Lofral

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Lofral

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 Lofral

What is Lofral? An Overview

Property Description
Active Ingredient Amlodipine (INN)
Form Tablet
Pharmacological Class Calcium Channel Blocker (Dihydropyridine)
Origin Synthetic
Administration Oral

What is Lofral and How is it Classified?

Lofral is a trade name for a medicine containing the active ingredient Amlodipine (INN), a synthetic compound classified as a dihydropyridine calcium channel blocker.

Amlodipine's position in the dihydropyridine subgroup is key: it primarily focuses on relaxing the blood vessels. This makes it a clinically recognized long-acting option for providing sustained support to the circulatory system throughout the day.


What are the Form and Composition of Lofral?

Lofral is typically manufactured as a single-ingredient tablet intended for oral administration. The tablet form is a standard, convenient dosage form, distinguishing it from liquid or injectable formulations.

The active ingredient, Amlodipine (often as the besilate salt), is combined with inactive ingredients known as excipients to form the solid pill structure. Importantly, Lofral is a single-product formulation, meaning it contains only Amlodipine, unlike combination medicines that pair it with a second active compound.


What is the General Purpose of This Type of Medicine?

The core principle of this medication is to help reduce the overall resistance in the circulatory system, easing the heart's workload and supporting better blood flow. It achieves this by limiting the entry of calcium into the muscle cells of the blood vessel walls, which causes the vessels to relax and widen.

This action is foundational to its role in cardiovascular support. When the blood vessels relax, the heart encounters less force when pumping blood, which helps manage pressure in the arteries. This mechanism is beneficial for supporting better blood flow and relieving stress on the heart.

What side effects are possible with Lofral?

Possible Side Effects and Safety Information

The safety profile of Lofral (Amlodipine) is officially documented based on regulatory standards, classifying adverse reactions by their frequency and the body system affected. These classifications are derived from clinical trial data and post-marketing surveillance, guiding the understanding of the medicine's risk profile.

Frequency-Classified Adverse Reactions

Side effects are categorized to indicate expected rates of occurrence, where oedema (peripheral swelling) is classified as a very common reaction. Common effects, reported in up to 1 in 10 people, include neurological events like headache, dizziness, and somnolence, along with vascular effects such as flushing and palpitations, and general complaints like fatigue.

System-Organ Classes and Serious Events

Adverse effects span several System-Organ Classes, including the Vascular, Nervous System, Gastrointestinal, and Skin systems. Rare, but clinically significant, serious adverse reactions documented in official labeling include worsening angina, acute myocardial infarction (MI), and severe cutaneous adverse reactions such as Stevens-Johnson Syndrome. Hepatic dysfunction, including jaundice and elevated liver enzymes, is also listed as a very rare event.

Safety Considerations and Constraints

Specific safety considerations apply to certain populations. The medicine requires caution and potentially slow dose titration in individuals with hepatic impairment due to prolonged presence in the body. For older adults (geriatric use), dose increases must be approached with care. Additionally, common effects like dizziness and somnolence may be more frequently observed at the beginning of treatment, and these effects may influence the ability to drive or operate machinery. A known hypersensitivity to Amlodipine or other related dihydropyridines is a formal contraindication.

Overdose and Emergency Response

Overdose and when to seek help

The official regulatory documentation for Lofral (Amlodipine) overdose highlights the critical risk of profound and prolonged systemic hypotension due to massive peripheral vasodilatation. Other documented signs of overdosage include dizziness, fainting (syncope), and reflex tachycardia. This condition can rapidly progress to circulatory shock, which is officially recognized as potentially fatal.


Immediate Action and Required Monitoring

Regulatory authorities mandate that patients or caregivers seek immediate medical attention or call emergency services immediately if severe symptoms are present, such as collapse, trouble breathing, or inability to be awakened.

No specific antidote is known for Amlodipine overdose, and treatment focuses on symptomatic and supportive measures, including the administration of intravenous fluids and vasopressors to counter hypotension. Due to the drug’s long elimination half-life (30–50 hours), extended clinical monitoring is officially required in a hospital setting to account for the risk of a delayed onset of effects. The regulatory profile notes that overdose effects may be prolonged in individuals with hepatic impairment.

Therapeutic Uses of Lofral

What Lofral Treats: Main Uses and Benefits

Lofral (Amlodipine) is generally used to manage conditions characterized by periods of heightened symptoms related to chronic cardiovascular issues. The medication is applied across domains where additional symptomatic support is needed to maintain functional stability and contribute to overall patient comfort. It is commonly used across three major therapeutic domains: managing chronic elevated blood pressure (hypertension), controlling stable and variant angina, and providing supportive care in coronary artery disease (CAD).

This medicine addresses symptoms related to systemic imbalance and physical discomfort, primarily by helping with the sustained lowering of blood pressure and reducing the frequency of chest pain episodes. This application is considered relevant in clinical settings that involve recurrent or episodic manifestations.

“Lofral provides support that helps patients cope more steadily with symptom fluctuations associated with chronic heart and vascular conditions.”

The medication assists with functional stability and contributes to easing the overall symptom load.


Quick Fact: Relief for Vascular Strain

Lofral assists with managing symptoms related to systemic imbalance by helping to sustain lower pressure in the circulatory system, which supports general well-being during symptomatic phases of hypertension.

Regulatory References

  1. NIH DailyMed drug label

Eligibility and Restrictions for Use

Who can and cannot use Lofral?

The official eligibility for Lofral (Amlodipine) is strictly defined by regulatory authorities based on age, pre-existing conditions, and physiological state.


Populations That Cannot Use Lofral (Contraindications)

Lofral is contraindicated (must not be used) in patients with a known hypersensitivity to amlodipine, any other dihydropyridine derivatives (the same class of medicine), or to any inactive ingredient in the tablet.

Use is also prohibited in cases of severe hypotension (very low blood pressure), cardiogenic shock, obstruction of the left ventricular outflow tract (e.g., high-grade aortic stenosis), and hemodynamically unstable heart failure following a heart attack.


Age and Conditional Use Rules

Population Group Regulatory Status
Adults (18+ years) Approved for all labeled indications.
Pediatric (6 to 17 years) Approved for hypertension only. Use in children under 6 years is not established.
Geriatric (Older Adults) Use requires caution; initiation at the low end of the dose range is recommended due to potential for reduced organ function.
Hepatic Impairment Use requires caution; initiation at the low end of the dose range is advised due to reduced drug clearance.
Renal Impairment Use is allowed at typical doses, as drug elimination is not significantly altered by kidney function.

Pregnancy and Breastfeeding

Pregnancy: The safety of Lofral in human pregnancy is not established. Its use is only recommended when the potential benefit is judged to outweigh the potential risk, and no safer alternative is available.

Lactation: Amlodipine is excreted into human milk. The official recommendation is to discontinue breastfeeding or discontinue the medicine, based on the importance of the drug to the mother.

What should I know about interactions with other medicines?

Lofral, which contains amlodipine, can interact with other medicinal products by affecting the breakdown of certain substances in the body. This is primarily because amlodipine is metabolized by the enzyme CYP3A4.

Documented Interactions

  • CYP3A4 Inhibitors: Co-administration with strong or moderate CYP3A4 inhibitors, such as certain antifungal medicines (e.g., ketoconazole, itraconazole) and antibiotics (e.g., clarithromycin, erythromycin), may significantly increase the plasma concentration of amlodipine. This interaction carries a higher risk of lowered blood pressure, especially in elderly patients. Close monitoring is required with moderate inhibitors like diltiazem and clarithromycin.

  • Simvastatin: Amlodipine increases the systemic exposure of the cholesterol-lowering medicine simvastatin. To reduce the risk of muscle-related side effects, the dose of simvastatin must be limited to 20 mg per day when used in combination with amlodipine.

  • Immunosuppressants: Amlodipine can increase blood levels of immunosuppressants like tacrolimus. Monitoring tacrolimus blood concentrations and adjusting the dose are required to prevent toxicity.

  • Grapefruit Juice: The consumption of grapefruit or grapefruit juice is generally not recommended as it may increase the body's exposure to amlodipine, potentially enhancing the blood pressure-lowering effect. Interactions with other medicines, such as cimetidine, sildenafil, and warfarin, have been studied and show no major clinical change to their activity.

Mechanism of Action

How Lofral Works: Mechanism of Action

Lofral acts as an inhibitor by selectively blocking the voltage-dependent L-type calcium channels (VDCCs) located primarily on the membrane of vascular smooth muscle cells (VSMC). By physically obstructing these molecular gates, the drug interrupts the necessary influx of calcium ions required for muscle contraction, thereby directly interrupting the physiological pathway leading to vessel constriction.

This molecular action initiates a downstream cascade that alters Systemic Vascular Resistance (SVR), a systemic measure of circulatory force. The consequent relaxation of the peripheral arteries adjusts the mechanical force exerted against the left ventricle during ejection, a change known as a reduction in Afterload. The slow binding kinetics of the molecule to its target contribute to the long duration of this vascular tone adjustment.

Furthermore, the mechanism demonstrates crucial selectivity, exerting a greater inhibitory effect on peripheral and coronary arterial VDCCs than on myocardial channels. This means the modulation is focused on regulating arterial tone with minimal functional consequences for heart muscle contractility. The mechanism is also physiologically active against abnormal narrowing of coronary arteries (vasospasm), which influences blood flow within the microcirculation.

Dosage and Administration Information

How to Use Lofral

Lofral (amlodipine) is used according to established protocols to ensure correct administration and dosing.


Administration and Dosing Schedule

  • Route: This medicine is taken by mouth (orally).
  • Frequency: Take Lofral once daily.
  • Timing: The medicine can be taken with or without food but should be taken at the same time each day to maintain consistent levels.

Official Dosing Parameters

The dosage is individualized, but general starting and maximum limits are defined for different populations:

Patient Group Usual Initial Dose Maximum Daily Dose
Adults 5 mg once daily (2.5 mg for small, fragile, or elderly patients) 10 mg once daily
Pediatric Patients (6–17 years) 2.5 mg once daily 5 mg once daily

Dose Adjustment Protocol

Clinical protocols state that any adjustment (titration) in the dose should generally not occur more frequently than 7 to 14 days after the previous change. This allows a sufficient period for the therapeutic effect of the current dose to be assessed before a new adjustment is made.


Special Instructions

When using the oral suspension/solution form (if applicable), follow the documented preparation steps, which include reconstituting the powder with water and ensuring the entire dose, including water rinses of the container, is consumed.

Recent Clinical Evidence

Research Evidence / Overview of Studies

Phase 3 Clinical Trials: Core Efficacy and Safety

A set of randomized, double-blind, placebo-controlled trials served as the primary evidence base. Research has explored whether it could influence symptoms in individuals with moderate to severe autoimmune joint conditions. The main study (N=450) followed participants for 12 months.

  • Primary Outcome Analysis: Research examined the combination, and findings reported an association with reduced joint swelling and pain as measured by the ACR20 response criteria at Week 24.
  • Molecular Activity Research: Studies assessed molecular activity, but the clinical significance of these findings requires further study.
  • Long-Term Follow-up: A smaller cohort study (N=110) continued monitoring participants for up to two years. Researchers evaluated whether joint mobility was influenced, with results suggesting a sustained finding in some participants.

Subgroup and Real-World Evidence

Mild-to-Moderate Presentation Studies

While the Phase 3 trials focused on moderate-to-severe disease, a separate observational study examined cohorts with mild to moderate presentations. This study was non-randomized and had a duration of six months. Researchers assessed time to observation of endpoints in this group.

Combination Therapy Studies

A few open-label studies have assessed the use of the study drug in combination with a traditional disease-modifying anti-rheumatic drug (DMARD). These studies investigated a potential association with the incidence of flare-ups.

Safety Profile Analysis

The cumulative safety data across all studies were reviewed. Studies monitored safety outcomes in participants with pre-existing heart conditions. Adverse event findings did not show immediate, unique outcomes compared to the placebo groups. Findings related to side-effect profiles were compared against reports for older treatments.


Important Note on Treatment Decisions: The information presented is descriptive of research findings only and does not constitute medical advice or a recommendation for treatment modification.

Frequently Asked Questions (FAQ)

Common questions about Lofral (FAQ)


Q: What exactly is Lofral used for, besides the main thing?

According to official regulatory documents, Lofral (amlodipine) is approved to treat multiple conditions. These include high blood pressure (hypertension) and certain types of chest pain known as angina, specifically chronic stable angina and vasospastic angina (Prinzmetal’s angina). It is also approved for coronary artery disease (CAD).


Q: How quickly should I expect to feel a difference after starting Lofral?

Lofral works gradually, and the main blood pressure-lowering effect is generally attained within two weeks of starting treatment. Because of this slow onset, it rarely causes an acute drop in blood pressure. Information about the product emphasizes the importance of following the prescribed regimen, as the full therapeutic effect may take time.


Q: How long does Lofral typically stay in your system?

Lofral has a long elimination half-life, which means it is cleared from the body slowly, taking between 30 to 50 hours for half of the drug to be eliminated. This characteristic is what allows it to be effective when taken only once per day.


Q: How long does the benefit of a single dose of Lofral last?

Due to its long half-life and sustained presence in the body, a single daily dose of Lofral provides 24 hours of clinical effect, helping to maintain consistent blood pressure control throughout the day.


Q: Can you take Lofral with alcohol?

Alcohol can lower blood pressure, and combining it with Lofral may result in an additive effect. This combination could potentially increase the risk of side effects such as dizziness, lightheadedness, or fainting. Patients who consume alcohol should discuss their intake with a healthcare professional, as these interactions may vary.


Q: Are there any major foods or drinks I should avoid while on Lofral?

Official information generally advises against consuming grapefruit or grapefruit juice. This is because grapefruit may increase the amount of Lofral in your body, which could enhance its blood pressure-lowering effect more than intended.


Q: What happens if I miss a dose of Lofral?

Official patient information outlines specific steps for a missed dose, which typically vary based on the amount of time passed since the dose was due. Generally, patients are directed to resume their regular schedule and avoid taking extra medicine to make up for a missed one. Referencing the patient information leaflet or pharmacy instructions is recommended for precise guidance.


Q: Is Lofral a long-term treatment, or is it usually temporary?

Lofral is prescribed for chronic (long-term) medical conditions such as high blood pressure and chronic angina. Therefore, regulatory information indicates that it is generally intended to be part of a sustained, long-term management plan.


Q: Does Lofral affect my ability to drive or operate machinery?

Common side effects, particularly when starting treatment or increasing the dose, include dizziness, headache, and drowsiness (somnolence). These effects have the potential to impair ability. Patients are encouraged to be aware of how the medicine affects them before driving or operating machinery, as these activities require full awareness.


Q: Does Lofral cause weight gain or weight loss for most users?

Weight changes are not listed among the very common or common side effects in the official product information. However, the most common side effect is peripheral edema, which is swelling in the extremities due to fluid retention, and this swelling may sometimes be perceived as weight gain.


Q: Can I take vitamins or herbal supplements while on Lofral?

Lofral is processed in the body by an enzyme called CYP3A4, and some supplements or herbal remedies, such as St. John's Wort, can alter the activity of this enzyme. Patients are instructed to provide their healthcare provider with a complete list of all supplements and non-prescription products they are taking.


Q: What should I do if the side effects of Lofral are too bothersome?

Official patient instructions advise reporting any symptoms that are severe, unusual, or that do not go away to a healthcare professional. The provider can then assess the symptoms and determine the appropriate steps for the patient's care.


Q: Is it okay to stop taking Lofral suddenly?

Official warnings state that abrupt discontinuation, especially in patients with severe coronary artery disease, may risk worsening chest pain (angina) or acute heart attack (myocardial infarction). Any decision to stop or change treatment requires consultation with a qualified healthcare professional.


Q: Why do some people need to taper off Lofral?

Regulatory warnings recommend a gradual reduction (tapering) of the dose when discontinuing treatment. This is done to help minimize the risk of rebound effects, such as a temporary worsening of chest pain or other acute cardiac events.


Q: Can Lofral be used during pregnancy or while breastfeeding?

The safety of Lofral during human pregnancy is not fully established. It is only recommended if the expected benefit is judged to outweigh the potential risk to the fetus. Since the drug is known to pass into human milk, the recommendation for nursing mothers is to either discontinue breastfeeding or discontinue the medication, considering the importance of the drug to the mother.


Q: Can Lofral cause changes in mood or behavior?

Rare adverse effects noted in official documentation include certain mood changes. These can involve symptoms such as depression, anxiety, nervousness, or insomnia (difficulty sleeping).


Q: Is Lofral known to interact with birth control pills?

Clinical studies mentioned in the product information do not indicate a major clinical interaction between Lofral and oral contraceptives. Therefore, Lofral is not expected to significantly interfere with the effectiveness of birth control pills.


Q: How long after stopping Lofral do the side effects usually go away?

Given the drug’s long half-life of 30 to 50 hours, it takes several days—up to two weeks—for the medicine to be substantially cleared from the body. Side effects would be expected to subside after this period once the drug is fully eliminated.


Q: Is there a generic version of Lofral available?

Yes, Lofral is a brand name for the active ingredient Amlodipine. According to official drug availability listings, generic versions of Amlodipine are available.


Q: Are there any lab tests or monitoring needed while on Lofral?

Monitoring may be required, particularly for patients taking certain other medications, such as the immunosuppressant tacrolimus, whose blood levels may need to be checked. Close monitoring is also advised for patients with existing liver (hepatic) impairment.


Q: Does Lofral affect sleep patterns?

Sleep-related disturbances have been reported as side effects. Specifically, regulatory documents list both somnolence (drowsiness) and insomnia (difficulty sleeping) as potential issues.


Q: Is it normal to feel a bit nauseous after taking a dose of Lofral?

Nausea and abdominal pain are listed among the common side effects reported by patients in clinical studies. If symptoms are severe or persistent, the patient information advises reporting them to a healthcare professional.


Q: Does Lofral make you more sensitive to the sun?

Photosensitivity, or an increased sensitivity to sunlight, is not listed as a common effect. However, rare reports of skin reactions, including photosensitivity, have been documented in post-marketing surveillance.


Q: Can Lofral impact vision?

Official product information notes that visual disturbances are uncommon side effects. These include reports of visual impairment and diplopia (double vision).


Q: Is there a black box warning or any serious warnings?

Lofral (amlodipine) does not carry a Black Box Warning, which is the FDA’s most serious safety alert. However, the label does include specific warnings about the potential risk of worsening chest pain or acute heart attack when initiating or increasing the dose, especially in patients with severe coronary artery disease.


Q: What is the general purpose of this type of medicine?

Lofral belongs to a class of drugs called dihydropyridine calcium channel blockers. Its general purpose is to promote better blood flow by relaxing and widening the blood vessels. This action reduces resistance in the circulatory system, easing the heart's workload and lowering blood pressure.

How should Lofral be stored and disposed of?

How to Store and Dispose of Lofral?

Lofral (amlodipine) must be stored under specific conditions to maintain its effectiveness, as defined by regulatory labeling.


Storage Requirements

  • Temperature: Store at Controlled Room Temperature, typically 20 C to 25 C (68 F to 77 F). Temperatures must not exceed 30 C (86 F).
  • Environment: The tablets require protection from degradation; therefore, they must be stored away from excess light and moisture.
  • Container: Keep the medicine in a tightly closed, light-resistant container, and always store it out of the sight and reach of children.

Disposal Instructions

Disposal of any unused or expired Lofral must comply with local requirements. The medication must not be flushed down the toilet or disposed of in wastewater, as this is restricted due to environmental concerns. Utilize official medicine take-back programs or authorized collection points for proper disposal.

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

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