Candesartan


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Hypertension
Adult: Initially, 8 mg once daily adjusted according to response. Max: 32 mg/day as single or in 2 divided doses. Patients with intravascular volume depletion: Initially, 4 mg once daily.
Child: 1-<6 years Initially, 0.2 mg/kg once daily. Maintenance: 0.05-0.4 mg/kg/day as single daily dose or in 2 divided doses. Max: 0.4 mg/kg daily. 6-<17 years <50 kg: Initially, 4-8 mg once daily, adjusted according to response to 2-16 mg/day; >50 kg: 8-16 mg once daily, adjusted according to response to 4-32 mg/day.

Oral
Heart failure with reduced ejection fraction
Adult: In patients with left ventricular systolic dysfunction who cannot tolerate ACE-inhibitors or as add-on therapy to ACE-inhibitors: Initially, 4 mg once daily, may be doubled at intervals of not <2 weeks if needed. Max: 32 mg once daily.
Nhóm bệnh nhân đặc biệt
Hypertension:
Black patients: Dose increase may be necessary.
Suy thận
Including patients on haemodialysis: Initially, 4 mg once daily.
Suy gan
Mild to moderate: Initially, 4 mg once daily, adjusted according to response. Severe: Contraindicated.
Cách dùng
May be taken with or without food.
Chống chỉ định
Severe hepatic impairment and/or cholestasis. Children (<1 year). Pregnancy. Concomitant use with aliskiren in patients with diabetes mellitus or moderate to severe renal impairment (GFR <60 mL/min/1.73m2).
Thận trọng
Patient with unstented unilateral/bilateral renal artery stenosis or stenosis of the artery to a solitary kidney, history of angioedema, relevant aortic or mitral valve stenosis or obstructive hypertrophic cardiomyopathy, primary hyperaldosteronism. Black patients. Patients undergoing surgery. Renal and mild to moderate hepatic impairment. Children. Lactation.
Tác dụng không mong muốn
Significant: Angioedema, hypotension, hyperkalaemia, renal impairment.
Blood and lymphatic system disorders: Agranulocytosis, leucopenia, neutropenia.
Gastrointestinal disorders: Nausea.
Hepatobiliary disorders: Abnormal hepatic function or hepatitis.
Immune system disorders: Urticaria.
Infections and infestations: Respiratory infection.
Investigations: Increased liver enzymes.
Metabolism and nutrition disorders: Hyponatraemia.
Musculoskeletal and connective tissue disorders: Arthralgia, back pain, myalgia.
Nervous system disorders: Dizziness, headache, vertigo.
Respiratory, thoracic and mediastinal disorders: Cough.
Skin and subcutaneous tissue disorders: Rash, pruritus.
Chỉ số theo dõi
Monitor blood pressure, electrolytes, renal function (e.g. serum creatinine, BUN), urinalysis, signs and symptoms of hypotension, tachycardia, CNS changes, hyperglycaemia, signs of angioedema; serum K during dose increase and periodically thereafter (in heart failure).
Quá liều
Symptoms: Hypotension, dizziness, tachycardia. Management: Symptomatic and supportive treatment. Monitor vital signs and place the patient in a supine position with the legs elevated to manage symptomatic hypotension. If insufficient, increase plasma volume by infusion of isotonic saline solution. If still insufficient, may administer sympathomimetic drugs.
Tương tác
Increased risk of hypotension with high dose diuretics and anaesthesia. Increased serum K levels with K-sparing diuretics (e.g. spironolactone), K supplements, K-containing salt substitutes or other drugs that increase K levels (e.g. heparin). May increase serum lithium concentration. Reduced antihypertensive effect, and increased risk of worsening renal function and increased serum K with NSAIDs (e.g. selective COX-2 inhibitors, aspirin).
Potentially Fatal: Coadministration with aliskiren in diabetic patients may increase the risk of renal impairment, hypotension and hyperkalaemia.
Tác dụng
Description:
Mechanism of Action: Candesartan is an angiotensin receptor antagonist which binds to AT1 angiotensin II receptor in many tissues (e.g. vascular smooth muscle, adrenal gland), thereby inhibiting angiotensin II from binding to the receptor which leads to blocking of vasoconstriction and aldosterone release.
Onset: 2-3 hours; within 2 weeks (antihypertensive effect).
Duration: >24 hours.
Pharmacokinetics:
Absorption: Rapidly and completely absorbed from the gastrointestinal tract after conversion. Bioavailability: 15%. Time to peak plasma concentration: 3-4 hours.
Distribution: Enters breast milk. Volume of distribution: 0.13 L/kg. Plasma protein binding: >99%.
Metabolism: Rapidly converted via ester hydrolysis into active candesartan during absorption from the gastrointestinal tract; metabolised in the liver (minor) via O-deethylation into inactive metabolite.
Excretion: Via faeces (67%); urine (33%; 26% as unchanged drug). Elimination half-life: 5-9 hours.
Đặc tính

Chemical Structure Image
Candesartan

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2541, Candesartan. https://pubchem.ncbi.nlm.nih.gov/compound/2541. Accessed Aug. 25, 2022.

Bảo quản
Store below 30°C.
Phân loại MIMS
Thuốc đối kháng thụ thể angiotensin II
Phân loại ATC
C09CA06 - candesartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
Tài liệu tham khảo
Anon. Candesartan. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/02/2021.

Blopress Tablets (Takeda Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 02/02/2021.

Buckingham R (ed). Candesartan Cilexetil. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/02/2021.

Candesartan 4 mg Tablets (Accord-UK Ltd). MHRA. https://products.mhra.gov.uk. Accessed 02/02/2021.

Candesartan 8 mg Tablets (Accord-UK Ltd). MHRA. https://products.mhra.gov.uk. Accessed 02/02/2021.

Candesartan Cilexetil Tablet (Alembic Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/02/2021.

Joint Formulary Committee. Candesartan Cilexetil. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/02/2021.

Mylan New Zealand Ltd. Candestar 4 mg, 8 mg, 16 mg and 32 mg Tablets data sheet 13 February 2018. Medsafe. http://www.medsafe.govt.nz. Accessed 02/02/2021.

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