Insulina Glargina

Insulina Glargina Uses, Dosage, Side Effects, Food Interaction and all others data.

Insulin Glargine (rDNA) is a sterile, clear, colourless solution of insulin human. It is a long-acting insulin and has a relatively long duration of action as compared with other insulin. Insulina Glargina have substitution 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.

Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic individuals, the pancreas produces a continuous supply of low levels of basal insulin along with spikes of insulin following meals. Increased insulin secretion following meals is responsible for the metabolic changes that occur as the body transitions from a postabsorptive to absorptive state. Insulin promotes cellular uptake of glucose, particularly in muscle and adipose tissues, promotes energy storage via glycogenesis, opposes catabolism of energy stores, increases DNA replication and protein synthesis by stimulating amino acid uptake by liver, muscle and adipose tissue, and modifies the activity of numerous enzymes involved in glycogen synthesis and glycolysis. Insulin also promotes growth and is required for the actions of growth hormone (e.g. protein synthesis, cell division, DNA synthesis). Insulina Glargina is a long-acting insulin analogue with a flat and predictable action profile. It is used to mimic the basal levels of insulin in diabetic individuals.

Insulina Glargina
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Insulina Glargina
Generic	Insulin glargine
Insulin glargine Other Names	Insulin glargine, Insulin glargine (rDNA origin), Insulin glargine recombinant, Insulina glargina
Type
Formula	C₂₆₇H₄₀₄N₇₂O₇₈S₆
Weight	6063.0 Da
Groups	Approved
Therapeutic Class	Long Acting Insulin
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Insulin Glargine is used for once-daily subcutaneous administration for the treatment of adult and pediatric patients with type 1 diabetes mellitus or adult patients with type 2 diabetes mellitus who require basal (long-acting) insulin for the control of hyperglycemia.

Insulina Glargina is also used to associated treatment for these conditions: Diabetes Mellitus, Type 1 Diabetes Mellitus, Type 2 Diabetes Mellitus

How Insulina Glargina works

Insulina Glargina 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 signalling 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. Insulina Glargina is completely soluble at pH 4, the pH of administered solution, and has low solubility at physiological pH 7.4. Upon subcuteous injection, the solution is neutralized resulting in the formation of microprecipitates. Small amounts of insulin glargine are released from microprecipitates giving the drug a relatively constant concentration over time profile over 24 hours with no pronounced peak. This release mechanism allows the drug to mimic basal insulin levels within the body.

Dosage

Insulina Glargina dosage

The recommended starting dose of Insulin Glargine in patients with type 1 diabetes should be approximately one-third of the total daily insulin requirements. Short-acting, premeal insulin should be used to satisfy the remainder of the daily insulin requirements.

The recommended starting dose of Insulin Glargine in patients with type 2 diabetes who are not currently treated with insulin is 10 units (or 0.2 Units/kg) once daily, which should subsequently be adjusted to the patient’s needs.

The dose of Insulin Glargine should be adjusted according to blood glucose measurements. The dosage of Insulin Glargine should be individualized under the supervision of a healthcare provider in accordance with the needs of the patient.

Do not dilute or mix with any other insulin or solution. Do not administer subcutaneously via an Insuliln pump or intravenously because severe hypoglycemia can occur. Do not share reusable or disposable insulin glargine devices or needles between patients.

Side Effects

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

Toxicity

Inappropriately high dosages relative to food intake and/or energy expenditure may result in severe and sometimes prolonged and life-threatening hypoglycemia. 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. Other adverse events that may occur include allergic reaction, injection site reaction, lipodystrophy, pruritis, and rash.

Precaution

Dose adjustment and monitoring: Monitor blood glucose in all patients. insulin glargine regimens should be modified cautiously and only under medical supervision.

Hypoglycemia: Most common adverse reaction of insulin glargine therapy and may be life threatening.

Allergic reactions: Severe life threatening, generalized allergy, including anaphylaxis can occur.

Renal and hepatic impairment: May require a reduction in insulin glargine dose.

Interaction

The following substances may reduce the Insulin as well as Insulina Glargina requirements: oral anti-diabetic products, angiotensin converting enzyme (ACE) inhibitors, disopyramide, fibrates, fluoxetine, monoamine oxidase inhibitors, propoxyphene, pentoxifylline, salicylates and sulfonamide antibiotics.

The following substances may increase the Insulin as well as Insulina Glargina requirements: Thiazides, glucocorticoids, thyroid hormones, beta-sympathomimetics, growth hormone and danazol. Beta-blockers, clonidine, lithium salts, and alcohol may either potentiate or weaken the blood-glucose-lowering effect of insulin.

Food Interaction

No interactions found.

Elimination Route

Because of the modifications to the A and B chain, the isoelectric point shifts towards a neutral pH and insulin glargine is more stable in acidic conditions than regular insulin. As insulin glargine is less soluble at neutral pH, once injected, forms microprecipitates. Slow release of insulin glargine from microprecipitates provides a relatively constant concentration of insulin over 24 hours. Onset of action is approximately 1.1 hours.

The pharmacokinetic profiles for single 0.4, 0.6, and 0.9 U/kg doses of Toujeo in 24 patients with type 1 diabetes mellitus was evaluated in a euglycemic clamp study. The median time to maximum serum insulin concentration was 12 (8–14), 12 (12–18), and 16 (12–20) hours, respectively. Steady-state insulin concentrations are reached by at least 5 days of once-daily subcutaneous administration of 0.4 U/kg to 0.6 U/kg doses of Toujeo over 8 days in patients with type 1 diabetes mellitus.

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.

Pregnancy & Breastfeeding use

Pregnancy category C. Insulina Glargina should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation: It is unknown whether insulin glargine is excreted in human milk. Because many drugs, including human insulin, are excreted in human milk, caution should be exercised when Insulina Glargina is administered to a nursing woman. Lactating women may require adjustments in insulin dose & diet.

Contraindication

Insulina Glargina is contraindicated in patients with hypersensitivity to insulin glargine or any of its excipients.

Special Warning

Use in Renal/ Hepatic impairment: Reduction in the insulin glargine doses may be required in these cases.

Acute Overdose

Insulina Glargina overdose may result in hypoglycemia. Mild episodes of hypoglycemia can usually be treated with oral carbohydrates. Severe hypoglycemia may be treated with parenteral glucose or injections of glucagon. Adjustments in drug dosage, meal patterns, or exercise may be needed.