Acilog

Uses

Acilog is a rapid acting human insulin analog used to improve glycemic control in adults and children with diabetes mellitus.

Acilog is also used to associated treatment for these conditions: Diabetes Mellitus, Diabetic Ketoacidosis, Gestational Diabetes Mellitus (GDM), Hyperglycemia during critical illness

How Acilog works

Insulin aspart binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor autophosphorylates and phosphorylates numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. Activation of these proteins leads to the activation of downstream signaling molecules including PI3 kinase and Akt. Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC), both of which play critical roles in metabolism and catabolism. In humans, insulin is stored in the form of hexamers; however, only insulin monomers are able to interact with IR. Substitution of the proline residue at B28 with aspartic acid reduces the tendency to form hexamers and results in a faster rate of absorption and onset of action and shorter duration of action.

Dosage

Acilog dosage

Usual range: 0.5-1 units/kg/day. When used in a meal-related SC inj treatment regimen, insulin aspart may provide 50-70% of total insulin requirement with the remainder provided by an intermediate-acting or long-acting insulinThe dosage of insulin aspart must be individualized

Subcutaneous injection: insulin aspart should generally be given immediately (within 5-10 minutes) prior to the start of a meal

Use in pumps: Change the insulin aspart in the reservoir at least every 6 days, change the infusion set, and the infusion set insertion site at least every 3 daysinsulin aspart should not be mixed with other insulins or with a diluent when it is used in the pump

Intravenous use: Insulin aspart should be used at concentrations from 0.05 U/mL to 1.0 U/mL insulin aspart in infusion systems using polypropylene infusion bags. insulin aspart has been shown to be stable in infusion fluids such as 0.9% sodium chloride

Administer 5-10 min before meal

Side Effects

Hypoglycaemia; oedema; pruritus; rash; hypersensitivity reactions; lipoatrophy or lipohypertrophy with SC Inj (rotate Inj site).

Toxicity

Inappropriately high dosages relative to food intake and/or energy expenditure may result in severe and sometimes prolonged and life-threatening hypoglycemia. Neurogenic (autonomic) signs and symptoms of hypoglycemia include trembling, palpitations, sweating, anxiety, hunger, nausea and tingling. Neuroglycopenic signs and symptoms of hypoglycemia include difficulty concentrating, lethargy/weakness, confusion, drowsiness, vision changes, difficulty speaking, headache, and dizziness. Mild hypoglycemia is characterized by the presence of autonomic symptoms. Moderate hypoglycemia is characterized by the presence of autonomic and neuroglycopenic symptoms. Individuals may become unconscious in severe cases of hypoglycemia.

Precaution

Renal or hepatic impairment; pregnancy; lactation. Transferring from other insulin. Monitor serum glucose, potassium, electrolytes, HbA1c and lipid profile. Concomitant illness esp infections; hypokalaemia.

Interaction

Effects may be increased by: oral antidiabetic agents, ACE inhibitors, disopyramide, fibrates, fluoxetine, MAOIs, propoxyphene, salicylates, somatostatin analog (e.g., octreotide), sulfonamide antibiotics. Effects may be decreased by: corticosteroids, niacin, danazol, diuretics, sympathomimetic agents, isoniazid, phenothiazine derivatives, somatropin, thyroid hormones, oral contraceptives, lithium. Signs of hypoglycaemia may be masked by β-blockers, clonidine.

Food Interaction

• Take with food. Dose adjust as needed. Changes in meal composition may alter the response to insulin aspart.

Elimination Route

In studies of healthy volunteers and patients with type 1 diabetes, the median time to maximum concentration of insulin aspart in these trials was 40 to 50 minutes versus 80 to 120 minutes, for regular human insulin respectively. Compared to human insulin, insulin aspart has a faster absorption, a faster onset of action, and a shorter duration of action than regular human insulin after subcutaneous injection. It takes 40 - 50 minutes to reach maximum concentration. When a dose of 0.15 U/kg body weight was injected in type 1 diabetes patients, the mean maximum concentration (Cmax) was 82 mU/L. The site of injection has no impact on extent or speed of absorption.

Half Life

Elimination half-life was found to be 81 minutes (following subcutaneous administration in healthy subjects).

Clearance

1.2 L/h/kg

Pregnancy & Breastfeeding use

Pregnancy Category B. All pregnancies have a background risk of birth defects, loss, or other adverse outcome regardless of drug exposure. This background risk is increased in pregnancies complicated by hyperglycemia and may be decreased with good metabolic control. It is essential for patients with diabetes or history of gestational diabetes to maintain good metabolic control before conception and throughout pregnancy. Insulin requirements may decrease during the first trimester, generally increase during the second and third trimesters, and rapidly decline after delivery. Careful monitoring of glucose control is essential in these patients. Therefore, female patients should be advised to tell their physician if they intend to become, or if they become pregnant while taking insulin aspart.

Contraindication

Insulin Acilog is contraindicated-

• during episodes of hypoglycemia
• in patients with hypersensitivity to Acilog or one of its excipients

Special Warning

Renal Impairment: Decreased dose may be necessary.

Hepatic Impairment: Decreased dose may be necessary.

Innovators Monograph

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