- ACRONYMS AND DEFINITIONS
- DPP-4 - Dipeptidyl peptidase-4
- ER - Extended-release
- SGLT2 - Sodium-glucose co-transporter 2
- DPP-4 INHIBITORS
Alogliptin (Nesina®)
Dosage forms
Tablet
- 6.25 mg
- 12.5 mg
- 25 mg
Dosing
Type 2 diabetes
- Dosing: 25 mg once daily
- Max: 25 mg once daily
- May take without regard to food
Kidney disease
- CrCl ≥ 60 ml/min: no dosage adjustment necessary
- CrCl 30 - 59 ml/min: dose of 12.5 mg once daily should be used
- CrCl < 30 ml/min: dose of 6.25 mg once daily should be used
Liver disease
- Child-Pugh A and B: no dose adjustment is necessary
- Child-Pugh C: has not been studied
- There have been postmarketing reports of liver failure in patients taking alogliptin. No causal link between alogliptin and liver toxicity has been established. In clinical trials, the incidence of significantly elevated liver function tests with alogliptin was no different than comparator treatments.
- The manufacturer recommends checking liver function tests before initiating alogliptin therapy and if symptoms of liver toxicity occur (ex. fatigue, anorexia, right upper abdominal discomfort, dark urine or jaundice)
Generic / Price
- YES/$$-$$$Linagliptin (Tradjenta®)
Dosage forms
Tablet
- 5 mg
Dosing
Type 2 diabetes
- Dosing: 5 mg once daily
- Max: 5 mg once daily
- May take without regard to food
Kidney disease
- No dose adjustment is recommended in kidney disease
Liver disease
- No dose adjustment is recommended in liver disease
Generic / Price
- NO/$$$$Saxagliptin (Onglyza®)
Dosage forms
Tablet
- 2.5 mg
- 5 mg
Dosing
Type 2 diabetes
- Dosing: 2.5 - 5 mg once daily
- Max: 5 mg once daily
- May take without regard to food
Kidney disease
- CrCl > 50 ml/min: no dosage adjustment necessary
- CrCl ≤ 50 ml/min: dose of 2.5 mg once a day should be used
Liver disease
- No dose adjustment is recommended in liver disease
Generic / Price
- NO/$$$$Other
- Do not cut or split tablets
Sitagliptin (Januvia®)
Dosage forms
Tablet
- 25 mg
- 50 mg
- 100 mg
Dosing
Type 2 diabetes
- Dosing: 100 mg once daily
- Max: 100 mg once daily
- May take without regard to food
Kidney disease
- CrCl ≥ 45 ml/min: no dosage adjustment necessary
- CrCl 30 - 44 ml/min: dose is 50 mg once daily
- CrCl < 30 ml/min: dose is 25 mg once daily
- Postmarketing reports of kidney failure have been reported in patients taking sitagliptin. No causal link has been established. In clinical trials, sitagliptin did not adversely affect kidney function.
Liver disease
- Child-Pugh A and B: no dose adjustment is necessary
- Child-Pugh C: has not been studied extensively
Generic / Price
- NO/$$$$Janumet® (sitagliptin + metformin)
Dosage forms
Tablet
- Sitagliptin - Metformin
- 50 mg - 500 mg
- 50 mg - 1000 mg
Dosing
Type 2 diabetes
- Starting: 50/500 mg twice daily with meals
- Max: 50/1000 mg twice daily with meals
- Take with meals
Generic / Price
- NO/$$$$Other
- Do not break or cut Janumet
Janumet® XR (sitagliptin + metformin ER)
Dosage forms
Tablet, extended-release
- Sitagliptin - Metformin ER
- 50 mg - 500 mg
- 50 mg - 1000 mg
- 100 mg - 1000 mg
Dosing
Type 2 diabetes
- Starting: 100/1000 mg once daily with evening meal
- Max: 100/2000 mg once daily
- Take with evening meal
Generic / Price
- NO/$$$$Other
- Do not split, crush, or chew tablets
- There have been reports of incompletely dissolved Janumet XR tablets seen in the feces. It is not known whether this material seen in feces contains active drug. If tablet is repeatedly seen in feces, assess adequacy of glycemic control.
Jentadueto® (linagliptin + metformin)
Dosage forms
Tablet
- Linagliptin - Metformin
- 2.5 mg - 500 mg
- 2.5 mg - 850 mg
- 2.5 mg - 1000 mg
Dosing
Type 2 diabetes
- Starting: 2.5/500 mg twice daily
- Max: 2.5/1000 mg twice daily
- Take with meals
Generic / Price
- NO/$$$$Jentadueto® XR (linagliptin + metformin ER)
Dosage forms
Tablet, extended-release
- Linagliptin - Metformin ER
- 2.5 mg - 1000 mg
- 5 mg - 1000 mg
Dosing
Type 2 diabetes
- Starting: 5/1000 mg once daily with a meal
- Max: 5/2000 mg once daily
- Take with a meal
Generic / Price
- NO/$$$$Other
- Do not split, chew, crush, or dissolve tablet
- Incompletely dissolved tablets have been reported with other metformin ER products. If a tablet is seen in the feces, assess adequacy of glycemic control.
Kazano® (alogliptin + metformin)
Dosage forms
Tablet
- Alogliptin - Metformin
- 12.5 mg - 500 mg
- 12.5 mg - 1000 mg
Dosing
Type 2 diabetes
- Dosing: 12.5/500 - 12.5/1000 mg twice daily
- Max: 12.5/1000 mg twice daily
- Take with food
Generic / Price
- NO/$$$$Other
- Do not split tablets
Kombiglyze™ XR (saxagliptin + metformin ER)
Dosage forms
Tablet, extended-release
- Saxagliptin - Metformin ER
- 5 mg - 500 mg
- 5 mg - 1000 mg
- 2.5 mg - 1000 mg
Dosing
Type 2 diabetes
- Starting: 5/500 mg once daily with evening meal
- Max: saxagliptin 5 mg/day; metformin 2000 mg/day
- Take with evening meal
Generic / Price
- NO/$$$$Other
- Do not crush, cut, or chew tablets
- Occasionally, the inactive ingredients of Kombiglyze XR will be eliminated in the feces as a soft, hydrated mass that may resemble the original tablet
Oseni® (pioglitazone + alogliptin)
Dosage forms
Tablet
- Alogliptin - Pioglitazone
- 12.5 mg - 15 mg
- 12.5 mg - 30 mg
- 12.5 mg - 45 mg
- 25 mg - 15 mg
- 25 mg - 30 mg
- 25 mg - 45 mg
Dosing
Type two diabetes
- Starting: 25/15 - 25/30 mg once daily
- Max: 25/45 mg once daily
- Titrate to effect
- May take without regard to food
Generic / Price
- YES/$$$-$$$$Other
- Do not split tablets
Glyxambi® (empagliflozin + linagliptin)
Dosage forms
Tablet
- Empagliflozin - Linagliptin
- 10 mg - 5 mg
- 25 mg - 5 mg
Dosing
Type 2 diabetes
- Starting: 10/5 mg once daily
- Maintenance: 10/5 - 25/5 mg once daily
- Max: 25/5 mg once daily
- May take without regard to food
Generic / Price
- NO/$$$$Qtern® (dapagliflozin + saxagliptin)
Dosage forms
Tablet
- Dapagliflozin - Saxagliptin
- 5 mg - 5 mg
- 10 mg - 5 mg
Dosing
Type 2 diabetes
- Starting: 5/5 mg once daily
- Maintenance: 5/5 - 10/5 mg once daily
- Max: 10/5 mg once daily
- Take in the morning
- May take without regard to food
Generic / Price
- NO/$$$$Other
- Swallow whole. Do not crush, cut, or chew tablets.
- Do not use in patients with GFR < 45 ml/min
- Do not use with CYP3A4 strong inhibitors
Steglujan® (ertugliflozin + sitagliptin)
Dosage forms
Tablet
- Ertugliflozin - Sitagliptin
- 5 mg - 100 mg
- 15 mg - 100 mg
Dosing
Type 2 diabetes
- Starting: 5/100 mg once daily
- Maintenance: 5/100 - 15/100 mg once daily
- Max: 15/100 mg once daily
- Take in the morning
- May take without regard to food
Generic / Price
- NO/$$$$Trijardy® XR (empagliflozin + linagliptin + metformin ER)
Dosage forms
Tablet, extended-release
- Empagliflozin - Linagliptin - Metformin ER
- 5 mg - 2.5 mg - 1000 mg
- 10 mg - 5 mg - 1000 mg
- 12.5 mg - 2.5 mg - 1000 mg
- 25 mg - 5 mg - 1000 mg
Dosing
Type 2 diabetes
- Starting:
- For patients switching from metformin with or without linagliptin, use a dosage that gives a similar total daily dose of metformin and a total daily dose of empagliflozin 10 mg and linagliptin 5 mg
- For patients switching from metformin and any regimen containing empagliflozin with or without linagliptin, use a dosage that gives a similar total daily dose of metformin, the same total daily dose of empagliflozin, and linagliptin 5 mg
- Max: Empagliflozin 25 mg/day | Linagliptin 5 mg/day | Metformin ER 2000 mg/day
- Take once daily with a meal in the morning
Generic / Price
- NO/$$$$Other
- Swallow tablets whole. Do not crush, cut, dissolve, or chew.
- Incompletely dissolved tablets may be seen in the feces. Patients should report this finding to their healthcare provider, and the provider should assess their glycemic control.
- Kidney disease dosing
- Alogliptin (Nesina®)
- CrCl ≥ 60 ml/min: no dosage adjustment necessary
- CrCl 30 - 59 ml/min: dose of 12.5 mg once daily should be used
- CrCl < 30 ml/min: dose of 6.25 mg once daily should be used [11]
- Linagliptin (Tradjenta®)
- No dose adjustment is recommended in kidney disease [3]
- Saxagliptin (Onglyza®)
- CrCl > 50 ml/min: no dosage adjustment necessary
- CrCl ≤ 50 ml/min: dose of 2.5 mg once a day should be used [2]
- Sitagliptin (Januvia®)
- CrCl ≥ 45 ml/min: no dosage adjustment necessary
- CrCl 30 - 44 ml/min: dose is 50 mg once daily
- CrCl < 30 ml/min: dose is 25 mg once daily
- Postmarketing reports of kidney failure have been reported in patients taking sitagliptin. No causal link has been established. In clinical trials, sitagliptin did not adversely affect kidney function. [1]
- Liver disease dosing
- Alogliptin (Nesina®)
- Child-Pugh A and B: no dose adjustment is necessary
- Child-Pugh C: has not been studied
- There have been postmarketing reports of liver failure in patients taking alogliptin. No causal link between alogliptin and liver toxicity has been established. In clinical trials, the incidence of significantly elevated liver function tests with alogliptin was no different than comparator treatments.
- The manufacturer recommends checking liver function tests before initiating alogliptin therapy and if symptoms of liver toxicity occur (ex. fatigue, anorexia, right upper abdominal discomfort, dark urine or jaundice)
- Linagliptin (Tradjenta®)
- No dose adjustment is recommended in liver disease [3]
- Saxagliptin (Onglyza®)
- No dose adjustment is recommended in liver disease [2]
- Sitagliptin (Januvia®)
- Child-Pugh A and B: no dose adjustment is necessary
- Child-Pugh C: has not been studied extensively
- DRUG INTERACTIONS
- NOTE: The drug interactions presented here are NOT all-inclusive. Other interactions may exist. Drug interaction checkers provide the most efficient and practical way to check for interactions among multiple medications. A free interaction checker is available from Drugs.com (see Drugs.com interactions checker).
- Linagliptin (Tradjenta®)
- Strong CYP3A4 inducers - Strong CYP3A inducers may lower linagliptin blood levels to subtherapeutic levels. The manufacturer recommends alternative therapy.
- P-glycoprotein inducers - P-glycoprotein inducers may lower linagliptin blood levels to subtherapeutic levels. The manufacturer recommends alternative therapy.
- Saxagliptin (Onglyza®)
- Strong CYP3A4 inducers and inhibitors - The dose of saxagliptin should not exceed 2.5 mg when taken with strong CYP3A inhibitors. Strong CYP3A inducers may lower saxagliptin blood levels to subtherapeutic levels
- Sitagliptin (Januvia®)
- Digoxin - Sitagliptin may increase digoxin levels. Monitor levels closely. No dose adjustment is recommended.
| Metabolism and clearance | ||||
|---|---|---|---|---|
| Drug | CYP2C8 | CYP3A4 | P-glycoprotein | OAT |
| Alogliptin | No significant liver metabolism | - | - | |
| Linagliptin | - | Substrate and inhibitor | Substrate and inhibitor | - |
| Saxagliptin | - | Substrate | Substrate | - |
| Sitagliptin | Substrate | Substrate | Substrate | Substrate |
- PRICE ($) INFO
Pricing legend
- $ = 0 - $50
- $$ = $51 - $100
- $$$ = $101 - $150
- $$$$ = > $150
- Pricing based on one month of therapy at standard dosing in an adult
- Pricing based on information from GoodRX.com®
- Pricing may vary by region and availability
- BIBLIOGRAPHY
- Manufacturer's package insert