Insulin aspart protamine and insulin aspart
Insulin aspart protamine and insulin aspart Uses, Dosage, Side Effects, Food Interaction and all others data.
The primary activity of Insulin Aspart is the regulation of glucose metabolism. Insulin Aspart bind to the insulin receptors on muscle and fat cells and lower blood glucose by facilitating the cellular uptake of glucose and simultaneously inhibiting the output of glucose from the liver.
Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic individuals, a basal level of insulin is supplemented with insulin spikes following meals. Postprandial insulin spikes are responsible for the metabolic changes that occur as the body transitions from a postabsorptive to absorptive state. Insulin promotes cellular uptake of glucose, particularly in muscle and adipose tissues, promotes energy storage via glycogenesis, opposes catabolism of energy stores, increases DNA replication and protein synthesis by stimulating amino acid uptake by liver, muscle and adipose tissue, and modifies the activity of numerous enzymes involved in glycogen synthesis and glycolysis. Insulin also promotes growth and is required for the actions of growth hormone (e.g. protein synthesis, cell division, DNA synthesis). Insulin aspart is a rapid-acting insulin analogue used to mimic postprandial insulin spikes in diabetic individuals. The onset of action of insulin aspart is 10-15 minutes. Its activity peaks 60-90 minutes following subcutaneous injection and its duration of action is 4-5 hours.
| Trade Name | Insulin aspart protamine and insulin aspart |
| Generic | Insulin aspart + insulin aspart protamine |
| Type | Subcutaneous |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Insulin Aspart is a rapid acting human insulin analog used to improve glycemic control in adults and children with diabetes mellitus.
Insulin aspart protamine and insulin aspart is also used to associated treatment for these conditions: Diabetes Mellitus, Diabetic Ketoacidosis, Gestational Diabetes Mellitus (GDM), Hyperglycemia during critical illness
How Insulin aspart protamine and insulin aspart 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
Insulin aspart protamine and insulin aspart 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.
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 Insulin Aspart is contraindicated-
- during episodes of hypoglycemia
- in patients with hypersensitivity to Insulin Aspart or one of its excipients
Special Warning
Renal Impairment: Decreased dose may be necessary.
Hepatic Impairment: Decreased dose may be necessary.
Innovators Monograph
You find simplified version here Insulin aspart protamine and insulin aspart
