SITAGLIPTIN

SITAGLIPTIN

  • Brand: GLIPLESS®
  • Generic name:SITAGLIPTIN
  • Pharmaceutical form:Tab
  • Amount: 30
  • Pharmaceutical group: GASTRO INTESTINAL
Download brochure SITAGLIPTIN
SITAGLIPTIN
SITAGLIPTIN

Glipless®
Sitagliptin F.C tablet 
Introduction
 
Category:
inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme.                          (Drug Facts)
 
Chemistry:
 
Mechanism of action:
DPP-4 inhibitor; therefore, increase and prolongs incretin hormone activity, which is inactivated by DPP-4 enzyme
Incretins increase insulin release and synthesis from pancreatic beta cells and reduce glucagon secretion from pancreatic alpha cells. 
                                                                                                                                              (Drug Facts)
 
 
Pharmacokinetics:
Absorptio

Absorption

bioavailability is approximately 87%

Protein binding

38%

Metabolism

Approximately 79% is excreted unchanged in the urine

Time to Peak Concentration

1-4 hours

Elimination

Urine : 87%

Feces : 13%

 
(Facts, Martindale)
 
Indications:
Sitagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.                                                                  (PDR)
Contraindications:
Known serious hypersensitivity (e.g., anaphylaxis, angioedema) to sitagliptin or any ingredient in formulation.                                                                                  (PDR)
 
Warnings & Precautions:
1.Tell your doctor if you have or have had:
a disease of the pancreas (such as pancreatitis)
gallstones, alcohol dependence or very high levels of triglycerides (a form of fat) in your blood. These medical conditions can increase your chance of getting pancreatitis 
type 1 diabetes
diabetic ketoacidosis (a complication of diabetes with high blood sugar, rapid weight loss, nausea or vomiting)
any past or present kidney problems.
an allergic reaction to  Sitagliptin
2.Children and adolescents below 18 years should not use this medicine.
3.Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines.
- In particular, tell your doctor if you are taking digoxin (a medicine used to treat heart problems). The level of digoxin in your blood may need to be checked if taking with Sitagliptin.
4.This medicine has no or negligible influence on the ability to drive and use machines. However, dizziness and drowsiness have been reported, which may affect your ability to drive or use machines.
5.Taking this medicine in combination with medicines called sulphonylureas or with insulin can cause hypoglycemia, which may affect your ability to drive and use machines or work without safe foothold.
(www.medicines.org.uk )
 
Pregnancy:
There are no adequate data from the use of sitagliptin in pregnant women. Studies in animals have shown reproductive toxicity at high doses. The potential risk for humans is unknown. Due to lack of human data, Sitagliptin should not be used during pregnancy.  
                                                                                                                                 (www.medicines.org.uk )
Breast-feeding:
not known whether distributed into human milk.
(PDR)
Drug Interactions:
 
Drugs Metabolized by Hepatic Microsomal Enzymes
Does not inhibit CYP isoenzymes 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, or 3A4 in vitro or induce CYP3A4. Pharmacokinetic interactions with drugs metabolized by these isoenzymes unlikely. 
Inhibitors of P-glycoprotein Transport System
Substrate of p-glycoprotein transport system. Potential pharmacokinetic interaction (increased absorption and renal clearance of sitagliptin) with p-glycoprotein inhibitors
Clinically important pharmacokinetic interactions with p-glycoprotein inhibitors unlikely. Does not appear to inhibit p-glycoprotein transport system. 
Drugs Secreted by Renal Tubular Cationic Transport
Substrate of organic anion transport system; pharmacokinetic interaction unlikely with substrates of organic cationic transport system. 
Protein-bound Drugs
Pharmacokinetic interaction unlikely
 (Martindale/ Drug Facts)
 
Adverse Reactions:
 
Adverse effects reported with sitagliptin include upper respiratory-tract infections, headache, and nasopharyngitis. Hypersensitivity reactions including anaphylaxis, angioedema, urticaria, rash, and Stevens-Johnson syndrome have also been reported.
(Martindale)
Over dosage:
During controlled clinical trials in healthy subjects, single doses of up to 800 mg sitagliptin were administered. Minimal increases in QTc, not considered to be clinically relevant, were observed in one study at a dose of 800 mg sitagliptin. There is no experience with doses above 800 mg in clinical studies.
(www.medicines.org.uk)
 
Dosage & Administration:
Adults
Diabetes Mellitus
Oral
Sitagliptin monotherapy: Maximum 100 mg daily. Fixed combination with metformin hydrochloride: Maximum 100 mg of sitagliptin and 2 g of metformin hydrochloride daily (in divided doses).
 
 (PDR) 
Storage:
Store below 30˚ C and protect from humidity and direct light.
How supplied:
Sitagliptin is as available as 25&50&100 mg, Pink, mustard, peach. There are blisters of 10’s in a box of 30’s. 
 
 
 

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