Sitagliptin

Indications
 Oral
Type 2 diabetes mellitus
Adult: 100 mg once daily.
CrCl (ml/min)Dosage Recommendation
30-<5050 mg daily.
<30 25 mg daily; may be given without regard to the timing of the haemodialysis.
Contraindications
 Type 1 diabetes. Diabetic ketoacidosis.
Warnings / Precautions
 Discontinue treatment if there are signs of hypersensitivity. Caution when used with sulphonylureas and/or other antidiabetic medications; monitor blood glucose regularly. Renal impairment; dose adjustment may be needed. Children <18 yr. Pregnancy, lactation.
Adverse Reactions
 Headache, diarrhoea, upper respiratory tract infection, nasopharyngitis. Angioedema, exfoliative dermatitis, hypoglycaemia.
Potentially Fatal: Anaphylaxis and/or severe dermatologic reactions such as Stevens-Johnson syndrome.
Overdose Reactions
 Treatment: Supportive measures; remove unabsorbed material from the GI tract, clinical monitoring and institute supportive therapy as needed.
Drug Interactions
 Concurrent use may increase serum levels of digoxin. Increased risk of hypoglycaemia when used with sulphonylureas.
See Below for More sitagliptin Drug Interactions
Mechanism of Actions
 Sitagliptin inhibits dipeptidyl peptidase IV (DPP-IV), resulting in prolonged active incretin levels. Incretin hormones increases insulin synthesis and release from pancreatic β-cells and reduces glucagon secretion from pancreatic α-cells. Reduced glucagon secretion leads to decreased hepatic glucose production.
Absorption: Rapid absorption. Bioavailability: About 87%.
Distribution: Protein binding: 38%.
Metabolism: Not extensively metabolised.
Excretion: Elimination half-life: 12 hr. 87% excreted in urine (mainly as unchanged drug) and 13% excreted in faeces.
Administration
 May be taken with or without food.
Storage Conditions
 Oral: Store at 20-25°C.
ATC Classification
 A10BH01 - sitagliptin ; Belongs to the class of dipeptidyl peptidase 4 (DPP-4) inhibitors. Used in the treatment of diabetes.
Storage
 Oral: Store at 20-25°C.
Available As
  • Sitagliptin 100 mg
  • Sitagliptin 25 mg
  • Sitagliptin 50 mg

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    One Response to Sitagliptin

    1. May 19, 2013 at 9:41 am #

      In the above page Sitagpliptin indication, dose , you have mentioned about Cr/Cl ml/min. What does it mean for a diabetic patient. How it is tested. What is the important of this value. Can you elaborate.
      Regards
      P.M. Rajendran

      Reply

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