Product Information
Registration Status: ActiveSIN15515P
LEVEMIR PENFILL 100 U/ML is approved to be sold in Singapore with effective from 2018-07-20. It is marketed by NOVO NORDISK PHARMA (SINGAPORE) PTE LTD, with the registration number of SIN15515P.
This product contains Insulin Detemir 100U/ml in the form of INJECTION, SOLUTION. It is approved for SUBCUTANEOUS use.
This product is manufactured by Novo Nordisk A/S (Bagsv?rd) (Bulk Production and Primary Packager) in FRANCE,Novo Nordisk A/S (Kalundborg) in DENMARK, andNovo Nordisk Produc?o Farmaceutica do Brasil Ltda. in BRAZIL.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
Insulin detemir is a long-acting human insulin analogue used to maintain basal levels of insulin in diabetic individuals. It is produced using recombinant DNA technology in yeast cells. This insulin analogue has a 14-C fatty acid, myristic acid, bound to the lysine amino acid at position B29. The myristoyl side chain increases self-association and albumin binding. This along with slow systemic absorption from the injection site prolongs distribution of the hormone into tissues and results in a long duration of action. Novo Nordisk markets insulin detemir under the trade name Levemir.
Indication
For the treatment of type 1 or 2 diabetes mellitus. May be used in combination with oral anti-diabetic agents in type 2 diabetic patients who are not in adequate metabolic control with oral anti-diabetic agents alone.
Mechanism of Action
Insulin detemir 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. Insulin detemir’s long duration of action appears to be a result of slow systemic absorption from the injection site and delayed distribution to target tissues. The myristic acid side chain on insulin detemir increases self-association and gives it a high binding affinity to serum albumin. These features slows its distribution into target tissues and prolongs its duration of action.
Pharmacokinetics
- Absorption
- Maximum serum concentrations are reached 6 to 8 hours following subcutaneous injection. When single dose of 0.5 units/kg of insulin detemir was given to adult type 1 diabetes patients, the maximum serum concentration (Cmax) was 4,641 ± 2,299 pmol/L. Absorption is also dependent on the site of injection. When injected into the thigh, the AUC was lower than when injected into the deltoid and abdominal regions. Bioavailability is approximately 60%.
- Distribution
- * 0.1 L/kg
- Metabolism
- As with natural insulin, all metabolites formed are inactive.
- Elimination
Clearance
Apparent clearance (CL/F), type 1 diabetes adult patients = 3.41 ± 1.00 L/min·kg
Toxicity
Hypoglycemia may occur with inappropriately high doses. 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. Injection site reactions may also occur. Symptoms include: redness, inflammation, bruising, swelling and itching at the injection site.
Active Ingredient/Synonyms
Detemir | Insulin detemir recombinant | Insulin,detemir,human | Insulin Detemir |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.