Introduction
NovoLog (insulin aspart) is a rapid-acting human insulin analog used to improve glycemic control in patients with diabetes mellitus. It is designed to mimic the physiological prandial insulin response and is typically administered immediately before meals to manage postprandial blood glucose elevations.
Mechanism of Action
NovoLog functions as a rapid-acting insulin analog that lowers blood glucose by facilitating cellular uptake of glucose into skeletal muscle and adipose tissue while simultaneously inhibiting hepatic glucose production. Insulin aspart differs from human insulin by a single amino acid substitution (aspartic acid for proline at position B28), which reduces self-association into hexamers, allowing for more rapid absorption and onset of action compared to regular human insulin.
Indications
- Treatment of type 1 diabetes mellitus in adults and pediatric patients
- Treatment of type 2 diabetes mellitus in adults
- Continuous subcutaneous insulin infusion (CSII) via insulin pump in patients with diabetes
Dosage and Administration
Route: Subcutaneous injection (abdomen, thigh, buttocks, or upper arm) or continuous subcutaneous infusion via insulin pump Dosing:- Individualized based on metabolic needs, blood glucose monitoring, and glycemic control goals
- Typically administered 5-10 minutes before meals
- Dosage requirements vary considerably among patients (generally 0.5-1.0 unit/kg/day)
- Approximately 50-70% of total daily insulin requirement may be provided as NovoLog, with the remainder as intermediate or long-acting insulin
- Renal impairment: Requires careful glucose monitoring and dose adjustment
- Hepatic impairment: Requires careful glucose monitoring and dose adjustment
- Elderly: May require more conservative dosing due to increased risk of hypoglycemia
Pharmacokinetics
Absorption: Rapidly absorbed with onset of action within 15 minutes after subcutaneous administration. Peak concentration occurs 40-50 minutes after dosing. Distribution: Distributed throughout extracellular fluid. Minimal protein binding. Metabolism: Metformed primarily in liver and kidney via insulin protease or insulin-specific endopeptidase. Elimination: Half-life approximately 60-90 minutes. Duration of action is 3-5 hours.Contraindications
- Hypersensitivity to insulin aspart or any component of the formulation
- During episodes of hypoglycemia
- During periods of hypoglycemia unawareness
Warnings and Precautions
Hypoglycemia: Most common adverse effect. Risk increased with changes in meal pattern, exercise, renal/hepatic impairment, and concomitant glucose-lowering medications. Hypokalemia: May cause hypokalemia, which can be life-threatening if severe. Lipodystrophy: May occur at injection sites; rotate injection sites to reduce risk. Weight gain: Can occur due to anabolic effects of insulin. Fluid retention: Can occur with initiation or rapid improvement in glycemic control. Allergic reactions: Both local and systemic reactions may occur. Pump malfunctions: With CSII use, pump malfunctions can lead to hyperglycemia and ketoacidosis.Drug Interactions
Drugs that may increase hypoglycemic risk:- Oral antidiabetic agents
- ACE inhibitors
- Disopyramide
- Fluoxetine
- MAO inhibitors
- Pentoxifylline
- Propoxyphene
- Salicylates
- Somatostatin analogs
- Sulfonamide antibiotics
- Corticosteroids
- Danazol
- Diuretics
- Sympathomimetics
- Phenothiazines
- Somatropin
- Thyroid hormones
- Estrogens/progestogens
- Atypical antipsychotics
Adverse Effects
Very common (>10%):- Hypoglycemia
- Injection site reactions (redness, swelling, itching)
- Lipodystrophy
- Weight gain
- Peripheral edema
- Hypersensitivity reactions
- Pruritus
- Rash
- Anaphylaxis
- Severe hypoglycemia
- Sodium retention
- Visual refractive changes
Monitoring Parameters
- Blood glucose monitoring (preprandial, postprandial, bedtime, and occasionally overnight)
- HbA1c every 3-6 months
- Periodic assessment of injection sites
- Serum potassium in patients at risk for hypokalemia
- Renal and hepatic function
- Signs and symptoms of hypoglycemia
- Weight changes
- Visual acuity in patients with retinopathy
Patient Education
- Proper injection technique and site rotation
- Timing of administration (5-10 minutes before meals)
- Recognition and management of hypoglycemia
- Importance of regular blood glucose monitoring
- Never share insulin pens or needles
- Proper storage (refrigerate unopened vials/pens; room temperature for in-use products for up to 28 days)
- Sick day management
- Carry glucose source at all times
- Wear diabetes identification
- Inform healthcare providers about diabetes and insulin therapy
- Pump users: Regular pump maintenance and troubleshooting
References
1. NovoLog Prescribing Information. Novo Nordisk Inc. 2022. 2. American Diabetes Association. Standards of Medical Care in Diabetes - 2023. Diabetes Care. 2023;46(Suppl 1):S1-S291. 3. Hirsch IB. Insulin analogues. N Engl J Med. 2005;352(2):174-183. 4. Home PD. The pharmacokinetics and pharmacodynamics of rapid-acting insulin analogues and their clinical consequences. Diabetes Obes Metab. 2012;14(9):780-788. 5. Heinemann L, Muchmore DB. Ultrafast-acting insulins: state of the art. J Diabetes Sci Technol. 2012;6(4):728-742. 6. Plank J, et al. A double-blind, randomized, dose-response study investigating the pharmacodynamic and pharmacokinetic properties of the long-acting insulin analog detemir. Diabetes Care. 2005;28(5):1107-1112. 7. FDA-approved labeling for NovoLog. Accessible at: https://www.accessdata.fda.gov