Dosage and administration | Dosage: |
---|---|
Contraindications | Hypersensitivity to sitagliptin and any of excipients. |
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. |
Recommendation for pregnancy and breastfeeding | Pregnancy: |
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. |
Interactions, incompatibilities of medicine | Increased effect and toxicity: |
Undesirable effects (ADRs) | Common, ADR > 1/100 |
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. |
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). |
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. |
Storage conditions, shelf-life, quality specification of the medicine | Storage conditions: Protect from humidity and light, below 30 degrees C. |
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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