Ingliptin

Orange round, biconvex with film coated tablet. One side has letter "S". Another side has figure "100".
Each film-coated tablet contains Sitagliptin phosphate 100 mg.

Pharmacology: Pharmacodynamics: Mechanism of action: Sitagliptin inhibits dipeptidyl peptidase IV (DPP-IV) enzyme resulting in prolonged active incretin levels. Incretin hormones (eg. glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP)) regulate glucose homeostasis by increasing insulin synthesis and release from pancreatic beta cells and decreasing glucagon secretion results in decreased hepatic glucose production. Under normal physiologic circumstances, incretin hormones are released by the intestine throughout the day and levels are increased in response to a meal; incretin hormones are rapidly inactivated by the DPP-IV enzyme.
Pharmacokinetics: Absorption: Rapid.
Distribution: ~198 L.
Protein-binding: 38%.
Metabolism: CYP3A4 and 2C8.
Bioavailability: ~87%.
Half-life elimination: 12.4 hours.
Time to peak: 1-4 hours.
Excretion: Urine 87% (~79% as unchanged drug, 16% as metabolites); feces 13%.

Sitagliptin phosphate is indicated for the treatment of type 2 diabetes mellitus as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus (noninsulin dependent) as monotherapy or combination therapy.

Recommended Dose: Adult: Usual dosage: 1 tablet once daily.
Concomitant therapy: When Sitagliptin phosphate is used in combination with an insulin secretagogue (eg. sulfonylurea) or with insulin, a Sitagliptin dosage of 100 mg once daily has been used. A lower dose of insulin secretagogue or insulin may be required to reduce the risk of hypoglycemia. When Sitagliptin phosphate is used in combination with a thiazolidinedione antidiabetic agent (eg. pioglitazone, rosiglitazone) with or without metformin, a Sitagliptin dosage of 100 mg once daily has been used.
Renal impairment: Dosage adjustment is recommended for patients with moderate or severe renal impairment or end-stage renal disease requiring hemodialysis or peritoneal dialysis.
Patients with moderate renal impairment (creatinine clearance of 30 to less than 50 ml/minute), the recommended dosage of Sitagliptin is 50 mg once daily.
Patients with severe renal impairment (creatinine clearance less than 30 ml/minute), the recommended dosage of Sitagliptin is 25 mg once daily.
Patients with end-stage renal disease requiring hemodialysis or peritoneal dialysis should receive a dosage of 25 mg once daily. Sitagliptin phosphate may be administered without regard to the timing of dialysis.
Mode of Administration: Sitagliptin phosphate should be administered orally once daily with or without food.

Overdose and Treatment: In the event of an overdose, it is reasonable to employ the usual supportive, eg. remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy if required.

Sitagliptin phosphate is contraindicated in patients with known serious hypersensitivity (eg. anaphylaxis, angioedema) to Sitagliptin phosphate or to any ingredient in the formulation.

Acute pancreatitis, including fatal and nonfatal hemorrhagic and necrotizing pancreatitis, has been reported; monitoring recommended and discontinue therapy if signs or symptoms develop.
Heart failure may occur; monitoring recommended and consider discontinuation.
Sitagliptin phosphate is not indicated for use in patients with type 1 diabetes mellitus.
Sitagliptin phosphate is not indicated for the treatment of diabetes ketoacidosis.
Severe and disabling arthralgia has been reported with DPP-IV inhibitor use; onset may occur within 1 day to years after treatment initiation and may resolve with discontinuation of therapy. Some patients may experience a recurrence of symptoms if DPP-IV inhibitor therapy resumed.
Serious hypersensitivity and allergic reactions such as angioedema, anaphylaxis and Stevens-Johnson syndrome have been reported, particularly within first 3 months of treatment.
Sitagliptin phosphate requires a dosage adjustment in patients with moderate or severe renal insufficiency and in patients with ESRD requiring hemodialysis or peritoneal dialysis. There have been reports of worsening renal function and acute renal failure requiring dialysis in patients treated with Sitagliptin phosphate.
Bullous pemphigoid has been reported with dipeptidyl peptidase-4 inhibitors; if blisters or erosions develop during treatment and bullous pemphigoid is suspected, discontinue treatment and medically manage.

Pregnancy: Pregnancy category B.
There are no adequate and well-controlled studies in pregnant women; therefore, the safety of Sitagliptin phosphate in pregnant women is not known. Sitagliptin phosphate, like other oral antihyperglycemic agents, is not recommended for use in pregnancy.
Lactation: Sitagliptin phosphate is secreted in the milk of lactating rats. It is not known whether Sitagliptin phosphate is secreted in human milk. Therefore, Sitagliptin phosphate should not be used by a woman who is nursing.

Endocrine & metabolic: hypoglycemia.
Gastrointestinal: diarrhea, nausea.
Renal: increased serum creatinine.
Respiratory: nasopharyngitis.
Rare but important or life-threatening: acute pancreatitis (including hemorrhagic or necrotizing forms), acute renal failure (possibly requiring dialysis), anaphylaxis, angioedema, arthralgia, back pain, bullous pemphigoid, constipation, exfoliative dermatitis, headache, hypersensitivity, hypersensitivity vasculitis, increased liver enzymes, limb pain, myalgia, oral mucosa ulcer, pain, pemphigoid, pruritus, renal insufficiency, severe arthralgia, skin rash (including macular), Stevens-Johnson syndrome, stomatitis, urticaria, vomiting.

Sitagliptin phosphate may increase the levels/effects of Angiotensin-Converting Enzyme Inhibitors, Digoxin, Hypoglycemia-Associated Agents, Insulins, Sulfonylureas.
The levels/effects of Sitagliptin phosphate may be increased by Alpha-Lipoic Acid, Androgens, Guanethidine, Lumacaftor, Monoamine Oxidase Inhibitors, Pegvisomant, P-glycoprotein/ABCB1 Inhibitors, Prothioamide, Quinolones, Ranolazine, Salicylates, Selective Serotonin Reuptake Inhibitors.
The levels/effects of Sitagliptin phosphate may be decreased by Hyperglycemia-Associated Agents, Lumacaftor, P-glycoprotein/ABCB1 inducers, Quinolones, Thiazide and Thiazide-Like Diuretics.

Do not store above 30°C.

Antidiabetic Agents

A10BH01 - sitagliptin ; Belongs to the class of dipeptidyl peptidase 4 (DPP-4) inhibitors. Used in the treatment of diabetes.

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