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Gliptin 100 ( Sitagliptin )

  • Effective Material
    Sitagliptin 100 mg
  • Caliber
    100 mg
  • Pharmacologic Form
    - Dipeptidyl peptidase-4 inhibitors
  • Therapeutic Categories
    Antidiabetic Drugs
  • Pharmaceutical Form
    F.C. Tablets
  • Download PDF file
Each coated tablet contains:
Sitagliptin phosphate monohydrate, equivalent to 100 mg of sitagliptin.
Pharmacodynamics properties
Antihypertensive drugs for oral blood sugar.
Pharmacodynamics properties
gliptin is a member of a class of oral anti-hyperglycaemic agents called dipeptidyl peptidase 4 (DPP-4) inhibitors.
The improvement in glycaemic control observed with this agent may be mediated by enhancing the levels of active incretin hormones.
Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal.
The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis.
When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells.
In addition, GLP-1 lowers glucagon secretion from pancreatic alpha cells.
Decreased glucagon concentrations, along with higher insulin levels, lead to reduced hepatic glucose production, resulting in a decrease in blood glucose levels.
The activity of GLP-1 and GIP is limited by the DPP-4 enzyme, which rapidly hydrolyses the incretin hormones to produce inactive products.
gliptin prevents the hydrolysis of incretin hormones by DPP-4, thereby increasing plasma concentrations of the active forms of GLP-1 and GIP, By enhancing active incretin levels, gliptin increases insulin release and decreases glucagon levels in a glucose-dependent manner. In patients with type 2 diabetes with hyperglycaemia, these changes in insulin and glucagon levels lead to lower haemoglobin A1c (HbA1c) and lower fasting and postprandial glucose concentrations.
gliptin decreases the amount of sugar made by the body. gliptin is unlikely to cause your blood sugar to be lowered to a dangerous level (hypoglycemia) because it does not work when your blood sugar is low.
Metabolism and excretion
Approximately 79% of this drug is excreted unchanged in the urine. In vitro studies indicated that the primary enzyme responsible for the limited metabolism of this drug was CYP3A4, with contribution from CYP2C8.
The apparent terminal t1/2 following a 100 mg oral dose of this drug was approximately 12.4 hours. The renal clearance was approximately 350 ml/min. This drug is eliminated in feces (13%) and urine (87%).
Therapeutic indications
– gliptin is indicated as an adjunct to diet and exercise to improve glycaemic control in patients with type 2 diabetes mellitus.
– gliptin is indicated as a monotherapy or combination therapy with metformin or a peroxisome proliferator-activated receptor gamma (PPARγ) agonist (e.g. thiazolidinediones) when the single agent does not provide adequate glycaemic control.
Side effect
The apparent terminal t1/2 following a 100 mg oral dose of this drug was approximately 12.4 hours. The renal clearance was approximately 350 ml/min. This drug is eliminated in feces (13%) and urine (87%).
Hypersensitivity to the active substance or to any of the excipients, ketoacidosis.
Warnings and precautions
A dosage adjustment is recommended in patients with moderate or severe renal insufficiency or with end stage renal disease (ESRD) requiring hemodialysis or peritoneal dialysis.
Pregnancy and lactation
Pregnancy Category B. There are no adequate data from the use of this drug in pregnant women, so this drug should be used during pregnancy only if clearly needed.
It is unknown whether this drug is excreted in human breast milk. Caution should be exercised when this drug is administered to a nursing woman.
geriatric Use:
No overall differences in safety or effectiveness were observed between subjects 65 years and over and younger subjects
pediatric Use:
Safety and effectiveness in pediatric patients under 18 years of age have not been established.
Drug interactions
gliptin had a small effect on plasma digoxin concentrations. Following administration of 0.25 mg digoxin concomitantly with 100 mg of this drug daily for 10 days, the plasma AUC of digoxin was increased on average by 11%, and the plasma Cmax on average by 18%. No dosage adjustment of digoxin or this drug is recommended.
The recommended dose of this drug is 100 mg once daily, it can be taken with or without food as a monotherapy or a combination therapy with metformin or thiazolidinediones or as an adjunct to diet and exercise.
Patients with Renal insufficiency:
For patients with mild renal insufficiency (creatinine clearance (CrCl) ≥ 50 mL/min, no dosage adjustment for this drug is required.
For patients with moderate renal insufficiency (CrCl ≥ 30 to <50 mL/min, the dose of gliptin is 50 mg once daily.
For patients with severe renal insufficiency (CrCl < 30 mL/min, or with end-stage renal disease (ESRD) requiring hemodialysis or peritoneal dialysis, the dose of gliptin is 25 mg once daily. gliptin may be administered without regard to the timing of hemodialysis.
Single doses of up to 800 mg of this drug were generally well tolerated. Minimal increases in QTc, not considered to be clinically relevant, were observed in one study at a dose of 800 mg sitagliptin.
gliptin 100: Carton box of 10 coated tablets, blister packed.
gliptin 100: Carton box of 20 coated tablets, blister packed.
Store in dry place up to 25°C.

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