Linarol

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

Linarol is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP-4 Linarol increases the concentrations of active incretin hormones and stimulates the release of Insulin in a glucose dependent manner and decreases the level of Glucagon in the circulation and thus regulates the glucose homeostasis. Incretin hormones are secreted at a low basal level throughout the day and levels rise immediately after meal intake. GLP-1 and GIP increase Insulin biosynthesis and secretion from pancreatic beta-cells in the presence of elevated blood glucose levels. Furthermore, GLP-1 also reduces Glucagon secretion from pancreatic alpha-cells, resulting in a reduction in hepatic glucose output.

A 5mg oral dose of linagliptin results in >80% inhibition of dipeptidyl peptidase 4 (DPP-4) for ≥24 hours. Inhibition of DPP-4 increases the concentration of glucagon-like peptide 1 (GLP-1), leading to decreased glycosylated hemoglobin and fasting plasma glucose.

Linarol
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	Linarol
Availability	Prescription only
Generic	Linagliptin
Linagliptin Other Names	Linagliptin, Linagliptina
Related Drugs	Farxiga, metformin, Trulicity, Lantus, Victoza, Tresiba, Levemir
Weight	5mg
Type	Tablet
Formula	C₂₅H₂₈N₈O₂
Weight	Average: 472.5422 Monoisotopic: 472.23352218
Protein binding	Linagliptin is 99% protein bound at a concentration of 1nmol/L and 75-89% protein bound at a concentration of >30nmol/L.
Groups	Approved
Therapeutic Class	Dipeptidyl Peptidase-4 (DPP-4) inhibitor
Manufacturer	Drug International Ltd
Available Country	Bangladesh
Last Updated:	September 19, 2023 at 7:00 am

Uses

Linarol is used for an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Linarol may be used as monotherapy or in combination with other common antidiabetic medications including Metformin, Sulfonylurea, Pioglitazone, or Insulin. As a replacement therapy it is suitable when Metformin therapy is not appropriate due to intolerance or do not provide adequate glycemic control as monotherapy or other antidiabetic drugs are to be discontinued due to renal or hepatic impairment.

Linarol is also used to associated treatment for these conditions: Type 2 Diabetes Mellitus

How Linarol works

Linarol is a competitive, reversible DPP-4 inhibitor. Inhibition of this enzyme slows the breakdown of GLP-1 and glucose-dependant insulinotropic polypeptide (GIP). GLP-1 and GIP stimulate the release of insulin from beta cells in the pancreas while inhibiting release of glucagon from pancreatic beta cells. These effects together reduce the breakdown of glycogen in the liver and increase insulin release in response to glucose.

Dosage

Linarol dosage

The recommended dose of Linarol is 5 mg once daily and can be taken with or without food. If added with Metformin, the dose of Metformin should be maintained and Linarol administered concomitantly. When used in combination with Sulfonylurea, a lower dose of Sulfonylurea may be considered to reduce the risk of hypoglycemia.

Pediatric patients: Safety and effectiveness of Linarol in patients below the age of 18 have not been established.

Renal or hepatic impairment: No dose adjustment required.

Side Effects

Treatment with Linarol is well tolerated; some of the less common side effects are nasopharyngitis and hypoglycemia.

Toxicity

No dosage adjustment is necessary based on race, age, weight, sex, renal impairment, or hepatic impairment.

Studies of efficacy and safety in pediatric populations were not included in the original drug approval but recent clinical trials show linagliptin to be well tolerated in patients 10 to 18 years old.

Animal studies showed an increased risk of lymphoma in female rats at over 200 times the clinical dose. Aside from this effect, linagliptin was not shown to be mutagenic, clastogenic, or have an effect on fertility.

Precaution

When used with an Insulin secretagogue (e.g., sulfonylurea) or Insulin, consider lowering the dose of the Insulin secretagogue or Insulin to reduce the risk of hypoglycemia. If pancreatitis is suspected, Linarol should be discontinued. There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with Linarol or any other antidiabetic drug.

Interaction

Linarol doesn't interact with Metformin, Glyburide, Simvastatin, Warfarin, Digoxin or oral contraceptives. Linarol is a weak competitive and a weak to moderate mechanism-based inhibitor of CYP isozyme CYP3A4, but does not inhibit other CYP isozymes. Again it doesn't act as an inducer of CYP isozymes.

Food Interaction

Avoid excessive or chronic alcohol consumption. Chronic or binge drinking can increase the risk of serious side effects.
Take with or without food. High fat meals reduce the maximum concentration and increase the AUC, but not to a clinically significant extent.

[Moderate] GENERALLY AVOID: Alcohol may cause hypoglycemia or hyperglycemia in patients with diabetes.

Hypoglycemia most frequently occurs during acute consumption of alcohol.

Even modest amounts can lower blood sugar significantly, especially when the alcohol is ingested on an empty stomach or following exercise.

The mechanism involves inhibition of both gluconeogenesis as well as the counter-regulatory response to hypoglycemia.

Episodes of hypoglycemia may last for 8 to 12 hours after ethanol ingestion.

By contrast, chronic alcohol abuse can cause impaired glucose tolerance and hyperglycemia.

Moderate alcohol consumption generally does not affect blood glucose levels in patients with well controlled diabetes.

A disulfiram-like reaction (e.g., flushing, headache, and nausea) to alcohol has been reported frequently with the use of chlorpropamide and very rarely with other sulfonylureas.

MANAGEMENT: Patients with diabetes should avoid consuming alcohol if their blood glucose is not well controlled, or if they have hypertriglyceridemia, neuropathy, or pancreatitis.

Patients with well controlled diabetes should limit their alcohol intake to one drink daily for women and two drinks daily for men (1 drink = 5 oz wine, 12 oz beer, or 1.5 oz distilled spirits) in conjunction with their normal meal plan.

Alcohol should not be consumed on an empty stomach or following exercise.

Linarol Drug Interaction

Moderate: insulin glargine, insulin glargine, furosemide, lithiumUnknown: aspirin, aspirin, rosuvastatin, omega-3 polyunsaturated fatty acids, empagliflozin, atorvastatin, pregabalin, metoprolol, esomeprazole, acetaminophen, valproic acid, thiamine, cyanocobalamin, pyridoxine, ascorbic acid, cholecalciferol

Linarol Disease Interaction

Major: pancreatitis

Volume of Distribution

A single intravenous dose of 5mg results in a volume of distribution of 1110L. However an intravenous infusion of 0.5-10mg results in a volume of distribution of 380-1540L.

Elimination Route

Oral bioavailability of linagliptin is 30%.

Half Life

The terminal half life of linagliptin is 155 hours.

Clearance

Total clearance of linagliptin is 374mL/min.

Elimination Route

84.7% of linagliptin is eliminated in the feces and 5.4% is eliminated in the urine.

Pregnancy & Breastfeeding use

Pregnancy: There are no adequate and well-controlled studies in pregnant women. Linarol tablets should be used during pregnancy only if the potential benefit of mother justifies the potential risk of the fetus.

Nursing mothers: Caution should be exercised when Linarol is administered to a nursing woman.