SITAGIBES 100

Composition: Each film-coated tablet contains:
Sitagliptin. . . . . . . . . . . . . . . . . . . . . . . . . . . . . .100 mg
(As Sitagliptin phosphate monohydrate. . . . . . . .128.5 mg)
Presentation:
4 blisters of 7 film-coated tablets in a cardboard box.
Indications:
Sitagibes 100 tablets (sitagliptin) are indicated as monotherapy to improve glycemic control in patients with type II diabetes mellitus (insulin-independent diabetes) in combination with diet and physical activity.
Sitagliptin is used in combination with other anti-diabetic agents to control type II diabetes in those whose blood glucose levels are not controlled by oral antidiabetic drugs as monotherapy.
Sitagliptin is also used as triple oral therapy in combination with metformin and pioglitazone when dual therapy with these medicinal products do not provide adequate glycemic control.
Sitagliptin is also indicated as add-on to insulin (with or without metformin) when insulin do not provide adequate glycemic control.

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Dosage and administration	Dosage: For previously untreated patients: Monotherapy: Adult dose 100mg once a day. In combination with metformin hydrochloride: 100mg once daily. Patients switching over to combination therapy with other anti-diabetic drugs: Combination with metformin hydrochloride: The dose of sitagliptin is 100mg once daily. Pre-existing dose of metformin hydrochloride can be maintained when initiating the combination therapy with sitagliptin. Combination with a sulfonylurea: The dose of sitagliptin is 100mg once daily. Sulfonylurea dose may be reduced to minimize the risk of hypoglycemia. Combination with metformin hydrochloride and a sulfonylurea: The dose of sitagliptin is 100mg once daily. Sulfonylurea dose may be reduced to minimize the risk of hypoglycemia. Combination with thiazolidinedione: The dose of sitagliptin is 100mg once daily. Pre-existing thiazolidinedione dose can be maintained when initiating the combination therapy with sitagliptin. Combination therapy with sitagliptin/metformin hydrochloride fixed-dose combination: Dosage adjustment is individualized based on the current treatment regimen, clinical response and tolerability. Caution should be exercised when changing treatment regimens as it may cause changes in blood glucose control. In patients with uncontrolled glucose levels who are receiving sitagliptin monotherapy: Initially, sitagliptin with metformin in fixed-dose combination of 50/500mg is administered, twice daily. If necessary, metformin dose is increased with fixed dose combination of sitagliptin/metformin 50/1, 000mg twice daily. In patients with uncontrolled glucose levels who are receiving metformin monotherapy: Depending on the dose of metformin currently used, starting treatment should be sitagliptin with metformin in fixed-dose combination of 50/500mg or fixed dose combination of sitagliptin/metformin 50/1, 000mg, taken twice daily. In patients with uncontrolled blood glucose levels who are receiving metformin 850mg twice daily: Fixed dose combination of sitagliptin/metformin 50/1, 000mg, taken twice daily. In patients with uncontrolled blood glucose levels who are receiving combination therapy of sitagliptin and metformin hydrochloride, sitagliptin and a sulfonylurea or metformin hydrochloride and a sulfonylurea: A fixed dose of 50mg sitagliptin is taken, twice daily. Dose of metformin in combination is determined, based on current metformin dose and blood glucose level. Limit of dose: Sitagliptin monotherapy: Maximum dose is 100mg/daily. Combination therapy with metformin hydrochloride: Maximum recommended daily dose of 100mg sitagliptin and 2000mg metformin hydrochloride. Special populations: Hepatic impairment: No dose adjustment is necessary for patients with mild to moderate hepatic impairment. The safety and efficacy of sitagliptin in patients with severe hepatic impairment have not yet been established. Renal impairment: Sitagliptin monotherapy: Dose adjustment is recommended and caution should be used in patients with moderate to severe renal impairment or in patients with end-stage renal disease requiring hemodialysis or peritoneal dialysis. For patients with moderate renal impairment (ClCr ≥ 30 to < 50ml/min, approximately corresponding to serum creatinine levels of > 1.7 to 3mg/dl in men or > 1.5 to 2.5mg/dl in women): The recommended dose of sitagliptin is 50mg once daily. For patients with severe renal impairment (ClCr < 30ml/min, approximately corresponding to serum creatinine levels of > 3mg/dl in men or > 2.5mg/dl in women): Recommended sitagliptin dose is 25mg once daily. Persons with end-stage renal disease requiring hemodialysis or peritoneal dialysis: The recommended dose of sitagliptin is 25mg once daily. Sitagliptin may be administered without regard to the timing of hemodialysis. Combination therapy in the form of fixed dose combination of sitagliptin/metformin hydrochloride: Sitagliptin dose should be adjusted in patients with renal impairment switchover to sitagliptin/metformin hydrochloride fixed-dose combination therapy is not recommended. For elderly: Caution should be used to determinine an appropriate dose for elderly patients because renal function may be impaired. Administration: Monotherapy: Sitagibes 100 can be taken orally, once daily with or without food. If a dose is missed, take it as soon as possible and continue regular dosing schedule. If the dose is close to the next dose, skip the missed dose and go back to regular schedule. Do not take a double dose of this medicine. Combination therapy: When sitagliptin is used in combination therapy in the form of fixed dose combination of sitagliptin/metformin hydrochloride, combined medicine is taken twice daily with meal. The dose is up-titrated gradually to minimize ADRs of metformin hydrochloride on GI tract. If a dose is missed, it is taken as soon as possible, and regular dosing schedule is continued. If the missed dose is remembered at the time of present dose, skip the missed dose and go back to regular schedule. Not to compensate the missed dose by using double dose.
Contraindications	Hypersensitivity to sitagliptin and any of excipients. Type I diabetes (insulin-dependent diabetes mellitus). Diabetic ketoacidosis.
Warnings and precautions for use	Acute pancreatitis has been reported in patients using sitagliptin or sitagliptin in combination with metformin. There have been no studies on the use of sitagliptin in patients with a history of pancreatitis and it is unknown whether pancreatitis is increased in these subjects when they are treated with sitagliptin. When administering sitagliptin to patients with a history of pancreatitis, caution should be exercised, and close supervision should be recommended. Signs of pancreatitis such as nausea, vomiting, loss of appetite, severe persistent abdominal pain should be monitored. If pancreatitis is suspected, stop taking sitagliptin. Pancreatitis usually occurs within the first 30 days of treatment. Risk factors include obesity, hypercholesterolemia, hypertriglyceridemia. Renal impairment: Assessment of renal function is recommended prior to initiation of sitagliptin treatment and periodically thereafter. In some patients impaired renal function has been observed, including acute renal failure that hemodialysis is required. Among these patients, some had pre-existing impaired kidney function and some received inappropriate dosage of sitagliptin. Sitagliptin should be used with caution in patients with moderate to severe renal impairment or patients with end-stage renal disease requiring hemodialysis or peritoneal dialysis; if necessary, dose adjustment is required. In times of stress (fever, infections, surgery) during periods of stress such as fever, trauma, infection, or surgery blood glucose control may be lost, suspend sitagliptin use and insulin is indicated to control blood glucose. Resume sitagliptin therapy when the acute phase of hyperglycemia has passed. Rare hypersensitivity reactions: These reactions include anaphylaxis, angioedema, and exfoliative skin conditions including Stevens-Johnson syndrome. Onset of these reactions occurred within the first 3 months after initiation of treatment, with some reports occurring after the first dose. If signs/symptoms or hypersensitivity reactions occur, discontinue taking sitagliptin immediately. Caution should be exercised when sitagliptin is combined with sulfonylurea derivatives. This combination may increase the risk of hypoglycemia. Blood glucose levels should be monitored closely, dose adjustment is recommended, if necessary. Children: The safety and efficacy of sitagliptin in children and adolescents under 18 years of age have not yet been established.
Recommendation for pregnancy and breastfeeding	Pregnancy: Sitagliptin should not be used during pregnancy. Lactation: It is unknown whether sitagliptin is excreted in human breast milk, so sitagliptin should not be used during breast-feeding unless there is careful consideration of the potential risks to the breastfed infants and potential benefits to the mother.
Effects on ability to drive and use machines	Sitagliptin has no or negligible influence on the ability to drive and use machines. However, when driving or using machines, it should be taken into account that dizziness and somnolence have been reported. In addition, patients should be alerted to the risk of hypoglycaemia when sitagliptin is used in combination with a sulphonylurea or with insulin.
Interactions, incompatibilities of medicine	Increased effect and toxicity: Alcohol, anabolic steroids, MAO inhibitors, testosterone: May increase the hypoglycemic effect of sitagliptin. Sitagliptin increases plasma digoxin concentrations. Beta-adrenergic blocking agents may mask usual warning signs and symptoms of hypoglycemia caused by antidiabetic drugs. Decreased effect: Corticoids, loop diuretics and thiazide diuretics, birth control pills: May antagonize hypoglycemic effect of sitagliptin. CYP3A4 and 2C8 inhibitors or inducers have no effect on the metabolism of sitagliptin.
Undesirable effects (ADRs)	Common, ADR > 1/100 Digestive: Diarrhea, abdominal pain, nausea. Respiratory: Nasopharyngitis. Other ADRs: Peripheral oedema, upper respiratory tract infections, pain, dry mouth, anorexia, drowsiness, headache, dizziness, hypoglycemia (increased risk with the combination with sulphonylurea), chronic osteoarthritis, increased liver enzymes, increased serum creatinine, leukocytosis, and hypersensitivity reactions such as anaphylaxis, angioedema, Stevens-Johnson syndrome, exfoliative dermatitis, urticaria, pruritus, rash. Management of ADRs: If acute pancreatitis is suspected, the patient should be monitored closely with appropriate laboratory studies (such as serum and urine amylase, amylase/creatinine clearance ratio, electrolytes, serum calcium, glucose and lipase). Discontinue sitagliptin and timely supportive treatment is required.
Overdose and management	Symptoms: There have been so few reported cases of overdoses with sitagliptin. Clinical studies at a single dose of 800mg sitagliptin showed that it was well tolerated. Minimal increases in QTc, not considered to be clinically relevant, were observed in one study at a dose of 800mg sitagliptin. There is no experience with doses above 800mg in clinical studies. In Phase I multiple-dose studies, there were no dose-related clinical adverse reactions observed with sitagliptin with doses of up to 600mg per day for periods of up to 10 days and 400mg per day for periods of up to 28 days. Treatment: In case of overdose, usual supportive measures should be applied, such as removal of unabsorbed substances from the gastrointestinal tract, clinical monitoring (including obtaining an electrocardiogram), and supportive therapy, if necessary. Sitagliptin can be modestly dialysable. In clinical studies, about 13.5% of the dose was removed over a 3-4 hours of hemodialysis session. Prolonged haemodialysis may be considered if clinically appropriate. It is not known if sitagliptin is dialysable by peritoneal dialysis.
Pharmacodynamic properties	Sitagliptin inhibits dipeptidyl peptidase-4 (DPP-4) which is an enzyme inactivating incretin hormones stimulating the release of insulin from the pancreas, including glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1(GLP-1). GLP-1 and GIP stimulate the synthesis and release of insulin from pancreatic beta cells, which are glucose dependent (ie, dependent on normal or elevated blood glucose concentrations. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. In normal physiological conditions, incretin hormones are released by the small intestine throughout the day and their levels are increased in response to a meal; these hormones are rapidly inactivated by the enzyme DPP-4. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses. Sitagliptin increases GIP and GLP-1 levels in the circulation in a glucose-dependent manner. Co-administration of sitagliptin and metformin has additive effect on active GLP-1 concentrations. Sitagliptin lowers fasting plasma glucose levels and reduces changes in blood glucose levels after glucose intake or after meals in patients with type II diabetes.
Pharmacokinetic properties	Absorption: Sitagliptin is rapidly absorbed from the gastrointestinal tract. The absolute bioavailability of sitagliptin is approximately 87%. At steady state (usually achieved within 3 days after initiation of treatment), peak plasma concentrations occur within about 3 hours (ranging from 1 to 4 hours) after ingestion. Food does not affect the extent of absorption. Sitagliptin starts to decrease its effect on changes in plasma glucose levels approximately 60 minutes after meals. DPP-4 activity is possibly inhibited by about 80%, persisting for 12 or 24 hours, corresponding to oral dose of ≥ 50mg or ≥ 100mg, respectively. Distribution: The volume of distribution is approximately 198 litres. Sitagliptin is about 38% bound to plasma proteins. It is unknown whether sitagliptin is excreted into breast milk. Metabolism: Sitagliptin undergoes limited metabolism by the cytochrome system via isoenzymes 3A4 and 2C8 to form inactive metabolites. Elimination: Approximately 87% of dose is excreted in the urine (75% unchanged, 16% metabolized) and 13% in the faeces. Elimination of sitagliptin occurs primarily via renal excretion and involves active tubular secretion. The elimination half-life is about 12 hours. Renal impairment: The area under the curve (AUC) is increased, the elimination half-life is prolonged. Moderate hepatic impairment: Plasma peak concentrations and area under the curve (AUC) are increased but clinically insignificant. Elderly: Plasma concentrations increase insignificantly compared to younger subjects.
Storage conditions, shelf-life, quality specification of the medicine	Storage conditions: Protect from humidity and light, below 30 degrees C. Shelf – life: 36 months from the manufacture date. Quality specification: In house specification.

SITAGIBES 100

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