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Sitagliptin C16H15F6N5O

Molecular Weight: 407g/mol
Dissociation Constant: 8.78
Indication

It is primarily indicated for treating Diabetes Mellitus type 2.

Mechanism of Action

It is a pyrazine derived dipeptidyl peptidase 4 Inhibtor that stops the activity of hormone Incretin which is responsible for releasing insulin and reducing glucagon release from pancreatic cells. It may also cause inflammation in pancreas.

Dosage

Strength: 100mg

Form: tablet

Dosing interval: 24 Hr

Maximum Dose: Maximum recommended dose for sitagliptin is 100mg

Dialyzable:Yes

Maintainance dose

100mg once a day

Hepatic Adjustment

The medicine does not require any dose adjustments in mild to moderate hepatic insufficiency

Renal Adjustment

Data based study suggests in patients with creatinine clearence 30-50ml/min initaite 50mg once daily. In patients with creatinine clearence less than 50ml/min, 25mg Once daily. Also, 25mg per day for patients with end-stage renal disease or peritoneal dialysis.

  • pregnant

    Pregnancy

    Research on animals showed no effect and no human research was conducted. Or research on animals have shown some degree of effect but human research did not show any effects.

  • mother

    Lactation

    Study suggests to be used with caution. Risk for neonates and infants not known.

ContraIndication
Cautions

End stage renal diseased patients should be closely monitored. Dermatologic conditions for eg. Blister formation (Bullous pemphigoid) should be taken in care. Pancreatic Hemorrhage or acute inflammatory conditions must be immediately reported. Angioedemic patients.

Pharmacokinetics

Tmax: 198 Liters

Bioavailability: 87%

Protein Binding : 38%

Elimination Half Life (t1/2): 12 Hr

Metabolism: The molecule has found to have a limited metabolism through liver

Volume of Distribution (Vd): 198 Liters

Metabolites:

Sitagliptin is known to not undergo extensive metabolism as per studies, so no metabolites identified.

Disclaimer

Dawaai's intention is to make sure that it's consumers get information that is accurate, reviewed by an expert and error-free. However, the information mentioned here should not be used as a replacement for the advice of a qualified physician. The information given here is for informational purposes only, which may not cover all possible precautions, side effects, contraindications or drug interactions. Consult your doctor and discuss your queries related to any medicine or disease.

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