Active substanceGabapentinGabapentin
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  • Dosage form: & nbspCapsules 100 mg, 300 mg, 400 mg.
    Composition:Active substance: 100, 300 or 400 mg of gabapentin in each capsule.

    Excipients: lactose monohydrate 14,25 / 42,75 / 57,00 mg, corn starch 13,42 / 40,26 / 53,68 mg, talc 6,58 / 19,74 / 26,32. mg.

    The gelatin capsule composition is 100 mg:
    Cover: dye quinoline yellow (E104) 0.0077 mg, indigocarmine (E132) 0.0048 mg, titanium dioxide (E171) 0.288 mg, gelatin min. 16,1155 mg;
    body: iron dye oxide yellow (E172) 0.0123 mg, titanium dioxide (E171) 0.576 mg, gelatin min. 24.048 mg.
    The gelatin capsule composition is 300 and 400 mg:
    Cover: iron dye oxide yellow (E172) 0.6583 / 0.0922 mg, indigocarmine (E132) 0.1152 / 0.0384 mg, titanium dioxide (E171) 0.384 / 0.96 mg, gelatin min. 31.6745 / 31.7414 mg;
    body: titanium dioxide (E171) 1.152 / 1.152 mg, gelatin min. 48,096 / 48,096 mg.
    Description:
    Capsules 100 mg: hard gelatin capsules with a size of 3 with a light green lid and a white body with a yellowish tinge, containing powder from white to almost white.
    Capsules 300 mg: hard gelatin capsules with a size of 0 with a dark green lid and a white body containing powder from white to almost white.
    Capsules 400 mg: hard gelatin capsules with a size of 0 with a blue-green cover and a white body containing powder from white to almost white.
    Pharmacotherapeutic group:Antiepileptic drug
    ATX: & nbsp

    N.03.A.X.12   Gabapentin

    Pharmacodynamics:
    Gabapentin is structurally related to the neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action is different from the mechanisms of action of some other substances interacting with GABAergic synapses, including valproate, barbiturates, benzodiazepines, inhibitors of GABA transaminases, GABA capture inhibitors, agonists GAMK and predecessors GAMK.
    The binding site of gabapentin has been identified as the alpha2-delta subunit of potentiated calcium channels.
    Gabapentin does not bind to other common receptors of drugs or brain neurotransmitters, including GABA-AA, GABA-AB, benzodiazepine, glutamate, glycine or N-methyl-D-aspartate (NMDA) in clinically usable concentrations.
    Gabapentin does not interact. with sodium channels in vitro, and this is different from phenytoin and carbamazepine. Gabapentin partially reduces the responses to the N-methyl-D-aspartate (NMDA) glutamate agonist in some in vitro test systems, but only at concentrations exceeding 100 μM that are not achieved in vivo. Gabapentin weakly reduces the release of monoamine neurotransmitters in vitro.
    Pharmacokinetics:
    Suction
    After oral administration Cmax gabapentin in plasma is achieved after 2-3 hours. The bioavailability of gabapentin is not proportional to the dose, When the dose is increased, it decreases. Absolute bioavailability at reception, gabapentin in the form of capsules makes about 60%. Simultaneous food intake, incl. with a high fat content, does not affect the pharmacokinetics. Distribution
    Pharmacokinetics does not change with repeated application; Css in plasma can be predicted based on the results of a single dose of the drug. Gabapentin practically does not bind to plasma proteins (<3%), the volume of distribution (Vd) is about 57.7 liters.
    Metabolism
    Metabolism is not affected. Does not induce oxidative liver enzymes with a mixed function involved in the metabolism of drugs. Excretion
    The elimination of gabapentin from the plasma is linear. T1/2 does not depend on the dose and averages 5-7 hours. It is excreted exclusively with urine in unchanged form.
    Pharmacokinetics in special clinical cases
    The pharmacokinetics of gabapentin in children is studied at the age from 1 month to 12 years. It was found that the concentrations of gabapentin in the blood plasma of children older than 5 years are similar to the concentrations achieved in adults when calculating the dose per mg / kg of body weight.
    The clearance of gabapentin from plasma decreases in elderly people and in patients with impaired renal function. The rate of elimination constant, clearance from plasma and renal clearance are directly proportional to the creatinine clearance (CK). Gabapentin is removed from the plasma during hemodialysis. It is recommended that the dose be adjusted to patients with impaired renal function or who are on hemodialysis.
    Indications:Monotherapy of partial seizures in epilepsy with secondary generalization and without it in adults and children over 12 years of age (efficacy and safety of monotherapy in children under 12 years of age have not been established).
    In the combination therapy of partial seizures in epilepsy with secondary generalization and without it in adults and children 3 years and older.
    Treatment of neuropathic pain in adults aged 18 years older (efficacy and safety in patients younger than 18 years of age is not established).
    Contraindications:Hypersensitivity to the components of the drug.
    Children under 3 years.
    Carefully:renal failure, pancreatitis.
    Pregnancy and lactation:
    There is insufficient data on the use of gabapentin in pregnant women. Do not use gabapentin during pregnancy, if the potential benefit to the mother does not exceed the possible risk to the fetus.
    It is impossible to pinpoint whether gabapentin is associated with an increased risk of congenital malformations due to the presence of epilepsy itself and the use of concomitant antiepileptic drugs during pregnancy in all reported cases.
    Gabapentin is secreted with difficult milk. Since its effect on the infant is unknown, caution should be exercised in the case of the administration of gabapentin to a nursing mother.
    Gabapentin can be used during breastfeeding only when the benefits of taking the drug clearly outweigh the risk.
    Dosing and Administration:
    EGYPTENIN Capsules are taken orally, regardless of food intake. The capsule should be swallowed whole, with enough liquid.
    If it is necessary to reduce the dose, cancel the drug or replace it with an alternative remedy, this should be done gradually for at least one week.

    With partial seizures for adults and children over the age of 12, the effective dose is from 900 mg to 3600 mg per day. Therapy can begin with a dose of 300 mg 3 times a day on the first day or increase gradually to 900 mg according to the scheme:
    1 day - 300 mg of the drug once a day;
    Day 2 - 300 mg twice a day;
    Day 3 - 300 mg 3 times a day.
    Subsequently, the dose can be increased to a maximum of 3600 mg per day (divided into 3 equal doses). A good tolerability of the drug at doses up to 4800 mg / day was noted.The maximum interval between doses with a three-time intake of the drug should not exceed 12 hours in order to avoid the resumption of seizures.
    For children aged 3-12 years, the initial dose of the drug varies from 10 to 15 mg / kg per day, the frequency of administration is 3 times a day in equal doses, the increase to the effective dose is carried out for approximately 3 days. The effective dose in children aged 5 years and older is 25-35 mg / kg per day in equal doses in 3 divided doses. Effective dose EGYPTENIN in children aged 3 to 5 years is 40 mg / kg per day in equal doses in 3 divided doses. A good tolerability of the drug in doses up to 50 mg / kg per day with long-term use was noted. The maximum interval between taking doses of the drug should not exceed 12 hours in order to avoid the resumption of seizures.
    There is no need to monitor the concentration of gabapentin in plasma. EGYPTENIN can be used in combination with other anticonvulsants without taking into account changes in plasma concentration or concentration of other anticonvulsants in serum.

    With neuropathic pain, adults are prescribed in an initial dose of 900 mg / day in 3 divided doses. If necessary, depending on the effect, the dose gradually (300 mg per day every 2-3 days) is increased to a maximum of 3600 mg / day.The minimum time to achieve a dose of 1800 mg per day is 1 week, to achieve a dose of 2,400 mg per day, it takes 2 weeks, and to achieve a dose of 3600 mg per day, it takes 3 weeks. Some patients may need a slower titration.
    Treatment can begin immediately with a dose of 900 mg / day (300 mg 3 times a day) or within the first 3 days the dose can be increased gradually to 900 mg / day as follows:
    1 day - 300 mg of the drug once a day;
    Day 2 - 300 mg twice a day;
    Day 3 - 300 mg 3 times a day.
    The effectiveness of this drug has not been studied in the treatment of neuropathic pain for more than 5 months. If the patient needs to take the drug for more than 5 months, the attending physician should assess the clinical condition of the patient and determine the need for additional therapy.
    If the patient's general condition is poor, for example, at a low body weight, after organ transplantation, etc., titration of the dose should be performed more slowly, using lower doses or longer intervals between dose increases.

    The elderly patients (over 65 years of age) according to the age-related decrease in QC, patients with renal insufficiency (CC less than 80 ml / min), as well as patients on hemodialysis,The therapeutic dose should be selected individually.

    Recommended doses of gabapentin for renal dysfunction.

    Creatinine clearance (ml / min)

    The daily dose of gabapentin (mg) *

    > 80 ml / min

    900-2400

    50-79

    600-1800

    30-49

    300-900

    15-29

    150**-600

    <15

    150**-300

    * The daily dose should be divided into 3 doses
    ** take 300 mg every other day

    Patients who are on hemodialysis and have not previously taken gabapentin, it is recommended to appoint a saturating dose equal to 300-400 mg, then every 4 h of hemodialysis session, appoint 200-300 mg of the drug.
    In days free from dialysis, EGYPTENIN can not be accepted.
    Capsules should be taken orally, without chewing and washing down with the necessary amount of liquid, regardless of food intake.
    Side effects:
    Undesirable reactions are presented according to frequency: very often (> 1/10), often (> 1/100, <1/10), infrequently (> 1/1000, <1/100) and rarely (> 1/10 000; 1/1000).
    From the side of the cardiovascular system: often: hypertension, symptoms of vasodilation; rarely: palpitations.
    From the digestive system: dyspepsia; rarely - nausea, vomiting, abdominal pain, increased appetite; extremely rarely - dryness of the oral mucosa or pharynx, constipation or diarrhea, pancreatitis, increased activity of "hepatic" transaminases, hepatitis, jaundice. When appointed in conjunction with others.antiepileptic drugs - flatulence, anorexia, gingivitis.
    From the musculoskeletal system: rarely - myalgia, arthralgia, gait disturbance. When appointed in conjunction with other antiepileptic drugs - pain in the back, increased brittle bones.
    From the nervous system: drowsiness, dizziness, ataxia, nystagmus (dose-dependent), increased fatigue, tremor, dysarthria, increased nervous excitability; rarely headache, amnesia, depression; very rarely a violation of thinking; confusion, hallucinations, tics, paresthesia, hypoesthesia, asthenia, malaise, hyperkinesia; amplification, hypo- or areflexia, anxiety; hostility, choreoathetosis, dyskinesia, dystonia. When appointed in conjunction with other antiepileptic drugs - insomnia.
    From the respiratory system: rarely - rhinitis, bronchitis, pharyngitis. When appointed in conjunction with other antiepileptic drugs - cough, pneumonia.
    From the genitourinary system: very rarely urinary incontinence, acute renal failure. When appointed in conjunction with other antiepileptic drugs - reduced potency, infection of the urinary tract.
    From the sense organs: impaired vision (diplopia, amblyopia), ringing in the ears.
    From the hematopoiesis: extremely rare - leukopenia, thrombocytopenia.
    Allergic reactions: extremely rare - skin rash, hives, itching, fever, angioedema, multiforme exudative erythema (including Stevens-Johnson syndrome).
    Other: purpura, weight gain; extremely rare - peripheral and generalized edema, discoloration of tooth enamel, alopecia, acne, face swelling, fluctuations in blood glycemia in diabetic patients, pneumonia, respiratory tract infection, urinary tract infection, otitis media. Cancellation reactions: rarely: anxiety, insomnia, nausea, pain, sweating, chest pain. Children often observed aggressive behavior and hyperkinesis.
    Overdose:Symptoms: dizziness, double vision, speech disturbance, drowsiness, lethargy and diarrhea.
    Treatment: washing, stomach, the appointment of activated charcoal, the conduct of symptomatic therapy.
    Patients with severe renal insufficiency can be shown hemodialysis.
    Interaction:
    With the joint administration of gabapentin and morphine, when morphine in the form of capsules with controlled release of 60 mg was taken 2 hours before taking gabapentin, an increase in AUC of gabapentin by 44% was observed, and compared with monotherapy with gabapentin, which was accompanied by an increase in the pain threshold (cold pressor test). The clinical significance of these changes is not established. When gabapentin was administered 2 hours after morphine administration, there was no change in the pharmacokinetic parameters of morphine. The side effects of morphine when combined with gabapentin did not differ from those observed when taking morphine with placebo.
    The interactions between gabapentin and phenytoin, carbamazepine, valproic acid, and phenobarbital are not noted. The pharmacokinetics of gabapentin in an equilibrium state is the same in healthy people and patients receiving other antiepileptic drugs.
    GABAPENTIN does not affect the pharmacokinetics and efficacy of oral contraceptives containing norethisterone and / or ethinyl estradiol.
    Means that neutralize the acidity of the stomach, containing magnesium or aluminum, reduce the bioavailability of gabapentin by 24%. It is recommended that gabapentin at least 2 hours after taking antacid preparations.
    With the combination of cimetidine with gabapentin, the excretion of the latter by the kidneys slightly decreases, which probably has no clinical significance. Other drugs that affect the central nervous system, as well as ethanol, are able to enhance the side effects of gabapentin on the CNS (eg, drowsiness, ataxia).
    Probenecid does not affect renal excretion of gabapentin.
    Special instructions:
    Reduce the dose, cancel the drug or substitute for another alternative means should be gradually over a minimum of 1 week. A sharp cessation of therapy can provoke an epileptic status.
    As with the use of other antiepileptic drugs, in some patients the frequency of seizures may increase or new types of seizures may appear.
    As with other antiepileptic drugs, attempts to discontinue concomitant antiepileptic drugs with a view to switching to gabapentin monotherapy in refractory patients receiving multiple antiepileptic drugs rarely lead to success.
    The drug is not considered effective in absences.
    When the first signs of acute pancreatitis (prolonged pain in the abdominal cavity, nausea, repeated vomiting) should stop treatment with gabapentin. It is necessary to conduct a thorough examination of the patient (clinical and laboratory tests) for the purpose of early diagnosis of acute pancreatitis.
    When gabapentin was added to other anticonvulsants, false positive results were recorded in determining the total protein in the urine using semiquantitative tests. If positive results are obtained with these tests, it is recommended that a more specific precipitation method be used with sulfosalicylic acid or biuret assay.
    Suicidal behavior is described in patients receiving antiepileptic drugs for some indications. Analysis of trials of antiepileptic drugs also revealed a slight increase in the risk of suicidal ideation and suicidal behavior. Existing data is not. exclude the possibility of such an increased risk in the treatment of gabapentin. Therefore, it is necessary to monitor the appearance of signs of suicidal ideation and suicidal behavior in patients and, if necessary, prescribe appropriate treatment.Patients who assist patients should be advised to seek medical help if signs of suicidal ideation and suicidal behavior occur.
    The drug contains lactose, which should be taken into account when lactose intolerance, hereditary galactose deficiency, lactose deficiency, glucose-galactose malabsorption.
    Use in Pediatrics
    The safety and efficacy of gabapentin in children under 3 years of age as part of combined therapy for epilepsy and in children under 12 years of age have not been established as monotherapy.
    The safety and efficacy of therapy for neuropathic pain in patients under the age of 18 years have not been established.
    Effect on the ability to drive transp. cf. and fur:Gabapentin may cause drowsiness, dizziness, and other such symptoms. Patients should be advised not to start work that requires increased attention and speed of psychomotor reactions until the patient's individual response to the drug is determined (especially at the beginning of the course of treatment and with increasing doses).
    Form release / dosage:Capsules 100, 300 and 400 mg.
    Packaging:For 20 capsules in a blister of PVC / PVDC / aluminum foil. 3 or 6 blisters in a cardboard box together with instructions for medical use.
    Storage conditions:Store at a temperature not exceeding 30 ° C.
    Keep the drug out of the reach of children!
    Shelf life:
    Shelf life 3 years.
    Do not use after the expiration date indicated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-000684
    Date of registration:28.09.2011 / 12.01.2015
    The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary
    Manufacturer: & nbsp
    Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary
    Information update date: & nbsp12.01.2015
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