Neoglip (metformin + sitagliptin): Uses, Dosage & Side Effects

What it's for (Indications)

Indicated for the treatment of Type II diabetes mellitus (maturity-onset diabetes), either as monotherapy or in combination with sulfonylureas.
It can also be used as adjuvant therapy in insulin-dependent diabetes, particularly in obese patients.

Dosage Information

Type	Guideline
Standard	Take sitagliptin and metformin hydrochloride extended-release tablets orally once daily with a meal. Patients taking two tablets should take them together. Individualize the dosage based on the patient's current regimen, effectiveness, and tolerability. The maximum recommended daily dose is 100 mg of sitagliptin and 2,000 mg of metformin hydrochloride extended-release. For patients not currently treated with metformin, the recommended starting dose is 100 mg sitagliptin and 1,000 mg metformin hydrochloride once daily, with gradual dose escalation recommended to reduce gastrointestinal side effects. For patients already treated with metformin, the starting dose should provide sitagliptin dosed as 100 mg and the dose of metformin already being taken once daily.

Type

Guideline

Standard

Take sitagliptin and metformin hydrochloride extended-release tablets orally once daily with a meal. Patients taking two tablets should take them together. Individualize the dosage based on the patient's current regimen, effectiveness, and tolerability. The maximum recommended daily dose is 100 mg of sitagliptin and 2,000 mg of metformin hydrochloride extended-release. For patients not currently treated with metformin, the recommended starting dose is 100 mg sitagliptin and 1,000 mg metformin hydrochloride once daily, with gradual dose escalation recommended to reduce gastrointestinal side effects. For patients already treated with metformin, the starting dose should provide sitagliptin dosed as 100 mg and the dose of metformin already being taken once daily.

Safety & Warnings

Common Side Effects

Common side effects include gastrointestinal upset (such as diarrhea, abdominal pain), taste disturbance, upper respiratory tract infection, and headache.
Other reported adverse reactions include abnormal liver function tests, hepatitis, skin reactions, reduced Vitamin B12 absorption, pancreatitis, heart failure, acute renal failure, hypoglycemia (especially with concomitant use of insulin or insulin secretagogues), and severe and disabling arthralgia.
Serious hypersensitivity reactions, including anaphylaxis, angioedema, and bullous pemphigoid, have been reported.
Lactic acidosis, though rare, is a severe and potentially fatal side effect.

Serious Warnings

Black Box Warning: WARNING: LACTIC ACIDOSIS Postmarketing cases of metformin-associated lactic acidosis have resulted in death, hypothermia, hypotension, and resistant bradyarrhythmias. The onset of metformin-associated lactic acidosis is often subtle, accompanied only by nonspecific symptoms such as malaise, myalgias, respiratory distress, somnolence, and abdominal pain. Metformin-associated lactic acidosis was characterized by elevated blood lactate levels (>5 mmol/Liter), anion gap acidosis (witho
**Lactic Acidosis:** This medicine carries a Boxed Warning for lactic acidosis (see Black Box Warning).
Assess risk factors for lactic acidosis, and discontinue immediately if metabolic acidosis is suspected.
Avoid excess alcohol consumption as it may increase the risk of lactic acidosis.
**Renal Impairment:** Use with caution in kidney patients; proper dose adjustment is required.
Monitor renal (kidney) function at least annually.
The medicine is contraindicated in severe renal impairment (eGFR below 30 mL/min/1.
73 m2).
Acute renal failure has been reported.
**Hepatic Impairment:** Use with caution in liver patients; proper dose adjustment is required.
Abnormal liver function tests and hepatitis have been reported.
**Pregnancy and Lactation:** Not recommended during pregnancy or for nursing females.
Consult a doctor for more information.
**Hypersensitivity Reactions:** Serious hypersensitivity reactions, including anaphylaxis, angioedema, and bullous pemphigoid, have been reported.
Discontinue if such reactions occur.
**Pancreatitis:** Cases of pancreatitis have been reported.
**Heart Failure:** Cases of heart failure have been reported.
**Vitamin B12 Deficiency:** Reduced Vitamin B12 absorption can occur.
**Hypoglycemia:** Increased risk of hypoglycemia when used concomitantly with insulin or insulin secretagogues.
**Elective Surgery:** Discontinue the medicine for 48 hours before and after elective surgery.
**Driving:** This medicine does not usually affect driving ability.
However, if experiencing trouble, please avoid driving and consult your doctor.
**Severe and Disabling Arthralgia:** Cases of severe and disabling joint pain have been reported.

How it Works (Mechanism of Action)

Sitagliptin and metformin hydrochloride extended-release tablets combine two antihyperglycemic agents: sitagliptin and metformin extended-release. Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. Concentrations of the active intact hormones are increased by sitagliptin, thereby increasing and prolonging the action of these hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. These hormones are rapidly inactivated by the enzyme DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells, and GLP-1 also decreases glucagon secretion from pancreatic alpha cells. This glucose-dependent mechanism leads to lower blood glucose levels. The mechanism of action for metformin primarily involves decreasing hepatic glucose production, decreasing intestinal absorption of glucose, and improving insulin sensitivity by increasing peripheral glucose uptake and utilization.