Gabangting 300

General characteristics. Structure:

Active ingredient: габапентин;
1 capsule contains 300 mg of a gabapentin in terms of 100% anhydrous substance;

Excipients: cellulose microcrystallic, starch corn, talc;

Structure of the capsule: gelatin, titanium dioxide (Е 171).

Pharmacological properties:

Pharmacodynamics. Gabapentin - 1 (aminomethyl) - cyclohexaneacetic acid - is the cyclic analog of GAMK capable to get through a blood-brain barrier. Anticonvulsant activity of a gabapentin was shown on many experimental models of convulsive states. The final mechanism of antiepileptic action of a gabapentin remains obscure for today. Despite structural similarity to Gamk, габапентин is not GAMK-mimetik as does not contact neither GAMKA, nor with GAMKV-retseptorami, does not inhibit the return capture of GAMK or degradation of GAMK with GAMK-transaminase participation. It does not interact about potential - dependent natrium channels, with benzodiazepine receptors, with the centers of binding of exciting neurotransmitters; does not influence katekholaminovy, atsetilkholinovy or opiate receptors. Thus, габапентин possesses absolutely new mechanism of action, contacting highly specific centers in TsNS which have the proteinaceous nature, are localized preferential in a neocortex and have no affinity with other antiepileptic means. 
Gabapentin also effectively stops neuropathic pain.

Pharmacokinetics. Absorption - bystry. Bioavailability makes about 60%. Bioavailability is not proportional to a dose: at increase in a dose decreases and makes at a dose 300 mg -    60%, and at a dose of 1600 mg - 30%. Food does not exert impact on pharmacokinetics of a gabapentin. Time of achievement of the maximum concentration makes 2-3 hours. Concentration of drug in plasma is proportional to a dose. The pharmacokinetics does not change at repeated reception. Gets through GEB; at patients with epilepsy concentration of a gabapentin in cerebrospinal fluid makes about 20% of the corresponding equilibrium concentration of drug in plasma. Gets into breast milk. Gabapentin does not contact proteins of a blood plasma, the volume of distribution makes 57,7 liters. Gabapentin is practically not metabolized. Does not induce oxidizing enzymes of a liver. It is removed by kidneys in not changed look. Time of semi-removal does not depend on a dose and averages about 5-7 hours at patients with normal secretory function of kidneys. At patients of advanced age and at patients with a renal failure the speed of removal decreases in direct ratio to the level of clearance of creatinine. It is brought out of blood at a hemodialysis. Dose adjustment is recommended to patients with a renal failure and to the patients who are on a hemodialysis.

Indications to use:

Epilepsy. As monotherapy at treatment of partial convulsive attacks with secondary generalization or without it at adults and children is more senior than 12 years.
As additional therapy at treatment of partial convulsive attacks with secondary generalization or without it at adults and children is more senior than 6 years.
Treatment of peripheral neuropathic pain at post-herpetic neuralgia or a diabetic neuropathy at adults.

Route of administration and doses:

Inside, irrespective of meal, washing down with enough water.

In the initiation of treatment to adults and children from 12 years is also more senior the scheme of titration presented in table 1 is recommended.

 

Table 1

The scheme of use of drug - initial titration.
1st day	2nd day	3rd day
300 mg of 1 times a day	300 mg 2 times a day	300 mg 3 times a day

 

Epilepsy.

Patients with epilepsy demand long therapy. Dosing is defined according to individual portability and efficiency of drug. When, according to the doctor, there is a need for reduction of a dose, the termination of administration of drug or its substitution by alternative means, it needs to be carried out gradually within at least one week.

Adults and children since 12 years.

The effective dose of Gabangting makes 900-3600 mg a day (divided into 3 receptions).

Treatment can be begun with titration of a dose as it is described in table 1, or from appointment on 300 mg three times a day in the 1st day. Further, depending on the individual response of the patient to treatment and portability of drug, it is possible to increase a dose gradually on 300 mg a day each 2-3 days to the maximum dose of 3600 mg a day. For some patients slower titration of a dose of a gabapentin can be required. The minimum time before achievement of a dose of 1800 mg a day corresponds to one week, doses of 2400 mg a day - 2 weeks, doses of 3600 mg a day - in general 3 weeks. The maximum break between administrations of drug should not exceed 12 hours for the prevention of development of spasms.

Children from 6 to 12 years.

To begin treatment with a dose 10-15 mg/kg/days. The effective dose makes 25-35 mg/kg/days, is reached by a titration method within about 3 days. The daily dose is divided into three receptions, the maximum break between administrations of drug should not exceed 12 hours.

Neuropathic pain at adults.

Treatment can be begun with titration of a dose as it is described in table 1, or from purpose of the initial dose of 900 mg a day divided into three receptions. Further, depending on the individual response of the patient to treatment and portability of drug, it is possible to increase a dose gradually on 300 mg a day each 2-3 days to the maximum dose of 3600 mg a day.

For some patients slower titration of a dose of a gabapentin can be required. The minimum time of achievement of a dose of 1800 mg a day corresponds to one week, doses of 2400 mg a day - 2 weeks, doses of 3600 mg a day - in general 3 weeks are necessary. The maximum break between administrations of drug should not exceed 12 hours.

Safety of therapy more than 5 months at treatment of peripheral neuropathic pain was not studied. In need of use of a gabapentin at treatment of peripheral neuropathic pain more than 5 months the doctor has to estimate a clinical condition of the patient and define need of additional treatment.

In case of the admission of the next dose of drug the passed dose needs to be accepted provided that reception of the following dose will be not earlier than in 4 hours. Otherwise the passed dose should not be accepted.

For patients with the weakened general condition of an organism, with low body weight, after organ transplantation the dose of a gabapentin should be titrated more slowly by use of a dosage form with a smaller dosage of drug or increase in an interval between increase in a dose.

Patients of advanced age (65 years are more senior).

For patients of advanced age change of a dosage in connection with age depression of function of kidneys can be required (see table 2).

Patients with a renal failure.

At patients with a renal failure or being on a hemodialysis correction of a dose as it is described in table 2 is recommended.


Table 2

Doses of a gabapentin at adults depending on function of kidneys.
Clearance of creatinine (ml/min.)	The general daily dozaa (mg/days)
≥ 80	900-3600
50-79	600-1800
30-49	300-900
15-29	150b-600
<15c	150b-300

^{the General} daily dose should be distributed on three receptions. Decrease in a dosage is applied to patients with a renal failure (clearance of creatinine <79 ml/min.).

to Appoint ^b in a dose 300 mg every other day.

^c At patients with clearance of creatinine <15ml/mines a daily dose needs to be reduced in proportion to clearance to creatinine (for example at clearance of creatinine of 7,5 ml/min. it is necessary to accept a half of the daily dose accepted by patients with clearance of creatinine of 15 ml/min.

The patients who are on a hemodialysis.

The patients with an anury who are on a hemodialysis and which never received earlier габапентин are recommended to apply doses of saturation from 300 to 400 mg, further 200-300 mg of a gabapentin after each 4-hour session of a hemodialysis. In days, when dialysis not of Provo -

it ditsya, габапентин it is impossible to accept.

To patients with the renal failure which is on a hemodialysis, the maintenance dose of a gabapentin is appointed according to the recommendations stated in table 2. In addition to a maintenance dose it is recommended to appoint 200-300 mg of drug after each 4 sentries of a session of a hemodialysis.

Features of use:

Use during pregnancy or feeding by a breast.
Gabangting it is not necessary to apply during pregnancy; at the solution of a question concerning purpose of drug during pregnancy it is necessary to estimate the expected advantage for mother and possible risk for a fruit.

Gabapentin gets into breast milk. In this regard it is necessary to stop feeding by a breast during treatment by Gabangting.

Children.
Gabangting is shown only for treatment of children with epilepsy: as additional therapy for children over 6 years, as monotherapy for children over 12 years.

At emergence of symptoms of pancreatitis administration of drug needs to be stopped.
The sharp termination of therapy by antiepileptic drugs can provoke increase in frequency of attacks.
As well as in a case with other antiepileptic drugs, at some patients increase in frequency or emergence of new types of attacks at use of a gabapentin can be observed. Attempts of refusal of the accompanying therapy by antiepileptic drugs at treatment of patients with refractory pathology who receive more than one antiepileptic drug in the aspiration to pass to monotherapy gabapentiny seldom are successful.

Drug is inefficient for treatment of absansny epileptic seizures and can even worsen their current at some patients. Therefore patients with the mixed attacks, including absentias epileptica, гапапентин should appoint with care.

It is necessary to watch attentively manifestation of signs of suicide intentions and behavior at the patients accepting antiepileptic means and if necessary to carry out the corresponding treatment.

In case of a renal failure to select a dose of a gabapentin according to clearance of creatinine.

To patients of 65 years is also more senior than system researches on use of a gabapentin were not carried out, however the existing data indicate that at patients of advanced age can arise more often drowsiness, peripheral hypostases, an adynamy.

Effects long (more than 36 weeks) treatments gabapentiny on ability to training, intelligence and development in children and teenagers are studied insufficiently. For this reason the useful effect from the prolonged therapy has to be carefully weighed rather potential risk of such treatment.

Laboratory tests.
When carrying out semi-quantitative definition of crude protein in urine wrong positive takes can be received by method of rapid tests. Therefore it is recommended to check such results of rapid tests by means of methods which are based on other analytical principle, such as biuretic test, a turbidimetrichesky method or a method of binding of dye, or to use these methods right at the beginning.   

Ability to influence speed of response at control of motor transport or work with other mechanisms.
Gabapentin affects the central nervous system and can cause drowsiness, dizziness and other similar symptoms. It can be potentially dangerous to the patients managing motor transport or performing other potentially dangerous works which require special attention and speed of psychomotor reactions. It especially concerns the periods of an initiation of treatment and after increase in a dose.

Side effects:

Side reactions are classified by emergence frequency: very often (≥ 1/10); often (≥1/100 to <1/10); infrequently (≥1/1000 to <1/100); single (≥1/10000 to <1/1000); seldom (<1/10000); it is unknown (frequency cannot be determined on the basis of the existing data).

Infections and invasions: very often - viral infections; often - pneumonia, respiratory infections, infections of an urinary system, otitis of a middle ear.
From blood and a lymph: often - a leukopenia; it is unknown - thrombocytopenia.
From immune system: infrequently - allergic reactions (including a small tortoiseshell); it is unknown - a lymphadenopathy, an eosinophilia.
From metabolic processes: often - anorexia, increase in appetite, increase in body weight; it is unknown - fluctuations of level of glucose at patients with a diabetes mellitus.

Mental disturbances: often - hostility, confusion of consciousness, emotional lability, a depression, uneasiness, the increased nervous irritability, disturbance of thinking; it is unknown - hallucinations.
From a nervous system: very often - drowsiness, dizziness, an ataxy; often - spasms, a hyperkinesia, a dysarthtia, amnesia, a tremor, sleeplessness, a headache, paresthesias, a hypesthesia, an incoordination, a nystagmus; strengthening, reduction or lack of reflexes; infrequently - a hypokinesia; it is unknown - other motive disturbances (a choreoathetosis, dyskinesia, dystonia).
From organs of sight: often - a diplopia, an amblyopia.
From acoustic organs: often - вертиго; it is unknown - a ring in ears.
From cardiovascular system: often - arterial hypertension, vazodilatation symptoms; infrequently - a heart consciousness.
From respiratory system: often - rhinitis, pharyngitis, dispny, bronchitis, cough.
From the alimentary system: often - nausea, vomiting, an abdominal pain, an ulitis, locks or diarrhea, dryness in a mouth, dyspepsia, dental changes, a meteorism, increase in activity of hepatic transaminases; it is unknown - pancreatitis, hepatitis, jaundice, increase in level of bilirubin.
From skin and hypodermic cellulose: often - a face edema, a purpura, skin rash, an itch, an acne; it is unknown - a multiformny exudative erythema, Stephens-Johnson's syndrome, a Quincke's disease, an alopecia.
From a musculoskeletal system: often - a mialgiya, an arthralgia, a dorsodynia, twitching of muscles; it is unknown - a myoclonus.
From an urinary system: often - an urine incontience; it is unknown - an acute renal failure.
From reproductive system: often - impotence; it is unknown - a hypertrophy of mammary glands, a gynecomastia.

General disturbances: very often - increased fatigue, fever; often - peripheral hypostases, walking disturbance, an adynamy, an indisposition, grippopodobny symptoms; infrequently - generalized hypostases; it is unknown - cancellation reaction (concern, sleeplessness, pains, nausea, perspiration), a stethalgia.
Others: often - cases of injuries, fractures.

It was reported about a myopathy with the increased creatinine levels at patients on a hemodialysis with a renal failure of the last stage.

Interaction with other medicines:

As габапентин practically does not contact proteins of serum, it is not metabolized, very low does not induce oxidizing enzymes of a liver, probability of its interaction with other medicines. Perhaps combined use of Gabangting with other antiepileptic drugs (Phenytoinum, carbamazepine, Valproatums, phenobarbital), interaction between them is not revealed.
Gabangting does not influence efficiency of the peroral contraceptive drugs containing norethindrone or ethinylestradiol.

At simultaneous use with the antiacid means containing aluminum and magnesium, bioavailability of a gabapentin decreases approximately by 24%. In this regard Gabangting not earlier than in 2 hours after reception of antiacid drugs is recommended to accept.

At combined use with morphine concentration of a gabapentin in blood can increase. Careful observation of a condition of the patient is necessary for identification of manifestations of oppression of the central nervous system, such as drowsiness. At the same time the dose of morphine or a gabapentin has to be properly corrected.

Probenetsid does not influence excretion of a gabapentin kidneys.
At combined use with Cimetidinum the clearance of a gabapentin slightly decreases, however it has no clinical importance.

Contraindications:

Hypersensitivity to a gabapentin or to any of drug components.

Overdose:

  Cases of overdose of a gabapentin at one-time administration of drug in a dose to 49 g are known. At the same time, despite development of some symptoms (dizziness, diarrhea, doubling in eyes, disturbance of the speech, drowsiness, a lethargy), there were no cases of the menacing state for the patient, and it was normalized after symptomatic therapy. Reduced absorption of a gabapentin in high doses reduces its toxicity at overdose.

The overdose gabapentiny in a combination with depressants of TsNS can lead to a coma.
Depending on a clinical picture it is possible to carry out a hemodialysis though the accumulated experience shows that in it there is no need. The hemodialysis can be shown to patients with heavy renal failures.

Storage conditions:

To store in the place, unavailable to children, in original packaging at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 capsules in the blister; on 3 or 6 blisters in a pack cardboard.