Sitagliptin

Sitagliptin phosphate, an orally-active inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme. It is described chemically as 7-[(3R)-3-amino-1-oxo-4-(2,4,5trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine phosphate (1:1) monohydrate. The empirical formula is C16H15F6N5O€¢H3PO4€¢H2O. 1 It is licensed for the treatment of patients with type 2 diabetes to improve glycaemic control in combination with metformin or a glitazone, when diet and exercise, plus metformin or a glitazone do not provide adequate glycaemic control.


Adult Dose
Dose: 100 mg
Single Dose: 100 (100)
Frequency: 24 hourly
Route: oral
Instructions: take with or without food. If drug bothers your stomach, try taking it with food._x000D_ In moderate renal insufficiency (CrCl >30 to 1.7 to 1.5 to 3.0 mg/dL in men and > 2.5 mg/dL in women) or with end-stage renal disease (ESRD) requiring hemodialysis or peritoneal dialysis, the dose of sitagliptin is 25 mg once daily
Neonatal
Paedriatic
Characteristics
belongs to oral hypoglycemic. . The Molecular Weight of Sitagliptin is 523.32. It is weakly alkaline drug and Its pKa is 7.7.
Contraindications
Sitagliptin is contraindicated in conditions like Trauma,Insulin dependent diabetes mellitus,Type I diabetes mellitus,Diabetic ketoacidosis,Severe infections.
Effects
The severe or irreversible adverse effects of Sitagliptin, which give rise to further complications include Fever, Pancreatitis, Hypersensitivity reactions, Chills, Peeling & redness of skin.Sitagliptin produces potentially life-threatening effects which include Hypoglycemia, Hypoglycemia, Pancreatitis. which are responsible for the discontinuation of Sitagliptin therapy.The signs and symptoms that are produced after the acute overdosage of Sitagliptin include Tachycardia, Coma, Seizures, Drowsiness, Confusion, Hypoglycemia, Dizziness, Fainting, Sweating, Headache, Irritability, Tremor, Weakness.The symptomatic adverse reactions produced by Sitagliptin are more or less tolerable and if they become severe, they can be treated symptomatically, these include Headache, Nausea, Diarrhea, Sore throat, Stomach upset, Stuffy nose.
Indications
Sitagliptin is primarily indicated in conditions like Type II diabetes mellitus.
Interactions
No data regarding the interactions of Sitagliptin was found.
Interfrence
Risks
Drug should not be given to Paediatrics, Pregnant Mothers, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Store .
Warnings
Patients should be observed carefully for signs and symptoms of pancreatitis. If pancreatitis is suspected, Sitagliptin should promptly be discontinued and appropriate management should be initiated. A dosage adjustment is recommended in patients with moderate or severe renal insufficiency and in patients with ESRD requiring hemodialysis or peritoneal dialysis. Use caution when used in conjunction with sulfonylureas; risk of hypoglycemia is increased. Monitor blood glucose closely; dosage adjustments of the sulfonylurea may be necessary. Safety and efficacy have not been established in children
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