Амлодипин-Боримед

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Амлодипин-Боримед

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Overview of Амлодипин-Боримед

Property Description
Active Ingredient Amlodipine (as besilate)
Form Tablets (Oral administration)
Pharmacological Class Calcium Channel Blocker (Dihydropyridine)
General Purpose Antihypertensive and Antianginal agent
Origin Synthetic

Definition and Pharmacological Class

Амлодипин-Боримед is a synthetic, single-ingredient pharmaceutical product classified as a long-acting Calcium Channel Blocker (CCB) of the dihydropyridine type. The active substance is Amlodipine (INN). This medicine is characterized by its long-acting profile, which allows for once-daily therapeutic use.

Composition and Pharmaceutical Form

The medication is chemically synthesized and provided for oral administration, most commonly in the solid form of tablets. These tablets contain the active component in salt form, typically Amlodipine besilate. This specific formulation supports the slow and sustained release of the drug. Amlodipine's chemical structure is designed to be selective for the peripheral vascular smooth muscle. This characteristic selectivity is associated with minimized adverse effects related to cardiac conduction, which differentiate it within the broader CCB class.

General Purpose as an Antihypertensive Agent

The fundamental purpose of Амлодипин-Боримед is to reduce elevated arterial pressure, defining it as an antihypertensive agent. The core mechanism involves blocking the entry of calcium ions into the arterial walls, which in turn causes the blood vessels to relax and widen. By performing this function, the medicine facilitates easier blood flow. Amlodipine reduces peripheral resistance by achieving vasodilation. This action eases the physical burden on the heart and is generally utilized to maintain stable, long-term circulatory function.

Regulatory References

  1. World Health Organization's Model List of Essential Medicines
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What side effects are possible with Амлодипин-Боримед?

Official Safety Profile and Adverse Reactions

The safety profile of Amlodipine is defined by official regulatory documentation, which classifies adverse reactions by frequency and the body system affected. These classifications reflect how government authorities organize and communicate the medicine’s risk profile, strictly excluding advice or instructions.

Frequency-Classified Adverse Reactions

The most frequently reported adverse reactions are classified as Common (occurring in 1 to less than 10 out of 100 patients). These effects often include peripheral edema (ankle swelling), headache, fatigue, dizziness, somnolence, palpitations, and flushing. Official documentation notes that peripheral edema is the most frequently reported effect and is often observed as dose-dependent.

Reactions classified as Uncommon (less than 1 in 100 patients) involve systems such as the Gastrointestinal tract (nausea, abdominal pain), the Nervous System (tremor, mood changes), and the Skin (pruritus, rash).

Very Rare reactions (occurring in less than 1 in 10,000 patients) are serious and clinically significant. These include severe skin conditions, such as Exfoliative dermatitis and Stevens-Johnson syndrome, as well as reports of Hepatitis, Jaundice, and specific cardiovascular events like Myocardial Infarction and Arrhythmias.

Safety Considerations and Restrictions

Regulatory labels include specific safety considerations for certain patient groups. Individuals with hepatic (liver) impairment require caution, as reduced clearance may prolong the drug's effects. For older adults, a slower dose titration or lower initial dose may be considered due to altered clearance.

The use of Amlodipine is officially contraindicated in patients with conditions such as severe hypotension, cardiogenic shock, and significant aortic stenosis. Furthermore, official regulatory documents state that worsening angina and acute myocardial infarction may occur upon initiation or dosage increase, particularly in patients with severe obstructive coronary artery disease.

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Overdose and Emergency Response

An overdose of Амлодипин-Боримед is primarily characterized by excessive peripheral vasodilation, resulting in marked and prolonged systemic hypotension. Documented clinical manifestations of severe overdosage include reflex tachycardia and the potential for syncope.

Life-threatening outcomes defined in regulatory documents include refractory hypotension and shock, which may further lead to tissue hypoperfusion or secondary cerebral or myocardial ischemia.


When to Seek Help and Management

Immediate medical attention must be sought for any symptomatic overdose, particularly in cases of clinically significant hypotension.

No specific antidote is known for Amlodipine overdosage; management is entirely reliant on symptomatic and supportive treatment. Regulatory guidance requires active cardiovascular support to manage hypotension, which may include administering a vasoconstrictor (if not contraindicated) and careful attention to circulating fluid volume. Procedural measures like gastric lavage may be considered in certain situations.

Due to the drug's long elimination half-life, extended clinical monitoring is mandated by regulatory documents, with continuous cardiac and respiratory function monitoring being necessary in the emergency setting.

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Therapeutic Uses of Амлодипин-Боримед

The medication is commonly used to provide long-term support for the cardiovascular system, focusing on managing blood pressure and recurrent ischemic discomfort. The medicine is applied across domains where additional symptomatic support is needed, primarily in the management of sustained High Blood Pressure (Hypertension), Chronic Stable Angina, and Vasospastic Angina. It is also considered relevant in clinical scenarios involving angiographically documented Coronary Artery Disease.

Management of Sustained High Blood Pressure (Hypertension)

This domain covers the treatment of conditions marked by increased physiological stress from chronic, elevated arterial pressure in adults and children (aged 6 and older). The medicine is applied in clinical settings where supportive management is needed to help address symptoms related to systemic imbalance. A key patient-oriented benefit is contributing to easing the overall symptom load by supporting the vascular system, which may assist in managing the functional stress related to sustained high pressure.

Prevention of Recurrent Angina Attacks

This therapeutic area addresses symptoms related to physical discomfort that manifest as chest pain or pressure, common in patients with chronic stable angina or vasospastic angina. The medicine is used proactively to help manage these symptomatic patterns. A key benefit is that the treatment may contribute to improved day-to-day comfort, as it assists with easing symptoms that interfere with routine activities.

Stabilization in Coronary Artery Disease (CAD)

The medication is considered relevant in clinical scenarios involving angiographically documented Coronary Artery Disease. It is used to provide supportive therapeutic benefit to patients with conditions characterized by periods of heightened symptoms of chest pain. For this group, the treatment may play a role in managing the overall symptomatic burden in the context of documented heart disease.


Quick Fact: Support for Chronic Vascular Conditions
Амлодипин-Боримед is commonly used in settings where supportive management is needed to help address symptoms related to systemic imbalance and may assist in managing the symptomatic patterns of recurrent chest pain.
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Eligibility and Restrictions for Use

Eligibility: Who Can and Cannot Use Amlodipine

The eligibility for Amlodipine is governed by official regulatory criteria, defining specific populations that are permitted, restricted, or prohibited from using the medicine, based on age, physiological status, and pre-existing conditions.

Absolute Contraindications

Use is strictly prohibited for patients with documented hypersensitivity to Amlodipine or any related dihydropyridine compounds. The medicine is also contraindicated in acute clinical states, including severe hypotension, shock (cardiogenic shock), severe obstruction of the left ventricular outflow tract, and hemodynamically unstable heart failure following a recent heart attack.

Restricted and Special Populations

  • Age: The medicine is approved for use in adults for all labeled indications. In pediatrics, use is established only for children aged 6 years and older, and specifically for the treatment of hypertension. Use in children under 6 is currently not established. Older adults typically require caution and a lower initial dose.
  • Organ Function: Patients with hepatic impairment require cautious dosing and slow titration due to the drug’s decreased clearance. Eligibility is generally not restricted by renal impairment alone.
  • Pregnancy and Lactation: Safety has not been established in human pregnancy, and use is restricted to cases where the benefit outweighs the potential risk. Amlodipine is excreted into human milk, and regulatory guidance often recommends discontinuing nursing during administration.
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What should I know about interactions with other medicines?

Interactions with other medicines and products

Impact of Other Medicines on Amlodipine

Amlodipine is primarily metabolized by the cytochrome P450 enzyme CYP3A4. Concomitant use with strong or moderate CYP3A4 inhibitors can significantly increase amlodipine exposure, potentially raising the risk of hypotension (low blood pressure). Examples include certain azole antifungals (like ketoconazole, itraconazole), macrolide antibiotics (like clarithromycin, erythromycin), and HIV protease inhibitors (ritonavir). Close clinical monitoring and possible dose adjustments are required. Conversely, co-administration with CYP3A4 inducers, such as rifampicin or the herbal product St. John's Wort (Hypericum perforatum), may decrease amlodipine plasma concentrations.

Impact of Amlodipine on Other Medicines

Amlodipine can increase the systemic exposure of other medicines. The dose of the cholesterol-lowering medicine simvastatin must be limited to 20 mg daily when co-administered with amlodipine due to an increased risk of simvastatin side effects. Amlodipine may also raise blood levels of immunosuppressants such as tacrolimus and ciclosporin, necessitating frequent monitoring and dose adjustment of the immunosuppressant. The co-administration of amlodipine and Dantrolene (infusion) should be avoided in patients susceptible to malignant hyperthermia due to the risk of hyperkalemia. Additionally, co-administration with other antihypertensive agents can result in an additive blood pressure-lowering effect.

Food/Substance Interactions

Administration with grapefruit or grapefruit juice is not recommended as it may increase amlodipine's bioavailability, leading to enhanced blood pressure-lowering effects.

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Mechanism of Action

Selective Blockade of L-Type Calcium Channels

The action of Амлодипин-Боримед is centered on the selective modulation of mechanisms for muscle contraction, specifically within the arterial walls. The drug acts as a selective inhibitor that binds to L-type voltage-dependent calcium channels ( L-VDCC) found predominantly on the membranes of arteriolar smooth muscle cells. By physically blocking these channels, Amlodipine impedes the influx of extracellular calcium ions ( Ca^2+), which are essential signals for initiating muscle contraction. The drug’s slow dissociation from the channel results in prolonged channel blockade.


Interruption of Excitation-Contraction Coupling

The molecular blockade triggers a cascade that interrupts the excitation-contraction coupling pathway within the muscle cells. The resulting low concentration of free intracellular calcium prevents the necessary activation of contractile proteins, causing the arterial smooth muscle to relax, a process known as vasodilation. This selective action on arterioles results in minimal interaction with the cardiac conduction system and contractility.


Systemic Reduction of Vascular Resistance

The widespread and sustained vasodilation of the small arteries leads to the physiological consequence of a marked reduction in peripheral vascular resistance ( PVR). This reduction decreases the mechanical resistance the heart encounters while pumping blood, leading to a reduction in cardiac afterload and decreasing the mechanical load on the cardiovascular system.

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Dosage and Administration Information

How to Use Амлодипин-Боримед

Амлодипин-Боримед is administered through the oral route as a tablet and is intended for a once-daily dosing regimen, typically as part of a long-term therapeutic plan. The tablets are available in strengths of 2.5 mg, 5 mg, and 10 mg.


Standard Dosing and Administration

The initial adult starting dose for most indications is 5 mg once daily, with a usual maintenance range spanning 5 mg to 10 mg daily. The maximum recommended dose is 10 mg once daily. The tablet can be taken regardless of meals (with or without food), but consistency is maintained by taking it at the same time each day.

Titration Schedule

Due to the drug's extended half-life, dose adjustments, or titrations, are performed slowly. Subsequent dose increases should generally be separated by a minimum of 7 to 14 days. This timing is intended to ensure that the drug achieves steady-state plasma concentrations before the next dose adjustment is considered.


Population-Specific Dose Rules

Specific starting doses are established for certain groups. A lower initial dose of 2.5 mg once daily is used for elderly patients and individuals with hepatic impairment. For pediatric patients (ages 6–17) with hypertension, the dose range is limited to 2.5 mg to 5 mg once daily. No dosage adjustment is required for patients with renal impairment.

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Recent Clinical Evidence

Research evidence / Overview of Studies for Амлодипин-Боримед

Evidence for Use in Managing Sustained High Blood Pressure (Hypertension)

Research for this use primarily relies on extensive, long-term Randomized Controlled Trials (RCTs) and supporting Meta-analyses. These rigorous study types often compare Amlodipine to an inactive substance or to other established types of blood pressure medications. The main focus of these studies was to measure patterns of change in systolic and diastolic blood pressure (BP) in the observed populations.

Furthermore, many of the largest studies monitored long-term outcomes over several years, tracking the incidence of major cardiovascular events, specifically stroke and myocardial infarction (heart attack). Findings describe patterns where studies tracked measurements of blood pressure change data and the monitoring of major cardiac outcomes. However, when examining long-term outcomes, such as hospitalization for heart failure, the patterns observed in the data have been described as showing variability across different studies.

Evidence for Use in Managing Angina Symptoms

Amlodipine was studied for managing physical discomfort that manifests as chest pain or pressure, which occurs in conditions characterized by fluctuating or episodic manifestations like chronic stable angina and vasospastic (Prinzmetal’s) angina. The research design for this use involves Randomized Controlled Trials (RCTs) that focus on symptomatic relief.

The studies explored outcomes related to physical discomfort. Research examined changes measured during the study period, tracking metrics such as the frequency of angina episodes reported per week and changes in the need for rescue medications. The follow-up duration is a defining characteristic of this research area, with most studies focusing on short-term symptom changes (e.g., 8 to 16 weeks). Information on long-term effects for these specific symptomatic outcomes is limited from dedicated trials.

What is Still Uncertain About Amlodipin-Borimed Research

While many of the core findings are supported by large-scale RCTs, comparative evidence is lacking for some of the secondary outcomes when Amlodipine is measured directly against all available drug classes for hypertension. Also, research suggests that the results apply only to the populations studied. Data for lower-risk, younger adults with hypertension remain less comprehensive, and information for certain narrow populations (like patients with severe heart failure) who were excluded from the main trials remains insufficient.

Key Studies & References

  1. Amlodipine - StatPearls (NCBI Bookshelf)
  2. Tolerability and effectiveness of (S)-amlodipine compared with racemic amlodipine in hypertension: a systematic review and meta-analysis (CRD Commentary)
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Frequently Asked Questions (FAQ)

Common questions about Амлодипин-Боримед (FAQ)

Q: What are the main side effects people most often notice from Amlodipine-Borimed?

According to official product information, the most frequently reported adverse reactions include swelling in the ankles (peripheral edema), headache, fatigue, dizziness, somnolence (drowsiness), palpitations, and flushing (redness of the face). Peripheral edema is often observed and noted as a frequent adverse reaction.

Q: What happens if I miss a dose of Amlodipine-Borimed?

If a dose is missed, the recommended action in product information is generally to take it as soon as it is remembered. However, if it is almost time for your next scheduled dose, the missed dose should be skipped entirely to follow the regular schedule. It is specified that a double dose should not be taken to compensate for the missed dose.

Q: What should I do if blood pressure doesn't decrease with Amlodipine-Borimed?

If the desired blood pressure reduction is not achieved, official dosing guidelines indicate that the medicine is typically started at a lower level and may be slowly adjusted upward to the maximum recommended dose. Due to the medicine's extended half-life, any dose adjustment is generally separated by a minimum of 7 to 14 days to allow the drug's full effect to be established.

Q: Are there any rare but serious side effects of Amlodipine-Borimed?

Official safety documents list reactions classified as very rare (occurring in less than 1 in 10,000 patients) which are considered serious. These include severe skin conditions, such as Stevens-Johnson syndrome and Exfoliative dermatitis, as well as reports of serious liver problems like hepatitis and jaundice.

Q: Can Amlodipine-Borimed affect the ability to drive?

Yes. Official precautions state that this medicine may cause side effects such as dizziness and lightheadedness due to its effect on blood pressure. Caution is therefore advised when performing activities that require concentration, such as driving or operating machinery.

Q: Is Amlodipine-Borimed addictive or does tolerance develop?

Based on clinical and regulatory information, amlodipine is not associated with dependency, addiction, or the type of withdrawal phenomena commonly seen with controlled substances.

Q: Can Amlodipine-Borimed cause drowsiness or fatigue?

Yes, regulatory documents list both somnolence (drowsiness) and fatigue as common adverse reactions that may occur while taking this medicine.

Q: Can Amlodipine-Borimed cause constipation or other digestive problems?

Adverse reactions affecting the gastrointestinal tract commonly include abdominal pain and nausea. While not always listed among the most frequent reactions, constipation has also been reported.

Q: Does Amlodipine-Borimed affect potency in men?

Regulatory documents list impotence or erectile dysfunction as uncommon adverse reactions. This means they are reported in less than 1 out of 100 patients.

Q: Does Amlodipine-Borimed interact with dietary supplements or vitamins?

Specific warnings exist regarding the use of amlodipine with the herbal product St. John's Wort, which may decrease the concentration of amlodipine in the blood. General interactions with common vitamins are not typically highlighted in official product information.

Q: Can the Amlodipine-Borimed tablet be split in half?

This depends on the specific tablet formulation. If the tablet has a score line (a deep indentation), it may be divided. If there is no score line, it should be swallowed whole.

Q: Why do some people feel palpitations after taking Amlodipine-Borimed?

Palpitations (a fast or irregular heart beat) are a common adverse reaction. Since the drug causes blood vessels to relax (vasodilation) to lower blood pressure, this change can sometimes cause a physiological reflex response in the body.

Q: Can Amlodipine-Borimed interact with pain relievers?

Official information indicates that amlodipine may interact with Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), such as ibuprofen. This interaction can potentially reduce the effectiveness of the blood pressure lowering effect or increase the risk of certain side effects.

Q: Is there a difference in effectiveness between different doses of Amlodipine-Borimed?

Effectiveness is dose-related. The dose is typically adjusted by healthcare providers, often starting at a lower strength and potentially increasing up to the maximum recommended dose to achieve the desired blood pressure response.

Q: Why is Amlodipine-Borimed sometimes prescribed in combination with other blood pressure medicines?

Combination therapy is often used when a single medicine is not sufficient to control blood pressure. Prescribing two different classes of agents, such as amlodipine and another anti-hypertensive drug, is intended to achieve enhanced blood pressure lowering efficacy due to their complementary mechanisms of action.

Q: How long should I wait for my condition to improve while taking Amlodipine-Borimed?

The blood pressure lowering effect is achieved gradually. Official pharmacological data indicates that the full therapeutic effect is seen when steady-state plasma concentrations are reached, which occurs after approximately 7 to 8 days of consecutive daily dosing.

Q: What is the reason for dizziness when taking Amlodipine-Borimed?

Dizziness is a common side effect. It is typically a direct consequence of the drug's intended action of lowering blood pressure by causing blood vessels to relax (vasodilation).

Q: Why do some people experience abdominal pain while taking Amlodipine-Borimed?

Abdominal pain is a commonly reported adverse reaction. While the exact physiological reason is not detailed in patient-facing regulatory labels, it is noted as a possible side effect of the oral tablet.

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How should Амлодипин-Боримед be stored and disposed of?

Official Storage Requirements

Official regulatory documents establish mandatory conditions for the storage of Амлодипин-Боримед tablets.

  • Temperature and Light: The medication must be stored at controlled room temperature, generally defined as 15 to 30 C (59 to 86 F). The product must be stored in its original package to ensure protection from light and should not be stored above 30 C.
  • Container and Moisture: The container must be kept tightly closed and stored away from excess heat and moisture.
  • Child Safety: It is strictly required that the medication be kept out of the sight and reach of children, with safety caps always locked, in accordance with official labeling.

Disposal Instructions

Disposal of unused or expired tablets must adhere to the formal instructions provided in the regulatory labeling.

  • Local Compliance: Any unused medicinal product should be disposed of in accordance with local requirements.
  • Environmental Caution: To prevent environmental contamination, the product must not be flushed down the toilet or discarded in household trash, and release to the environment must be avoided.

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

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