Diabetol (Tolbutamide)
Diabetol is a brand name for tolbutamide, a first-generation sulfonylurea oral hypoglycemic medication for T2D.
Mechanism of Action
Tolbutamide blocks ATP-sensitive potassium channels (K_ATP) on pancreatic beta-cell plasma membranes. This blockade causes depolarization, opening voltage-gated calcium channels. The resulting calcium influx triggers insulin granule exocytosis, increasing circulating insulin levels and lowering blood glucose.
Clinical Use
- Indication: Adjunct to diet and exercise in adults with type 2 diabetes when glycemic control is insufficient by lifestyle alone.
- Not for: Type 1 diabetes, diabetic ketoacidosis.
- Route: Oral (tablets).
- Standard dosing: 500–2000 mg/day (typical tablets are 500 mg); maximum 3000 mg/day.
- Duration: Short-acting (half-life 4.5–6.5 hours), preferred in elderly due to rapid clearance.
Properties
| Property | Detail |
|---|---|
| Class | First-generation sulfonylurea |
| Brand names | Diabetol, Orinase, Tol-Tab |
| ATC code | A10BB03 |
| Metabolism | Hepatic (CYP2C19-mediated) |
| Excretion | Renal |
| Protein binding | 96% |
Side Effects
- Hypoglycemia
- Weight gain
- Hypersensitivity (cross-allergenicity with sulfonamides)
- Drug interactions: enhanced hypoglycemia with salicylates, cimetidine, insulin
Note on 60mg Dose
The standard available formulation is 500 mg tablets. The “60 mg” noted in some patient medication lists does not match any standard tolbutamide dosage form. Possible explanations include: misrecorded dosage, a different drug sharing the name, or a reference to 60 tablets rather than milligrams. This discrepancy should be verified against original pharmacy records.
Status
Tolbutamide (Orinase) was discontinued by the manufacturer in 2000. It has been largely replaced by newer, second-generation sulfonylureas (glibenclamide/glyburide, gliclazide, glimepiride) with improved safety profiles. It is now rarely used in contemporary clinical practice.
References
- Wikipedia: Tolbutamide (https://en.wikipedia.org/wiki/Tolbutamide) — redirected from “Diabetol”
- Drugs.com Tolbutamide monograph (https://www.drugs.com/mtm/tolbutamide.html)