Saxagliptin

Saxagliptin is a prescription medication used to treat type 2 diabetes. Saxagliptin belongs to a group of drugs called dipeptidyl peptidase-4 (DPP-4) inhibitors. It works by increasing the amount of insulin made by the body after meals, and by decreasing the amount of glucose produced by the liver.

This medication comes in tablet form. It is usually taken once daily, with or without food. Do not split or cut saxagliptin tablets. Swallow the tablets whole.

Common side effects of saxagliptin includes upper respiratory tract infection, urinary tract infection, and headache.

Serious side effects can happen to people taking saxagliptin, including inflammation of the pancreas (pancreatitis) which may be severe and lead to death.

Certain medical problems make you more likely to get pancreatitis.

Before you start taking saxagliptin:

Tell your healthcare provider if you have ever had:

• inflammation of your pancreas (pancreatitis)
• stones in your gallbladder (gallstones)
• a history of alcoholism
• high blood triglyceride levels
• a history of a serious hypersensitivity reaction to saxagliptin, such as anaphylaxis, angioedema, or exfoliative skin conditions.

It is not known if having these medical problems will make you more likely to get pancreatitis with saxagliptin.

Stop taking saxagliptin and contact your healthcare provider right away if you have pain in your stomach area (abdomen) that is severe and will not go away. The pain may be felt going from your abdomen through to your back. The pain may happen with or without vomiting. These may be symptoms of pancreatitis.

Saxagliptin may cause severe and persistent joint pain. 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 saxagliptin if you:

• have a history of a serious hypersensitivity reaction to saxagliptin, such as anaphylaxis, angioedema, or exfoliative skin conditions.

• swelling of your face, lips, throat, and other areas on your skin
• difficulty with swallowing or breathing
• raised, red areas on your skin (hives)
• skin rash, itching, flaking, or peeling

If you have these symptoms, stop taking saxagliptin and contact your healthcare provider right away.

• Take saxagliptin by mouth one time each day exactly as directed by your healthcare provider. Do not change your dose without talking to your healthcare provider.
• Saxagliptin can be taken with or without food.
• Do not split or cut saxagliptin tablets.
• During periods of stress on the body, such as:
  • fever
  • trauma
  • infection
  • surgery

• Your healthcare provider should test your blood to measure how well your kidneys are working before and during your treatment with saxagliptin. You may need a lower dose of saxagliptin if your kidneys are not working well.
• Follow your healthcare provider’s instructions for treating blood sugar that is too low (hypoglycemia). Talk to your healthcare provider if low blood sugar is a problem for you.
• If you miss a dose of saxagliptin, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose. Just take the next dose at your regular time. Do not take two doses at the same time unless your healthcare provider tells you to do so. Talk to your healthcare provider if you have questions about a missed dose.
• If you take too much saxagliptin, call your healthcare provider or Poison Control Center at 1-800-222-1222, or go to the nearest hospital emergency room right away.

• Store saxagliptin at room temperature between 68°F and 77°F (20°C and 25°C).
• Keep saxagliptin and all medicines out of the reach of children.

Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not take this medicine in larger or smaller amounts or for longer than recommended.

You may take this medicine with or without food. Follow your doctor's instructions.

Do not crush, chew, or break a saxagliptin tablet. Swallow it whole.

Your blood sugar will need to be checked often, and you may need other blood tests at your doctor's office.

Low blood sugar (hypoglycemia) can happen to everyone who has diabetes. Symptoms include headache, hunger, sweating, pale skin, irritability, dizziness, feeling shaky, or trouble concentrating. Always keep a source of sugar with you in case you have low blood sugar. Sugar sources include fruit juice, hard candy, crackers, raisins, and non-diet soda. Be sure your family and close friends know how to help you in an emergency.

If you have severe hypoglycemia and cannot eat or drink, use a glucagon injection. Your doctor can prescribe a glucagon emergency injection kit and tell you how to use it.

Check your blood sugar carefully during times of stress, travel, illness, surgery or medical emergency, vigorous exercise, or if you drink alcohol or skip meals. These things can affect your glucose levels and your dose needs may also change. Do not change your medication dose or schedule without your doctor's advice.

Your doctor may want you to stop taking saxagliptin for a short time if you become ill, have a fever or infection, or if you have surgery or a medical emergency.

Saxagliptin is only part of a complete program of treatment that also includes diet, exercise, weight control, and possibly other medications. It is important to use this medicine regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely.

Store at room temperature away from moisture and heat

Get emergency medical help if you have signs of an allergic reaction: hives, a purple or red skin rash that spreads and causes blistering and peeling; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop taking saxagliptin and call your doctor right away if you have symptoms of pancreatitis: severe pain in your upper stomach spreading to your back, nausea and vomiting, loss of appetite, or fast heartbeats.

Call your doctor at once if you have:

• severe or ongoing pain in your joints;

• pain or burning when you urinate; or

• heart problems--shortness of breath (even while lying down), feeling weak or tired, rapid weight gain, swelling (especially in your feet, legs, or midsection.

Common side effects may include:

• runny or stuffy nose, sore throat, cough; or

• headache.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Usual Adult Dose for Diabetes Type 2:

2.5 or 5 mg orally once a day, regardless of meals

Coadministration with strong CYP450 3A4/5 inhibitors: 2.5 mg orally once a day

Use: Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes in multiple clinical settings

Other drugs may increase or decrease the effects of saxagliptin on lowering your blood sugar. Tell your doctor about all medications you use. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

• Anxiety
• bladder pain
• bloating or swelling of the face, arms, hands, lower legs, or feet
• bloody or cloudy urine
• blurred vision
• body aches or pain
• chills
• cold sweats
• confusion
• cool, pale skin
• cough
• depression
• difficult, burning, or painful urination
• difficulty with breathing
• dizziness
• ear congestion
• fast heartbeat
• fever
• frequent urge to urinate
• headache
• increased hunger
• loss of voice
• lower back or side pain
• nasal congestion
• nausea
• nightmares
• rapid weight gain
• runny nose
• seizures
• shakiness
• slurred speech
• sneezing
• sore throat
• tingling of the hands or feet
• unusual tiredness or weakness
• unusual weight gain or loss

• Chest pain
• constipation
• darkened urine
• decreased urine output
• difficulty with swallowing
• dilated neck veins
• extreme fatigue
• flaking or peeling of the skin
• hives or skin rash
• indigestion
• irregular breathing
• irregular heartbeat
• large, hard skin blisters
• large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
• loss of appetite
• pains in the stomach, side, or abdomen, possibly radiating to the back
• puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
• severe joint pain
• swelling of face, fingers, feet, or lower leg
• tightness in the chest
• troubled breathing
• vomiting
• weight gain
• yellow eyes or skin

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

• Diarrhea
• pain or tenderness around the eyes and cheekbones
• redness of the skin
• weakness
• welts

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

• Tell all of your health care providers that you take this medicine. This includes your doctors, nurses, pharmacists, and dentists.
• Do not drive if your blood sugar has been low. There is a greater chance of you having a crash.
• Check your blood sugar as you have been told by your doctor.
• Have blood work checked as you have been told by the doctor. Talk with the doctor.
• It may be harder to control your blood sugar during times of stress like when you have a fever, an infection, an injury, or surgery. A change in level of physical activity or exercise and a change in diet may also affect your blood sugar. Talk with your doctor.
• Talk with your doctor before you drink alcohol.
• Follow the diet and workout plan that your doctor told you about.
• A skin reaction called bullous pemphigoid has happened with drugs like this one. Sometimes, people have had to go to the hospital. Call your doctor right away if you have blisters or if your skin starts to break down.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using saxagliptin while you are pregnant.
• Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

Use this medicine as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• Take with or without food.
• Swallow whole. Do not chew, break, or crush.
• To gain the most benefit, do not miss doses.
• Keep taking saxagliptin as you have been told by your doctor or other health care provider, even if you feel well.

What do I do if I miss a dose?

• Take a missed dose as soon as you think about it.
• If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

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

Aprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

CYP3A4 Inducers (Strong): May decrease the serum concentration of SAXagliptin. Monitor therapy

CYP3A4 Inhibitors (Moderate): May increase the serum concentration of SAXagliptin. Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of SAXagliptin. Management: Saxagliptin U.S. product labeling recommends limiting saxagliptin adult dose to 2.5 mg/day when used with a strong CYP3A4 inhibitor. Monitor for increased saxagliptin levels/effects. A similar recommendation is not made in the Canadian product labeling. Consider therapy modification

Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination

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

Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

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

MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates. Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Consider therapy modification

Netupitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Palbociclib: May increase the serum concentration of CYP3A4 Substrates. 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

Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Stiripentol: May increase the serum concentration of CYP3A4 Substrates. Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

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

Applies to saxagliptin: oral tablet

Along with its needed effects, saxagliptin may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking saxagliptin:

• Anxiety
• bladder pain
• bloating or swelling of the face, arms, hands, lower legs, or feet
• bloody or cloudy urine
• blurred vision
• body aches or pain
• chills
• cold sweats
• confusion
• cool, pale skin
• cough
• depression
• difficult, burning, or painful urination
• difficulty with breathing
• dizziness
• ear congestion
• fast heartbeat
• fever
• frequent urge to urinate
• headache
• increased hunger
• loss of voice
• lower back or side pain
• nasal congestion
• nausea
• nightmares
• rapid weight gain
• runny nose
• seizures
• shakiness
• slurred speech
• sneezing
• sore throat
• tingling of the hands or feet
• unusual tiredness or weakness
• unusual weight gain or loss

• Chest pain
• constipation
• darkened urine
• decreased urine output
• difficulty with swallowing
• dilated neck veins
• extreme fatigue
• flaking or peeling of the skin
• hives or skin rash
• indigestion
• irregular breathing
• irregular heartbeat
• large, hard skin blisters
• large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
• loss of appetite
• pains in the stomach, side, or abdomen, possibly radiating to the back
• puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
• severe joint pain
• swelling of face, fingers, feet, or lower leg
• tightness in the chest
• troubled breathing
• vomiting
• weight gain
• yellow eyes or skin

Some side effects of saxagliptin may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

• Diarrhea
• pain or tenderness around the eyes and cheekbones
• redness of the skin
• weakness
• welts

No adjustment recommended.

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.