sitagliptin (Rx)

Brand and Other Names:Januvia
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 25mg
  • 50mg
  • 100mg

Type 2 Diabetes Mellitus

Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus (T2DM)

100 mg PO qDay

Dosage Modifications

Renal impairment

  • eGFR ≥45 to <90 mL/min/1.73 m2: No dosage adjustment necessary
  • eGFR 30 to <45 mL/min/1.73 m2: 50 mg PO qDay
  • eGFR <30 mL/min/1.73 m2: 25 mg PO qDay
  • End-stage renal disease requiring hemodialysis or peritoneal dialysis: 25 mg PO qDay regardless of timing of dialysis

Hepatic impairment

  • Mild to moderate impairment: Dose adjustment not necessary
  • Severe impairment: Not studied

Dosing Considerations

Limitations of use

  • Should not be used in patients with type 1 diabetes
  • Not studied in patients with a history of pancreatitis; unknown whether these patients are at increased risk for development of pancreatitis while using sitagliptin

Safety and efficacy not established

Three double-blind, placebo-controlled studies evaluated the efficacy and safety of sitagliptin in patients (n=410) aged 10-17 years with uncontrolled T2DM, with or without insulin therapy; results showed effects of patients treated with sitagliptin were not significantly different from placebo

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Interactions

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    Contraindicated

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            Adverse Effects

            >10%

            Combination with insulin with or without metformin

            • Hypoglycemia (15.5%)

            Combination with glimepiride with or without metformin

            • Hypoglycemia (12.2%)

            1-10%

            Monotherapy

            • Nasopharyngitis (5.2%)
            • Upper respiratory tract infection (4.5%)
            • Headache (1.1%)

            Combination with pioglitazone

            • Upper respiratory tract infection (6.3%)
            • Headache (5.1%)

            Combination with metformin

            • Nasopharyngitis (6.2%)
            • Upper respiratory tract infection (5.9%)

            Combination with metformin and rosiglitazone

            • Nasopharyngitis (6.1%)
            • Upper respiratory tract infection (5.5%)

            Combination with glimepiride with or without metformin

            • Nasopharyngitis (6.3%)
            • Upper respiratory tract infection (5.9%)

            Postmarketing Reports

            Hypersensitivity reactions including anaphylaxis, angioedema, rash, urticaria, cutaneous vasculitis, and exfoliative skin conditions including Stevens-Johnson syndrome

            Hepatic enzyme elevations; acute pancreatitis, including fatal and nonfatal hemorrhagic and necrotizing pancreatitis

            Worsening renal function, including acute renal failure (sometimes requiring dialysis)

            Severe and disabling arthralgia

            Tubulointerstitial nephritis

            Constipation, vomiting

            Headache, myalgia, pain in extremity, back pain

            Rhabdomyolysis

            Pruritus

            Bullous pemphigoid

            Mouth ulceration; stomatitis

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            Warnings

            Contraindications

            Serious hypersensitivity to sitagliptin (eg, anaphylaxis, angioedema)

            Cautions

            Acute pancreatitis reported, including fatal and nonfatal hemorrhagic or necrotizing pancreatitis; if pancreatitis suspected, discontinue promptly

            Acute renal failure reported, sometimes requiring dialysis; assess renal function before initiation and periodically thereafter

            Serious allergic and hypersensitivity reactions (eg, anaphylaxis, angioedema, exfoliative skin conditions including Stevens-Johnson syndrome) reported; promptly stop treatment and assess for other potential causes; appropriately monitor and treat

            Severe and disabling arthralgia reported in patients taking DPP-4 inhibitors; consider as a possible cause for severe joint pain and discontinue drug if appropriate

            Heart failure observed with other DPP-4 inhibitors; consider risks and benefits in patients with risk factors for heart failure; monitor for signs and symptoms; if heart failure develops, manage accordingly to standard of care and consider interrupting treatment

            Bullous pemphigoid reported with DPP-4 inhibitor use, which required hospitalization; in reported cases, patients recovered with topical or systemic immunosuppressive treatment and discontinuation of DPP-4 inhibitor; advise to report any developing blisters/erosions; discontinue DPP-4 therapy and consult a dermatologist if bullous pemphigoid suspected

            Drug interaction overview

            • Sitagliptin is a P-gp and organic anion transporter-3 substrate; weak CYP3A4 and CYP2C8 substrates
            • Insulin or insulin secretagogues
              • Increased risk of hypoglycemia when concomitantly used with insulin and/or an insulin secretagogue; consider lowering dose of insulin or insulin secretagogue
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            Pregnancy & Lactation

            Pregnancy

            Limited available data in pregnant females are not sufficient to inform a drug-associated risk for major birth defects and miscarriage

            Pregnancy registry

            • Monitors pregnancy outcomes in females exposed to drug during pregnancy
            • Encourage patients to report any prenatal exposure to drug by calling 1-800-986-8999

            Animal data

            • No adverse developmental effects were observed when administered to pregnant rats and rabbits during organogenesis at oral doses up to 30x and 20x, respectively, the 100-mg clinical dose, based on AUC

            Clinical considerations

            • Poorly controlled diabetes in pregnancy increases maternal risk for diabetic ketoacidosis, preeclampsia, spontaneous abortions, preterm delivery, still birth, and delivery complications
            • Poorly controlled diabetes increases fetal risk for major birth defects, stillbirth, and macrosomia related morbidity

            Lactation

            There is no information regarding presence of drug in human milk, effects on breastfed infants, or on milk production

            Present in rat milk and therefore possibly present in human

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Dipeptyl peptidase-IV (DPP-4) inhibitor; increases and prolongs incretin hormone activity, which is inactivated by DPP-4 enzyme

            Incretins increase insulin release and synthesis from pancreatic beta cells and reduce glucagon secretion from pancreatic alpha cells

            Absorption

            Bioavailability: 87%

            Peak plasma time: 1-4 hr

            Peak plasma concentration: 950 nM (single oral 100-mg dose)

            AUC: 8.52 microM·hr (single oral 100-mg dose)

            Distribution

            Protein bound: 38%

            Vd: 198 L

            Metabolism

            Limited; primarily via CYP3A4 and CYP2C8

            Elimination

            Renal clearance: 350 mL/min

            Half-life, terminal: 12.4 hr

            Excretion: Urine (87% [79% unchanged]), feces (13%)

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            Administration

            Oral Administration

            Take with or without food

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

            Storage

            Store at 20-25ºC (68-77ºF), excursions permitted to 15-30ºC (59-86ºF)

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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            Januvia oral
            -
            25 mg tablet
            Januvia oral
            -
            50 mg tablet
            Januvia oral
            -
            100 mg tablet

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Patient Education
            sitagliptin phosphate oral

            SITAGLIPTIN - ORAL

            (sit-a-GLIP-tin)

            COMMON BRAND NAME(S): Januvia

            USES: Sitagliptin is used with a proper diet and exercise program and possibly with other medications to control high blood sugar. It is used in people with type 2 diabetes. Controlling high blood sugar helps prevent kidney damage, blindness, nerve problems, loss of limbs, and sexual function problems. Proper control of diabetes may also lessen your risk of a heart attack or stroke.Sitagliptin is a diabetes drug that works by increasing levels of natural substances called incretins. Incretins help to control blood sugar by increasing insulin release, especially after a meal. They also decrease the amount of sugar your liver makes.

            HOW TO USE: Read the Medication Guide provided by your pharmacist before you start using sitagliptin and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food, as directed by your doctor, usually once daily.The dosage is based on your medical condition, kidney function, and response to treatment. Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day. Carefully follow the medication treatment plan, meal plan, and exercise program your doctor has recommended.Check your blood sugar regularly as directed by your doctor. Keep track of the results, and share them with your doctor. Tell your doctor if your blood sugar measurements are too high or too low. Your dosage/treatment may need to be changed.

            SIDE EFFECTS: Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Although sitagliptin by itself usually does not cause low blood sugar (hypoglycemia), low blood sugar may occur if this drug is prescribed with other diabetes medications. Talk with your doctor or pharmacist about whether the dose of your other diabetes medication(s) needs to be lowered.Symptoms of low blood sugar include sudden sweating, shaking, fast heartbeat, hunger, blurred vision, dizziness, or tingling hands/feet. It is a good habit to carry glucose tablets or gel to treat low blood sugar. If you don't have these reliable forms of glucose, rapidly raise your blood sugar by eating a quick source of sugar such as table sugar, honey, or candy, or drink fruit juice or non-diet soda. Tell your doctor about the reaction right away. Low blood sugar is more likely if you drink large amounts of alcohol, do unusually heavy exercise, or do not consume enough calories from food. To help prevent low blood sugar, eat meals on a regular schedule, and do not skip meals. Check with your doctor or pharmacist to find out what you should do if you miss a meal.Symptoms of high blood sugar (hyperglycemia) include thirst, increased urination, confusion, drowsiness, flushing, rapid breathing, and fruity breath odor. If these symptoms occur, tell your doctor right away. Your doctor may need to adjust your diabetes medication(s).Tell your doctor right away of any serious side effects, including: signs of kidney problems (such as change in the amount of urine), joint pain, unusual skin blisters, signs of heart failure (such as shortness of breath, swelling ankles/feet, unusual tiredness, unusual/sudden weight gain).Get medical help right away if you have any very serious side effects, including: signs of pancreatitis (such as nausea/vomiting that doesn't stop, loss of appetite, severe stomach/abdominal/back pain).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any of the following symptoms of a serious allergic reaction: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: Before taking sitagliptin, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease, heart failure, disease of the pancreas (pancreatitis), stones in your gallbladder (gallstones).You may experience blurred vision, dizziness, or drowsiness due to extremely low or high blood sugar. Do not drive, use machinery, or do any activity that requires alertness or clear vision until you are sure you can perform such activities safely.Limit alcohol while taking this medication because it can increase your risk of developing low blood sugar.It may be harder to control your blood sugar when your body is stressed (such as due to fever, infection, injury, or surgery). Consult your doctor because increased stress may require a change in your treatment plan, medications, or blood sugar testing.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy this medication should be used only when clearly needed. Pregnancy may cause or worsen diabetes. Discuss a plan with your doctor for managing your blood sugar while pregnant. Your doctor may change your diabetes treatment during your pregnancy. Discuss the risks and benefits of different treatments (such as diet, exercise, and medications including insulin).It is unknown whether this drug passes into breast milk. Consult your doctor before breast-feeding.

            DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Beta-blocker medications (such as metoprolol, propranolol, glaucoma eye drops such as timolol) may prevent the fast/pounding heartbeat you would usually feel when your blood sugar falls too low (hypoglycemia). Other symptoms of low blood sugar, such as dizziness, hunger, or sweating, are unaffected by these drugs.Many drugs can affect your blood sugar, making it harder to control. Before you start, stop, or change any medication, talk with your doctor or pharmacist about how the medication may affect your blood sugar. Check your blood sugar regularly as directed and share the results with your doctor. Tell your doctor right away if you have symptoms of high or low blood sugar. (See also Side Effects section.) Your doctor may need to adjust your diabetes medication, exercise program, or diet.

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

            NOTES: Do not share this medication with others.Lab and/or medical tests (such as kidney function, blood glucose, hemoglobin A1c) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.Attend a diabetes education program to learn more about how to manage your diabetes with medications, diet, exercise, and regular medical exams.Learn the symptoms of high and low blood sugar and how to treat low blood sugar. Check your blood sugar regularly as directed.

            MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

            STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

            MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

            Information last revised December 2022. Copyright(c) 2022 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.