Insulin aspart protamine and insulin aspart is a sterile suspension of human insulin analog containing 30% soluble insulin aspart and 70% protamine-crystallised insulin aspart. It is a blood glucose lowering agent with an earlier onset and an intermediate duration of action. Insulin Aspart is homologous with regular human insulin with the exception of a single substitution of the amino acid proline by aspartic acid in position B28, and is produced by recombinant DNA technology.

Pharmacology

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.

Each ml suspension contains 100 IU (equivalent to 3.50 mg) Insulin Aspart (rDNA) BP as 30% soluble Insulin Aspart and 70% protamine-crystallised Insulin Aspart.

Insulin Aspart is a rapid acting human insulin analog indicated to improve glycemic control in adults and children with diabetes mellitus.

Dosage of Insulin Aspart is individual and determined by the physician in accordance with the needs of the patient. In patients with type 2 diabetes, Insulin Aspart can be given in mono therapy or in combination with oral antidiabetic drugs when the blood glucose is inadequately controlled with those oral antidiabetic drugs alone. For patients with type 2 diabetes, the recommended starting dose of Insulin Aspart is 6 IU at breakfast and 6 IU at dinner (evening meal). Insulin Aspart can also be initiated once daily with 12 IU at dinner (evening meal). When using Insulin Aspart once daily, it is generally recommended to move to twice-daily when reaching 30 units by splitting the dose into equal breakfast and dinner doses. If twice daily dosing with Insulin Aspart results in recurrent daytime hypoglycaemic episodes, the morning dose can be split into morning and lunchtime doses (thrice daily dosing).

The dose should not be increased if hypoglycemia occurred within three days. Dose adjustments can be made once a week until target HbA1c is reached. In patients with type 1 diabetes the individual insulin requirement is usually between 0.5 and 1.0 IU/kg/day. Insulin Aspart may fully or partially meet this requirement. When transferring a patient from biphasic human insulin to Insulin Aspart, start with the same dose and regimen. Then titrate according to individual needs (according to the titration guidelines in table above). Insulin Aspart can be used in elderly patients; however there is limited experience with the use of Insulin Aspart in combination with OADs in patients older than 75 years.

Administration

Administer 5-10 min before meal

Insulin Insulin Aspart is contraindicated-

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

Side effects of Insulin Aspart are hypoglycemia, allergic reactions, injection site reaction, lipodystrophy, pruritus and rash.

Overdose Effects

A specific overdose for insulin cannot be defined, however, hypoglycaemia may develop over sequential stages if too high doses relative to the patient’s requirement are administered. Mild hypoglycaemic episodes can be treated by oral administration of glucose or sugary products. Severe hypoglycaemic episodes, where the patient has become unconscious, can be treated by glucagon (0.5 to 1 mg) given intramuscularly or subcutaneously. Glucose must also be given intravenously if the patient does not respond to glucagon within 10 to 15 minutes. Upon regaining consciousness administration of oral carbohydrate is recommended for the patient in order to prevent relapse.

Dose adjustment and monitoring: Blood glucose should be monitored in all patients treated with insulin. Insulin regimens should be modified cautiously and only under medical supervision.

Use in Special Populations

Renal Impairment: Decreased dose may be necessary.

Hepatic Impairment: Decreased dose may be necessary.

Pregnancy & Lactation

Pregnancy category B. There are no restrictions on treatment with Insulin Aspart during lactation. Insulin treatment of the nursing mother should not affect the baby. However, dosage may need to be adjusted.