Insulin Glargine Pharmacology

Insulin Glargine

About Insulin Glargine
Pancreatic hormone, A long-acting basal insulin analogue, Antidiabetic Agent.
Mechanism of Action of Insulin Glargine
It is a long acting Insulin used for the control of hyperglycaemia. Insulin acts through binding to a subunit of insulin receptors located on the cell membrane of all cells (highest densities are seen in muscle, liver, and adipose tissue).This binding induces aggregation and internalization of the receptor along with the bound Insulin. This activates tyrosine kinase activity of the ? subunits and tyrosine residues of the ? subunits get autophosphorylated; thus the activity of this subunit to phosphorylate tyrosine residues of Insulin Receptor Substrate proteins (IRS1, IRS2) is increased. These results in a cascade of phosphorylation and dephosphorylation reactions which lead to stimulation or inhibition of enzymes involved in the metabolic actions of Insulin. Action of Insulin on metabolic enzymes are also mediated through second messengers like phosphatidyl inositol glycan (PIG) and Diacyl glycerol (DAG) which are generated through activation of specific phospholipase C.
Insulin stimulates glucose transport across cell membrane by ATP dependent translocation of glucose transporters GLUT1 and GLUT4 to the plasma membrane and by increasing their activity. Insulin promotes the expression of genes directing synthesis of glucose transporters. It also regulates genes for a large number of enzymes and carriers primarily through muscle action potential (MAP) kinases
Insulin causes increased production of glucokinase improves intracellular utilization of glucose. It also stimulates glycogen synthetase and enhances glycogen synthesis and inhibits phosphorylase and thus decreases glycogenolysis in liver. Insulin reduces synthesis of phosphoenol pyruvate carboxykinase and inhibits gluconeogenesis. It inhibits lipolysis in adipose tissue and favours triglyceride synthesis. Insulin increases clearance of VLDL and chylomicrons by stimulating transcription of vascular endothelial lipoprotein lipase. Insulin improves synthesis of proteins from amino acids and prevents breakdown of proteins.

Pharmacokinets of Insulin Glargine
Absorption: Administered subcutaneously and slowly absorbed from injection site.
Distribution: It is widely distributed throughout the body
Metabolism: It is metabolized in liver, muscles, and kidney.
Onset of Action for Insulin Glargine
Within 60 minutes
Duration of Action for Insulin Glargine
24 hours
Peak action: 10-30 hours.
Half Life of Insulin Glargine
5 to 6minutes
Side Effects of Insulin Glargine
1. Allergic reactions at the injection site
2. Lipodystrophy at injection site
3. Hypoglycaemia
4. Insulin resistance
5. Oedema

Contra-indications of Insulin Glargine
1. Hypersensitivity to the drug
2. Insulinoma
3. Hypoglycaemia
4. Should not administer intravenously
5. Should not be mixed with other Insulins or diluted
Special Precautions while taking Insulin Glargine
1. Control diet and exercise regularly along with therapy
2. Along with other drugs
3. Along with alcohol
4. Rotate the injection site
5. Renal impairment
6. Hepatic impairment
7. Stress
8. Infections
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution
Children (below 6 years) : Contraindicated
Indications for Insulin Glargine
1. Type 1 diabetes mellitus
2. Type II diabetes mellitus
Interactions for Insulin Glargine
Drugs which decrease hypoglycaemic effect of insulin : Oral contraceptives, corticosteroids, diltiazem, dobutamine, epinephrine, smoking, thiazide diuretics, thyroid hormone.
Drugs which increase hypoglycaemic effect of insulin : Alcohol, anabolic steroids, beta-blockers, clofibrate, guanethidine, MAO inhibitors, phenylbutazone, salicylates, tetracyclines.
Typical Dosage for Insulin Glargine
Initially 10 U as once daily dose; preferably at the same time of the day. Dose is individualized based on the severity of diabetes; usually ranges from 2 to 100U/day.
Schedule of Insulin Glargine
G
Storage Requirements for Insulin Glargine
Store at a temperature range of 2 to 8 degree C in a refrigerator. Protect from direct light and heat. Keep out of reach of children.
Effects of Missed Dosage of Insulin Glargine
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Insulin Glargine
Treatment based on symptoms of hypoglycaemia. Glucose must be given orally or I.V. (for severe cases); at an infusion rate of 10 to 20mg/kg/minute. If patient is responsive give 10 to 15g of a fast acting oral carbohydrate. If patient`s signs and symptoms persist give an additional 10g of carbohydrate.

Home Delivery for Insulin Glargine in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including insulin glargine.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for insulin glargine and other medicines and health products. Home delivery services for insulin glargine may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take insulin glargine only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for insulin glargine before they complete the sale. You can get this information while placing the order for insulin glargine with the pharmacy.

Insulin Glargine is a generic medicine name and there are several brands available for it. Some of the brands for insulin glargine might be better known than insulin glargine itself. If the pharmacy that's willing to deliver medicines to your home doesn't have insulin glargine in stock, you can ask for one of the branded alternatives for insulin glargine.