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Drugs, Supplies and Delivery
Insulin Glulisine (Apidra® Injection)
Insulin glulisine, marketed as Apidra®, is a rapid-acting human insulin analog used to manage hyperglycemia in type 1 and type 2 diabetes mellitus. Designed for mealtime glucose control, it offers a faster onset and shorter duration compared to regular human insulin. This article synthesizes evidence from the British National Formulary (BNF), Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology to outline its pharmacology, clinical applications, and safety profile.
Insulin glulisine mimics endogenous insulin by binding to insulin receptors on target cells (muscle, fat, liver). Key actions include:
- Glucose Uptake: Promotes cellular glucose absorption via GLUT4 transporters.
- Glycogen Synthesis: Enhances glycogen storage in the liver and muscle.
- Lipogenesis/Protein Synthesis: Stimulates fat and protein synthesis while inhibiting lipolysis and proteolysis.
- Hepatic Glucose Suppression: Reduces hepatic glucose output by inhibiting gluconeogenesis and glycogenolysis (Lippincott).
As a rapid-acting analog, insulin glulisine has a faster onset (10–15 minutes) and shorter duration (3–5 hours) than regular insulin due to amino acid substitutions (asparagine at B3 replaced by lysine, lysine at B29 replaced by glutamic acid) (Lange).
- Type 1 Diabetes: Administered subcutaneously before meals to control postprandial hyperglycemia, often paired with basal insulin.
- Type 2 Diabetes: Adjunctive therapy when oral agents or other injectables fail to achieve glycemic targets.
- Continuous Subcutaneous Insulin Infusion (CSII): Compatible with insulin pumps for flexible dosing (BNF).
- Hyperglycemic Emergencies: Off-label intravenous use in diabetic ketoacidosis (DKA) under clinical supervision.
- Administration:
- Subcutaneous: Injected into abdomen, thigh, or upper arm 0–15 minutes before meals.
- Intravenous: Reserved for emergencies (e.g., DKA) in hospital settings.
- Initial Dosing:
- Type 1 Diabetes: 0.2–0.4 units/kg/day, divided into pre-meal doses.
- Type 2 Diabetes: 10 units pre-meal or 0.1–0.2 units/kg/day, adjusted based on glucose monitoring (BNF).
- Titration: Adjust doses weekly based on pre- and postprandial glucose readings.
- Special Populations:
- Renal/Hepatic Impairment: Reduced insulin clearance may necessitate lower doses; monitor closely.
- Elderly: Higher hypoglycemia risk; conservative dosing advised (Lange).
- Hypoglycemia (tremors, sweating, confusion).
- Injection-site reactions (erythema, itching, lipodystrophy with prolonged use).
- Weight gain (anabolic effects of insulin).
Serious:
- Severe Hypoglycemia: Risk with overdose, erratic eating, or strenuous exercise.
- Hypokalemia: Insulin shifts potassium intracellularly; monitor in critical care settings.
- Allergic Reactions: Rare angioedema or anaphylaxis (Lippincott).
- Contraindications: Hypoglycemia, hypersensitivity to insulin glulisine or excipients.
- Blood glucose (pre-/postprandial and bedtime).
- HbA1c (every 3–6 months).
Renal/hepatic function in impaired patients
- Pregnancy: Category C; use with caution as insulin requirements may fluctuate.
Lactation: Safe; insulin does not pass into breast milk (BNF
- Beta-Blockers: Mask hypoglycemia symptoms (e.g., tachycardia).
- Corticosteroids/Thiazides: Antagonize insulin effects, increasing glucose levels.
- Alcohol: Potentiates hypoglycemia; avoid concurrent use.
- ACE Inhibitors/Pioglitazone: Enhance insulin sensitivity, raising hypoglycemia risk (Lange).
Generic Names in Pharmacy
- Generic: Insulin glulisine.
- Brand Name: Apidra® (Sanofi).
