Jimvia

JIMVIA 50: Orange, round, biconvex film coated tablet with engraved 50 on one side and plain on the other.
Each film coated tablet contains Sitagliptin phosphate monohydrate 64.25 mg eq. to Sitagliptin 50 mg.
JIMVIA 100: Orange, round, biconvex film coated tablet with engraved 100 on one side and plain on the other.
Each film coated tablet contains Sitagliptin phosphate monohydrate 128.50 mg eq. to Sitagliptin 100 mg.

Pharmacology: Pharmacodynamics: Sitagliptin is a dipeptidyl peptidase IV (DPP-IV) inhibitor.
Sitagliptin inhibit dipeptidyl peptidase IV (DPP-IV) enzyme resulting in prolonged active incretin levels.
lncretin 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 from pancreatic alpha cells. Decrease 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: Not exclusively metabolized, minor metabolism via CYP3A4 and 2C8 to metabolites (inactive).
Bioavailability: ~87%.
Half-life elimination: 12.4 hours.
Time to peak, plasma: 1 to 4 hours.
Excretion: Urine 87% (~79% as unchanged drug, 16% as metabolites).
Feces 13%.

Monotherapy: SITAGLIPTIN is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus.
Combination with Metformin: SITAGLIPTIN is indicated in patients with type 2 diabetes mellitus to improve glycemic control in combination with metformin as initial therapy or when the single agent alone, with diet and exercise, does not provide adequate glycemic control.
Combination with Sulfonylurea: SITAGLIPTIN is indicated in patients with type 2 diabetes mellitus to improve glycemic control in combination with a sulfonylurea when treatment with the single agent alone, with diet and exercise, does not provide adequate glycemic control.
Combination with PPARy agonist: SITAGLIPTIN is indicated in patients with type 2 diabetes mellitus to improve glycemic control in combination with a PPARy agonist (i.e., thiazolidinediones) as initial therapy or when the single agent alone, with diet and exercise, does not provide adequate glycemic control.
Combination with Metformin and a sulfonylurea: SITAGLIPTIN is indicated in patients with type 2 diabetes mellitus to improve glycemic control in combination with metformin and a Sulfonylurea when dual therapy with these agents, with diet and exercise, does not provide adequate glycemic control.
Combination with Metformin and PPARy agonist: SITAGLIPTIN is indicated in patients with type 2 diabetes mellitus to improve glycemic control in combination with metformin and a PPARy agonist (i.e., thiazolidinediones) when dual therapy with these agents, with diet and exercise, does not provide adequate glycemic control.
Combination with Insulin: SITAGLIPTIN is indicated in patients with type 2 diabetes mellitus as an adjunct to diet and exercise to improve glycemic control in combination with insulin (with or without metformin).

Administer without regard to meals.
100 mg once daily as monotherapy or as combination therapy with metformin, a sulfonylurea, insulin (with or without metformin), a PPARy agonist (i.e., thiazolidinediones), metformin plus a sulfonylurea, or metformin plus a PPARy agonist.
When SITAGLIPTIN is used in combination with a sulfonylurea or with insulin, a lower dose of sulfonylurea or insulin may be considered to reduce the risk of sulfonylurea or insulin-induced hypoglycemia.
Dosage adjustment: Renal Impairment: Because there is a dosage adjustment based upon renal function, assessment of renal function is recommended prior to initiation of SITAGLIPTIN and periodically thereafter.
For patients with mild renal impairment (estimated glomerular filtration rate (eGFR) ≥60 ml/min/1.73 m² to <90 ml/min/1.73 m²), no dosage adjustment for SITAGLIPTIN is required.
For patients with moderate renal impairment (eGFR ≥45 ml/min/1.73 m² to <60 ml/min/1.73 m²), no dosage adjustment for SITAGLIPTIN is required.
For patients with moderate renal impairment (eGFR ≥30 ml/min/1.73 m² to <45 ml/min/1.73 m²), the dose of SITAGLIPTIN is 50 mg once daily.
For patients with severe renal impairment (eGFR ≥15 ml/min/1.73 m² to <30 ml/min/1.73 m²) or with end-stage renal disease (ESRD) (eGFR <15 ml/min/1.73 m²), including those requiring hemodialysis or peritoneal dialysis, the dose of SITAGLIPTIN is 25 mg once daily. SITAGLIPTIN may be administered without regard to the timing of dialysis.
Hepatic Impairment: Mild to moderate impairment (Child-Pugh classes A and B): No dosage adjustment necessary.
Severe impairment (Child-Pugh class C) has not been studied.

Overdose is uncommon.
Mild to moderate toxicity: Limited data.
Severe toxicity: Has not been reported.
Treatment is symptomatic and supportive. Monitor serial blood glucose concentration. Monitor for symptoms of hypoglycemia.

Serious hypersensitivity to sitagliptin or any component of the formulation.

Based on announcement of Ministry of Public Health: Do not use in patient with known hypersensitivity to this medicine.
Do not use in type 1 diabetes treatment, patients with ketoacidosis, severe infection or serious accident.
Avoid to use in pregnancy and lactation.
Should not use concomitantly with alcohol.
This drug may increase risk of severe joint pain.

Avoid use in type 1 diabetes mellitus (insulin dependent) and diabetic ketoacidosis due to lack of efficacy in those populations.
Worsening renal function, including acute renal failure, sometimes requiring dialysis has been reported.
Severe and disabling arthralgia has been reported with DPP-IV inhibitor use, onset may occur within one day to years after treatment initiation and may resolve with discontinuation of therapy.
Serious hypersensitivity reactions, including anaphylaxis, angioedema, and exfoliative skin reactions such as Stevens-Johnson syndrome, have been reported; discontinue if signs/symptoms of hypersensitivity reaction occur.
Case of acute pancreatitis (including hemorrhagic and necrotizing with some fatalities) have been reported with use; monitor for signs/symptoms of pancreatitis. (Severe and prolonged stomach pain) Discontinue use immediately if pancreatitis is suspected and initial appropriate management.
Use in Children: Safety and effectiveness of Sitagliptin in pediatric patients under 18 years have not been established.
Use in the Elderly: In clinical studies, the safety and effectiveness of Sitagliptin in the elderly (≥65 years) were comparable to those seen in younger patients (<65 years). No dosage adjustment is required based on age. Elderly patients are more likely to have renal impairment; as with other patients, dosage adjustment may be required in the presence of significant renal impairment (see Dosage & Administration).

Sitagliptin was not teratogenic in rats at oral doses up to 250 mg/kg or in rabbits given up to 125 mg/kg during organogenesis (up to 32 and 22 times, respectively, the human exposure based on the recommended daily adult human dose of 100 mg/day). In rats, a slight increase in the incidence of fetal rib malformations (absent, hypoplastic and wavy ribs) was observed at oral doses of 1000 mg/kg/day (approximately 100 times the human exposure bases on the recommended daily adult human dose of 100 mg/day). Slight decrease in mean preweaning body weight of both sexes and postweaning body weight gains of males were observed in the offering of rats given oral dose of  1000 mg/kg/day. However, animal reproduction studies are not always predictive of the human response.
There are no adequate and well-controlled studies in pregnant; therefore, the safety of sitagliptin in pregnant women is not known. Sitagliptin, like other oral antihyperglycemic agents, is not recommended for use in pregnancy.
It is not known if sitagliptin is excreted in breast milk. Caution should be exercised when administering sitagliptin to breast-feeding women.

Reported with monotherapy: Cardiovascular: Peripheral edema.
Endocrine & metabolic: Hypoglycemia.
Gastrointestinal: Constipation, diarrhea, nausea.
Neuromuscular & skeletal: Osteoarthritis.
Respiratory: Nasopharyngitis, pharyngitis, upper respiratory tract infection (viral).
Rare but important or life-threatening: Acne rosacea, acute pancreatitis (including hemorrhagic and necrotizing with some fatalities), acute renal failure (possibly requiring dialysis), anaphylaxis, anemia, bundle branch block, depression, erectile dysfunction, exfoliative dermatitis, gastritis (Helicobacter), gastroesophageal reflux disease, hypertension, hypersensitivity, hypersensitivity vasculitis, hypotension, increased liver enzymes, liver steatosis, migraine, orthostatic hypotension, pemphigoid, peripheral neuropathy, renal insufficiency, severe arthralgia, Stevens-Johnson syndrome.

Sitagliptin is a substrate of P-glycoprotein.
There are no known interactions where it is recommended to avoid concomitant use.
Concurrent use of sitagliptin and insulin secretagogues may result in increased risk of hypoglycemia.
Concurrent use of sitagliptin and digoxin may result in increased digoxin exposure and plasma concentration.
Concurrent use of antidiabetic agents and somatostatin analogues may result in impaired glucose regulation.
Concurrent use of antidiabetic agents and fluoroquinolones may result in changes in blood glucose and increased risk of hypoglycemia or hyperglycemia.
Concurrent use of antidiabetic agents and thioctic acid may result in increased risk of hypoglycemia.
Concurrent use of antidiabetic agents and beta-adrenergic blockers may result in hypoglycemia or hyperglycemia; decreased symptoms of hypoglycemia.
Concurrent use of antidiabetic agents and insulin or pramlintide may result in increased risk of hypoglycemia.
Concurrent use of antidiabetic agents and selected diuretics may result in increased hyperglycemia risk; increased insulin requirement.
Concurrent use of antidiabetic agents and ACE inhibitors may result in increased hypoglycemia risk.

Store below 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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