Losartan


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Hypertension
Adult: 50 mg daily. Dosage is individualised and may be increased to 100 mg once daily according to clinical response. Patients with intravascular volume depletion: Initially, 25 mg daily.
Child: 6-18 years >20-<50 kg: 0.7 mg/kg once daily (up to total of 25 mg). Max: 50 mg daily, as necessary. >50 kg: Same as adult dose. Adjust dose based on blood pressure response.
Elderly: >75 years 25 mg daily.

Oral
Diabetic nephropathy in Type 2 diabetes mellitus
Adult: Initially, 50 mg daily, may increase to 100 mg daily depending on blood pressure response.
Elderly: >75 years 25 mg daily.

Oral
Heart failure
Adult: Initially, 12.5 mg daily, may titrate dose at weekly intervals. Max dose: 150 mg daily.
Elderly: >75 years 25 mg daily.
Hepatic Impairment
Mild to moderate: Initially, 25 mg daily. Severe: Contraindicated.
Cách dùng
May be taken with or without food.
Chống chỉ định
Concomitant use with aliskiren-containing products in patients with diabetes mellitus or renal impairment (GFR <60 mL/min). Severe hepatic impairment. Pregnancy (2nd-3rd trimester).
Thận trọng
Patient with history of angioedema, volume- and/or Na-depletion, heart failure, unstented unilateral/bilateral renal artery stenosis, aortic or mitral stenosis, cirrhosis. Black race. Renal impairment and mild to moderate hepatic impairment. Children and elderly. Lactation.
Phản ứng phụ
Significant: Renal failure, renal insufficiency, symptomatic hypotension (in volume- or Na-depleted patients), hyperkalaemia, rarely, angioedema.
Blood and lymphatic system disorders: Anaemia.
Cardiac disorders: Chest pain, atrial fibrillation, palpitations, dyspnoea.
Ear and labyrinth disorders: Tinnitus.
Gastrointestinal disorders: Diarrhoea, constipation, nausea, vomiting.
General disorders and admin site conditions: Asthenia, fatigue.
Immune system disorders: Urticaria.
Investigations: Increase in serum creatinine.
Metabolism and nutrition disorders: Hypoglycaemia, oedema.
Musculoskeletal and connective tissue disorders: Back pain, arthralgia, myalgia.
Nervous system disorders: Dizziness, vertigo, headache, migraine, paraesthesia, cerebrovascular accident.
Psychiatric disorders: Sleep disorder, depression.
Renal and urinary disorders: UTI.
Respiratory, thoracic and mediastinal disorders: Upper respiratory tract infection, cough, nasal congestion.
Skin and subcutaneous tissue disorders: Pruritus, photosensitivity, rash.
Vascular disorders: Orthostatic hypotension, syncope.
Thông tin tư vấn bệnh nhân
This drug may occasionally cause dizziness or drowsiness, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor blood pressure, renal function, and electrolytes level e.g. serum K, urininalysis. Correct volume depletion prior to therapy. Assess for signs of angioedema.
Quá liều
Symptoms: Hypotension, tachycardia, bradycardia (may occur from parasympathetic stimulation). Management: Supportive and symptomatic treatment. Prioritise stabilisation of CVS. Administration of activated charcoal and close monitoring of vital parameters may be performed. Correct vital parameters, as necessary.
Tương tác
May potentiate hypotensive effect with other antihypertensive agents. May increase risk of hypotension as an adverse reaction of antipsychotics and amifostine. Decreased plasma concentration with rifampicin and fluconazole. Increased serum K levels and enhance hyperkalaemic effect with K-sparing diuretics (e.g. amiloride, spironolactone), K supplements or K-containing salt substitutes (e.g. heparin). May increase serum lithium concentrations and toxicity. May increase risk of renal impairment and may decrease hypotensive effect with NSAIDs.
Potentially Fatal: Increased risk of hypotension, hyperkalaemia, and nephrotoxicity with ACE-inhibitors or aliskiren.
Food Interaction
Decreased absorption with food.
Tác dụng
Description: Losartan is a competitive angiotensin II receptor antagonist. It selectively blocks AT1 receptors found in many tissues (e.g. vascular smooth muscle, adrenal gland), thereby reducing the vasoconstricting and aldosterone-secreting effects of angiotensin II. Losartan is less likely to be associated with non renin-angiotensin effects (e.g. cough, angioedema) due to the lack of effect to the response to bradykinin.
Onset: Approx 6 hours.
Pharmacokinetics:
Absorption: Well absorbed from the gastrointestinal tract. Decreased absorption with food. Bioavailability: Approx 33%. Time to peak plasma concentration: 1 hour.
Distribution: Volume of distribution: 34 L. Plasma protein binding: >98%, primarily to albumin.
Metabolism: Undergoes extensive hepatic first-pass metabolism by CYP2C9 and CYP3A4 to active metabolite (E-3174).
Excretion: Via urine (35%; approx 4% as unchanged drug, approx 6% as metabolite), faeces (approx 60%). Elimination half-life: Approx Aprox 1.5-2.5 hours; approx 3-9 hours (active metabolite).
Đặc tính

Chemical Structure Image
Losartan

Source: National Center for Biotechnology Information. PubChem Database. Losartan, CID=3961, https://pubchem.ncbi.nlm.nih.gov/compound/Losartan (accessed on Jan. 22, 2020)

Bảo quản
Store at 25°C. Protect from light.
Phân loại MIMS
Phân loại ATC
C09CA01 - losartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
References
Anon. Losartan. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/04/2019.

Buckingham R (ed). Losartan. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/04/2019.

Joint Formulary Committee. Losartan. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/04/2019.

Losartan (Aurolife Pharma, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 08/04/2019.

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