Vasotec 10 mg Tablets

Brand Name

This medication is marketed under the trade name Vasotec, widely acknowledged among healthcare practitioners for its effectiveness in managing cardiovascular conditions.

International Nonproprietary Name (INN)

The active ingredient is universally identified as enalapril, ensuring its consistent recognition across global medical standards.

Form of Release

The drug is available as tablets, designed for oral administration, and an injectable solution for intravenous use, offered in various strengths to meet diverse patient needs. These formulations are crafted for ease of administration and maintain stability under typical storage conditions.

Composition

Enalapril maleate serves as the primary active component, engineered to influence blood pressure and cardiac function. In tablets, auxiliary substances such as lactose monohydrate, microcrystalline cellulose, magnesium stearate, and sodium bicarbonate support structural integrity and facilitate disintegration upon ingestion. The injectable solution includes sodium chloride and benzyl alcohol to ensure compatibility with intravenous delivery. Some tablet formulations may feature colorants like iron oxides for visual distinction. Each element is carefully selected to enhance the therapeutic action of enalapril while preserving its reliability.

Pharmacologic Properties

Pharmacodynamics

This medication operates as an angiotensin-converting enzyme (ACE) inhibitor, targeting the renin-angiotensin-aldosterone system to exert its effects. By blocking the conversion of angiotensin I to angiotensin II, it prevents vasoconstriction and aldosterone secretion, leading to relaxation of blood vessels and reduced blood volume. This action lowers peripheral resistance and blood pressure while decreasing cardiac preload and afterload. It also reduces bradykinin breakdown, contributing to vasodilation and potential protective effects on vascular endothelium. Effects typically begin within one hour of oral administration or minutes of intravenous use, peaking at four to six hours, with sustained benefits over 24 hours. This mechanism supports its role in cardiovascular regulation and organ protection.

Pharmacokinetics

Following oral intake, the drug absorbs rapidly from the gastrointestinal tract, with bioavailability around 60% as it is a prodrug converted to enalaprilat in the liver. Food does not affect absorption significantly. Peak plasma concentrations of the active metabolite occur within three to four hours orally or immediately via intravenous route. Enalaprilat binds minimally to plasma proteins, about 50%, and distributes widely, reaching tissues like the kidneys and heart. It undergoes negligible further metabolism, with elimination primarily through urine, where 60% to 80% is excreted as enalaprilat and the rest as unchanged enalapril. The half-life ranges from 11 to 35 hours, prolonged in renal impairment due to reduced clearance, requiring careful monitoring.

Indications for Use

This medication is recommended for conditions involving elevated blood pressure or cardiac strain. It is primarily indicated for hypertension, effectively reducing pressure to mitigate cardiovascular risk, suitable across a range of severities. It also manages heart failure by decreasing cardiac workload and improving survival, particularly in symptomatic patients with reduced ejection fraction. In asymptomatic left ventricular dysfunction, it delays progression to overt heart failure, offering preventive benefits. Its versatility supports use in both acute and chronic settings, often integrated into broader therapeutic plans to enhance heart and vascular health.

Contraindications

Specific conditions restrict the use of this drug to ensure patient safety. Hypersensitivity to enalapril, other ACE inhibitors, or formulation components prohibits its use, as reactions could range from rashes to anaphylaxis. A history of angioedema, whether spontaneous or linked to prior ACE inhibitor use, excludes it due to recurrence risks. Severe renal artery stenosis, bilateral or unilateral in a single kidney, contraindicates it, as reduced renal perfusion could worsen kidney function. It is avoided in pregnancy beyond the first trimester due to potential fetal harm, including renal damage. Significant hyperkalemia or uncorrected electrolyte imbalances also preclude its use to prevent further disruption.

Method of Administration and Dosage

How to Take

Tablets are taken orally, with or without food, offering flexibility in timing, though a consistent schedule supports stable blood levels. Swallowing them whole with water ensures proper delivery to the digestive system. The injectable form is administered intravenously by healthcare professionals, typically in acute settings.

Dosage for Adults and Children

For adults with hypertension, treatment typically starts at 5 mg once daily, adjustable to 10 mg to 40 mg daily in one or two doses based on response. In heart failure, 2.5 mg twice daily is common, increasing to 20 mg twice daily as tolerated, guided by clinical stability. Pediatric dosing for hypertension begins at 0.08 mg per kilogram once daily, up to 5 mg, with a maximum of 0.58 mg per kilogram or 40 mg, tailored under specialist supervision. Intravenous use in emergencies starts at 1.25 mg every six hours, adjusted as needed. Regular monitoring ensures dosing aligns with efficacy and safety across age groups.

Dose Adjustment in Specific Conditions

Renal impairment requires lower doses; if creatinine clearance is 30 to 80 mL/min, start at 5 mg daily, reducing to 2.5 mg if below 30 mL/min, with careful potassium monitoring. Hepatic dysfunction typically needs no adjustment, as metabolism is minimal post-conversion, though severe cases warrant caution. Older adults or those with reduced renal reserve may initiate at 2.5 mg daily to minimize hypotension risks. Frequent assessments tailor dosing to each patient’s physiological state, especially in compromised conditions.

Side Effects

This medication may provoke a variety of unintended responses, though most are manageable. Persistent dry cough, linked to bradykinin accumulation, is common, often resolving upon discontinuation. Dizziness or lightheadedness might occur, typically tied to blood pressure drops, especially early in use. Fatigue, headache, or nausea can affect some individuals, usually diminishing over time. Hyperkalemia or elevated potassium levels may arise, causing muscle weakness or irregular heartbeats in at-risk patients. Rarely, severe reactions like angioedema—swelling of the face or throat—or significant renal impairment emerge, requiring immediate medical attention. Patient reports and periodic lab checks help address these effects effectively.

Overdose

Symptoms of Overdose

Excessive intake can lead to profound hypotension, resulting in dizziness, fainting, or circulatory collapse due to excessive vasodilation. Bradycardia or slowed heart rate might develop, though tachycardia could occur as compensation. Electrolyte imbalances, particularly hyperkalemia, may cause muscle cramps or arrhythmias, posing risks if uncorrected. Symptoms typically appear within hours and escalate without intervention, reflecting the drug’s strong systemic influence.

First Aid Measures

In an overdose scenario, discontinue administration immediately and seek urgent medical assistance. If ingestion is recent, activated charcoal may curb absorption, applied under professional supervision. Intravenous fluids or vasopressors like norepinephrine address hypotension, while monitoring corrects potassium levels and stabilizes heart rhythm. Supportive care, including positioning the patient flat, assists until medical support arrives. Focus is on restoring circulatory balance rapidly.

Drug Interactions

Effects on Other Medications

This drug can alter the effects of other medications when used concurrently. It may amplify the pressure-lowering action of other antihypertensives, requiring dose tweaks to avoid excessive drops. Potassium-sparing diuretics or supplements increase hyperkalemia risks, needing electrolyte oversight. Nonsteroidal anti-inflammatory drugs might reduce its efficacy and strain kidneys, particularly with prolonged use. Lithium levels could rise due to decreased clearance, necessitating plasma checks. Adjustments minimize these interaction risks effectively.

Compatibility with Alcohol and Food

Alcohol consumption may intensify hypotension, increasing dizziness risks, so moderation is advised. Food does not significantly affect absorption, allowing flexible timing, with no specific dietary restrictions beyond avoiding excessive potassium intake to prevent imbalance. A balanced diet supports overall efficacy.

Special Precautions

Use During Pregnancy and Breastfeeding

This medication is contraindicated in pregnancy beyond the first trimester, as it may cause fetal renal damage or death, based on extensive evidence. It passes into breast milk in small amounts, potentially affecting infant kidney function, so nursing mothers should consult their physician, possibly opting for alternatives to minimize exposure.

Impact on Driving and Machinery Operation

Dizziness or fatigue, especially at initiation or dose changes, may impair driving or machinery operation. Patients should evaluate their tolerance before such activities, ensuring safety for themselves and others.

Considerations for Elderly and Pediatric Populations

Older adults may require lower initial doses due to reduced renal clearance, with monitoring for hypotension or electrolyte shifts. In children, its use is tailored for hypertension, with weight-based doses adjusted cautiously under specialist guidance to avoid developmental impact. Personalized care optimizes safety and efficacy across these groups.