Imidapril


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Essential hypertension
Adult: Initially, 5 mg once daily, may be increased to 10 mg daily if optimum blood pressure control has not been achieved after at least 3 weeks of therapy. Max: 20 mg daily.
Elderly: Initially, 2.5 mg once daily, may be titrated according to blood pressure response. Max: 10 mg daily.
Nhóm bệnh nhân đặc biệt
Patients with cardiac failure, cerebrovascular disease, or angina pectoris: Initially, 2.5 mg once daily. Close monitoring of the patient is required.
Suy thận
CrCl (mL/min) Dosage
<10
Contraindicated.
10-29
Not recommended.
30-80
Initially, 2.5 mg once daily, then titrate the dose cautiously.

Suy gan
Initially, 2.5 mg once daily.
Cách dùng
Should be taken on an empty stomach. Take 15 min before meals. However, when initiating therapy, 1st dose should be given at bedtime.
Chống chỉ định
History of angioneurotic oedema related to previous ACE inhibitor therapy; hereditary or idiopathic angioedema. Patients undergoing haemodialysis with high-flux membranes (e.g. acrylonitrile methallyl sulfonate Na) and LDL apheresis with dextran sulfate cellulose. Renal failure with or without haemodialysis (CrCl <10 mL/min). Pregnancy. Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73 m2).
Thận trọng
Patient with cardiac failure, ischaemic heart disease, cerebrovascular disease, angina pectoris, aortic or mitral valve stenosis, hypertrophic cardiomyopathy with outflow tract obstruction, collagen vascular disease (e.g. SLE), diabetes mellitus, volume depletion, unilateral or bilateral renal artery stenosis; hyperkalaemia or risk factors of hyperkalaemia. Patient undergoing major surgery and desensitisation therapy with hymenoptera venom. Black race. Renal and hepatic impairment. Elderly. Lactation.
Tác dụng không mong muốn
Significant: Symptomatic hypotension with or without syncope (particularly after the initial dose), dry and nonproductive cough; hyperkalaemia, renal function deterioration, increased serum creatinine. Rarely, intestinal angioedema, haematologic effects (e.g. neutropenia or agranulocytosis, thrombocytopenia, anaemia), proteinuria; exfoliative dermatitis, Stevens-Johnson syndrome, pemphigoid-like lesion.
Cardiac disorders: Palpitations, chest pain.
Gastrointestinal disorders: Nausea, vomiting, dyspepsia, epigastric pain.
General disorders and administration site conditions: Fatigue, oedema (joint and peripheral).
Infections and infestations: Viral infection.
Investigations: Increased BUN, ALT, AST, gamma-glutamyl transferase.
Musculoskeletal and connective tissue disorders: Pain in limbs.
Nervous system disorders: Dizziness, headache, somnolence, cerebrovascular disorders, paraesthesia.
Respiratory, thoracic and mediastinal disorders: Bronchitis, upper respiratory tract infection, rhinitis.
Skin and subcutaneous tissue disorders: Rash, pruritus.
Potentially Fatal: Angioneurotic oedema associated with laryngeal oedema; anaphylactic/anaphylactoid reactions. Rarely, cholestatic jaundice or hepatitis that may progress to fulminant hepatic necrosis.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness or lightheadedness, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor BUN, serum creatinine, WBC, and serum K levels. Obtain CBC with differential at baseline, every 2 weeks during the 1st 3 months of treatment and periodically thereafter in patients with collagen vascular disease and renal impairment.
Quá liều
Symptoms: Severe hypotension, bradycardia, electrolyte disturbances, stupor, shock and renal failure. Management: If ingestion is recent, perform gastric lavage or administer adsorbents and Na sulfate within 30 minutes following intake. Closely observe the patient, preferably in an intensive care unit. Frequently monitor serum electrolytes and creatinine. In case of hypotension, place the patient in a shock position and immediately give salt and volume supplementation; consider treatment with angiotensin II. Administer atropine for the treatment of bradycardia and extensive vagal reactions; may consider the use of a pacemaker. Haemodialysis may be performed to remove imidapril and imidaprilat from the circulation.
Tương tác
Increased risk of hyperkalaemia with K-sparing diuretics (e.g. spironolactone, triamterene, amiloride), K supplements or K-containing salt substitutes. Increased serum concentration and toxicity of lithium. NSAIDs (e.g. indometacin, aspirin), rifampicin, and sympathomimetics may decrease the antihypertensive effect of imidapril. May increase the risk of leucopenia with allopurinol, procainamide, and immunosuppressants. Enhanced hypotensive effect with other antihypertensive agents, diuretics (e.g. hydrochlorothiazide), nitrates, TCAs, and neuroleptics. May cause nitritoid reactions (e.g. facial flushing, nausea, vomiting, hypotension) with Na aurothiomalate. May enhance the hypoglycaemic effect of antidiabetic agents (e.g. insulin).
Potentially Fatal: Increased risk of hypotension, hyperkalaemia, and reduced renal function (including acute renal failure) with aliskiren. May result in severe anaphylactoid reactions when administered in patients undergoing LDL apheresis with dextran sulfate cellulose adsorption and haemodialysis with high-flux acrylonitrile methallyl sulfonate Na membranes.
Tương tác với thức ăn
High-fat meals significantly decrease imidapril absorption.
Ảnh hưởng đến kết quả xét nghiệm
May result in false-negative aldosterone/renin ratio (ARR).
Tác dụng
Description: Imidapril, a prodrug of imidaprilat, is a competitive ACE inhibitor that prevents the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor responsible for arterial vasoconstriction, increased blood pressure, and stimulation of aldosterone secretion. This action leads to lower angiotensin II levels, thereby increasing plasma renin activity and reducing aldosterone secretion.
Duration: 24 hours.
Pharmacokinetics:
Absorption: Rapidly but incompletely absorbed from the gastrointestinal tract. Reduced absorption with high-fat meals. Bioavailability: Approx 70% (imidapril); approx 42% (imidaprilat). Time to peak plasma concentration: Approx 2 hours (imidapril); 6-8 hours (imidaprilat).
Distribution: Plasma protein binding: 85% (imidapril); 53% (imidaprilat).
Metabolism: Metabolised in the liver via hydrolysis to imidaprilat (active metabolite).
Excretion: Via faeces (approx 50%); urine (approx 40%). Elimination half-life: Imidapril: Approx 2 hours. Imidaprilat: 7-9 hours (initial); >24 hours (terminal).
Đặc tính

Chemical Structure Image
Imidapril

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5464343, Imidapril. https://pubchem.ncbi.nlm.nih.gov/compound/Imidapril. Accessed May 26, 2022.

Bảo quản
Store below 30°C.
Phân loại MIMS
Thuốc ức chế men chuyển angiotensin/Thuốc ức chế trực tiếp renin
Phân loại ATC
C09AA16 - imidapril ; Belongs to the class of ACE inhibitors. Used in the treatment of cardiovascular disease.
Tài liệu tham khảo
Anon. Imidapril. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/05/2022.

Buckingham R (ed). Imidapril Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/05/2022.

Joint Formulary Committee. Imidapril Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/05/2022.

Tanatril 20 mg Tablets (Northumbria Pharma Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 04/05/2022.

Tanatril Tablets 5 mg, 10 mg (Mitsubishi Tanabe Pharma Malaysia Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 04/05/2022.

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