Sitagliptin
DRUG STATUS
Government Approvals
US(FDA), UK(BNF)
WHO Essential Medicine
NO
Known Teratogen
Unlisted
Pharmaceutical Class
Dipeptidyl Peptidase 4 Inhibitor

Sitagliptin
Learn more about this medicine -
Click HereSummary
Sitagliptin is primarily used to treat type 2 diabetes. It helps control blood sugar levels in adults. It may also be used to reduce the risk of cardiovascular events in patients with diabetes and other cardiovascular conditions.
Sitagliptin works by blocking an enzyme called dipeptidyl peptidase-4 (DPP4). This increases the levels of hormones that help regulate blood sugar by stimulating insulin release and reducing glucose production by the liver. This helps control blood sugar levels, particularly after meals.
The usual daily dosage of Sitagliptin for adults is 100 mg taken once a day. It can be taken with or without food. For patients with kidney problems, the dosage may need to be adjusted.
The most common side effects of Sitagliptin include upper respiratory tract infections, headaches, and stomach issues like nausea and diarrhea. Rare but serious side effects may include pancreatitis, severe allergic reactions, and joint pain.
Sitagliptin should be used cautiously in patients with a history of pancreatitis. It is not recommended for individuals with severe hypersensitivity to the drug. Also, it should not be used during pregnancy unless absolutely necessary, and breastfeeding is not advised without consulting a healthcare provider.
Indications and Purpose
What is Sitagliptin used for?
Sitagliptin is indicated for the management of type 2 diabetes in adults. It is used to improve glycemic control in conjunction with diet and exercise. Sitagliptin can be used alone or in combination with other diabetes medications, such as metformin, sulfonylureas, or insulin, to help lower blood sugar levels and reduce the risk of diabetes-related complications.
How does Sitagliptin work?
Sitagliptin works by inhibiting the enzyme dipeptidyl peptidase-4 (DPP-4), which slows the inactivation of incretin hormones. This leads to increased levels of active incretins, such as GLP-1 and GIP, which enhance insulin release and decrease glucagon levels in a glucose-dependent manner. This helps lower blood sugar levels in individuals with type 2 diabetes.
Is Sitagliptin effective?
Sitagliptin has been shown to effectively improve glycemic control in adults with type 2 diabetes. Clinical trials have demonstrated significant reductions in HbA1c, fasting plasma glucose, and postprandial glucose levels when used as monotherapy or in combination with other diabetes medications. These improvements help manage blood sugar levels and reduce the risk of diabetes-related complications.
How does one know if Sitagliptin is working?
The benefit of Sitagliptin is evaluated by regularly monitoring blood sugar levels, including fasting plasma glucose and HbA1c. These tests help determine how well the medication is controlling blood sugar over time. Regular follow-up appointments with your healthcare provider are essential to assess the effectiveness of the treatment and make any necessary adjustments.
Directions for Use
What is the usual dose of Sitagliptin?
The usual daily dose of Sitagliptin for adults is 100 mg taken orally once a day. For patients with moderate renal impairment, the dose is reduced to 50 mg once daily, and for those with severe renal impairment or end-stage renal disease, the dose is 25 mg once daily. Sitagliptin is not recommended for use in children as its safety and effectiveness have not been established in pediatric patients.
How do I take Sitagliptin?
Sitagliptin should be taken once daily, with or without food, at the same time each day to maintain consistent blood levels. There are no specific food restrictions associated with Sitagliptin, but it is important to follow a balanced diet as recommended by your healthcare provider. Always follow your doctor's instructions regarding dosage and any additional dietary guidelines.
For how long do I take Sitagliptin?
Sitagliptin is typically used as a long-term treatment for managing type 2 diabetes. It is important to continue taking it as prescribed by your healthcare provider, even if you feel well, as it helps control blood sugar levels over time. Regular monitoring and follow-up with your doctor are essential to assess its effectiveness and make any necessary adjustments.
How long does it take for Sitagliptin to start working?
Sitagliptin begins to work shortly after ingestion, but it may take several weeks to see the full effect on blood sugar levels. Regular monitoring of blood glucose and HbA1c levels will help assess its effectiveness over time. It is important to continue taking the medication as prescribed and maintain regular follow-up appointments with your healthcare provider.
How should I store Sitagliptin?
Sitagliptin should be stored at room temperature, between 68°F to 77°F (20°C to 25°C), and protected from moisture. It should be kept in its original container, tightly closed, and out of reach of children. Once the bottle is opened, the medication should be used within 6 months. Avoid storing it in the bathroom to prevent exposure to moisture.
Warnings and Precautions
Who should avoid taking Sitagliptin?
Important warnings for Sitagliptin include the risk of acute pancreatitis, which can be severe and life-threatening. Patients should be aware of symptoms like severe abdominal pain. Sitagliptin is contraindicated in patients with a history of serious hypersensitivity reactions to the drug. Caution is advised for those with renal impairment, and dosage adjustments may be necessary. Monitoring for heart failure symptoms is also recommended.
Can I take Sitagliptin with other prescription drugs?
Sitagliptin may interact with insulin or insulin secretagogues, increasing the risk of hypoglycemia. A lower dose of these medications may be required when used with Sitagliptin. Additionally, caution is advised when using Sitagliptin with other medications that affect renal function, as it is primarily excreted by the kidneys. Always inform your healthcare provider of all medications you are taking to avoid potential interactions.
Can I take Sitagliptin with vitamins or supplements?
From all available and reliable information, there is no confirmed data on this. Please consult a doctor for personalized advice.
Can Sitagliptin be taken safely while pregnant?
There is limited data on the use of Sitagliptin during pregnancy, and its effects on fetal development are not well established. Animal studies have not shown adverse developmental effects at doses much higher than the human dose. However, due to the lack of human data, it is recommended to use Sitagliptin during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult your healthcare provider for personalized advice.
Can Sitagliptin be taken safely while breastfeeding?
There is no information on the presence of Sitagliptin in human breast milk or its effects on the breastfed infant. Animal studies have shown that Sitagliptin is present in rat milk. Due to the lack of human data, it is recommended to weigh the benefits of breastfeeding against the mother's need for Sitagliptin and any potential adverse effects on the infant. Consult your healthcare provider for personalized advice.
Is Sitagliptin safe for the elderly?
For elderly patients, no specific dose adjustment is necessary based on age alone. However, since Sitagliptin is excreted by the kidneys, and renal function can decline with age, it is important to assess renal function more frequently in elderly patients. This ensures that the dosage is appropriate and helps prevent potential side effects related to renal impairment.
Is it safe to exercise while taking Sitagliptin?
Sitagliptin does not specifically limit the ability to exercise. However, it is important for individuals with diabetes to monitor their blood sugar levels before, during, and after exercise, as physical activity can affect glucose levels. If you experience any unusual symptoms while exercising, such as dizziness or fatigue, consult your healthcare provider for guidance.
Is it safe to drink alcohol while taking Sitagliptin?
Drinking alcohol can affect blood sugar levels and may interfere with the effectiveness of Sitagliptin. It is important to discuss alcohol consumption with your healthcare provider, as excessive alcohol intake can increase the risk of pancreatitis, a serious side effect associated with Sitagliptin. Moderation and medical guidance are advised.