Neurontin capsules 300mg N50
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Active ingredients
Gabapentin
Release form
Capsules
Composition
Gabapentin 300 mg. Adjuvants: lactose monohydrate - 42.75 mg, corn starch - 30 mg, talc - 30 mg. The composition of the shell of capsules: gelatin - 64.07 mg, titanium dioxide (E171) - 0.76 mg, dye of iron yellow oxide (E172) - 0.15 mg, sodium lauryl sulfate - less than 0.15 mg. Ink composition: shellac - 0.075 mg, titanium dioxide (E171) - 0.027 mg, indigo carmine - 0.021 mg.
Pharmacological effect
Anticonvulsant drug. According to the structure gabapentin similar to the neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action differs from that of some other drugs that interact with GABA receptors, including valproate, barbiturates, benzodiazepines, inhibitors of GABA-transaminase reuptake inhibitors GABA agonists, GABA and prodrugs of GABA: it does not possess GABA-ergic properties and does not affect the uptake and metabolism of GABA. It is assumed that gabapentin binds to the α2-δ-subunit of voltage-dependent calcium channels and inhibits the flow of calcium ions, which plays an important role in the occurrence of neuropathic pain. Gabapentin does not affect the reuptake of dopamine, norepinephrine and serotonin. Gabapentin in clinically significant concentrations does not bind to the receptor drugs or neurotransmitters, including GABAA, GABAH, benzodiazepine, glutamate, glycine or N-methyl-d-aspartate receptors. Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro. Gabapentin partially attenuates the effects of the N-methyl-d-aspartate glutamate receptor agonist in some in vitro tests, but only at a concentration of more than 100 mcmol / l, which is not achieved in vivo. Gabapentin somewhat reduces the release of monoamine neurotransmitters in vitro. The use of gabapentin in rats led to an increase in the exchange of GABA in some areas 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 has not been established. In animals, gabapentin easily penetrates into the brain tissue and prevents seizures caused by maximum electroshock, chemicals, including inhibitors of GABA synthesis, as well as due to genetic factors.
Pharmacokinetics
All the pharmacological effects of gabapentin are related to the activity of the unchanged compound.In humans, the body is practically not metabolized. Absorption The bioavailability of gabapentin is not proportional to the dose; so, with an increase in the dose, it decreases and amounts to 60, 47, 34, 33 and 27% at the intake of 900, 1200, 2400, 3600 and 4800 mg / day, divided into 3 doses, respectively. Meal has little effect on the rate and extent of absorption of gabapentin (there is an increase in the maximum plasma concentration (Cmax) and area under the concentration-time curve (AUC) by 14%). The distribution of gabapentin is practically not associated with plasma proteins (less than 3%) and has a Vd of 57.7 l. Metabolism and elimination. Excreted from the systemic blood flow by the kidneys in unchanged form. In humans, almost not metabolized. The half-life (T1 / 2) of blood plasma does not depend on the dose and averages 5-7 hours. The rate of excretion is constant, plasma and renal clearance is directly proportional to creatinine clearance (CK). In patients with renal impairment, plasma clearance of gabapentin decreases . It is removed from plasma using hemodialysis. Patients with impaired renal function or on hemodialysis are recommended to adjust the dose. Pharmacokinetics in special groups of patients Renal failure Patients (n = 60) with renal insufficiency (average CC 13-114 ml / min) took 400 mg gabapentin . The average T1 / 2 ranged from 6.5 h (CK> 60 ml / min) to 52 h (CK less than 30 ml / min), and renal clearance of gabapentin from 90 ml / min (CK> 60 ml / min) to 10 ml / min (CC less than 30 ml / min). The mean plasma clearance (C1 / F) decreased from 190 ml / min to 20 ml / min. In adult patients with renal insufficiency, dose adjustment is necessary. Children with renal failure have not been studied. The clearance of gabapentin from plasma decreases in the elderly and patients with impaired renal function. HemodialysisGabapentin is removed from plasma during hemodialysis. In patients with anuria, hemodialysis has a significant effect on the elimination of gabapentin. Hepatic insufficiency. gabapentin is not metabolized in the liver, its use in patients with impaired liver function has not been studied. The age of the clearance of gabapentin decreases with increasing age. Patients under the age of 30 years, the clearance of gabapentin is 225 ml / min, and in patients at the age of 70 years - 125 ml / min. Renal clearance and clearance per unit of the body surface of the subject also decreases with age.Reduction of renal clearance with age may be explained by a decrease in renal function. Children It has been established that plasma concentrations of gabapentin in children aged 1 month to 12 years are generally similar. Cmax reached after 2-3 hours. In children aged 1 month to 5 years, AUC gabapentin was 30% lower than in children aged 5 years and older. Clearance in terms of body weight in children of the younger group is higher. The apparent clearance of gabapentin is proportional to QC. The average T1 / 2 is about 4.7 hours and is similar between the indicated age groups. According to pharmacokinetic data, the effective daily dose in children with epilepsy at the age of 3–4 years is 40 mg / kg / day, while plasma concentrations are similar to plasma concentrations in children aged 5 years and older when they are last treated with a dose of 30 mg / kg / day. Despite the fact that the comparison of gabapentin pharmacokinetics in men and women has not been carried out, it is assumed that their pharmacokinetic parameters do not differ significantly. Rasovyjastiya gabapentin pharmacokinetic differences among representatives of different their races have not been investigated. Since gabapentin is mainly excreted by the kidneys, and there are no differences in renal function in patients of different races, then no differences in pharmacokinetic parameters are expected.
Indications
treatment of neuropathic pain in adults aged 18 years and older; monotherapy of partial seizures with secondary generalization and without it in adults and children over the age of 12 years; as an additional remedy for the treatment of partial seizures with secondary generalization and without it in adults and children 3 years and older.
Contraindications
- use as a monotherapy of partial seizures with secondary generalization and without it in children under the age of 12 years; - use as an additional means in the treatment of partial seizures with secondary generalization and without it in children under the age of 3 years; - for the treatment of neuropathic pain in children and adolescents under the age of 18; - lactase deficiency, lactose intolerance, glucose-galactose malabsorption; - hypersensitivity to gabapentin or auxiliary components of the drug. Caution should be given be a drug in renal failure.
Precautionary measures
Do not exceed the recommended daily dose.
Use during 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 with breast milk, its effect on the fed infant is unknown, therefore during breastfeeding Neurontin should be prescribed only if the benefit to the mother clearly outweighs the risk to the infant.
Dosage and administration
Neurontin is prescribed by mouth regardless of food intake. If it is necessary to reduce the dose, discontinue the drug or replace it with an alternative remedy, this should be done gradually for at least one week. Neuropathic pain in adults The initial dose is 900 mg / day in 3 divided doses in equal doses; If necessary, depending on the effect, the dose is gradually increased to the maximum - 3600 mg / day. It should be borne in mind that when Neurontin is used in a dose higher than 1800 mg / day, additional effectiveness is not observed. Treatment can be started immediately with a dose of 900 mg / day (300 mg 3 times / day) or you can gradually increase the dose to 900 mg / day during the first 3 days according to the following scheme: 1st day - 300 mg of the drug 1 time / day; 2nd day - 300 mg 2 times / day; Day 3 - 300 mg 3 times / day. Partial seizures In adults and children over the age of 12, the effective dose ranges from 900 to 3,600 mg / day. Therapy can be started with a dose of 300 mg 3 times / day on the first day or gradually increased to 900 mg according to the scheme described above (see the subsection Neuropathic Pain in Adults). Subsequently, the dose can be increased to a maximum of 3,600 mg / day (divided by 3 equal reception). There was a good tolerability of the drug in doses up to 4800 mg / day. The maximum interval between doses when taking the drug three times should not exceed 12 hours in order to avoid recurrence of convulsions. In children aged 3-12 years, the initial dose of the drug varies from 10 to 15 mg / kg / day, which is prescribed in equal doses 3 times / day and increased to be effective for approximately 3 days. The effective dose of gabapentin in children aged 5 years and older is 25-35 mg / kg / day in equal doses in 3 doses. The effective dose of gabapentin in children aged 3 to 5 years is 40 mg / kg / day in equal doses of 3 doses. There was a good tolerability of the drug in doses up to 50 mg / kg / day with prolonged use.The maximum interval between doses of the drug should not exceed 12 hours in order to avoid the resumption of seizures. There is no need to control the concentration of gabapentin in the blood plasma. It can be used in combination with other anticonvulsants without taking into account changes in its plasma concentration or concentration of other anticonvulsant drugs in serum.
Overdose
With a single dose of gabapentin in a dose of 49 g, the following symptoms were observed: dizziness, double vision, impaired speech, drowsiness, lethargy and mild diarrhea. Treatment: symptomatic therapy; Hemodialysis may be indicated in patients with severe renal failure.
Interaction with other drugs
When using 600 mg of gabapentin 2 hours after taking morphine in the form of 60 mg prolonged-release capsules, an increase in the average AUC value of gabapentin is noted by 44% compared with gabapentin monotherapy, which is associated with an increase in the pain threshold (cold pressor test). The clinical significance of this change has not been established, and the pharmacokinetic characteristics of morphine did not change. The side effects of morphine when taken together with gabapentin did not differ from those of taking morphine together with placebo. The degree of interaction of these drugs in other doses is unknown. The interaction between gabapentin and phenobarbital, phenytoin, valproic acid and carbamazepine is not marked. The pharmacokinetics of gabapentin in the equilibrium state are the same in healthy people and patients receiving other anticonvulsants. Simultaneous use of gabapentin with oral contraceptives containing norethisterone and / or ethinylestradiol is not accompanied by changes in the pharmacokinetics of both components. Simultaneous use of gabapentin with antacids, with a glutandin, with an antacid, with a gluten, antacids with antacids will not be accompanied by changes in the pharmacokinetics of both components. gabapentin bioavailability of approximately 20% (see section Special instructions). Probenecid does not affect the renal excretion gabapentin response. A slight decrease (14%) in renal excretion of gabapentin while taking cimetidine is probably not of clinical significance. With simultaneous use of naproxen (250 mg) and gabapentin (125 mg), gabapentin absorption increased from 12% to 15%. Gabapentin does not affect the pharmacokinetic parameters of naproxen. The indicated doses of drugs are less than the minimum therapeutic.The simultaneous use of these drugs in high doses has not been studied. With the simultaneous use of gabapentin and hydrocodone, a dose-dependent decrease in C max and AUC of hydrocodone is observed compared 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 occurrence or worsening of depression, the appearance of suicidal thoughts or behavior, and also for any changes in behavior. In the case of acute pancreatitis with gabapentin, the possibility of drug withdrawal should be evaluated. cancellation, accompanied by the development of seizures, with treatment with gabapentin is not marked, abrupt cessation of therapy with anticonvulsant drugs in patients with epilepsy may provoke the development of epilepsy status (see the section on the route of administration and dosage). Gabapentin is not considered an effective treatment for the absence of epilepsy. An increase in the concentration of gabapentin in the blood plasma can be observed when used simultaneously with morphine. In this regard, the patient needs to be carefully monitored for the development of signs of depression of the central nervous system (CNS), such as drowsiness. The dose of gabapentin or morphine should be adequately reduced (see the section on Interaction with Other Drugs). On the background of taking antiepileptic drugs, incl. gabapentin, cases of severe life-threatening hypersensitivity reactions, such as a drug rash with concomitant eosinophilia and systemic symptoms, have been reported. It must be remembered that early signs of a hypersensitivity reaction, such as an increase in body temperature, lymphadenopathy, can develop even in the absence of a skin rash. In the event of these symptoms, an immediate examination of the patient is necessary. If no other reasons, except for the use of gabapentin, have been found, the use of the drug should be discontinued. It is recommended to take gabapentin approximately 2 hours after taking the antacid. The effect of long-term therapy (more than 36 weeks) with gabapentin on the ability to learn, the intelligence and development of the child has not been sufficiently studied.It is necessary to evaluate the ratio of the possible risk and benefit when prescribing long-term therapy. As with other anti-epileptic drugs, an increase in the frequency of seizures or the appearance of another type of seizures can be observed while using gabapentin. in the urine using test strips Ames N-Multistix SG. To determine protein in urine, it is recommended to use a more specific method of precipitation with sulfosalicylic acid. Effect on the ability to drive vehicles and control mechanisms. While taking the drug, patients are not recommended to drive or use potentially dangerous equipment until there is no negative effect of the drug on these functions.