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Medicine overview

Indications of Lipril

Lipril is an angiotensin-converting enzyme (ACE) inhibitor with the following evidence-based indications:

  • Hypertension (established/FDA-approved): Treatment of high blood pressure in adults and pediatric patients 6 years of age and older, alone or in combination with other antihypertensive agents.
  • Heart Failure (established/FDA-approved): Used as adjunct therapy (with diuretics and, where appropriate, digitalis) to reduce the signs and symptoms of symptomatic systolic (congestive) heart failure.
  • Acute Myocardial Infarction (established/FDA-approved): To improve survival in hemodynamically stable patients within 24 hours of an acute myocardial infarction.
  • Diabetic nephropathy / proteinuric chronic kidney disease (guideline-supported, often off-label): ACE inhibitors including Lipril are widely used per clinical practice guidelines to slow progression of proteinuric kidney disease, particularly in patients with diabetes.

Use of Lipril for any indication should be individualized and directed by a physician based on clinical assessment.

Composition

Each tablet of Lisinopril contains Lisinopril (as lisinopril dihydrate) as the active ingredient, typically formulated as oral tablets in strengths such as 2.5 mg, 5 mg, 10 mg, and 20 mg. Excipients vary by manufacturer and formulation.

Description

Lipril is a long-acting, orally active angiotensin-converting enzyme (ACE) inhibitor used primarily to manage high blood pressure and certain forms of heart disease. Unlike some other ACE inhibitors, Lipril is not a prodrug — it is pharmacologically active in its administered form and does not require hepatic metabolism for activation. It has a relatively long duration of action, allowing once-daily dosing in most patients.

Therapeutic Class

Lipril belongs to the therapeutic class of Angiotensin-Converting Enzyme (ACE) Inhibitors, a group of medicines used mainly for cardiovascular and renal conditions.

Pharmacology

Lisinopril inhibits angiotensin-converting enzyme (ACE), the enzyme responsible for converting angiotensin I to angiotensin II, a potent vasoconstrictor that also stimulates aldosterone secretion. By blocking this conversion, Lisinopril reduces peripheral vascular resistance, lowers blood pressure, and decreases aldosterone-mediated sodium and water retention. It also reduces degradation of bradykinin, a vasodilator peptide, which contributes to its antihypertensive effect but is also implicated in the characteristic dry cough and angioedema associated with this drug class.

Pharmacokinetics

  • Absorption: Oral bioavailability is approximately 25%; largely unaffected by food.
  • Distribution: Minimal plasma protein binding; does not appear to undergo hepatic metabolism.
  • Elimination: Excreted unchanged in urine; effective half-life of approximately 12 hours with an accumulation half-life of 30+ hours at steady state, permitting once-daily dosing.

Dosage & Administration of Lipril

Dosage of Lipril must be individualized by a physician based on the indication, blood pressure response, and renal function.

Hypertension

PopulationDose
Adults (not on diuretic)Initial 10 mg once daily; usual maintenance 20-40 mg once daily; maximum 80 mg/day
Adults on diureticInitial 5 mg once daily to reduce risk of symptomatic hypotension
Pediatric ≥6 yearsInitial 0.07 mg/kg (up to 5 mg) once daily; titrated per response up to a maximum of 0.61 mg/kg or 40 mg/day

Heart Failure

Initial dose 5 mg once daily (2.5 mg once daily if serum sodium is low or the patient is hypotensive), titrated as tolerated toward a target dose of 20-40 mg once daily.

Acute Myocardial Infarction

2.5-5 mg within 24 hours of symptom onset, followed by 5 mg at 24 hours, 10 mg at 48 hours, and 10 mg once daily thereafter for at least 6 weeks; lower starting doses are used if systolic blood pressure is low.

Renal Impairment

Dose reduction of Lipril is required based on creatinine clearance; see Use in Special Populations for details.

Administration of Lipril

Lipril is taken orally, once daily, with or without food, at approximately the same time each day. Tablets should be swallowed with water. Do not stop taking Lipril or change the dose without consulting a physician, even if blood pressure feels normal.

Interaction of Lipril

Lipril has several clinically significant drug interactions:

  • Potassium-sparing diuretics, potassium supplements, salt substitutes: Increased risk of hyperkalemia.
  • NSAIDs (e.g., ibuprofen, indomethacin): May reduce the antihypertensive effect of Lipril and increase the risk of renal impairment, particularly in volume-depleted or elderly patients.
  • Lithium: ACE inhibitors reduce lithium excretion, increasing the risk of lithium toxicity; monitor lithium levels closely.
  • Other antihypertensives and diuretics: Additive hypotensive effect, especially with the first dose.
  • Aliskiren: Combination with Lipril is contraindicated in patients with diabetes due to increased risk of hyperkalemia, hypotension, and renal impairment (see Contraindications).
  • Sacubitril/valsartan and mTOR inhibitors (e.g., sirolimus, everolimus, temsirolimus): Increased risk of angioedema; do not administer Lipril within 36 hours of switching to or from sacubitril/valsartan.
  • Antidiabetic agents (insulin, oral hypoglycemics): May enhance blood-glucose-lowering effect, increasing hypoglycemia risk.

Contraindications

Lisinopril is contraindicated in:

  • Patients with known hypersensitivity to Lisinopril or any other ACE inhibitor.
  • Patients with a history of angioedema related to previous treatment with an ACE inhibitor.
  • Patients with hereditary or idiopathic angioedema.
  • Pregnancy — Lisinopril can cause fetal injury and death when used during pregnancy (see boxed warning under Pregnancy and Lactation).
  • Concomitant use with aliskiren in patients with diabetes mellitus.

Side Effects of Lipril

Common side effects of Lipril include:

  • Dry, persistent, non-productive cough (a well-known class effect of ACE inhibitors)
  • Dizziness or lightheadedness, especially after the first dose
  • Headache
  • Fatigue
  • Nausea
  • Hyperkalemia (elevated blood potassium)
  • Hypotension

Less common but serious effects include angioedema (swelling of the face, lips, tongue, or throat — see Precautions and Warnings), acute renal failure, neutropenia/agranulocytosis (rare), hepatic dysfunction, and severe skin reactions such as Stevens-Johnson syndrome. Any signs of facial or throat swelling, or difficulty breathing or swallowing, while taking Lipril require immediate emergency medical attention.

Pregnancy & Lactation

Pregnancy

Boxed Warning: Lipril can cause fetal injury and death when used during pregnancy, particularly during the second and third trimesters. Lipril must be discontinued as soon as possible once pregnancy is detected, unless continued use is considered essential and no suitable alternative exists. Women of childbearing potential should be counseled about this risk before starting therapy.

Lactation

Small amounts of Lipril may pass into breast milk. Because of the potential for serious adverse effects in a nursing infant, breastfeeding is generally not recommended during treatment with Lipril; use only if clearly needed and the potential benefit justifies the potential risk, and only under close medical supervision. Consult a physician before breastfeeding while taking Lipril.

Precautions & Warnings

Angioedema: Lipril can cause angioedema of the face, lips, tongue, glottis, and/or larynx at any time during treatment, including after the first dose. If there is any evidence of airway involvement (stridor, difficulty breathing or swallowing), Lipril should be discontinued immediately and emergency medical treatment sought. Patients with a history of angioedema unrelated to ACE inhibitor use may be at increased risk.

Hypotension: Symptomatic hypotension may occur, particularly after the first dose, in volume- or salt-depleted patients (e.g., those on diuretics, a low-salt diet, dialysis, or with vomiting/diarrhea). Correct volume depletion before starting Lipril where possible.

Renal impairment: In patients with bilateral renal artery stenosis or stenosis of the artery to a single functioning kidney, Lipril may cause deterioration of renal function and acute renal failure. Monitor renal function periodically during treatment.

Hyperkalemia: Risk is increased in patients with renal impairment, diabetes, or those taking potassium supplements, potassium-sparing diuretics, or potassium-containing salt substitutes.

Neutropenia/agranulocytosis: Rare but reported, more often in patients with collagen vascular disease and/or renal impairment; periodic monitoring of white blood cell counts may be considered in such patients.

Cough: A persistent, dry, non-productive cough is a recognized class effect of Lipril and other ACE inhibitors, typically resolving after discontinuation.

Anaphylactoid reactions: Rare reactions have been reported during desensitization treatments or dialysis/apheresis procedures using certain membranes in patients taking Lipril; inform the treating team if taking this medicine before such procedures.

Overdose Effects of Lipril

The most likely manifestation of Lipril overdose is significant hypotension, which may be accompanied by dizziness, weakness, bradycardia, electrolyte disturbances, and renal impairment. If overdose of Lipril is suspected, seek immediate medical attention or contact a poison control center right away. Treatment is generally supportive; the patient should be closely monitored, and emergency medical personnel may administer intravenous fluids and other supportive measures as needed. Do not attempt to manage a suspected Lipril overdose at home.

Storage Conditions

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Use In Special Populations

Renal Impairment

Creatinine ClearanceRecommended Dose Adjustment
>30 mL/minNo dose adjustment typically required
10-30 mL/minInitial dose 5 mg once daily
<10 mL/min (including hemodialysis)Initial dose 2.5 mg once daily; adjust based on blood pressure response

Hepatic Impairment

No specific dose adjustment is established for hepatic impairment, but ACE inhibitors including Lipril have rarely been associated with a syndrome of cholestatic jaundice progressing to fulminant hepatic necrosis; discontinue Lipril immediately if jaundice or marked liver enzyme elevation occurs.

Elderly

Elderly patients may be more sensitive to the blood-pressure-lowering effects of Lipril; dosing typically starts at the lower end of the range with close monitoring.

Pediatric

Safety and efficacy of Lipril for hypertension have been established in children 6 years of age and older; safety and efficacy in children under 6 years or in pediatric patients with glomerular filtration rate less than 30 mL/min/1.73m² have not been established. See Pediatric Uses.

Duration Of Treatment

Lipril is generally used long-term for chronic conditions such as hypertension and heart failure, often for the remainder of the patient's life, since these are ongoing conditions requiring sustained blood pressure and cardiac risk control. For post-myocardial infarction use, treatment with Lipril is typically continued indefinitely or as directed by the treating physician, with a minimum treatment period of about 6 weeks studied in clinical trials. Duration should always be determined by a physician based on ongoing clinical assessment.

Drug Classes

Lisinopril is classified as an Angiotensin-Converting Enzyme (ACE) Inhibitor.

Mode Of Action

Lisinopril works by inhibiting the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. This reduces vasoconstriction and aldosterone release, resulting in lowered blood pressure, decreased cardiac workload, and reduced sodium/water retention. It also increases levels of bradykinin, which contributes further to vasodilation.

Pregnancy

D

Pediatric Uses

Lipril is approved for the treatment of hypertension in pediatric patients 6 years of age and older. Dosing is weight-based, starting at approximately 0.07 mg/kg once daily (up to a maximum of 5 mg), titrated based on blood pressure response, up to a maximum of 0.61 mg/kg (not exceeding 40 mg) once daily. Lipril has not been studied in children under 6 years of age or in pediatric patients with glomerular filtration rate less than 30 mL/min/1.73m², and safety and efficacy in these groups have not been established. Lipril is not indicated for the treatment of heart failure or acute myocardial infarction in pediatric patients, as these uses have not been studied in children.

Frequently Asked Questions

Q: What is Lipril 5 mg Tablet used for?

A: Lipril 5 mg Tablet is mainly used to treat high blood pressure (hypertension), manage heart failure alongside other medicines, and improve survival after a heart attack. It may also be used off-label to help protect kidney function in certain patients with diabetes.

Q: How should I take Lipril 5 mg Tablet?

A: Lipril 5 mg Tablet is usually taken once daily, by mouth, with or without food, at the same time each day. Do not stop or change your dose without talking to your doctor, even if you feel well, since blood pressure control needs consistent daily dosing.

Q: Can I take Lipril 5 mg Tablet during pregnancy?

A: No. Lipril 5 mg Tablet carries a boxed warning because it can cause serious injury or death to an unborn baby, especially if used during the second or third trimester. If you become pregnant while taking Lipril 5 mg Tablet, contact your doctor immediately so treatment can be reviewed. Women who may become pregnant should discuss safer alternatives with their doctor.

Q: Why do I have a dry cough since starting Lipril 5 mg Tablet?

A: A persistent, dry, tickling cough is a well-known side effect of Lipril 5 mg Tablet and other ACE inhibitors, thought to be related to increased bradykinin levels. It is not dangerous but can be bothersome; if troublesome, talk to your doctor, who may consider switching you to a different class of medicine.

Q: What should I do if my face or throat starts swelling while on Lipril 5 mg Tablet?

A: Facial, lip, tongue, or throat swelling (angioedema) is a rare but potentially life-threatening reaction to Lipril 5 mg Tablet. Stop taking Lipril 5 mg Tablet immediately and seek emergency medical care right away if you notice any swelling, difficulty breathing, or difficulty swallowing.

Q: What happens if I take too much Lipril 5 mg Tablet?

A: An overdose of Lipril 5 mg Tablet can cause a significant drop in blood pressure, dizziness, and weakness. If you or someone else has taken more than the prescribed amount of Lipril 5 mg Tablet, seek immediate medical attention or contact a poison control center; do not try to treat an overdose at home.

Disclaimer

The information provided is accurate to the best of our knowledge, but it does not replace professional medical advice. We cannot guarantee its completeness or accuracy, and the absence of specific information about a drug should not be taken as an endorsement. We are not responsible for any consequences arising from this information, so please consult a healthcare professional for any concerns or questions.

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