Amlodipine + Benazepril

Oral
Hypertension

CrCl ≤30 mL/min: Contraindicated.

Start w/ 2.5 mg amlodipine component once daily.

May be taken with or without food.

History of angioedema. Concomitant use w/ aliskiren esp in patient w/ DM. Severe renal impairment (CrCl ≤30 mL/min). Pregnancy and lactation.

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.

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.

PO: D

Monitor BUN, serum creatinine, electrolytes, and BP.

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.

Description:
Mechanism of Action: 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.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2162, Amlodipine. https://pubchem.ncbi.nlm.nih.gov/compound/Amlodipine. Accessed Oct. 26, 2023.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5362124, Benazepril. https://pubchem.ncbi.nlm.nih.gov/compound/Benazepril. Accessed June 27, 2022.

Store at 25°C. Protect from moisture.

Thuốc ức chế men chuyển angiotensin/Thuốc ức chế trực tiếp renin / Thuốc đối kháng calci

C09BB13 - benazepril and amlodipine ; Belongs to the class of ACE inhibitors and calcium channel blockers. Used in the treatment of cardiovascular diseases.

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.