Active substanceGabapentinGabapentin
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  • Dosage form: & nbspcapsules
    Composition:
    Each capsule contains:
    active substance - gabapentin 100 mg, 300 mg or 400 mg;
    Excipients: corn starch 24.0 mg / 72.0 mg / 96.0 mg, talc 10 mg / 30 mg / 40 mg;
    composition of the capsule: iron dye oxide red (for dosage of 400 mg) 0.1167%, iron dye oxide yellow (for dosages of 300 mg and 400 mg) 0.1500% / 0.6667%, titanium dioxide 2.1119% (0.7779%) 1.4062%, sodium lauryl sulfate 0.08% (0.08% / 008%), gelatin up to 100% / 100% / 100%.
    ink composition: shellac 24-27%, alcohol anhydrous 23-26%, isopropanol 1-3%, butanol 1-3%, propylene glycol 3-7%, iron dye oxide black 24-28%, potassium hydroxide 0.05-0.1% , ammonia solution concentrated 1-2%, water purified 151-218%.
    Description:Dosage of 100 mg. Hard gelatin capsules №3, white capsule body, white capsule porch, white capsule porch, with inscriptions in black ink: on the capsule casing - "02"; on the cap of the capsule - "D". The contents of the capsule are crystalline powder of white or almost white color.
    Dosage of 300 mg. Hard gelatin capsules number 1, the capsule body is yellow, the cap of the capsule is yellow, with the inscriptions in black ink: on the capsule body - "03"; on the cap of the capsule - "D". The contents of the capsule are crystalline powder of white or almost white color.
    Dosage of 400 mg. Hard gelatin capsules №0, orange capsule body, orange capsule cap, with inscriptions, marked with black ink: on the capsule casing - "04"; on the cap of the capsule - "D". The contents of the capsule are crystalline powder white or almost white.
    Pharmacotherapeutic group:Antiepileptic remedy
    ATX: & nbsp

    N.03.A.X.12   Gabapentin

    Pharmacodynamics:By structure gabapentin similar to a neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action is different from other drugs,interacting with the GABA receptors, including valproate, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA reuptake inhibitors, GABA agonists, prodrugs of GABA and he has no GABA-ergic properties and no effect for capturing GABA metabolism. It is assumed that gabapentin binds to α2-δ-subunit of potentially dependent calcium channels and suppresses the current of calcium ions, which plays an important role in the occurrence of neuropathic pain.
    Gabapentin does not affect the re-uptake of dofmine, norepinephrine and sertonin.
    Gabapentin at clinically significant concentrations does not bind to receptors of other common drugs or transmitters, including GABA receptorsA, GABAAT, benzodiazepine, glutamate, glycine or N-methyl-D-aspartate.
    Unlike phenytoin and carbamazepine gabapentin does not interact with sodium channels in vitro. Gabapentin partially attenuates the effects of glutamate receptor antagonist N-methyl-D-aspartate in some tests in vitro, but only at concentrations above 100 umol / liter, which is not achieved in vivo. Gabapentin slightly reduces the release of monoamine neurotransmitters in vitro.The use of gabapentin in rats resulted in an increase in GABA metabolism in some parts of the brain; this effect was similar to that of valproic acid, although it was observed in other parts of the brain. The significance of these effects of gabapentin for its anticonvulsant activity is not established. In animals gabapentin easily penetrates into the brain tissue and prevents seizures caused by maximal electroshock, chemical preparations, including inhibitors of GABA synthesis, as well as caused by genetic factors.
    Pharmacokinetics:
    All pharmacological effects of gabapentin are related to the activity of the unchanged compound. The human body is practically not metabolized.
    Bioavailability for ingestion
    The bioavailability of gabapentin is not proportional to the dose. So, with an increase in the dose, it decreases and is 6,0, 47, 34, 33 and 27% with the intake of 900, 1200, 2400, 3600 and 4800 mg / day, divided into 3 doses, respectively. Eating slightly affects the rate and extent of absorption of gabapentin (there is an increase in the maximum concentration in the blood plasma (Cmax) and the area under the concentration-time curve (AUC) by 14%).
    Distribution
    Gabapentin practically does not bind to blood plasma proteins (<3%) and has a volume distribution of 57.7 liters.
    Excretion
    It is excreted from the systemic blood stream by the kidneys in unchanged form. The human body is practically not metabolized. Half-life (T1/2) from the blood plasma does not depend on the dose and is an average of 5-7 hours. The rate of excretion is constant, plasma and renal clearance is directly proportional to the creatinine clearance. In elderly patients and patients with impaired renal function, plasma clearance of gabapentin decreases. It is removed from the plasma by hemodialysis. In patients with impaired renal function or who are on hemodialysis, it is recommended to perform dose adjustment (see section "Dosage and Administration").
    Special patient groups
    Renal insufficiency Patients (n = 60) with renal insufficiency (average creatinine clearance 13-114 ml / min) took 400 mg gabapentin. Average T1/2 (creatinine clearance <30 ml / min), and renal clearance of gabapentin from 90 ml / min (creatinine clearance> 60 ml / min) to 10 ml / min (creatinine clearance <30 mL / min). The average plasma clearance (C1 / F) decreased from 190 ml / min to 20 ml / min. In adults with renal insufficiency, dose adjustment should be performed (see p.See section "Dosing and Administration"). Children with kidney failure were not investigated.
    Hemodialysis
    Gabapentin is removed from the blood plasma during hemodialysis. In patients with anuria, hemodialysis has a significant effect on the excretion of gabapentin.
    Liver failure
    As gabapentin is not metabolized in the liver, its use in patients with impaired liver function has not been studied.
    The clearance of gabapentin from plasma is reduced in elderly people and patients with impaired renal function.
    Age
    The clearance of gabapentin decreases with increasing age. In patients under the age of 30, gabapentin clearance is 225 ml / min, and in patients over the age of 70 years - 125 ml / min. The renal clearance and clearance in the recalculation per unit body surface of the subject also decrease with age. Reduction of renal clearance with age can be explained by a decrease in renal function.
    Children
    It has been established that concentrations of gabapentin in blood plasma in children aged 1 month to 12 years are generally similar. Cmax was achieved in 2-3 hours.
    In children aged 1 month to 5 years, gabapentin AUC was 30% lower than in children 5 years and older.The clearance in terms of body weight in children of the younger group is higher. The apparent clearance of gabapentin is proportional to the clearance of creatinine. Average T1/2 about 4.7 hours and is similar between the specified age groups.
    According to pharmacokinetic data, the effective daily dose in children with epilepsy of 3-4 years of age is 40 mg / kg / day, while plasma concentrations are similar to plasma concentrations in children 5 years and older with the last 30 mg / kg / day (see " Method of administration and dose ").
    Floor
    Despite the fact that comparison of pharmacokinetics of gabapentin in men and women was not carried out, it is assumed that the pharmacokinetic parameters in them do not differ significantly.
    Race
    Differences in the pharmacokinetics of gabapentin in representatives of different races have not been studied. As gabapentin is mainly excreted by the kidneys, and there are no differences in renal function in patients of different races, then differences in pharmacokinetic parameters are not expected.
    Indications:
    Treatment of neuropathic pain in adults aged 18 years and older. Efficacy and safety in patients under the age of 18 years are not established.
    Monotherapy of partial seizures with secondary generalization and without it in adult children over 12 years of age. The efficacy and safety of monotherapy in children under 12 years of age have not been established.
    As an additional tool in the treatment of partial seizures with secondary generalization and without it in adults and children aged 3 years and older. The safety and efficacy of additional therapy with gabapentin in children less than 3 years of age have not been established.
    Contraindications:Hypersensitivity to gabapentin or auxiliary components of the drug.
    Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.
    Carefully:Renal failure (see section "Method of administration and dose").
    Pregnancy and lactation:There are no data on the use of the drug in pregnant women, so gabapentin should be used during pregnancy only if the intended benefit to the mother justifies the possible risk to the fetus. Gabapentin is excreted in breast milk, its influence on the infant is unknown, so during treatment should abandon breastfeeding.
    Dosing and Administration:
    GABAPENTIN is administered internally, regardless of food intake. If you need to reduce the dose to cancel the drug or replace it with an alternative remedy, this should be done gradually for at least one week.
    Neuropathic pain of adults
    The initial daily dose is 900 mg divided into three doses; if necessary, the dose is gradually increased to a maximum of 3600 mg / day. 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 per day according to the following scheme:
    1st day: 300 mg once a day;
    Day 2: 300 mg twice daily;
    Day 3: 300 mg three times a day.
    Partial cramps
    Adults and children from 12 years: The effective dose is from 900 to 2400 mg / 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 described above (see the section "Neuropathic pain of adults"). Subsequently, the dose can be increased to a maximum of 3600 mg / day (divided into 3 equal doses). A good tolerability of the drug in doses up to 4800 mg / day was noted. The maximum interval between doses with a triple take of the drug should not exceed 12 hours in order to avoid the resumption of seizures.
    Children aged 3-12 years: the initial dose of the drug varies from 10 to 15 mg / kg / day, which is given in equal doses 3 times a day and increased to about 3 days. Effective dose of gabapentin in children aged 5 years and older is 25-35 mg / kg / day in equal doses in 3 divided doses. Effective doses of gabapentin in children aged 3 to 5 years are 40 mg / kg / day in equal doses in 3 divided doses. A good tolerability of the drug in doses up to 50 mg / kg / 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 the blood plasma. It can be used in combination with other anticonvulsants without taking into account changes in its concentration in the blood plasma or the concentration of other anticonvulsants in the serum.
    Selection of a dose for renal failure
    Patients with renal failure are recommended to reduce the dose of gabapentin according to the table:

    Creatinine clearance

    Daily dose (mg / day)A

    ≥80

    900-2400

    50-79

    600-1200

    30-49

    300-600

    15-29

    150B -300

    <15

    150B

    AThe daily dose should be given in three doses
    B Assign 300 mg every other day
    Recommendations for patients on hemodialysis
    Patients on hemodialysis who had not previously taken gabapentin, the drug is recommended to be prescribed in a saturating dose of 300-400 mg, and then apply it at 200-300 mg every 4 hours of hemodialysis.
    Side effects:
    In the treatment of neuropathic pain
    The main undesirable reactions that occurred on the background of treatment at least, in 1% of patients:
    From the digestive system: constipation, diarrhea, dryness of the oral mucosa, dyspepsia, flatulence, nausea, vomiting, abdominal pain.
    From the nervous system: impaired gait, impaired coordination, amnesia, ataxia, confusion, dizziness, hypoesthesia, drowsiness, thinking, tremor, headache.
    From the respiratory system: shortness of breath, pharyngitis.
    From the skin: skin rash.
    From the sense organs: amblyopia, vertigo, conjunctivitis, otitis media.
    Other: accidental injuries, asthenia, back pain, flu-like syndrome, infections, pain of different localization, peripheral edema, weight gain, hyperglycemia.
    When treating partial seizures
    The safety of gabapentin as an additional tool studied in more than 200 patients; its tolerability was satisfactory. Gabapentin most often it is used in combination with other anticonvulsants, so it is impossible to determine which drug causes an undesirable reaction (if such a relationship exists at all). The main undesirable reactions that occurred on the background of treatment at least, in 1% of patients:
    From the cardiovascular system: symptoms of vasodilation or hypertension.
    From the digestive system: constipation, dental disease, diarrhea, dyspepsia, increased appetite, dryness of the oral mucosa or pharynx, nausea and / or vomiting, abdominal pain, flatulence, anorexia, gingivitis.
    From the hematopoiesis: leucopenia, a decrease in the concentration of white blood cells, purpura (most often it was described as bruising caused by physical trauma).
    From the musculoskeletal system: fractures, myalgia, arthralgia.
    From the nervous system: amnesia, ataxia, confusion, coordination disorder, depression, dysarthria, emotional lability, insomnia, nervousness nystagmus, drowsiness,impaired thinking, tremor, muscle twitching, dizziness, hyperkinesia, strengthening, weakening or lack of reflexes, paresthesia, anxiety, hostility, headache. From the respiratory system: cough, pharyngitis, rhinitis, pneumonia, bronchial airway infection.
    From the skin: abrasions, acne, skin itching, skin rash.
    From the sense organs: amblyopia, diplopia, impaired vision, vertigo. From the genitourinary system: urinary tract infection, impotence. Other: back pain, fatigue, fever, viral infection, peripheral edema, weight gain, asthenia, general malaise, face swelling, erectile dysfunction.
    These undesirable reactions were easily or moderately expressed. The adverse reactions observed in elderly patients did not differ from those of younger people. Against the background of monotherapy, no new or unexpected adverse reactions were noted.
    When comparing the tolerability of the drug at doses of 300 and 360 mg / day, the dependence on the dose of such phenomena as dizziness, ataxia, drowsiness, paresthesia and nystagmus is noted.
    Children
    Listed below are the side effects observed with additional therapy for children 3-12 years of age with a frequency of about 2% and higher than with placebo.
    From the digestive system: nausea and / or vomiting.
    From the nervous system: drowsiness, hostility, emotional lability, dizziness, hyperkinesia.
    From the respiratory system: bronchitis, respiratory infection.
    Other: viral infection, fever, weight gain, fatigue. Other adverse events observed in more than 2% of children who had a similar or higher incidence of placebo: pharyngitis, upper respiratory tract infection, headache, rhinitis, convulsions, diarrhea, anorexia, cough and otitis media.
    Termination of treatment due to adverse events
    Undesirable reactions that most often led to the withdrawal of the drug used as an auxiliary therapy: drowsiness, ataxia, dizziness fatigue, nausea and (or) vomiting; as a monotherapy: dizziness, nervousness, weight gain, nausea and / or vomiting and drowsiness.
    Undesirable effects, most often leading to the withdrawal of the drug in children: drowsiness, hyperkinesia and hostility.
    Post-registration application experience
    Cases of sudden unexplained death have been reported, the relationship of which with treatment with gabantin has not been established. Other adverse events were recorded during the post-registration of the drug have included acute renal failure, allergic reactions including urticaria, alopecia angioneurotic edema, generalized edema; fluctuations in blood glucose concentration in diabetics, chest pain, an increase in the volume of the mammary glands, a drug rash that includes zosinophilia and systemic reactions; gynecomastia, increased liver function tests, hepatitis, jaundice, exudative erythema multiforme, including Stevens-Johnson syndrome, hallucinations, hypersensitivity, including systemic reactions, movement disorders such as choreoathetosis dyskinesia and dystopia, myoclonus, palpitations, pancreatitis, anemia, noise in the ears, urinary incontinence.
    Abolition of therapy
    After abrupt abolition of gabapentin therapy, the following undesirable reactions were most often noted: anxiety, insomnia, nausea, pain of different localization and increased sweating.
    Overdose:
    In single dose of 49 g of gabapentin observed the following symptoms: dizziness, double vision, impaired speech, drowsiness, lethargy and mild diarrhea, which disappeared completely during the symptomatic therapy.
    Patients with severe renal insufficiency can be shown hemodialysis.
    Interaction:
    When applying 600 mg of gabapentin through 2 hours after administration of morphine in a capsule with the sustained release 60 mg marked increase in the average values ​​of the area under the curve "concentration-time" (AUC) of gabapentin by 44% compared to a monotherapy gabanentinom that associated with increased pain threshold (cold pressor test). The clinical significance of this change has not been established, the pharmacokinetic characteristics of morphine remain unchanged. The undesirable reactions of morphine with simultaneous use with gabapentin did not differ from those when taking morphine simultaneously with placebo. The degree of interaction of these drugs in other doses is unknown. Interactions between gabapentin and phenobarbital, phenytoin, valproic acid and carbamazepine have not been observed.The pharmacokinetics of gabapentin in the equilibrium state is the same in healthy people and patients receiving other anticonvulsants. The simultaneous use of gabapentin with oral contraceptives containing norethisterone and (or) ethinyl estradiol, is accompanied by changes in the pharmacokinetics of both components.
    The simultaneous use of gabapentin with antacids containing aluminum and magnesium is accompanied by a decrease in bioavailability of gabapentin by approximately 20% (see section "Special instructions").
    Probenecid does not affect renal excretion of gabapentin.
    A slight decrease (14%) of renal excretion of gabapentin with simultaneous administration of cimetidine is probably of no clinical significance.
    With the simultaneous use of naproxen (250 mg) and gabapentin (125 mg), there was an increase in absorption of gabapentin from 12% to 15%. Gabapentin does not affect the pharmacokinetic parameters of naproxen. The indicated doses of drugs are less than minimal therapeutic. Simultaneous use of these drugs in large doses has not been studied.
    With the simultaneous use of gabapentin and hydrocodone, a dose-dependent decrease in Cmax and AUC of hydrocodone in comparison with hydrocodone monotherapy.
    Special instructions:
    Antiepileptic drugs, including gabapentin, may increase the risk of suicidal thoughts or behavior. Therefore, patients receiving these drugs should be carefully monitored for the appearance or deterioration of depression, the appearance of suicidal thoughts or behavior, as well as for any changes in behavior.
    In the case of acute pancreatitis with gabapentin, the possibility of drug cancellation should be evaluated.
    Although the syndrome of "cancellation", accompanied by the development of seizures in the treatment of gabapentin is not checked, abrupt cessation of therapy of anticonvulsants in patients with epilepsy could provoke the development of status epilepticus (see section "Dosage and administration"). Gabapentin is not considered as an effective tool for treating absences-epilepsy.
    With simultaneous application with morphine, there may be an increase in the concentration of gabapentin in the blood plasma. In this regard, the patient needs careful observation for the development of signs of central nervous system (CNS) depression, such as drowsiness.The dose of gabapentin or morphine should be adequately reduced (see section "Interaction with other drugs").
    Against the background of taking antiepileptic drugs, including gabapentin, there have been reports of cases of development of severe, life-threatening hypersensitivity reactions, such as drug rash with concomitant eosinophilia and systemic symptoms. It should be remembered that early signs of hypersensitivity reactions, such as fever, lymphadenopathy, can develop even in the absence of skin rash. In the case of such symptoms, an immediate examination of the patient is necessary. If no other cause is found other than gabapentin, the drug should be discontinued.
    It is recommended to take gabapentin approximately 2 hours after taking the antacid. The effect of prolonged therapy (more than 36 weeks) with gabapentin on learning ability, intelligence and child development has not been sufficiently studied. It is necessary to estimate the ratio of possible risk and benefit in the appointment of long-term therapy.
    As with the use of other antiepileptic drugs, against the background of gabapentin, there may be an increase in the frequency of seizures or the appearance of another type of seizures.
    With the combined use of gabapentin and other anticonvulsants, false-positive results were detected in urine protein determination using the Ames N-Multistix SG® test strips. To determine the protein in the urine, use a more specific method of precipitation with sulfosalicylic acid.
    Effect on the ability to drive transp. cf. and fur:During the administration of the drug, it is not recommended for patients to drive and use potentially dangerous equipment until the negative effect of the drug on the performance of these functions is confirmed.
    Form release / dosage:Capsules 100, 300, 400 mg.
    Packaging:10 capsules per blister A1 / A1.
    For 3 or 10 blisters together with the instructions for use are placed in a cardboard box.
    Storage conditions:In dry, dark place at a temperature of no higher than 25 ° C.
    Keep out of the reach of children.
    Shelf life:2 years.
    Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-002191
    Date of registration:21.08.2013
    Expiration Date:21.08.2018
    The owner of the registration certificate:Aurobindo Pharma Co., Ltd.Aurobindo Pharma Co., Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspAurobindo Pharma, ZAOAurobindo Pharma, ZAO
    Information update date: & nbsp11.03.2017
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