lixisenatide (DSC) (Discontinued)

Type 2 Diabetes Mellitus

Discontinued: As of January 1, 2023, lixisenatide is no longer available in the U.S.

Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus

Starting dose: 10 mcg SC qDay for 14 days

Maintenance: Increase dose to 20 mcg SC qDay starting on Day 15

Dosage Modifications

Renal impairment

• Mild (CrCl 60-89 mL/min): No dosage adjustment required; monitoring for changes in renal function recommended because of a higher incidence of hypoglycemia, nausea, and vomiting observed in these patients during clinical trials
• Moderate (CrCl 30 to <60 mL/min): No dosage adjustment required; closely monitoring for adverse GI adverse effects and for changes in renal function is recommended because these symptoms may lead to dehydration and acute renal failure and worsening of chronic failure in these patients
• Severe (CrCl 15 to <30 mL/min): Data are limited; there were only 5 patients with severe renal impairment in all controlled studies; lixisenatide exposure was higher in these patients; closely monitor for GI adverse effects and for changes in renal function
• End-stage renal disease (CrCl <15 mL/min): Not recommended; no therapeutic experience

Dosing Considerations

Limitations of use

• Has not been studied in patients with chronic pancreatitis or a history of unexplained pancreatitis; consider other antidiabetic treatment options
• Not a substitute for insulin
• Not indicated for patients with type 1 DM
• Not indicated for treatment of ketoacidosis
• Concurrent use with short-acting insulin has not been studied and is not recommended
• Has not been studied with gastroparesis and is not recommended in patients with gastroparesis

Contraindicated (0)

Serious - Use Alternative (0)

Monitor Closely (16)

• acetaminophen

  lixisenatide (DSC) will decrease the level or effect of acetaminophen by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. GLP1 agonists delay gastric emptying, which may affect absorption of concomitantly administered oral medications. No effects on acetaminophen Cmax and Tmax were observed when acetaminophen was administered 1 hr before lixisenatide. When administered 1 or 4 hr after lixisenatide, acetaminophen Cmax was decreased by 29% and 31% respectively and median Tmax was delayed by 2 and 1.75 hr, respectively.

• chlorpropamide

  lixisenatide (DSC), chlorpropamide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with sulfonylureas. Sulfonylurea dosage reduction may be required.

• dienogest/estradiol valerate

  lixisenatide (DSC) will decrease the level or effect of dienogest/estradiol valerate by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. GLP1 agonists delay gastric emptying, which may affect absorption of concomitantly administered oral medications. Oral contraceptives should be taken at least 1 hr before lixisenatide administration or 11 hr after lixisenatide.

• ethinylestradiol

  lixisenatide (DSC) will decrease the level or effect of ethinylestradiol by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. GLP1 agonists delay gastric emptying, which may affect absorption of concomitantly administered oral medications. Oral contraceptives should be taken at least 1 hr before lixisenatide administration or 11 hr after lixisenatide.

• glimepiride

  lixisenatide (DSC), glimepiride. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with sulfonylureas. Sulfonylurea dosage reduction may be required.

• glipizide

  lixisenatide (DSC), glipizide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with sulfonylureas. Sulfonylurea dosage reduction may be required.

• glyburide

  lixisenatide (DSC), glyburide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with sulfonylureas. Sulfonylurea dosage reduction may be required.

• insulin degludec

  lixisenatide (DSC), insulin degludec. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with basal insulins. Basal insulin dose reduction may be required.

• insulin detemir

  lixisenatide (DSC), insulin detemir. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with basal insulins. Basal insulin dose reduction may be required.

• insulin glargine

  lixisenatide (DSC), insulin glargine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with basal insulins. Basal insulin dose reduction may be required.

• levonorgestrel oral/ethinylestradiol/ferrous bisglycinate

  lixisenatide (DSC) will decrease the level or effect of levonorgestrel oral/ethinylestradiol/ferrous bisglycinate by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. GLP1 agonists delay gastric emptying, which may affect absorption of concomitantly administered oral medications. Oral contraceptives should be taken at least 1 hr before lixisenatide administration or 11 hr after lixisenatide.

• lonapegsomatropin

  lonapegsomatropin decreases effects of lixisenatide (DSC) by Other (see comment). Use Caution/Monitor. Comment: Closely monitor blood glucose when treated with antidiabetic agents. Lonapegsomatropin may decrease insulin sensitivity, particularly at higher doses. Patients with diabetes mellitus may require adjustment of their doses of insulin and/or other antihyperglycemic agents.

• mestranol

  lixisenatide (DSC) will decrease the level or effect of mestranol by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. GLP1 agonists delay gastric emptying, which may affect absorption of concomitantly administered oral medications. Oral contraceptives should be taken at least 1 hr before lixisenatide administration or 11 hr after lixisenatide.

• somapacitan

  somapacitan decreases effects of lixisenatide (DSC) by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Growth hormone products may decrease insulin sensitivity, particularly at higher doses. Antidiabetic agents may require dose adjustment after initiating somapacitan. .

• tolazamide

  lixisenatide (DSC), tolazamide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with sulfonylureas. Sulfonylurea dosage reduction may be required.

• tolbutamide

  lixisenatide (DSC), tolbutamide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with sulfonylureas. Sulfonylurea dosage reduction may be required.

Minor (0)

• acetaminophen

  Monitor Closely (1)lixisenatide (DSC) will decrease the level or effect of acetaminophen by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. GLP1 agonists delay gastric emptying, which may affect absorption of concomitantly administered oral medications. No effects on acetaminophen Cmax and Tmax were observed when acetaminophen was administered 1 hr before lixisenatide. When administered 1 or 4 hr after lixisenatide, acetaminophen Cmax was decreased by 29% and 31% respectively and median Tmax was delayed by 2 and 1.75 hr, respectively.

• chlorpropamide

  Monitor Closely (1)lixisenatide (DSC), chlorpropamide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with sulfonylureas. Sulfonylurea dosage reduction may be required.

• dienogest/estradiol valerate

  Monitor Closely (1)lixisenatide (DSC) will decrease the level or effect of dienogest/estradiol valerate by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. GLP1 agonists delay gastric emptying, which may affect absorption of concomitantly administered oral medications. Oral contraceptives should be taken at least 1 hr before lixisenatide administration or 11 hr after lixisenatide.

• ethinylestradiol

  Monitor Closely (1)lixisenatide (DSC) will decrease the level or effect of ethinylestradiol by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. GLP1 agonists delay gastric emptying, which may affect absorption of concomitantly administered oral medications. Oral contraceptives should be taken at least 1 hr before lixisenatide administration or 11 hr after lixisenatide.

• glimepiride

  Monitor Closely (1)lixisenatide (DSC), glimepiride. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with sulfonylureas. Sulfonylurea dosage reduction may be required.

• glipizide

  Monitor Closely (1)lixisenatide (DSC), glipizide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with sulfonylureas. Sulfonylurea dosage reduction may be required.

• glyburide

  Monitor Closely (1)lixisenatide (DSC), glyburide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with sulfonylureas. Sulfonylurea dosage reduction may be required.

• insulin degludec

  Monitor Closely (1)lixisenatide (DSC), insulin degludec. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with basal insulins. Basal insulin dose reduction may be required.

• insulin detemir

  Monitor Closely (1)lixisenatide (DSC), insulin detemir. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with basal insulins. Basal insulin dose reduction may be required.

• insulin glargine

  Monitor Closely (1)lixisenatide (DSC), insulin glargine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with basal insulins. Basal insulin dose reduction may be required.

• levonorgestrel oral/ethinylestradiol/ferrous bisglycinate

  Monitor Closely (1)lixisenatide (DSC) will decrease the level or effect of levonorgestrel oral/ethinylestradiol/ferrous bisglycinate by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. GLP1 agonists delay gastric emptying, which may affect absorption of concomitantly administered oral medications. Oral contraceptives should be taken at least 1 hr before lixisenatide administration or 11 hr after lixisenatide.

• lonapegsomatropin

  Monitor Closely (1)lonapegsomatropin decreases effects of lixisenatide (DSC) by Other (see comment). Use Caution/Monitor. Comment: Closely monitor blood glucose when treated with antidiabetic agents. Lonapegsomatropin may decrease insulin sensitivity, particularly at higher doses. Patients with diabetes mellitus may require adjustment of their doses of insulin and/or other antihyperglycemic agents.

• mestranol

  Monitor Closely (1)lixisenatide (DSC) will decrease the level or effect of mestranol by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. GLP1 agonists delay gastric emptying, which may affect absorption of concomitantly administered oral medications. Oral contraceptives should be taken at least 1 hr before lixisenatide administration or 11 hr after lixisenatide.

• somapacitan

  Monitor Closely (1)somapacitan decreases effects of lixisenatide (DSC) by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Growth hormone products may decrease insulin sensitivity, particularly at higher doses. Antidiabetic agents may require dose adjustment after initiating somapacitan. .

• tolazamide

  Monitor Closely (1)lixisenatide (DSC), tolazamide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with sulfonylureas. Sulfonylurea dosage reduction may be required.

• tolbutamide

  Monitor Closely (1)lixisenatide (DSC), tolbutamide. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Risk of hypoglycemia increased when coadministered with sulfonylureas. Sulfonylurea dosage reduction may be required.