Comprehensive Overview on Antidiabetic Drugs

Antidiabetic Drugs

Antidiabetic Drugs: Classification, Mechanism, Uses, Adverse Effects & Interactions

Classification of Antidiabetic Drugs

I. Injectable (Not covered in this lesson):

• Insulin
• GLP-1 Agonists (e.g., Exenatide)

II. Oral Hypoglycemics:

1. Sulfonylureas – Glibenclamide, Glimepiride, Gliclazide
2. Biguanides – Metformin
3. Meglitinides – Repaglinide
4. Thiazolidinediones (TZDs) – Rosiglitazone
5. α-Glucosidase inhibitors – Acarbose
6. DPP-4 inhibitors – Sitagliptin, Linagliptin

Memory Tip:
“Some Boys Make The Alpha Sugar Down”
(Sulfonylureas, Biguanides, Meglitinides, TZDs, α-glucosidase inhibitors, DPP-4 inhibitors)

Drug Classes with Mechanism, Uses, Adverse Effect

I. Sulfonylureas (Glibenclamide, Glimepiride, Gliclazide)

Mechanism:
Stimulates insulin release by closing ATP-sensitive K⁺ channels in β-cells.

Uses:

• Type 2 DM (requires functioning pancreas)
• Combine with Metformin if needed

Adverse Effects:

• Hypoglycemia (most common)
• Weight gain
• GI upset, allergy (rare)

Interactions:

• Alcohol → disulfiram-like reaction
• Potentiated by NSAIDs, warfarin

Agent Sulfo says, “I squeeze insulin out of tired β-cells, but sometimes I squeeze too much!”

II. Biguanides – Metformin

Mechanism:

• ↓ Hepatic glucose production
• ↑ Insulin sensitivity
• ↓ Intestinal absorption of glucose

Uses:

• First-line in T2DM
• PCOS (off-label)

Adverse Effects:

• Lactic acidosis (rare but fatal)
• GI discomfort
• Vitamin B12 deficiency

Agent Bigua blocks sugar factories in the liver and opens muscle gates to glucose, but hates acid!

III. Meglitinides – Repaglinide

Mechanism:
Similar to sulfonylureas, but faster onset and shorter duration
→ Stimulates insulin release

Uses:

• Postprandial hyperglycemia
• Type 2 DM

Adverse Effects:

• Hypoglycemia
• Weight gain (less than sulfonylureas)

IV. Thiazolidinediones – Rosiglitazone

Mechanism:
PPAR-γ agonist → ↑ insulin sensitivity in muscle & fat

Uses:

• Type 2 DM (esp. with insulin resistance)

Adverse Effects:

• Fluid retention → CHF
• Weight gain
• ↑ Risk of fractures
• Rosiglitazone: ↑ risk of MI (use restricted)

Memory Tip:
“Rosi the Risky Rider of PPAR-gamma”

Agent Rosi whispers: “I fix sensitivity quietly... but sometimes flood the heart!”

V. α-Glucosidase Inhibitor – Acarbose

Mechanism:
Inhibits intestinal brush-border enzyme → slows carb digestion

Uses:

• Postprandial hyperglycemia
• Type 2 DM

Adverse Effects:

• Flatulence, bloating, diarrhea
• Not systemic, so minimal systemic AEs

Memory Tip:
“Acarbose = Anti-Carb Breakdown”

Agent Alpha: “I block sugar from breaking in, but I cause quite a gas storm!”

VI. DPP-4 Inhibitors – Sitagliptin, Linagliptin

Mechanism:
Inhibit DPP-4 enzyme → ↑ GLP-1 → ↑ insulin, ↓ glucagon

Uses:

• Type 2 DM
• Can be used with Metformin

Adverse Effects:

• Mild infections (nasopharyngitis)
• Headache
• Rare pancreatitis

Memory Tip:
“DPP-4 = Don’t Pinch the Peptide-4” → Keeps GLP-1 alive

Agent Dippi says: “I protect the good hormone GLP-1 from getting eaten!”

Quick Quiz for MCQS

1. Which drug causes lactic acidosis?
2. Who is the “Snack Attack” agent?
3. Who is contraindicated in CHF?
4. What protects GLP-1?

Mnemonic:
“SUGAR BAD”

• Sulfonylureas
• U (Metformin) – Used first
• Glinides
• Acarbose
• Rosi (TZDs)
• Beta incretin (DPP-4)
• Adverse effects
• Drug Interactions

References & Further Reading

1. Goodman & Gilman’s Pharmacological Basis of Therapeutics

2. Katzung’s Basic & Clinical Pharmacology

3. Clinical Practice Guidelines: ADA 2025

                                                         END OF THE DOCUMENT

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