lixisenatide (Rx)

Brand and Other Names:Adlyxin
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

SC solution in prefilled pen

  • Starter dose (green pen)
    • 50mcg/mL in 3mL prefilled pen (provides 14 doses of 10mcg/dose)
  • Maintenance dose (burgundy pen)
    • 100mcg/mL in 3 mL prefilled pen (provides 14 doses of 20mcg/dose)

Type 2 Diabetes Mellitus

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

Safety and efficacy not established

Next:

Interactions

Interaction Checker

and lixisenatide

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (0)

                Monitor Closely (15)

                • acetaminophen

                  lixisenatide 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, 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 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 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, 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, 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, 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, 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, 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, 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 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.

                • mestranol

                  lixisenatide 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 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, 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, 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)

                  Previous
                  Next:

                  Adverse Effects

                  >10%

                  Nausea (25%)

                  Hypoglycemia

                  • Coadministered with basal insulin +/- sulfonylurea (47.2%)
                  • Coadministered with basal insulin +/- metformin (28.3%)
                  • Coadministered with insulin glargine and metformin +/- thiazolidinedione (22%)
                  • Coadministered with sulfonylurea +/- metformin (14.5%)

                  1-10%

                  Vomiting (10%)

                  Headache (9%)

                  Diarrhea (8%)

                  Dizziness (7%)

                  Injection site reactions (4%)

                  Dyspepsia (3.2%)

                  Constipation (2.8%)

                  Attenuated glycemic response with high antibodies (ie, >100 nmol/L) (2.4%)

                  Abdominal distension (2.2%)

                  Upper abdominal pain (2.2%)

                  Abdominal pain (2%)

                  <1%

                  Anaphylaxis (0.1%)

                  Acute pancreatitis

                  Previous
                  Next:

                  Warnings

                  Contraindications

                  Documented hypersensitivity; hypersensitivity reactions, including anaphylaxis, have occurred with lixisenatide

                  Cautions

                  Anaphylaxis (0.1%) and other hypersensitivity reactions, including angioedema, have been reported; if hypersensitivity occurs, discontinue drug and promptly seek medical attention (see Contraindications)

                  Acute pancreatitis, including fatal, and nonfatal hemorrhagic or necrotizing pancreatitis reported postmarketing in patients treated with GLP-1 receptor agonists; observe for signs and symptoms (eg, persistent severe abdominal pain that sometimes radiates to the back which may or may not be accompanied by vomiting); promptly discontinue if suspected; if pancreatitis confirmed, do not restart drug

                  Do not share pen between patients, even if the needle is changed; pen-sharing poses risk for transmission of blood-borne pathogens

                  Risk for hypoglycemia increased if coadministered with a sulfonylurea or basal insulin; risk of hypoglycemia may be lowered by a reduction in the dose of sulfonylurea (or other concomitantly administered insulin secretagogues) or insulin; inform patients using these concomitant medications of the risk of hypoglycemia and educate them on the signs and symptoms of hypoglycemia

                  Acute kidney injury and worsening of chronic renal failure (sometimes requiring hemodialysis); some reports were in patients without known underlying renal disease; most of the reports described patients who had experienced nausea, vomiting, diarrhea, or dehydration

                  Antibody development to lixisenatide occurred in 70% of patients by week 24; a subset of patients (2.4%) with the highest antibody concentrations (ie, >100 nmol/L) showed an attenuated glycemic response; a higher incidence of allergic reactions and injection site reactions occurred in antibody-positive patients

                  Clinical studies have NOT shown macrovascular risk reduction with lixisenatide or any other antidiabetic drug

                  Drug interaction overview

                  • Lixisenatide delays gastric emptying, which may affect absorption of concomitantly administered oral medications
                  • Caution if coadministered with drugs that have a narrow therapeutic index or drugs that require careful clinical monitoring; if these medications are to be administered with food, patients should take them with a meal or snack when lixisenatide is not being administered
                  • Oral medications that are particularly dependent on minimum serum concentrations (eg, antibiotics) or medications in which a delayed effect may be undesirable (pain medications) should be administered 1 hr before lixisenatide
                  • Oral contraceptives should be taken at least 1 hr before lixisenatide administration or 11 hr after lixisenatide
                  • Risk of hypoglycemia when coadministered with sulfonylurea or basal insulin; dose reduction of sulfonylurea or basal insulin may be required
                  Previous
                  Next:

                  Pregnancy

                  Pregnancy

                  Limited data available are not sufficient to inform a drug-associated risk of major birth defects and miscarriage

                  Use during pregnancy only if the benefit justifies the potential risk to the fetus

                  Clinical considerations

                  • Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic ketoacidosis, preeclampsia, spontaneous abortions, preterm delivery, stillbirth, and delivery complications
                  • Poorly control diabetes increases fetal risk for major birth defects, stillbirth, and macrosomia-related morbidity

                  Animal data

                  • Lixisenatide administered to pregnant rats and rabbits during organogenesis was associated with visceral closure and skeletal defects at systemic exposures that decreased maternal food intake and weight gain during gestation, and that are 1x and 6x higher than the 20-mcg/day clinical dose, respectively, based on plasma AUC

                  Lactation

                  Unknown if distributed in human breast milk

                  Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

                  Animal data

                  • A study in lactating rats showed low (9.4%) transfer of lixisenatide and its metabolites into milk and negligible (0.01%) levels of unchanged lixisenatide peptide in the gastric contents of weaning offspring

                  Pregnancy Categories

                  A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                  B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                  C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                  D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                  X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                  NA: Information not available.

                  Previous
                  Next:

                  Pharmacology

                  Mechanism of Action

                  Incretin mimetic; glucagonlike peptide-1 (GLP-1) receptor agonist; increases glucose-dependent insulin release, decreases glucagon secretion, and slows gastric emptying

                  Absorption

                  Peak plasma concentration time: 1-3.5 hr

                  Peak plasma concentration increased with renal impairment

                  • Mild (CrCl 60-89 mL/min): Increased by 60%
                  • Moderate (CrCl 30-59 mL/min): Increased by 42%
                  • Severe (CrCl 15-29 mL/min): Increased by 83%

                  AUC increased with renal impairment

                  • Mild (CrCl 60-89 mL/min): Increased by 34%
                  • Moderate (CrCl 30-59 mL/min): Increased by 69%
                  • Severe (CrCl 15-29 mL/min): Increased by 124%

                  Distribution

                  Vd: 100 L

                  Metabolism

                  Not metabolized by the liver

                  Elimination

                  Half-life: 3 hr

                  Clearance: 25 L/hr

                  Presumed to be eliminated through glomerular filtration and proteolytic degradation

                  Previous
                  Next:

                  Administration

                  SC Preparation

                  The pen must be activated before the first use

                  Instruct patients and caregivers on preparation and use of the pen prior to first use

                  Training should include a practice injection

                  Visually inspect solution, it should appear clear and colorless; do not use if particulate matter or coloration is observed

                  SC Administration

                  Administer by SC injection in abdomen, thigh, or upper arm once daily

                  Rotate injection sites with each dose; do not use the same site for each injection

                  Administer an injection within 1 hr before the first meal of the day, preferable the same meal each day

                  Missed dose: If a dose is missed, administer within 1 hr prior to the next meal

                  Storage

                  Before first use

                  • Keep refrigerated at 36-46°F (2-8°C)
                  • Do not freeze
                  • Protect the pen from light by keeping it in its original packaging

                  After first use

                  • Store at <86°F (30°C)
                  • Replace the pen cap after each use to protect from light
                  • Discard the pen 14 days after its first use
                  Previous
                  Next:

                  Images

                  No images available for this drug.
                  Previous
                  Next:

                  Patient Handout

                  A Patient Handout is not currently available for this monograph.
                  Previous
                  Next:

                  Formulary

                  FormularyPatient Discounts

                  Adding plans allows you to compare formulary status to other drugs in the same class.

                  To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

                  Adding plans allows you to:

                  • View the formulary and any restrictions for each plan.
                  • Manage and view all your plans together – even plans in different states.
                  • Compare formulary status to other drugs in the same class.
                  • Access your plan list on any device – mobile or desktop.

                  The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                  Tier Description
                  1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                  2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                  3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                  4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  NC NOT COVERED – Drugs that are not covered by the plan.
                  Code Definition
                  PA Prior Authorization
                  Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                  QL Quantity Limits
                  Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                  ST Step Therapy
                  Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                  OR Other Restrictions
                  Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
                  Additional Offers
                  Email to Patient

                  From:

                  To:

                  The recipient will receive more details and instructions to access this offer.

                  By clicking send, you acknowledge that you have permission to email the recipient with this information.

                  Email Forms to Patient

                  From:

                  To:

                  The recipient will receive more details and instructions to access this offer.

                  By clicking send, you acknowledge that you have permission to email the recipient with this information.

                  Previous
                  Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.