Lisinopril

Brand names: Lisinopril and Hydrochlorothiazide, Lisinopril, LISINOPRIL, lisinopril, Zestril, Qbrelis

Boxed warning

WARNING: FETAL TOXICITY When pregnancy is detected, discontinue l isinopril as soon as possible [see Warnings and Precautions (5.1)] . Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus [see Warnings and Precautions (5.1)]. WARNING: FETAL TOXICITY See full prescribing information for complete boxed warning. When pregnancy is detected, discontinue lisinopril tablets as soon as possible. ( 5.1 ) Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. ( 5.1 )

Warnings

BOXED WARNING: BOXED WARNING - FETAL TOXICITY: "When pregnancy is detected, discontinue Lisinopril Tablets as soon as possible." ACE inhibitors can cause injury and death to developing fetuses, particularly during the second and third trimesters. Key warnings include: - Angioedema: Can occur at any time; may involve face, lips, tongue, or airway—potentially fatal - Renal impairment: Monitor kidney function; risk of acute renal failure in vulnerable patients - Hypotension: Risk especially in heart failure, volume depletion, or concurrent diuretic use - Hyperkalemia: Monitor potassium levels; increased risk with renal insufficiency or diabetes | BOXED WARNING - FETAL TOXICITY: "When pregnancy is detected, discontinue Lisinopril Tablets as soon as possible." ACE inhibitors can cause injury and death to developing fetuses, particularly during the second and third trimesters. Key warnings include: - Angioedema: Can occur at any time; may involve face, lips, tongue, or airway—potentially fatal - Renal impairment: Monitor kidney function; risk of acute renal failure in vulnerable patients - Hypotension: Risk especially in heart failure, volume depletion, or concurrent diuretic use - Hyperkalemia: Monitor potassium levels; increased risk with renal insufficiency or diabetes

Contraindications

4 CONTRAINDICATIONS Lisinopril tablets are contraindicated in combination with a neprilysin inhibitor (e.g., sacubitril). Do not administer lisinopril tablets within 36 hours of switching to or from sacubitril/valsartan, a neprilysin inhibitor [see Warnings and Precautions ( 5.2 )]. Lisinopril tablets are contraindicated in patients with: a history of angioedema or hypersensitivity related to previous treatment with an angiotensin converting enzyme inhibitor hereditary or idiopathic angioedema Do not co-administer aliskiren with lisinopril tablets in patients with diabetes [see Drug Interactions ( 7.4 )]. Angioedema or a history of hereditary or idiopathic angioedema ( 4 ) Hypersensitivity ( 4 ) Co-administration of aliskiren with lisinopril tablets in patients with diabetes ( 4 , 7.4 )

Overdose

10 OVERDOSAGE Following a single oral dose of 20 g/kg no lethality occurred in rats, and death occurred in one of 20 mice receiving the same dose. The most likely manifestation of overdosage would be hypotension, for which the usual treatment would be intravenous infusion of normal saline solution. Lisinopril can be removed by hemodialysis [see Clinical Pharmacology ( 12.3 )] .

Drug interactions

7 DRUG INTERACTIONS Diuretics: Excessive drop in blood pressure ( 7.1 ) NSAIDS: Increased risk of renal impairment and loss of antihypertensive efficacy ( 7.3 ) Dual inhibition of the renin-angiotensin system: Increased risk of renal impairment, hypotension and hyperkalemia ( 7.4 ) Lithium: Symptoms of lithium toxicity ( 7.5 ) Gold: Nitritoid reactions have been reported ( 7.6 ) Concomitant mTOR inhibitor or neprilysin inhibitor use may increase angioedema risk ( 7.7 , 7.8) 7.1 Diuretics Initiation of lisinopril in patients on diuretics may result in excessive reduction of blood pressure. The possibility of hypotensive effects with lisinopril can be minimized by either decreasing or discontinuing the diuretic or increasing the salt intake prior to initiation of treatment with lisinopril. If this is not possible, reduce the starting dose of lisinopril [see Dosage and Administration ( 2.2 ) and Warnings and Precautions ( 5.4 )] . Lisinopril attenuates potassium loss caused by thiazide-type diuretics. Potassium-sparing diuretics (spironolactone, amiloride, triamterene, and others) can increase the risk of hyperkalemia. Therefore, if concomitant use of such agents is indicated, monitor the patient’s serum potassium frequently. 7.2 Antidiabetics Concomitant administration of lisinopril and antidiabetic medicines (insulins, oral hypoglycemic agents) may cause an increased blood-glucose-lowering effect with risk of hypoglycemia. 7.3 Non-Steroidal Anti-Inflammatory Agents Including Selective Cyclooxygenase-2 Inhibitors (COX-2 Inhibitors) In patients who are elderly, volume-depleted (including those on diuretic therapy), or with compromised renal function, coadministration of NSAIDs, including selective COX-2 inhibitors, with ACE inhibitors, including lisinopril, may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible. Monitor renal function periodically in patients receiving lisinopril and NSAID therapy. The antihypertensive effect of ACE inhibitors, including lisinopril, may be attenuated by NSAIDs. 7.4 Dual Blockade of the Renin-Angiotensin System (RAS) Dual blockade of the RAS with angiotensin receptor blockers, ACE inhibitors, or aliskiren is associated with increased risks of hypotension, hyperkalemia, and changes in renal function (including acute renal failure) compared to monotherapy. The VA NEPHRON trial enrolled 1448 patients with type 2 diabetes, elevated urinary-albumin-to-creatinine ratio, and decreased estimated glomerular filtration rate (GFR 30 to 89.9 mL/min), randomized them to lisinopril or placebo on a background of losartan therapy and followed them for a median of 2.2 years. Patients receiving the combination of losartan and lisinopril did not obtain any additional benefit compared to monotherapy for the combined endpoint of decline in GFR, end state renal disease, or death, but experienced an increased incidence of hyperkalemia and acute kidney injury compared with the monotherapy group. In general, avoid combined use of RAS inhibitors. Closely monitor blood pressure, renal function and electrolytes in patients on lisinopril and other agents that affect the RAS. Do not co-administer aliskiren with lisinopril in patients with diabetes. Avoid use of aliskiren with lisinopril in patients with renal impairment (GFR < 60 mL/min). 7.5 Lithium Lithium toxicity has been reported in patients receiving lithium concomitantly with drugs, which cause elimination of sodium, including ACE inhibitors. Lithium toxicity was usually reversible upon discontinuation of lithium and the ACE inhibitor. Monitor serum lithium levels during concurrent use. 7.6 Gold Nitritoid reactions (symptoms include facial flushing, nausea, vomiting and hypotension) have been reported rarely in patients on therapy with injectable gold (sodium aurothiomalate) and concomitant ACE inhibitor therapy including lisinopril. 7.7 mTOR Inhibitors Patients taking concomitant mTOR inhibitor (e.g., temsirolimus, sirolimus, everolimus) therapy may be at increased risk for angioedema [see Warnings and Precautions ( 5.2 )] . 7.8 Neprilysin Inhibitor Patients taking concomitant neprilysin inhibitors may be at increased risk for angioedema [see Warnings and Precautions (5.2)].

Uses

Lisinopril is indicated for: treatment of hypertension in adults and pediatric patients 6 years and older; adjunct therapy for heart failure; and reduction of mortality following acute myocardial infarction. The medication works by lowering blood pressure to reduce risk of cardiovascular events like strokes and heart attacks.

Dosage forms & strengths

Tablet TABLET POWDER SOLUTION
LISINOPRIL 10 mg HYDROCHLOROTHIAZIDE 12.5 mg LISINOPRIL 2.5 mg LISINOPRIL 20 mg HYDROCHLOROTHIAZIDE 25 mg LISINOPRIL 30 mg LISINOPRIL 40 mg LISINOPRIL 5 mg LISINOPRIL 40 mg/1 LISINOPRIL 10 mg/1 LISINOPRIL 2.5 mg/1 LISINOPRIL 30 mg/1 LISINOPRIL 20 mg/1 LISINOPRIL 5 mg/1 LISINOPRIL 10 kg/10kg LISINOPRIL 1 kg/kg LISINOPRIL 1 mg/mL

2 DOSAGE AND ADMINISTRATION Hypertension: Initial adult dose is 10 mg once daily. Titrate up to 40 mg daily based on blood pressure response. Initiate patients on diuretics at 5 mg once daily ( 2.1 ) Pediatric patients with glomerular filtration rate > 30 mL/min/1.73m 2 : Initial dose in patients 6 years of age and older is 0.07 mg per kg (up to 5 mg total) once daily ( 2.1 ) Heart Failure: Initiate with 5 mg once daily. Increase dose as tolerated to 40 mg daily ( 2.2 ) Acute Myocardial Infarction (MI): Give 5 mg within 24 hours of MI. Followed by 5 mg after 24 hours, then 10 mg once daily ( 2.3 ) Renal Impairment: For patients with creatinine clearance ≥ 10 mL/min and ≤ 30 mL/min, halve usual initial dose. For patients with creatinine clearance < 10 mL/min or on hemodialysis, the recommended initial dose is 2.5 mg ( 2.4 ) 2.1 Hypertension Initial Therapy in adults: The recommended initial dose is 10 mg once a day. Dosage should be adjusted according to blood pressure response. The usual dosage range is 20 mg to 40 mg per day administered in a single daily dose. Doses up to 80 mg have been used but do not appear to give greater effect. Use with diuretics in adults If blood pressure is not controlled with lisinopril tablets alone, a low dose of a diuretic may be added (e.g., hydrochlorothiazide, 12.5 mg). After the addition of a diuretic, it may be possible to reduce the dose of lisinopril tablets. The recommended starting dose in adult patients with hypertension taking diuretics is 5 mg once per day. Pediatric Patients 6 years of age and older with hypertension For pediatric patients with glomerular filtration rate > 30 mL/min/1.73m 2 , the recommended starting dose is 0.07 mg per kg once daily (up to 5 mg total). Dosage should be adjusted according to blood pressure response up to a maximum of 0.61 mg per kg (up to 40 mg) once daily. Doses above 0.61 mg per kg (or in excess of 40 mg) have not been studied in pediatric patients [see Clinical Pharmacology ( 12.3 )] . Lisinopril tablets are not recommended in pediatric patients < 6 years or in pediatric patients with glomerular filtration rate < 30 mL/min/1.73m 2 [see Use in Specific Populations ( 8.4 ) and Clinical Studies ( 14.1 )] . 2.2 Heart Failure The recommended starting dose for lisinopril tablets, when used with diuretics and (usually) digitalis as adjunctive therapy for systolic heart failure, is 5 mg once daily. The recommended starting dose in these patients with hyponatremia (serum sodium < 130 mEq/L) is 2.5 mg once daily. Increase as tolerated to a maximum of 40 mg once daily. Diuretic dose may need to be adjusted to help minimize hypovolemia, which may contribute to hypotension [see Warnings and Precautions ( 5.4 ), and Drug Interactions ( 7.1 )] . The appearance of hypotension after the initial dose of lisinopril tablets does not preclude subsequent careful dose titration with the drug, following effective management of the hypotension. 2.3 Reduction of Mortality in Acute Myocardial Infarction In hemodynamically stable patients within 24 hours of the onset of symptoms of acute myocardial infarction, give lisinopril tablets 5 mg orally, followed by 5 mg after 24 hours, 10 mg after 48 hours and then 10 mg once daily. Dosing should continue for at least six weeks. Initiate therapy with 2.5 mg in patients with a low systolic blood pressure (≤ 120 mmHg and > 100 mmHg) during the first 3 days after the infarct [see Warnings and Precautions ( 5.4 )] . If hypotension occurs (systolic blood pressure ≤ 100 mmHg) a daily maintenance dose of 5 mg may be given with temporary reductions to 2.5 mg if needed. If prolonged hypotension occurs (systolic blood pressure < 90 mmHg for more than 1 hour) lisinopril tablets should be withdrawn. 2.4 Dose in Patients with Renal Impairment No dose adjustment of lisinopril tablets is required in patients with creatinine clearance > 30 mL/min. In patients with creatinine clearance ≥ 10 mL/min and ≤ 30 mL/min, reduce the initial dose of lisinopril tablets to half of the usual recommended dose i.e., hypertension, 5 mg; systolic heart failure, 2.5 mg and acute MI, 2.5 mg. Up titrate as tolerated to a maximum of 40 mg daily. For patients on hemodialysis or creatinine clearance < 10 mL/min, the recommended initial dose is 2.5 mg once daily [see Use in Specific Populations ( 8.7 ) and Clinical Pharmacology ( 12.3 )] .

All identified pills

Side effects

Hypertension: headache (3.8% above placebo), dizziness (3.5%), cough (2.5%) Heart Failure: hypotension (3.8% above placebo), chest pain (2.1%) Acute MI: higher incidence of hypotension and renal dysfunction compared to untreated patients

Official source

DailyMed