Formulary
Exenatide: Indications, Dosing, Side Effects and Interactions
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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Exenatide: Indications, Dosing, Side Effects and Interactions
Binds to, and activates, the GLP-1 (glucagon-like peptide-1) receptor to increase insulin secretion, suppresses glucagon secretion, and slows gastric emptying.
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.
Indications and dose
**Type 2 diabetes mellitus in combination with other antidiabetic drugs (including insulin) if existing treatment fails to achieve adequate glycaemic control**
- **Adult** (By Subcutaneous Injection Using Immediate-Release Medicines): Initially 5 micrograms twice daily for at least 1 month, dose to be taken within 1 hour before 2 main meals (at least 6 hours apart), 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).
- **Adult** (By Subcutaneous Injection Using Modified-Release Medicines): 2 mg once weekly.
Cautions
Elderly; general anaesthesia or deep sedation (risk of pulmonary aspiration due to delayed gastric emptying); may cause weight loss greater than 1.5 kg weekly; pancreatitis
Contraindications
Ketoacidosis; severe gastro-intestinal disease
Side effects
Common or very common Appetite decreased; asthenia; constipation; diarrhoea; dizziness; gastrointestinal discomfort; gastrointestinal disorders; headache; nausea; skin reactions; vomiting Uncommon Alopecia; burping; drowsiness; gallbladder disorders; hyperhidrosis; hypoglycaemia; pancreatitis acute; renal impairment; taste altered Frequency not known Angioedema; pancreatitis haemorrhagic Side-effects, further information Discontinue if symptoms of acute pancreatitis occur, such as persistent, severe abdominal pain. If pancreatitis confirmed, do not restart treatment.
Interactions
**Severe interactions:**
- Gastric emptying The results of a study using paracetamol as a marker of gastric emptying suggest that the effect of prolonged-release exenatide to slow gastric emptying is minor and not expected to...
- When 1,000 mg paracetamol tablets were administered, either with or without a meal, following 14 weeks of prolonged-release exenatide therapy, no significant changes in paracetamol AUC were observed...
**Other interactions (10):**
- Paracetamol C max decreased by 16% (fasting) and 5 % (fed) and t max was increased from approximately 1 hour in the control period to 1.4 hours (fasting) and 1.3 hours (fed).
- The following interaction studies have been conducted using 10 mcg immediate-release exenatide but not prolonged-release exenatide formulations: Warfarin A delay in t max of about 2 h was observed...
- Increased INR has been spontaneously reported during concomitant use of warfarin and prolonged-release exenatide.
- INR should be monitored during initiation of prolonged-release exenatide therapy in patients on warfarin and/or cumarol derivatives (see sections 4.4 and 4.8).
- Hydroxy methyl glutaryl coenzyme A reductase inhibitors Lovastatin AUC and C max were decreased approximately 40% and 28%, respectively, and t max was delayed about 4 h when immediate-release...
- In 30-week placebo-controlled clinical studies with immediate-release exenatide, concomitant use of exenatide and HMG CoA reductase inhibitors was not associated with consistent changes in lipid...
Pregnancy
Avoid-toxicity in animal studies.
Breast feeding
Avoid-no information available.
Renal impairment
For immediate-release injection, use with caution if creatinine clearance 30-50 mL/minute; avoid if creatinine clearance less than 30 mL/minute. M For modified-release injection, avoid if eGFR less than 30 mL/minute/1.73 m 2 . M See Prescribing in renal impairment .
Medicinal forms
Medicinal forms No licensed medicines listed.
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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