Amlodipine + Benazepril


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Cách dùng
May be taken with or without food.
Chống chỉ định
History of angioedema. Concomitant use w/ aliskiren esp in patient w/ DM. Severe renal impairment (CrCl ≤30 mL/min). Pregnancy and lactation.
Thận trọng
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.
Phản ứng phụ
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.
Tương tác
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.
Tác dụng
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.
Đặc tính

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)

Bảo quản
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.

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