Amlodipine + Benazepril


Concise Prescribing Info
Indications/Uses
HTN.
Dosage/Direction for Use
Adult : PO Each cap contains amlodipine (mg)/benazepril (mg): 2.5/10, 5/10, 5/20, 5/40, 10/20 or 10/40: Initial: 2.5 mg/10 mg once daily, may be titrated according to response. Max: Amlodipine 10 mg and benazepril 40 mg once daily.
Dosage Details
Oral
Hypertension
Adult: Each cap contains amlodipine (mg)/benazepril (mg): 2.5/10, 5/10, 5/20, 5/40, 10/20 or 10/40: Initially, 2.5 mg/10 mg once daily, may be titrated according to clinical response. Max: Amlodipine 10 mg and benazepril 40 mg once daily.
Elderly: Start w/ 2.5 mg amlodipine component once daily.
Renal Impairment
CrCl ≤30 mL/min: Contraindicated.
Hepatic Impairment
Start w/ 2.5 mg amlodipine component once daily.
Administration
May be taken with or without food.
Contraindications
History of angioedema. Concomitant use w/ aliskiren esp in patient w/ DM. Severe renal impairment (CrCl ≤30 mL/min). Pregnancy and lactation.
Special Precautions
Patient w/ severe obstructive coronary artery disease, aortic/mitral stenosis, obstructive hypertrophic cardiomyopathy, volume and salt depletion, CHF w/ or w/o renal insufficiency, DM, collagen vascular disease (e.g. SLE), severe heart failure, MI. Patient undergoing surgery or during anaesthesia. Hepatic and severe renal impairment. Elderly.
Adverse Reactions
Cough, peripheral oedema, angioedema, headache, dizziness; asthenia, fatigue; insomnia, nervousness, anxiety, tremor, decreased libido; flushing, hot flashes, rash, skin nodule, dermatitis; dry mouth, nausea, abdominal pain, constipation, diarrhoea, dyspepsia, oesophagitis, neutropenia; hypokalaemia, back and musculoskeletal pain, muscle cramps; pharyngitis, impotence, polyuria.
MonitoringParameters
Monitor BUN, serum creatinine, electrolytes, and BP.
Drug Interactions
Increased risk of hyperkalaemia w/ K supplements and K-sparing diuretics. Increased amlodipine systemic exposure w/ CYP3A4 inhibitors. May cause worsening of renal function and loss of antihypertensive effect w/ NSAIDs. May increase systemic exposure of simvastatin. May increase serum levels and toxicity of lithium. May cause nitritoid reaction w/ Na aurothiomalate. May increase risk of angioedema w/ mammalian target of rapamycin (mTOR) inhibitors (e.g. sirolimus, everolimus, temsirolimus).
Potentially Fatal: May increase risk of hypotension, hyperkalaemia, and changes in renal function w/ aliskiren.
Action
Description: Amlodipine, a dihydropyridine Ca channel blocker, inhibits transmembrane influx of Ca ions into vascular smooth muscles to produce peripheral arterial vasodilation, thereby reducing vascular resistance and BP. Additionally, it also acts on cardiac muscles. Benazepril, a prodrug of benazeprilat, is an inhibitor of ACE, which results in decreased plasma angiotensin II, thereby reducing both vasopressor activity and aldosterone secretion.
Onset: Amlodipine: 24-48 hr.
Duration: Amlodipine: 24-72 hr.
Pharmacokinetics:
Absorption: Amlodipine: Well absorbed. Bioavailability: 64-90%. Time to peak plasma concentration: 6-12 hr. Benazepril: Rapidly (37%) absorbed. Time to peak plasma concentration: 0.5-1 hr.
Distribution: Amlodipine: Volume of distribution: 21 L/kg. Plasma protein binding: Approx 93%. Benazepril: Volume of distribution: 0.7 L/kg. Plasma protein binding: Approx 97%.
Metabolism: Amlodipine: Extensively metabolised in the liver into inactive metabolites. Benazepril: Rapidly and extensively metabolised in the liver via enzymatic hydrolysis into its active metabolite, benazeprilat; undergoes extensive first-pass effect.
Excretion: Amlodipine: Via urine (10% as unchanged drug; 60% as metabolites). Terminal elimination half-life: 30-50 hr. Benazepril: Via urine (<1% as unchanged drug, 20% as benazeprilat, 12% as other metabolites). Terminal elimination half-life: Approx 22 hr.
Chemical Structure

Chemical Structure Image
Amlodipine

Source: National Center for Biotechnology Information. PubChem Database. Amlodipine, CID=2162, https://pubchem.ncbi.nlm.nih.gov/compound/Amlodipine (accessed on Jan. 20, 2020)


Chemical Structure Image
Benazepril

Source: National Center for Biotechnology Information. PubChem Database. Benazepril, CID=5362124, https://pubchem.ncbi.nlm.nih.gov/compound/Benazepril (accessed on Jan. 20, 2020)

Storage
Store at 25°C. Protect from moisture.
References
Anon. Amlodipine and Benazepril. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/11/2016.

Anon. Amlodipine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/11/2016.

Anon. Benazepril. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/11/2016.

Lotrel Capsule (PD-Rx Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 07/11/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Amlodipine Besylate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 07/11/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Benazepril Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 07/11/2016.

Disclaimer: This information is independently developed by MIMS based on Amlodipine + Benazepril from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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