A human GLP-1 receptor agonist.

A human GLP-1 receptor agonist with 90% amino acid sequence homology to endogenous human GLP-1.

Activates the GLP-1 receptor, a membrane-bound cell-surface receptor coupled to adenylyl cyclase in pancreatic beta cells.

Increases intracellular cyclic AMP (cAMP) in beta cells leading to glucose-dependent insulin release.

Decreases glucagon secretion and slows gastric emptying.

Dulaglutide injection, for subcutaneous use.

Brand Name: Trulicity

In male and female rats, dulaglutide causes a dose-related and treatment-duration-dependent increase in the incidence of thyroid C-cell tumors.

It is unknown whether TRULICITY causes thyroid C-cell tumors, including medullary thyroid carcinoma (MTC), in humans

Contraindicated in patients with a personal or family history of MTC and in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2).

A fusion protein that consists of 2 identical, disulfide-linked chains, each containing an N-terminal GLP-1 analog sequence covalently linked to the Fc portion of a modified human immunoglobulin G4 (IgG4) heavy chain by a small peptide linker and is produced using mammalian cell culture.

A clear, colorless, sterile solution.

Each 0.5 mL solution contains 0.75 mg or 1.5 mg of dulaglutide.

Each single-dose pen or prefilled syringe contains 0.5 mL of solution.

Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

It is not recommended as a first-line therapy for patients who have inadequate glycemic control on diet and exercise because of the uncertain relevance of rodent C-cell tumor findings to humans.

Conside other antidiabetic therapies in patients with a history of pancreatitis.

Not to be used in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis.

It is not a substitute for insulin.

Use is not recommended in patients with pre-existing severe gastrointestinal disease.

Its concurrent use with basal insulin has not been studied.

The recommended initiating dose is 0.75 mg once weekly.

The dose may be increased to 1.5 mg once weekly for additional glycemic control.

The maximum recommended dose is 1.5 mg once weekly.

Administered once weekly, any time of day, with or without food.

Injected subcutaneously in the abdomen, thigh, or upper arm.

When initiating this drug, reducing the dosage of concomitantly administered insulin secretagogues or insulin to reduce the risk of hypoglycemia

No dose adjustment is needed in patients with renal impairment including end-stage renal disease (ESRD).

It is acceptable to inject the drug and insulin in the same body region but the injections should not be adjacent to each other.

Must not be administered intravenously or intramuscularly.

Dosage forms and strengths:

Injection: 0.75 mg/0.5 mL or solution in a single-dose pen

Injection: 1.5 mg/0.5 mL solution in a single-dose pen

Injection: 0.75 mg/0.5 mL solution in a single-dose prefilled syringe

Injection: 1.5 mg/0.5 mL solution in a single-dose prefilled syringe

Adverse reactions: Nausea, diarrhea, vomiting, abdominal pain, decreased appetite, dyspepsia, and fatigue.

Hypoglycemia is more frequent when used in combination with a sulfonylurea or insulin.

Symptomatic hypoglycemia occurs in 39% and 40% of patients when TRULICITY 0.75 mg and 1.5 mg, respectively, is co-administered with a sulfonylurea.

Severe hypoglycemia occurs in 0% and 0.7% of patients when TRULICITY 0.75 mg and 1.5 mg, respectively, us co-administered with a sulfonylurea.

Documented symptomatic hypoglycemia occurs in 85% and 80% of patients when TRULICITY 0.75 mg and 1.5 mg, respectively, was co-administered with prandial insulin.

Severe hypoglycemia occurs in 2.4% and 3.4% of patients when TRULICITY 0.75 mg and 1.5 mg, respectively, was co-administered with prandial insulin.

Treatment results in a mean increase in heart rate (HR) of 2-4 beats per minute (bpm).

Systemic hypersensitivity adverse reactions sometimes severe (e.g., severe occurred in 0.5% of patients.

Injection-site reactions were reported in 0.5% of treated patients.

Associated with a mean increase from baseline in PR interval of 2-3 milliseconds.

Patients have mean increases from baseline in lipase and/or pancreatic amylase of 14% to 20%.

It slows gastric emptying and thus has the potential to reduce the rate of absorption of concomitantly administered oral medications.

Drug levels of oral medications with a narrow therapeutic index should be adequately monitored when concomitantly administered with dulaglutide .

Use is contraindicated in patients with a personal or family history of MTC or in patients with MEN 2.

After initiation of therapy, patients should be observed for signs and symptoms of pancreatitis, and other antidiabetic therapies should be considered in patients with a history of pancreatitis.

The risk of hypoglycemia is increased when used in combination with insulin secretagogues or insulin.

It may require a lower dose of sulfonylurea or insulin to reduce the risk of hypoglycemia in this setting.

Reports of acute renal failure and worsening of chronic renal failure have occurred.

Each weekly dose can be administered at any time of day, with or without food.

The day of administration can be changed if necessary, as long as the last dose was administered 3 or more days before.

Human relevance of thyroid C-cell tumors in rats is unknown and has not be determined.

Pregnancy Category C

Should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

It is not known whether it is excreted in human milk.

Safety and effectiveness not been established in pediatric patients, and is not recommended for use in pediatric patients younger than 18 years.

There is limited clinical experience in patients with severe renal impairment or ESRD.

It slows gastric emptying.

Overdoses associated with these overdoses are mild or moderate gastrointestinal events and non-severe hypoglycemia.

Lowers fasting glucose and reduces postprandial glucose levels in patients with type 2 diabetes mellitus.

Reduction in fasting and postprandial glucose can be observed after a single dose.

Stimulates glucose-dependent insulin secretion and reduces glucagon secretion.

Gastric emptying delay is largest after the first dose and diminishes with subsequent dosing.

Does not produce QTc prolongation.

Following subcutaneous administration, the time to maximum plasma concentration at steady-state ranges from 24 to 72 hours, with a median of 48 hours.

Site of subcutaneous administration has no statistically significant effect on the exposure to dulaglutide.

The mean bioavailability following subcutaneous administration of single 0.75 mg and 1.5 mg doses is 65% and 47%, respectively.

Degraded into its component amino acids by general protein catabolism pathways.

The elimination half-life of dulaglutide for both doses is approximately 5 days.

Dose adjustment of dulaglutide is it needed based on age, gender, race, ethnicity, body weight, or renal or hepatic impairment.

Dulaglutide systemic exposure was increased by 20, 28, 14 and 12% for mild, moderate, severe, and ESRD renal impairment sub-groups, respectively, compared to subjects with normal renal function.

Dulaglutide systemic exposure decreased by 23, 33 and 21% for mild, moderate and severe hepatic impairment groups, respectively, compared to subjects with normal hepatic function.

It slows gastric emptying and, as a result, may reduce the extent and rate of absorption of orally coadministered medications.

In patients with type 2 diabetes mellitus produced reductions from baseline in HbA1c compared to placebo.

No overall differences in glycemic effectiveness were observed across demographic subgroups: age, gender, race/ethnicity, duration of diabetes.

Use at a once weekly dose of 0. 75 mg or 1.55 mg was superior to placebo in improving glycemic control through 26 weeks among youth with type two diabetes who are being treated with metformin or basal insulin, without an effect on BMI(Arslanian SA).

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