Sita Tablet 50 mg: Each film coated tablet contains: Sitagliptin phosphate monohydrate equivalent to Sitagliptin 50 mg.
Sita Tablet 100 mg: Each film coated tablet contains: Sitagliptin phosphate monohydrate equivalent to Sitagliptin 100 mg.
Sita tablets contain Sitagliptin phosphate, an orally-active, potent, and selective inhibitor of dipeptidyl peptidase 4 (DPP-4) enzymes.
Pharmacology: Pharmacokinetics: After oral administration of a 100-mg dose to healthy subjects, Sitagliptin was rapidly absorbed, with peak plasma concentrations (median Tmax) occurring 1 to 4 hours post-dose. Plasma AUC of Sitagliptin increased in a dose-proportional manner. Plasma AUC of Sitagliptin increased approximately 14% following 100-mg doses at steady-state compared to the first dose. The pharmacokinetics of Sitagliptin were generally similar in healthy subjects and in patients with type 2 diabetes.
Absorption: The absolute bioavailability of Sitagliptin is approximately 87%. Since coadministration of a high-fat meal with Sitagliptin had no effect on the pharmacokinetics, Sitagliptin may be administered with or without food.
Distribution: The mean volume of distribution at steady state following a single 100-mg intravenous dose of Sitagliptin to healthy subjects is approximately 198 litres. The fraction of Sitagliptin reversibly bound to plasma proteins is low (38%).
Elimination: Sitagliptin is eliminated in faeces (13%) or urine (87%) within one week of dosing. The apparent terminal t½ following a 100-mg oral dose of Sitagliptin was approximately 12.4 hours and renal clearance was approximately 350 mL/min.
Special populations: Gender: No dosage adjustment is necessary based on gender.
Elderly: No dosage adjustment is required based on age.
Race: No dosage adjustment is required based on race.
Hepatic Insufficiency: No dosage adjustment for Sitagliptin is necessary for patients with mild or moderate hepatic insufficiency. There is no clinical experience in patients with severe hepatic insufficiency.
Renal Insufficiency: Dosage adjustment is needed in renal insufficiency (see Dosage & Administration).
Pediatric Patients: No studies with Sitagliptin have been performed in paediatric patients.
Body Mass Index (BMI): No dosage adjustment is necessary based on BMI.
Toxicology: Animal Toxicology: Acute Toxicity: The approximate LD50 of Sitagliptin given orally to rats is >3000 mg/kg (maximum dose tested). This dose is equivalent to ≥200 times the human exposure based on the recommended daily adult human dose of 100 mg/day. In mice the approximate oral LD50 of Sitagliptin is 4000 mg/kg. This dose is equivalent to >385 times the human exposure based on recommended daily adult human dose of 100 mg/day.
Carcinogenicity: There was an increased incidence of hepatic adenomas and carcinomas in the high-dose males and hepatic carcinomas in the high-dose females. The clinical significance of these findings for humans is unknown.
Mutagenesis: Sitagliptin was not mutagenic or clastogenic in a battery of genetic toxicology studies, including the Ames bacterial assay (microbial mutagenesis test), Chinese hamster ovary cells (CHO cells) chromosome aberration assay, an in vitro cytogenetics assay using CHO cells, an in vitro rat hepatocyte DNA alkaline elution assay (an assay which measures the compound's ability to induce single strand breaks in DNA), and an in vivo micronucleus assay.
Monotherapy: Sitagliptin is indicated as an adjunct to diet and exercise to improve glycaemic control in patients with type 2 diabetes mellitus.
Combination with Metformin: Sitagliptin is indicated in patients with type 2 diabetes mellitus to improve glycaemic control in combination with metformin as initial therapy or when diet and exercise, plus the single agent do not provide adequate glycaemic control.
Combination with a Sulfonylurea: Sitagliptin is indicated in patients with type 2 diabetes mellitus to improve glycaemic control in combination with a sulfonylurea when treatment with the single agent alone, with diet and exercise, does not provide adequate glycaemic control.
Combination with a PPARγ agonist: Sitagliptin is indicated in patients with type 2 diabetes mellitus to improve glycaemic control in combination with a PPARγ agonist (i.e., thiazolidinediones) as initial therapy or when the single agent alone, with diet and exercise, does not provide adequate glycaemic control.
Combination with Metformin and a Sulfonylurea: Sitagliptin is indicated in patients with type 2 diabetes mellitus to improve glycaemic control in combination with metformin and a sulfonylurea when dual therapy with these agents, with diet and exercise, does not provide adequate glycaemic control.
Combination with Metformin and a PPAγ agonist: Sitagliptin is indicated in patients with type 2 diabetes mellitus to improve glycaemic control in combination with metformin and a PPARγ agonist (i.e., thiazolidinediones) when dual therapy with these agents, with diet and exercise, does not provide adequate glycaemic control.
The recommended dose of Sitagliptin is 100 mg once daily as monotherapy or as combination therapy with metformin, a sulfonylurea, a PPARγ agonist (i.e., thiazolidinediones), metformin plus a sulfonylurea, or metformin plus a PPARγ agonist. Sitagliptin can be taken with or without food. When Sitagliptin is used in combination with a sulfonylurea, a lower dose of sulfonylurea may be considered to reduce the risk of sulfonylurea-induced hypoglycaemia. If a dose of Sitagliptin is missed, it should be taken as soon as the patient remembers. A double dose Sitagliptin should not be taken on the same day.
Patients with Renal Insufficiency: Mild renal insufficiency: For patients with mild renal insufficiency (creatinine clearance [CrCl ≥50 mL/min), no dosage adjustment is required.
Moderate renal insufficiency: For patients with moderate renal insufficiency (CrCl ≥30 to <50 mL/min), the dose of Sitagliptin is 50 mg once daily.
Severe renal insufficiency: For patients with severe renal insufficiency (CrCl <30 mL/min) or with end-stage renal disease (ESRD) requiring haemodialysis or peritoneal dialysis, the dose of Sitagliptin is 25 mg once daily. Sitagliptin may be administered without regard to the timing of haemodialysis. Because there is a dosage adjustment based upon renal function, assessment of renal function is recommended prior to initiation of Sitagliptin and periodically thereafter.
Patients with Hepatic Insufficiency: No dosage adjustment is necessary for patients with mild to moderate hepatic insufficiency.
Sitagliptin has not been studied in patients with severe hepatic insufficiency.
Elderly: No dosage adjustment is necessary for elderly patients.
Paediatric Population: There are no data available on the use of Sitagliptin in patients younger than 18 years of age.
Employ the usual supportive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy if required. Sitagliptin is modestly dialysable. It is not known whether Sitagliptin is dialysable by peritoneal dialysis or not.
Effects on blood pressure: In hypertensive patients on one or more anti-hypertensive medicines (including angiotensin-converting enzyme inhibitors, angiotensin-II antagonists, calcium-channel blockers, beta-blockers and diuretics), co-administration with Sitagliptin was generally well tolerated. In these patients, Sitagliptin had a modest blood pressure lowering effect; 100 mg per day of Sitagliptin reduced 24-hour mean ambulatory systolic blood pressure by approximately 2 mm Hg. Reductions have not been observed in subjects with normal blood pressure.
Cardiac Electrophysiology: At the recommended dose of 100 mg, there was no effect on the QTc interval obtained at the peak plasma concentration.
Sitagliptin is contraindicated in patients who are hypersensitive to any components of this product.
General: Sitagliptin should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.
Pancreatitis: Patients should be informed about characteristic symptom of acute pancreatitis: persistent, severe abdominal pain. Resolution of pancreatitis has been observed after discontinuation of Sitagliptin. If pancreatitis is suspected, Sitagliptin and other potentially suspect medicinal products should be discontinued.
Use in Patients with Renal Insufficiency: Sitagliptin is excreted renally. To achieve plasma concentrations of Sitagliptin similar to those in patients with normal renal function, lower dosages are recommended in patients with moderate and severe renal insufficiency, as well as in ESRD patients requiring haemodialysis or peritoneal dialysis.
Hypoglycaemia in Combination with a Sulfonylurea: As is typical with other anti-hyperglycaemic agents used in combination with a sulfonylurea, when Sitagliptin was used in combination with a sulfonylurea, a medication known to cause hypoglycaemia, the incidence of sulfonylurea-induced hypoglycaemia was increased over that of placebo. Therefore, to reduce the risk of sulfonylurea-induced hypoglycaemia, a lower dose of sulfonylurea may be considered. The use of Sitagliptin in combination with insulin has not been adequately studied.
Hypersensitivity Reactions: There have been reports of serious hypersensitivity reactions in patients treated with Sitagliptin. These reactions include anaphylaxis, angioedema, and exfoliative skin conditions including Stevens-Johnson syndrome. If a hypersensitivity reaction is suspected, discontinue Sitagliptin, assess for other potential causes for the event, and institute alternative treatment for diabetes.
Use in Pregnancy: There are no adequate and well-controlled studies in pregnant women; therefore, the safety of Sitagliptin in pregnant women is not known.
Use in Lactation: Sitagliptin is secreted in the milk of lactating rats. It is not known whether Sitagliptin is secreted in human milk. Therefore, Sitagliptin should not be used by a woman who is nursing.
Use in Children: Safety and effectiveness of Sitagliptin in paediatric patients under 18 years have not been established.
Use in the Elderly: No dosage adjustment is required based on age. Elderly patients are more likely to have renal insufficiency; as with other patients, dosage adjustment may be required in the presence of significant renal insufficiency.
Pregnancy: There are no adequate and well-controlled studies in pregnant women; therefore, the safety of Sitagliptin in pregnant women is not known.
Nursing Mothers: Sitagliptin is secreted in the milk of lactating rats. It is not known whether Sitagliptin is secreted in human milk. Therefore, Sitagliptin should not be used by a woman who is nursing.
The incidences of selected gastrointestinal adverse experiences in patients treated with Sitagliptin were: abdominal pain, nausea, vomiting and diarrhea.
Add-on Combination with a Sulfonylurea: More common side effect is hypoglycemia.
Add-on Combination with Metformin and a PPARγ Agonist: Common side effects are headache, diarrhoea, nausea, hypoglycaemia, vomiting, upper respiratory tract infection, nausea, cough, fungal skin infection, peripheral oedema, and vomiting.
Initial Combination Therapy with Metformin: diarrhoea; metformin: dyspepsia, flatulence, vomiting, headache.
Initial Combination Therapy with a PPARγ Agonist: Asymptomatic decreased blood glucose, symptomatic hypoglycaemia.
Sitagliptin does not inhibit CYP isozymes CYP3A4, 2C8, or 2C9. Based on in vitro data, Sitagliptin is also not expected to inhibit CYP2D6, 1A2, 2C19 or 2B6 or to induce CYP3A4. Co-administration of multiple twice-daily doses of metformin with Sitagliptin did not meaningfully alter the pharmacokinetics of Sitagliptin in patients with type 2 diabetes. Concomitant medications did not have a clinically meaningful effect on the pharmacokinetics of Sitagliptin. Medications assessed were those that are commonly administered to patients with type 2 diabetes including cholesterol-lowering agents (e.g., statins, fibrates, ezetimibe), anti-platelet agents (e.g., clopidogrel), anti-hypertensives (e.g., ACE inhibitors, angiotensin receptor blockers, beta-blockers, calcium channel blockers, hydrochlorothiazide), analgesics and non-steroidal anti-inflammatory agents (e.g., naproxen, diclofenac, celecoxib), anti-depressants (e.g., bupropion, fluoxetine, sertraline), antihistamines (e.g., cetirizine), proton pump inhibitors (e.g., omeprazole), and medications for erectile dysfunction (e.g., sildenafil). Patients receiving digoxin should be monitored appropriately. No dosage adjustment of digoxin or Sitagliptin is recommended. No dosage adjustment for Sitagliptin is recommended when co-administered with cyclosporine or other p-glycoprotein inhibitors (eg, ketoconazole).
Store below 30°C.
Protect from heat, sunlight & moisture.
A10BH01 - sitagliptin ; Belongs to the class of dipeptidyl peptidase 4 (DPP-4) inhibitors. Used in the treatment of diabetes.
FC tab 50 mg x 2 x 7's. 100 mg x 10 x 7's.
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