Adult: Amlodipine 5 mg and losartan 50 mg tab Amlodipine 5 mg and losartan 100 mg tab
In patients whose blood pressure is inadequately controlled with monotherapy: Initially, 5 mg/50 mg once daily, then increase dose to 5 mg/100 mg once daily as necessary. Dosage is individualised and adjusted based on clinical response. Available preparations may vary between countries (refer to specific product guidelines).
What are the brands available for Amlodipine + Losartan in Malaysia?
Patients on dialysis: Not recommended. Moderate to severe: Not recommended.
Hepatic Impairment
Severe: Contraindicated.
Administration
Amlodipine + Losartan May be taken with or without food.
Contraindications
Severe aortic valvular stenosis, unstable cardiovascular disease, shock (including cardiogenic shock). Severe hepatic impairment. Pregnancy and lactation. Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (<GFR 60 mL/minute/1.73 m2).
Special Precautions
Patient with volume depletion, aortic stenosis, heart failure, hypertrophic cardiomyopathy with outflow tract obstruction, bilateral renal artery stenosis, stenosis of the artery to a solitary kidney, severe obstructive CAD; history of angioedema associated with ACE inhibitor therapy; diabetes mellitus. Moderate to severe renal (including patients on dialysis) and mild to moderate hepatic impairment.
Adverse Reactions
Significant: Electrolyte imbalance, renal function deterioration including acute renal failure, hyperkalaemia, symptomatic hypotension; angioedema involving the head and neck region; worsening angina and/or MI. Cardiac disorders: Palpitation. Ear and labyrinth disorders: Vertigo. Gastrointestinal disorders: Reflux oesophagitis, nausea, dyspepsia, abdominal discomfort. General disorders and administration site conditions: Pitting oedema, peripheral oedema, asthenia, chest pain or discomfort, early satiety. Nervous system disorders: Dizziness, headache. Renal and urinary disorders: Pollakiuria. Respiratory, thoracic and mediastinal disorders: Dyspnoea. Skin and subcutaneous tissue disorders: Urticaria, pruritus. Vascular disorders: Orthostatic hypotension, flushing.
Monitoring Parameters
Correct volume depletion prior to treatment initiation. Monitor electrolytes, renal and liver function, blood pressure and heart rate. Assess for signs of peripheral oedema.
Overdosage
Symptoms: Amlodipine: Excessive peripheral vasodilation with marked hypotension and reflex tachycardia; non-cardiogenic pulmonary oedema. Losartan: Hypotension, tachycardia and bradycardia. Management: Supportive treatment. Elevate extremities and administer fluids in case of hypotension. If hypotension persists despite conservative measures, consider giving vasopressors (e.g. phenylephrine) while monitoring circulating volume and urine output.
Drug Interactions
Amlodipine: Concurrent use with strong CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, ritonavir) may significantly increase the plasma concentrations of amlodipine.
Losartan: Increased risk of hyperkalaemia with K-sparing diuretics (e.g. spironolactone, triamterene, amiloride), K supplements, salt substitutes containing K or other drugs that may increase serum K (e.g. trimethoprim). May increase serum concentration of lithium. Concomitant use with NSAIDs (e.g. selective COX-2 inhibitors, aspirin, non-selective NSAIDs) may increase the risk of worsening renal function (including possible acute renal failure) and may decrease the hypotensive effect of losartan. Potentially Fatal: Losartan: Increased risk of hypotension, hyperkalaemia, and changes in renal function (including acute renal failure) with ACE inhibitors or aliskiren.
Food Interaction
Losartan: Reduced therapeutic effect with grapefruit juice.
Action
Description: Mechanism of Action: Amlodipine, a dihydropyridine Ca channel blocker, reduces peripheral vascular resistance and blood pressure by relaxing the coronary vascular smooth muscle and coronary vasodilation through inhibition of Ca ion transmembrane influx into cardiac and vascular smooth muscles.
Losartan is a competitive and selective nonpeptide angiotensin II receptor antagonist. It inhibits the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking its binding to the angiotensin II subtype 1 (AT1) receptors found in many tissues (e.g. vascular smooth muscle, adrenal gland, kidneys, heart). 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: Amlodipine: Antihypertensive effect: 24-48 hours.
Losartan: Approx 6 hours. Duration: Amlodipine: Antihypertensive effect: At least 24 hours. Pharmacokinetics: Absorption: Amlodipine: Well absorbed. Bioavailability: 64-90%. Time to peak plasma concentration: 6-12 hours.
Losartan: Readily absorbed from the gastrointestinal tract. Bioavailability: Approx 33%. Time to peak plasma concentration: 1 hour (losartan); 3.5 hours (active metabolite). Distribution: Amlodipine: Crosses the placenta and enters breast milk. Volume of distribution: 21 L/kg. Plasma protein binding: Approx 93%.
Losartan: Volume of distribution: 34 L (losartan); 12 L (active metabolite). Plasma protein binding: >98%, mainly to albumin. Metabolism: Amlodipine: Extensively metabolised in the liver to inactive metabolites.
Losartan: Metabolised in the liver by CYP2C9 and CYP3A4 isoenzymes into E-3174 (active metabolite; more potent than losartan). Undergoes extensive first-pass metabolism. Excretion: Amlodipine: Via urine (10% of total dose as unchanged drug; 60% of total dose as metabolites). Terminal elimination half-life: 30-52 hours.
Losartan: 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).
Chemical Structure
Amlodipine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2162, Amlodipine. https://pubchem.ncbi.nlm.nih.gov/compound/Amlodipine. Accessed Feb. 25, 2025.
Losartan Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3961, Losartan. https://pubchem.ncbi.nlm.nih.gov/compound/Losartan. Accessed Feb. 25, 2025.
C09DB06 - losartan and amlodipine ; Belongs to the class of angiotensin II receptor blockers (ARBs) and calcium channel blockers. Used in the treatment of cardiovascular disease.
References
Amlife (Therapharma, Inc). MIMS Philippines. http://www.mims.com/philippines. Accessed 31/01/2025.Amlodipine and Losartan. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 10/02/2025.Amlodipine. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 10/02/2025.Brayfield A, Cadart C (eds). Amlodipine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 31/01/2025.Brayfield A, Cadart C (eds). Losartan Potassium. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 31/01/2025.Cozaar XQ 5/50 mg and 5/100 mg Tablet (Organon Malaysia Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 31/01/2025.Losartan. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 10/02/2025.
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