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Insulin Aspart (NovoLog® Injection)

Insulin aspart, marketed as NovoLog® (NovoRapid® in some regions), is a rapid-acting human insulin analog used to manage hyperglycemia in type 1 and type 2 diabetes mellitus. Engineered for rapid onset and short duration, it mimics physiological insulin secretion to control postprandial glucose spikes. This article synthesizes evidence from the British National Formulary (BNF)Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology to detail its pharmacology, clinical use, and safety profile.

Insulin aspart is structurally modified (proline replaced with aspartic acid at position B28) to accelerate absorption and action. It binds to insulin receptors, initiating:

  • Glucose Uptake: Promotes cellular glucose absorption via GLUT4 transporters in muscle and adipose tissue.
  • Hepatic Glucose Suppression: Inhibits glycogenolysis and gluconeogenesis.
  • Peripheral Utilization: Enhances glycogen synthesis and protein/lipid metabolism.
  • Onset: 10–20 minutes (subcutaneous).
  • Peak: 1–3 hours.
  • Duration: 3–5 hours (Lippincott).
  • Intravenous Use: Reserved for emergencies (e.g., diabetic ketoacidosis [DKA]) under clinical supervision (BNF).
  1. Type 1 Diabetes:
    • Mealtime insulin in basal-bolus regimens, paired with long-acting insulin.
    • Continuous subcutaneous insulin infusion (CSII) via insulin pumps.
  2. Type 2 Diabetes:
    • Adjunctive therapy when oral agents or non-insulin injectables fail.
  3. Gestational Diabetes:
    • Safe under specialist guidance if diet/exercise insufficient.
  4. Hyperglycemic Emergencies:
    • Transition to subcutaneous insulin aspart after IV insulin stabilizes DKA (BNF).
  • Administration:
    • Subcutaneous: Inject into abdomen, thigh, or upper arm 5–15 minutes before meals.
    • IV: Diluted in infusion systems for critical care (0.05–0.1 units/kg/h).
  • Initial Dosing:
    • Adults: 0.2–0.4 units/kg/day, divided into pre-meal doses.
    • Children: 0.5–1.0 units/kg/day, adjusted by carbohydrate intake and activity (BNF).
  • Titration: Adjust based on pre- and postprandial glucose monitoring.
  • Special Populations:
    • Renal/Hepatic Impairment: Monitor closely; hypoglycemia risk increases with reduced insulin clearance.

Elderly: Conservative dosing to avoid hypoglycemia

  • Hypoglycemia (palpitations, sweating, confusion).
  • Injection-site reactions (redness, lipodystrophy with chronic use).
  • Weight gain (anabolic effects).

Serious:

  • Severe Hypoglycemia: Risk with missed meals, exercise, or overdose.
  • Hypokalemia: Insulin shifts potassium intracellularly; monitor in critical care.
  • Allergic Reactions: Rare urticaria or anaphylaxis (Lange).
  • Contraindications: Hypoglycemia, hypersensitivity to insulin aspart.
    • Blood glucose (pre-/postprandial and bedtime).
    • HbA1c (every 3–6 months), renal/hepatic function.
    • Injection sites for lipodystrophy.
    • Unopened vials/pens: Refrigerate (2–8°C).

In-use: Store at room temperature (<30°C) for up to 28 days

    • Pregnancy: Category B; dose adjustments may be needed.
    • Lactation: Safe; insulin does not enter breast milk (BNF).
  • Beta-Blockers: Mask hypoglycemia symptoms (e.g., tachycardia).
  • Corticosteroids/Thiazides: Increase insulin resistance, requiring dose escalation.
  • Alcohol: Potentiates hypoglycemia; avoid concurrent use.
  • SGLT2 Inhibitors/GLP-1 Agonists: Additive hypoglycemia risk; monitor closely (Lippincott).
  • Generic: Insulin aspart.
  • Brand Names: NovoLog® (US), NovoRapid® (EU/UK).

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