Adult: Initially, 5 mg given within 24 hours of MI for 2 days, then increased to 10 mg once daily. In patients with low systolic blood pressure: Initially, 2.5 mg once daily. Maintenance dose: 10 mg once daily; may decrease to 5 mg once daily with temporary reductions to 2.5 mg if needed. Continue treatment for 6 weeks. Adjust dose based on patient’s clinical response and tolerability.
Oral Diabetic nephropathy
Adult: In hypertensive patients with type 2 diabetes mellitus: 10 mg once daily. May increase to 20 mg once daily if needed, to achieve a sitting diastolic blood pressure of <90 mmHg.
Oral Hypertension
Adult: As monotherapy or in combination with other antihypertensives: Initially, 10 mg once daily. Give 1st dose preferably at bedtime. Patients with renovascular hypertension, salt and/or volume depletion, cardiac decompensation, severe hypertension: Initially, 2.5-5 mg once daily. Maintenance dose: 20-40 mg once daily. Max: 80 mg daily. Patients on diuretic: 5 mg once daily. Dose is adjusted according to blood pressure response. Child: 6-16 years weighing 20-<50 kg: Initially, 2.5 mg once daily. Max: 20 mg daily. ≥50 kg: 5 mg once daily. Max: 40 mg daily. Alternatively, 0.07 mg/kg once daily. Max 5 mg daily. Adjust dose according to blood pressure response. Max 0.61 mg/kg up to 40 mg once daily.
Oral Heart failure
Adult: As adjunctive therapy with diuretics and digitalis: Initially, 2.5 mg or 5 mg once daily, may increase by increments of not more than 10 mg at intervals of at least 2 weeks. Max: 35 mg or 40 mg daily. Dose is adjusted according to patient’s clinical response and tolerability.
Renal Impairment
Patient on dialysis: Initially, 2.5 mg once daily. Dose can be adjusted up to Max 40 mg daily according to patient's response.
CrCl (mL/min)
Dosage
<10
Initially, 2.5 mg once daily. Dose can be adjusted up to Max 40 mg daily according to patient's response.
10-30
Initially, 2.5-5 mg once daily. Dose can be adjusted up to Max 40 mg daily according to patient's response.
31-80
Initially, 5-10 mg once daily. Dose can be adjusted up to Max 40 mg daily according to patient's response.
Administration
May be taken with or without food.
Contraindications
Hypersensitivity. History of angioedema related to previous ACE inhibitor treatment, hereditary or idiopathic angioedema. Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73 m2). Concomitant use or within 36 hours of switching to or from a neprilysin inhibitor (e.g. sacubitril) or sacubitril/valsartan therapy. Pregnancy.
Special Precautions
Patient with severe aortic stenosis, hypertrophic cardiomyopathy and left ventricular outflow tract obstruction, CV disease (e.g. ischaemic heart disease, cerebrovascular disease), collagen vascular disease (e.g. SLE), ascites due to cirrhosis or refractory ascites, stenosis of the artery to a solitary kidney and bilateral renal artery stenosis; history of angioedema unrelated to ACE inhibitor therapy; risk factors for developing hyperkalaemia (e.g. diabetes mellitus, hypoaldosteronism); volume depletion (e.g. dietary salt restriction, dialysis, diarrhoea, vomiting, severe renin-dependent hypertension). Patient undergoing major surgery or during anaesthesia, and desensitisation treatment. Black race. Renal and hepatic impairment. Lactation. Children.
Adverse Reactions
Significant: Symptomatic hypotension with or without syncope; haematologic effects (e.g. neutropenia or agranulocytosis, anaemia, thrombocytopenia), cough, hyperkalaemia, cholestatic jaundice. Cardiac disorders: Tachycardia, palpitations. Ear and labyrinth disorders: Tinnitus. Gastrointestinal disorders: Nausea, diarrhoea, vomiting, abdominal pain, dry mouth, constipation, taste disturbance. General disorders and administration site conditions: Fatigue, asthenia. Investigations: Elevated serum creatinine, BUN increased. Musculoskeletal and connective tissue disorders: Arthralgia, myalgia. Nervous system disorders: Headache, vertigo, paraesthesia, dizziness. Psychiatric disorders: Hallucinations, mood alterations, sleep disturbance. Renal and urinary disorders: Renal dysfunction, oliguria, anuria. Reproductive system and breast disorders: Impotence, gynaecomastia. Respiratory, thoracic and mediastinal disorders: Rhinitis, sinusitis. Skin and subcutaneous tissue disorders: Pruritus, rash. Vascular disorders: Raynaud's phenomenon, flushing. Potentially Fatal: Hypersensitivity reactions (e.g. angioedema of the face, extremities, lips, tongue, anaphylactic or anaphylactoid reactions). Rarely, fulminant hepatic necrosis.
This drug may cause occasional dizziness or tiredness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor BP, heart rate, BUN, CBC with differential, LFTs, serum K, and creatinine levels. Assess for signs of angioedema, jaundice or hepatic failure.
Overdosage
Symptoms: Hypotension, circulatory shock, tachycardia, palpitations, bradycardia, hyperventilation, renal failure, electrolyte disturbances, anxiety, dizziness, and cough. Management: Administer IV infusion NaCl 0.9%. May perform gastric lavage, induce emesis, administer adsorbents and Na sulfate if ingestion is recent. In case of hypotension, place the patient in shock position. May also consider administration of angiotensin II infusion and/or IV catecholamines. May perform haemodialysis to remove from general circulation; pacemaker therapy for therapy-resistant bradycardia.
Drug Interactions
Increased risk of angioedema with racecadotril; mTOR inhibitors (e.g. everolimus, sirolimus, temsirolimus); vildagliptin, and tissue plasminogen activators. Increased risk of hyperkalaemia with K-sparing diuretics (e.g. spironolactone, amiloride), K supplements or K-containing salt substitutes, and drugs affecting serum K concentrations (e.g. heparin, trimethoprim, ciclosporin). May increase serum levels and toxicity of lithium. Additive hypotensive effect with other antihypertensives (e.g. nitrates, vasodilators), diuretics, TCAs, antipsychotics. Concomitant use with NSAIDs including selective COX-2 inhibitors may result to renal function deterioration and reduced antihypertensive effect. Coadministration with parenteral gold (e.g. Na aurothiomalate) may cause nitritoid reaction characterised by facial flushing, nausea, vomiting, and hypotension. Reduced antihypertensive effect with sympathomimetics. May increase hypoglycaemic effect of antidiabetics (e.g. insulin, oral hypoglycaemics agents). Potentially Fatal: Increased risk of angioedema with neprilysin inhibitors (e.g. sacubitril) or sacubitril/valsartan. May cause anaphylactoid reactions during LDL apheresis with dextran sulfate. Increased risk of hypotension, hyperkalaemia and decreased renal function (including acute renal failure) with aliskiren.
Lab Interference
May result to false-negative aldosterone/renin ratio (ARR).
Action
Description: Mechanism of Action: Lisinopril, a peptidyl dipeptidase inhibitor, is a competitive ACE inhibitor which prevents conversion of angiotensin I to angiotensin II (a potent vasoconstrictor), thereby increasing plasma renin activity and decreasing aldosterone secretion. Additionally, the decreased secretion of aldosterone may cause a small increase in serum K. Onset: 1 hour. Duration: 24 hours. Pharmacokinetics: Absorption: Slowly and incompletely absorbed from the gastrointestinal tract. Bioavailability: Approx 25%. Time to peak plasma concentration: Approx 7 hours. Distribution: Crosses the placenta. Metabolism: Not metabolised. Excretion: Mainly via urine (as unchanged drug). Elimination half-life: 12 hours.
Chemical Structure
Lisinopril Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5362119, Lisinopril. https://pubchem.ncbi.nlm.nih.gov/compound/Lisinopril. Accessed Apr. 27, 2022.
Storage
Store between 20-25°C. Protect from freezing and excessive heat.
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