II. Indications
- Type II Diabetes Mellitus
-
Insulin deficiency and Insulin Resistance
- Adjunct to Glucophage, Sulfonylureas, Glitazones
III. Precautions
- Gliptins are less than half as effective as lower cost medications (e.g. Metformin, Sulfonylureas)
- No longterm evidence of improved outcomes
- Expensive (>$400/month)
- May consider for those close to goal AND
- Already either on other Oral Hypoglycemics or in whom they are contraindicated (e.g. Chronic Kidney Disease)
IV. Contraindications
- Type I Diabetes Mellitus
- Concurrent Insulin use
- Prior history of malignancy
- Due to increased risk of cancer invasion and metastases
- Women of child bearing age (relative contraindication)
- Teratogenicity risk
- Congestive Heart Failure
V. Adverse Effects
-
Acute Pancreatitis
- Incidence may be as high as 1 in 50 for two years
- Singh (2013) JAMA Intern Med 173(7):534-9 [PubMed]
- Serious Allergic Reaction (Sitagliptin)
- Hepatotoxicity (Vildagliptin)
-
Congestive Heart Failure exacerbation
- Risk of hospitalized CHF exacerbation: 1 in 150 patients/2 years using Saxigliptin or Alogliptin
- Sitagliptin (Januvia) is less associated with CHF exacerbation
- Scirica (2013) N Engl J Med 369(14):1317-26 [PubMed]
- Severe, persistent Joint Pain (rare)
VI. Mechanism
VII. Preparations
- Sitagliptin (Januvia)
- May be dosed with or without food
- Fewer Drug Interactions than Saxagliptin (Onglyza) and Linagliptin (Tradjenta)
- Standard dosing
- Creatinine Clearance >50 ml/min: 100 mg once daily
- Renal Insufficiency
- Consider Tradjenta instead, as does not require Renal Dosing adjustment
- Creatinine Clearance 30-49 ml/min: 50 mg once daily
- Creatinine Clearance <30 ml/min: 25 mg once daily
- Saxagliptin (Onglyza)
- Significant CYP3A4 Drug Interactions
- Adjust for renal Impairment
- CHF risk
- Linagliptin (Tradjenta)
- Significant CYP3A4 inducer and P-Glycoprotein Inducer
- No Renal Dosing required
- Alogliptin (Nesina)
- Fewer Drug Interactions than Saxagliptin (Onglyza) and Linagliptin (Tradjenta)
- Adjust for renal Impairment
- CHF risk
- First Gliptin to be generic as of 2016
VIII. Preparations: Combination
- Kanzano (Alogliptin and Metformin)
- Oseni (Alogliptin and Pioglitazone)
IX. Efficacy
- No longterm cardiovascular benefit
- Lowers HBA1C 0.6%
- Contrast with Metformin, Sulfonylureas, GLP-1 Agonists, Pioglitazone lower A1C 1.0 to 1.5% at generic costs
X. References
- (2013) Presc Lett 20(8):46
- Jones (2007) Am Fam Physician 75:1831-5 [PubMed]
- Steinberg (2019) Am Fam Physician 99(4): 237-43 [PubMed]
Images: Related links to external sites (from Bing)
Related Studies
januvia (on 6/8/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
JANUVIA 100 MG TABLET | $12.67 each | |
JANUVIA 25 MG TABLET | $12.80 each | |
JANUVIA 50 MG TABLET | $12.68 each | |
onglyza (on 2/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
ONGLYZA 2.5 MG TABLET | $12.29 each | |
ONGLYZA 5 MG TABLET | $12.34 each | |
tradjenta (on 2/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
TRADJENTA 5 MG TABLET | $12.23 each | |
alogliptin (on 4/19/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
ALOGLIPTIN 12.5 MG TABLET | Generic | $6.09 each |
ALOGLIPTIN 25 MG TABLET | Generic | $5.67 each |
ALOGLIPTIN 6.25 MG TABLET | Generic | $5.61 each |
ALOGLIPTIN-METFORMIN 12.5-1000 | Generic | $2.71 each |
ALOGLIPTIN-METFORMIN 12.5-500 | Generic | $3.00 each |
ALOGLIPTIN-PIOGLIT 25-15 MG TB | Generic | $6.44 each |
ALOGLIPTIN-PIOGLIT 25-30 MG TB | Generic | $6.48 each |
nesina (on 2/22/2017 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
NESINA 25 MG TABLET | Generic | $5.67 each |
Ontology: sitagliptin (C1565750)
Definition (NCI) | An orally available, competitive, beta-amino acid-derived inhibitor of dipeptidyl peptidase 4 (DDP-4) with hypoglycemic activity. Sitagliptin may cause an increased risk in the development of pancreatitis. |
Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
MSH | C496398 |
SnomedCT | 424106006, 423307000 |
English | 4-oxo-4-(3-(trifluoromethyl)-5,6-dihydro(1,2,4)triazolo(4,3-a)pyrazin-7(8H)-yl)-1-(2,4,5-trifluorophenyl)butan-2-amine, sitagliptin, Sitagliptin (product), Sitagliptin, Sitagliptin (substance), SITAGLIPTIN, sitagliptin [Chemical/Ingredient], sitaGLIPtin |
Spanish | sitagliptina (producto), sitagliptina, sitagliptina (sustancia) |
Ontology: Januvia (C1702177)
Concepts | Organic Chemical (T109) , Pharmacologic Substance (T121) |
MSH | C496398 |
English | Januvia |
Ontology: Dipeptidyl-Peptidase IV Inhibitors (C1827106)
Definition (MSH) | Compounds that suppress the degradation of INCRETINS by blocking the action of DIPEPTIDYL-PEPTIDASE IV. This helps to correct the defective INSULIN and GLUCAGON secretion characteristic of TYPE 2 DIABETES MELLITUS by stimulating insulin secretion and suppressing glucagon release. |
Concepts | Pharmacologic Substance (T121) |
MSH | D054873 |
SnomedCT | 423837000, 422403005 |
English | Dipeptidyl peptidase IV inhibitor, Dipeptidyl peptidase IV inhibitor (substance), Dipeptidyl peptidase IV inhibitor (product), Gliptins, Dipeptidyl Peptidase IV Inhibitors, Inhibitors, Dipeptidyl-Peptidase IV, Dipeptidyl-Peptidase IV Inhibitors, Dipeptidyl-Peptidase 4 Inhibitors, Dipeptidyl Peptidase 4 Inhibitors |
Spanish | inhibidor de dipeptidil peptidasa IV (sustancia), inhibidor de dipeptidil peptidasa IV (producto), inhibidor de dipeptidil peptidasa IV, Inhibidores de Dipeptidil-Peptidasa IV, Gliptinas |
Portuguese | Gliptinas, Inibidores da Dipeptidil Peptidase IV |
Finnish | Dipeptidyylipeptidaasi IV:n salpaajat |
French | Gliptines, Inhibiteurs de la dipeptidyl-peptidase de type 4, Inhibiteurs de la dipeptidyl-peptidase IV |
German | Gliptine, Dipeptidyl-Peptidase IV-Inhibitoren, DPP IV-Inhibitoren |
Italian | Gliptine, Inibitori della dipeptidil peptidasi IV |
Russian | DIPEPTIDIL-PEPTIDAZY IV INGIBITORY, GLIPTINY, ДИПЕПТИДИЛ-ПЕПТИДАЗЫ IV ИНГИБИТОРЫ, ГЛИПТИНЫ |
Czech | gliptiny, DPP-4 inhibitory, dipeptidylpeptidasa IV - inhibitory, inhibitory DPP-4, inhibitory dipeptidylpeptidázy 4 |
Swedish | Dipeptidylpeptidas IV-hämmare |
Polish | Inhibitory dipeptydylopeptydazy IV, Gliptyny, Inhibitory peptydazy dipeptydylowej IV |
Japanese | ジペプチジルペプチダーゼIV阻害剤, DPP-4阻害薬, DPP-IV阻害薬, ジペプチジルペプチダーゼIV阻害薬, DPP-IV阻害剤 |