Onglyza 2.5mg Tablets
It is used to lower blood sugar in patients with high blood sugar (diabetes).
Drug Class
Antidiabetic
Pharmacologic Class
Dipeptidyl Peptidase-4 (DPP-4) Inhibitor
Pregnancy Category
Not available
FDA Approved
Jul 2009
DEA Schedule
Not Controlled
Overview
What is this medicine?
Onglyza (saxagliptin) is a medication used to help control blood sugar levels in adults with type 2 diabetes. It works by helping your body produce more insulin when your blood sugar is high and by reducing the amount of sugar your liver makes. It is usually taken once a day, with or without food.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. You can take this medication with or without food, but be sure to swallow the tablet whole. Do not chew, break, or crush it.
Continue taking your medication as instructed by your doctor or healthcare provider, even if you start to feel better. It's essential to complete the full course of treatment as prescribed.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature in a dry place, away from the bathroom. Keep all medications in a secure location, out of the reach of children and pets.
When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless specifically instructed to do so. Instead, consult with your pharmacist for guidance on the best disposal method. You may also want to check if there are any drug take-back programs available in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. You can take this medication with or without food, but be sure to swallow the tablet whole. Do not chew, break, or crush it.
Continue taking your medication as instructed by your doctor or healthcare provider, even if you start to feel better. It's essential to complete the full course of treatment as prescribed.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature in a dry place, away from the bathroom. Keep all medications in a secure location, out of the reach of children and pets.
When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless specifically instructed to do so. Instead, consult with your pharmacist for guidance on the best disposal method. You may also want to check if there are any drug take-back programs available in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Maintain a healthy diet as recommended by your doctor or dietitian.
- Engage in regular physical activity.
- Monitor blood sugar levels regularly as instructed by your healthcare provider.
- Do not skip meals.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
2.5 mg or 5 mg orally once daily
Dose Range:
2.5 - 5 mg
Condition-Specific Dosing:
Type 2 Diabetes Mellitus:
2.5 mg or 5 mg orally once daily, regardless of meals.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment necessary (CrCl > 50 mL/min)
Moderate:
2.5 mg orally once daily (CrCl ≤ 50 mL/min)
Severe:
2.5 mg orally once daily (CrCl ≤ 50 mL/min)
Dialysis:
2.5 mg orally once daily. Administer after dialysis.
Hepatic Impairment:
Mild:
No dosage adjustment necessary
Moderate:
No dosage adjustment necessary
Severe:
No dosage adjustment necessary
Pharmacology
Mechanism of Action
Saxagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor. It slows the inactivation of incretin hormones, such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), by inhibiting the DPP-4 enzyme. This increases the concentrations of active incretin hormones, which enhances glucose-dependent insulin secretion from pancreatic beta cells and decreases glucagon secretion from pancreatic alpha cells. This leads to improved glycemic control.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 67%
Tmax:
Approximately 2-4 hours (saxagliptin), 2-4 hours (active metabolite)
FoodEffect:
Food does not affect the absorption of saxagliptin.
Distribution:
Vd:
210 L (saxagliptin), 343 L (active metabolite)
ProteinBinding:
Minimal (< 4%)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 2.5 hours (saxagliptin), 3.1 hours (active metabolite)
Clearance:
Not available
ExcretionRoute:
Renal (75%), Fecal (22%)
Unchanged:
Approximately 36% (renal), 22% (fecal)
Pharmacodynamics
OnsetOfAction:
Rapid (within hours)
PeakEffect:
Within 24 hours (sustained DPP-4 inhibition)
DurationOfAction:
24 hours (due to sustained DPP-4 inhibition)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of pancreatitis (pancreas problem), such as:
+ Severe stomach pain
+ Severe back pain
+ Severe upset stomach or vomiting
Signs of a urinary tract infection (UTI), such as:
+ Blood in the urine
+ Burning or pain while urinating
+ Frequent or urgent need to urinate
+ Fever
+ Lower stomach pain
+ Pelvic pain
Low blood sugar (hypoglycemia), which may be more likely when taking this medication with other diabetes drugs. Signs include:
+ Dizziness
+ Headache
+ Feeling sleepy or weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
Contact your doctor immediately if you experience any of these symptoms. Follow your doctor's instructions for managing low blood sugar, which may include taking glucose tablets, liquid glucose, or certain fruit juices.
Heart failure, which has occurred in people taking this medication. If you have a history of heart failure or kidney problems, inform your doctor. Seek medical help right away if you experience:
+ Extreme fatigue
+ Shortness of breath
+ Significant weight gain
+ Swelling in the arms or legs
Severe and disabling joint pain. Contact your doctor immediately if you experience:
+ Very bad joint pain
+ Joint pain that does not go away
Bullous pemphigoid, a skin reaction that may require hospitalization. Seek medical help right away if you notice:
+ Blisters
+ Skin breakdown
Other Possible Side Effects
Like all medications, this drug may cause side effects. Many people experience no side effects or only mild ones. If you are bothered by any of the following side effects or if they persist, contact your doctor or seek medical help:
Headache
* Signs of a common cold
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of pancreatitis (pancreas problem), such as:
+ Severe stomach pain
+ Severe back pain
+ Severe upset stomach or vomiting
Signs of a urinary tract infection (UTI), such as:
+ Blood in the urine
+ Burning or pain while urinating
+ Frequent or urgent need to urinate
+ Fever
+ Lower stomach pain
+ Pelvic pain
Low blood sugar (hypoglycemia), which may be more likely when taking this medication with other diabetes drugs. Signs include:
+ Dizziness
+ Headache
+ Feeling sleepy or weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
Contact your doctor immediately if you experience any of these symptoms. Follow your doctor's instructions for managing low blood sugar, which may include taking glucose tablets, liquid glucose, or certain fruit juices.
Heart failure, which has occurred in people taking this medication. If you have a history of heart failure or kidney problems, inform your doctor. Seek medical help right away if you experience:
+ Extreme fatigue
+ Shortness of breath
+ Significant weight gain
+ Swelling in the arms or legs
Severe and disabling joint pain. Contact your doctor immediately if you experience:
+ Very bad joint pain
+ Joint pain that does not go away
Bullous pemphigoid, a skin reaction that may require hospitalization. Seek medical help right away if you notice:
+ Blisters
+ Skin breakdown
Other Possible Side Effects
Like all medications, this drug may cause side effects. Many people experience no side effects or only mild ones. If you are bothered by any of the following side effects or if they persist, contact your doctor or seek medical help:
Headache
* Signs of a common cold
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Symptoms of low blood sugar (hypoglycemia): sweating, shaking, dizziness, confusion, fast heartbeat, hunger. If these occur, consume a quick source of sugar (e.g., glucose tablets, fruit juice, hard candy).
- Symptoms of heart failure: unusual shortness of breath, rapid weight gain, swelling in your feet, ankles, or legs, unusual tiredness.
- Symptoms of pancreatitis: severe pain in your stomach area that may spread to your back, with or without vomiting.
- Severe joint pain.
- Severe skin reactions: blisters or erosions on the skin.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have type 1 diabetes, as this medication is not intended to treat this condition.
* If you have a condition that affects the acidity of your blood.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication in combination with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you have type 1 diabetes, as this medication is not intended to treat this condition.
* If you have a condition that affects the acidity of your blood.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication in combination with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
If you experience low blood sugar, do not operate a vehicle, as this increases the risk of an accident. Monitor your blood sugar levels as directed by your doctor to ensure safe driving and overall health.
Regularly check your blood sugar levels as instructed by your doctor. Additionally, have your blood work checked as recommended by your doctor, and discuss the results with them.
Be aware that stress, such as fever, infection, injury, or surgery, can make it more challenging to control your blood sugar levels. Changes in physical activity, exercise, or diet can also impact your blood sugar control. If you experience any of these situations, consult with your doctor.
Before consuming alcohol, discuss the potential effects with your doctor. It is crucial to follow the diet and exercise plan recommended by your doctor to maintain optimal blood sugar control.
There is a risk of developing a severe pancreas problem, known as pancreatitis, which can be life-threatening. If you have any questions or concerns, consult with your doctor.
If you are pregnant, plan to become pregnant, or are breast-feeding, inform your doctor. You and your doctor will need to discuss the benefits and risks of this medication to both you and your baby.
If you experience low blood sugar, do not operate a vehicle, as this increases the risk of an accident. Monitor your blood sugar levels as directed by your doctor to ensure safe driving and overall health.
Regularly check your blood sugar levels as instructed by your doctor. Additionally, have your blood work checked as recommended by your doctor, and discuss the results with them.
Be aware that stress, such as fever, infection, injury, or surgery, can make it more challenging to control your blood sugar levels. Changes in physical activity, exercise, or diet can also impact your blood sugar control. If you experience any of these situations, consult with your doctor.
Before consuming alcohol, discuss the potential effects with your doctor. It is crucial to follow the diet and exercise plan recommended by your doctor to maintain optimal blood sugar control.
There is a risk of developing a severe pancreas problem, known as pancreatitis, which can be life-threatening. If you have any questions or concerns, consult with your doctor.
If you are pregnant, plan to become pregnant, or are breast-feeding, inform your doctor. You and your doctor will need to discuss the benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Hypoglycemia (if co-administered with sulfonylurea or insulin)
- Gastrointestinal disturbances (e.g., nausea, vomiting, diarrhea)
- Other adverse effects seen at higher therapeutic doses
What to Do:
In case of overdose, contact a poison control center immediately (e.g., 1-800-222-1222). Supportive treatment should be initiated as dictated by the patient’s clinical status. Saxagliptin and its active metabolite are dialyzable.
Drug Interactions
Major Interactions
- Strong CYP3A4/5 inhibitors (e.g., ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin): May significantly increase saxagliptin exposure. Saxagliptin dose should be reduced to 2.5 mg once daily.
Moderate Interactions
- Moderate CYP3A4/5 inhibitors (e.g., diltiazem, erythromycin, verapamil, fluconazole): May increase saxagliptin exposure, but no dose adjustment is typically required.
Monitoring
Baseline Monitoring
Renal function (eGFR or CrCl)
Rationale: To determine appropriate starting dose and identify need for dose adjustment.
Timing: Prior to initiation
HbA1c
Rationale: To establish baseline glycemic control.
Timing: Prior to initiation
Routine Monitoring
HbA1c
Frequency: Every 3-6 months
Target: Individualized, typically <7%
Action Threshold: If target not met, consider dose adjustment or addition of other antidiabetic agents.
Renal function (eGFR or CrCl)
Frequency: Annually or more frequently if clinically indicated (e.g., in elderly or those with risk factors for renal impairment)
Target: Not applicable
Action Threshold: If CrCl ≤ 50 mL/min, reduce saxagliptin dose to 2.5 mg once daily.
Signs/symptoms of hypoglycemia (if co-administered with sulfonylurea or insulin)
Frequency: Regularly
Target: Not applicable
Action Threshold: If hypoglycemia occurs, consider reducing dose of sulfonylurea or insulin.
Symptom Monitoring
- Signs of hypoglycemia (shakiness, sweating, confusion, dizziness, hunger, rapid heartbeat)
- Signs of heart failure (unusual shortness of breath, rapid weight gain, swelling in feet/ankles/legs, unusual tiredness)
- Signs of pancreatitis (severe abdominal pain, radiating to the back, with or without vomiting)
- Signs of severe joint pain (arthralgia)
- Signs of bullous pemphigoid (blisters or erosions on the skin)
Special Patient Groups
Pregnancy
Limited data on saxagliptin use in pregnant women. Studies in animals have shown no direct harmful effects with respect to reproductive toxicity. Should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Risk not established, consider alternatives if possible.
Second Trimester:
Risk not established.
Third Trimester:
Risk not established.
Lactation
It is not known whether saxagliptin or its active metabolite are excreted in human milk. Saxagliptin is excreted in the milk of lactating rats. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Risk not established. Potential for adverse effects on the breastfed infant.
Pediatric Use
Safety and effectiveness in pediatric patients have not been established. Not recommended for use in patients younger than 18 years of age.
Geriatric Use
No dosage adjustment is recommended based on age alone. However, elderly patients are more likely to have decreased renal function, so renal function should be assessed and dose adjusted accordingly.
Clinical Information
Clinical Pearls
- Saxagliptin can be taken with or without food.
- If co-administered with a strong CYP3A4/5 inhibitor (e.g., ketoconazole), the dose of saxagliptin should be reduced to 2.5 mg once daily.
- Patients should be advised about the symptoms of hypoglycemia, especially if taking saxagliptin with a sulfonylurea or insulin.
- There have been post-marketing reports of severe and disabling arthralgia (joint pain) with DPP-4 inhibitors, including saxagliptin. Consider discontinuing the drug if severe joint pain develops.
- Cases of bullous pemphigoid requiring hospitalization have been reported with DPP-4 inhibitor use. If bullous pemphigoid is suspected, saxagliptin should be discontinued.
- The FDA has warned about an increased risk of heart failure hospitalization with saxagliptin in patients with established cardiovascular disease or multiple cardiovascular risk factors. Monitor patients for signs and symptoms of heart failure.
Alternative Therapies
- Other DPP-4 inhibitors (e.g., sitagliptin, linagliptin, alogliptin)
- Metformin
- Sulfonylureas (e.g., glipizide, glyburide, glimepiride)
- Thiazolidinediones (e.g., pioglitazone, rosiglitazone)
- SGLT2 inhibitors (e.g., empagliflozin, canagliflozin, dapagliflozin)
- GLP-1 receptor agonists (e.g., liraglutide, semaglutide, dulaglutide)
- Insulin
Cost & Coverage
Average Cost:
$400 - $550 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (Preferred or Non-Preferred Brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. This medication is accompanied by a Medication Guide, which is a crucial patient fact sheet. Please read it carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, consult your doctor, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. Be prepared to provide detailed information about the overdose, including the substance taken, the amount, and the time it occurred.