Insulin analogue

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Insulin analogs are modified forms of human insulin designed to improve pharmacokinetics and pharmacodynamics, providing better glycemic control for people with diabetes mellitus. These synthetic insulins have altered amino acid sequences, affecting their absorption, distribution, metabolism, and elimination (ADME) properties.

Types of Insulin Analogs[edit | edit source]

Insulin analogs are classified into rapid-acting, long-acting, and ultra-long-acting formulations based on their onset and duration of action.

Rapid-acting Insulin Analogs[edit | edit source]

Used to control postprandial blood glucose spikes.

Rapid-Acting Insulin Analogs
Name Brand Names Onset of Action Peak Effect Duration
Insulin lispro Humalog, Admelog ~15 min 1–2 hours 3–5 hours
Insulin aspart NovoLog, Fiasp ~10–20 min 1–3 hours 3–5 hours
Insulin glulisine Apidra ~15 min 1–2 hours 3–5 hours

Long-acting and Ultra-long-acting Insulin Analogs[edit | edit source]

Used to maintain basal insulin levels throughout the day.

Long-Acting and Ultra-Long-Acting Insulin Analogs
Name Brand Names Onset of Action Peak Effect Duration
Insulin glargine Lantus, Toujeo, Basaglar ~1–2 hours No significant peak 18–24 hours
Insulin detemir Levemir ~1–2 hours Minimal peak 12–24 hours
Insulin degludec Tresiba ~1 hour No significant peak >42 hours

Mechanism of Action[edit | edit source]

Insulin analogs work by: 1. Binding to the insulin receptor (IR) on target cells (liver, muscle, adipose). 2. Stimulating glucose uptake via GLUT4 transporters. 3. Inhibiting hepatic glucose production and promoting glycogen synthesis. 4. Suppressing lipolysis and proteolysis.

The modifications in insulin analogs affect their absorption rate and receptor affinity, providing a more physiological insulin profile.

Advantages of Insulin Analogs[edit | edit source]

Compared to human insulin, insulin analogs offer:

  • Faster onset (e.g., rapid-acting analogs for meal coverage).
  • Prolonged basal action (e.g., ultra-long-acting insulin reduces nocturnal hypoglycemia).
  • Lower risk of hypoglycemia (especially long-acting formulations).
  • More predictable absorption with less variability.

Clinical Indications[edit | edit source]

Insulin analogs are used for:

  • Type 1 diabetes mellitus (T1DM) – Requires both basal and bolus insulin.
  • Type 2 diabetes mellitus (T2DM) – Used when oral hypoglycemic agents fail.
  • Gestational diabetes mellitus (GDM) – Preferred over human insulin for better glycemic control.
  • Diabetic ketoacidosis (DKA)IV insulin analogs used in critical care settings.

Comparison with Human Insulin[edit | edit source]

Comparison of Insulin Analogs vs. Human Insulin
Feature Human Insulin Insulin Analogs
Onset of action Slower (30–60 min) Faster (10–15 min for rapid-acting)
Duration Shorter or longer (varies) More predictable
Risk of hypoglycemia Higher Lower (especially nocturnal hypoglycemia)
Absorption variability Higher Lower

Potential Side Effects[edit | edit source]

Common side effects include:

  • Hypoglycemia (risk varies by type of insulin).
  • Weight gain (due to anabolic effects of insulin).
  • Injection site reactions (e.g., lipodystrophy).
  • Allergic reactions (rare but possible).
  • Hypokalemia (can lead to cardiac arrhythmias).

Special Considerations[edit | edit source]

  • Renal impairment – Adjust dosing for patients with chronic kidney disease (CKD).
  • Liver dysfunction – Insulin metabolism is reduced in hepatic impairment.
  • Pregnancy and lactation – Some analogs (e.g., insulin detemir) are FDA-approved for pregnancy.

Future Developments[edit | edit source]

Research is ongoing for:

  • Oral insulin formulations (to improve compliance).
  • Smart insulin pumps (automated insulin delivery systems).
  • Ultra-rapid insulins (faster onset for meal-time control).

See Also[edit | edit source]

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Contributors: Prab R. Tumpati, MD, Dr.T