Last Updated on February 19, 2017 by Dr.Derek Fhisher

Neurontin Gabapentin 100, 300, 400, 600 mg
Most popular brand: Neurontin
Active ingredient: Gabapentin
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SAMe is present within the cells of the body. We shall now examine the negative effects this drug can have on the body. Studies continue to be in the first phases and much more research should be done in this regards however, researchers have located a few benefits of SAMe that are mentioned below. It’s likewise employed as a dietary supplement by lots of people. If Mucinex or some other combination product which contains guaifenesin is given to a young child, the package label has to be read carefully to guarantee that it is the proper product for a young child of that particular age. Let us determine the answer.

Bearing this in mind, ketoprofen in virtually any form is regularly not prescribed when pregnant. This is due to the fact that the existence of the disease may trigger some sort of side effect. It might be detected in blood in a period of 24 hours. In addition, It can cause a number of gastrointestinal or digestive problems in a few individuals. They could alter the mind and affect your emotions. Incredibly, in a few places it’s directly sold over the counter.

There is a single theory about the way that it works in treating seizure. On the opposite hand, fatigue may be experienced by about 4.5% of the individuals who are on this drug, according to clinical studies. Several research have pointed out that people using non-steroidal anti-inflammatory drugs for a prolonged time period, can get a greater risk of strokes as well as heart attacks. This really is slightly more complex in operation, in comparison with injecting alcohol. Anticonvulsants act as treatment for those with CP that have seizures. Another substantial improvement is positive change within the mood.

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Gabapentin (Gabapentin): instruction, and the use of a formula

Code CAS

Feature substance gabapentin

The white or off-white crystalline solid, readily soluble in water and in acidic and basic water solutions. Molecular weight 171,24.


Mode of action -. Anticonvulsant, analgesic

Prevents the occurrence of epileptic seizures in inducing maximal electroshock seizures and pentylenetetrazole in mice and rats, as well as other pre-clinical models (for example, lines with genetically determined epilepsy et al.). The relevance of these models in epilepsy has not been established in humans.

Gabapentin is structurally similar to the neurotransmitter GABA. but it does not change the radioligand binding of GABA to GABA A , or GABA B receptor, is not metabolized in GABA agonist or GABA – receptors and does not inhibit the seizure or destruction of GABA. In studies using a radioligand binding assay, gabapentin at concentrations up to 100 uM showed no affinity for a number of other receptors including benzodiazepine, glutamate, N – methyl – D – aspartate, kviskvalatnye, kainate, glycine (strychnine – insensitive and strychnine – sensitive), alpha 1 -, alpha 2 – and beta – adrenergic, adenosine A 1 and A 2 . muscarinic and nicotinic cholinergic, dopamine D 1 and D 2 . H 1 – histamine, serotonin 5 – HT 1 and 5 – HT 2 . Opiate mu -, delta and kappa, cannabinoid 1, as well as binding sites voltage – sensitive calcium channel (diltiazem or labeled nitrendipine) or voltage – sensitive sodium channels (labeled 20 – alpha – benzoate – batrahotoksininom A). Additionally, gabapentin did not influence the cellular uptake of dopamine, noradrenaline and serotonin.

The study in vitro with radiolabeled gabapentin binding sites were found gabapentin in the brain tissue of rats, including the neocortex and hippocampus. Protein in the brain tissue of animals with high affinity to further identified as gabapentin voltazhaktivirovannogo subunit calcium channel. The clinical significance of this fact is binding until set.

In experimental studies, gabapentin prevents hyperalgesia and allodynia, pain response and especially for different models of neuropathic pain in rats and mice (model streptozocin – induced diabetes, spinal cord injury, etc.). Additionally, it reduces pain response to peripheral inflammation model, but does not directly affect the behavior caused by pain. The relevance of these models has not been established for pain in humans.

The effectiveness of gabapentin as a means of adjuvant antiepileptic therapy in adults and children (3 years and older) with refractory partial seizures set in a multi-center, placebo – controlled, double-blind clinical trials with parallel groups

Confirmations efficiency were obtained in three studies conducted with the participation of 705 patients (aged 12 years and older) and in one study involving 247 children (aged 3 to 12 years). All included in the study patients had a history of at least four partial seizures per month in spite of the use of one or more antiepileptic drugs at therapeutic doses, and in the mode of its established antiepileptic therapy seizures were observed within 12 – week baseline period (for kids ; for 6 weeks). Patients with ongoing seizures (not less than 2, and in some studies ; 4 seizures per month) to ongoing therapy was added gabapentin or placebo for 12 weeks. Efficacy was assessed by the number of patients in whom the frequency of seizures decreased by 50% or more compared to baseline, and expected “response rate” by (T – V) / (T + B), where B ; the base frequency of epileptic seizures and T ; frequency of epileptic seizures in a patient during treatment. response factor ranged from 1 to 1. A value of zero indicates no change; complete disappearance of seizures provides a value of 1, an increase in seizure frequency response gives positive values ​​index. 50% – mu decrease in the frequency of epileptic seizures appropriate response factor ; 0,33.

In one study gabapentin at a dose of 1200 mg / day. divided into 3 doses, compared to placebo. The response rate was 23% (14/61) in the group receiving gabapentin, and 9% (6/66) in the placebo group; differences between the groups were statistically significant. response factor was also higher in the group receiving gabapentin (& minus; 0,199), than in the placebo group (& minus; 0,044); differences also reached the degree of statistical significance.

In the second study compared gabapentin (1200 mg / day in 3 divided doses, n = 101) to placebo (n = 98), but to determine the dose-response in the study additionally included two smaller number of the group of patients who were prescribed gabapentin 600 mg / day (n = 53) and 1800 mg / day (n = 54). Response rate in the group treated with gabapentin at a dose of 1200 mg / day (16%) was higher than in the placebo group (8%), but the differences were not statistically significant. Response rate in the group receiving 600 mg / day of gabapentin (17%) was also not significantly higher than in the placebo group, but the group treated with 1800 mg / day. the response rate (26%) of statistically greater than that in the placebo group. Coefficient response in patients treated with gabapentin at a dose of 1200 mg / day (& minus; 0,103), was higher than the placebo group (& minus; 0,022), but also this difference did not reach statistical significance (p = 0,224). The best response observed in the group treated with gabapentin at 600 mg / day (& minus; 0,105) and at a dose of 1800 mg / day (& minus; 0,222), than in patients receiving 1200 mg / day. while in the group treated with gabapentin at a dose of 1800 mg / day. It achieved a statistically significant difference compared to placebo.

In the third study compared gabapentin (900 mg / day in 3 divided doses, n = 111) to placebo (n = 109) and for the study of dose-response in the study additionally included a group of patients (n = 52), which was administered in 1200 mg / day of gabapentin. There were statistically significant differences in the degree of response in the group receiving gabapentin at a dose of 900 mg / day (22%) compared with placebo (10%). The coefficients of the response in the groups treated with gabapentin at 900 mg / day (& minus; 0,119) and at a dose of 1200 mg / day (& minus; 0,184), significantly higher than that of the placebo group (& minus; 0,027).

In all three of the above studies, the study of the effect of gabapentin in the prevention of secondary generalized tonic – clonic seizures showed statistically significant results and positive trends in virtually all patients included in the study.

An analysis of the degree of response in the combined data from all three trials for all applied doses (gabapentin ; n = 162, placebo ; n = 89) also demonstrates the significant benefits of gabapentin over placebo in reducing the frequency of secondarily generalized tonic – clonic seizures

Two of the three controlled studies used more than one dose of gabapentin. In each of these studies, no significant increase in the response, depending on the dose. Nevertheless, the general trend is obvious to improve the effectiveness of gabapentin with increasing dose.

The fourth study involving pediatric patients (from 3 to 12 years old) at a dose of 25, Gabapentin – 35 mg / kg / day (n = 118) compared with placebo (n = 127). response factor for all patients with partial seizures was significantly higher with gabapentin (& minus; 0,146), than in the placebo group (& minus; 0,079).

The studies in children aged 1 month to 3 years, treated with 40 mg / kg / day of gabapentin (N = 38) compared with placebo (N = 38) revealed no statistically significant difference in response rate and response rate in the studied patients.

The effectiveness of gabapentin for postherpetic neuralgia control was evaluated in two randomized, double-blind, placebo – controlled multicenter studies involving 563 patients. The criterion for the selection of patients was to preserve the pain for more than 3 months after healing of skin lesions caused by shingles. Gabapentin was administered at a dose of 1800 to 3600 mg / day in 3 divided doses. In both studies found significant differences from placebo in the range of doses applied. Typically, a significant pain relief was observed within the first week of treatment and was maintained to the end.

on mice and rats studies gabapentin treated orally in a dose of 8000 mg / kg and lethal dose not been established. The animals were observed following acute toxicity Symptoms: ataxia, dyspnea, ptosis, sedation, decreased activity or excitement.

In experiments on mice and rats, which gabapentin mixed into food for 2 years, we found a statistically significant increase in the number of cases atsinarnokletochnoy adenoma and carcinoma of the pancreas in male rats in the preparation of high dose ; 2000 mg / kg / day. At this dose, the peak plasma concentration of gabapentin in the rat was 10 times higher than that of the people who received gabapentin at a dose of 3600 mg / day. Atsinarnokletochnaya pancreatic carcinoma had no effect on survival, not metastasized and showed no local invasion. The relevance of these data in relation to carcinogenic risk in humans has not been established.

The standard tests in vitro and in vivo gabapentin showed no mutagenic or genotoxic properties.

Not observed effect on reproduction and fertility in rats treated with gabapentin at a dose of 2000 mg / kg (approximately 5 times greater than the maximum recommended dose for humans based on mg / m 2).

Pharmacokinetics . Gabapentin does not undergo significant metabolism in humans.

gabapentin Bioavailability decreases with increasing dose and after administration of doses of 900, 1200, 2400, 3600 and 4800 mg / day (divided into 3 doses), respectively 60, 47, 34, 33 and 27%. Food intake has little effect on the rate and extent of absorption of gabapentin (14% increase in area under the curve AUC and C max ).

Binding to plasma proteins ; less than 3%, the apparent volume of distribution after / in a dose of 150 mg is 58 & plusmn; 6 l. In patients with epilepsy C min in the cerebrospinal fluid was approximately 20% of the corresponding plasma levels.

gabapentin displayed by renal excretion. T 1/2 ; 5 & ​​ndash; 7 hours and is independent of dose and multiple dose subsequent doses. The elimination rate constant, plasma clearance, and renal clearance of gabapentin is directly proportional to creatinine clearance. In the elderly and in patients with impaired renal function gabapentin plasma clearance is reduced. Gabapentin can be removed from plasma by hemodialysis.

Patients with impaired renal function, the elderly and hemodialysis dose adjustment is needed. In children with renal impairment has not been studied gabapentin. Patients with age-related weakening of the kidney function may require dose reduction.

Because gabapentin is not metabolized by the liver, studies in people with impaired liver function have not been conducted.

The study of the pharmacokinetics of gabapentin in children with epilepsy showed that children between the ages of 3 to 4 years to reach the same mean plasma concentration, which is observed in children from 5 to 12 years at a daily dose of 30 mg / kg, required daily dose of 40 mg / kg.

Special comparative studies of the pharmacokinetics of gabapentin in men and women has been conducted, however, on – apparently, there are no significant differences in the pharmacokinetic parameters of gabapentin in men and women.

The pharmacokinetic differences have not been studied in people of different racial groups, but because gabapentin is derived primarily by the kidneys, and creatinine clearance in people of different races are not significantly different, the existence of such differences is not expected.

Application of the substance gabapentin

Gabapentin is indicated for partial seizures with or without secondary generalization in adults and children older than 12 years (as an adjunct), partial seizures in children 3 – 12 years (as a further means), as well as for the treatment of postherpetic neuralgia in adults.


Hypersensitivity, children up to 3 years with partial seizures (efficacy as an adjunct in the treatment has not been established), and up to 12 years with post-herpetic neuralgia (efficacy and safety studies were not performed).

Application of pregnancy and breastfeeding

It is possible during pregnancy only if the expected effect of therapy outweighs the risk to the fetus (adequate and well-controlled studies in pregnant women has not been).

Category effects on the fetus by FDA ; C.

At the time of treatment should stop breastfeeding (gabapentin passes into breast milk when taken orally).

Side effects of substance gabapentin

The most commonly observed adverse events associated with the use of gabapentin in adults whose frequency is different from that in patients treated with placebo, were dizziness, somnolence, and peripheral edema.

In two controlled clinical trials, 16% of the 336 patients who received gabapentin and 9% of 227 placebo-treated patients discontinued treatment because of – because of side effects. The most frequent adverse events which led to the cancellation of gabapentin were dizziness, somnolence, and nausea.

Table 1 lists the signs and symptoms of disease were observed in at least 1% of the patients with postherpetic neuralgia treated with gabapentin involved in the placebo – controlled trial, and the incidence of which was higher than the placebo group. The intensity of the side effects were mild to moderate.

The system of the body / side effects

* The report described as blurred vision

Other side effects observed in more than 1% of patients, but there are equally or even more frequently in the placebo group were pain, tremor, neuralgia, back pain, dyspepsia, dyspnea, flu-like symptoms.

There were no significant clinical differences between men and women according to the type and frequency of adverse events. Because the study included only a few patients non-white race, the data to support a statement regarding the distribution of adverse events by race, is not enough.

The most commonly observed adverse events associated with the use of gabapentin in combination with other antiepileptic drugs in patients older than 12 years do not occur with the same frequency in placebo-treated patients, were somnolence, dizziness, ataxia, fatigue, and nystagmus. The most commonly observed adverse events associated with the use of gabapentin in combination with other antiepileptic drugs in children aged 3 to 12 years do not occur with the same frequency in placebo-treated patients, were viral infection, fever, nausea and / or vomiting, somnolence, and hostility.

Approximately 7% of 2074 patients aged over 12 years old and about 7% of 449 children aged 3 to 12 years who received gabapentin in pre-marketing clinical trials discontinued treatment because of – because of side effects. The most common adverse events which led to the abolition of the drug in patients older than 12 years, was somnolence (1.2%), ataxia (0.8%), fatigue (0.6%), nausea and / or vomiting (0.6% ) and dizziness (0.6%). The most common adverse events which led to the abolition of the drug in children, were emotional lability (1.6%), hostility (1.3%), and hyperkinesia (1,1%).

Table 2 lists the signs of the disease and symptoms that occurred in at least 1% of patients older than 12 years with epilepsy treated with gabapentin, participated in placebo – controlled trials, and the incidence of which was higher in the group treated with gabapentin. The intensity of the side effects were mild to moderate.

The system of the body / side effects

* In addition to the ongoing antiepileptic therapy

When prescribing the medicine should be kept in mind that the data obtained by adding gabapentin to ongoing antiepileptic treatment, can not be used to predict the frequency of adverse events in general medical practice, where the characteristics of the patients and other factors may be different from those which prevailed in clinical trials. Similarly, the frequency of the said side effects can not be directly compared with those obtained in other clinical trials including different treatment regimens, subjects or other researchers. rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; rare ; Johnson’s.



Dosing and Administration

The initial dose of ;


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