Sitagliptin
Indications
Sitagliptin is used for:
Type 2 diabetes mellitus
Adult Dose
Oral
Type 2 diabetes mellitus
Adult: 100 mg once daily.
Hepatic impairment
Mild to moderate impairment: Dose adjustment not necessary
Severe impairment: Not studied
Child Dose
Safety and efficacy not established
Renal Dose
Renal impairment
CrCl >50 mL/min: Dose adjustment not necessary
CrCl 30-50 mL/min: 50 mg PO qDay
CrCl <30 mL/min: 25 mg PO qDay
ESRD: 25 mg PO qDay regardless of hemodialysis
Administration
May be taken with or without food.
Contra Indications
Hypersensitivity reactions such as anaphylaxis, angioedema, and exfoliative skin conditions including Stevens-Johnson syndrome can occur. Type 1 diabetes. Diabetic ketoacidosis.
Precautions
Patient w/ type 1 diabetes, history of angioedema. Not intended for the treatment of diabetic ketoacidosis. Moderate and severe renal impairment. Pregnancy and lactation. Monitoring Parameters Monitor glycosylated Hb (HbA1c), serum glucose. Assess renal function prior to initiation of therapy and periodically thereafter.
Lactation: Not known whether excreted in breast milk: use caution
Pregnancy-Lactation
Pregnancy
Limited available data in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy; no adverse developmental effects were observed when sitagliptin was administered to pregnant rats and rabbits during organogenesis at oral doses up to 30-times and 20-times, respectively, the 100 mg clinical dose, based on AUC
Poorly controlled diabetes in pregnancy increases maternal risk for diabetic ketoacidosis, preeclampsia, spontaneous abortions, preterm delivery, still birth, and delivery complications; poorly controlled diabetes increases fetal risk for major birth defects, still birth, and macrosomia related morbidity
Lactation
There is no information regarding presence of drug in human milk, effects on breastfed infant, or on milk production; drug is present in rat milk and therefore possibly present in human; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from therapy or from the underlying maternal condition
Interactions
Increased risk of hypoglycaemia when used in combination w/ sulfonylureas or insulin.
Side Effects
Side effects of Sitagliptin :
1-10%
Nasopharyngitis (5%), Diarrhea (4%), Headache (3.6%), Constipation (3%), Peripheral edema (2%), Nausea (2%), Pharyngitis (1%), Osteoarthritis (1%), URI (1%)
<1%
Hypersensitivity reactions such as anaphylaxis, angioedema, rash, urticaria, cutaneous vasculitis, and exfoliative skin conditions (including Stevens-Johnson syndrome)
Hepatic enzyme elevations, Acute pancreatitis, including fatal and nonfatal hemorrhagic and necrotizing pancreatitis.Constipation.Vomiting.Worsening renal function, including acute renal failure (sometimes requiring dialysis), Severe and disabling arthralgia, Myalgia, Pain in extremity, Back pain
Mode of Action
Sitagliptin inhibits dipeptidyl peptidase IV (DPP-IV), resulting in prolonged active incretin levels. Incretin hormones increases insulin synthesis and release from pancreatic beta-cells and reduces glucagon secretion from pancreatic beta-cells. Reduced glucagon secretion leads to decreased hepatic glucose production.