Insulin Aspart [Protamine Crystallised]

Insulin Aspart [Protamine Crystallised] is indicated for glycemic control in patients with diabetes mellitus:

Approved Indications:

• Type 1 Diabetes Mellitus (T1DM):
  Used as part of a basal-prandial insulin regimen to provide intermediate-duration insulin coverage, typically in combination with rapid-acting insulin for postprandial glucose control.
• Type 2 Diabetes Mellitus (T2DM):
  For patients inadequately controlled on oral antidiabetic agents or other insulin regimens who require both basal and postprandial glycemic management.

Clinically Accepted Off-Label Uses:

• Gestational diabetes under strict clinical supervision.
• Inpatient hyperglycemia management where intermediate-duration basal coverage is needed.

Administration Route: Subcutaneous injection into the thigh, upper arm, or abdomen. Rotate injection sites to minimize lipodystrophy. Do not mix with other insulin products in the same syringe.

Adults:

• Dose individualized based on prior insulin use, body weight, and blood glucose targets.
• Typically administered once or twice daily depending on glucose monitoring results and regimen design.
• Dose titration: Adjust by 2–4 units every 3–4 days based on fasting and pre-meal glucose levels.

Pediatrics (≥1 year):

• Initial dose calculated based on body weight and prior insulin therapy.
• Frequent glucose monitoring required during initiation and titration.

Elderly:

• Begin with lower doses due to increased risk of hypoglycemia.
• Monitor renal and hepatic function closely.

Special Populations:

• Renal Impairment: Dose adjustment may be necessary; monitor glucose closely.
• Hepatic Impairment: Initiate cautiously; titrate according to glycemic response.
• Transition from Other Insulins: Calculate total daily insulin and adjust basal portion accordingly.

Insulin Aspart [Protamine Crystallised] is an intermediate-acting insulin formed by complexing rapid-acting insulin Aspart with protamine, which slows its absorption and prolongs its action. After subcutaneous injection, it is gradually released into the bloodstream, where it binds to insulin receptors on target cells. This facilitates glucose uptake in muscle and adipose tissue and suppresses hepatic glucose production, providing sustained basal insulin coverage and reducing blood glucose fluctuations between meals and overnight.

• Absorption: Slow and prolonged due to protamine complexation; onset typically 1–2 hours.
• Distribution: Distributed in extracellular fluid; minimal protein binding.
• Metabolism: Degraded proteolytically in liver and kidneys; no active metabolites.
• Elimination: Primarily renal; half-life approximately 4–6 hours.
• Onset of Action: 1–2 hours.
• Peak Action: 4–12 hours.
• Duration: 12–16 hours.
• Bioavailability: Similar to other subcutaneously administered insulin analogs.

• Pregnancy: Insulin is the preferred therapy for glycemic control during pregnancy. Limited specific data on Aspart Protamine; used safely under clinical supervision.
• Lactation: Compatible with breastfeeding. Minimal transfer into milk; monitor infant for hypoglycemia.
• Caution: Dose adjustments may be required based on frequent glucose monitoring.

• Primary Class: Antidiabetic Agent
• Subclass: Insulin analog, intermediate-acting (protamine-complexed)

• Known hypersensitivity to Insulin Aspart [Protamine Crystallised] or any excipients.
• Severe hypoglycemia.
• Diabetic ketoacidosis unless used as part of a comprehensive insulin regimen.

• Hypoglycemia: High-risk groups include elderly, renal/hepatic impairment, or patients on other hypoglycemic agents.
• Allergic Reactions: Rare anaphylaxis possible; discontinue if severe.
• Fluid Retention/Heart Failure: Monitor patients on thiazolidinediones.
• Injection Site Reactions: Lipodystrophy may occur; rotate injection sites.
• Monitoring: Regular blood glucose and HbA1c assessments; ketone monitoring if hyperglycemia persists.

Common:

• Hypoglycemia (most frequent)
• Injection site reactions: redness, swelling, itching
• Weight gain

Less Common:

• Edema
• Allergic reactions
• Lipodystrophy at injection sites

Rare/Severe:

• Severe hypoglycemia with neuroglycopenic symptoms
• Anaphylaxis

• Sulfonylureas, meglitinides: Increased risk of hypoglycemia.
• Beta-blockers: May mask hypoglycemia symptoms.
• Alcohol: May potentiate or reduce hypoglycemic effect.
• Corticosteroids, thiazide diuretics: May reduce insulin effectiveness.
• CYP450: Minimal involvement; insulin is metabolized proteolytically.

• Recognized for intermediate-duration basal coverage in T1DM and T2DM patients.
• Guidelines emphasize individualized dosing and frequent glucose monitoring to prevent hypoglycemia.
• Flexible administration timing is allowed for twice-daily dosing.

• Temperature: Store 2°C–8°C (refrigerated); do not freeze.
• Room Temperature Use: Can be kept at ≤30°C for up to 4 weeks (specific to pen/vial).
• Light Protection: Keep in original pen/vial; protect from direct sunlight.
• Handling: Roll gently before use; do not shake vigorously.
• Reconstitution: Not required; solution is clear and ready-to-use.