Aliskiren + Hydrochlorothiazide

Thông tin thuốc gốc
Chỉ định và Liều dùng
Adult: Available preparations:
Aliskiren 150 mg and Hydrochlorothiazide 12.5 mg
Aliskiren 150 mg and Hydrochlorothiazide 25 mg
Aliskiren 300 mg and Hydrochlorothiazide 12.5 mg
Aliskiren 300 mg and Hydrochlorothiazide 25 mg

1 tab once daily. Dosage is individualised and may be increased after at least 2-4 weeks, according to response. Max: Aliskiren 300 mg and hydrochlorothiazide 25 mg daily.
Renal Impairment
Severe (GFR <30 mL/min/1.73m2): Contraindicated.
Hepatic Impairment
Severe: Contraindicated.
Cách dùng
May be taken with or without food. Take w/ a light meal, preferably at the same time each day. Swallow whole w/ water. Avoid taking w/ fruit juices.
Chống chỉ định
Hypersensitivity to aliskiren and other sulfonamide-derived drugs. Anuria, volume depletion, history of angioedema, hereditary or idiopathic angioedema. Severe hepatic and renal impairment (GFR <30 mL/min/1.73m2). Concomitant use with ACE inhibitors or angiotensin II receptor antagonists in patient with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73m2). Concomitant use with potent P-glycoprotein (P-gp) inhibitors (e.g. ciclosporin, itraconazole and quinidine). Pregnancy.
Thận trọng
Patient with prediabetes or diabetes, history or risk for gout, history of allergy or bronchial asthma; volume or salt depletion, renal artery stenosis, CV disease, post MI, hypercalcaemia, moderate or high cholesterol levels, parathyroid disease, SLE. Mild to moderate renal and hepatic impairment. Lactation.
Phản ứng phụ
Significant: Electrolyte disturbances (e.g, hyper or hypokalaemia, hypochloraemic alkalosis, hypomagnesaemia, hypophosphataemia, hypercalcaemia, hyponatraemia), hypersensitivity reactions (e.g. urticaria), gout, hypotension, syncope, acute transient myopia, acute angle-closure glaucoma, photosensitivity, acute renal failure, metabolic disturbances (e.g. hypercholesterolaemia, hypertriglyceridaemia, altered glucose tolerance, hyperuricaemia), SLE exacerbation or activation.
Cardiac disorders: Palpitations.
Gastrointestinal disorders: Diarrhoea, decreased appetite, nausea, vomiting, oral mucosal reactions.
Investigations: Increased liver enzymes.
Metabolism and nutrition disorders: Peripheral oedema.
Musculoskeletal and connective tissue disorders: Arthralgia.
Nervous system disorders: Dizziness.
Reproductive system and breast disorders: Impotence.
Respiratory, thoracic and mediastinal disorders: Cough.
Skin and subcutaneous tissue disorders: Urticaria, rash, Stevens Johnson syndrome, toxic epidermal necrolysis, pruritus.
Potentially Fatal: Anaphylactic reactions, angioedema.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness or drowsiness, if affected, do not drive or operate machinery.
Monitoring Parameters
Correct hypovolaemia or salt depletion prior to initiation of therapy. Monitor blood pressure, serum electrolytes, BUN, serum creatinine, fluid status; parathyroid and renal function.
Quá liều
Symptoms: Hypotension, electrolyte depletion (e.g. hypokalaemia, hypochloraemia, hyponatraemia), dehydration. Management: Symptomatic and supportive treatment.
Tương tác
Aliskiren: Increased risk of hypotension with other antihypertensives. Increased risk of acute renal failure with ACE inhibitors, angiotensin II receptor antagonists or NSAIDs. Antihypertensive effect may be reduced with NSAIDs. Increased serum levels with atorvastatin, ketoconazole, verapamil. Decreases furosemide concentrations. Increased risk of hyperkalaemia with potassium-sparing diuretics, potassium supplements or any substances that may increase serum potassium levels.
Hydrochlorothiazide: Increases toxicity of lithium. May potentiate orthostatic hypotension with barbiturates and narcotics. Increased hypokalaemic effect with corticosteroids or ACTH. Potentiation of orthostatic hypotension with barbiturates or opioids. Reduced antihypertensive effect by drugs that cause fluid retention (e.g. corticosteroids, NSAIDs, carbenoxolone). Enhanced nephrotoxicity of NSAIDs. May reduce the therapeutic effect of antidiabetics.
Potentially Fatal: Increased risk of renal impairment, stroke, hypotension and hyperkalaemia with ACE inhibitors or angiotensin II receptor antagonists. Markedly increased plasma concentration with ciclosporin, itraconazole and quinidine.
Food Interaction
Aliskiren: Reduced bioavailability with high fat meals. Reduced serum concentration with grapefruit juice.
Hydrochlorothiazide: Enhanced orthostatic hypotensive effect with alcohol.
Lab Interference
Hydrochlorothiazide: May interfere with parathyroid function tests.
Tác dụng
Description: Aliskiren is a direct inhibitor of renin, an enzyme essential for the conversion of angiotensinogen into angiotensin I. It decreases plasma renin activity therefore inhibiting the production of angiotensin II and aldosterone.
Hydrochlorothiazide inhibits the reabsorption of Na in the distal tubules causing increased excretion of Na and water including K and hydrogen ions.
Onset: Aliskiren: Within 2 weeks.
Hydrochlorothiazide: Approx 2 hours.
Duration: Hydrochlorothiazide: 6-12 hours.
Absorption: Aliskiren: Poorly absorbed from gastrointestinal tract. Food, particularly high fat meal, decreases rate and extent of absorption. Bioavailability: Approx 3%. Time to peak plasma concentration: 1-3 hours.
Hydrochlorothiazide: Fairly rapid absorption from the gastrointestinal tract. Time to peak plasma concentration: Approx 1-5 hours. Bioavailability: Approx 65-70%.
Distribution: Aliskiren: Distributes extensively into extravascular space. Plasma protein binding: Approx 50%.
Hydrochlorothiazide: Crosses the placenta and enters breast milk; distributes in erythrocytes. Volume of distribution: 3.6-7.8 L/kg. Plasma protein binding: Approx 40-68%.
Metabolism: Aliskiren: Minimal metabolism by CYP3A4 isoenzyme.
Excretion: Aliskiren: Mainly via faeces as unchanged drug; urine (approx 25% as unchanged drug). Elimination half-life: Approx 24-40 hours.
Hydrochlorothiazide: Via urine (≥61 % as unchanged drug). Elimination half-life: Approx 5-15 hours.
Đặc tính

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Aliskiren, CID=5493444, (accessed on Jan. 20, 2020)

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Hydrochlorothiazide, CID=3639, (accessed on Jan. 20, 2020)

Bảo quản
Store at 25°C. Protect from moisture.
Phân loại ATC
C09XA52 - aliskiren and hydrochlorothiazide ; Belongs to the class of renin-inhibitors. Used in the treatment of cardiovascular disease.
Anon. Aliskiren and Hydrochlorothiazide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 02/03/2018.

Anon. Aliskiren. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 02/03/2018.

Anon. Hydrochlorothiazide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 02/03/2018.

Buckingham R (ed). Aliskiren Fumarate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. Accessed 02/03/2018.

Buckingham R (ed). Hydrochlorothiazide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. Accessed 02/03/2018.

McEvoy GK, Snow EK, Miller J et al (eds). Aliskiren Hemifumarate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). Accessed 02/03/2018.

Rasilez (Noden Pharma DAC). European Medicines Agency [online]. Accessed 02/03/2018.

Tekturna HCT Tablet, Film Coated (Noden Pharma USA, Inc.). DailyMed. Source: U.S. National Library of Medicine. Accessed 02/03/2018.

Thông báo miễn trừ trách nhiệm: Thông tin này được MIMS biên soạn một cách độc lập dựa trên thông tin của Aliskiren + Hydrochlorothiazide từ nhiều nguồn tài liệu tham khảo và được cung cấp chỉ cho mục đích tham khảo. Việc sử dụng điều trị và thông tin kê toa có thể khác nhau giữa các quốc gia. Vui lòng tham khảo thông tin sản phẩm trong MIMS để biết thông tin kê toa cụ thể đã qua phê duyệt ở quốc gia đó. Mặc dù đã rất nỗ lực để đảm bảo nội dung được chính xác nhưng MIMS sẽ không chịu trách nhiệm hoặc nghĩa vụ pháp lý cho bất kỳ yêu cầu bồi thường hay thiệt hại nào phát sinh do việc sử dụng hoặc sử dụng sai các thông tin ở đây, về nội dung thông tin hoặc về sự thiếu sót thông tin, hoặc về thông tin khác. © 2021 MIMS. Bản quyền thuộc về MIMS. Phát triển bởi
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in