Saxagliptin

Brand names: Onglyza

What is saxagliptin?

Saxagliptin is used to lower blood sugar in patients with high blood sugar (diabetes).

Description

Saxagliptin is an orally-active inhibitor of the DPP-4 enzyme.

Saxagliptin monohydrate is described chemically as (1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile, monohydrate or (1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxyadamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrate. The empirical formula is C18H25N3O2•H2O and the molecular weight is 333.43. The structural formula is:

Saxagliptin Chemical Structure

Saxagliptin monohydrate is a white to light yellow or light brown, non-hygroscopic, crystalline powder. It is sparingly soluble in water at 24°C ± 3°C, slightly soluble in ethyl acetate, and soluble in methanol, ethanol, isopropyl alcohol, acetonitrile, acetone, and polyethylene glycol 400 (PEG 400).

Each film-coated tablet of ONGLYZA for oral use contains either 2.79 mg saxagliptin hydrochloride (anhydrous) equivalent to 2.5 mg saxagliptin or 5.58 mg saxagliptin hydrochloride (anhydrous) equivalent to 5 mg saxagliptin and the following inactive ingredients: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, and magnesium stearate. In addition, the film coating contains the following inactive ingredients: polyvinyl alcohol, polyethylene glycol, titanium dioxide, talc, and iron oxides.

Mechanism of Action

Increased concentrations of the incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are released into the bloodstream from the small intestine in response to meals. These hormones cause insulin release from the pancreatic beta cells in a glucose-dependent manner but are inactivated by the DPP-4 enzyme within minutes. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, reducing hepatic glucose production.

In patients with type 2 diabetes, concentrations of GLP-1 are reduced but the insulin response to GLP-1 is preserved. Saxagliptin is a competitive DPP-4 inhibitor that slows the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus.

Before taking saxagliptin:

  • If you are allergic to saxagliptin; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
  • If you have any of these health problems: Acidic blood problem or type 1 diabetes.

This is not a list of all drugs or health problems that interact with saxagliptin.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take saxagliptin with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take saxagliptin?

  • Tell all of your health care providers that you take saxagliptin. 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 blood sugar during times of stress such as fever, infection, injury, or surgery. A change in physical activity, exercise, or diet may also affect blood sugar.
  • Talk with your doctor before you drink alcohol.
  • Follow the diet and workout plan that your doctor told you about.
  • A severe pancreas problem (pancreatitis) has happened with saxagliptin. Sometimes, this may be deadly. If you have questions, talk with your doctor.
  • 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, plan on getting pregnant, or are breast-feeding. You will need to talk about the benefits and risks to you and the baby.

How is saxagliptin taken?

Use saxagliptin 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.
  • 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.

What are the side effects of saxagliptin that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Signs of a pancreas problem (pancreatitis) like very bad stomach pain, very bad back pain, or very bad upset stomach or throwing up.
  • Signs of a urinary tract infection (UTI) like blood in the urine, burning or pain when passing urine, feeling the need to pass urine often or right away, fever, lower stomach pain, or pelvic pain.
  • Low blood sugar can happen. The chance may be raised when saxagliptin is used with other drugs for diabetes. Signs may be dizziness, headache, feeling sleepy or weak, shaking, fast heartbeat, confusion, hunger, or sweating. Call your doctor right away if you have any of these signs. Follow what you have been told to do for low blood sugar. This may include taking glucose tablets, liquid glucose, or some fruit juices.
  • Heart failure has happened in people taking saxagliptin. Tell your doctor if you have ever had heart failure or kidney problems. Call your doctor right away if you feel very tired or you have shortness of breath, a big weight gain, or swelling in the arms or legs.
  • Drugs like this one may cause joint pain that can be very bad and disabling. Call your doctor right away if you have very bad joint pain or any joint pain that does not go away.

What are some other side effects of saxagliptin?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

  • Headache.
  • Signs of a common cold.
  • Urinary tract infection
  • Nausea 

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

Label

 DISPLAY PANEL – 5 MG

  • 30 Tablets
  •   NDC 0310-6105-30
    onglyza® (saxagliptin) tablets
    5 mg
    DISPENSE WITH MEDICATION GUIDE
    Rx only
    AstraZeneca
Onglyza 5 mg Bottle Label

 

 DISPLAY PANEL – 2.5 MG

  • 30 Tablets          NDC 0310-6100-30
    onglyza® (saxagliptin) tablets
    2.5 mg
    DISPENSE WITH MEDICATION GUIDE
    Rx only
    AstraZeneca
Onglyza 2.5 Bottle Label

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How Supplied

ONGLYZA (saxagliptin) tablets have markings on both sides and are available in the strengths and packages listed in Table 16.

Table 16: ONGLYZA Tablet Presentations
Tablet
Strength
Film-Coated Tablet
Color/Shape
Tablet
Markings
Package Size NDC Code

5 mg

pink
biconvex, round

“5” on one side and “4215” on the reverse, in blue ink

Bottles of 30
Bottles of 90

0310-6105-30
0310-6105-90

2.5 mg

pale yellow to light yellow
biconvex, round

“2.5” on one side and “4214” on the reverse, in blue ink

Bottles of 30
Bottles of 90

0310-6100-30
0310-6100-90

 

Storage and Handling

Store at 20°-25°C (68°-77°F); excursions permitted to 15°-30°C (59°-86°F) [see USP Controlled Room Temperature].

 

SRC: NLM .

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