amlodipine besilate: clinical use

Prescribing considerations

• Not established as treatment for hypertensive crisis.
• Use caution in heart failure, particularly severe congestive heart failure, because pulmonary oedema has been reported more frequently.
• Exposure and elimination half-life increase with hepatic impairment; use careful selection, titration and monitoring.
• Escalation requires additional care in older people.
• Selected products support treatment of hypertension in children aged 6–17 years; evidence below 6 years is limited.

Contraindications and cautions

• Hypersensitivity to amlodipine, dihydropyridines or formulation excipients
• Severe hypotension
• Shock, including cardiogenic shock
• Left-ventricular outflow obstruction, such as high-grade aortic stenosis
• Haemodynamically unstable heart failure after acute myocardial infarction

Monitoring

• Blood pressure and clinical response
• Dizziness, symptomatic hypotension, flushing and palpitations
• Peripheral oedema and symptoms of heart failure
• Liver function when clinically indicated, particularly if jaundice or other signs of hepatic injury develop
• Tacrolimus or ciclosporin concentrations when co-administered, as appropriate

Clinical pharmacology

Amlodipine is a highly protein-bound, hepatically metabolised dihydropyridine with predominantly vascular effects, slow onset and a long terminal elimination half-life. Food does not materially affect bioavailability, renal impairment has little effect on plasma concentration, and dialysis is unlikely to remove it.

Formulation and product differences

• The referenced tablet is scored and can be divided into equal halves.
• The oral suspension requires resuspension before measurement and has specific upright, light-protected storage instructions.
• The Thame oral solutions use a supplied measuring spoon, require refrigerated storage and contain propylene glycol, glycerol and methyl parahydroxybenzoate.
• The Rosemont oral solution is supplied with an oral syringe, requires refrigerated upright storage and may be administered through compatible NG or PEG tubes as described in its product information.
• Liquid formulations are not interchangeable volume-for-volume; verify the concentration, measuring device, excipients and storage requirements.

Oral solution

Route: Oral

Strengths: 1 mg/mL, 2 mg/mL, 5 mg/5 mL, 10 mg/5 mL

Oral suspension

Route: Oral

Strengths: 1 mg/mL