Active substancePregabalinPregabalin
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  • Dosage form: & nbspcapsules
    Composition:

    1 capsule contains:

    active substance: pregabalin 25.0 mg / 50.0 mg / 75.0 mg / 150.0 mg / 300.0 mg;

    Excipients: mannitol 43.0 mg / 86.0 mg / 10.0 mg / 20.0 mg / 40.0 mg, corn pregelatinized starch 7.0 mg / 14.0 mg / 7.0 mg / 14.0 mg / 28.0 mg, talc 9.0 mg / 18.0 mg / 8.0 mg / 16.0 mg / 32.0 mg.

    Capsule shell:

    Capsules № 3 "7622 / TEVA" (dosage of 25 mg) 48.0 mg: cap - titanium dioxide 2.0%, iron oxide dye yellow 0.1%, gelatin up to 100%; housing - titanium dioxide 2.0%, iron oxide dye yellow 0.1%, gelatin up to 100%.

    Capsules number 2 "7623 /TEVA" (dosage of 50 mg) 61.0 mg: cap - titanadioxide 2.0%, iron dye oxide yellow 0.1%, gelatin up to 100%; housing - titanium dioxide 2.0%, iron oxide dye yellow 0.1%, gelatin up to 100%.

    Capsules number 3 "7624 /TEVA" (dosage: 75 mg) 48.0 mg: cap - titanium dioxide 2,1747%, iron dye oxide red 0.6996%, gelatin up to 100%; housing - titanium dioxide 2.0%, iron oxide dye yellow 0.1%, gelatin up to 100%.

    Capsules number 2 "7626 /TEVA" (dosage of 150 mg) 61.0 mg: cap - titanium dioxide 2.0%, iron oxide dye yellow 0.1%, gelatin up to 100%; housing - titanium dioxide 2.0%, iron oxide dye yellow 0.1%, gelatin up to 100%.

    Capsules № 0 "7621 /TEVA" (dosage of 300 mg) 96.0 mg: cap - titanium dioxide 2,1747%, iron dye oxide red 0.6996%, gelatin up to 100%; housing - titanium dioxide 2.0%, iron oxide dye yellow 0.1%, gelatin up to 100%.

    Inks used for labeling capsules include the following components: glaze pharmaceutical [shellac solution in ethanol] 59.420%, iron dye oxide black 24.650%, butanol * 9.750%, water purified * 3.249%, propylene glycol 1.300%, isopropanol * 0.550%, ethanol * 1.080%, ammonia water * 0.001%.

    * - components that are deleted in the process application to the capsule.

    Description:

    Dosage of 25 mg. Opaque capsules of light yellow color with a black print "TEVA"on the lid and" 7622 "on the body.

    Dosage 50 mg. Opaque capsules of light yellow color with a black print "TEVA"and a radial black stripe on the lid and a black seal" 7623 "and a radial black stripe on the body.

    Dosage of 75 mg. Opaque capsules: pink lid with black print "TEVA"and a body of light yellow color with a black print" 7624 ".

    Dosage of 150 mg. Opaque capsules of light yellow color with a black print "TEVA"on the lid and" 7626 "on the body.

    Dosage of 300 mg. Opaque capsules: pink lid with black print "TEVA"and a body of light yellow color with a black print" 7621 ".

    Contents of capsules: white or almost white granular and partially compressed powder (for all dosages).

    Pharmacotherapeutic group:antiepileptic agent
    ATX: & nbsp

    N.03.A.X.16   Pregabalin

    Pharmacodynamics:

    Pregabalin alkylated analog of gamma-aminobutyric acid (GABA) - (S) -3 (aminomethyl) -5-methylhexanoic acid - has antiepileptic and anticonvulsant activity.

    However, despite the structural similarity of molecules, pregabalinum does not possess the activity inherent in GABA. Pregabalin has no direct or indirect GABA-ergic effect. The mechanism of action of pregabalin is based on its ability to bind to additional subunits (alpha2-delta protein) of voltage-gated neuronal calcium channels (calcium channels N- and P / O-type), resulting in marked reduction in the calcium transport in neuronal cells in response to the action potential. Pregabalin has a high affinity for alpha2-delta protein found in the tissues of the central nervous system (CNS). Use of pregabalin reduces the neurotransmitter release pain (including glutamate, noradrenaline, and substance P) in the synaptic cleft when excited neurons. Due to such changes, the pulse is selectively suppressed by the action of pregabalin. It should be noted that pregabalinum suppresses the excitability of the network of neurons only in pathological conditions.

    Pharmacokinetics:

    The pharmacokinetics of pregabalin in the range of recommended daily doses is linear.

    Interindividual variability is low (less than 20%). The pharmacokinetics of pregabalin after single dose administration corresponds to pharmacokineticspregabalinum at repeated application, therefore there is no necessity in the regular control of concentration pregabalinum.

    Suction

    After oral administration on an empty stomach pregabalinum OK absorbed in the gastrointestinal tract (GIT), the maximum concentration (CmOh) pregabalinum in a blood plasma it is noted in 1 hour at single reception. Upon repeated admission, the time to reach the maximum plasma concentration (TmOh) pregabalin does not change.

    Bioavailability of pregabalin does not depend on the dose taken and is not less than 90%. With repeated administration of pregabalin, equilibrium concentrations are reached within 24-48 hours.

    Eating lowers the speed and degree of absorption of pregabalin. So while taking pregabalin with food TmOh increases approximately 2.5 hours, and CmOh Pregabalin decreases by 25-30% (in comparison with the data obtained after taking pregabalin on an empty stomach). It should be noted that eating is not has a clinically significant effect on the absorption of pregabalin.

    Distribution and Metabolism

    Apparent volume of distribution Pregabalinum after ingestion is approximately 0.56 l / kg.For pregabalin, binding to plasma proteins is not characteristic. Pregabalin well penetrates through blood-brain and hematoplacental barriers, and also excreted in breast milk.

    Metabolism

    Pregabalinum is practically not exposed to a metabolism.

    An insignificant part of pregabalin (less than 1% of the dose) is metabolized with formation N-methylated a compound that is the main metabolite and is excreted by the kidneys. Signs of racemization Senantiomer of pregabalin in R-enantiomer was not detected.

    Excretion

    Pregabalin is excreted mainly by the kidneys in unchanged form. The average half-life is 6.3 hours. The clearance of pregabalin from the plasma and the kidney clearance are directly proportional to the creatinine clearance (CC).

    In patients with impaired renal function the decrease in clearance of pregabalin is directly proportional to the decrease in QC. Patients on hemodialysis after 4 hours from the blood plasma are excreted about 50% of the dose.

    In patients with impaired function liver. Disturbance of liver function does not significantly affect the pharmacokinetics of pregabalin.

    In elderly patients (over 65 years of age) there is a downward trend in QC associated with age. Clearance of pregabalin decreases in accordance with QC, therefore dose adjustment is possible.

    Indications:

    - Neuropathic pain in adults;

    - additional epilepsy therapy with partial convulsive seizures (accompanied or unaccompanied secondary generalization) in adults;

    - generalized anxiety disorders in adults;

    - fibromyalgia in adults.

    Contraindications:

    - Hypersensitivity to pregabalin or any of the components of the drug;

    - children's age till 18 years;

    - Pregnancy;

    - the period of breastfeeding.

    Carefully:

    - Impaired renal function;

    - simultaneous use with lorazepam, ethanol, oxycodone;

    - elderly patients (over 65 years);

    - heart failure;

    - drug dependence in history, encephalopathy in the anamnesis;

    - diabetes.

    Pregnancy and lactation:

    When using Algeric, women of reproductive age should use effective methods of contraception.

    There is no reliable data on the efficacy and safety of pregabalin in pregnancy.In this regard, the use of Algeric during pregnancy is contraindicated.

    There is no information about the excretion of pregabalin with breast milk in women. However, in experimental studies it has been established that pregabalinum is excreted in breast milk in rats. In this regard, during treatment with Algerica, breastfeeding is recommended to be suspended.

    Dosing and Administration:

    Inside, regardless of food intake, in a daily dose of 150 to 600 mg, dividing into 2 or 3 admission.

    Capsules are recommended to be swallowed whole, without chewing or grinding, with plenty of water. The duration of treatment and the dose of Algeric is determined by the attending physician individually for each patient, depending on the nature of the disease and individual characteristics of the patient.

    Neuropathic pain

    The initial dose of 150 mg per day, divided into 2 or 3 admission.

    Depending on the individual response to treatment and individual patient tolerance after 3-7 days, the dose may be increased to 300 mg per day, and if necessary, after 7 days the dose can be increased to 600 mg per day. The maximum daily dose of 600 mg / day.

    Additional epilepsy therapy with partial convulsive seizures (accompanied or not accompanied by secondary generalization)

    The initial dose of 150 mg per day, divided into 2 or 3 admission.

    Depending on the individual response to treatment and individual patient tolerance after 7 days, the dose can be increased to 300 mg per day, and if necessary, after 7 days the dose can be increased to 600 mg per day. The maximum daily dose of 600 mg / day.

    Generalized disturbing disorders

    The initial dose of 150 mg per day, divided into 2 or 3 admission.

    Depending on the individual response to treatment and individual patient tolerance after 7 days, the dose may be increased to 300 mg per day. In the absence of positive dynamics after 7 days, the dose is increased to 450 mg per day, if necessary, after 7 days to 600 mg / day. The maximum daily dose of 600 mg / day.

    Fibromyalgia

    The initial dose of 150 mg per day, divided into 2 or 3 admission.

    Depending on the individual response to treatment and individual patient tolerance after 7 days, the dose may be increased to 300 mg per day. In the absence of positive dynamics after 7 days, the dose increase to 450 mg per day, and if necessary, after 7 days, the dose can be increased to 600 mg per day. The maximum daily dose of 600 mg / day.

    If it is necessary to stop treatment, it is recommended that the Algeric preparation be withdrawn gradually for a minimum of 1 week.

    Patients with impaired renal function

    The dose of the Algeric preparation is selected individually, taking into account the QC (see Table 1).

    The QC is calculated by the following formula:

    For men:

    CK (ml / min) = (body weight in kg) x (140 - age in years) / 72 x concentration of creatinine in plasma (mg / dl)

    For women:

    KK (ml / min) = KK for males x 0.85

    In patients on hemodialysis, daily dose Pregabalin is selected taking into account the kidney function (see the section "Pharmacokinetics"). Immediately after each 4-hour hemodialysis session, an additional dose is used (Table 1).

    Table 1. Selection of a dose of the Algeric medication taking into account the function of the kidneys

    Daily dose

    Algeric

    KK

    (ml / min)

    Multiplicity

    reception per day

    Initial

    dose

    (mg / day)

    Maximum

    dose

    (mg / day)

    More than 60

    150

    600

    2 or 3

    30 to 60

    75

    300

    2 or 3

    15 to 29

    25-50

    150

    1 or 2

    Less than 15

    25

    75

    1

    Additional dose after dialysis (mg)

    25

    100

    once

    In patients with impaired liver function correction of the dose is not required (see the section "Pharmacokinetics").

    Patients elderly (over 65 years) may require a reduction in the dose of pregabalin due to a decrease in renal function (see section "Pharmacokinetics").

    If you miss a dose of Algeric, take the next dose as soon as possible, but do not take the missed dose if the next time is already appropriate
    Side effects:

    The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely (including isolated cases) - less than 0.01%.

    Infectious diseases: infrequently - nasopharyngitis.

    On the part of the blood and lymphatic system: rarely - neutropenia, leukopenia, thrombocytopenia.

    From the side of metabolism and nutrition: often - increased appetite, weight gain; infrequently - anorexia, hypoglycemia, hyperglycemia; rarely - weight loss.

    From the nervous system: very often - dizziness, drowsiness; often - euphoria, confusion, decreased libido, irritability, insomnia, disorientation,ataxia, impaired attention, impaired coordination, memory impairment, tremor, paresthesia, imbalance, amnesia, sedation, lethargy; infrequent - depersonalization, anorgasmia, anxiety, depression, agitation, mood lability, increased insomnia, depressed mood, difficulty in word selection, hallucinations, nightmarish dreams, increased libido, panic attacks, apathy, cognitive disorders, hypoesthesia, nystagmus, speech impairment , myoclonic spasms, weakening of reflexes, dyskinesia, psychomotor agitation, postural dizziness, hyperesthesia, loss of taste sensations, burning sensation on the mucous membranes and skin, intentional tremor, stu op, fainting; rarely - disinhibition, elevated mood, hypokinesia, parosmia, dysgraphia.

    From the side of the organ of vision: often - blurred vision, diplopia; infrequent - visual impairment, narrowing of visual fields, reduced visual acuity, eye pain, asthenopia, as well as dry eyes, puffiness of the eyes, increased lacrimation; rarely - flashing of "sparks" before the eyes, eye irritation, mydriasis,Oscilloscopy (subjective sensation of fluctuations in the subjects under consideration), impaired perception of the depth of vision, loss of peripheral vision, strabismus, increased brightness of visual perception.

    From the side of the hearing organ and labyrinthine disorders: often - vertigo; rarely - overexercise.

    From the cardiovascular system: infrequently - "hot flashes", skin hyperemia, lowering blood pressure (BP), increasing blood pressure, tachycardia, atrioventricular blockade of the I degree; rarely - sinus tachycardia, sinus bradycardia, sinus arrhythmia.

    On the part of the respiratory system, the organs of the thorax and the mediastinum: infrequently - shortness of breath, dryness of the mucous membrane of the nasal cavity; rarely - nasal congestion, epistaxis, rhinitis, snoring, a feeling of "restraint" in the throat.

    From the digestive system: often - dryness of the oral mucosa, bloating, vomiting, constipation, flatulence; infrequently - increased salivation, gastroesophageal reflux, hypoesthesia of the oral mucosa; rarely - ascites, dysphagia, pancreatitis.

    From the skin and subcutaneous tissues: infrequently - papular rash, sweating; rarely - cold sweat, hives.

    From the side of the kidneys and urinary tract: infrequently - dysuria, urinary incontinence; rarely - oliguria, renal insufficiency.

    From the musculoskeletal system and connective tissue: infrequently - muscle twitching, joint swelling, stiffness of muscles, muscle spasms, myalgia, arthralgia, back pain, pain in the limbs; rarely - spasm of the neck muscles, pain in the neck, rhabdomyolysis.

    From the side of the reproductive system: often - erectile dysfunction; infrequently - sexual dysfunction, ejaculation delay; rarely - amenorrhea, pain in the mammary glands, enlargement of mammary glands in the volume, dysmenorrhea, discharge from the mammary glands.

    Other: often - fatigue, swelling, including peripheral, feeling of "intoxication", violation of gait; infrequently - asthenia, falls, thirst, a feeling of "restraint" in the chest, generalized edema, chills, pain; rare - hyperthermia.

    Laboratory and instrumental data: infrequently - increased activity alanine aminotransferase, aspartate aminotransferase, creatine phosphokinase; rarely - hypercreatininaemia, hypokalemia.

    Side Effects in Post-Marketing Surveillance

    The following adverse reactions were identified during the practical use of pregabalin.Since these messages were received from patients, it was not always possible to assess their frequency or to establish a causal relationship with taking pregabalin.

    From the nervous system: frequency unknown - headache, loss of consciousness, cognitive impairment.

    From the side of the organ of vision: frequency unknown - loss of vision.

    From the digestive system: rarely - swelling of the tongue, nausea, diarrhea.

    From the skin and subcutaneous tissues: rarely - edema of the face, itchy skin.

    Allergic reactions: frequency unknown - hypersensitivity reaction, allergic reaction, angioedema, Stevens-Johnson syndrome.

    From the side of the cardiovascular system: frequency unknown - chronic heart failure, QT interval elongation.

    From the urinary system: frequency unknown - urinary retention.

    From the respiratory system: frequency unknown - pulmonary edema.

    Overdose:

    Symptoms: overdose data are limited. A random dose of 8 g of pregabalin was reported during a clinical trial, which was not accompanied by any significant clinical manifestations.

    Treatment: gastric lavage, reception of activated charcoal, symptomatic therapy, hemodialysis should be applied if necessary.

    Interaction:

    Because the pregabalinum mainly excreted unchanged in kidneys and only slightly metabolized in the human body (less than 1% of the administered dose is excreted by the kidneys in the form of metabolites), does not inhibit in vitro metabolism of other drugs and does not bind to blood proteins, it is unlikely that pregabalinum can enter into pharmacokinetic interaction with other or be the object of such interaction.

    With simultaneous application, there is no significant clinical pharmacokinetic interaction between pregabalin and phenytoin, carbamazepine, valproic acid, lamotrigine, gabapentin, lorazepam, oxycodone or ethanol.

    The presented pharmacokinetic analysis showed that oral hypoglycemic agents, diuretics and insulin, as well as phenobarbital, tiagabine and topiramate have no clinically significant effect on the clearance of pregabalin.

    The simultaneous use of pregabalin and oral contraceptives (norethisterone and / or ethinylestradiol) does not affect the pharmacokinetics in the equilibrium state of each of the drugs.

    Multiple oral administration of pregabalin and oxycodone, lorazepam or ethanol does not have a clinically significant effect on respiratory function. Pregabalin increased the impairment of mnestic and basic motor functions caused by oxycodone. Pregabalin may enhance the effects of ethanol and lorazepam.

    With simultaneous use with opioid analgesics, it is possible to weaken the function of the lower parts of the digestive tract, including constipation, intestinal obstruction (see section "Special instructions").

    Special instructions:

    In some patients with diabetes mellitus, in the case of weight gain on the background of Algeric treatment, dosage adjustment of hypoglycemic drugs may be required.

    In the course of postmarketing studies, there have been cases of development of hypersensitivity reactions, including angioedema. In case of symptoms of angioedema, therapy with Algeric should be stopped immediately.

    With Algeric's treatment, visual organ impairments can occur, such as reduced visual acuity, loss of vision, which in most cases go away on their own, both during treatment and when pregabalin is withdrawn.

    There were reported cases of development of renal failure, which was reversible after the abolition of pregabalin therapy.

    Before starting therapy, the patient should be informed of the possible development of withdrawal syndrome after discontinuation of treatment with Algeric. Data on the incidence and severity of withdrawal symptoms depending on the dose and duration of treatment with pregabalin is not enough.

    During treatment with Algeric or immediately after its withdrawal, the appearance of convulsive seizures by type grand mal and the development of epileptic status.

    Treatment with Algeric can be accompanied by dizziness and drowsiness, which can increase the risk of accidental injury (falls) in the elderly. Care should be taken until patients can appreciate the possible effects of Algeric.

    Information on the possibility of canceling other antiepileptic drugs when suppressing seizures with Algeric's drug and the advisability of monotherapy with this drug are not enough.

    Cases of chronic heart failure in elderly patients with cardiovascular diseases were reported in the treatment of pain syndrome with pregabalin neuropathy.

    In the treatment of pain in patients with spine trauma, the risk of unwanted reactions from the CNS, in particular, drowsiness, increases, which may be due to interaction with other drugs, including antispasmodics.

    If suicidal ideation or attempts are made, patients or caregivers should consult a doctor immediately.

    There are reports of the emergence of drug dependence on pregabalin, so patients who have a history of information on the development of dependence on any medications, Algeric should be used with caution.

    There have been reports of cases of encephalopathy in the use of pregabalin, mainly in patients with concomitant conditions that predispose to the development of encephalopathy.

    In case of necessity of simultaneous application with opioid analgesics it is necessary to take measures of prevention of constipation and intestinal obstruction, in particular in elderly patients (see the section "Interaction with other medicinal products").

    Effect on the ability to drive transp. cf. and fur:

    During the treatment with Algeric, it is necessary to refrain from driving vehicles and practicing potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions, due to the fact that it is possible to develop side effects such as dizziness, drowsiness and impaired vision.

    Form release / dosage:

    Capsules, 25, 50, 75, 150 and 300 mg.

    Packaging:

    For 7 capsules in a PVC / aluminum foil blister or PVC / PE / PVDC / PE / PVC / aluminum foil.

    For 2 or 8 blisters together with instructions for use in a cardboard box.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002029
    Date of registration:21.03.2013
    The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
    Manufacturer: & nbsp
    Representation: & nbspTeva Teva Israel
    Information update date: & nbsp27.08.2015
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