Sitagliptin
Also known as: incretin enhancers,
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.
Primary Characteristics
Sitagliptin is also known as incretin enhancers, , Sitagliptin Phosphate.
It belongs to oral hypoglycemic.
Molecular Weight: 523.32 · pKa: 7.7 · Solubility in Water: 42.2mg/ml · Non-proprietary name: Sitagliptin · pH: 7.1.
Pharmacokinetics
Absorption: Sitagliptin has an oral bioavailability is 87%.
Distribution: Sitagliptin has a volume of distribution is 198 liters. plasma protein binding is 38%.
Elimination: it is metabolised via by CYP3A4 and CYP2C8, plasma half-life is 8-14 hours, renal excretion is primarily active tubular secretion.
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Indications
Sitagliptin is primarily indicated in conditions like Type II diabetes mellitus.
Contraindications
Sitagliptin is contraindicated in conditions like Trauma, Diabetic ketoacidosis, Insulin dependent diabetes mellitus, Severe infections, Type I diabetes mellitus.
Dosage
Sitagliptin's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 100 mg | 100 mg | Every 24h | oral | take with or without food. If drug bothers your stomach, try taking it with food. In moderate renal insufficiency (CrCl >30 to < 50 mL/min or serum creatinine levels of > 1.7 to < 3.0 mg/dL in men and > 1.5 to < 2.5 mg/dL in women ), the dose is 50 mg once daily. In severe renal insufficiency (CrCl < 30 mL/min or serum creatinine levels of > 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 |
| Paediatric Dosage (20kg) | ||||
| No data. | ||||
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Sitagliptin in overdosage may give rise to further complications which include Peeling & redness of skin , Hypersensitivity reactions , Chills , Fever , Pancreatitis .
Sitagliptin produces potentially life-threatening effects which include Hypoglycemia , Hypoglycemia, Pancreatitis . Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Sitagliptin are Coma, Seizures, Hypoglycemia, Tachycardia , Sweating , Irritability, Confusion , Drowsiness, Tremor, Weakness , Dizziness, Headache, Fainting .
Sitagliptin is known to cause more or less tolerable side effects which are usually transient. These include Diarrhea, Headache, Nausea, Sore throat, Stomach upset, Stuffy nose.
Warnings / Precautions
Available Brands
Storage Conditions
Drug Classification
- 1.18.7.2 — Oral hypoglycemics