Drug Action
Binds to, and activates, the GLP-1 (glucagon-like peptide-1) receptor to increase insulin secretion, suppresses glucagon secretion, and slows gastric emptying.
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Drug reference
Binds to, and activates, the GLP-1 (glucagon-like peptide-1) receptor to increase insulin secretion, suppresses glucagon secretion, and slows gastric emptying.
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Type 2 diabetes mellitus in combination with metformin or a sulfonylurea, or both, or with pioglitazone, or with both metformin and pioglitazone, in patients who have not achieved adequate glycaemic control with these drugs alone or in combination ▶BY SUBCUTANEOUS INJECTION USING IMMEDIATE-RELEASE MEDICINES ▶Adult: Initially 5 micrograms twice daily for at least 1 month, then increased if necessary up to 10 micrograms twice daily, dose to be taken within 1 hour before 2 main meals (at least 6 hours apart) ▶BY SUBCUTANEOUS INJECTION USING MODIFIED-RELEASE MEDICINES ▶Adult: 2 mg once weekly Type 2 diabetes mellitus in combination with basal insulin alone or with metformin or pioglitazone (or both) ▶BY SUBCUTANEOUS INJECTION USING IMMEDIATE-RELEASE MEDICINES ▶Adult: Initially 5 micrograms twice daily for at least 1 month, then increased if necessary up to 10 micrograms twice daily, dose to be taken within 1 hour before 2 main meals (at least 6 hours apart)
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DUE TO INTERACTIONS ▶Dose of concomitant sulfonylurea may need to be reduced.
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▶Effect of modified-release exenatide injection (Bydureon ®) may persist for 10 weeks after discontinuation.
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Ketoacidosis. severe gastro- intestinal disease
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Elderly. may cause weight loss greater than 1.5 kg weekly. pancreatitis
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Scottish Medicines Consortium (SMC) decisions SMC No. 376/07 The Scottish Medicines Consortium has advised (July 2007) that standard-release exenatide (Byetta ®) is accepted for restricted use within NHS Scotland for the treatment of type 2 diabetes in combination with metformin or sulfonylurea (or both), as an alternative to treatment with insulin in patients where treatment with metformin or sulfonylurea (or both) at maximally tolerated doses has been inadequate, and treatment with insulin would be the next option. SMC No. 684/11 The Scottish Medicines Consortium has advised (March 2011) that standard-release exenatide (Byetta ®) is accepted for restricted use within NHS Scotland for the treatment of type 2 diabetes in combination with metformin and a thiazolidinedione as a third-line pre- insulin treatment option. SMC No. 748/11 The Scottish Medicines Consortium has advised (January 2012) that modified-release exenatide (Bydureon ®) is accepted for restricted use within NHS Scotland for the treatment of type 2 diabetes as a third-line treatment option. SMC No. 785/12 The Scottish Medicines Consortium has advised (June 2012) that standard-release exenatide (Byetta ®) is accepted for use within NHS Scotland as adjunctive therapy to basal insulin with or without metformin and/or pioglitazone in patients with type 2 diabetes who have not achieved adequate glycaemic control with these agents.
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MHRA/CHM ADVICE: GLP-1 RECEPTOR AGONISTS: REPORTS OF DIABETIC KETOACIDOSIS WHEN CONCOMITANT INSULIN WAS RAPIDLY REDUCED OR DISCONTINUED (JUNE 2019) Serious and life-threatening cases of diabetic ketoacidosis have been reported in patients with type 2 diabetes mellitus on a combination of a glucagon-like peptide-1 (GLP-1) receptor agonist and insulin, particularly after discontinuation or rapid dose reduction of concomitant insulin. Healthcare professionals are advised that any dose reduction of insulin should be done in a stepwise manner with careful blood glucose self-monitoring, particularly when GLP-1 receptor agonist therapy is initiated. Patients should be informed of the risk factors for and signs and symptoms of diabetic ketoacidosis, and advised to seek immediate medical attention if these develop.
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→Appendix 1: exenatide
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▶Common or very common Appetite decreased. asthenia. constipation. diarrhoea. dizziness. gastrointestinal discomfort. gastrointestinal disorders. headache. nausea. skin reactions. vomiting ▶Uncommon Alopecia. burping. drowsiness. hyperhidrosis . renal impairment. taste altered ▶Frequency not known Angioedema. pancreatitis acute SIDE-EFFECTS, FURTHER INFORMATION Severe pancreatitis (sometimes fatal), including haemorrhagic or necrotising pancreatitis, has been reported rarely; discontinue permanently if diagnosed.
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Women of child- bearing age should use effective contraception during treatment with modified-release exenatide and for 12 weeks after discontinuation.
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Avoid—toxicity in animal studies.
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Avoid—no information available.
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For standard-release injection, use with caution if eGFR 30–50 mL/minute/1.73 m2. For standard-release injection, avoid if eGFR less than 30 mL/minute/1.73 m2. For modified-release injection, avoid if eGFR less than 50 mL/minute/1.73 m2.
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There can be variation in the licensing of different medicines containing the same drug. Solution for injection CAUTIONARY AND ADVISORY LABELS 10 ▶Byetta (AstraZeneca UK Ltd) Exenatide 250 microgram per 1 ml Byetta 5micrograms/0.02ml solution for injection 1.2ml pre-filled pens | 1 pre-filled disposable injection P £81.89 DT = £81.89 Byetta 10micrograms/0.04ml solution for injection 2.4ml pre-filled pens | 1 pre-filled disposable injection P £81.89 DT = £81.89 Powder and solvent for prolonged-release suspension for inj CAUTIONARY AND ADVISORY LABELS 10 ▶Bydureon (AstraZeneca UK Ltd) Exenatide 2 mg Bydureon 2mg powder and solvent for prolonged- release suspension for injection pre-filled pens | 4 pre-filled disposable injection P £73.36 DT = £73.36
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Patients changing from standard-release to modified-release exenatide formulation may experience initial transient increase in blood glucose. Some oral medications should be taken at least 1 hour before or 4 hours after exenatide injection— consult product literature for details. Patients or their carers should be told how to recognise signs and symptoms of pancreatitis and advised to seek prompt medical attention if symptoms such as abdominal pain, nausea, and vomiting develop. Missed doses If a dose of the immediate-release medicine is missed, continue with the next scheduled dose—do not administer after a meal.
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Initially 5 micrograms twice daily for at least
First-line fragment. Read the complete Indications and Dose section above.
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2 mg once weekly
First-line fragment. Read the complete Indications and Dose section above.
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Initially 5 micrograms twice daily for at least
First-line fragment. Read the complete Indications and Dose section above.
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