Zestril: Effective Blood Pressure Control and Heart Failure Management
Zestril
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| Product dosage: 2.5mg | |||
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| Product dosage: 5mg | |||
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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 and once-daily dosing regimen make it a widely trusted option for long-term cardiovascular risk reduction. This medication represents a critical component in comprehensive treatment plans aimed at improving cardiac outcomes and patient survival.
Features
- Active pharmaceutical ingredient: Lisinopril
- Available in tablet strengths: 2.5 mg, 5 mg, 10 mg, 20 mg, 30 mg, 40 mg
- Administration: Oral, once daily
- Mechanism: Competitive inhibitor of angiotensin-converting enzyme (ACE)
- Half-life: Approximately 12 hours
- Bioavailability: ~25%, with peak plasma concentrations achieved within 7 hours
- Excretion: Primarily renal (unchanged)
- Pregnancy category: D (contraindicated in second and third trimester)
Benefits
- Significantly reduces systolic and diastolic blood pressure through effective vasodilation
- Decreases mortality in patients with congestive heart failure when used as part of standard therapy
- Improves survival rates following acute myocardial infarction
- Slows progression of diabetic nephropathy in hypertensive patients with type 2 diabetes
- Reduces afterload on the heart, improving cardiac output in heart failure patients
- Provides 24-hour blood pressure control with single daily dosing in most patients
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, typically as adjunctive therapy with diuretics and digitalis. Additionally, it is used to improve survival in hemodynamically stable patients within 24 hours of acute myocardial infarction. Off-label uses may include prevention of migraine headaches and management of proteinuria in certain renal conditions, though these applications require careful specialist supervision.
Dosage and direction
The initial dosage for hypertension in adults not taking diuretics is 10 mg once daily, which may be increased to a maintenance dose of 20-40 mg daily based on blood pressure response. For heart failure, starting dose is typically 2.5-5 mg once daily, with gradual titration to a target maintenance dose of 20-40 mg daily. Post-myocardial infarction patients may begin with 5 mg within 24 hours of symptoms, followed by 5 mg after 24 hours, 10 mg after 48 hours, and then 10 mg daily for six weeks. Dosage adjustment is necessary in renal impairment: for creatinine clearance 10-30 mL/min, initial dose is 2.5-5 mg daily; below 10 mL/min, initial dose is 2.5 mg daily. Tablets should be taken at approximately the same time each day, with or without food, and swallowed whole with water.
Precautions
Patients should be monitored for hypotension, especially during initial titration and in volume-depleted individuals. Regular assessment of renal function and serum potassium is essential, particularly in patients with renal impairment, diabetes, or those taking potassium supplements or potassium-sparing diuretics. Angioedema may occur at any time during treatment, requiring immediate discontinuation. Neutropenia/agranulocytosis has been reported, making periodic white blood cell counts advisable in patients with collagen vascular disease or renal impairment. Cough, usually non-productive and persistent, may develop and typically resolves upon discontinuation. Use with caution in patients with aortic stenosis or hypertrophic cardiomyopathy.
Contraindications
Zestril is contraindicated in patients with a history of angioedema related to previous ACE inhibitor treatment or hereditary angioedema. It must not be used during the second and third trimesters of pregnancy due to risk of fetal injury and death. Concomitant use with aliskiren in patients with diabetes is contraindicated. Additional contraindications include hypersensitivity to lisinopril or any component of the formulation and concomitant use with sacubitril/valsartan (must allow 36-hour washout period).
Possible side effect
Common adverse reactions include dizziness (6-12%), headache (5-6%), cough (3-9%), fatigue (3-5%), and nausea (2-4%). Less frequently observed effects include orthostatic hypotension, rash, impotence, diarrhea, and taste disturbance. Serious side effects requiring medical attention include angioedema (0.1-0.7%), hyperkalemia, renal impairment, neutropenia/agranulocytosis, and hepatotoxicity. Hypotension may occur particularly in volume-depleted patients or those with heart failure.
Drug interaction
Significant interactions occur with potassium supplements, potassium-sparing diuretics, and salt substitutes containing potassium, increasing hyperkalemia risk. Nonsteroidal anti-inflammatory drugs (NSAIDs) may reduce antihypertensive effects and increase renal impairment risk. Dual blockade of the renin-angiotensin system with ARBs or aliskiren increases adverse event risk. Lithium levels may increase due to reduced renal clearance. Antidiabetic agents may require dosage adjustment due to potential hypoglycemic effects. Diuretics may potentiate first-dose hypotension.
Missed dose
If a dose is missed, it should be taken as soon as remembered on the same day. However, if it is near the time for the next scheduled dose, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not take a double dose to make up for a missed dose. Consistency in daily administration is important for maintaining stable blood pressure control, so establishing a routine (such as taking the medication with a daily activity) is recommended.
Overdose
Symptoms of overdose may include severe hypotension, bradycardia, circulatory shock, electrolyte disturbances, and renal failure. Management involves supportive care with volume expansion with normal saline to treat hypotension. Lisinopril is not effectively removed by hemodialysis due to extensive tissue binding. Patients should be monitored in an intensive care setting with continuous blood pressure and ECG monitoring. Vasopressors may be required in cases of severe hypotension unresponsive to volume expansion.
Storage
Store at controlled room temperature between 20-25°C (68-77°F), with excursions permitted between 15-30°C (59-86°F). Keep container tightly closed and protect from moisture and light. Keep out of reach of children and pets. Do not use tablets that are discolored or show signs of deterioration. Properly discard any unused medication after the expiration date printed on the packaging.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Individual patient requirements may vary based on specific health conditions, concomitant medications, and other factors. Always consult with a qualified healthcare professional before starting, stopping, or changing any medication regimen. Do not disregard professional medical advice or delay seeking it based on information contained herein. The prescribing physician should be the ultimate authority regarding appropriate treatment decisions.
Reviews
Clinical studies demonstrate Zestril’s efficacy in reducing blood pressure by 10-15 mmHg systolic and 5-10 mmHg diastolic in most hypertensive patients. In the SOLVD treatment trial, lisinopril reduced mortality by 16% in heart failure patients. The GISSI-3 trial showed a 11% reduction in mortality when started within 24 hours of myocardial infarction. Long-term follow-up data indicate sustained efficacy over years of treatment with maintained tolerability profile. Patient satisfaction surveys note appreciation for once-daily dosing and generally manageable side effect profile, though cough remains a notable reason for discontinuation in some cases.