Alogliptin is an active pharmaceutical ingredient in the Dipeptidyl Peptidase 4 (Dpp-4) Inhibitors group (A10BH). The information below is compiled per regulator from the product labels on record, with direct links to the original documents.
GBOfficial regulatory label· revised May 8, 2026[1]
1 for available data on different combinations).
How to take
GBOfficial regulatory label
CACanada· Health Canada
6 products
Uses
CAOfficial regulatory label· revised March 22, 2025[2]
Monotherapy:
NESINA (alogliptin as alogliptin benzoate) is indicated for use as an adjunct to diet and exercise to improve glycemic control in adult patients with type 2 diabetes mellitus (T2DM) for whom metformin is inappropriate due to contraindications or intolerance.
1 Pediatrics Pediatrics (< 18 years of age): No data are available to Health Canada; therefore, Health Canada has not authorized an indication for pediatric use. 2 Geriatrics Geriatrics (≥ 65 years of age): No dose adjustment is necessary based on age.
However, dosing of NESINA should be conservative in patients with advanced age due to the potential for decreased renal function in this population. Any dosage adjustment should be based on an assessment of renal function. See 4 DOSAGE AND ADMINISTRATION, 7 WARNINGS AND PRECAUTIONS, and 10 CLINICAL PHARMACOLOGY.
EUEuropean Union· EMA
2 products
Uses
EUOfficial regulatory label· revised May 19, 2025[3]
Vipdomet is indicated in the treatment of adult patients aged 18 years and older with type 2 diabetes mellitus: - as an adjunct to diet and exercise to improve glycaemic control in adult patients, inadequately controlled on their maximal tolerated dose of metformin alone, or those already being treated with the combination of alogliptin and metformin.
e. triple combination therapy) as an adjunct to diet and exercise in adult patients inadequately controlled on their maximal tolerated dose of metformin and pioglitazone. e. triple combination therapy) as an adjunct to diet and exercise to improve glycaemic control in patients when insulin at a stable dose and metformin alone do not provide adequate glycaemic control.
3
How to take
USUnited States· FDA
1 product
Uses
USOfficial regulatory label· revised April 11, 2025[4]
1 INDICATIONS AND USAGE Alogliptin and metformin HCl tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Alogliptin and metformin HCl tablets are a combination of alogliptin, a dipeptidyl-peptidase-4 (DPP-4) inhibitor and metformin hydrochloride (HCl), a biguanide, indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
( 1 ) Limitations of Use: Should not be used in patients with type 1 diabetes mellitus. ( 1 ) Limitations of Use Alogliptin and metformin HCl tablets should not recommended for use in patients with type 1 diabetes mellitus.
How to take
Drug interactions
Known interactions involving Alogliptin. Select one for details. This list is informational and not a complete interaction checker.
Interaction data compiled from DDInter (academic, CC-BY). Severity classification only - this is not a complete interaction checker and not medical advice.
[2]Health Canada (DPD) · 02417189 · revised March 22, 2025
[3]European Medicines Agency · EMEA/H/C/002654 · revised May 19, 2025
[4]FDA DailyMed · 14d98490-4f8f-4d… · revised April 11, 2025 [PDF]
[5]OpenFDA adverse-event reports (US), 12 months ending June 4, 2026.
Information on this page is compiled from public regulatory records. Drugvu is not affiliated with any regulator or pharmaceutical manufacturer. This is not medical advice. Always consult a qualified healthcare professional.
5 mg and 25 mg film-coated tablets. Adults (≥ 18 years old) The recommended dose of alogliptin is one tablet of 25 mg once daily as add-on therapy to metformin, a thiazolidinedione, a sulphonylurea, or insulin or as triple therapy with metformin and a thiazolidinedione or insulin.
When alogliptin is used in combination with metformin and/or a thiazolidinedione, the dose of metformin and/or the thiazolidinedione should be maintained, and Alogliptin administered concomitantly. 4). 4). In case of hypoglycaemia, a lower dose of the thiazolidinedione or metformin may be considered.
Special populations Elderly (≥ 65 years old) No dose adjustment is necessary based on age. However, dosing of alogliptin should be conservative in patients with advanced age due to the potential for decreased renal function in this population.
2). 2). 25 mg once daily). Alogliptin may be administered without regard to the timing of dialysis. Experience in patients requiring renal dialysis is limited. 2). 4). Hepatic impairment No dose adjustment is necessary for patients with mild to moderate hepatic impairment (Child-Pugh scores of 5 to 9).
2). Paediatric population The safety and efficacy of Alogliptin in children and adolescents < 18 years old have not been established. 2, but no recommendation on a posology can be made. Alogliptin should not be used in the paediatric population because of lack of efficacy.
1. Method of administration Oral use. Alogliptin should be taken once daily with or without food. The tablets should be swallowed whole with water. If a dose is missed, it should be taken as soon as the patient remembers. A double dose should not be taken on the same day.
This is not medical advice. Consult a qualified healthcare professional.
Side effects & warnings
GBOfficial regulatory label· Adverse reactions· revised May 8, 2026[1]
5 mg alogliptin, who participated in one phase 2 or 12 phase 3 double- blind, placebo- or active- controlled clinical studies. In addition, a cardiovascular outcomes study with 5,380 patients with type 2 diabetes mellitus and a recent acute coronary syndrome event was conducted with 2,701 randomised to alogliptin and 2,679 randomised to placebo.
These studies evaluated the effects of alogliptin on glycaemic control and its safety as monotherapy, as initial combination therapy with metformin or a thiazolidinedione, and as add-on therapy to metformin, or a sulphonylurea, or a thiazolidinedione (with or without metformin or a sulphonylurea), or insulin (with or without metformin).
5 mg alogliptin, active control or placebo. The most common adverse reaction in patients treated with 25 mg alogliptin was headache. The safety of alogliptin between the elderly (≥ 65 years old) and non-elderly (< 65 years old) was similar.
Tabulated list of adverse reactions The adverse reactions are listed by system organ class and frequency. Frequencies are defined as very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000); not known (cannot be estimated from available data).
In the pooled pivotal phase 3 controlled clinical studies of alogliptin as monotherapy and as add-on combination therapy involving 5,659 patients, the observed adverse reactions are listed below (Table 1).
Table 1:
Adverse reactions System organ class Adverse reaction Frequency of adverse reactions Infections and infestations upper respiratory tract infections common nasopharyngitis common Immune system disorders hypersensitivity not known Metabolism and nutrition disorders hypoglycaemia common Nervous system disorders headache common Gastrointestinal disorders abdominal pain common gastroesophageal reflux disease common diarrhoea common acute pancreatitis not known Hepatobiliary disorders hepatic dysfunction including hepatic failure not known Skin and subcutaneous tissue disorders pruritus common rash common exfoliative skin conditions including Stevens-Johnson syndrome not known erythema multiforme not known angioedema not known urticaria not known bullous pemphigoid not known Renal and urinary disorders interstitial nephritis not known Paediatric population In a clinical trial with alogliptin in paediatric patients with type 2 diabetes mellitus aged 10 to17 years, the profile of adverse reactions was comparable to that observed in adults.
Reporting of suspected adverse reactions Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store.
GBOfficial regulatory label· Warnings and precautions· revised May 8, 2026[1]
General Alogliptin should not be used in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis. Alogliptin is not a substitute for insulin in insulin- requiring patients. 2). Combinations not studied Alogliptin has not been studied in combination with sodium glucose co-transporter 2 (SGLT- 2) inhibitors or glucagon like peptide 1 (GLP-1) analogues nor formally as triple therapy with metformin and a sulphonylurea.
2). Experience in patients requiring renal dialysis is limited. 2). 2). Cardiac failure Experience of alogliptin use in clinical studies in patients with congestive heart failure of New York Heart Association (NYHA) functional class III and IV is limited and caution is warranted in these patients.
Hypersensitivity reactions Hypersensitivity reactions, including anaphylactic reactions, angioedema and exfoliative skin conditions including Stevens-Johnson syndrome and erythema multiforme have been observed for DPP-4 inhibitors and have been spontaneously reported for alogliptin in the post- marketing setting.
In clinical studies of alogliptin, anaphylactic reactions were reported with a low incidence. Acute pancreatitis Use of DPP-4 inhibitors has been associated with a risk of developing acute pancreatitis. 5 mg alogliptin, active control or placebo were 2, 1, 1 or 0 events per 1,000 patient years, respectively.
In the cardiovascular outcomes study the rates of pancreatitis reports in patients treated with alogliptin or placebo were 3 or 2 events per 1,000 patient years, respectively. There have been spontaneously reported adverse reactions of acute pancreatitis in the post- marketing setting.
Patients should be informed of the characteristic symptom of acute pancreatitis: persistent, severe abdominal pain, which may radiate to the back. If pancreatitis is suspected, Alogliptin should be discontinued; if acute pancreatitis is confirmed, Alogliptin should not be restarted.
Caution should be exercised in patients with a history of pancreatitis. Hepatic effects Postmarketing reports of hepatic dysfunction including hepatic failure have been received. A causal relationship has not been established. Patients should be observed closely for possible liver abnormalities.
This is not medical advice. Consult a qualified healthcare professional.
Who should not take it
GBOfficial regulatory label· Contraindications· revised May 8, 2026[1]
8).
This is not medical advice. Consult a qualified healthcare professional.
How to take
CAOfficial regulatory label· revised March 22, 2025[2]
, 7 WARNINGS AND PRECAUTIONS, and 10 CLINICAL PHARMACOLOGY. 2 CONTRAINDICATIONS NESINA is contraindicated in patients who are hypersensitive to this drug or to any ingredient in the formulation, including any non-medicinal ingredient, or component of the container.
For a complete listing, see
This is not medical advice. Consult a qualified healthcare professional.
Side effects & warnings
CAOfficial regulatory label· Adverse reactions· revised March 22, 2025[2]
Driving and Operating Machinery Patients should be warned about driving or operating a vehicle or potentially dangerous machinery under conditions where a risk of hypoglycemia is present (see 7 WARNINGS AND PRECAUTIONS, Hypoglycemia).
When NESINA is used in combination with metformin and a sulfonylurea or in combination with insulin (with or without metformin) patients should be advised to take precautions to avoid hypoglycemia while driving or operating a vehicle or potentially dangerous machinery.
Endocrine and Metabolism Hypoglycemia:
As sulfonylureas and insulin are each known to cause hypoglycemia, a lower dose of sulfonylurea or insulin may be considered to reduce the risk of hypoglycemia when these drugs are used in combination with NESINA. See 4 DOSAGE AND ADMINISTRATION.
Caution should be exercised when NESINA is used in combination with metformin and pioglitazone, as an increased risk of hypoglycemia has been observed with this regimen. NESINA® alogliptin (as alogliptin benzoate) Page 8 of 52 Hepatic/Biliary/Pancreatic Hepatic: There have been post-marketing reports of fatal and non-fatal hepatic failure in patients taking NESINA, although some of the reports contain insufficient information necessary to establish the probable cause.
See 8 ADVERSE REACTIONS. Patients with type 2 diabetes may have fatty liver disease which may cause liver test abnormalities, and they may also have other forms of liver disease, many of which can be treated or managed. Therefore, obtaining a liver test panel and assessing the patient before initiating NESINA therapy is recommended.
In patients with abnormal live r tests, NESINA should be initiated with caution. Measure liver tests promptly in patients who report symptoms that may indicate liver injury, including fatigue, anorexia, right upper abdominal discomfort, dark urine or jaundice.
In this clinical context, if the patient is found to have clinically significant liver enzyme elevations and if abnormal liver tests persist or worsen, NESINA should be interrupted and investigation done to establish the probable cause.
NESINA has not been studied in patients with severe hepatic impairment (Child-Pugh score > 9) and is therefore, not recommended for use in such patients. See 4 DOSAGE AND ADMINISTRATION and 10 CLINICAL PHARMACOLOGY.
Pancreatitis:
Events of acute pancreatitis have been reported with NESINA in clinical trials and in post- marketing reports. Reports of acute pancreatitis, including fatal and non-fatal hemorrhagic or necrotizing pancreatitis, were noted in patients taking NESINA and other members of this class.
After initiation of NESINA, patients should be observed carefully for signs and symptoms of pancreatitis. If pancreatitis is suspected, NESINA should be promptly discontinued and appropriate management should be initiated. See 8 ADVERSE REACTIONS.
Immune Hypersensitivity Reactions:
Post-marketing events of serious hypersensitivity reactions in patients treated with NESINA such as anaphylaxis, angioedema, and severe cutaneous adverse reactions including Stevens - Johnson syndrome have been reported and have been associated with other DPP -4 inhibitors.
A single event of serum sickness was observed with NESINA treatment in a clinical trial. If a hypersensitivity reaction is suspected, discontinue NESINA, assess for other potential causes for the event, and institute alternative treatment for diabetes.
See 2 CONTRAINDICATIONS and 8 ADVERSE REACTIONS. Use caution in a patient with a history of angioedema with another DPP-4 inhibitor, since it is unknown whether such patients will be predisposed to angioedema with NESINA.
Immunocompromised Patients:
A dose-related mean decrease in absolute lymphocyte count was observed with other dipeptidyl peptidase 4 (DPP-4) inhibitors. When clinically indicated, such as in settings of NESINA® alogliptin (as alogliptin benzoate) Page 9 of 52 unusual or prolonged infection, lymphocyte count should be measured.
g. human immunodeficiency virus) is unknown. Immunocompromised patients, such as patients who have undergone organ transplantation or patients diagnosed with human immunodeficiency syndrome have not been studied in the alogliptin clinical program.
Therefore, the efficacy and safety profile of alogliptin in these patients has not been established.
Monitoring and Laboratory Tests Blood Glucose and HbA1c:
Response to all diabetic therapies should be monitored by periodic measurements of blood glucose and HbA1c levels, with a goal of decreasing these levels towards the normal range. HbA1c is especially useful for evaluating long-term glycemic control.
Renal Function:
Because there is a need for dose adjustment based upon re nal function, assessment of renal function is recommended prior to initiation of NESINA therapy and periodically thereafter.
Hepatic Function:
Patients with type 2 diabetes may have fatty liver disease which may cause liver test abnormalities, and they may also have other forms of liver disease, many of which can be treated or managed. Therefore, obtaining a liver test panel and assessing the patient before initiating NESINA therapy is recommended.
In patients with abnormal liver tests, NESINA should be initiated with caution. Renal As there is a need for dose adjustment in patients with moderate or severe renal impairment, or End-Stage Renal Disease (ESRD) requiring dialysis, assessment of renal function is recommended prior to initiation of NESINA and periodically thereafter.
See 4 DOSAGE AND ADMINISTRATION. Experience in patients with severe renal impairment or ESRD requiring dialysis is limited and NESINA should be used with caution in such patients. See 4 DOSAGE AND ADMINISTRATION and 10 CLINICAL PHARMACOLOGY.
Skin Bullous pemphigoid:
Post-marketing cases of bullous pemphigoid requiring hospitalization have been reported with the use of NESINA and other DPP-4 inhibitors. In reported […]
CAOfficial regulatory label· Warnings and precautions· revised March 22, 2025[2]
, Driving and Operating Machinery 02/2022 TABLE OF CONTENTS Sections or subsections that are not applicable at the time of authorization are not listed. RECENT MAJOR LABEL CHANGES............................................................................................
2 TABLE OF CONTENTS .............................................................................................................. 2 PART I: HEALTH PROFESSIONAL INFORMATION .....................................................................
6 5 OVERDOSAGE ............................................................................................................. 6 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING ................................. 6 7 WARNINGS AND PRECAUTIONS ..................................................................................
1 Special Populations .......................................................................................... 1 Pregnant Women ....................................................................................... 2 Breast-feeding............................................................................................
This is not medical advice. Consult a qualified healthcare professional.
Who should not take it
CAOfficial regulatory label· Contraindications· revised March 22, 2025[2]
NESINA is contraindicated in patients who are hypersensitive to this drug or to any ingredient in the formulation, including any non-medicinal ingredient, or component of the container. For a complete listing, see 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING.
This is not medical advice. Consult a qualified healthcare professional.
EUOfficial regulatory label· revised May 19, 2025[3]
5 mg/1 000 mg film-coated tablets. Adults (≥ 18 years old) with normal renal function (glomerular filtration rate (GFR) ≥ 90 mL/min) The dose should be individualised on the basis of the patient’s current treatment regimen. 5 mg/1 000 mg twice daily, corresponding to 25 mg alogliptin plus 1 700 mg or 2 000 mg metformin hydrochloride daily, depending on the dose of metformin hydrochloride already being taken.
5 mg twice daily (25 mg total daily dose) and metformin hydrochloride at a similar dose (either 850 mg or 1 000 mg twice daily) to that already being taken. 4). In case of hypoglycaemia, a lower dose of the thiazolidinedione or metformin may be considered.
For patients switching from separate tablets of alogliptin and metformin (as dual therapy or as part of triple therapy with insulin), both alogliptin and metformin should be dosed at the total daily dose already being taken; the individual dose of alogliptin should be halved as it will be taken twice daily whilst the dosing of metformin should remain unchanged.
5 mg twice daily (25 mg total daily dose) and a dose of metformin similar to the dose already being taken. A lower dose of insulin may be considered to reduce the risk of hypoglycaemia. Maximum daily dose The maximum recommended daily dose of 25 mg alogliptin should not be exceeded.
Special populations Elderly (≥ 65 years old) No dose adjustment is necessary based on age. However, dosing of alogliptin should be conservative in patients with advanced age due to the potential for decreased renal function in this population Renal impairment A GFR should be assessed before initiation of treatment with metformin containing medicinal products and at least annually thereafter.
g every 3-6 months. The maximum daily dose of metformin should preferably be divided into 2-3 daily doses. 4) should be reviewed before considering initiation of metformin in patients with GFR < 60 mL/min. If no adequate strength of Vipdomet is available, individual monocomponents should be used instead of the fixed dose combination.
4 GFR mL/min Metformin Alogliptin* 60-89 Maximum daily dose is 3 000 mg Dose reduction may be considered in relation to declining renal function. No dose adjustment Maximum daily dose is 25 mg 45-59 Maximum daily dose is 2 000 mg The starting dose is at most half of the maximum dose.
5 mg 30-44 Maximum daily dose is 1 000 mg. The starting dose is at most half of the maximum dose. 25 mg *Alogliptin dose adjustment is based on a pharmacokinetic study where kidney function was assessed using creatinine clearance (CrCl) levels estimated from the Cockcroft-Gault equation.
2). Paediatric population The safety and efficacy of Vipdomet in children and adolescents < 18 years old have not been established. No data are available. Method of administration Oral use. Vipdomet should be taken twice daily because of the pharmacokinetics of its metformin component.
It should also be taken with meals to reduce the gastrointestinal adverse reactions associated with metformin. The tablets should be swallowed whole with water. If a dose is missed, it should be taken as soon as the patient remembers.
A double dose should not be taken at the same time. In that case, the missed dose should be skipped.
This is not medical advice. Consult a qualified healthcare professional.
Side effects & warnings
EUOfficial regulatory label· Adverse reactions· revised May 19, 2025[3]
4). 4). 4). 4) which are attributed to Vipdomet. Clinical studies conducted to support the efficacy and safety of Vipdomet involved the co-administration of alogliptin and metformin as separate tablets. However, the results of bioequivalence studies have demonstrated that Vipdomet film-coated tablets are bioequivalent to the corresponding doses of alogliptin and metformin co-administered as separate tablets.
The information provided is based on a total of 7 150 patients with type 2 diabetes mellitus, including 4 201 patients treated with alogliptin and metformin, who participated in 7 phase 3 double-blind, placebo- or active-controlled clinical studies.
These studies evaluated the effects of co-administered alogliptin and metformin on glycaemic control and their safety as initial combination therapy, as dual therapy in patients initially treated with metformin alone, and as add-on therapy to a thiazolidinedione or insulin.
Tabulated list of adverse reactions The adverse reactions are listed by system organ class and frequency. Frequencies are defined as very common (≥ 1/10); common (≥ 1/100 to < 1/10); uncommon (≥ 1/1 000 to < 1/100); rare (≥ 1/10 000 to < 1/1 000); very rare (< 1/10 000), not known (cannot be estimated from available data).
4). Gastrointestinal symptoms occur most frequently during initiation of therapy and resolve spontaneously in most cases. These may be prevented by taking metformin in 2 daily doses during or after meals. Isolated cases of hepatitis or liver function test abnormalities resolving on discontinuation of metformin have been reported.
Reporting of suspected adverse reactions Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system listed in Appendix V.
EUOfficial regulatory label· Warnings and precautions· revised May 19, 2025[3]
General Vipdomet should not be used in patients with type 1 diabetes mellitus. Vipdomet is not a substitute for insulin in insulin-requiring patients. Lactic acidosis Lactic acidosis, a very rare but serious metabolic complication, most often occurs at acute worsening of renal function or cardiorespiratory illness or sepsis.
Metformin accumulation occurs at acute worsening of renal function and increases the risk of lactic acidosis. In case of dehydration (severe diarrhoea or vomiting, fever, heat, reduced fluid intake) Vipdomet should be temporarily discontinued and contact with a health care professional is recommended.
Medicinal products that can acutely impair renal function (such as antihypertensives, diuretics and nonsteroidal anti-inflammatory drugs (NSAIDs)) should be initiated with caution in metformin-treated patients. 5). Patients and/or care-givers should be informed on the risk of lactic acidosis.
Lactic acidosis is characterised by acidotic dyspnoea, abdominal pain, muscle cramps, asthenia and hypothermia followed by coma. In case of suspected symptoms, the patient should stop taking Vipdomet and seek immediate medical attention.
35), increased plasma lactate levels (> 5 mmol/L) and an increased anion gap and lactate/pyruvate ratio. Patients with known or suspected mitochondrial diseases In patients with known mitochondrial diseases such as Mitochondrial Encephalopathy with Lactic Acidosis, and Stroke-like episodes (MELAS) syndrome and Maternal inherited diabetes and deafness (MIDD), metformin is not recommended due to the risk of lactic acidosis exacerbation and neurologic complications which may lead to worsening of the disease.
In case of signs and symptoms suggestive of MELAS syndrome or MIDD after the intake of metformin, treatment with metformin should be withdrawn immediately and prompt diagnostic evaluation should be performed. Administration of iodinated contrast agents Intravascular administration of iodinated contrast media may lead to contrast induced nephropathy, resulting in metformin accumulation and an increased risk of lactic acidosis.
5). 2). 3). Decreased renal function in elderly patients is frequent and asymptomatic. Special caution should be exercised in situations where renal function may become impaired, for example when initiating 6 antihypertensive or diuretic therapy or when starting treatment with a nonsteroidal anti-inflammatory drug (NSAID).
This is not medical advice. Consult a qualified healthcare professional.
Who should not take it
EUOfficial regulatory label· Contraindications· revised May 19, 2025[3]
5) 5
This is not medical advice. Consult a qualified healthcare professional.
USOfficial regulatory label· revised April 11, 2025[4]
2 DOSAGE AND ADMINISTRATION Individualize the starting dosage based on the patient's current regimen. 1 ) Given orally twice daily with food. 1 ) Adjust the dosage based on effectiveness and tolerability while not exceeding the maximum recommended daily dosage of 25 mg alogliptin and 2000 mg metformin HCl.
1 ) Prior to initiation, assess renal function with estimated glomerular filtration rate (eGFR). 73 m 2 . Alogliptin and metformin HCl tablets may need to be discontinued at time of, or prior to, iodinated contrast imaging procedures.
1 Recommended Dosage Individualize the starting dosage of alogliptin and metformin HCl tablets based on the patient’s current regimen. Alogliptin and metformin HCl tablets should be taken orally twice daily with food with gradual dose escalation to reduce the gastrointestinal (GI) side effects due to metformin.
Do not split tablets. Adjust the dosage based on effectiveness and tolerability while not exceeding the maximum recommended daily dose of 25 mg alogliptin and 2000 mg metformin hydrochloride (HCl). 2 Recommendations for Use in Renal Impairment Assess renal function prior to initiation of alogliptin and metformin HCl tablets and periodically thereafter.
1) ] . 73 m 2 because these patients require a lower daily dosage of alogliptin than what is available in the fixed combination alogliptin and metformin HCl tablets product. 73 m 2 or greater. 73 m 2 ; in patients with a history of liver disease, alcoholism or heart failure; or in patients who will be administered intra-arterial iodinated contrast.
1) ] .
This is not medical advice. Consult a qualified healthcare professional.
Most-reported reactions to the US regulator (12 mo to June 4, 2026): 88 reports total. [5]
Acute Kidney Injury 7
Dyspnoea 7
Pemphigoid 7
Nausea 5
Rash 5
Renal Impairment 5
Fatigue 4
Hot Flush 4
Impaired Gastric Emptying 4
Malaise 4
Off Label Use 4
Rash Erythematous 4
Side effects & warnings
USOfficial regulatory label· Adverse reactions· revised April 11, 2025[4]
9) ] Most common adverse reactions (incidence ≥4%) are upper respiratory tract infection, nasopharyngitis, diarrhea, hypertension, headache, back pain and urinary tract infection. gov/medwatch . 1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
Alogliptin and Metformin HCl Over 2,700 patients with type 2 diabetes mellitus have received alogliptin coadministered with metformin in four large, randomized, double-blind controlled clinical trials. The racial distribution of patients exposed to trial medication was 65% White, 20% Asian, 7% Black or African American, 4% American Indian or Alaska Native, 0% Native Hawaiian/Other Pacific Islander and 4% Multiracial or other racial groups.
The ethnic distribution was 23% Hispanic or Latino and 77% was not Hispanic or Latino. The mean exposure to alogliptin and metformin HCl tablets was 58 weeks, with more than 1,400 subjects treated for more than one year. These included two 26 week placebo-controlled trials, one 52 week active control study and an interim analysis of a 104 week active-controlled trial.
In the alogliptin and metformin HCl tablets arm, the mean duration of diabetes mellitus was approximately six years, the mean body mass index (BMI) was 31 kg/m 2 (56% of patients had a BMI ≥30 kg/m 2 ) and the mean age was 55 years (18% of patients ≥65 years of age).
In a pooled analysis of these four controlled clinical studies, the overall incidence of adverse reactions was 74% in patients treated with alogliptin and metformin HCl tablets compared to 75% treated with placebo. 0% in alogliptin.
Adverse reactions reported in ≥4% of patients treated with alogliptin and metformin HCl tablets and more frequently than in patients who received alogliptin, metformin or placebo are summarized in Table 1. Table 1. 5 mg Metformin Metformin – includes data pooled for patients receiving various doses of metformin Placebo N=2794 N=222 N=1592 N=106 Upper respiratory tract infection 224 (8) 6 (3) 105 (7) 3 (3) Nasopharyngitis 191 (7) 7 (3) 93 (6) 2 (2) Diarrhea 155 (6) 4 (2) 105 (7) 3 (3) Hypertension 154 (6) 5 (2) 96 (6) 6 (6) Headache 149 (5) 11 (5) 74 (5) 3 (3) Back pain 119 (4) 1 (1) 72 (5) 1 (1) Urinary tract infection 116 (4) 4 (2) 59 (4) 2 (2) Alogliptin A total of 14,778 patients with type 2 diabetes mellitus participated in 14 randomized, double-blind, controlled clinical trials of whom 9,052 subjects were treated with alogliptin, 3,469 subjects were treated with placebo and 2,257 were treated with an active comparator.
The racial distribution of patients exposed to trial medication was 71% White, 17% Asian, 6% Black or African American, 2% American Indian or Alaska Native, 0% Native Hawaiian/Other Pacific Islander and 5% Multiracial or other racial groups.
The ethnic distribution was 30% Hispanic or Latino and 70% was not Hispanic or Latino. The mean duration of diabetes mellitus was seven years, the mean body mass index (BMI) was 31 kg/m 2 (49% of patients had a BMI ≥30 kg/m 2 ), and the mean age was 58 years (26% of patients ≥65 years of age).
The mean exposure to alogliptin was 49 weeks with 3,348 subjects treated for more than one year. In a pooled analysis of these 14 controlled clinical trials, the overall incidence of adverse reactions was 73% in patients treated with alogliptin 25 mg compared to 75% with placebo and 70% with active comparator.
2% with active comparator. Adverse reactions reported in ≥4% of patients treated with alogliptin 25 mg and more frequently than in patients who received placebo are summarized in Table 2. Table 2. 3% in the metformin HCl 1000 mg treatment groups.
9% in the placebo treatment groups. 5% in the pioglitazone 45 mg with metformin group. 8% in the glipizide with metformin group. Alogliptin Hypoglycemic events were documented based upon a blood glucose value and/or clinical signs and symptoms of hypoglycemia.
6% with placebo. The use of alogliptin as add-on therapy to glyburide or insulin did not increase the incidence of hypoglycemia compared to placebo. 4% with alogliptin compared to 26% with glipizide. 5% in patients receiving placebo. 6% of patients treated with placebo.
Metformin HCl Table 3. 8 Laboratory Abnormalities Alogliptin and Metformin HCl No clinically meaningful differences were observed among treatment groups regarding hematology, serum chemistry or urinalysis results. Metformin HCl In metformin clinical trials of 29 week duration, a decrease to subnormal levels of previously normal serum vitamin B12 levels was observed in approximately 7% of patients.
2 Postmarketing Experience The following adverse reactions have been identified during postmarketing use. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Alogliptin Gastrointestinal Disorders: acute pancreatitis, diarrhea, constipation, nausea, ileus Hepatobiliary Disorders: fulminant hepatic failure Immune System Disorders: hypersensitivity reactions including anaphylaxis Investigations: hepatic enzyme elevations Musculoskeletal and Connective Tissue Disorders: severe and disabling arthralgia, rhabdomyolysis Renal and Urinary Disorders: tubulointerstitial nephritis Skin and Subcutaneous Tissue Disorders: angioedema, rash, urticaria and severe cutaneous adverse reactions including Stevens-Johnson syndrome, bullous pemphigoid Metformin Hepatobiliary Disorders: Cholestatic, hepatocellular, mixed hepatocellular liver injury
USOfficial regulatory label· Warnings and precautions· revised April 11, 2025[4]
5 WARNINGS AND PRECAUTIONS Lactic acidosis: See boxed warning. 1 ) Pancreatitis: There have been postmarketing reports of acute pancreatitis. If pancreatitis is suspected, promptly discontinue alogliptin and metformin HCl tablets. 2 ) Heart failure: Consider the risks and benefits of alogliptin and metformin HCl tablets prior to initiating treatment in patients at risk for heart failure.
If heart failure develops, evaluate and manage according to current standards of care and consider discontinuation of alogliptin and metformin HCl tablets. 3 ) Hypersensitivity: There have been postmarketing reports of serious hypersensitivity reactions in patients treated with alogliptin such as anaphylaxis, angioedema and severe cutaneous adverse reactions, including Stevens-Johnson syndrome.
If hypersensitivity reactions occur, discontinue alogliptin and metformin HCl tablets, treat promptly and monitor until signs and symptoms resolve. 4 ) Hepatic effects: Postmarketing reports of hepatic failure, sometimes fatal. Causality cannot be excluded.
If liver injury is detected, promptly interrupt alogliptin and metformin HCl tablets and assess patient for probable cause, then treat cause if possible, to resolution or stabilization. Do not restart alogliptin and metformin HCl tablets if liver injury is confirmed and no alternative etiology can be found.
5 ) Vitamin B 12 deficiency: Metformin may lower vitamin B 12 levels. Measure hematologic parameters annually and B 12 at 2 to 3 year intervals and manage any abnormalties. 6 ) Hypoglycemia: Consider lowering the dosage of insulin secretagogue or insulin to reduce the risk of hypoglycemia when initiating Alogliptin and metformin HCl tablets.
7 ) Arthralgia: Severe and disabling arthralgia has been reported in patients taking DPP-4 inhibitors. Consider as a possible cause for severe joint pain and discontinue drug if appropriate. 8 ) Bullous pemphigoid: There have been postmarketing reports of bullous pemphigoid requiring hospitalization in patients taking DPP-4 inhibitors.
Tell patients to report development of blisters or erosions. If bullous pemphigoid is suspected, discontinue alogliptin and metformin HCl tablets. 1 Lactic Acidosis Lactic Acidosis There have been postmarketing cases of metformin-associated lactic acidosis, including fatal cases.
This is not medical advice. Consult a qualified healthcare professional.
Who should not take it
USOfficial regulatory label· Contraindications· revised April 11, 2025[4]
1) ]. Acute or chronic metabolic acidosis, including diabetic ketoacidosis with or without coma. 2) ] . 73 m 2 . ( 4 ) Metabolic acidosis, including diabetic ketoacidosis. ( 4 ) History of serious hypersensitivity to alogliptin or metformin or any of the excipients.
( 4 )
This is not medical advice. Consult a qualified healthcare professional.
Obtain liver function tests promptly in patients with symptoms suggestive of liver injury. If an abnormality is found and an alternative etiology is not established, consider discontinuation of alogliptin treatment. Bullous Pemphigoid There have been post-marketing reports of bullous pemphigoid in patients taking DPP-4 inhibitors including alogliptin.
If bullous pemphigoid is suspected, alogliptin should be discontinued. 5 mg film-coated tablets contains sodium This medicine contains less than 1 mmol sodium (23 mg) per tablet, that is to say essentially ‘sodium-free’. 5 mg film-coated tablets contains lactose monohydrate Patients with rare hereditary problems of galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take this medicine.
24 12 SPECIAL HANDLING INSTRUCTIONS........................................................................... 24 PART II: SCIENTIFIC INFORMATION ......................................................................................
44 PATIENT MEDICATION INFORMATION ................................................................................. 47 NESINA® alogliptin (as alogliptin benzoate) Page 4 of 52 PART I: HEALTH PROFESSIONAL INFORMATION 1 INDICATIONS Monotherapy: NESINA (alogliptin as alogliptin benzoate) is indicated for use as an adjunct to diet and exercise to improve glycemic control in adult patients with type 2 diabetes mellitus (T2DM) for whom metformin is inappropriate due to contraindications or intolerance.
Add-on combination: […]
Surgery As Vipdomet contains metformin it must be discontinued at the time of surgery under general, spinal or epidural anesthesia. Therapy may be restarted no earlier than 48 hours following surgery or resumption of oral nutrition and provided that renal function has been re-evaluated and found to be stable.
2). Use with other antihyperglycaemic medicinal products and hypoglycaemia Insulin is known to cause hypoglycaemia. 2). 2). Combinations not studied Vipdomet should not be used in combination with a sulphonylurea, as the safety and efficacy of this combination have not been fully established.
Change in clinical status of patients with previously controlled type 2 diabetes mellitus As Vipdomet contains metformin, any patient with type 2 diabetes mellitus previously well controlled on Vipdomet who develops laboratory abnormalities or clinical illness (especially vague and poorly defined illness) should be evaluated promptly for evidence of ketoacidosis or lactic acidosis.
Evaluation should include serum electrolytes and ketones, blood glucose and, if indicated, blood pH, lactate, pyruvate and metformin levels. If acidosis of either form occurs, Vipdomet must be stopped immediately and other appropriate corrective measures initiated.
Hypersensitivity reactions Hypersensitivity reactions, including anaphylactic reactions, angioedema and exfoliative skin conditions including Stevens-Johnson syndrome and erythema multiforme have been observed for DPP-4 inhibitors and have been spontaneously reported for alogliptin in the post-marketing setting.
In clinical studies of alogliptin, anaphylactic reactions were reported with a low incidence. 7 Acute pancreatitis Use of DPP-4 inhibitors has been associated with a risk of developing acute pancreatitis. 5 mg alogliptin, active control or placebo were 2, 1, 1 or 0 events per 1 000 patient years, respectively.
In the cardiovascular outcomes study the rates of pancreatitis reports […]
These cases had a subtle onset and were accompanied by nonspecific symptoms such as malaise, myalgias, abdominal pain, respiratory distress, or increased somnolence; however, hypothermia, hypotension and resistant bradyarrhythmias have occurred with severe acidosis.
Metformin-associated lactic acidosis was characterized by elevated blood lactate concentrations (greater than 5 mmol/L), anion gap acidosis (without evidence of ketonuria or ketonemia), and an increased lactate:pyruvate ratio; metformin plasma levels generally greater than 5 mcg/mL.
Metformin decreases liver uptake of lactate increasing lactate blood levels which may increase the risk of lactic acidosis, especially in patients at risk. If metformin-associated lactic acidosis is suspected, general supportive measures should be instituted promptly in a hospital setting, along with immediate discontinuation of alogliptin and metformin HCl tablets.
In alogliptin and metformin HCl tablets-treated patients with a diagnosis or strong suspicion of lactic acidosis, prompt hemodialysis is recommended to correct the acidosis and remove accumulated metformin (metformin HCl is dialyzable, with a clearance of up to 170 mL/min under good hemodynamic conditions).
Hemodialysis has often resulted in reversal of symptoms and recovery. Educate patients and their families about the symptoms of lactic acidosis and if these symptoms occur instruct them to discontinue alogliptin and metformin HCl tablets and report these symptoms to their healthcare provider.
For each of the known and possible risk factors for metformin-associated lactic acidosis, recommendations to reduce the risk of and manage metformin-associated lactic acidosis are provided below: Renal Impairment The postmarketing metformin-associated lactic acidosis cases primarily occurred in patients with significant renal impairment.
The risk of metformin accumulation and metformin-associated lactic acidosis increases with the severity of renal impairment because metformin is substantially excreted by the kidney. 3) ]: Before initiating alogliptin and metformin HCl tablets, obtain an eGFR.
73 m 2 [see Contraindications (4) ] . 73 m 2 because these patients require a lower dosage of alogliptin than what is available in the fixed combination alogliptin and metformin HCl tablets product. Obtain an eGFR at least annually in all patients taking alogliptin and metformin HCl tablets.
, the elderly), renal function should be assessed more frequently. Drug Interactions The concomitant use of alogliptin and metformin HCl tablets with specific drugs may increase the risk of metformin-associated lactic acidosis: those that impair renal function, result in significant hemodynamic change, interfere with acid-base balance or increase metformin accumulation [see Drug Interactions (7) ].
Therefore, consider more frequent monitoring of patients. Age 65 or Greater The risk of metformin-associated lactic acidosis increases with the patient's age because elderly patients have a greater likelihood of having hepatic, renal, or cardiac impairment than younger patients.
5) ]. Radiological Studies with Contrast Administration of intravascular iodinated contrast agents in metformin-treated patients has led to an acute decrease in renal function and the occurrence of lactic acidosis. 73 m 2 ; in patients with a history of hepatic impairment, alcoholism, or heart failure; or in patients who will be administered intra-arterial iodinated contrast.
Re-evaluate eGFR 48 hours after the imaging procedure, and restart alogliptin and metformin HCl tablets if renal function is stable. Surgery and Other Procedures Withholding of food and fluids during surgical or other procedures may increase the risk for volume depletion, hypotension and renal impairment.
Alogliptin and metformin HCl tablets should be temporarily discontinued while patients have restricted food and fluid intake. Hypoxic States Several of the postmarketing cases of metformin-associated lactic acidosis occurred in the setting of acute congestive heart failure (particularly when accompanied by hypoperfusion and hypoxemia).
Cardiovascular collapse (shock), acute myocardial infarction, sepsis, and other conditions associated with hypoxemia have been associated with lactic acidosis and may also cause prerenal azotemia. When such events occur, discontinue alogliptin and metformin HCl tablets.
Excessive Alcohol Intake Alcohol potentiates the effect of metformin on lactate metabolism and this may increase the risk of metformin-associated lactic acidosis. Warn patients against excessive alcohol intake while receiving alogliptin and metformin HCl tablets.
Hepatic Impairment Patients with hepatic impairment have developed with cases of metformin-associated lactic acidosis. This may be due to impaired lactate clearance resulting in higher lactate blood levels. Therefore, avoid use of alogliptin and metformin HCl tablets in patients with clinical or laboratory evidence of hepatic disease.
2 Pancreatitis Acute pancreatitis has been reported in the postmarketing setting and in randomized clinical trials. 1%) patients treated with active comparators or placebo. 3%) patients treated with placebo. It is unknown whether patients with a history of pancreatitis are at increased risk for pancreatitis while using alogliptin and metformin HCl tablets .
After initiation of alogliptin and metformin HCl tablets, patients should be observed for signs and symptoms of pancreatitis. If pancreatitis is suspected, alogliptin should promptly be discontinued and appropriate management should be initiated.
3%) of patients treated with placebo were hospitalized for congestive heart failure. Consider the risks and benefits of alogliptin and metformin HCl tablets prior to initiating treatment in patients at risk for heart failure, such as those with a prior history of heart failure and a history of renal impairment, and observe these patients for signs and symptoms of heart failure during therapy.
Patients should be advised of the characteristic symptoms of heart failure and should be instructed to immediately report such symptoms. If heart failure develops, evaluate and manage according to current standards of care and consider discontinuation of alogliptin and metformin HCl tablets.
2) ] . These reactions include anaphylaxis, angioedema and severe cutaneous adverse reactions, including Stevens-Johnson syndrome. If a serious hypersensitivity reaction is suspected, discontinue alogliptin and metformin HCl tablets, assess for other potential causes for the event and institute alternative treatment for diabetes mellitus.
Use caution in patients with a history of angioedema with another dipeptidyl peptidase-4 (DPP-4) inhibitor because it is unknown whether such patients will be predisposed to angioedema with alogliptin and metformin HCl tablets. 2) ].
7% of patients treated with active comparators or placebo. 8% of patients treated with placebo. Measure liver tests promptly in patients who report symptoms that may indicate liver injury, including fatigue, anorexia, right upper abdominal discomfort, dark urine or jaundice.
In this clinical context, if the patient is found to have clinically significant liver enzyme elevations and if abnormal liver tests persist or worsen, alogliptin and metformin HCl tablets should be interrupted and investigation done to establish the probable cause.
Alogliptin and metformin HCl tablets should not be restarted in these patients without another explanation for the liver test abnormalities. 6 Vitamin B 12 Levels In metformin clinical trials of 29 week duration, a decrease to subnormal levels of previously normal serum vitamin B 12 levels was observed in approximately 7% of patients.
Such decrease, possibly due to interference with B 12 absorption from the B 12 -intrinsic factor complex, may be associated with anemia but appears to be rapidly reversible with discontinuation of metformin or vitamin B 12 supplementation.
Certain individuals (those with inadequate vitamin B 12 or calcium intake or absorption) appear to be predisposed to developing subnormal vitamin B 12 levels. 1) ] . 7 Hypoglycemia with Concomitant Use with Insulin or Insulin Secretagogues Insulin and insulin secretagogues, such as sulfonylureas, are known to cause hypoglycemia.
Therefore, a lower dosage of insulin or insulin secretagogue may be required to minimize the risk of hypoglycemia when used in combination with alogliptin and metformin HCl tablets. 8 Severe and Disabling Arthralgia There have been postmarketing reports of severe and disabling arthralgia in patients taking DPP-4 inhibitors.
The time to onset of symptoms following initiation of drug therapy varied from one day to years. Patients experienced relief of symptoms upon discontinuation of the medication. A subset of patients experienced a recurrence of symptoms when restarting the same drug or a different DPP-4 inhibitor.
Consider DPP-4 inhibitors as a possible cause for severe joint pain and discontinue drug if appropriate. 9 Bullous Pemphigoid Postmarketing cases of bullous pemphigoid requiring hospitalization have been reported with DPP-4 inhibitor use.
In reported cases, patients typically recovered with topical or systemic immunosuppressive treatment and discontinuation of DPP-4 inhibitor. Tell patients to report development of blisters or erosions while receiving alogliptin and metformin HCl tablets.
If bullous pemphigoid is suspected, alogliptin and metformin HCl tablets should be discontinued and referral to a dermatologist should be considered for diagnosis and appropriate treatment.