Adult: In cases where oral treatment is impractical: As enalaprilat: 1.25 mg 6 hourly via slow IV push over at least 5 minutes or IV infusion. Available preparations may vary between countries (refer to specific product guidelines). Elderly: Initiate at the lower end of the dosing range.
Oral Hypertension
Adult: As enalapril maleate: Initially, 5 mg once daily. Maintenance: 10-20 mg once daily, increase up to Max of 40 mg daily if needed. Doses may be given in 2 divided doses if control is inadequate. Dosage must be individualised based on patient profile and blood pressure response. Elderly: Initially, 2.5 mg once daily, then adjust according to response. Child: 20-<50 kg: Initially, 2.5 mg once daily, may increase to Max of 20 mg daily; ≥50 kg: Initially, 5 mg once daily, may increase to Max of 40 mg daily. Alternatively, initiate with 0.08 mg/kg once daily, may increase to Max of 5 mg once daily. Dosage must be individualised based on patient profile and blood pressure response. Dosing recommendations may vary among individual products and between countries (refer to specific product guidelines).
Oral Asymptomatic left ventricular dysfunction, Heart failure
Adult: As enalapril maleate: Initially, 2.5 mg once daily, increase gradually up to 20 mg. Usual maintenance dose: 20 mg daily as a single or in 2 divided doses. Titrate dose according to patient tolerance over 2-4 weeks. Max: 40 mg daily in 2 divided doses. Dosage must be individualised based on patient profile and blood pressure response. Dosing recommendations may vary among individual products and between countries (refer to specific product guidelines). Elderly: Initially, 2.5 mg once daily, then adjust according to response.
Nhóm bệnh nhân đặc biệt
Hypertension: Oral:
Patients taking diuretics: Initially, 2.5 mg daily. If possible, discontinue the diuretic 2-3 days before initiating enalapril.
Intravenous:
Patients taking diuretics: Initially, 0.625 mg via slow IV push over 5 minutes. If the clinical response is inadequate after 1 hour, may repeat the 0.625 mg dose and give 1.25 mg 6 hourly thereafter.
Suy thận
Oral:
Dialysis patients: Initially, 2.5 mg on dialysis days. Dosage on non-dialysis days must be adjusted based on the blood pressure response.
CrCl (mL/min)
Dosage
≤30
Initially, 2.5 mg daily, then adjust according to response.
Intravenous:
CrCl (mL/min)
Dosage
≤30
Initially, 0.625 mg via slow IV push over 5 minutes. If the clinical response is inadequate after 1 hour, may repeat the 0.625 mg dose and give 1.25 mg 6 hourly thereafter.
Cách dùng
May be taken with or without food.
Hướng dẫn pha thuốc
IV infusion: Dilute with up to 50 mL of a compatible diluent (e.g. dextrose 5% in water, NaCl 0.9% solution).
Tương kỵ
IV: Incompatible with phenytoin and amphotericin B.
Chống chỉ định
History of angioedema related to previous ACE inhibitor treatment, idiopathic or hereditary angioedema. Pregnancy. Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73m2). Concomitant use with or within 36 hours of switching to or from a neprilysin inhibitor (e.g. sacubitril).
Thận trọng
Patient with Na or volume depletion, diabetes, ascites due to cirrhosis or refractory ascites; cerebrovascular disease, ischaemic heart disease, collagen vascular disease, hypertrophic cardiomyopathy and left ventricular outflow tract obstruction, severe aortic stenosis, bilateral renal artery stenosis or stenosis of the artery to a single functioning kidney; history of angioedema unrelated to ACE inhibitor treatment. Patient undergoing major surgery, desensitisation treatment with hymenoptera venom, LDL apheresis with dextran sulfate or haemodialysis with high-flux dialysis membranes. Black race. Renal and hepatic impairment. Neonates, children, and elderly. Lactation.
Tác dụng không mong muốn
Significant: Symptomatic hypotension, syncope, haematologic effects (e.g. neutropenia, agranulocytosis, thrombocytopenia, anaemia), cough, hyperkalaemia. Cardiac disorders: Tachycardia, rhythm disturbances, chest pain, angina pectoris. Eye disorders: Blurred vision. Gastrointestinal disorders: Nausea, abdominal pain, diarrhoea, taste alteration. General disorders and administration site conditions: Asthenia, fatigue. Investigations: Increased serum creatinine. Nervous system disorders: Headache, dizziness. Psychiatric disorders: Depression. Respiratory, thoracic and mediastinal disorders: Dyspnoea. Skin and subcutaneous tissue disorders: Rash. Potentially Fatal: Angioneurotic oedema of the face, extremities, lips, tongue, glottis and/or larynx. Rarely, cholestatic jaundice or hepatitis that may progress to fulminant hepatic necrosis.
PO: D; IV/Parenteral: D (2nd & 3rd trimesters), C (1st trimester)
Thông tin tư vấn bệnh nhân
This drug may cause occasional dizziness or weariness, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor blood pressure and renal function before and after treatment. Obtain CBC, BUN, serum creatinine and electrolytes. Evaluate for signs of angioedema.
Quá liều
Symptoms: Marked hypotension, circulatory shock, electrolyte distubances, renal failure, hyperventilation, tachycardia, palpitations, bradycardia, dizziness, anxiety, cough and stupor. Management: Administer NaCl 0.9% solution via IV infusion. Put the patient in the shock position if hypotension occurs. May consider giving angiotensin II infusion and/or IV catecholamines if available. May perform gastric lavage, induce emesis, administer adsorbents and Na sulfate for recent ingestion. May also perform haemodialysis.
Tương tác
Increased risk of angioedema with racecadotril, mTOR inhibitors (e.g. everolimus, sirolimus, temsirolimus), vildagliptin. Increased risk of hyperkalaemia with K-sparing diuretics (e.g. spironolactone, triamterene, amiloride), K supplements, K-containing salt substitutes, and other drugs associated with increases in serum K (e.g. trimethoprim/sulfamethoxazole, heparin, ciclosporin). Increased risk of volume depletion and hypotension with diuretics. Increased hypotensive effect with other antihypertensive drugs, vasodilators (e.g. nitrates), TCAs, antipsychotics. May increase serum lithium concentration and enhance risk of lithium toxicity. Coadministration with NSAIDs (including COX-2 inhibitors) may result in deterioration of renal function. Increased risk of hypoglycaemia with insulin and oral antidiabetic drugs. Nitritoid reactions (e.g. facial flushing, nausea, vomiting, hypotension) may occur when used concurrently with injectable gold (Na aurothiomalate). Decreased antihypertensive effects with sympathomimetics. Potentially Fatal: Increased risk of angioedema with neprilysin inhibitors (e.g. sacubitril). Concomitant use with aliskiren increases the risk of hypotension, hyperkalaemia, and decreased renal function (including acute renal failure).
Tương tác với thức ăn
Enhanced hypotensive effect with alcohol.
Tác dụng
Description: Mechanism of Action: Enalapril is a prodrug of enalaprilat which competitively inhibits ACE from converting angiotensin I to angiotensin II (a potent vasoconstrictor). This results in reduced levels of angiotensin II leading to increased plasma renin activity and decreased aldosterone secretion. Onset: Oral: Approx 1 hour. IV: Within 15 minutes. Duration: Oral: 12-24 hours. IV: Approx 6 hours. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Time to peak plasma concentration: 0.5-1.5 hours (enalapril); 3-4.5 hours (enalaprilat). Distribution: Crosses the placenta and enters breast milk. Plasma protein binding: Approx 50%. Metabolism: Rapidly and extensively hydrolysed in the liver into enalaprilat (active metabolite). Excretion: Via urine (61%; 18% as enalapril, 43% as enalaprilat); faeces (33%; 6% as enalapril, 27% as enalaprilat). Elimination half-life: 2 hours (enalapril); approx 35 hours (enalaprilat).
Đặc tính
Enalapril Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5388962, Enalapril. https://pubchem.ncbi.nlm.nih.gov/compound/Enalapril. Accessed Aug. 24, 2023.
Bảo quản
Tab: Store between 15-30°C. Protect from moisture. Oral solution: Store between 2-8°C. Do not freeze. May be stored between 20-25°C for up to 60 days. Solution for inj or infusion: Store between 15-30°C.
C09AA02 - enalapril ; Belongs to the class of ACE inhibitors. Used in the treatment of cardiovascular disease.
Tài liệu tham khảo
Anon. Enalapril (Pediatric and Neonatal Lexi-Drugs). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/05/2023.Anon. Enalapril. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 06/03/2023.Anon. Enalapril. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/03/2023.Anon. Enalaprilat. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/07/2023.Buckingham R (ed). Enalapril. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/03/2023.Enalapril Maleate 2.5 mg Tablets (Milpharm Limited). MHRA. https://products.mhra.gov.uk. Accessed 06/03/2023.Enalapril Maleate Oral Solution (Ascend Laboratories, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 06/03/2023.Enalapril Maleate Tablet (Wockhardt USA LLC.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 06/03/2023.Enalapril, Enalaprilat. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 04/05/2023.Enalaprilat Injection (HF Acquisition Co LLC, DBA Healthfirst). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 06/03/2023.Joint Formulary Committee. Enalapril Maleate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/03/2023.Paediatric Formulary Committee. Enalapril Maleate. BNF for Children [online]. London. BMJ Group, Pharmaceutical Press, and RCPCH Publications. https://www.medicinescomplete.com. Accessed 03/05/2023.Renitec (Organon Malaysia Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 04/05/2023.Viatris Ltd. Acetec Tablet data sheet 02 May 2022. Medsafe. http://www.medsafe.govt.nz. Accessed 06/03/2023.
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