Zestril: Effective Blood Pressure Control and Cardiovascular Protection
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Synonyms | |||
Zestril (lisinopril) is an angiotensin-converting enzyme (ACE) inhibitor prescribed for the management of hypertension, heart failure, and post-myocardial infarction care. As a cornerstone therapy in cardiovascular medicine, it works by inhibiting the conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, thereby promoting vasodilation and reducing peripheral arterial resistance. Its well-established efficacy, once-daily dosing convenience, and demonstrated organ-protective effects make it a first-line choice for clinicians seeking to mitigate long-term cardiovascular risk in appropriate patient populations. This comprehensive profile details its pharmacological characteristics, clinical applications, and essential safety information.
Features
- Active ingredient: Lisinopril
- Pharmacological class: Angiotensin-converting enzyme (ACE) inhibitor
- Available strengths: 2.5 mg, 5 mg, 10 mg, 20 mg, 30 mg, 40 mg tablets
- Standard dosing: Once daily administration
- Onset of action: Within 1 hour; peak antihypertensive effect at 6 hours
- Duration of action: 24 hours
- Elimination half-life: 12 hours
- Excretion: Primarily renal
Benefits
- Effectively lowers systolic and diastolic blood pressure, reducing strain on the heart and arterial system
- Demonstrates cardioprotective properties by improving survival rates following myocardial infarction
- Provides renal protective effects in hypertensive patients with diabetes by reducing proteinuria
- Decreases preload and afterload in heart failure patients, improving exercise tolerance and symptoms
- Offers convenient once-daily dosing that supports medication adherence
- Shows evidence of reducing hospitalizations for heart failure exacerbations
Common use
Zestril is primarily indicated for the treatment of hypertension, either as monotherapy or in combination with other antihypertensive agents. It is also approved for the management of congestive heart failure as adjunctive therapy when diuretics and digitalis provide insufficient response. Additionally, it is used to improve survival in hemodynamically stable patients within 24 hours of acute myocardial infarction. Off-label uses may include diabetic nephropathy management and prevention of migraine headaches in certain patient populations, though these applications require careful clinical consideration.
Dosage and direction
For hypertension: Initial dose typically ranges from 10-40 mg once daily, with maintenance doses adjusted according to blood pressure response. Maximum recommended daily dose is 80 mg.
For heart failure: Starting dose is usually 5 mg once daily, with gradual titration to a maximum of 40 mg daily as tolerated.
Post-myocardial infarction: Initiate with 5 mg within 24 hours of onset, followed by 5 mg after 24 hours, 10 mg after 48 hours, then maintenance of 10 mg daily for 6 weeks.
Dosage adjustment is necessary in renal impairment: CrCl 10-30 mL/min: initial dose 2.5-5 mg daily; CrCl <10 mL/min: initial dose 2.5 mg daily.
Administration should occur at approximately the same time each day, with or without food. Tablets should be swallowed whole with a glass of water.
Precautions
Patients should be monitored for signs of angioedema, particularly during the first month of therapy. Renal function and serum potassium levels require regular assessment, especially in patients with pre-existing renal impairment, diabetes, or those taking potassium supplements or potassium-sparing diuretics. Volume-depleted patients (from diuretic therapy, salt restriction, or gastrointestinal losses) may experience excessive hypotension with initial dosing. Caucasian patients may have increased risk of angioedema compared to other racial groups. Periodic monitoring of white blood cell counts is recommended in patients with collagen vascular disease or renal impairment.
Contraindications
Zestril is contraindicated in patients with known hypersensitivity to lisinopril or any other ACE inhibitor. It must not be used in patients with a history of angioedema related to previous ACE inhibitor therapy. Additional contraindications include concomitant use with aliskiren in patients with diabetes and use during the second and third trimesters of pregnancy due to risk of fetal injury and death. It is also contraindicated in patients with hereditary or idiopathic angioedema.
Possible side effect
Common adverse reactions (≥1%) include: dizziness (12%), headache (5%), cough (5%), fatigue (3%), diarrhea (3%), upper respiratory infection (2%), nausea (2%), and chest pain (2%). Less frequent but serious side effects may include: angioedema (0.1-0.7%), hypotension (2-4%), hyperkalemia (2-5%), renal impairment (1-2%), and neutropenia/agranulocytosis (rare). The characteristic dry, persistent cough typically resolves upon discontinuation of therapy.
Drug interaction
Significant interactions occur with potassium supplements, potassium-sparing diuretics, and salt substitutes containing potassium, increasing hyperkalemia risk. Concurrent use with NSAIDs may reduce antihypertensive effects and increase renal impairment risk. Diuretic therapy may potentiate hypotensive effects, particularly with initial dosing. Lithium levels may increase with concomitant ACE inhibitor use. Dual blockade of the renin-angiotensin system with ARBs or aliskiren increases risks of hypotension, hyperkalemia, and renal impairment. Antidiabetic agents may require dosage adjustment due to potential hypoglycemic effects.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed administration. Consistent daily timing is recommended to maintain stable blood pressure control.
Overdose
Symptoms of overdose primarily manifest as marked hypotension, which may progress to shock. Bradycardia, electrolyte disturbances, and renal failure may also occur. Management includes volume expansion with normal saline and placing the patient in supine position. Hemodialysis effectively removes lisinopril from the circulation. Supportive measures should include continuous monitoring of vital signs, electrolyte levels, and renal function. Vasopressors may be required in severe cases of hypotension unresponsive to volume expansion.
Storage
Store at controlled room temperature (20-25°C or 68-77°F) in the original container with the lid tightly closed. Protect from moisture and excessive heat. Keep out of reach of children and pets. Do not use beyond the expiration date printed on the packaging. Tablets should be discarded if they show signs of discoloration, cracking, or other physical deterioration.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Zestril is a prescription medication that should only be used under the supervision of a qualified healthcare professional. Dosage and treatment decisions must be made by a physician based on individual patient assessment. Patients should not alter their medication regimen without consulting their healthcare provider. The full prescribing information contains complete details regarding indications, warnings, and precautions.
Reviews
Clinical studies demonstrate Zestril’s efficacy in reducing blood pressure by approximately 8-12/5-8 mmHg in hypertensive patients. The GISSI-3 trial showed a significant reduction in mortality when initiated early after myocardial infarction. SOLVD trials demonstrated 16% reduction in mortality and 26% reduction in hospitalization for heart failure exacerbations. Patient satisfaction surveys indicate high adherence rates due to once-daily dosing and generally favorable side effect profile, though the characteristic cough remains a notable reason for discontinuation in approximately 3-5% of patients. Long-term follow-up studies confirm sustained antihypertensive efficacy and cardiovascular protection over treatment periods exceeding 10 years.