Reglutide SC Injection 1.34 mg/ml

Uses

Reglutide SC Injection 1.34 mg/ml is a glucagon-like peptide 1 receptor agonist used to improve glycemic control in type 2 diabetes mellitus.

Reglutide SC Injection 1.34 mg/ml is indicated to improve glycemic control in adults diagnosed with type 2 diabetes mellitus, and is used as an adjunct to diet and exercise. However, semaglutide is not a suitable first-line drug for diabetes that has not been controlled by diet and exercise. In addition, it has not been studied in patients with pancreatitis. Reglutide SC Injection 1.34 mg/ml is not intended for use in patients with type 1 diabetes or to treat diabetic ketoacidosis.

Reglutide SC Injection 1.34 mg/ml is indicated for chronic weight management in adults with obesity or overweight with at least one weight-related condition (such as high blood pressure, type 2 diabetes, or high cholesterol), for use in addition to a reduced-calorie diet and increased physical activity.

Reglutide SC Injection 1.34 mg/ml is also used to associated treatment for these conditions: BMI >27 kg/m2, BMI >30 kg/m2, Type 2 Diabetes Mellitus, Chronic Weight Management

How Reglutide SC Injection 1.34 mg/ml works

Mechanism of glycemic control

GLP-1 is a physiological hormone that promotes glycemic control via several different mechanisms, including insulin secretion, slowing gastric emptying, and reducing postprandial glucagon secretion. The homeostasis of glucose is dependent on hormones such as insulin and amylin, which are secreted by the beta cells of the pancreas. Reglutide SC Injection 1.34 mg/ml is 94% similar to human GLP-1. Analogs of this hormone such as semaglutide stimulate the synthesis of insulin by stimulating pancreatic islet cells and reducing glucagon secretion. They directly bind with selectivity to the GLP-1 receptor, causing various beneficial downstream effects that reduce blood glucose in a glucose-dependent fashion.

Mechanism of cardiovascular benefit and weight loss

In hypercholesterolemia, semaglutide is believed to reduce the progression of atherosclerosis via decreased gut permeability and decreased inflammation. Weight loss is believed to occur via the reduction of appetite and food cravings after semaglutide administration.

Toxicity

Overdoses of up to 4 mg in one ingestion have been reported, with nausea being the most commonly reported symptom. All patients in clinical trials who experienced an overdose recovered fully. Appropriate supportive care should be given according and dictated by the patient's condition. Prolonged observation and treatment may be required, as the half-life of this drug is about one week. There is no antidote to an overdose with semaglutide.

Food Interaction

• Take on an empty stomach. For oral use of semaglutide, take 30 minutes before the first meal of the day.
• Take with plain water. For oral use of semaglutide, do not exceed 4 ounces of water (1/2 cup).

[Moderate] MONITOR: Glucagon-like peptide-1 (GLP-1) receptor agonists and dual GLP-1 and glucose-dependent insulinotropic polypeptide (GIP) receptor agonists delay gastric emptying, which may impact the absorption of concomitantly administered oral medications.

Mild to moderate decreases in plasma concentrations of coadministered drugs have been demonstrated in pharmacokinetic studies for some GLP-1 receptor agonists (e.g., exenatide, lixisenatide), but not others.

The impact of dual GLP-1 and GIP receptor agonist tirzepatide on gastric emptying was reported to be greatest after a single dose of 5 mg but diminished after subsequent doses.

According to the prescribing information, liraglutide did not affect the absorption of several orally administered drugs to any clinically significant extent, including acetaminophen, atorvastatin, digoxin, griseofulvin, lisinopril, and an oral contraceptive containing ethinyl estradiol-levonorgestrel.

Likewise, no clinically relevant effect on absorption was observed for concomitantly administered oral drugs studied with albiglutide (digoxin, ethinyl estradiol-norethindrone, simvastatin, warfarin), dulaglutide (acetaminophen, atorvastatin, digoxin, ethinyl estradiol-norelgestromin, lisinopril, metformin, metoprolol, sitagliptin, warfarin), or semaglutide (atorvastatin, digoxin, ethinyl estradiol-levonorgestrel, metformin, warfarin).

In addition, coadministration of acetaminophen after a first dose of tirzepatide 5 mg reduced the acetaminophen peak plasma concentration (Cmax) by 50% and delayed its median time to peak plasma concentration (Tmax) by 1 hour, but no significant impact on Cmax and Tmax was observed after coadministration at week 4, and the overall exposure of acetaminophen was unaffected.

Nevertheless, potential clinical impact on other oral medications cannot be ruled out, particularly those with a narrow therapeutic index or low bioavailability, those that depend on threshold concentrations for efficacy (e.g., antibiotics), and those that require rapid gastrointestinal absorption (e.g., hypnotics, analgesics).
br> MANAGEMENT: Pharmacologic response to concomitantly administered oral medications should be monitored more closely following the initiation or discontinuation of treatment with a GLP-1 receptor agonist or a dual GLP-1 and GIP receptor agonist.

Reglutide SC Injection 1.34 mg/ml Alcohol interaction

[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.

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.

Reglutide SC Injection 1.34 mg/ml Drug Interaction

Moderate: insulin glargine, albuterolUnknown: aspirin, aspirin, diphenhydramine, ubiquinone, rosuvastatin, duloxetine, empagliflozin, escitalopram, atorvastatin, pregabalin, metoprolol, metoprolol, cyanocobalamin, ascorbic acid, cholecalciferol, alprazolam, zinc sulfate, cetirizine

Reglutide SC Injection 1.34 mg/ml Disease Interaction

Major: suicidal behavior and ideation, thyroid cancerModerate: GI adverse events, hypoglycemia, pancreatitis, retinopathy

Volume of Distribution

The volume of distribution of semaglutide is 8L to 9.4L. It crosses the placenta in rats.

Elimination Route

The Cmax of semaglutide was 10.9 nmol/L, with AUC of 3123.4 nmol h/L and a Tmax of 56 h in one clinical trial, achieved within 1-3 days. The absolute bioavailability is 89%. Steady-state concentration of the oral tablet is achieved in 4-5 weeks. Average steady state concentrations of semaglutide are the mean steady state concentrations after dosing at 0.5mg to 1mg range from 16 nmol/L to 30 nmol/L.

Half Life

One of the major properties of semaglutide is its long half-life of 168 h. The long half-life is attributed to its albumin binding. This lowers the renal clearance and protects semaglutide from metabolic breakdown.

Clearance

The clearance rate of semaglutide is 0.039 L/h according to one clinical study. On the FDA label, semaglutide clearance is reported to be about 0.05 L/h in patients with type 2 diabetes mellitus.

Elimination Route

This drug is mainly cleared by the kidneys, and is found excreted in both the urine and feces. The main elimination route is the urine by corresponding to 53% of an ingested radiolabeled dose, with 18.6% found in the feces. A smaller amount of 3.2% was found to be exhaled. Hepatic impairment does not appear to affect the clearance of this drug and dose adjustments are not required in patients with decreased liver function.

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