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Medically reviewed by Oliinyk Elizabeth Ivanovna, PharmD. Last updated on 23.05.2022
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Monotherapy: Onglyza 5 mg is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus.
Combination Therapy: Add-On Combination: Onglyza 5 mg is indicated in patients with type 2 diabetes mellitus to improve glycemic control in combination with metformin, a thiazolidinedione (TZD), a sulfonylurea (SU), or insulin (with or without metformin) when the single agent alone, with diet and exercise, does not provide adequate glycemic control.
Onglyza 5 mg is indicated in patients with type 2 diabetes mellitus to improve glycemic control in triple combination with metformin plus a sulfonylurea when the two agents, with diet and exercise, do not provide adequate glycemic control.
Initial Combination: Onglyza 5 mg is indicated for use as initial combination therapy with metformin, as an adjunct to diet and exercise, to improve glycemic control in patients with type 2 diabetes mellitus when dual Onglyza 5 mg and metformin therapy is appropriate.
Limitation of Use: Onglyza 5 mg should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.
Onglyza 5 mg is used to treat high blood sugar levels in patients with type 2 diabetes mellitus. In type 2 diabetes, the body does not store excess sugar in the normal way, so the sugar remains in the blood. If a person has high blood sugar levels for a long time, they may develop serious health problems.
Having a proper diet is the first step in managing type 2 diabetes, but medicines may be needed to help the body store excess sugar. Onglyza 5 mg helps to control blood sugar levels by making the pancreas gland release more insulin. It also signals the liver to stop producing sugar when there is too much sugar in the blood.
Onglyza 5 mg does not help patients who have insulin-dependent or type 1 diabetes. Patients with type 1 diabetes do not produce insulin from the pancreas gland. The blood sugar is controlled with insulin injections.
Onglyza 5 mg is available only with your doctor's prescription.
Onglyza 5 mg tablets must not be split or cut.
Recommended Dosage:
Initial Combination Therapy: The recommended starting doses of Onglyza 5 mg and metformin when used as initial combination therapy is 5 mg Onglyza 5 mg plus 500 mg metformin once daily. Patients with inadequate glycemic control on this starting dose should further have their metformin dose increased according to approved local label guidelines.
Renal Impairment: No dosage adjustment for Onglyza 5 mg is recommended for patients with mild renal impairment [creatinine clearance (CrCl) >50 mL/min, approximately corresponding to serum creatinine levels of <1.7 mg/dL in men and <1.5 mg/dL in women].
The dose of Onglyza 5 mg is 2.5 mg once daily for patients with moderate or severe renal impairment, or with end-stage renal disease (ESRD) requiring hemodialysis (CrCl ≤50 mL/min, approximately corresponding to serum creatinine levels of ≥1.7 mg/dL in men and ≥1.5 mg/dL in women). Onglyza 5 mg should be administered following hemodialysis. Onglyza 5 mg has not been studied in patients undergoing peritoneal dialysis.
Because there is a need for a single dosage adjustment based upon renal function, assessment of renal function is recommended prior to initiation of Onglyza 5 mg and periodically thereafter. Creatinine clearance can be estimated from serum creatinine using the Cockcroft-Gault formula.
Hepatic Impairment: No dosage adjustment for Onglyza 5 mg is necessary for patients with mild, moderate, or severe hepatic impairment.
Pediatric and Adolescent: Safety and effectiveness of Onglyza 5 mg in pediatric and adolescent patients have not been established.
Geriatric: No dosage adjustment for Onglyza 5 mg is required based solely on age. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection in the elderly based on renal function.
See also:
What is the most important information I should know about Onglyza 5 mg?
Do not use this medication if you are allergic to Onglyza 5 mg or if you are in a state of diabetic ketoacidosis (call your doctor for treatment with insulin).
Before you take Onglyza 5 mg, tell your doctor if you have kidney disease or if you are on dialysis.
You may take this medicine with or without food. Follow your doctor's instructions.
Onglyza 5 mg 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.
Use Onglyza 5 mg as directed by your doctor. Check the label on the medicine for exact dosing instructions.
- Onglyza 5 mg comes with an extra patient information sheet called a Medication Guide. Read it carefully. Read it again each time you get Onglyza 5 mg refilled.
- Take Onglyza 5 mg by mouth with or without food.
- Swallow Onglyza 5 mg whole. Do not break, crush, or chew before swallowing.
- Continue to take Onglyza 5 mg even if you feel well. Do not miss any doses.
- If you miss a dose of Onglyza 5 mg, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.
Ask your health care provider any questions you may have about how to use Onglyza 5 mg.
There are specific as well as general uses of a drug or medicine. A medicine can be used to prevent a disease, treat a disease over a period or cure a disease. It can also be used to treat the particular symptom of the disease. The drug use depends on the form the patient takes it. It may be more useful in injection form or sometimes in tablet form. The drug can be used for a single troubling symptom or a life-threatening condition. While some medications can be stopped after few days, some drugs need to be continued for prolonged period to get the benefit from it.Onglyza 5 mg is used with a proper diet and exercise program to control high blood sugar 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.
Onglyza 5 mg 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 Onglyza 5 mg
Read the Medication Guide and, if available, the Patient Information Leaflet provided by your pharmacist before you start using Onglyza 5 mg 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 manufacturer directs not to split/cut the tablet before taking it. However, many similar drugs (immediate-release tablets) can be split/cut. Follow your doctor's directions on how to take this medication.
The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).
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.
See also:
What other drugs will affect Onglyza 5 mg?
The metabolism of Onglyza 5 mg is primarily mediated by cytochrome P450 3A4/5 (CYP3A4/5).
In in vitro studies, Onglyza 5 mg and its major metabolite neither inhibited CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, or 3A4, nor induced CYP1A2, 2B6, 2C9, or 3A4. Therefore, Onglyza 5 mg is not expected to alter the metabolic clearance of coadministered drugs that are metabolized by these enzymes. Onglyza 5 mg is neither a significant inhibitor of P-glycoprotein (P-gp) nor an inducer of P-gp.
The in vitro protein binding of Onglyza 5 mg and its major metabolite in human serum is below measurable levels. Thus, protein binding would not have a meaningful influence on the pharmacokinetics of Onglyza 5 mg or other drugs.
Effect of Other Drugs on Onglyza 5 mg: In studies conducted in healthy subjects, described as follows, the pharmacokinetics of Onglyza 5 mg, its major metabolite, or the exposure to the total active components of Onglyza 5 mg (parent + metabolite), were not meaningfully altered by metformin, glyburide, pioglitazone, digoxin, simvastatin, diltiazem, ketoconazole, rifampin, omeprazole, aluminum hydroxide + magnesium hydroxide + simethicone combination, or famotidine.
Metformin: Coadministration of a single dose of Onglyza 5 mg (100 mg) and metformin (1,000 mg), an hOCT-1 and hOCT-2 substrate, decreased the Cmax of Onglyza 5 mg by 21%; however, the AUC was unchanged. Therefore, meaningful interactions of Onglyza 5 mg with other hOCT-1 and hOCT-2 substrates would not be expected.
Glyburide: Coadministration of a single dose of Onglyza 5 mg (10 mg) and glyburide (5 mg), a CYP2C9 substrate, increased the Cmax of Onglyza 5 mg by 8%; however, the AUC of Onglyza 5 mg was unchanged. Therefore, meaningful interactions of Onglyza 5 mg with other CYP2C9 substrates would not be expected.
Pioglitazone: Coadministration of multiple once-daily doses of Onglyza 5 mg (10 mg) and pioglitazone (45 mg), a CYP2C8 (major) and CYP3A4 (minor) substrate, did not alter the pharmacokinetics of Onglyza 5 mg. Therefore, meaningful interactions of Onglyza 5 mg with other CYP2C8 substrates would not be expected.
Digoxin: Coadministration of multiple once-daily doses of Onglyza 5 mg (10 mg) and digoxin (0.25 mg), a P-gp substrate, did not alter the pharmacokinetics of Onglyza 5 mg. Therefore, meaningful interactions of Onglyza 5 mg with other P-gp substrates would not be expected.
Simvastatin: Coadministration of multiple once-daily doses of Onglyza 5 mg (10 mg) and simvastatin (40 mg), a CYP3A4/5 substrate, increased the Cmax of Onglyza 5 mg by 21%; however, the AUC of Onglyza 5 mg was unchanged. Therefore, meaningful interactions of Onglyza 5 mg would not be expected with other substrates of CYP3A4/5.
Diltiazem: Coadministration of a single dose of Onglyza 5 mg (10 mg) and diltiazem (360 mg long-acting formulation at steady state), a moderate inhibitor of CYP3A4/5, increased the Cmax of Onglyza 5 mg by 63% and the AUC for the total active components of Onglyza 5 mg by 21%. Therefore, meaningful interactions of Onglyza 5 mg with other moderate CYP3A4/5 inhibitors would not be expected.
Ketoconazole: Coadministration of a single dose of Onglyza 5 mg (100 mg) and ketoconazole (200 mg every 12 hours at steady state), a potent inhibitor of CYP3A4/5 and P-gp, increased the Cmax for Onglyza 5 mg by 62% and the AUC for the total active components of Onglyza 5 mg by 13%. Therefore, meaningful interactions of Onglyza 5 mg would not be expected with other potent CYP3A4/5 and P-gp inhibitors.
Rifampin (Rifampicin): Coadministration of a single dose of Onglyza 5 mg (5 mg) and rifampin (600 mg once daily to steady state), a potent inducer of CYP3A4/5 and P-gp, decreased the Cmax for Onglyza 5 mg by 53% and the AUC for the total active components of Onglyza 5 mg by 26%. The plasma DPP4 activity inhibition by Onglyza 5 mg over a dose interval (24 h) was not meaningfully affected by the coadministration of rifampin.
Omeprazole: Coadministration of multiple once-daily doses of Onglyza 5 mg (10 mg) and omeprazole (40 mg), a CYP2C19 (major) and CYP3A4 substrate, an inhibitor of CYP2C19, and an inducer of MRP-3, did not alter the pharmacokinetics of Onglyza 5 mg. Therefore, meaningful interactions of Onglyza 5 mg with other CYP2C19 inhibitors or MRP-3 inducers would not be expected.
Aluminum Hydroxide + Magnesium Hydroxide + Simethicone: Coadministration of a single dose of Onglyza 5 mg (10 mg) and a liquid containing aluminum hydroxide (2,400 mg), magnesium hydroxide (2,400 mg), and simethicone (240 mg) decreased the Cmax of Onglyza 5 mg by 26%; however, the AUC of Onglyza 5 mg was unchanged. Therefore, meaningful interactions of Onglyza 5 mg with antacid and anti-gas formulations of this type would not be expected.
Famotidine: Administration of a single dose of Onglyza 5 mg (10 mg) three hours after a single dose of famotidine (40 mg), an inhibitor of hOCT-1, hOCT-2, and hOCT-3, increased the Cmax of Onglyza 5 mg by 14%; however, the AUC of Onglyza 5 mg was unchanged. Therefore, meaningful interactions of Onglyza 5 mg would not be expected with other inhibitors of hOCT-1, hOCT-2, and hOCT-3.
Effect of Onglyza 5 mg on Other Drugs: In studies conducted in healthy subjects, described as follows, Onglyza 5 mg did not meaningfully alter the pharmacokinetics of metformin, glyburide, pioglitazone, digoxin, simvastatin, diltiazem, ketoconazole, or an estrogen/progestin combined oral contraceptive.
Metformin: Coadministration of a single dose of Onglyza 5 mg (100 mg) and metformin (1,000 mg), an hOCT-1 and hOCT-2 substrate, did not alter the pharmacokinetics of metformin in healthy subjects. Therefore, Onglyza 5 mg is not an inhibitor of hOCT-1 and hOCT-2-mediated transport.
Glyburide: Coadministration of a single dose of Onglyza 5 mg (10 mg) and glyburide (5 mg), a CYP2C9 substrate, increased the plasma Cmax of glyburide by 16%; however, the AUC of glyburide was unchanged. Therefore, Onglyza 5 mg does not meaningfully inhibit CYP2C9-mediated metabolism.
Pioglitazone: Coadministration of multiple once-daily doses Onglyza 5 mg (10 mg) and pioglitazone (45 mg), a CYP2C8 substrate, increased the plasma Cmax of pioglitazone by 14%; however, the AUC of pioglitazone was unchanged. Therefore, Onglyza 5 mg does not meaningfully inhibit or induce CYP2C8-mediated metabolism.
Digoxin: Coadministration of multiple once-daily doses of Onglyza 5 mg (10 mg) and digoxin (0.25 mg), a P-gp substrate, did not alter the pharmacokinetics of digoxin. Therefore, Onglyza 5 mg is not an inhibitor or inducer of P-gp-mediated transport.
Simvastatin: Coadministration of multiple once-daily doses of Onglyza 5 mg (10 mg) and simvastatin (40 mg), a CYP3A4/5 substrate, did not alter the pharmacokinetics of simvastatin. Therefore, Onglyza 5 mg is not an inhibitor or inducer of CYP3A4/5-mediated metabolism.
Diltiazem: Coadministration of multiple once-daily doses of Onglyza 5 mg (10 mg) and diltiazem (360 mg long-acting formulation at steady state), a moderate inhibitor of CYP3A4/5, increased the plasma Cmax of diltiazem by 16%; however, the AUC of diltiazem was unchanged. Therefore, Onglyza 5 mg would not be expected to meaningfully alter the pharmacokinetics of moderate CYP3A4/5 inhibitors.
Ketoconazole: Coadministration of a single dose of Onglyza 5 mg (100 mg) and multiple doses of ketoconazole (200 mg every 12 hours at steady state), a potent inhibitor of CYP3A4/5 and P-gp, decreased the plasma Cmax and AUC of ketoconazole by 16% and 13%, respectively. Therefore, Onglyza 5 mg would not be expected to meaningfully alter the pharmacokinetics of potent CYP3A4/5 and P-gp inhibitors.
Oral Contraceptives:
Other Interactions: The effects of smoking, diet, herbal products, and alcohol use on the pharmacokinetics of Onglyza 5 mg have not been specifically studied.
See also:
What are the possible side effects of Onglyza 5 mg?
Clinical Trials: In randomized, controlled, double-blind clinical trials, over 17.000 patients with type 2 diabetes have been treated with Onglyza 5 mg.
Adverse Reactions Associated with Onglyza 5 mg in the SAVOR Trial: The SAVOR trial included 8240 patients treated with Onglyza 5 mg 5 mg or 2.5 mg once daily and 8173 patients on placebo. The mean duration of Onglyza 5 mg exposure regardless of interruptions was 1.8 years. A total of 3698 subjects (45%) were treated with Onglyza 5 mg for between 2 and 3 years.
The overall incidence of adverse events in patients treated with Onglyza 5 mg in this trial was similar to placebo (72.5% versus 72.2%, respectively). Discontinuation of therapy due to adverse events was similar between the two treatment groups [4.9% in the Onglyza 5 mg group and 5.0% in the placebo group].
The cardiovascular safety of Onglyza 5 mg was evaluated in the SAVOR trial which established that Onglyza 5 mg did not increase the cardiovascular risk (CV death, nonfatal MI, or nonfatal ischemic stroke) in patients with type 2 diabetes mellitus (T2DM) compared to placebo when added to current background therapy [Hazard Ratio (HR) 1.00; 95% Confidence Interval (CI): 0.89, 1.12; P<0.001 for noninferiority]..
In the SAVOR trial, the incidence of adjudicated pancreatitis events was 0.3% in both Onglyza 5 mg-treated patients and placebo-treated patients in the intent-to-treat population.
The incidence of hypersensitivity reactions was 1.1% in both Onglyza 5 mg-treated patientsand placebo-treated patients.
Hypoglycemia: In the SAVOR trial, the overall incidence of reported hypoglycemia (recorded in daily patient diaries) was 17.1% in Onglyza 5 mg-treated patients and 14.8% in placebo-treated patients.
The percent of subjects with reported on-treatment events of major hypoglycemia (defined as an event that required assistance of another person) was higher in the Onglyza 5 mg group than in the placebo group (2.1% and 1.6%, respectively).
The increased risk of overall hypoglycemia and major hypoglycemia observed in the Onglyza 5 mg-treated group occurred primarily in subjects treated with a sulfonylurea at baseline and not in subjects on insulin or metformin monotherapy at baseline.
The increased risk of overall and major hypoglycemia was primarily observed in subjects with A1C <7% at baseline.
Adverse Reactions Related to Onglyza 5 mg in Studies of Glycemic Control: There were 4148 patients with type 2 diabetes randomized, including 3021 patients treated with Onglyza 5 mg, in six, double-blind, controlled clinical safety and efficacy studies conducted to evaluate the effects of Onglyza 5 mg on glycemic control.
In a pre-specified pooled analysis of the two monotherapy studies, the add-on to metformin study, the add-on to TZD study, and the add-on to glyburide study, the overall incidence of adverse events in patients treated with Onglyza 5 mg 5 mg was similar to placebo. Discontinuation of therapy due to adverse events was higher in patients who received Onglyza 5 mg 5 mg as compared to placebo (3.3% as compared to 1.8%).
The adverse reactions reported in patients treated with Onglyza 5 mg are shown in Table 10. The adverse reactions are listed by system organ class and absolute frequency. Frequencies are defined as very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1,000, <1/100), rare (≥1/10,000, <1/1,000), or very rare (<1/10,000).
A grouping of hypersensitivity-related events in the 5-study pooled analysis up to Week 24 showed an incidence of 1.5% and 0.4% in patients who received Onglyza 5 mg 5 mg and placebo, respectively. None of these events in patients who received Onglyza 5 mg required hospitalization or were reported to be life-threatening by the investigators.
Adverse Reactions Associated with Onglyza 5 mg and Concomitant Therapy in Studies of Glycemic Control: In the add-on to glibenclamide (glyburide) study, the incidence of confirmed hypoglycemia (defined as symptoms of hypoglycemia accompanied by a fingerstick glucose value of ≤50 mg/dL) was uncommon for Onglyza 5 mg 5 mg (0.8%) and placebo (0.7%). In the two monotherapy studies, the add-on to metformin study, and the add-on to TZD study, the incidence of adverse reactions of confirmed hypoglycemia in patients treated with Onglyza 5 mg 5 mg was similar to placebo.
In the add-on to insulin study, the overall incidence of reported hypoglycemia was 18.4% for Onglyza 5 mg 5 mg and 19.9% for placebo. The incidence of confirmed hypoglycemia for Onglyza 5 mg 5 mg was 5.3% versus 3.3% for placebo.
In the add-on to combination with metformin plus SU study, the overall incidence of reported hypoglycemia was 10.1% for Onglyza 5 mg 5 mg and 6.3% for placebo. Confirmed hypoglycemia was reported in 1.6% of the Onglyza 5 mg-treated patients and in none of the placebo-treated patients.
In the add-on to TZD study, the incidence of peripheral edema was common and higher for Onglyza 5 mg 5 mg as compared to placebo (8.1% as compared to 4.3%). All of the reported adverse reactions of peripheral edema were of mild to moderate intensity and none resulted in study drug discontinuation. In a pooled analysis of the two monotherapy studies, the add-on to metformin study, and the add-on to SU study, the overall incidence of adverse reactions of peripheral edema observed in patients treated with Onglyza 5 mg 5 mg was similar to placebo (1.7% as compared to 2.4%).
In the initial combination of Onglyza 5 mg 5 mg with metformin therapy, the incidence of nasopharyngitis was common and higher for Onglyza 5 mg plus metformin (6.9%) as compared to Onglyza 5 mg 10 mg (4.2%) and metformin alone (4.0%). The incidence of headache was common and higher for Onglyza 5 mg 5 mg plus metformin (7.5%) as compared to Onglyza 5 mg 10 mg (6.3%) and metformin alone (5.2%).
Postmarketing Experience: During postmarketing experience, the following adverse reactions have been reported with use of Onglyza 5 mg: Acute pancreatitis, arthralgia and hypersensitivity reactions, including anaphylaxis, angioedema, rash, and urticaria. Because these reactions are reported voluntarily from a population of uncertain size, it is not possible to reliably estimate their frequency.
Laboratory Findings: Across clinical studies, the incidence of laboratory adverse events was similar in patients treated with Onglyza 5 mg 5 mg compared to patients treated with placebo. A small decrease in absolute lymphocyte count was observed. From a baseline mean absolute lymphocyte count of approximately 2,200 cells/microL, a mean decrease of approximately 100 cells/microL relative to placebo was observed in a pooled analysis of five placebo-controlled clinical studies. Mean absolute lymphocyte counts remained stable and within normal limits with daily dosing up to 102 weeks in duration. The decreases in lymphocyte count were not associated with clinically relevant adverse reactions. The clinical significance of this decrease in lymphocyte count relative to placebo is not known.
In the SAVOR trial, decreased lymphocyte counts were reported in 0.5% of Onglyza 5 mg-treated patients and 0.4% of placebo-treated patients.
Each film-coated tablet of Onglyza 5 mg for oral use contains either 2.79 mg Onglyza 5 mg hydrochloride (anhydrous) equivalent to 2.5 mg Onglyza 5 mg or 5.58 mg Onglyza 5 mg hydrochloride (anhydrous) equivalent to 5 mg Onglyza 5 mg.
Onglyza 5 mg is an orally-active inhibitor of the DPP4 enzyme.
Onglyza 5 mg 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 andthe molecular weight is 333.43.
Onglyza 5 mg 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).
Excipients/Inactive Ingredients: Lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, and magnesium stearate.
Film coating: Polyvinyl alcohol, polyethylene glycol, titanium dioxide, talc, and iron oxides.