Sitagliptin

Instructions

Take with or without food

Swallow tablet whole; do not chew, crush, or split

Tablets: 25, 50, and 100 mg

Tablets should be stored at room temperature, 15-30 C (59-86 F)

If you experience severe and persistent joint pain, contact your doctor right away. Do not stop taking your medication. Your doctor will decide if your medication is the possible cause of severe  joint pain and will discontinue the drug if appropriate.

Do not take sitagliptin if you are allergic to any of the ingredients in sitagliptin.

Symptoms of a serious allergic reaction to sitagliptin may include:

• rash
• raised red patches on your skin (hives)
• swelling of the face, lips, tongue, and throat that may cause difficulty in breathing or swallowing

Tell your doctor if you have or have had inflammation of the pancreas (pancreatitis).

Tell your doctor if you have kidney problems or any other medical conditions.

Store sitagliptin at 68°F to 77°F (20°C to 25°C).

Keep sitagliptin and all medicines out of the reach of children.

You should not use sitagliptin if you are allergic to it, or if you are in a state of diabetic ketoacidosis (call your doctor for treatment with insulin).

To make sure sitagliptin is safe for you, tell your doctor if you have ever had:

• kidney disease (or if you are on dialysis);

• heart problems;

• pancreatitis;

• high triglycerides (a type of fat in the blood);

• gallstones; or

• a history of alcoholism.

This medicine is not expected to harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant.

Your name may need to be listed on a sitagliptin pregnancy registry when you start using this medicine.

It is not known whether sitagliptin passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Sitagliptin is not approved for use by anyone younger than 18 years old.

Usual Adult Dose for Diabetes Type 2:

Usual dose: 100 mg orally once a day

Comments: When used in combination with an insulin secretagogue (e.g. sulfonylurea) or insulin, a lower dose of the insulin secretagogue or insulin may be required to reduce the risk of hypoglycemia.

Use: As an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus.

Your doctor will tell you how much of sitagliptin to use and how often. Your dose may need to be changed several times in order to find out what works best for you. Do not use more medicine or use it more often than your doctor tells you to.

sitagliptin should come with a Medication Guide. Read and follow these instructions carefully. Ask your doctor if you have any questions.

Carefully follow the special meal plan your doctor gave you. This is the most important part of controlling your diabetes, and is necessary if the medicine is to work properly. Exercise regularly and test for sugar in your blood or urine as directed.

You may take sitagliptin with or without food.

Dosing

The dose of sitagliptin will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of sitagliptin. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (tablets):
  • For type 2 diabetes:
    • Adults—100 milligrams (mg) once a day.
    • Children—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of sitagliptin, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Elderly patients had ~19% higher plasma concentration.

Diabetes mellitus, type 2: As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus (noninsulin dependent) as monotherapy or combination therapy.

Diabetes mellitus, type 2: Oral: 100 mg once daily

Concomitant use with insulin and/or insulin secretagogues (eg, sulfonylureas): Reduced dose of insulin and/or insulin secretagogues may be needed.

CrCl ≥50 mL/minute: No dosage adjustment necessary.

CrCl ≥30 to <50 mL/minute (approximate SCr of >1.7 to ≤3 mg/dL [males] or >1.5 to ≤2.5 mg/dL [females]): 50 mg once daily

CrCl <30 mL/minute (approximate SCr of >3 mg/dL [males] or >2.5 mg/dL [females]): 25 mg once daily

ESRD requiring hemodialysis or peritoneal dialysis: 25 mg once daily; administer without regard to timing of hemodialysis

ACE Inhibitors: DPP-IV Inhibitors may enhance the adverse/toxic effect of ACE Inhibitors. Specifically, the risk of angioedema may be increased. Monitor therapy

Alpha-Lipoic Acid: May enhance the hypoglycemic effect of Antidiabetic Agents. Monitor therapy

Androgens: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Exceptions: Danazol. Monitor therapy

Digoxin: SITagliptin may increase the serum concentration of Digoxin. Monitor therapy

Guanethidine: May enhance the hypoglycemic effect of Antidiabetic Agents. Monitor therapy

Hyperglycemia-Associated Agents: May diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy

Hypoglycemia-Associated Agents: Antidiabetic Agents may enhance the hypoglycemic effect of Hypoglycemia-Associated Agents. Monitor therapy

Insulin: DPP-IV Inhibitors may enhance the hypoglycemic effect of Insulin. Management: Consider a decrease in insulin dose when initiating therapy with a dipeptidyl peptidase-IV inhibitor and monitor patients for hypoglycemia. Consider therapy modification

Lumacaftor: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. Lumacaftor may increase the serum concentration of P-glycoprotein/ABCB1 Substrates. Monitor therapy

MAO Inhibitors: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy

Pegvisomant: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy

P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Monitor therapy

P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Monitor therapy

Prothionamide: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy

Quinolone Antibiotics: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Quinolone Antibiotics may diminish the therapeutic effect of Blood Glucose Lowering Agents. Specifically, if an agent is being used to treat diabetes, loss of blood sugar control may occur with quinolone use. Monitor therapy

Ranolazine: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. Monitor therapy

Salicylates: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy

Selective Serotonin Reuptake Inhibitors: May enhance the hypoglycemic effect of Blood Glucose Lowering Agents. Monitor therapy

Sulfonylureas: DPP-IV Inhibitors may enhance the hypoglycemic effect of Sulfonylureas. Management: Consider a decrease in sulfonylurea dose when initiating therapy with a dipeptidyl peptidase-IV inhibitor and monitor patients for hypoglycemia. Consider therapy modification

Thiazide and Thiazide-Like Diuretics: May diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy

Mild or moderate hepatic impairment: No adjustment recommended
Severe hepatic impairment: Use caution; no data available