closely monitor urine glucose and ketone levels (about three times per day).
• Patients should not be switched to gliclazide therapy and should instead stay on insulin therapy if they have ketones and glucose in their urine 12 to 24 hours after stopping their insulin therapy.

Use in Children:

Not indicated.

Gliclazide (Diamicron) Pregnancy Category: C

• It is not advised to be used while pregnant.
• The foetus could suffer from the negative effects of maternal hyperglycemia.
• These include hyperbilirubinemia, macrosomia, and neonatal hypoglycemia.
• If the HbA1c values are higher than the range considered to be normal, congenital abnormalities are more frequent.
• Mothers with diabetes can experience adverse effects.
• Poor glycemic control during pregnancy can cause end-organ damage, and poor outcomes.
• To reduce the chance of adverse events for the mother and baby, it is important to maintain physiological glucose levels during and before pregnancy.
• Insulin is the preferred drug to control sugars during pregnancy.

Use of Gliclazide while breastfeeding

• Gliclazide cannot be found in milk.
• Breastfeeding mothers should not use it as it can cause hypoglycemia.

Gliclazide (Diamicron) Dose in Kidney disease:

• Mild to moderate impairment

  • The literature does not recommend any dose adjustments, but renal impairment may require dose reductions.

• Severe impairment

  • It is not recommended for severe renal dysfunction.

Gliclazide (Diamicron) Dose in Liver disease:

• Mild to moderate impairment

  • A dose decrease can be required in cases of mild to moderate liver damage.

• Severe impairment

  • It is not recommended for severe impairment.

Common Side Effects of Gliclazide (Diamicron):

• Endocrine & metabolic:

  • Hypoglycemia

Less Common Side Effects of Gliclazide (Diamicron):

• Cardiovascular:

  • Hypertension
  • Angina Pectoris
  • Peripheral Edema

• Central Nervous System:

  • Headache
  • Dizziness
  • Depression
  • Insomnia
  • Neuralgia

• Dermatologic:

  • Dermatological Disease
  • Dermatitis
  • Skin Rash
  • Pruritus

• Endocrine & Metabolic:

  • Hyperglycemia
  • Hyperlipidemia
  • Lipid Metabolism Disorder
  • Increased lactate dehydrogenase

• Gastrointestinal:

  • Diarrhea
  • Constipation
  • Gastroenteritis
  • Abdominal Pain
  • Gastritis
  • Nausea

• Genitourinary:

  • Urinary Tract Infection

• Infection:

  • Viral Infection

• Neuromuscular & Skeletal:

  • Back Pain
  • Arthralgia
  • Weakness
  • Arthropathy
  • Myalgia
  • Arthritis
  • Tendonitis

• Ophthalmic:

  • Conjunctivitis

• Otic:

  • Otitis Media

• Respiratory:

  • Bronchitis
  • Rhinitis
  • Pharyngitis
  • Upper Respiratory Tract Infection
  • Cough
  • Pneumonia
  • Sinusitis

• Renal:

  • Increased serum creatinine

Contraindications to Gliclazide (Diamicron):

• Hypersensitivity to gliclazide or other sulfonylureas and sulfonamides is a contraindication.
• Unstable type 1 diabetes mellitus (IDDM; insulin-dependent IDDM), particularly in children.
• Diabetic ketoacidosis.
• Diabetic precoma and coma.
• Grave renal or liver impairment.
• Serious infections, trauma, and surgery are examples of stress-related conditions.
• Use oral gel and systemic miconazole together.
• Breast-feeding and pregnancy
• Although this medication is listed as contraindicated with certain sulfonamide-containing drugs, various studies have not confirmed that.

Warnings and precautions

• Cardiovascular mortality

  • Oral hypoglycemic drugs may be linked to increased cardiovascular mortality than treatment with diet and insulin, according to the US product labelling for sulfonylureas.
  • This statement is supported by scanty data.
  • Other agents are recommended for patients suffering from atherosclerotic heart disease (ASCVD)

• Hypersensitivity

  • There have been reports of severe erythematous and maculopapular red rashes, pruritus and angioedema, bullous reactions  (including Stevens Johnson syndrome and toxic epidermal necrolysis), and drug reactions with eosinophilia (DRESS).

• Hypoglycemia

  • Sulfonylureas can all produce severe low sugars. Hypoglycemia is much less common in gliclazide than with other sulfonylureas, such as glimepiride or glyburide.
  • Hypoglycemia can be exacerbated by poor oral intake, stress conditions or large amounts of ethanol.
  • Patients who are malnourished and elderly are more likely to experience it.
  • Hypoglycemic symptoms such as weakness and dizziness, can lead to impairment of mental or physical abilities. 
  • When engaging in activities requiring mental acuity, such as operating machinery or operating a vehicle, it is crucial to exercise  caution.

• Allergy to sulfonamide ("sulfa")

  • Wide ranging contraindications for patients who have previously experienced an adverse reaction to  sulfonamides are listed on FDA-approved product labels for drugs that contain sulfonamide chemical groups.
  • There is a chance that certain sulfa-containing medications will interact with one another.
  • Concerns about cross-reactivity have been expressed for all substances having the sulfonamide sulfonamide structure.
  • However, current research on allergic pathways raises doubts about the likelihood of cross-reactivity between antibiotic and non-antibiotic sulfonamides.
  • Anaphylactic responses do not occur frequently.
  • Less research has been done on type IV hypersensitivity reactions, such as maculopapular skin rash. Given what is known at the  moment, it is challenging to entirely rule out this option.
  • If there is a history of severe SJS/TEN, the doctors would typically avoid prescribing this medication.

• Deficiency of Glucose-6phosphate dehydrogenase(G6PD)

  • Patients with G6PD deficits may be more susceptible to hemolytic anaemia brought on by sulfonylureas.

  • Patients without a G6PD deficiency have also had cases, according to post-marketing surveillance.

  • Patients with G6PD deficiency should exercise caution

• Hepatic impairment

  • Dosage adjustments are necessary because it is subject to hepatic metabolism.
  • Rarely have we seen cholestasis, jaundice, or hepatitis. If cholestatic jaundice is present, you should withhold the drug.
  • It is not recommended to use in cases of severe impairment.

• Renal impairment

  • In renal disease, adjust the dose. It is important to exercise caution.
  • It is not recommended to use in cases of severe impairment.

• Stress-related disorders:

  • It should not be used during an acute illness or other stress-related conditions.
  • If the patient is under stress, it may be necessary for them to stop taking insulin and to restart therapy.

Gliclazide: Drug Interaction

Monitoring parameters:

• You should be aware of warning signs and symptoms include extreme appetite, perspiration, and exhaustion.
• Blood sugar and HbA1c should be measured at least twice a year in patients who have achieved glycemic control stability and treatment goals.
• Reporting blood glucose and HbA1c on a quarterly basis is advised for patients who are not achieving their treatment objectives or who have undergone therapeutic adjustments.
• Tests of renal function.

[/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="How to administer?" collapse_text="How to administer?" ]

How to administer Gliclazide (Diamicron)?

• Oral:
  • Lower doses may be required for patients who are NPOs or who consume less calories in order to prevent hypoglycemia.
  • Take with food (modified release tablet should be taken with breakfast).
  • Modified-release 60 mg pills can be broken in half. 
  • Modified-release 30 mg pills, however, must be taken whole.
  • Modified-release tablets must not be eaten or torn into pieces.

Mechanism of action of Gliclazide (Diamicron):

• Insulin sensitivity increases at peripheral target sites.
• Microthrombosis is reduced by decreasing platelet adhesion and platelet aggregation, and by increasing tissue plasminogen activator activity (t-PA).
• The antioxidant effects include a drop in plasma levels peroxidized cholesterol and an increase in erythrocyte superoxide dimutase activity.

Time of action:

• Modified-release tablet 24 hours

Absorption:

• Formulation for immediate release: Rapid
• Modified-release formulations: Slow and complete

Bioavailability:

• Modified release: 97%

Protein binding:

• 94% to 935%

Metabolism:

• Hepatic (via CYP2C9 or CYP2C19). To inactive metabolites

Eliminating half-life

• Tablets with immediate release: 10.4 hours
• Modified-release tablet 16 hours (range 12 to 20 hours).

Time to reach the peak

• Tablets with immediate release: 4 to 6 hours
• Modified-release tablet: 6 Hours

Excretion:

• Urine (60% - 70%). 1% for an unchanged drug
• Feces (10%-20%) as metabolites

International Brand Names of Gliclazide:

• APO-Gliclazide
• APO-Gliclazide MR
• Diamicron
• Diamicron MR
• Gliclazide-80
• GPC-Gliclazide MR
• MINT-Gliclazide MR
• MYLAN-Gliclazide MR
• MYLAN-Gliclazide
• PMS-Gliclazide
• RAN-Gliclazide MR
• SANDOZ Gliclazide MR
• TEVA-Gliclazide
• Azide
• Azukon
• Azukon MR
• Cadicon
• Claz
• Clazic SR
• Clizid
• Diabend
• Diabeside
• Diabeton
• Diabrezide
• Diaclide
• Diacronal
• Diagle
• Diamexon
• Diamicron
• Diamicron MR
• Diamicron Uno
• Diamid
• Dianid
• Dianorm
• Diaprel
• Diaprel MR
• Diglucron
• Dimetus
• Dorocron-MR
• Getzid-MR
• Glaze
• Glecloz
• Glicabit
• Glicada SR
• Glicalin
• Gliclada
• Glicron
• Glikamel
• Glimicron
• Glitab
• Glitrol
• Gliz
• Glizide
• Glubitor-OD
• Gluctam
• Glyade
• Glyade MR
• Glycinorm-80
• Glycon
• Glycon MR
• Glyzide
• Laaglyda MR
• Lazibet MR60
• Lozide
• Meltika
• Mezide
• Microzide
• Nidem
• Normodiab
• Oziclide MR
• Ranclazide MR
• Reclide
• Staclazide 30 MR
• Suclear
• Sugred
• Sunglizide
• Syncon
• Unava
• Uni Diamicron
• Vamju
• Xepabet
• Zebet
• Ziclin
• Zycron

Gliclazide Brand Names in Pakistan: