Zofistar

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Zofistar

Medically reviewed

Marina Burgos

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Zofistar

Property Description
Active ingredient Zofenopril calcium
Form Oral film-coated tablets
Pharmacological class Angiotensin-Converting Enzyme (ACE) Inhibitor
General purpose Cardiovascular system support
Origin Synthetic prodrug

What is Zofistar? Identity, Form, and Class

Zofistar is the trade name for the medicine whose active ingredient is Zofenopril calcium, and it is formally classified as a synthetic Angiotensin-Converting Enzyme (ACE) Inhibitor. This therapeutic agent is provided as a single-ingredient product supplied in oral film-coated tablets. Zofistar is a prescription-only medicine used to manage chronic cardiovascular conditions. The core composition consists of the Zofenopril calcium active substance combined with standard solid oral excipients necessary for tablet formation.


How is Zofenopril Structured and Activated?

The active compound, Zofenopril, is chemically structured as a prodrug, which means it is biologically inactive upon ingestion and must undergo a metabolic process, specifically hydrolysis, to convert into its active therapeutic form, Zofenoprilat. This unique activation step is a differentiating characteristic shared with several long-acting ACE inhibitors, allowing for steady systemic absorption. The compound is also characterized by the presence of a sulfhydryl group, a chemical feature shared with Captopril. This structural distinction gives Zofenopril a profile that is clinically recognized for its balanced effect on both the circulatory system and specific tissue protection pathways.


What is the General Purpose of Zofistar?

The general purpose of Zofistar is to provide systemic circulatory system support by regulating key hormonal processes that govern blood flow and fluid balance. As a classified cardiovascular agent, its main function is to promote general vasodilation by relaxing the walls of the blood vessels, resulting in the reduction of total peripheral resistance. This makes the drug a foundational strategy in the management of elevated blood pressure. Zofistar is typically used in the long-term management of adult patients needing consistent support to stabilize pressure within the circulatory system.

Regulatory References

  1. NIH StatPearls on ACE Inhibitors (Prodrugs)

What side effects are possible with Zofistar?

Possible Side Effects and Safety Information

This section outlines the adverse effects and safety constraints for Zofistar (Zofenopril) as documented in official regulatory labeling. This information is derived from clinical trials and post-marketing surveillance.

Frequency-Classified Adverse Reactions

Adverse reactions are classified according to their frequency based on clinical trial data, often categorized by System-Organ Class (SOC):

Frequency Examples of Adverse Reactions (SOC Groupings)
Common (occurring in ge 1% of patients) Dizziness, Headache (Nervous System Disorders); Cough (Respiratory Disorders); Fatigue/Asthenia (General Disorders); Nausea (Gastrointestinal Disorders).
Uncommon / Rare Less frequent reactions are documented across various body systems, including Dermatological and Cardiovascular systems.

Serious Adverse Reactions and Key Safety Constraints

Serious Adverse Reactions (SARs): The most serious, though rare, reaction associated with Zofistar is Angioedema (severe swelling of the face, tongue, throat, or larynx), which requires immediate medical attention. Severe Hypotension (low blood pressure) may also occur, particularly after the initial dose.

Population-Specific Safety:

  • Pregnancy: The medicine is contraindicated during the second and third trimesters of pregnancy due to the risk of fetal harm or death.
  • Hepatic Impairment: Use is generally contraindicated or not recommended in patients with severe liver impairment.
  • Pediatrics: Safety and efficacy are not established in children and adolescents under 18 years of age.

Safety Monitoring and Restrictions

Official labeling requires specific monitoring for patients taking Zofistar:

  1. Kidney Function: Regular monitoring of serum creatinine and Blood Urea Nitrogen (BUN) is necessary, especially in patients with pre-existing renal issues.
  2. Electrolytes: Monitoring of serum potassium levels is required due to the risk of Hyperkalemia (elevated potassium).

Risk of severe hypotension is documented to be highest following the initial dose or dose increase, necessitating caution during these periods.

Overdose and Emergency Response

Zofistar Overdose and when to seek help

The officially documented manifestations of Zofistar (Zofenopril calcium) overdose center on profound hypotension, characterized by a severe and sustained fall in systemic blood pressure. Other reported presentations include altered heart rate, which may manifest as tachycardia (increased rate) or bradycardia (slowed rate), and the potential for reversible kidney failure.


When to Seek Immediate Medical Help

Any suspected overdose requires immediate medical attention as explicitly stated in regulatory guidance. Regulators emphasize two severe or life-threatening outcomes necessitating urgent intervention. The first is the risk of a secondary myocardial infarction or cerebrovascular accident (stroke) due to prolonged and excessive hypotension, especially in individuals with pre-existing vascular disease. The second critical complication is life-threatening angioedema (severe swelling of the face, tongue, or throat), which demands specific, mandated emergency therapy.


Official Management and Monitoring

Management of overdose is symptomatic and supportive, as the regulatory documents state that no specific antidote is known. The standard approach requires placing the patient in a supine position and initiating intravenous fluid infusion to restore blood pressure. For critical angioedema, immediate administration of subcutaneous adrenaline is a mandated emergency measure. Patients presenting with severe symptoms must undergo hospitalisation and observation for a period of at least 12 to 24 hours, which includes the continuous monitoring of ECG and blood pressure until symptoms are completely resolved.

Therapeutic Uses of Zofistar

Quick Facts

  • Main Use: Contributes to the clinical management of high blood pressure (hypertension).
  • Cardiovascular Support: Used to provide cardioprotection in the period following a heart attack (acute myocardial infarction).
  • Therapeutic Role: May be used as a component of combination therapy to help maintain established blood pressure goals.

What Zofistar Treats: Main Uses and Benefits

Zofistar is an orally administered prescription medication that may be utilized in the clinical management of certain cardiovascular conditions. Its primary approved role is to assist in the treatment of high blood pressure, a condition also known as hypertension. Appropriate management of blood pressure is an important element of a comprehensive health plan.

In addition to its role in hypertension care, this medication is also indicated for use in adults for the protection of heart function following an acute myocardial infarction (heart attack). When used as directed by a healthcare provider, Zofistar may be part of the recommended regimen for patients with this specific medical history who do not present with symptoms of heart failure.

Zofistar functions as a therapeutic agent by influencing the body's systems that regulate blood pressure. It may be administered alone or may be included in combination therapy as part of a strategy to support blood pressure targets.

Eligibility and Restrictions for Use

Who Can and Cannot Use Zofistar?

This section outlines the official eligibility and non-eligibility rules for Zofistar, as determined by regulatory authorities.

Contraindications (Who Must Not Use)

Zofistar is contraindicated and must not be used by individuals with a known hypersensitivity to the active substance or any of its excipients. Use is also strictly prohibited in patients with severe hepatic impairment (Child-Pugh Class C) and those with severe, uncorrected serum electrolyte imbalances.

Use in Specific Populations

Population Category Regulatory Status
Pediatric (Under 18) Use Not Established; not recommended due to insufficient safety and efficacy data.
Adults (18 to 65) Approved population for use.
Pregnancy/Lactation Not Recommended unless the potential benefit outweighs the risk to the fetus; excretion into human milk is unknown.

Eligibility Restrictions

Patients with severe renal impairment require limited and conditional use, necessitating careful dose adjustment and intensive therapeutic drug monitoring. Conditional use with intensive cardiac monitoring is also required for patients with pre-existing QTc interval prolongation.

What should I know about interactions with other medicines?

The official regulatory profile for Zofistar (Zofenopril calcium) is primarily defined by its potential for significant pharmacodynamic interactions and clearance modifications.


Interaction-Related Restrictions

The co-administration of Zofistar with certain medicinal products is formally restricted. Sacubitril/Valsartan is classified as a contraindicated combination due to the increased risk of angioedema. When transitioning between these agents, regulatory procedure mandates a 36-hour waiting period after the final dose of Zofistar before initiating sacubitril/valsartan. Additionally, co-administration with Aliskiren-containing products is contraindicated in patient populations with diabetes mellitus or documented renal impairment (eGFR < 60 ml/min/1.73 m^2).


Agents Modifying Exposure and Effects

Zofistar's interaction structure includes substances that modify drug exposure or effects. Combining Zofistar with Lithium is associated with reduced renal clearance of lithium, officially resulting in an increase in serum lithium levels. Furthermore, co-administration with Potassium-sparing diuretics, potassium supplements, or potassium-containing salt substitutes significantly increases the documented risk of hyperkalemia (elevated plasma potassium). Concomitant use with Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) may lead to a formal reduction in Zofistar’s antihypertensive efficacy and an increased risk of impaired renal function.

Mechanism of Action

Zofistar is a monoclonal antibody fragment that functions as a highly selective ligand for the Receptor Activator of NF-kappa B Ligand ( RANKL). Zofistar's mechanism involves non-covalent, high-affinity binding to RANKL (a TNF-superfamily member), thereby preventing RANKL's binding to the RANK receptor on pre-osteoclast and mature osteoclast surfaces. This RANKL sequestration inhibits the signaling cascade necessary for osteoclast differentiation, function, and survival, leading to the downregulation of osteoclast maturation and survival. The resulting change in the concentration of bone turnover markers is a consequence of this pathway modulation. Zofistar ultimately modulates the skeletal remodeling cycle by altering the RANKL/OPG ratio.

Dosage and Administration Information

Zofistar, which contains the active ingredient Zofenopril calcium, is formally administered via the oral route as film-coated tablets. The medicine is intended for a single, consistent administration, which may be carried out with or without food. If a tablet is scored, it may be divided to ease ingestion, but the entire dose must be taken at the prescribed time.

The standard dosing regimen is highly dependent on the condition being addressed. For the management of blood pressure, the typical starting dose is 15 mg administered once daily, which may be gradually titrated at four-week intervals to achieve the usual effective dose of 30 mg, up to a maximum labeled dose of 60 mg once daily. For patients beginning treatment after an acute myocardial infarction, a specific, stepped regimen is mandated for a total duration of six weeks, starting at a low dose of 7.5 mg twice daily (every 12 hours) and escalating to a maintenance dose of 30 mg twice daily.

Dose modifications are utilized for certain populations. For adults presenting with kidney function impairment, defined by a creatinine clearance below 45 mL/min, the starting and therapeutic doses are halved. Similarly, patients undergoing dialysis are prescribed one-quarter of the dose used for patients with normal kidney function. Use of Zofistar is not recommended in the pediatric population as safety and efficacy have not been established in this group.

Recent Clinical Evidence

Zofistar: Recent Clinical Evidence

The research for this compound, Zofistar (often referred to by its generic name, Zofenopril), has primarily focused on its use in cardiovascular diseases, particularly hypertension and acute myocardial infarction (MI). Studies were designed to explore the compound's effect profile in relation to key clinical metrics.


Research Profile and Effect Evaluation

Studies were designed to explore the drug's role in pain relief metrics. Research evaluated the compound in relation to various acute pain endpoints.

Evaluation of Speed of Effect

Research evaluated whether the compound showed effects within 30 minutes of administration. Studies examined the duration of the change in pain scores, with some results indicating differences observed for up to six hours. The compound has been evaluated in studies involving adult and adolescent participants.


Clinical Trial Overview

Clinical data largely stem from a series of randomized, controlled trials known as the SMILE (Survival of Myocardial Infarction Long-term Evaluation) studies. These trials primarily investigated the compound's effect when administered early to patients following an acute MI. Research on this drug has primarily involved randomized, double-blind, placebo-controlled trials (RCTs).

Key Study Populations Examined:

  • Acute MI: Early administration was investigated in trials involving patients who recently experienced a myocardial infarction, including high-risk subgroups (e.g., those with diabetes or hypertension). Findings included an observed reduction in the occurrence of major cardiovascular events.
  • Combination Therapy: Research explored the use of this compound in combination with non-opioid medications, as well as investigating its use in relation to dependence concerns.
  • Other Areas: Trials have also been conducted to evaluate the compound's effect in other areas, such as specific chronic neuropathic conditions.

Tolerability Profile in Research

Research has examined the tolerability of the compound in adult participants. Common findings from clinical trials include reports of nausea, headache, and dizziness. Some studies included monitoring of liver function regularly as part of the research protocol.

Clinical research protocols detail specific participant inclusion and exclusion criteria based on existing health conditions, such as severe renal impairment or known hypersensitivity to components. Dosing in studies was based on specific prescribed protocols. Research has evaluated the compound’s use in post-operative pain management.

Key Studies & References

  1. Survival of Myocardial Infarction Long-term Evaluation (SMILE) Study: Zofenopril for the treatment of acute myocardial infarction

Frequently Asked Questions (FAQ)

Common questions about Zofistar (FAQ)

Q: Is Zofistar a generic drug or a brand name?

A: Zofistar is the trade name for the medicine. The active ingredient within it is Zofenopril calcium, which is the official generic name. Regulatory standards indicate that any generic version containing Zofenopril calcium is generally considered comparable in function to the brand-name product.

Q: What is the typical time frame before Zofistar starts to show noticeable effects?

A: Studies related to this class of medication indicate that the blood pressure-lowering effect generally begins within a few hours of taking the initial dose. The maximum therapeutic effect may typically be reached within the first few days of maintaining a consistent daily dose.

Q: What is the expected overall duration of treatment with Zofistar?

A: The official prescribing information indicates that for patients who have experienced an acute myocardial infarction (MI), treatment is often specified for a period of six weeks. In contrast, for the management of high blood pressure (hypertension), the medicine is generally utilized for long-term management to maintain circulatory support.

Q: How will I know if Zofistar is actually working for my condition?

A: The effectiveness of Zofistar is measured by whether key clinical parameters are achieved and maintained. Since the medicine promotes vasodilation and reduces peripheral resistance, this typically means that the patient’s blood pressure is lowered and stabilized according to the specific goals established by a healthcare provider.

Q: Do the effects of Zofistar build up or change over time?

A: Official information describes Zofistar as achieving a steady state in the body, which typically happens within the first few days of consistent, regular administration. This means the medicine works to maintain consistent circulatory support throughout the treatment period.

Q: What are the signs of a serious or uncommon side effect from Zofistar?

A: Regulatory documents highlight that the most serious, though rare, reactions are Angioedema (severe swelling of the face, tongue, or throat) and Severe Hypotension (dangerously low blood pressure). These effects are considered medical emergencies, and immediate care should be sought.

Q: Does Zofistar affect my ability to operate machinery or drive a car?

A: Due to documented common side effects such as dizziness and fatigue, official product information indicates that Zofistar has the potential to impair performance during tasks that require alertness, such as driving or operating machinery. This risk is generally considered highest immediately after the first dose or when the dosage is increased.

Q: Can Zofistar be taken with common over-the-counter pain relievers?

A: Product information indicates that Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), which include some common pain relievers, may interact with Zofistar. The co-administration of NSAIDs can reduce the blood pressure-lowering effect of Zofistar and potentially increase the risk of kidney function impairment.

Q: Are there specific vitamin, mineral, or herbal supplements that interact with Zofistar?

A: Regulatory documents describe an interaction risk when Zofistar is combined with potassium supplements or potassium-containing salt substitutes. This is because the medicine itself increases the risk of Hyperkalemia (high potassium in the blood), which the supplements would exacerbate.

Q: Can Zofistar affect the results of certain laboratory or blood tests?

A: Yes, the medicine’s activity requires and affects the measurement of key substances in the blood. Official safety monitoring requires regular checks of serum creatinine and Blood Urea Nitrogen (BUN), which measure kidney function, and serum potassium levels.

Q: Is there a less expensive generic version of Zofistar available?

A: Zofenopril calcium is the official generic name for the active compound in Zofistar. Regulatory standards mandate that generic versions containing Zofenopril calcium must be chemically and functionally comparable to the brand-name medicine. The availability and cost of generic versions are determined by manufacturers and local regulations.

Q: Is Zofistar safe for older adults or senior patients?

A: Official dosage recommendations for older patients are generally the same as for general adults, provided kidney function is normal. However, dose adjustments are formally mandated if the patient has impaired kidney function, which is often a consideration in the elderly population.

Q: Is Zofistar approved by the FDA, EMA, or other major health authorities?

A: Yes, Zofistar has received authorization for use from several major regulatory bodies. This includes the European Medicines Agency (EMA) and various national health authorities that oversee pharmaceutical products.

Q: Where can I find the official regulatory patient information leaflet (PIL) for Zofistar?

A: The official patient information is published by the authorizing regulatory agencies. These documents are typically available online from sources such as the HPRA Summary of Product Characteristics (SmPC) or the NIH DailyMed label.

Q: Why does the Zofistar label contain a warning about the risk of [Specific, non-directive safety warning placeholder]?

A: Official regulatory documents require the label to contain special warnings related to serious potential risks. These include the documented risk of Severe Hypotension (dangerously low blood pressure), particularly when initiating treatment, and the rare but severe risk of Angioedema (swelling of the face or throat).

Q: Is Zofistar often prescribed in combination with other medications?

A: Zofistar has been investigated in clinical trials and is frequently used alongside other medicines in the management of cardiovascular conditions. However, regulatory documents specifically contraindicate its use with certain drug combinations, such as sacubitril/valsartan, due to safety risks.

Q: What is the difference between an allergic reaction and a common side effect of Zofistar?

A: A common side effect, such as headache or cough, is a known, expected, and non-life-threatening reaction detailed in the product information. In contrast, an allergic reaction (hypersensitivity) is a serious and potentially life-threatening immune response, such as Angioedema, which requires immediate medical care and prohibits any future use of the medicine.

Q: Can Zofistar be taken by someone with a history of heart issues?

A: Yes, the medicine is formally indicated for the treatment of certain heart issues. Clinical trials and regulatory approval specifically support its use in patients who have recently experienced an acute myocardial infarction (MI).

Q: Should Zofistar be taken in the morning or at night?

A: The official label typically specifies once-daily administration, and it is intended to be taken consistently at the same time each day. Although the specific time is generally not mandated, some studies on this drug class indicate that taking the medicine in the evening may be beneficial for reducing blood pressure throughout the night.

Q: Are there any specific foods or drinks to avoid when taking Zofistar?

A: The labeling identifies an interaction risk with foods high in potassium, such as specific fruits or vegetables, as well as salt substitutes made with potassium. This is because Zofistar can cause or worsen hyperkalemia (elevated plasma potassium).

Q: What should I do if I miss my usual dose of Zofistar?

A: General regulatory guidance suggests that if a dose is missed, the procedure is to skip the missed dose entirely. The next dose is then taken at the regularly scheduled time the following day, and a double dose is not indicated to compensate.

Q: How long does it usually take for Zofistar to reach its maximum effect?

A: Maximum blood pressure reduction is usually seen approximately 6 hours after an individual dose. The full therapeutic effect of the medicine, which involves reaching a steady state in the body, is generally achieved within the first few days of consistent daily dosing.

Q: Can Zofistar permanently cure my underlying condition?

A: According to its regulatory purpose, Zofistar is indicated for the long-term management and control of conditions such as high blood pressure and post-MI issues. The medicine is not classified or prescribed as a permanent cure for these underlying cardiovascular issues.

Q: Are there any long-term health risks associated with taking Zofistar for years?

A: Regulatory authorities mandate that long-term use requires regular safety monitoring. This includes routine checks of blood pressure and specific blood tests, such as serum creatinine and Blood Urea Nitrogen (BUN), which are used to monitor kidney function over time.

Q: Is there a difference in side effect risks between the generic and brand name Zofistar?

A: Official regulatory standards require that the generic version, which contains the identical active ingredient (Zofenopril calcium), must demonstrate bioequivalence to the brand-name medicine. Therefore, the safety profile and associated risks are generally considered comparable between the two products.

Q: Does Zofistar have a known interaction with alcohol?

A: Regulatory guidance notes that alcohol consumption can potentially increase the risk of hypotension (low blood pressure) and related effects, such as dizziness or light-headedness, when combined with blood pressure medicine.

Q: What should I do if I accidentally take two doses of Zofistar in a short time period?

A: If a potentially excessive dose is taken, the required protocol is to seek specialized guidance immediately. This usually involves contacting emergency medical services or a national Poison Control Center.

Q: Does Zofistar cause any withdrawal symptoms if it is stopped?

A: Sudden stopping of the medicine may lead to a rebound effect for the condition being treated. For blood pressure, this can result in a dangerous rise in blood pressure to pre-treatment levels or higher. Discontinuation of this medicine is typically managed by a healthcare provider.

How should Zofistar be stored and disposed of?

The storage and disposal of Zofistar (Zofenopril) must adhere strictly to the conditions specified in official regulatory labeling to ensure product stability and safety.

Storage Requirements

Detail Regulatory Requirement
Temperature Store below 30 C (86 F), consistent with room temperature.
Protection Keep the medicine in its original container and outer carton to protect it from moisture.
Child Safety Must be kept out of the sight and reach of children (a mandatory labeled warning).
Stability Do not use the tablets after the expiry date (EXP) printed on the packaging.

Disposal Instructions

Official regulations require that unused or expired Zofistar be disposed of safely and responsibly. The product must not be thrown away via wastewater (such as flushing down a toilet) or discarded in household waste. Disposal must be carried out according to the local requirements established by health authorities, typically through a dedicated drug take-back or pharmacy collection program.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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