Insulin glargine

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Insulin glargine
Systematic (IUPAC) name
Recombinant human insulin
Identifiers
CAS number	160337-95-1
ATC code	A10AE04
PubChem	?
DrugBank	BTD00045
Chemical data
Formula	C267H408N72O77S6
Mol. mass	6063 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	C(US)
Legal status	POM(UK) ℞-only(US)
Routes	Subcutaneous

Insulin glargine, marketed by Sanofi-Aventis under the name Lantus, is a long-acting basal insulin analogue, usually given once or twice daily to help control the blood sugar level of those with diabetes. Its theoretical advantage is that it has a duration of action up to 24 hours, with a "less peaked" profile than NPH. Thus, it more closely resembles the basal insulin secretion of the normal pancreatic beta cells. In type 2 diabetes and in combination with a short acting sulfonylurea (drugs which stimulate the pancreas to make more insulin), it can offer moderate control of serum glucose levels. In the absence of endogenous insulin (Type 1 diabetes or depleted type 2), Lantus needs the support of a fast acting insulin taken with food to reduce the effect of prandially derived glucose. It is post-prandial glucose elevation which more significantly affects HbA_1c and thus determines the progression of the long-term complications of diabetes mellitus.

The peakless profile of Lantus also enables the dose to be relatively higher than standard NPH insulin. Because standard NPH is normally administered at night, its peak of action tends to coincide with the lower serum glucose levels associated with nocturnal metabolism. This can induce nocturnal hypoglycaemia. Lantus offers the benefit of a more consistent pharmacological dynamic without nocturnal hypoglycaemia. The result of this is a patient who feels more confident and more comfortable with a lower pre-bed and pre-breakfast capillary glucose level.

Lantus is formulated at an acidic pH 4, where it is completely water soluble. After subcutaneous injection of the acidic solute ( which can cause discomfort and a stinging sensation ), the body, at pH 7, slowly neutralizes the solution, causing insulin microcrystals to gradually precipitate from the insulin glargine solution, which then release insulin in bioloigically active form. This gradual process ensures that small amounts of Lantus are released into the body continuously, giving an almost peakless profile. Significant weight gain is seen in many patients using Lantus.

[edit] Mechanism of Action

Insulin glargine have subsitution of glycine for asparagine at A21 and two arginines added to the carboxy terminal of B chain. This allows insulin glargine to form a precipitate (hexamer) when injected subcutaneously into the patient. It can achieve a peakless level for at least 24 hours.

[edit] External links

• Insulin glargine - MedlinePlus
• Lantus website (Sanofi-Aventis)

v • d • e Oral antidiabetic drugs and Insulin analogs (A10) Biguanides Metformin Sulfonylureas Carbutamide, Chlorpropamide, Glibenclamide (Glyburide), Gliclazide, Glimepiride, Glipizide, Gliquidone, Tolazamide, Tolbutamide Alpha-glucosidase inhibitors Acarbose, Miglitol, Voglibose Thiazolidinediones (TZD) Pioglitazone, Rivoglitazone†, Rosiglitazone, Troglitazone‡ Meglitinides Nateglinide, Repaglinide, Mitiglinide Dipeptidyl peptidase-4 (DPP-4) inhibitors Alogliptin†, Saxagliptin†, Sitagliptin, Vildagliptin Glucagon-like peptide-1 analog Exenatide, Liraglutide†, Albiglutide† Amylin analog Pramlintide Insulin analogs fast acting (Insulin lispro, Insulin aspart, Insulin glulisine), long acting (Insulin glargine, Insulin detemir), Inhalable insulin (Exubera) Dual PPAR agonists Aleglitazar†, Muraglitazar§, Tesaglitazar§ SGLT2 inhibitor Dapagliflozin†, Remogliflozin† †Undergoing clinical trials. ‡ Withdrawn from market. §Development halted.