How is lantus metabolized? By Steven Fiorini / QnA Insulin glargine is metabolized in the liver into two active metabolites with similar activity to insulin: 21a-Gly-human insulin (M1) and 21a-Gly-des-30b- threonine insulin (M2), with M1 being the predominant metabolite.
Will I still use my mealtime insulin or other insulins with Lantus?
You might. Lantus is a long-acting insulin that’s meant work over the course of an entire day. Long-acting insulin is typically called basal or “ba...
Is it better to take Lantus in the morning or at night?
The best time to take Lantus depends on how your blood sugar levels change throughout the day. In clinical studies, blood sugar levels were reduced...
Will Lantus cause hypoglycemia?
It can. Hypoglycemia (low blood sugar levels) is one of the most common side effects of insulin products, including Lantus. Some factors that can i...
Does Lantus treat diabetic ketoacidosis?
No. Lantus isn’t used to treat diabetic ketoacidosis (DKA). DKA is a serious complication of diabetes. It occurs when your blood sugar levels are v...
What are the two insulin analogs?
Modifications of the insulin molecule have resulted in two long-acting insulin analogs (glargine and detemir ) and three rapid-acting insulins (aspart, lispro, and glulisine) with improved pharmacokinetic/pharmacodynamic (PK/PD) profiles.
What is lantus injection?
Lantus (insulin glargine [rDNA origin] injection): A therapeutic class review The beneficial effects of achieving blood glucose concentrations close to normal in type 1 and type 2 diabetes have been firmly established . However, the best means of attaining a near-normal physiological pattern of insulin secretion is still uncertain. In healthy individuals without diabetes, insulin secretion is characterized by continuous basal secretion, with peaks immediately after meals and steady release throughout the night, hence avoiding nocturnal hypoglycemia or hyperglycemia at dawn. To achieve the basal insulin requirement in diabetic patients, one or more doses of intermediate or long-acting insulin are necessary. Due to the short duration of NPH insulin, the considerable variation in absorption of long-acting insulins, and the peak-action profile of both, these current strategies may not provide an appropriate basal supply. Therefore, development of an improved, long-acting insulin is a critical step toward improving glycemic control and preventing long-term complications of diabetes. Lantus (insulin glargine, Aventis Pharmaceuticals) is a long-acting basal insulin approved by the Food and Drug Administration on April 20, 2000, and launched on May 14, 2001. The product is a synthetic human insulin that has been modified using DNA technology to slightly change the structure of the insulin molecule. Insulin glargine mimics normal basal secretion of endogenous insulin with a duration of action of up to 24 hours. The manufacturer suggests that this near-constant supply of low-level basal insulin appears to be essential to improving overall glycemic control. The extended action of the most commonly used basal insulin formulations, NPH and lente, is produced by combining insulin wit Continue reading >>
What is insulin glargine?
Insulin glargine, marketed under the names Lantus, among others, is a long-acting basal insulin analogue, given once daily to help control the blood sugar level of those with diabetes. It consists of microcrystals that slowly release insulin, giving a long duration of action of 18 to 26 hours, with a "peakless" profile (according to the insulin glargine package insert). Pharmacokinetically, it resembles basal insulin secretion of non-diabetic pancreatic beta cells. Sometimes, 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, depleted type 2 (in some cases) or latent autoimmune diabetes of adults in late stage—insulin glargine needs the support of fast acting insulin taken with food to reduce the effect of prandially derived glucose. Medical uses The long-acting insulin class, which includes insulin glargine, do not appear much better than neutral protamine Hagedorn (NPH) insulin but have a significantly greater cost making them, as of 2010, not cost effective. [1] It is unclear if there is a difference in hypoglycemia and not enough data to determine any differences with respect to long term outcomes. [2] Mixing with other insulins Unlike some other longer-acting insulins, glargine must not be diluted or mixed with other insulin or solution in the same syringe. [3] However, this restriction has been questioned. [4] Adverse effects Cancer As of 2012 tentative evidence shows no association between insulin glargine and cancer. [5] Previous studies had raised concerns. [6] Pharmacology Mechanism of action Insulin glargine has a substitution of glycine for Continue reading >>
How long does insulin glargine last?
Insulin Glargine acts as a long lasting (upto 24 hour duration) insulin, which reduces the amount of sugar in the blood and urine. The drug is used to treat patients with type 1diabetes or diabetes mellitus type 1.
What is the generic name for insulin glargine?
The drug is available under generic name Insulin Glargine and brand names Lantus , Toujeo,Abasaglar, and Basaglar What is the source of the drug (natural or synthetic)? Insulin Glargine is a synthetic bioengineered (man-made) injectable form of long-acting insulin.
Why is insulin released?
Insulin is released to help the body regulate blood glucose. Insulin release is triggered by an increase in blood glucose from food consumption. Lantus is a basal insulin analogue and it is equivalent to human insulin but it has a slower onset, no pronounced peak, and longer duration of action.
How much insulin is needed for diabetes mellitus?
Diabetes mellitus, type 1: SubQ: Insulin glargine-specific dosing: Initial dose: Approximately one-third to one-half of the total daily insulin requirement administered once daily. A rapid-acting or short-acting insulin should also be used to complete the balance (~1/2 to 2/3) of the total daily insulin requirement.
Is it better to take Lantus in the morning or at night?
The best time to take Lantus depends on how your blood sugar levels change throughout the day.
Will Lantus cause hypoglycemia?
It can. Hypoglycemia (low blood sugar levels) is one of the most common side effects of insulin products, including Lantus.
How many units of insulin is in a Lantus pen?
The drug comes as a solution inside 10-milliliter (mL) vials that hold 100 units of insulin glargine per mL. The vial is used with needles, which aren’t included with the vial. Lantus also comes as a prefilled SoloStar pen. Each pen contains 3 mL of drug solution that has 100 units of insulin per mL of solution.
Why do people with type 1 diabetes need Lantus?
People with type 1 diabetes will need to take Lantus along with a mealtime insulin. This is because Lantus is a basal insulin, a “background” insulin that helps control blood sugar levels in between meals. A mealtime insulin is needed to control spikes in blood sugar that occur after eating.
What is lantus used for?
Lantus is a brand-name prescription medication. It’s used to improve blood sugar levels in : adults and children ages 6 years and older with type 1 diabetes. adults with type 2 diabetes. For more information about type 1 and type 2 diabetes and how Lantus is used to manage these conditions, see the “ Lantus uses ” section below.
What are some ways to improve blood sugar levels in type 1 diabetes?
Examples of other insulins that may be used to improve blood sugar levels in people with type 1 or type 2 diabetes include: long-acting insulins, which help improve blood sugar levels for about 24 hours: insulin glargine (Basaglar, Toujeo)
How much weight can you gain with Lantus?
Weight gain is one of the most common side effects of Lantus. In clinical studies, the average weight gain was: up to 1.5 pounds (lb) in adults with type 1 diabetes who took Lantus over 16 to 28 weeks. up to 4.8 lb in children with type 1 diabetes who took Lantus and regular insulin for 28 weeks.
What is lantus injection?
LANTUS (insulin glargine injection) is a sterile solution of insulin glargine for subcutaneous use. Insulin glargine is a recombinant human insulin analog that is a long-acting, parenteral blood-glucose-lowering agent [see CLINICAL PHARMACOLOGY ]. Insulin glargine has low aqueous solubility at neutral pH. At pH 4 insulin glargine is completely soluble. After injection into the subcutaneous tissue, the acidic solution is neutralized, leading to formation of microprecipitates from which small amounts of insulin glargine are slowly released, resulting in a relatively constant concentration/time profile over 24 hours with no pronounced peak. This profile allows once-daily dosing as a basal insulin. LANTUS is produced by recombinant DNA technology utilizing a non- pathogenic laboratory strain of Escherichia coli (K12) as the production organism. Insulin glargine differs from human insulin in that the amino acid asparagine at position A21 is replaced by glycine and two arginines are added to the C-terminus of the B-chain. Chemically, insulin glargine is 21 A - Gly -30 B a-L-Arg-30 B b-L-Arg-human insulin and has the empirical formula C267H404N72O78S6 and a molecular weight of 6063. Insulin glargine has the following structural formula:
How long does insulin glargine stay in the body?
After injection into the subcutaneous tissue, the acidic solution is neutralized, leading to formation of microprecipitates from which small amounts of insulin glargine are slowly released, resulting in a relatively constant concentration/time profile over 24 hours with no pronounced peak.
How many times does insulin glargine affect rabbits?
Rats and rabbits were exposed to insulin glargine in animal reproduction studies during organogenesis, respectively 50 times and 10 times the human subcutaneous dose of 0.2 units/kg/day. Overall, the effects of insulin glargine did not generally differ from those observed with regular human insulin (see Data ).
How long does it take for insulin to work?
The median time between injection and the end of pharmacological effect was 14.5 hours (range: 9.5 to 19.3 hours) for NPH insulin, and 24 hours (range: 10.8 to >24.0 hours) (24 hours was the end of the observation period) for insulin glargine.
How to get insulin out of a vial?
If bubbles are in the syringe, hold the syringe straight up and tap the side of the syringe until the bubbles float to the top. Push the bubbles out with the plunger and draw insulin back in until you have the correct dose.
Where is insulin glargine metabolized?
A metabolism study in humans indicates that insulin glargine is partly metabolized at the carboxyl terminus of the B chain in the subcutaneous depot to form two active metabolites with in vitro activity similar to that of human insulin, M1 (21 A -Gly-insulin) and M2 (21 A -Gly-des30 B -Thr-insulin). Unchanged drug and these degradation products are also present in the circulation.
Can you take Lantus with insulin?
Type 1 Diabetes. In patients with type 1 diabetes, LANTUS must be used concomitantly with short-acting insulin. The recommended starting dose of LANTUS in patients with type 1 diabetes should be approximately one-third of the total daily insulin requirements.
What is a lantus injection?
LANTUS® (insulin glargine) Injection DESCRIPTION LANTUS (insulin glargine injection) is a sterile solution of insulin glargine for subcutaneous use . Insulin glargine is a recombinant human insulin analog that is a long-acting, parenteral blood-glucose-lowering agent [see CLINICAL PHARMACOLOGY]. Insulin glargine has low aqueous solubility at neutral pH. At pH 4 insulin glargine is completely soluble. After injection into the subcutaneous tissue, the acidic solution is neutralized, leading to formation of microprecipitates from which small amounts of insulin glargine are slowly released, resulting in a relatively constant concentration/time profile over 24 hours with no pronounced peak. This profile allows oncedaily dosing as a basal insulin. LANTUS is produced by recombinant DNA technology utilizing a non-pathogenic laboratory strain of Escherichia coli (K12) as the production organism. Insulin glargine differs from human insulin in that the amino acid asparagine at position A21 is replaced by glycine and two arginines are added to the C-terminus of the B-chain. Chemically, insulin glargine is 21A-Gly-30Ba-L-Arg-3030b-L-Arg-human insulin and has the empirical formula C267H404N72O78S6 and a molecular weight of 6063. Insulin glargine has the following structural formula: LANTUS consists of insulin glargine dissolved in a clear aqueous fluid. Each milliliter of LANTUS (insulin glargine injection) contains 100 Units (3.6378 mg) insulin glargine. The 10 mL vial presentation contains the following inactive ingredients per mL: 30 mcg zinc, 2.7 mg m-cresol, 20 mg glycerol 85%, 20 mcg polysorbate 20, and water for injection. The 3 mL prefilled pen presentation contains the following inactive ingredients per mL: 30 mcg zinc, 2.7 mg m-cresol, 20 mg glycerol 85%, and water for inje Continue reading >>
How does insulin glargine work?
It helps diabetic patients regulate glucose or sugar in the body. Insulin glargine works by promoting movement of sugar from blood into body tissues and also stops sugar production in liver. Insulin glargine is man-made insulin that mimics the actions of human insulin. The FDA approved insulin glargine in April 2000.
What happens after insulin injection?
After injection into the subcutaneous tissue, the acidic solution is neutralised, leading to the formation of microprecipitates from which small amounts of insulin glargine are released continuously, yielding a smooth, peakless, predictable concentration/time profile with a prolonged duration of action.
What is the mechanism of action of Lantus?
Lantus Mechanism Of Action. Pharmacotherapeutic Group: Long-acting insulins (A: Insulins and analogues). Pharmacology: Pharmacodynamics: Lantus is an antidiabetic agent, which contains insulin glargine. Insulin glargine is a human insulin analogue designed to have a low solubility at neutral pH.
What is lantus hormone?
Lantus (insulin Glargine) Dose, Indications, Adverse Effects, Interactions... From Pdr.net. Hormone secreted by pancreatic beta-cells of the islets of Langerhans and essential for the metabolism and homeostasis of carbohydrate, fat, and protein.
What are the two active metabolites of insulin?
Insulin glargine is metabolised into 2 active metabolites M1 and M2 (see Pharmacokinetics: Metabolism as follows). Insulin Receptor Binding: In vitro studies indicate that the affinity of insulin glargine and its metabolites M1 and M2 for the human insulin receptor is similar to the 1 of human insulin.
How long does it take for insulin to work?
Their activity gradually falls over the next 3 hours with about 5 to 6 hours of activity being common with these insulins.Although insulin action times are often quoted as 3-5 hours, the actual duration of insulin action is typically 5 hours or more .
What is the largest pharmaceutical export in Germany?
This makes Lantus Germany's largest and most important export pharmaceutical product. Sanofi-Aventis increased its turn-over with Lantus around 28% to €2.45 million, of which €130 million was from Germany, where approximately 1.8 million people with diabetes use the product.
What is the purpose of glycine substitution?
The glycine substitution prevents deamidation of the acid-sensitive asparagine at acidic pH. In the neutral subcutaneous space, higher-order aggregates form, resulting in a slow, peakless dissolution and absorption of insulin from the site of injection. It can achieve a peakless level for at least 24 hours.
How does insulin glargine differ from insulin glargine?
Insulin glargine differs from human insulin by replacing asparagine with glycine in position 21 of the A-chain and by carboxy-terminal extension of B-chain by 2 arginine residues. The arginine amino acids shift the isoelectric point from a pH of 5.4 to 6.7, making the molecule more soluble at an acidic pH and less soluble at physiological pH. The isoelectric shift also allows for the subcutaneous injection of a clear solution. The glycine substitution prevents deamidation of the acid-sensitive asparagine at acidic pH. In the neutral subcutaneous space, higher-order aggregates form, resulting in a slow, peakless dissolution and absorption of insulin from the site of injection. It can achieve a peakless level for at least 24 hours.
What is a lantus?
(what is this?) (verify) Insulin glargine, marketed under the names Lantus among others, is a long-acting insulin, used in the management of type I and type II diabetes. It is typically the recommended long acting insulin in the United Kingdom. It is used once a day as an injection just under the skin.
How long does it take for NPH to release?
NPH insulin rather than insulin glargine is generally preferred in pregnancy. After injection microcrystals slowly release insulin for about 24 hours. This insulin causes body tissues to absorb glucose from the blood and decreases glucose production by the liver.
What is insulin glargine?
This insulin causes body tissues to absorb glucose from the blood and decreases glucose production by the liver. Insulin glargine was approved for medical use in the United States in 2000. In 2018, it was the 26th most commonly prescribed medication in the United States with more than 24 million prescriptions.
When was Lantus first introduced?
On June 9, 2000, the European Commission formally approved the launching of Lantus by Sanofi-Aventis Germany Ltd. in the entire European Union. The admission was prolonged on June 9, 2005. A three-fold more concentrated formulation, brand name "Toujeo", was introduced after FDA approval in 2015.
How is insulin glargine produced?
Insulin glargine is produced by recombinant DNA technology using a non-pathogenic laboratory strain of Escherichia coli (K12) as the production organism. Insulin glargine differs from endogenous human insulin by the replacement of an asparagine residue at position A21 of the A-chain with glycine and addition of two arginines to the C-terminus (positions B31 and 32) of the B-chain. The resulting protein is soluble at pH 4 and forms microprecipitates at physiological pH 7.4 allowing for the slow release of small amounts of insulin glargine, giving the drug a long duration of action and no pronounced peak concentration.
How long does insulin glargine last?
Available as the brand name product Lantus, insulin glargine has a duration of action up to 24 hours allowing for once-daily dosing, typically at bedtime. Due to its duration of action, Lantus is considered "basal insulin" as it provides low concentrations of background insulin that can keep blood sugar stable between meals or overnight. Basal insulin is often combined with short-acting "bolus insulin" such as Insulin lispro, Insulin glulisine, and Insulin aspart to provide higher doses of insulin that are required following meals. Use of basal and bolus insulin together is intended to mimic the pancreas' production of endogenous insulin, with a goal of avoiding any periods of hypoglycemia.
What is glargine used for?
Insulin glargine is a long-acting form of insulin used for the treatment of hyperglycemia caused by Type 1 and Type 2 Diabetes. Insulin is typically prescribed for the management of diabetes mellitus to mimic the activity of endogenously produced human insulin, a peptide hormone produced by beta cells of the pancreas that promotes glucose metabolism. Insulin is released from the pancreas following a meal to promote the uptake of glucose from the blood into internal organs and tissues such as the liver, fat cells, and skeletal muscle. Absorption of glucose into cells allows for its transformation into glycogen or fat for storage. Insulin also inhibits hepatic glucose production, enhances protein synthesis, and inhibits lipolysis and proteolysis.
How long does Basaglar take to work?
The median time to maximum effect of Basaglar (measured by the peak rate of glucose infusion) was approximately 12.0 hours. The pharmacodynamic profile of Basaglar following subcutaneous injection demonstrated sustained glucose lowering activity over 24 hours with no pronounced peak. The mean area under the glucose infusion rate curves (measure of overall pharmacodynamic effect) and maximum glucose infusion rate were 1670 mg/kg and 2.12 mg/kg/min, respectively. On average, serum insulin concentrations declined to baseline by approximately 24 hours.
Where is insulin glargine metabolized?
Insulin glargine is metabolized in the liver into two active metabolites with similar activity to insulin: 21a-Gly-human insulin (M1) and 21a-Gly-des-30b- threonine insulin (M2), with M1 being the predominant metabolite. Hover over products below to view reaction partners. Insulin glargine. list-arrow.
What is the treatment for diabetes mellitus?
Insulin is also used in the treatment of Type 2 Diabetes (T2D), another form of diabetes mellitus that is a slowly progressing metabolic disorder caused by a combination of genetic and lifestyle factors that promote chronically elevated blood sugar levels.
Why is insulin important for diabetes?
Insulin is an important treatment in the management of Type 1 Diabetes (T1D), which is caused by an autoimmune reaction that destroys the beta cells of the pancreas, resulting in the body not being able to produce or synthesize the insulin needed to manage circulating blood sugar levels .
