Medicinal reference book geotar. Use in children

The drug Pregabalin-Richter is a drug from the group of antiepileptic drugs. By pharmacological action belongs to the group of anticonvulsant and analgesic drugs. The active substance is pregabalin. The mechanism of action is associated with the regulation of work calcium channels in neurons.

Pharmacokinetically, the drug is characterized by rapid and good absorption when taken on an empty stomach, the maximum concentration is reached approximately 1 hour after administration. Eating slightly reduces the rate at which pregabalin reaches its maximum concentration but does not affect overall bioavailability. medicine. There is no protein binding in blood plasma.

It is not actually metabolized in the body; approximately 99% of the total active substance is excreted unchanged through the kidneys. The half-life is six and a half hours. Given the mechanisms of elimination of pregabalin, the dosage of the drug should be reconsidered when used in people with renal failure. Doses are calculated based on creatinine clearance, which is directly proportional to drug clearance.

Based on data on the small percentage of metabolism of pregabalin, it should be assumed that liver diseases accompanied by liver failure, have virtually no effect on the concentration of the drug in the blood plasma.

Indications for use

Indications for prescribing the drug in neurological practice are following states:

Presence of neuropathic pain.
Epilepsy (commonly used as complementary therapy, monotherapy with the drug is ineffective).
Anxiety disorder.
Fibromyalgia.

Contraindications

Pregabalin-Richter is contraindicated for use in:

Allergies or other intolerance reactions, in the presence of hereditary enzymopathies (galactose intolerance, malabsorption), in childhood under 17 years of age.
Increased sensitivity to active substance or any other component of the drug.
Use with caution in persons with renal impairment. It should be taken into account that during hemodialysis most of the drug is excreted from the body.

The safety of Pregabalin-Richter has not been tested during pregnancy. During animal studies, signs of toxicity of the drug to the embryo were revealed. Based on these data, it is contraindicated for use during pregnancy. When using Pregabalin-Richter in women reproductive age contraceptive methods should be used to avoid a threat to the embryo when probable conception. Use during breastfeeding is also contraindicated. Refusal recommended breastfeeding, if it is impossible to avoid Pregabalin therapy.

Dosage

The dose of the drug is selected purely individually and is calculated based on the severity of the manifestations of the disease, the presence somatic diseases(primarily kidney pathology), drug tolerability, effect of concomitant therapy. The average daily dose should be in the range from 150 to 600 mg and divided into 2 or 3 doses. The drug is taken orally. Without chewing the capsule, regardless of food intake.

For neuropathic pain (the most common indication), the initial dose is usually 150 mg, divided into two doses. If necessary, after three to seven days1, if the drug is well tolerated, the dose can be increased by 150 mg; if the effect is insufficient, after another week the dose can be increased again to 600 mg.

Dose titration for other diseases is similar to that for neuropathic pain. It makes little sense to use the drug as a treatment for epilepsy if the effect is not achieved at a dosage of 450-600 mg per day.

An important point is the need for gradual withdrawal of Pregabalin. It is believed that withdrawal should take place over the course of a week, every day the dose is gradually reduced by 75 mg per day.

In case of insufficient renal function, a calculation method is used, taking creatinine clearance as a basis. There is no need to resort to such calculations when creatinine clearance is above 60 ml per minute. With a creatinine clearance of 30 to 60 ml per minute, the initial dose should not exceed 75 mg, the maximum daily dose is 300 mg, with a creatinine clearance of 15 to 30 ml per minute, the doses are respectively 25-50 mg and 150 mg. When creatinine clearance is less than 15 ml per minute (end stage renal failure) resort to prescribing Pregabalin with extreme caution, the initial dose cannot exceed 25 mg, the frequency of administration is 1 time per day, the maximum daily dose is 75 mg.

After a four-hour hemodialysis session, it makes sense to take an additional 25-100 mg of Pregabalin.

In older patients, if there is a decrease in creatinine clearance, the same dose adjustment of the drug is possible.

If you miss a dose, you must take the drug as soon as possible (especially with large daily dosages). The normal dosing schedule is resumed the next day.

Post-marketing studies have described sufficient quantity drug overdose. Even when taking 15 grams of Pregabalin, all phenomena disappeared after symptomatic therapy. The most common: confusion, disturbances mental sphere, drowsiness, decreased blood pressure. Specific therapy does not exist. Gastric lavage and administration of sorbents are indicated. If necessary, hemodialysis is performed.

Side effects

Clinical experience and careful evaluation of the development of side effects were carried out in major study, which involved more than 12 thousand patients. The most common side effects were: dizziness, drowsiness, general weakness. Below is a list of all side effects, noted during the tests. Designations: very common occurrence more than 10%, frequent - 1-10%, infrequently from 0.1 to 1%, rare less than 0.1%.

It should be taken into account that the listed phenomena could be associated with concomitant pathology, therapy and other reasons (you can read more about compiling the frequency of side effects).

From the mental sphere: often confusion, decreased libido, sleep disturbances, irritability. Anxiety, depression, mood variability, low mood, vivid dreams, changes in libido, apathy, and increased insomnia were uncommon. Rarely, disinhibition, increased background mood, euphoric states.

From the nervous system there were the most common adverse events. In the first place, very often, dizziness occurs. The following conditions were often encountered: impaired attention, ataxia, impairment of the coordination sphere, memory loss, sedative effect. Infrequently, hypoesthesia, the presence of nystagmus, speech impairment, myoclonus-type convulsions, decreased tendon reflexes, decreased taste sensations, tremors in the limbs, fainting. Hypokinesia, dysgraphia, and headaches were rarely observed.

From the outside of cardio-vascular system phenomena of pressure lability were noted (often a decrease in blood pressure, infrequently an increase in blood pressure), changes in pulse, and the development of atrioventricular blockades.

From other organs and systems. Often noted: fatigue, swelling, gait disturbance, changes in body weight, erectile disfunction, dry mouth, vomiting, flatulence, bloating, blurred vision. Uncommon: increased activity of ALT, CPK, AST, asthenia, thirst, chest tightness, chills, urinary incontinence, muscle twitching, swelling of the area large joints, painful sensations in the muscles, arthralgia, back pain, pain in the limbs, muscle stiffness (usually as a manifestation of the underlying disease), sweating, rash, increased salivation, shortness of breath, cough, constriction peripheral vision and, or visual acuity, hypoglycemia, eye swelling, lacrimation. Rarely: increased plasma creatinine concentration, changes in blood electrolyte composition, fever, pain in the mammary glands, enlarged mammary glands, menstrual irregularities, oliguria, acute renal failure, neck pain, rhabdomyolysis, sweat, nasal congestion, strabismus, snoring , flashing sparks before the eyes, loss of peripheral vision. Frequency unknown; extremely rare angioedema, severe allergic reactions(Quincke's edema).

Analogs

Pregabalin-Richter is a generic version of Lyrica. In comparison with the drug Lyrica, it should be noted that it has almost the same effectiveness and a high safety profile. The main advantage over the original drug is a much more affordable price.

special instructions

Pregabalin-Richter is excreted by the kidneys, does not bind to blood plasma proteins, and practically does not undergo transformation, as a result of which it can be assumed small degree interactions with other drugs, which has been confirmed in numerous trials. No interaction with the following drugs: finlepsin, phenobarbital, insulin, topiromate, tiagabine, phenytoin, depakine, lamotrigine, gabapentin, oxycodone. Simultaneous use with ethanol can enhance the effect of the latter, but does not affect vital centers, including the respiratory center.

Use of oral hormonal contraceptives, simultaneously with Pregabalin does not affect the pharmacokinetics of drugs.

There have been isolated cases of severe constipation up to paralytic intestinal obstruction when using Pregabalin with opioid analgesics and other drugs that can cause constipation.

Patients with diabetes mellitus changes in body weight may require adjustment of hypoglycemic therapy.

Pregabalin, especially in combination with antidepressants, may increase the risk of suicidal thoughts. If there is a history of suicide attempts, consultation with a psychotherapist is necessary.

Therapy with Pregabalin-Richter can and, unfortunately, is often accompanied by drowsiness and dizziness. In this regard, they are potentially contraindicated during treatment. dangerous species activities, including driving. The risk of accidental injury also increases, especially in older people.

There are separate development instructions convulsive syndrome, including epileptic seizures during therapy with Pregabalin or during its withdrawal.

If undesirable reactions develop, discontinuation of the drug or reduction in dosage, as a rule, leads to independent relief of undesirable manifestations.

There have been isolated cases of drug dependence. Special control in this regard, should be carried out for persons with a burdened medical history (drug addicts and persons with a history of drug addiction).

Price for capsules

Pregabalin-Richter is a frequently prescribed drug for central anesthesia. Attention! from October 1, 2015, the drug was included in the list potent drugs and is now dispensed according to a strictly numbered prescription with three seals, due to this, the availability of the drug has decreased, due to the lack of these recipes in some medical centers. The price of a medicine may vary depending on the specific pharmacy, region of residence, and dosage. Average prices for the drug are within the following limits (data current as of November 2015):

Capsules, 75 mg, package No. 14. 400-490 rubles.
Capsules, 75 mg, package No. 56. 1100-1500 rubles.
Capsules, 150 mg, package No. 14. 390-530 rubles.
Capsules, 150 mg, package No. 56. 1700-2100 rubles.
Capsules, 300 mg, package No. 14. 790-940 rubles.
Capsules, 300 mg, package No. 56. 2900-3400 rubles.

Dosage form"type="checkbox">

Dosage form

Compound

1 capsule contains:

active substance: pregabalin 75.0 mg, 150.0 mg, 300.0 mg;

excipients: lactose monohydrate, corn starch, talc.

Capsule shell:

capsule body composition: titanium dioxide, gelatin;

composition of the capsule cap: red iron dioxide dye E172 (for dosages of 75 mg and 300 mg), titanium dioxide (for dosage of 150 mg), gelatin.

Description

Dosage 75 mg. Solid gelatin capsules No. 4 with body white and the operculum is red-brown to dark red-brown in color.

Dosage 150 mg. Hard gelatin capsules No. 2 with a white body and a white cap.

Dosage 300 mg. Hard gelatin capsules No. 0 with a white body and a red-brown to dark red-brown cap.

The contents of the capsules are a homogeneous powder or compacted mass of white or white with a yellowish tint, which disintegrates when pressed with a glass rod.

Pharmacotherapeutic group

Drugs for the treatment of diseases of the nervous system. Antiepileptic drugs. Other antiepileptic drugs. Pregabalin.

ATX code N03AX16

Pharmacological properties"type="checkbox">

Pharmacological properties

Pharmacokinetics

Pharmacokinetic parameters of pregabalin in equilibrium state similar in healthy volunteers, in patients with epilepsy taking antiepileptic drugs, and in patients with chronic pain.

Suction

Pregabalin is rapidly absorbed on an empty stomach. The concentration of the drug in the blood plasma reaches a peak after one hour with both single and repeated use. The bioavailability of pregabalin when taken orally is

> 90% and does not depend on dose taken. At reuse the equilibrium state is achieved within 24-48 hours. Eating impairs the absorption of pregabalin. In this case, Cmax decreases by approximately 25-30%, and the time to reach maximum concentration (tmax) increases to approximately 2.5 hours. However, the use of pregabalin with food does not have a clinically significant effect on the degree of its absorption.

Distribution

The volume of distribution of pregabalin after oral administration is approximately 0.56 L/kg. The drug does not bind to blood plasma proteins.

Metabolism

Pregabalin undergoes little metabolism. Following a dose of radiolabeled pregabalin, approximately 98% of the radioactive material detected in the urine was unchanged pregabalin. The N‑methylated pregabalin derivative, which is the main metabolite of pregabalin found in urine, accounted for 0.9% of the dose taken.

Removal

Pregabalin is eliminated from systemic blood flow mainly by the kidneys in unchanged form.

The average half-life of pregabalin is 6.3 hours. Plasma and renal clearance pregabalin is directly proportional to creatinine clearance.

Linearity/nonlinearity

The pharmacokinetics of pregabalin in the recommended range of daily doses is linear. Interindividual variability in the pharmacokinetics of pregabalin is low (< 20 %). Фармакокинетику препарата при многократном приеме можно предсказать исходя из его фармакокинетики при однократном приеме. Поэтому необходимость в рутинном мониторинге концентрации прегабалина в плазме крови отсутствует.

Clinical studies indicate that gender does not have a clinically significant effect on pregabalin plasma concentrations.

Renal dysfunction

Pregabalin clearance is directly proportional to creatinine clearance. In addition, pregabalin is effectively eliminated from blood plasma during hemodialysis (after 4 hours of hemodialysis, the concentration of pregabalin in blood plasma decreases by approximately 50%). Since the main route of elimination is renal excretion, a dose reduction is required in patients with impaired renal function, and additional doses are required after hemodialysis.

Liver dysfunction

Specific pharmacokinetic studies have not been conducted in patients with impaired liver function. Because pregabalin is not significantly metabolized and is excreted primarily unchanged in the urine, hepatic impairment is not expected to significantly affect pregabalin plasma concentrations.

Patients childhood

The pharmacokinetics of pregabalin were evaluated in pediatric patients with epilepsy (age groups: 1 to 23 months, 2 to 6 years, 7 to 11 years, and 12 to 16 years) at dose level 2.5; 5; 10 and 15 mg/kg/day in a pharmacokinetics and tolerability study.

Following oral administration of pregabalin on an empty stomach in pediatric patients, the time to peak plasma concentrations was generally similar for all age groups, ranging from 0.5 to 2 hours after dosing.

The values of the Cmax and AUC parameters increased linearly with increasing dose in each age group. The AUC value in pediatric patients weighing up to 30 kg was lower by 30% due to a 43% increase in weight-adjusted clearance in these patients compared to patients weighing ≥ 30 kg.

In pediatric patients under 6 years of age, the terminal half-life of pregabalin averaged 3 to 4 hours, and in children 7 years of age and older, it averaged 4 to 6 hours.

Population pharmacokinetic analysis demonstrated that creatinine clearance was a significant covariate of pregabalin clearance at orally, body weight was a significant covariate of the apparent volume of distribution of oral pregabalin, and these relationships were similar in the pediatric and adult patient populations.

The pharmacokinetics of pregabalin in patients less than 3 months of age have not been studied.

Pregabalin clearance tends to decrease in older age. This decrease in clearance with oral pregabalin is comparable to the decrease in creatinine clearance associated with older age. Patients with age-related disorders renal function may require a dose reduction of pregabalin.

Breastfeeding women

The pharmacokinetics of pregabalin 150 mg every 12 hours (300 mg daily dose) were assessed in lactating women at least 12 weeks postpartum. Lactation had no or negligible effect on the pharmacokinetics of pregabalin. Pregabalin was excreted into breast milk at an average steady-state concentration of approximately 76% of the steady-state concentration in maternal plasma. The theoretical average daily dose of pregabalin given to a child with breast milk(estimated average milk intake: 150 ml/kg/day) of women taking 300 mg/day or the maximum dose of 600 mg/day is 0.31 to 0.62 mg/kg/day, respectively. These estimated doses represent approximately 7% of the total maternal daily dose calculated in mg/kg body weight.

Pharmacodynamics

The active ingredient of the drug is pregabalin - an analogue gamma-aminobutyric acid((S)-3-(aminomethyl)-5-methylhexanoic acid).

Mechanism of action

Pregabalin binds to the accessory subunit (α2-delta protein) of voltage-gated calcium channels in the central nervous system.

Indications for use

Treatment of peripheral and central neuropathic pain in adults

Epilepsy in adults with partial seizures with or without secondary generalization (as an adjuvant)

Treatment of generalized anxiety disorder in adults

Directions for use and doses

The drug is administered orally at a dose of 150 to 600 mg per day in two or three doses.

The drug can be taken regardless of meals.

Neuropathic pain

Treatment begins with a dose of 150 mg per day, divided into two or three doses. Depending on the patient's individual response and tolerability, after 3-7 days the dose can be increased to 300 mg per day, and, if necessary, after another 7 days - to a maximum dose of 600 mg per day.

Epilepsy

Treatment begins with a dose of 150 mg per day, divided into two or three doses. Depending on the patient's individual response and tolerability of the drug, after one week the dose can be increased to 300 mg per day, and after another week - to a maximum dose of 600 mg per day.

Generalized anxiety disorders

The drug is used in a dose of 150 to 600 mg per day in two or three doses. The need for treatment should be reviewed regularly.

Treatment begins with a dose of 150 mg per day. Depending on the patient's individual response and tolerability of the drug, after one week the dose can be increased to 300 mg per day, after another week the dose can be increased to 450 mg per day, and after another week to a maximum dose of 600 mg per day.

Pregabalin withdrawal

Patients with impaired renal function

Pregabalin is excreted from the systemic circulation primarily by the kidneys in unchanged form. Because pregabalin clearance is directly proportional to creatinine clearance, dose reduction in patients with renal impairment should be individualized based on creatinine clearance (CrCl) as indicated in Table 1 and determined using the following formula:

ClCr (ml/min) =

Pregabalin is effectively removed from blood plasma by hemodialysis (50% of the drug after 4 hours). In patients receiving hemodialysis, the daily dose of the drug is selected taking into account renal function. In addition to the daily dose of the drug, an additional dose is prescribed every 4 hours of hemodialysis (see Table 1).

Table 1. Pregabalin dose adjustment based on renal function

1 The total daily dose (mg/day) should be divided according to the dosing regimen to obtain the required mg/dose value

2 An additional dose is a single additional dose

Patients with liver dysfunction

In patients with impaired liver function, no dose adjustment is required.

Patients of childhood and adolescence

The safety and effectiveness of Pregabalin in children under 12 years of age and adolescents (aged 12-17 years) have not been established. The available data are presented in the sections “Side effects” and “Pharmacological properties”, but it is impossible to give dosage recommendations based on them.

Elderly patients (over 65 years old)

Elderly patients may require a dose reduction due to decreased renal function.

Side effects

When using Pregabalin, undesirable effects were registered, which were classified according to the frequency of their occurrence. in the following way: very often (≥ 1/10), often (from ≥ 1/100 to< 1/10), нечасто (от ≥ 1/1000 до < 1/100) и редко (≥ 1/10 000 и < 1/1000) и неизвестно (невозможно определить по имеющимся данным).

Often

Dizziness, headache, drowsiness

Nasopharyngitis

Increased appetite

Euphoria, confusion, irritability, disorientation, insomnia, decreased libido

Ataxia, incoordination, tremor, dysarthria, amnesia, memory impairment, attention impairment, paresthesia, hypoesthesia, sedation, imbalance, lethargy

Blurred vision, diplopia

Vertigo

Dry mouth, nausea*, vomiting, flatulence, bloating, constipation, diarrhea*

erectile disfunction

Increased fatigue peripheral edema, swelling, gait disturbance, falling, feeling drunk, feeling unwell

Weight gain

Muscle cramps, arthralgia, back pain, limb pain, muscle spasm cervical spine spine

Neutropenia

Hypersensitivity*

Anorexia, hypoglycemia

Hallucinations, panic attack, anxiety, agitation, depression, depressed mood, high spirits, aggression*, mood swings, depersonalization, difficulty finding words, unusual dreams, increased libido, anorgasmia, apathy

Fainting, stupor, myoclonus, loss of consciousness*, psychomotor hyperactivity, dyskinesia, postural dizziness, intention tremor, nystagmus, cognitive disorder, mental disorder*, speech disorder, hyporeflexia, hyperesthesia, burning sensation, ageusia, malaise*

Loss of peripheral vision, blurred vision, swollen eye, visual field defect, decreased visual acuity, eye pain, asthenopia, photopsia, dry eye syndrome, increased lacrimation, eye irritation

Hyperacusis

Tachycardia, first degree atrioventricular block, sinus bradycardia, chronic heart failure*

Hypotension, hypertension, hot flashes, flushing, cold hands and feet

Dyspnea, nose bleed, cough, nasal congestion, rhinitis, snoring, dry nasal mucosa

Gastroesophageal reflux disease, increased salivation, oral hypoesthesia

Papular rash, urticaria, hyperhidrosis, itching*

Joint swelling, myalgia, muscle cramps, neck pain, muscle stiffness

Urinary incontinence, dysuria

Sexual dysfunction, delayed ejaculation, dysmenorrhea, breast pain

Generalized edema, facial edema*, chest tightness, pain, pyrexia, thirst, chills, asthenia

Increased blood creatine phosphokinase level, increased blood alanine aminotransferase level, increased aspartate aminotransferase level, increased blood glucose level, decreased platelet count, increased blood creatinine level, hypokalemia, weight loss

Angioedema*, allergic reaction*

Disinhibition

Convulsions*, parosmia, hypokinesia, dysgraphia

Loss of vision*, keratitis*, oscillopsia, changes in the depth of visual perception, mydriasis, strabismus, brightness of visual perception

Prolongation of the QT interval*, sinus tachycardia, sinus arrhythmia

Tightness in the throat, pulmonary edema*

Swelling of the tongue*, dysphagia, ascites, pancreatitis

Stevens-Johnson syndrome*, cold sweat

Rhabdomyolysis

Oliguria, urinary retention*, renal failure

Amenorrhea, breast enlargement, breast discharge, gynecomastia*

Decreased white blood cell count

*Additional reactions recorded during post-marketing studies of the drug

Pediatric patients

The safety profile of pregabalin observed in studies in pediatric patients was similar to that in adult patients.

Reporting Suspected Adverse Reactions

Reporting information about suspected adverse reactions identified after registration of a medicinal product has great importance. This allows continued monitoring of the benefit-risk ratio of the drug.

Healthcare professionals and patients are asked to report any adverse reactions to the address listed at the end of this prescribing information.

Contraindications

Hypersensitivity to the active substance or to any of excipients drug

Children's and adolescence up to 18 years old

Pregnancy and lactation

Drug interactions"type="checkbox">

Drug interactions

Since in humans, pregabalin is predominantly excreted unchanged in the urine and undergoes little metabolism (< 2 % дозы выводится с мочой в виде метаболитов), не ингибирует in vitro метаболизм других препаратов и не связывается с белками плазмы крови, его фармакокинетическое взаимодействие с другими medicines unlikely.

In vivo studies and population pharmacokinetic analysis

There was no evidence of a clinically significant pharmacokinetic interaction between Pregabalin and phenytoin, carbamazepine, valproic acid, lamotrigine, gabapentin, lorazepam, oxycodone or ethanol. It has been established that oral antidiabetic agents, diuretics, insulin, phenobarbital, tiagabine and topiramate do not have a clinically significant effect on the clearance of Pregabalin.

Oral contraceptives, norethisterone and/or ethinyl estradiol

Concomitant use of pregabalin with oral contraceptives, norethisterone and/or ethinyl estradiol does not affect the pharmacokinetics of these substances at steady state.

Medicines affecting the central nervous system

Pregabalin may enhance the effects of ethanol and lorazepam.

In controlled clinical studies, no clinically significant effects on respiratory function were observed with repeated oral administration of Pregabalin with oxycodone, lorazepam or ethanol.

There are reports received during post-registration use of the drug about respiratory failure and coma in patients receiving Pregabalin and other central nervous system depressants.

Pregabalin appears to additively enhance the effects of oxycodone on cognitive and gross motor function.

Interactions and elderly patients

Specific studies of pharmacodynamic interactions in elderly volunteers have not been conducted. Drug-drug interaction studies were conducted only in adult patients.

special instructions"type="checkbox">

special instructions

Patients with diabetes mellitus

Some patients with diabetes who experience weight gain while using pregabalin may require dosage adjustments of their hypoglycemic medications.

Hypersensitivity reactions

There have been reports of hypersensitivity reactions, including cases angioedema. If you experience symptoms of angioedema, such as swelling of the face, swelling around the mouth, or swelling of the upper respiratory tract, you should stop taking pregabalin immediately.

Dizziness, drowsiness, loss of consciousness, confusion and mental disorder

Treatment with pregabalin has been associated with dizziness and drowsiness, which may increase the risk of accidental injury (falls) in elderly patients. During post-marketing use of the drug, there have been reports of loss of consciousness, confusion and mental disorder. Therefore, patients should exercise caution until they are aware of potential effects drug.

Effects related to vision

In controlled studies, patients treated with pregabalin experienced worsening of visual clarity more frequently than patients treated with placebo; in most cases, this side effect disappeared with continued use of the drug. In clinical studies in which ophthalmological examination, the incidence of decreased visual acuity and changes in visual fields was higher in patients receiving pregabalin compared with patients receiving placebo; the incidence of fundus changes was higher in patients receiving placebo.

During the period of post-registration use of the drug, adverse events from the organ of vision were also recorded, including loss of vision, blurred vision or other changes in visual acuity, many of which were short-term. Discontinuation of the drug may lead to the disappearance or reduction of the severity of these visual symptoms.

Kidney failure

Cases of renal failure have been reported, and in some cases, discontinuation of pregabalin resulted in reversibility of this adverse reaction.

Discontinuation of concomitant antiepileptic drugs

There is insufficient data on the discontinuation of concomitant antiepileptic drugs after seizure control has been achieved with pregabalin when the drug is added to antiepileptic therapy for use as monotherapy.

Withdrawal symptoms

After stopping the short-term and long-term treatment With pregabalin, some patients experienced withdrawal symptoms. Observed the following phenomena, indicating physical dependence: insomnia, headache, nausea, anxiety, diarrhea, flu-like syndrome, nervousness, depression, pain, cramps, hyperhidrosis and dizziness. The patient should be informed about this at the beginning of treatment.

Seizures may occur while using pregabalin or shortly after stopping it, including status epilepticus and expanded seizures. With regard to discontinuation of long-term pregabalin treatment, evidence suggests that the frequency and severity of withdrawal symptoms may be dose dependent.

Chronic heart failure

Cases of chronic heart failure have been reported in some patients taking pregabalin during the post-marketing period. These reactions were observed primarily in elderly patients with cardiovascular disorders during the use of pregabalin for neuropathic indications. Pregabalin should be used with caution in such patients. Discontinuation of pregabalin may resolve the reaction.

Treatment of central neuropathic pain due to injury spinal cord

During treatment of central neuropathic pain due to spinal cord injury, the overall incidence of adverse reactions, the incidence of central nervous system adverse reactions, and especially the incidence of somnolence were increased. This may be due to an additive effect caused by concomitant medications (eg, antispasmodics) needed to treat this condition. This should be taken into account when prescribing pregabalin for the treatment of this disease.

Suicidal thinking and behavior

Suicidal ideation and behavior have been reported in patients receiving antiepileptic drugs for several indications. A meta-analysis of randomized placebo-controlled trials of antiepileptic drugs also demonstrated slight increase risk of suicidal thoughts and suicidal behavior. The mechanism of this risk is unknown, and available data do not exclude the possibility of an increased risk with pregabalin use. Therefore, patients should be monitored for signs of emerging suicidal ideation and behavior, and the possibility of

appropriate treatment. Patients (and caregivers) should be advised to seek medical care if signs of suicidal thinking or behavior appear.

Decreased function lower sections gastrointestinal tract

During the post-marketing period, events associated with decreased function of the lower gastrointestinal tract (eg, intestinal obstruction, paralytic ileus bowel and constipation) when pregabalin was used concomitantly with drugs that may cause constipation, such as opioid analgesics. At simultaneous use pregabalin and opioid medications, measures to prevent constipation may be considered (especially in female and elderly patients).

Inappropriate use, potential for abuse and dependence

Cases of inappropriate use of the drug, abuse or dependence on it have been reported. In patients with a history of substance abuse, pregabalin should be administered with caution and such patients should be monitored for signs of drug misuse, abuse, or dependence (development of tolerance, dose escalation, drug-seeking behavior).

Encephalopathy

Cases of encephalopathy have been reported, predominantly in patients with underlying medical conditions that may lead to encephalopathy.

Lactose intolerance

Pregabalin contains lactose monohydrate. The drug should not be prescribed to patients with rare hereditary galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption syndrome.

Pregnancy and lactation

Women of childbearing potential/contraception in men and women

Because the potential risk to humans is unknown, women of childbearing potential should use effective methods of contraception.

Pregnancy

There are no sufficient data on the use of pregabalin in pregnant women.

Pregabalin should not be used during pregnancy unless clearly necessary (unless the expected benefit to the mother clearly exceeds possible risk for the fetus).

Lactation period

Pregabalin is excreted into breast milk. The effect of pregabalin in neonates/infants is unknown. The decision to discontinue breastfeeding or discontinue pregabalin therapy should be made taking into account the benefits of breastfeeding for the baby and the benefit of therapy for the woman.

Reproductive function

There are no clinical data on the effect of pregabalin on the reproductive function of women.

According to clinical trial There was no effect of pregabalin on sperm motility in men.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

The drug may have a slight or moderate effect on the ability to drive vehicles and work with machinery. Pregabalin may cause dizziness and drowsiness and thereby affect the ability to drive vehicles and use machines. Patients are advised to avoid driving vehicles, working with complex mechanisms or carrying out any other potentially hazardous activity until it has been determined whether this drug impact on their ability to carry out these activities.

Storage conditions

Store at a temperature not exceeding 25 ºC.

Keep out of the reach of children.

Best before date

Do not use after the expiration date stated on the package.

Conditions for dispensing from pharmacies

Dispensed by prescription.

Manufacturer

DONGBANG FUTURE TECH AND LIFE CO., LTD., Korea

78, Yeakgondan 4-gil, Hyangnam-yup, Hwaseong-si, Gyeonggi-do, Republic of Korea

Dosage form: TO capsules. Compound:

1 capsule contains:

active substance: pregabalin 75.0 mg, 150.0 mg, 300.0 mg;

Excipients: lactose monohydrate 8.25 mg / 16.5 mg / 33.0 mg, corn starch 14.25 mg / 28.5 mg / 57.0 mg, talc 2.5 mg / 5.0 mg / 10.0 mg.

Capsule shell: composition of the capsule body: titanium dioxide 1.2%/2%/1.2%, gelatin up to 100% (for all dosages); composition of the capsule cap: iron dye red dioxide E172 (for a dosage of 75 mg - 1.7%, for a dosage of 300 mg - 1.7%), titanium dioxide (for a dosage of 150 mg - 2%), gelatin up to 100% (for all dosages).

Description:

Dosage 75mg. Hard gelatin capsules No. 4 with a white body and a red-brown to dark red-brown cap.

Dosage 150 mg. Hard gelatin capsules No. 2 with a white body and a white cap.

Dosage 300mg. Hard gelatin capsules No. 0 with a white body and a red-brown to dark red-brown cap.

The contents of the capsules are a homogeneous powder or compacted mass of white or white with a yellowish tint, which disintegrates when pressed with a glass rod.

Pharmacotherapeutic group:antiepileptic drug ATX:

N.03.A.X.16 Pregabalin

Pharmacodynamics:

The active ingredient is an analogue of gamma-aminobutyric acid ((S)-3-(aminomethyl)-5-methylhexanoic acid).

Mechanism of action

Pregabalin binds to the accessory subunit (α2-delta protein) of voltage-gated calcium channels in the central nervous system, irreversibly replacing α-gabapentin. It is assumed that such binding may contribute to its analgesic and anticonvulsant effects.

Neuropathic pain

The effectiveness of pregabalin has been noted in patients with diabetic neuropathy and postherpetic neuralgia.

It has been established that when taking pregabalin in courses of up to 13 weeks, twice a day, and up to 8 weeks, three times a day, in general, the risk of side effects and the effectiveness of the drug when taken two or three times a day are the same.

When taken for a course of up to 13 weeks, pain decreased during the first week, and the effect persisted until the end of treatment.

There was a 50% decrease in pain index in 35% of patients receiving and 18% of patients receiving placebo. Among patients who did not experience drowsiness, this pain reduction effect was observed in 33% of patients in the pregabalin group and 18% of patients in the placebo group. 48% of patients taking and 16% of patients taking placebo experienced drowsiness.

Fibromyalgia

A marked reduction in pain symptoms associated with fibromyalgia is observed with the use of pregabalin in doses from 300 mg to 600 mg per day. The effectiveness of doses of 450 mg and 600 mg per day is comparable, but the tolerability of 600 mg per day is usually worse. Also, the use of pregabalin is associated with a marked improvement in functional activity patients and a decrease in the severity of sleep disorders. The use of pregabalin at a dose of 600 mg per day led to a more pronounced improvement in sleep compared with a dose of 300-450 mg per day.

Epilepsy

When taking the drug for 12 weeks two or three times a day, the noted risk of side effects and the effectiveness of the drug are the same for these dosing regimens. A decrease in seizure frequency began within the first week.

A decrease in the symptoms of generalized anxiety disorder is observed in the first week of treatment. When using the drug for 8 weeks, 52% of patients receiving and 38% of patients receiving placebo had a 50% reduction in symptoms on the Hamilton Anxiety Scale (HAM-A).

Pharmacokinetics:

Pharmacokinetic parameters of pregabalin at steady state in healthy volunteers, in patients with epilepsy receiving antiepileptic therapy, and in patients receiving it for chronic pain syndromes, were similar.

Suction

Pregabalin is rapidly absorbed on an empty stomach. The maximum concentration of nregabazine in plasma (Cmax) is achieved after 1 hour with both single and repeated use. The oral bioavailability of pregabalin is ≥ 90% and is independent of dose. With repeated use, the equilibrium concentration is achieved after 24-48 hours. When using the drug after a meal, C m ax decreases by approximately 25-30%, and the time to reach the maximum concentration (t max ) increases to approximately 2.5 hours. However, food intake does not has a clinically significant effect on the overall absorption of pregabalin.

Distribution

The apparent volume of distribution of pregabalin after oral administration is approximately 0.56 L/kg. does not bind to plasma proteins.

Animal studies of pregabalin have shown that it crosses the blood-brain barrier in mice, rats and monkeys. It has also been shown to penetrate the placenta and is found in the milk of lactating rats.

Metabolism

Pregabalin is practically not metabolized. After taking labeled pregabalin, approximately 98% of the radioactive tracer was detected unchanged in the urine. The proportion of N-methylated pregabalin derivative, which is the main metabolite found in urine, was 0.9% of the dose. In preclinical studies, there was no evidence of racemization of the S-enantiomer of pregabalin to the R-enantiomer.

Removal

Pregabalin is excreted primarily unchanged by the kidneys.

The average half-life is 6.3 hours. Plasma clearance of pregabalin and renal clearance are directly proportional to creatinine clearance (see section "Impaired renal function"). In patients with impaired renal function and patients on hemodialysis, dose adjustment is necessary (see section "Method of administration and dosage" Table 1).

Linearity/nonlinearity

The pharmacokinetics of pregabalin in the range of recommended daily doses is linear, interindividual variability is low (< 20%). Фармакокинетику прегабалина при повторном применении можно предсказать па основании данных приема однократной дозы. Следовательно, необходимости в регулярном мониторировании концентрации прегабалина нет.

Sex differences

Patient gender does not have a clinically significant effect on plasma pregabalin concentrations.

Renal dysfunction

Pregabalin clearance is directly proportional to creatinine clearance. Given that it is mainly excreted by the kidneys, it is recommended to reduce the dose of pregabalin in patients with impaired renal function. In addition, it is effectively removed from plasma during hemodialysis (after a 4-hour hemodialysis session, pregabalin concentrations in plasma are reduced by approximately 50%), after hemodialysis an additional dose of the drug must be prescribed (see section "Method of administration and dosage" in Table. 1 ).

Liver dysfunction

The pharmacokinetics of pregabalia in patients with impaired liver function have not been specifically studied. It is practically not metabolized and is excreted mainly unchanged in the urine, therefore, impaired liver function should not significantly change the concentration of pregabalin in plasma.

Elderly patients (over 65 years old)

Pregabalin clearance tends to decrease with age, reflecting age-related decline creatinine clearance. Elderly people with impaired renal function may require a reduction in the dose of the drug (see section "Method of administration and dosage" of table. 1 ).

Nursing mothers

The pharmacokinetics of pregabalin, 150 mg, administered every 12 hours (300 mg daily dose), were evaluated in 10 lactating women (at least 12 weeks postpartum period). Lactation had little or no effect on the pharmacokinetics of pregabalin. excreted through breast milk in an equilibrium concentration of about 76% of the amount contained in the mother's blood plasma. At 300 mg/day or a maximum dose of 600 mg/day, the dose of pregabalin received by a breastfed infant (assuming an average milk intake of 150 ml/kg/day) is approximately 0.31 and 0.62 mg/kg/day. respectively. The calculated doses represent about 7% of the total daily dose received by a lactating woman in mg/kg.

Indications:

Neuropathic pain

Treatment of neuropathic pain in adults.

Epilepsy

As an adjunctive therapy in adults with partial seizures, accompanied or not accompanied by secondary generalization.

Generalized anxiety disorder

Treatment of generalized anxiety disorder in adults.

Fibromyalgia

Treatment of fibromyalgia in adults.

Contraindications:

Hypersensitivity to the active substance or any other component of the drug.

Rare hereditary diseases, including galactose intolerance, lactase deficiency and glucose/galactose malabsorption.

Children and adolescents up to 17 years of age inclusive due to the lack of data on use.

Carefully:

Renal failure (see section "Method of administration and dosage"); heart failure (see section " Side effect").

Due to registered isolated cases uncontrolled use of pregabalin, it should be prescribed with caution to patients with a history of drug dependence. Such patients require close medical supervision during treatment with the drug.

Pregnancy and lactation:

Pregnancy

There are no reliable data on the effectiveness and safety of pregabalin during pregnancy. When used in animals, the drug had toxic effect on reproductive function. In this regard, it can be used during pregnancy only if the benefit to the mother clearly outweighs the possible risk to the fetus. When treated with pregabalin, women of reproductive age should use effective methods contraception.

Lactation

Pregabalin is excreted in breast milk. Since the safety of pregabalin in neonates is unknown, breastfeeding is not recommended during treatment with pregabalin. Breastfeeding or pregabalin therapy should be discontinued, taking into account the need for therapy for the mother and breastfeeding for the newborn.

Fertility

There are no clinical data on the effect of pregabalin on women's fertility. In a clinical trial to evaluate the effect of pregabalin on sperm motility healthy men taken at a dose of 600 mg/day. After 3 months of treatment, no effect of the drug on sperm motility was recorded. A study on female rats found negative effects on reproductive system. A study on male rats found unfavorable side effects on reproductive function and subsequent ontogenetic development. Clinical relevance these results are unknown.

Undesirable effects on the fertility of male and female rats were observed only when the drug was used in doses significantly higher than therapeutic ones. Undesirable effects on the genital organs and sperm parameters of male rats were reversible and were observed only when the drug was used in doses significantly higher than therapeutic ones, or were associated with spontaneous degenerative processes in the genital organs of rats.

Directions for use and dosage:

Inside, regardless of food intake. The drug is used in a dose of 150 to 600 mg/day in two or three doses.

Neuropathic pain

Pregabalin treatment begins with a dose of 150 mg/day, taken in two divided doses. Depending on the achieved effect and tolerability, after 3-7 days the dose can be increased to 300 mg/day, and if necessary, after another 7 days - to a maximum dose of 600 mg/day.

Epilepsy

Pregabalin treatment begins with a dose of 150 mg/day, taken in two divided doses. Taking into account the achieved effect and tolerability, after 1 week the dose can be increased to 300 mg/day, and if necessary, after another week - to a maximum dose of 600 mg/day.

Fibromyalgia

Pregabalin treatment begins with a dose of 150 mg/day, taken in two divided doses. Depending on the effect achieved and tolerability, after 7 days the dose can be increased to 300 mg/day. With absence positive effect the dose is increased to 450 mg/day, and if necessary, after another 7 days - to a maximum dose of 600 mg/day.

Generalized anxiety disorder

Pregabalin treatment begins with a dose of 150 mg/day. Depending on the effect achieved and tolerability, after 7 days the dose can be increased to 300 mg/day. If there is no positive effect, the dose is increased to 450 mg/day, and if necessary, after another 7 days - to a maximum dose of 600 mg/day.

Pregabalin withdrawal

If pregabalin treatment must be discontinued, it is recommended that this be done gradually over a period of at least 1 week.

Patients with impaired renal function

In patients with impaired renal function, the dose is selected individually taking into account creatinine clearance (CC) (Table 1), which is calculated using the following formula:

For men:

CC (ml/min) = x body weight (kg) / 72 x serum creatinine (mg/dl)

For women:

CC (ml/min) = x body weight (kg) / 72 x serum creatinine (mg/dl) x 0.85

In patients receiving hemodialysis treatment, the daily dose of pregabalin is adjusted based on renal function. After a 4-hour hemodialysis session, plasma pregabalin concentrations are reduced by approximately 50%. Immediately after each 4-hour hemodialysis session, an additional dose is prescribed (see Table 1).

Table 1. Pregabalin dosage based on renal function

Creatinine clearance, ml/min	Daily dose pregabalin		Frequency of intake per day
	Starting dose, mg/day	Maximum dose, mg/day




Additional dose after dialysis (mg)
			One time

Use in patients with liver dysfunction

In patients with impaired liver function, no dose adjustment is required (see section "Pharmacokinetics").

Use in children under 12 years of age and adolescents (12-17 years of age, inclusive)

The safety and effectiveness of pregabalin in children under 12 years of age and adolescents up to and including 17 years of age have not been established. The use of the drug in children and adolescents is not recommended.

Use in the elderly (over 65 years of age)

Elderly people may require a reduction in the dose of pregabalin due to decreased renal function (see section "Pharmacokinetics", use in patients with impaired renal function).

If you miss a dose of pregabalin, take the next dose as soon as possible, but do not take the missed dose if it is almost time for the next one.

Side effects:

Based on experience clinical application Pregabalin in more than 12,000 patients, the most common adverse events were dizziness and somnolence. The observed effects were usually mild or moderate. The discontinuation rates of pregabalin and placebo due to adverse reactions were 14% and 7%, respectively.

Main unwanted effects symptoms that required discontinuation of treatment were dizziness (4%) and runny nose (3%), depending on their subjective tolerability. Other side effects that also lead to drug withdrawal: ataxia, confusion, asthenia, impaired attention, blurred vision, impaired coordination, peripheral edema.

Also noted unwanted reactions symptoms that occur after discontinuation of pregabalin: insomnia, headache, nausea, anxiety, flu-like syndrome, convulsions, increased excitability, depression, pain, hyperhidrosis and diarrhea.

During the treatment of central neuropathic pain associated with spinal cord injury, there is an increase in the frequency adverse reactions in general, as well as adverse reactions from the central nervous system, especially drowsiness.

After stopping short- and long-term treatment with pregabalin, some patients experienced withdrawal symptoms. The following reactions have been recorded: insomnia, headache, nausea, anxiety, diarrhea, flu-like syndrome, convulsions, increased excitability, depression, pain, increased sweating and dizziness indicating physical dependence. The patient must be informed about this before starting therapy.

Observations suggest that when long-term pregabalin treatment is discontinued, the incidence and severity of withdrawal symptoms may depend on the dose of the drug.

The table lists all adverse events whose frequency exceeded that in the placebo group (observed in more than 1 person). They are distributed according to systemic organ classes and frequency (very common (≥1/10), common (≥1/100,<1/10), нечастые (≥1/1000, <1/100) и редкие (<1/1000)).

Reactions observed during post-registration use of the drug are highlighted italics.

The listed adverse events could be associated with the underlying disease and/or concomitant therapy.

System	Adverse reactions
Infections and infestations
Infrequent	Nasopharyngitis
Blood and lymphatic system
Infrequent	Neutropenia
Metabolic and nutritional disorders
	Increased appetite
Infrequent	Anorexia, hypoglycemia
Mental disorders
	State of euphoria, confusion, decreased libido, insomnia, irritability, disorientation, panic attack, apathy, depression
Infrequent	Hallucinations, anxiety, agitation, depressed mood, elevated mood, mood swings, aggressiveness, depersonalization, disturbing dreams, difficulty finding words, increased libido, anorgasmia, increased insomnia
	Disinhibition
Neurological disorders
Very frequent	Dizziness, drowsiness, headache
	Ataxia, impaired attention, impaired coordination, memory impairment, tremor, dysarthria, paresthesia, imbalance, amnesia, lethargy, kinesthesia, sedation, ageusia
Infrequent	Fainting, myoclonus, psychomotor agitation, dyskinesia, orthostatic dizziness, intention tremor, nystagmus, speech impairment, decreased reflexes, burning sensation on the skin and mucous membranes, hyperesthesia,loss of consciousness, cognitive impairment
Rare	Pathological numbness, hypokinesia, parosmia, dysgraphia,convulsions
Changes in the organ of vision
Frequent	Blurred vision, diplopia
Infrequent	Loss of peripheral vision, blurred vision, swollen eyes, visual field defect, decreased visual acuity, eye pain, asthenopia, photopsia, dry eye syndrome, increased tearing, irritation of the mucous membrane of the eyes
Rare	Oscillopsia (subjective sensation of vibration of the objects in question), changes in the depth of visual perception, mydriasis, strabismus, increased brightness of visual perception,keratitis, vision loss
Changes in the organ of hearing and vestibular apparatus
Frequent	Vertigo
Infrequent	Hyperacusis
From the cardiovascular system
Infrequent	Tachycardia, first degree atrioventricular block, sinus bradycardia,chronic heart failure
Rare	Sinus tachycardia, sinus arrhythmia,interval extensionQ T
Vascular disorders
Infrequent	Hypotension, hypertension, skin flushing, hot flashes, cold extremities
From the respiratory system
	Dry nasal mucosa
Infrequent	Shortness of breath, nosebleeds, cough, nasal congestion, rhinitis, snoring
	Feeling of tightness in the throat, pulmonary edema
From the digestive system
	Dry mouth, constipation, vomiting, flatulence, bloating, nausea, diarrhea
Infrequent	Increased salivation, gastroesophageal reflux, hypoesthesia of the oral mucosa
	Ascites, dysphagia, pancreatitis, tongue swelling
From the skin and subcutaneous tissues
Infrequent	Increased sweating, papular rash, urticaria, facial swelling, skin itching
	Cold sweat, Stevens-Johnson syndrome
From the musculoskeletal system
	Muscle cramps, arthralgia, back pain, pain in limbs, muscle spasm of the cervical spine
Infrequent	Joint swelling, myalgia, muscle cramp, neck pain, muscle stiffness
	Rhabdomyolysis
From the urinary system
Infrequent	Dysuria, urinary incontinence
	Oliguria, renal failure, urinary retention
From the reproductive system
	Erectile dysfunction, pain in the mammary glands
Infrequent	Delayed ejaculation, sexual dysfunction, dysmenorrhea
	Amenorrhea, breast discharge, breast enlargement, gynecomastia
General and administration site disorders
	Fatigue, peripheral edema, feeling of intoxication, gait disturbance, feeling unwell, falling
Infrequent	Chest tightness, thirst, chills, pain, fever, general weakness, generalized edema, malaise
Immune system disorders
Infrequent
	Angioedema
Laboratory and instrumental data
	Increased body weight, increased creatinine concentration in the blood
Infrequent	Increased activity of alanine aminotransferase, creatine phosphokinase, aspartate aminotransferase, decreased platelet count, increased blood glucose concentration, decreased potassium content in the blood, decreased body weight
	Decrease in the number of leukocytes in the blood

If any of the side effects indicated in the instructions get worse or you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

With an overdose of the drug (up to 15 g), no other (not described above) adverse reactions were recorded. During post-marketing use, the most common adverse events that developed with pregabalin overdose were: mood disorders, drowsiness, confusion, depression, agitation and anxiety. In rare cases, cases of coma have been reported.

Treatment: gastric lavage, supportive treatment and, if necessary, hemodialysis are performed (see section “Dosage and administration”, Table 1).

Interaction:

Pregabalin is excreted by the kidneys mainly unchanged, undergoes minimal metabolism in humans (less than 2% of the dose is excreted by the kidneys in the form of metabolites), does not inhibit the metabolism of other drugs in vitro and does not bind to plasma proteins, so it is unlikely to enter into pharmacokinetic interactions.

Study invivo and population pharmacokinetic analysis

There was no evidence of clinically significant pharmacokinetic interactions between pregabalin and phenytoin, carbamazepine, valproic acid, lamotrigine, gabapentin, lorazepam, oxycodone and ethanol.

It has been established that oral hypoglycemic agents, diuretics, insulin, and tiagabine do not have a clinically significant effect on the clearance of pregabalin.

Oral contraceptives, and/or

When oral contraceptives containing and/or were used simultaneously with pregabalin, the equilibrium pharmacokinetics of both drugs did not change.

Drugs affecting the central nervous system

Cases of respiratory failure and coma have been reported when pregabalin was used concomitantly with other drugs that depress the central nervous system.

Repeated oral administration of pregabalin with oxycodone, lorazepam, or ethanol did not have a clinically significant effect on breathing. appears to enhance cognitive and motor impairment caused by oxycodone. may enhance the effects of ethanol and lorazepam.

Effect on the gastrointestinal tract

Pregabalin has also been reported to have negative effects on the gastrointestinal tract (including ileus, paralytic ileus, constipation) when used concomitantly with drugs that cause constipation (such as opioids) (see Precautions).

Drug interactions when used at elderly patients

Specific studies of pharmacodynamic interactions with other drugs in elderly patients have not been conducted.

Special instructions:

Patients with diabetes mellitus

In some patients with diabetes mellitus, in case of weight gain during treatment with pregabalin, dose adjustment of hypoglycemic agents may be required.

Hypersensitivity reactions

Pregabalin should be discontinued if symptoms of angioedema (such as facial swelling, perioral edema or upper respiratory tract swelling) develop.

Suicidal thoughts and behavior

Antiepileptic drugs, including, may increase the risk of suicidal thoughts or behavior. Therefore, patients receiving these drugs should be closely monitored for new or worsening depression or suicidal thoughts or behavior.

Decreased gastrointestinal function

When using pregabalin and opioids concomitantly, consider the need for preventive measures to prevent the development of constipation (especially in older women)

Dizziness, drowsiness, loss of consciousness, confusion and cognitive impairment

Pregabalin treatment has been associated with dizziness and drowsiness, which increase the risk of accidental injury (falls) in older adults. During post-marketing use of the drug, cases of loss of consciousness, confusion and cognitive impairment have also been reported. Therefore, until patients appreciate the possible effects of the drug, they should exercise caution.

Discontinuation of concomitant anticonvulsant therapy

Information on the possibility of discontinuing other anticonvulsants when seizures are suppressed with pregabalin and the advisability of monotherapy with this drug is insufficient. There are reports of the development of seizures, including status epilepticus and petit mal seizures, during the use of pregabalin or immediately after the end of therapy.

Effect of pregabalin on vision

In clinical studies, patients receiving chronic treatment experienced a side effect such as blurred vision more often than patients receiving placebo. However, this side effect ceased as treatment continued.

In clinical studies during which patients were ophthalmologically examined, decreased visual acuity and changes in visual fields were observed more often in patients receiving than in patients receiving placebo. The incidence of fundus changes was higher in patients receiving placebo.

Although the clinical significance of these abnormalities has not been established, patients should report changes in vision during pregabalin therapy to their physician. If symptoms of visual impairment persist, monitoring should be continued. More frequent vision screenings should be performed in patients who are already seen regularly by an ophthalmologist. If adverse reactions such as loss of vision, blurred vision or other visual disturbances occur in response to the use of pregabalin, discontinuation of the drug may lead to the disappearance of these symptoms.

Kidney failure

There have also been cases of renal failure; in some cases, renal function was restored after discontinuation of pregabalin.

Pregabalin withdrawal symptoms

The following adverse events have been observed following discontinuation of pregabalin after long-term or short-term therapy: insomnia, headache, nausea, diarrhea, flu-like syndrome, depression, sweating, dizziness, convulsions and anxiety. Available data suggest that the incidence and severity of withdrawal symptoms may depend on the dose of pregabalin.

Pregabalin abuse

There is no evidence that it is active at receptors associated with the development of drug abuse by patients. During post-marketing studies, cases of abuse of pregabalin have been reported. As with any drug that affects the central nervous system, the patient's medical history should be carefully assessed for any history of drug abuse and the patient should be monitored for potential dosage irregularities or abuse of pregabalin (eg, development of resistance to pregabalin therapy, unreasonable increase in the dose of the drug, additive behavior of the patient).

Congestive heart failure

Although there has been no apparent association between pregabalin use and the development of heart failure, chronic heart failure has been reported in some patients during post-marketing use of the drug during pregabalin therapy. In patients without clinically significant signs of heart or vascular disease, there was no association between peripheral edema and cardiovascular complications, such as increased blood pressure or chronic heart failure. These reactions were predominantly observed in elderly patients who suffered from impaired cardiac function and received the drug for neuropathy. Therefore, it should be used with caution in this category of patients. After discontinuation of pregabalin, the manifestations of such reactions may disappear.

Treatment of central neuropathic pain associated with spinal cord injury

The incidence of adverse events from the central nervous system, especially somnolence, increases during the treatment of central neuropathic pain due to spinal cord damage, which, however, may be a consequence of the additive effects of pregabalin and other concomitantly taken drugs (for example, antispasticity). This circumstance should be taken into account when prescribing pregabalin for this indication.

Encephalopathy

Cases of encephalopathy have been reported, especially in patients with concomitant diseases that may lead to the development of this condition.

Impact on the ability to drive vehicles. Wed and fur.:

Pregabalin may cause dizziness and drowsiness and, accordingly, affect the ability to drive a car and use complex equipment. Patients should not drive a car, use complex machinery, or perform other potentially hazardous activities until it is clear whether this drug affects their performance of such tasks.

Release form/dosage:

Capsules, 75 mg, 150 mg and 300 mg.

Package:

14 capsules in a blister pack made of polyvinyl chloride film and aluminum foil; 1, 2 or 4 blister packs in a cardboard box along with instructions for medical use.

Storage conditions:

Store at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Best before date:

Do not use after the expiration date stated on the package.

Conditions for dispensing from pharmacies: On prescription Registration number: LP-003308 Registration date: 11.11.2015 Expiration date: 11.11.2020 Owner of the Registration Certificate: GEROPHARM, LLC Russia Manufacturer: Information update date: 16.12.2016 Illustrated instructions

This is a rather unpleasant sight. And a person cannot control the regularity of seizures or where and when they occur. All these are individual characteristics of the disease. It requires close attention from doctors and treatment. There is an excellent and popular drug among doctors called Pregabalin Richter. If you couldn’t find it at the pharmacy, the specialist will recommend analogues (generics).

Composition of the medicine and packaging

During illness, you need to take the medicine for two weeks, 2 capsules per day, and for a week, 3 capsules. This will not affect your health or cause side effects. Prescribed for epilepsy. The therapeutic effect is already observed after the first week of taking 2 capsules per day. During treatment, you should drink the product for 10 days, 1 capsule per day. Pregabalin Richter capsules have such indications for use. Analogues of the drug, like the drug itself, are prescribed by a highly specialized doctor - a neurologist.

The effect of the medicine and its dosage

After ingestion, the drug is quickly absorbed. It is recommended to take it on an empty stomach. After an hour, the drug already enters the plasma. Never combines with protein in the blood. It is excreted almost unchanged by the kidneys. Prescribed orally from 150 mg to 600 mg 2 or 3 times a day. Taking the drug does not depend on food intake. For neuropathic pain, take no more than 150 mg per day. If no side effects occur and the condition begins to improve, then you can increase the dosage to 300 mg after a week. And after a few more days, the drug Pregabalin can be taken at a dosage of 600 mg per day. Analogues, instructions for use, daily dosage - everything should be checked with your doctor before starting therapy.

The same regimen is used to prescribe medication during epilepsy attacks. For fibromyalgia, take the initial dose: 75 mg 2 times a day. Over the next few days, the dosage is gradually increased. The highest dose per dose will be 600 mg per day. A generalized state of anxiety requires the administration of the drug at a dosage of 150 mg once a day. The increase is also made with each subsequent week and reaches 600 mg per day. You cannot immediately stop taking the capsules, otherwise it may develop. You must do this for a week, reducing the dosage each time. The analogue can be taken according to the same scheme.

Overdose of Pregabalin Richter capsules

According to statistical data, during treatment with Pregabalin and generics, an overdose most often manifests itself in drowsiness and confusion. Treatment consists of additional symptomatic therapy. In some cases, gastric lavage is necessary.

The drug must be taken strictly according to the schedule. If the patient forgot to take the medicine, then double dosage is not recommended. Any analogue of Pregabalin has a similar dosage regimen.

Interaction with other drugs

The drug almost does not react with other drugs. It is excreted by the kidneys. Does not bind to blood proteins. It has also not been established that when treated with hypoglycemic drugs, diuretics, insulin, phenobarbital, the properties of the capsules may decrease.

When using contraceptives and other drugs that contain estrogens, the active ingredients do not interact with Pregabalin Richter capsules. Analogues can also be used in conjunction with birth control pills.

Capsules that are taken together with medications against diarrhea have a negative effect on the functioning of the gastrointestinal tract. It is not recommended for use in people who suffer from intestinal obstruction.

Side effects

The medicine in most cases causes drowsiness and dizziness. But such symptoms are moderate and do not actually bother the patient. In rare cases, nasopharyngitis, leukopenia, metabolic disorders, and hypoglycemia may develop.

Some patients experience insomnia, confusion, depression, euphoria and many other pathological processes that disappear after treatment. The cardiovascular system may react to taking the medication with tachycardia and surges in blood pressure. Redness of the skin may also be observed.

The Pregabalin analogue has similar side effects. Possible unpleasant symptoms should be studied before starting treatment.

Indications for use

The drug Pregabalin is prescribed for neuropathic pain in adults. During epilepsy, the drug is taken in combination with other medications. The medicine will help reduce the number of seizures and further reduce them to “no”. Also, Pregabalin may be prescribed for the treatment of anxiety and fibromyalgia. Side effects develop if the medication is not taken as directed. The patient should strictly adhere to the dosage, and also study the “drug interactions” section.

Contraindications to taking the drug

Rare cases of hereditary diseases associated with the inability to digest lactose or galactose are a serious contraindication to taking Pregabalin or its analogues. The drug is not prescribed to minor patients. The medicine is also contraindicated during pregnancy and lactation. Even if you are planning to conceive, you should not use Pregabalin. Side effects may affect the development of the unborn child.

If you have hypersensitivity to the main substance of the capsules or its additional components, you cannot use Pregabalin. The ban also applies to generics. Under the supervision of a doctor, it can be used for renal and liver failure, as well as if the patient has a drug dependence syndrome. Elderly patients should also take Pregabalin with caution. Generic analogues have identical contraindications

It is not always possible to find the right drug at the pharmacy. A qualified specialist will always be able to recommend a high-quality substitute. The most popular generics will be presented below.

Lyrica capsules

Anticonvulsant drug. An analogue of Lyrica, Pregabalin, is not always available. And this medicine is available in almost every pharmacy.

The main substance in the capsules is pregabalin. Additionally, Lyrica uses components such as lactose monohydrate, corn starch, and talc.

The dosage is 150-600 mg per day. The daily norm is divided into two doses. Do not use in children, as well as in patients with liver and heart failure. Which doctor can recommend an analogue of Lyrica? Pregabalin and other drugs with similar effects are prescribed exclusively by a neurologist.

Algerica capsules

As in the previous case, the main active component of the drug is pregabalin. Additionally, mannitol and corn starch are used. This analogue of "Pregabalin" is used as part of complex therapy for epilepsy. The medicine cannot be prescribed during pregnancy and lactation. There are also age restrictions. Capsules are not prescribed to minor patients.

"Pregabalin", "Gabapentin", "Lyrica", "Algerica" - these are all medications that have a similar composition. The effect on the body is also no different. It is worth using the drug that is available at the nearest pharmacy, but only as prescribed by a doctor.

An effective pharmaceutical drug with anticonvulsant activity is the drug “Pregabalin”. The instructions for use indicate that the tablets have proven themselves to be an effective assistant in the complex pharmacotherapy of various pathologies accompanied by a failure of the innervation of striated skeletal muscles. Why Pregabalin is prescribed, prices, reviews from patients and doctors, as well as analogues of the drug will also be discussed in the article.

What is the composition

The manufacturer, in the detailed instructions attached to each package of medication, indicates that the main active ingredient is pregabalin itself. The severity of the medicinal effect is directly determined by its volume in each capsule.

Lactose monohydrate and corn starch, as well as talc and titanium dioxide with gelatin are auxiliary components, the purpose of whose presence in the composition of the drug is to maintain the pharmacological effect of the main component.

Release form

On pharmacy shelves, the medication “Pregabalin”, the instructions for use explain this, is presented as a dosage form of capsules (tablets) taken orally. Each capsule has a cap with a yellowish or brownish tint. Medicinal components are placed inside in the form of crystalline fine powder.

Packaging of the medicine is 14 pcs. A consumer pack can contain from one to four blisters.

Pharmacological effects

Since the main substance of the drug Pregabalin is a structural analogue of gamma-aminobutyric acid, it is inherent in it to have the same pharmacological effects due to the ability to inhibit the release of mediators from CNS structures.

Pharmacological effects:

suppressive effect on specific calcium channels of neurocytes;
a pronounced decrease in the intensity of pain;
anticonvulsant effect on striated muscles.

After the capsules enter the intestines, the active substance is absorbed into the bloodstream, followed by the formation of a systemic effect. At the same time, Pregabalin is not metabolized; it is excreted by the kidneys in the urine.

Pregabalin tablets: what does the drug help with?

Experts prescribe an anticonvulsant and analgesic for pathologies accompanied by a failure of innervation from the central nervous system:

neuropathic form of pain syndrome:
generalized anxiety disorders;
fibromyalgia;
epileptic activity.

Why is Pregabalin still prescribed? In some cases, the drug acts as an additional component of pharmacotherapy, for example, in the absence of pronounced positive dynamics while taking other drugs.

Contraindications

Most pharmaceutical drugs have a certain list of restrictions on their use, especially the subgroup of anticonvulsants. The manufacturer's instructions for Pregabalin indicate the following contraindications:

individual hyperreaction to the components of the medication;
rare hereditary pathologies - for example, congenital galactose intolerance;
lactose deficiency;
pediatric category of patients.

The drug should be taken with extreme caution if a person has a disruption in activity or decompensated heart failure. Allergic reaction to subgroups of medications similar to anticonvulsants.

Instructions for use

Pregabalin is intended exclusively for oral administration. Capsules can be taken regardless of diet. As a rule, 150–600 mg/day is sufficient, divided into 2–3 doses.

Optimal doses for adults are indicated according to the severity of negative symptoms of diseases:

for the neuropathic form of pain impulses, the starting dose is 150 mg, but if this is not enough, after 5–7 days the dose is increased to 300 mg, then to 600 mg/day;
in case of increased readiness for epileptic attacks, the drug administration regimen is similar to the above - 150 mg / 300 mg / 600 mg / day;
for fibromyalgia, it is recommended to take the drug 75 mg every morning and evening, subsequently, in the absence of positive dynamics - 150 mg 2 times / day, the maximum dose is 600 mg / day;
generalized anxiety disorder can be corrected by taking 150 mg of the active substance pregabalin, however, it is permissible to increase the dose to 300 mg/day, according to individual needs - up to 600 mg/day.

Against the background of pharmacotherapy with medication, a specialist will evaluate the severity of negative symptoms and the advisability of taking capsules. If you stop taking the drug, a dosage reduction regimen is selected by the attending physician - at least 5-7 days.

Undesirable effects

Since the mechanism for providing the pharmacological effects of the drug is interconnected with the activity of the central nervous system structures, various undesirable effects may occur while taking the capsules:

It is recommended to notify a specialist about each case of deterioration in health while taking capsules with the substance pregabalin. They will undergo correction of therapeutic doses of the drug.

Analogs of the drug "Pregabalin"

Complete analogues for the active element:

Lyrics.
Algerica.
Pregabalin Zentiva (Canon, Richter, SZ).
Prabegin.
Prigabilon.
Pregabio.

Antiepileptic drugs include:

Neurontin.
Galodif.
Valparin.
Fycompa.
Misolin.
Acetazolamide.
Gapentek.
Convulsofin.
Inovelon.
Carbamazepine.
Trileptal.
Chlorakon.
Topiramate.
Lamitor.
Zonegran.
Diacarb.
Gabagamma.
Lamotrigine.
Benzonal.
Suxilep.
Levetiracetam.
Tegretol.
Depakine.
Convulsion.
Relium.
Sabril.
Phenobarbital.
Diazepam.
Convulex.
Gabapentin.
Encorat.
Difenin.
Topamax.
Primidon.
Exalief.
Epitope.
Finlepsin retard.
Lamolep.
Mazepin.
Finlepsin.
Sibazon.
Eplirontin.
Gabitril.
Hexamidine.
Valproic acid Sandoz.
Vimpat.
Sodium valproate.
Rivotril.
Carbapin.
Karbasan retard.
Epimax.
Topsaver.
Depakine chrono.
Pagluferal.
Benzobarbital.
Lameptil.
Clonazepam.
Actinerval.

Price and holiday conditions

The average price of Pregabalin capsules (Moscow) is 445 rubles. You can buy medicine in Minsk for 15 – 27 bel. rubles The price in Kyiv is 80 hryvnia, in Kazakhstan – 150 tenge. Sold according to prescription.