Sitagliptin

BRAND NAMES:

Steglujan: Its active components are ertugliflozin and sitagliptin. Together with diet and exercise, it is offered as pills to treat type 2 diabetes and improve blood sugar.

Janumet: Janumet comprises the active chemicals sitagliptin and metformin. It is offered as tablets.

Januvia: Januvia includes the active component sitagliptin. It is offered as tablets.

MECHANISM OF ACTION:

Sitagliptin belongs to the gliptin class of antidiabetic medicines. Its mode of action is to inhibit dipeptidyl peptidase-4, an enzyme that degrades and renders inactive glucagon-like peptide 1. The raised GLP-1 level in response to sitagliptin causes greater insulin release after meals and improves glucose tolerance.

PHARMACOKINETICS:

ABSORPTION: Sitagliptin has an oral bioavailability of 87%, and its pharmacokinetics are unaffected by whether it is taken with or without meals. Sitagliptin achieves its maximal plasma concentration in 2 hours.

DISTRIBUTION: The apparent mean volume  of distribution of sitagliptin is 198L.

METABOLISM: Cytochrome P4503A4 is the enzyme that metabolises sitagliptin, with CYP2C8 playing a small role.

EXCRETION:

Sitagliptin is eliminated through 87% in urine and 13% in feces.

PHARMACODYNAMICS:

Sitagliptin inhibits DPP-4, resulting in higher amounts of glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide, lower levels of glucagon, and a greater insulin sensitivity to glucose.

DRUG AND ADMINISTRATION:

Sitagliptin comes as a tablet taken orally. It is usually taken once a day with or without food. Take sitagliptin at around the same time every day.

Sitagliptin is available in the form of tablets with the strengths of 25 mg, 50 mg, and 100 mg.

DRUG INTERCATIONS:

Drug interactions of sitagliptin may include

• Anti-diabetic: insulin glargine
• Diuretic: furosemide
• Cardiac glycoside: digoxin

CONTRAINDICATIONS:

Sitagliptin tablets are not recommended for people who have had severe hypersensitivity responses to sitagliptin or any of its excipients. Sitagliptin has been associated with severe hypersensitivity responses such as anaphylaxis and angioedema.

SIDE EFFECTS:

Common side effects of sitagliptin include

Sore throat

Headache

Diarrhoea

Nausea

Serious side effects of sitagliptin include

Itching

Joint pain

Fever

Loss of appetite

Difficulty breathing

Rash

OVERDOSE:

If you increase your dose or take it too soon for your next scheduled time, you may be more likely to experience major side effects such as severe gastrointestinal issues or a low blood sugar response.

The symptoms of overdose may include

Excessive sweating

Tremor

Change in mental activity.

Have terrible stomach discomfort—pancreatitis.

TOXICITY:

In the case of an overdose, it is permissible to take the normal supportive measures, such as removing unabsorbed material from the gastrointestinal system, using clinical surveillance, and instituting supportive therapy based on the patient's clinical condition. Sitagliptin is somewhat dialysable. In clinical investigations, roughly 13.5% of the dosage was eliminated during a 3 to 4-hour haemolysis session. Prolonged haemolysis may be considered if clinically indicated. It is unclear whether sitagliptin can be dialysed by peritoneal dialysis.