Adjunct to Type 2 diabetes mellitus
Adult: Initial 5 mcg bid within 1 hr before morning and evening meals (or 2 main meals of the day). Doses should be at least 6 hr apart. May increase dose to 10 mcg bid after 1 mth based on response.
Warnings / Precautions
Moderate renal impairment or renal transplantation. Not recommended in patients with severe renal impairment (CrCl<30mL/min) or end-stage renal disease. Monitor renal function during treatment. Not to be used as a substitute for insulin in insulin-requiring patients. Not to be used for treatment of Type 1 DM or diabetic ketoacidosis. May require lower dose of sulphonylureas or other glucose-dependent insulin secretogues to reduce the risk of hypoglycaemia. Not recommended for use in patients with severe GI diseases. Monitor for signs and symptoms of acute pancreatitis such as unexplained, persistent severe abdominal pain that may radiate to the back, nausea, vomiting, increased amylase or lipase levels; discontinue treatment if pancreatitis is suspected. Safety and efficacy have not been established in children and adolescents below 18 yr. Concurrent use with meglitinides or alpha-glucosidase inhibitors. Drugs that have narrow therapeutic index; require rapid GI absorption or dependent on threshold level for efficacy (e.g. proton pump inhibitor, antibiotics and oral contraceptives) should be administered at least 1 hr prior to Exenatide or when Exenatide is not administered. Use may result in weight loss. Patients may develop antibodies to Exenatide following treatment. Lactation and pregnancy.
Adverse Reactions
Hypgoglycaemia, headache, dizziness, weakness, feeling jittery, nausea, vomiting, decrease appetite, diarrhoea, abdominal distension and pain, constipation, dyspepsia, flatulence, gastro-oesophageal reflux disease, and development of anti-exenatide antibodies, inj site reactions; generalized pruritus and/or urticaria, macular or papular rash, angioedema. Has been associated with acute pancreatitis including fatal and non-fatal haemorrhagic or necrotising pancreatitis. Post marketing experience: Altered renal functions including renal insufficiency, worsening chronic renal failure, acute renal failure sometimes require haemodialysis or kidney transplantation.
Potentially Fatal: Anaphylactic reaction.
Overdose Reactions
Signs and symptoms: Nausea, severe vomiting and rapidly declining blood glucose concentrations. Proper supportive treatment should be initiated according to the patient's clinical signs and symptoms.
Drug Interactions
May reduce rate and extent of absorption of concomitant administered oral drugs. Concurrent use may reduce the AUC and peak plasma levels of paracetamol. Concomitant use of oral hypoglycaemic (e.g. sulphonylureas) may lead to increased risk of hypoglycaemia. May enhance anticoagulant effect of warfarin; monitor INR.
See Below for More exenatide Drug Interactions
Food Interactions
Caution with alcohol.
Mechanism of Actions
Exenatide is an incretin mimic that acts as an agonist at glucagon-like peptide 1 (GLP-1) receptor. It increases glucose-dependent insulin secretion by the pancreatic beta-cells, suppresses inappropriately elevated glucagon secretion, increases beta-cell growth/replication, slows gastric emptying, and decreases food intake. The drug may also reduce appeptite and promote early satiety. It is used as adjunctive therapy in Type 2 DM.
Absorption: Median peak plasma concentrations reached in about 2.1 hr. Cmax: About 211 pg/mL (following SC admin of 10 mcg dose).
Distribution: Mean Vd: About 28.3 L (following SC admin).
Metabolism: Minimal systemic metabolism.
Excretion: Primarily eliminated by glomerular filtration with subsequent proteolytic degradation. Mean apparent clearance: About 9.1 L/hr. Terminal half-life: About 2.4 hr.
Should be taken on an empty stomach. (Administer at any time w/in the 60-min period before the morning & evening meals (or before the 2 main meals of the day, approx 6 hr or more apart). Do not administer after a meal.)
Storage Conditions
Subcutaneous: Prior to initial use, refrigerate at 2-8°C (36-46°F). May be stored at room temperature ≤25°C after initial use. Discard pen 30 days after first use. Do not freeze. Protect from light.
ATC Classification
A10BX04 - exenatide ; Belongs to the class of other blood glucose lowering drugs excluding insulins. Used in the management of diabetes.
Subcutaneous: Prior to initial use, refrigerate at 2-8°C (36-46°F). May be stored at room temperature ≤25°C after initial use. Discard pen 30 days after first use. Do not freeze. Protect from light.
Available As
  • Exenatide 25 mg
  • Exenatide 5 mg
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