Adult: 50 mg once daily, may increase to 100 mg once daily according to clinical response. Patient with intravascular volume depletion: Initially, 25 mg once daily. Child: ≥6 years weighing 20-50 kg: Initially, 0.7 mg/kg once daily, may adjust as necessary up to Max of 50 mg daily; >50 kg: Same as adult dose.
Oral Diabetic nephropathy in type 2 diabetes mellitus
Adult: Initially, 50 mg once daily, may increase to 100 mg once daily according to clinical response.
Oral Chronic heart failure
Adult: In patients with reduced LVEF where treatment with ACE-inhibitors is unsuitable or contraindicated: Initially, 12.5 mg once daily, may titrate dose at weekly intervals up to Max of 150 mg once daily according to clinical response and tolerability. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Oral Hypertension with left ventricular hypertrophy
Adult: To reduce the risk of stroke: Initially, 50 mg once daily. Hydrochlorothiazide should be added and/or losartan should be increased to 100 mg once daily according to clinical response. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Suy gan
Hypertension; Diabetic nephropathy in type 2 diabetes mellitus; Hypertension with left ventricular hypertrophy:
Mild to moderate: Initially, 25 mg once daily. Severe: Contraindicated.
Chronic heart failure:
Mild to moderate: Dose reduction may be required. Severe: Contraindicated.
Cách dùng
May be taken with or without food.
Hướng dẫn pha thuốc
Oral susp: Instruction for reconstitution may vary among individual products and between countries (refer to specific product guidelines).
Chống chỉ định
Severe hepatic impairment. Pregnancy. Concomitant use with aliskiren-containing products in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73 m2).
Thận trọng
Patient with history of angioedema, volume and/or Na depletion, heart failure, bilateral renal artery stenosis or stenosis of the artery to a solitary kidney, aortic or mitral stenosis, obstructive hypertrophic cardiomyopathy, ischaemic CV and cerebrovascular disease. Patient undergoing surgery. Black patients. Not recommended for use in patients with ascites due to cirrhosis or refractory ascites; primary hyperaldosteronism. Renal impairment and mild to moderate hepatic impairment. Children and elderly. Lactation.
Tác dụng không mong muốn
Significant: Renal failure (e.g. acute kidney injury), symptomatic hypotension (in volume- and/or Na-depleted patients), electrolyte imbalance (e.g. hyperkalaemia), angioedema. Blood and lymphatic system disorders: Anaemia. Cardiac disorders: Angina pectoris, palpitations. Ear and labyrinth disorders: Tinnitus, vertigo. Gastrointestinal disorders: Abdominal pain, nausea, vomiting, diarrhoea. General disorders and administration site conditions: Oedema, asthenia, fatigue. Hepatobiliary disorders: Rarely, hepatitis. Investigations: Increase in serum creatinine or blood urea. Metabolism and nutrition disorders: Hypoglycaemia. Musculoskeletal and connective tissue disorders: Back pain, arthralgia, myalgia; rarely, rhabdomyolysis. Nervous system disorders: Dizziness, headache, migraine, paraesthesia. Psychiatric disorders: Sleep disorders, depression. Respiratory, thoracic and mediastinal disorders: Dyspnoea. Skin and subcutaneous tissue disorders: Urticaria, pruritus, rash. Vascular disorders: Orthostatic hypotension, syncope.
This drug may occasionally cause dizziness or drowsiness, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor blood pressure (at baseline and periodically), renal function, and electrolytes (e.g. serum K). Assess for signs of angioedema.
Quá liều
Symptoms: Hypotension, tachycardia, bradycardia (may occur from parasympathetic [vagal] stimulation). Management: Supportive and symptomatic treatment. Prioritise stabilisation of the CV system. Administer activated charcoal as indicated. Perform close monitoring of vital parameters. Correct vital parameters as necessary.
Tương tác
May increase the risk of hypotension with TCAs, antipsychotics, baclofen, and amifostine. Concomitant use with fluconazole may increase the plasma concentration of losartan but decrease the plasma concentration of the active metabolite. Decreased plasma concentration with rifampicin. Increased serum K levels with K-sparing diuretics (e.g. amiloride, spironolactone, triamterene), K supplements, K-containing salt substitutes, or other drugs that may increase serum K (e.g. heparin, trimethoprim-containing products); not recommended for concomitant use. May increase serum lithium concentrations and toxicity. Concomitant use with NSAIDs (e.g. selective COX-2 inhibitors, aspirin, non-selective NSAIDs) may increase the risk of worsening of renal function (including possible acute renal failure) and may decrease the hypotensive effect of losartan. Potentially Fatal: Increased risk of hypotension, hyperkalaemia, and changes in renal function (including acute renal failure) with ACE-inhibitors or aliskiren.
Tác dụng
Description: Mechanism of Action: 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 blocking the vasoconstricting and aldosterone-secreting effects of angiotensin II. Additionally, losartan does not affect the response to bradykinin and is less likely to be associated with non-renin-angiotensin effects (e.g. cough, angioedema). Onset: Approx 6 hours. Pharmacokinetics: Absorption: Well absorbed from the gastrointestinal tract. Bioavailability: Approx 33%. Time to peak plasma concentration: 1 hour (losartan); 3-4 hours (active metabolite). Distribution: Volume of distribution: 34 L. Plasma protein binding: >98%, mainly to albumin. Metabolism: Metabolised in the liver by CYP2C9 and CYP3A4 isoenzymes into E-3174 (active metabolite; more potent than losartan). Undergoes extensive first-pass metabolism. Excretion: Via urine (35%; approx 4% as unchanged drug, approx 6% as active metabolite); faeces (approx 60%). Elimination half-life: 2.1 ± 0.7 hours (losartan); 7.4 ± 2.4 hours (active metabolite).
Đặc tính
Losartan Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3961, Losartan. https://pubchem.ncbi.nlm.nih.gov/compound/Losartan. Accessed May 27, 2022.
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