Gliclazide
JFDA label: Debaday tab
Mechanism of Action
Blocker of Sulfonylurea receptor 1, Kir6.2 — Sulfonylurea receptor 1, Kir6.2 blocker
| Target | Action | Gene / class |
|---|---|---|
| Sulfonylurea receptor 1, Kir6.2 efficacy | BLOCKER |
Indications
Approved
- Diabetes Mellitus — diabetes mellitus
Off-label
- Diabetes Mellitus, Type 2
Class profile
| mechanismClass | Sulfonylurea (2nd generation, modified release) |
|---|---|
| insulinSecretagogue | 1 |
| weightEffect | Neutral/slight gain |
| hypoglycemiaRisk | Moderate |
| renalContraindicated | 0 |
| cardioProtective | 0 |
| renalProtective | 0 |
| source | ADA-EASD2023/Maruthur2016 |
Contraindications
Source: Curated
- Type 1 diabetes mellitus or diabetic ketoacidosis Absolute
Adverse Reactions
Cardiac disorders (1)
Common Angina pectoris
Vascular disorders (1)
Common Hypertension
Nervous system disorders (3)
Common Dizziness · Headache · Neuralgia
Metabolism and nutrition disorders (1)
Common Hyperglycaemia
Gastrointestinal disorders (6)
Common Abdominal pain · Constipation · Diarrhoea · Gastroenteritis · Gastrointestinal pain · Nausea
Skin and subcutaneous tissue disorders (4)
Common Dermatitis · Pruritus · Rash · Skin disorder
Musculoskeletal and connective tissue disorders (7)
Common Arthralgia · Arthritis · Back pain · Musculoskeletal discomfort · Myalgia · Osteoarthritis · Tendonitis
Psychiatric disorders (2)
Common Depression · Insomnia
Eye disorders (1)
Common Conjunctivitis
Infections and infestations (8)
Common Bronchitis · Pharyngitis · Pneumonia · Rhinitis · Sinusitis · Upper respiratory tract infection · Urinary tract infection · Viral infection
General disorders and administration site conditions (7)
Common Arthropathy · Asthenia · Gastritis · Hyperlipidaemia · Lipid metabolism disorder · Oedema peripheral · Otitis media
Respiratory, thoracic and mediastinal disorders (1)
Common Cough
Injury, poisoning and procedural complications (1)
Common Injury
Pregnancy & Lactation
Pregnancy
Monitoring
| Efficacy | HbA1c every 3 months initially, then every 6–12 months when stable; fasting and post-prandial blood glucose; patient-reported hypoglycaemia episodes |
|---|---|
| Toxicity | Hypoglycaemia symptoms; eGFR for renally-cleared agents; weight; blood pressure |
| Clinical pearl | Individualise HbA1c targets based on patient age, comorbidities, and hypoglycaemia risk. Targets of < 7% are appropriate for most patients but < 8% may be safer in frail elderly. |
| Counseling | Monitor blood glucose regularly. Know how to recognise and treat hypoglycaemia. Keep carbohydrate snacks available. |
Chemistry & Properties
| Formula | C15H21N3O3S |
|---|---|
| Molecular weight | 323.42 g/mol |
| IUPAC name | 1-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)-3-(4-methylphenyl)sulfonylurea |
| CAS | 21187-98-4 |
| PubChem CID | 3475 |
| InChIKey | BOVGTQGAOIONJV-UHFFFAOYSA-N |
| logP | 1.63 (XLogP 1.5) |
| Polar surface area | 78.51 Ų |
| H-bond acceptors / donors | 4 / 2 |
| Drug-likeness (QED) | 0.89 |
| Lipinski violations | 0 |
SMILES
Cc1ccc(S(=O)(=O)NC(=O)NN2CC3CCCC3C2)cc1Biology & Pharmacokinetics
Pharmacokinetics
| BBB penetrant | No |
|---|
Enzyme interactions
| Enzyme | Role | Detail |
|---|---|---|
| CYP2C19 | Substrate | — |
| CYP2C9 | Substrate | — |
Transporters
BCRP (Inhibitor)BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)
Registered Products (10)
| Brand | Form / strength | Pack | Agent | Citizen (JOD) |
|---|---|---|---|---|
| Glicron 60mg Modified Release Tablet Tablet | Tablet 60 mg | 30 tab | Al-motakadema pharmaceutical Ltd/Jordan | 2.020 |
| Diamid Tablets | Tablet 80 mg | 20 tab pack varies | MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN | 2.690 |
| Microzide Tab | Tablet 80 mg | 20 tab pack varies | Hayat Pharmaceutical Industries CO.PLC/JORDAN | 2.690 |
| Diamicron MR | Tablet 60 mg | 30 tab | The Jordan Drugstore Co | 3.070 |
| Debaday tab | Tablet 80 mg | 30 tab pack varies | Pharma International Company/ Jordan | 3.300 |
| Debaday MR | Tablet 30 mg | 30 tab pack varies | Pharma International Company/ Jordan | 3.720 |
| Debaday tab | Tablet 80 mg | 500 tab pack varies | Pharma International Company/ Jordan | 47.000 |
| Debaday MR | Tablet 30 mg | 500 tab pack varies | Pharma International Company/ Jordan | 53.940 |
| Microzide | Tablet 80 mg | 500 tab pack varies | Hayat Pharmaceutical Industries CO.PLC/JORDAN | 57.160 |
| Diamid Tablets | Tablet 80 mg | 1000 tab pack varies | MIDDLE EAST PHARMA&CHEMICAL IND/JORDAN | 114.330 |