Прегабалин

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Medically reviewed

Laura Arias

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 Прегабалин

Что такое Прегабалин и к какому классу относится?

Свойство (Property) Описание (Description)
Активный ингредиент (Active ingredient) Прегабалин (Pregabalin)
Форма (Form) Капсулы, оральный раствор, таблетки с пролонгированным высвобождением
Фармакологический класс (Pharmacological class) Габапентиноид, Противосудорожное средство
Общее назначение (General purpose) Стабилизация возбудимости нервной системы, облегчение нейропатической боли
Происхождение (Origin) Синтетическое соединение

Pregabalin is a synthetic pharmaceutical agent that serves as an orally active compound used to stabilize nerve activity within the central nervous system (CNS). It belongs to the gabapentinoid class of medications, which are structural analogues of gamma-aminobutyric acid (GABA), and is categorized as an anticonvulsant. The active constituent is the single-ingredient compound Pregabalin ((S)-3-(Aminomethyl)-5-methylhexanoic acid). Pharmacological properties relate to its capacity for modulating neurological hyper-excitability.

Its mechanism involves high-affinity binding to the alpha2delta auxiliary subunit of presynaptic voltage-gated calcium channels found on neurons, an action that distinguishes it from agents that directly target GABA receptors. This specific binding reduces the release of excitatory neurotransmitters from overactive neurons. This mechanism characterizes its role as a central nervous system modulator.


Форма выпуска и общая терапевтическая цель Прегабалина

Pregabalin is administered orally and is available as standard immediate-release capsules, a liquid oral solution, and specialized extended-release tablets. The primary general purpose of this medication is the targeted dampening of excessive neural signaling. This helps control abnormal electrical activity, providing general relief in situations where the nervous system is chronically overstimulated, such as in cases of persistent nerve discomfort.

The compound is therapeutically employed for its capacity to exert an antiseizure effect, an antinociceptive effect (nerve pain relief), and an anxiolytic effect. The medication is used for indications involving chronic nerve pain and generalized anxiety disorder. The availability of the extended-release tablet form represents a differentiating feature, designed to sustain the therapeutic effect over a longer duration compared to the immediate-release capsules.

Regulatory References

  1. NIH MedlinePlus Drug Information for Pregabalin
  2. EMA EPAR for Lyrica (Pregabalin)

What side effects are possible with Прегабалин?

Possible Side Effects and Safety Information

The safety profile of Pregabalin is officially classified according to the frequency and type of documented adverse reactions, which is consistent across major government regulatory documents.

Frequency-Classified Adverse Reactions

The most commonly reported effects, classified as Very Common, are Dizziness and Somnolence (Drowsiness). These effects are officially noted to occur more frequently at the start of treatment and during dose escalation. Other reactions classified as Common include weight gain, blurred vision, dry mouth, constipation, and a loss of muscle coordination known as ataxia.

System-Organ Classes and Serious Reactions

Adverse reactions are formally grouped by the affected system, primarily involving Nervous system disorders, Psychiatric disorders, and Gastrointestinal disorders.

The official prescribing information highlights the potential for rare but serious adverse reactions, including Angioedema (swelling of the face, tongue, or throat) and other serious hypersensitivity reactions. A class-wide warning for anticonvulsants, including Pregabalin, exists regarding the documented risk of suicidal ideation and behaviour.

Population and Duration Safety Constraints

Official regulatory texts mandate that clearance of the medicine is dependent on kidney function, requiring specific considerations for individuals with renal impairment. Furthermore, the regulatory safety profile recognizes the potential for misuse and dependence. Consequently, the risk of withdrawal symptoms is officially documented following the rapid or abrupt cessation of long-term treatment.

Overdose and Emergency Response

Overdose and When to Seek Help

Official regulatory documentation describes Pregabalin overdose primarily through its effects on the central nervous system (CNS) and potential severe complications. Manifestations are often characterized by CNS depression, including somnolence, dizziness, confusional states, and impaired coordination (ataxia). In severe cases, official reports include loss of consciousness and coma.

Critical Risks and When to Seek Help The most critical risk associated with overdose is severe respiratory depression, which can escalate to respiratory failure, particularly when Pregabalin is consumed with other CNS depressants, such as opioids. This severity triggers the mandated requirement to seek immediate medical attention.

Immediate Emergency Action is Required If:

  • Breathing is slow, shallow, or difficult.
  • The individual is severely confused, disoriented, or extremely lethargic.
  • The person is unresponsive or cannot be awakened.

Regulatory Management Notes

  • No specific antidote for Pregabalin overdose is documented in official labeling. Treatment involves general symptomatic and supportive care, with monitoring of vital signs.
  • The drug is effectively removed from the bloodstream by haemodialysis, a measure often considered due to its primary renal excretion.
  • Elderly patients and individuals with pre-existing renal impairment are identified as being at higher risk for severe overdose manifestations.

Therapeutic Uses of Прегабалин

What Прегабалин Treats: Main Uses and Benefits

This medication is applied across domains where additional symptomatic support is needed, primarily focusing on conditions involving symptoms related to heightened physiological activity. Its therapeutic role is generally considered relevant for easing three main symptom categories in adults: chronic nerve pain (neuropathic pain), symptoms of Generalized Anxiety Disorder (GAD), and as an add-on treatment for partial seizures.

In these clinical contexts, the medication assists with maintaining functional stability by managing symptoms that create noticeable functional strain. For instance, in neuropathic pain (such as that caused by diabetes or shingles), it helps address the burning, tingling, and shooting sensations. In GAD, it supports the reduction of excessive worry and tension.

“Applied in scenarios where additional management of discomfort is required, the medication offers symptomatic relief that may help patients cope more steadily with symptom fluctuations.”

It is commonly used across conditions presenting with recurrent or episodic manifestations. By helping to ease the overall symptom load, it supports patients during episodes of heightened discomfort.


Quick Fact: Support for Chronic Neuropathic Pain Symptoms


Regulatory References

  1. European Medicines Agency (EMA) overview

Eligibility and Restrictions for Use

Who Can and Cannot Use Pregabalin? Official Regulatory Information

Official regulatory documentation strictly defines the populations eligible to use Pregabalin. The medicine is contraindicated for patients with known hypersensitivity to the active substance or any of the product's excipients.

Age-Specific Eligibility

Pregabalin is officially established and permitted for use in adult patients aged 18 years and older. Use is not recommended for children and adolescents under 18 years because efficacy and safety have not been adequately established in this pediatric population. For older adults (aged 65 and over), use is permitted but may require specific dosage adjustments due to the higher probability of reduced kidney function.

Condition-Based Restrictions

Eligibility is contingent upon renal function. Patients with impaired kidney function require mandatory dosage modification based on creatinine clearance to use the medication safely. Conversely, hepatic impairment does not typically necessitate specific dose adjustments. Patients with rare hereditary problems, such as galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption, should not take formulations containing lactose.

Pregnancy and Lactation Status

Use of Pregabalin is not recommended during pregnancy unless the benefit to the mother is determined to outweigh the potential risk to the fetus. Women of childbearing potential must use effective contraception during treatment. The drug is also not recommended for women who are breastfeeding.

What should I know about interactions with other medicines?

Pregabalin presents a low risk for many pharmacokinetic drug-drug interactions because it is minimally metabolized in the liver, with most of the medicine being excreted in the urine as the unchanged compound. It does not appear to inhibit or induce major CYP450 liver enzymes, which commonly affect the elimination of other medications.

However, significant interactions are possible through a shared mechanism of action known as pharmacodynamic interaction, where the effects of two medicines are combined or intensified.

Interactions with CNS Depressants

The most significant concern is the concomitant use of pregabalin with other Central Nervous System (CNS) depressants, which can lead to enhanced somnolence, dizziness, and a heightened risk of severe respiratory depression (slowed or shallow breathing). The CNS depressant categories of concern include:

  • Opioids (e.g., oxycodone, tramadol)
  • Benzodiazepines
  • Alcohol (ethanol)
  • Other agents that cause sedation (e.g., some antihistamines or muscle relaxants)

These combinations, particularly with opioids, require careful monitoring due to the potential for life-threatening respiratory events, especially in elderly patients or those with existing respiratory issues. It is generally recommended to avoid alcohol entirely during treatment.

Other Documented Interactions

Co-administration with thiazolidinedione antidiabetic agents (Glitazones) carries an increased risk of peripheral edema (swelling) and weight gain. This combination warrants close monitoring, particularly for patients with compromised cardiovascular function.

Mechanism of Action

Modulation of Presynaptic Calcium Channels

Pregabalin's core mechanism initiates with its high-affinity binding to the alpha-2-delta (alpha2delta) subunit of presynaptic voltage-gated calcium channels (VGCCs) located within the central nervous system (CNS). This molecular interaction acts as a functional modulator, altering the channel's activity and limiting the excessive influx of calcium ions ( Ca^2+) into the nerve terminal.


Mechanistic Cascade and Synaptic Output

The restricted Ca^2+ influx directly reduces the presynaptic release of excitatory neurotransmitters, primarily glutamate and Substance P. This dampening of neurotransmitter output weakens the pathological synaptic transmission and lessens abnormal electrical activity in hyperexcitable neural networks. The effect is activity-dependent, meaning the modulation is most pronounced in states of pathological hyperactivity.


System-Level Physiological Modulation

Through this molecular cascade—from alpha2delta binding to reduced transmitter output—Pregabalin effects a modulation of activity in hyperexcitable neuronal circuits. This mechanistic pathway dictates an alteration in the functional state of the nervous system, characterized by a reversal of the excessive, synchronous signaling patterns typical of sensitized CNS pathways.

Dosage and Administration Information

Pregabalin is administered exclusively through the oral route, available as immediate-release (IR) capsules, oral solution, and extended-release (CR) tablets. The distinction between these formulations governs the daily administration schedule. Treatment typically begins with a starting dose of 150 mg per day, which is then gradually increased over a minimum of one week to reach a maintenance dose. The maximum total daily dose for the IR forms is 600 mg for conditions such as partial seizures or certain neuropathic pain states.

The immediate-release forms are indicated for administration in two or three divided doses throughout the day and may be taken irrespective of meals. In contrast, the extended-release tablets are taken once daily after an evening meal. These tablets require specific handling; they are to be swallowed whole and must not be split, crushed, or chewed, to preserve the controlled-release mechanism.

A key structural principle of use is the mandatory dose adjustment for patients with reduced renal function, as the medicine is primarily cleared by the kidneys. For these individuals, the dose is systematically reduced based on creatinine clearance levels, and a supplementary dose is required following hemodialysis. Conversely, no dose adjustment is necessary for hepatic impairment. When discontinuing treatment, the dosage is gradually reduced over a minimum period of one week as part of the discontinuation process.

Recent Clinical Evidence

Research Evidence / Overview of Studies

Summary of Efficacy Findings

Research has examined the potential of pregabalin to be associated with a change in pain, and explored its relationship with self-reported quality of life measures. Researchers in early-phase studies and pivotal trials focused on changes in pain intensity over 12-week and 52-week periods, with results documented across various pain scales, including the Visual Analog Scale (VAS) and the Brief Pain Inventory (BPI).

Key research evaluated the hypothesis that a daily use of this medication might be associated with a change in mobility scores, particularly during activities of daily living, in subjects involved in the study.


Safety and Tolerability Profile

Clinical trials documented the safety profile and indicated that the majority of adverse events reported were non-serious and resolved without intervention. Serious adverse events were infrequently reported. The observed safety data was consistent across primary and long-term extension studies.

Tolerance was evaluated in the studied populations. Researchers monitored common adverse events such as dizziness, somnolence, dry mouth, and peripheral edema (swelling of the limbs). Concurrent use of certain existing therapies was an area of study.


Combination Therapy Investigations

Combination studies examined whether using pregabalin alongside other treatments, such as physical therapy or certain analgesics, was associated with changes in inflammation markers or functional assessment scores compared to either intervention alone. These studies aimed to evaluate the potential for combined approaches.

Researchers continue to explore the effect of this combined approach. The study outcomes suggested that the concurrent use of both interventions was associated with specific changes in patient-reported functional status.


Population-Specific Research

Evidence regarding the use of pregabalin in specific patient groups, such as elderly subjects and those with mild to moderate kidney impairment, has been explored in sub-group analyses of larger trials. Its role in subjects who have previously discontinued other treatment modalities is an area of ongoing investigation. Data remains limited in subjects under the age of 18.

Key Studies & References Evaluation of the safety and efficacy of pregabalin in older patients with neuropathic pain: results from a pooled analysis of 11 clinical studies

Frequently Asked Questions (FAQ)

Common questions about Прегабалин (FAQ)


Q: Is Pregabalin the same kind of drug as Gabapentin?

Pregabalin and Gabapentin belong to the same class of medicines, known as gabapentinoids. They share a similar mechanism, working by binding to a specific subunit of calcium channels in the central nervous system. Official information indicates that Pregabalin is absorbed more quickly and fully by the body. Additionally, regulatory bodies in the United States classify Pregabalin as a federal Schedule V controlled substance, a classification not applied to Gabapentin.


Q: How quickly does Pregabalin start working?

Clinical studies indicate that some patients may report noticing a change in symptoms, such as the onset of pain relief, within the first week of use. However, the full therapeutic effect may take a longer period, sometimes up to one month, to be achieved, according to official product information.


Q: Does Pregabalin cause weight gain?

Official prescribing information states that weight gain is a Common side effect associated with the use of Pregabalin. It is also documented that the drug can cause peripheral edema, which is swelling caused by fluid retention in the hands, legs, or feet.


Q: Can Pregabalin be taken with pain relievers like Tylenol (paracetamol)?

Pregabalin is minimally metabolized by the liver, which suggests a low risk of direct chemical interactions with pain relievers like paracetamol (acetaminophen). The primary regulatory warning for interactions relates to its combination with Central Nervous System (CNS) depressants, which can cause dizziness or drowsiness, as the combined effect may be enhanced.


Q: Is there a risk of becoming dependent on Pregabalin?

Regulatory documents confirm a documented potential for abuse and physical dependence with Pregabalin. For this reason, it is classified as a federal Schedule V controlled substance in the United States. The official usage protocol includes gradually reducing the dose over a period of at least one week when discontinuing treatment.


Q: Can older adults (seniors) use Pregabalin?

Use is generally permitted for older adults. However, regulatory guidance indicates that older adults may require specific considerations. Because the medicine is cleared by the kidneys, this population often requires a lower starting dose and subsequent dosage adjustments due to the higher probability of reduced kidney function.


Q: Is Pregabalin safe to use during pregnancy?

Pregabalin is generally not recommended during pregnancy. The official guidance is that use is not recommended unless the potential benefits are judged to outweigh the potential risks to the fetus. Regulatory information advises that women who are of childbearing potential use effective contraception throughout the course of treatment.


Q: Can Pregabalin affect a person's mood or behavior?

Yes, official safety information documents that antiepileptic drugs, including Pregabalin, are associated with a class-wide risk of suicidal thoughts or behavior. Other mood and psychiatric reactions officially reported include anxiety, agitation, irritability, and depression.


Q: Does Pregabalin affect memory or concentration?

Official safety data lists adverse reactions related to cognitive function. These include difficulty concentrating or paying attention and instances of forgetfulness or memory loss.


Q: Can I use Pregabalin if I have a history of substance abuse?

Due to its potential for misuse and dependence, regulatory documents state that individuals with a history of drug or alcohol abuse should be managed with careful surveillance or medical supervision during treatment.


Q: What is the typical length of time people take Pregabalin?

The duration of use is determined by the specific condition being addressed. The medication is approved for the management of chronic conditions, such as certain types of neuropathic pain and generalized anxiety disorder. Regulatory documents reference long-term clinical trials that studied the drug's effects for periods of up to 52 weeks or more to establish safety and efficacy for chronic use.


Q: What happens if a dose of Pregabalin is missed?

The official patient information describes the protocol for a missed dose: it may be taken as soon as it is remembered, unless it is almost time for the next scheduled dose. In that event, the missed dose should be skipped, and the individual should resume the regular schedule with the next dose. It is specifically stated that two doses should not be taken together.


Q: Is Pregabalin considered a narcotic or controlled substance?

The drug is not considered a narcotic, as it does not belong to the opioid class of pain medicines. However, due to its documented potential for misuse, regulatory bodies in the United States classify it as a federal Schedule V controlled substance.


Q: Does Pregabalin help with anxiety, even though it's mainly for nerve pain?

Yes, in addition to nerve pain, Pregabalin is officially approved in many regions, including the European Union, for the treatment of Generalized Anxiety Disorder (GAD) in adults.


Q: Is there a generic version of Pregabalin available?

Yes. Following the expiration of the original brand product's patent, regulatory bodies have approved multiple generic versions of Pregabalin capsules and oral solutions. Generic availability is determined by the specific regulatory body after patent expiration.


Q: Can taking Pregabalin cause vision changes?

Yes. Official safety data lists blurred vision as a Common side effect. Other documented visual disturbances, such as double vision, are also reported in the safety profile.


Q: Is there any research on long-term effects of Pregabalin?

Regulatory information is underpinned by clinical evidence that includes long-term extension studies. These trials, which monitored patients for periods of up to 52 weeks or longer, were specifically conducted to document the safety, tolerability, and efficacy profile of the drug over an extended duration of use.


Q: Does Pregabalin affect blood pressure or heart rate?

Official prescribing information includes a warning that Pregabalin is associated with a potential for PR interval prolongation, which is an effect on heart rhythm, observed during clinical trials. This effect was mainly seen at high doses.


Q: What conditions make someone unable to use Pregabalin?

The drug is contraindicated (should not be used) if a patient has a known hypersensitivity or allergic reaction to the active substance or its ingredients. Additionally, use is generally not recommended for children and adolescents under 18 years because efficacy and safety have not been adequately established in that population.


Q: Are there any food or diet restrictions while taking Pregabalin?

Official administration instructions state that the immediate-release capsule form can be taken with or without food. However, the extended-release tablet form is intended to be taken once daily after an evening meal, as described in the administration instructions.


Q: Is it normal to feel a tingling sensation when starting the drug?

A tingling or prickling sensation, medically known as paresthesia, is a documented adverse reaction reported in the official safety profile of Pregabalin.


Q: Does Pregabalin interact with supplements like St. John's Wort?

Official guidance warns about the risk of pharmacodynamic interaction with substances that affect the central nervous system. Combining Pregabalin with certain herbal supplements, such as St. John's Wort, may enhance side effects like dizziness, drowsiness, and confusion.


Q: What are the signs of an overdose of Pregabalin?

Symptoms reported following an overdose include excessive somnolence (drowsiness), confusional states, agitation, and restlessness. In rare cases, more severe events such as coma and seizures have been reported.


Q: Can Pregabalin be taken with antidepressants?

Official warnings primarily focus on the risk of combining Pregabalin with other Central Nervous System (CNS) depressants, which can include certain types of antidepressants. This combination is noted to potentially lead to enhanced somnolence and dizziness.


Q: What is the difference between Pregabalin and opioids for pain?

Pregabalin is officially classified as a gabapentinoid/anticonvulsant that modulates calcium channels to reduce the release of excitatory neurotransmitters. It is explicitly not an opioid and does not work by binding to the opioid receptors targeted by narcotic pain medicines.


Q: Is it common to experience changes in sexual function with Pregabalin?

Official safety documents include sexual dysfunction in the list of documented adverse reactions. These effects can include changes such as decreased libido or difficulties with erection.


Q: Are there special warnings for people with diabetes taking Pregabalin?

Yes. Patients with diabetes should be monitored for an increased risk of peripheral edema (swelling) and weight gain. Furthermore, regulatory information includes a recommendation for close monitoring of the skin condition for people with diabetes taking this medication.


Q: What are the main goals of treatment when using Pregabalin?

The general therapeutic goals are defined by the approved uses and include achieving relief of neuropathic pain, stabilization of excessive nerve activity (in conditions like seizures), and relief of generalized anxiety disorder symptoms (where approved).

How should Прегабалин be stored and disposed of?

Storage and Disposal Requirements

Pregabalin must be stored at controlled room temperature, specifically 20 C to 25 C (68 F to 77 F), with permitted excursions to 30 C (86 F). The medication must be protected from moisture and kept in the original container with the lid tightly closed.

Stability and Child Safety

To ensure safety, pregabalin must be stored out of the sight and reach of children and pets. For the oral solution, any unused portion must be discarded 47 days after the bottle is opened to maintain stability.

Disposal

Disposal of unused or expired pregabalin should follow all local and national regulations. The officially preferred method is to utilize a medicine take-back program. The product must not be disposed of via wastewater or regular household trash unless specifically instructed.

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

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