Universal reference book for medicines
Name of the preparation: NEURONTIN ® (NEURONTIN ® )

Active substance: gabapentin

Type: Anticonvulsant drug

Manufacturer: PFIZER MANUFACTURING DEUTSCHLAND (Germany)
Composition, form of production and packaging
Hard
gelatin capsules, size 3, opaque, with a lid and a white body, with blue ink inscriptions - on the cover "Neurontin ® " and "100 mg", on the body - "PD" in the circle;
the color of the inscription is blue; the contents of the capsules are white or almost white powder.
1 caps.

gabapentin 100 mg

Excipients: lactose monohydrate - 14.25 mg, corn starch - 10 mg, talc - 10 mg.

The composition of the shell capsules: gelatin - 39.6 mg, titanium dioxide (E171) - 1.44 mg, sodium lauryl sulfate - less than 0.1 mg.

Ink composition: shellac - 0.075 mg, titanium dioxide (E171) - 0.027 mg, indigocarmine - 0.021 mg.

10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (5) - packs cardboard.
10 pieces.
- packings cellular planimetric (10) - packs cardboard.
Capsules are hard gelatinous, size 1, opaque, with a lid and casing of light yellow color, with blue inscriptions on the cover - "Neurontin ® " and "300 mg", on the body - "PD" in the circle;
the color of the inscription is gray-blue; the contents of the capsules are white or almost white powder.
1 caps.

gabapentin 300 mg

Excipients: lactose monohydrate - 42.75 mg, corn starch - 30 mg, talc - 30 mg.

The composition of the shell capsules: gelatin - 64.07 mg, titanium dioxide (E171) - 0.76 mg, iron oxide oxide yellow (E172) - 0.15 mg, sodium lauryl sulfate - less than 0.15 mg.

Ink composition: shellac - 0.075 mg, titanium dioxide (E171) - 0.027 mg, indigocarmine - 0.021 mg.

10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (5) - packs cardboard.
10 pieces.
- packings cellular planimetric (10) - packs cardboard.
Capsules hard gelatinous, size №0, opaque, with a cover and a cream-orange colored body, with inscriptions in blue ink - on the lid "Neurontin ® " and "400 mg", on the body - "PD" in a circle;
the color of the inscription is gray-blue; the contents of the capsules are white or almost white powder.
1 caps.

gabapentin 400 mg

Excipients: lactose monohydrate - 57 mg, corn starch - 40 mg, talc - 40 mg.

The composition of the shell capsules: gelatin - 80.01 mg, titanium dioxide (E171) - 1.28 mg, iron oxide yellow oxide (E172) - 0.62 mg, iron oxide red oxide (E172) - 0.06 mg, sodium lauryl sulfate - less than 0.19 mg.

Ink composition: shellac - 0.075 mg, titanium dioxide (E171) - 0.027 mg, indigocarmine - 0.021 mg.

10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (5) - packs cardboard.
10 pieces.
- packings cellular planimetric (10) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2015.

PHARMACHOLOGIC EFFECT

Anticonvulsant drug.
By construction, gabapentin is similar to a neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action differs from that of some other drugs interacting with GABA receptors, including valproic acid, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA capture inhibitors, GABA agonists and prodrugs of GABA: it does not possess GABA-ergic properties and does not affect GABA capture and metabolism. Is it supposed that gabapentin binds to? 2 -? - subunit of potential-dependent calcium channels and suppresses the flow of calcium ions, which plays an important role in the occurrence of neuropathic pain.
Gabapentin does not affect the re-uptake of dopamine, noradrenaline and serotonin.

Gabapentin does not bind to receptors of other drugs or neurotransmitters, including GABA A receptors, GABA B , benzodiazepine, glutamate, glycine or N-methyl-d-aspartate at clinically significant concentrations.
Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro. Gabapentin partially attenuates the effects of the glutamate receptor agonist N-methyl-d-aspartate in some in vitro tests, but only at a concentration of more than 100 μmol / L, which is not achieved in vivo. Gabapentin somewhat 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, and also 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.
Suction

The bioavailability of gabapentin is not proportional to the dose;
so, with an increase in the dose, it decreases and is 60, 47, 34, 33 and 27% with the intake of 900, 1200, 2400, 3600 and 4800 mg / day, divided into 3 doses, respectively. Food intake has a slight effect on the rate and extent of absorption of gabapentin (increased maximum plasma concentration (C max ) and area under the concentration-time curve (AUC) by 14%).
Distribution

Gabapentin practically does not bind to blood plasma proteins (<3%) and has a V d of 57.7 l.

Metabolism and excretion

It is excreted from the systemic blood stream by the kidneys in unchanged form.
The human body is practically not metabolized. The half-life period (T 1/2 ) from the blood plasma is dose-independent and averages 5-7 hours. The elimination rate is constant, plasma and renal clearance is directly proportional to the creatinine clearance (CC).
In elderly patients and patients with impaired renal function, the 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.

Pharmacokinetics in specific patient groups

Renal insufficiency

Patients (n = 60) with renal insufficiency (mean CK 13-114 ml / min) took 400 mg gabapentin.
Mean T 1/2 was from 6.5 h (CC> 60 ml / min) to 52 h (CK <30 ml / min), and renal clearance of gabapentin from 90 ml / min to> 10 ml / min (KC <30 ml / min). The average 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 kidney failure were not investigated. The clearance of gabapentin from plasma is reduced in elderly people and in patients with impaired renal function.
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

Because
gabapentin is not metabolized in the liver, its use in patients with impaired liver function has not been studied.
Age

The clearance of gabapentin decreases with increasing age.
In patients under 30 years of age gabapentin clearance is 225 ml / min, and in patients aged 70 years - 125 ml / min. Kidney clearance and clearance in terms of 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.
With MAX is achieved in 2-3 hours. In children aged 1 month to 5 years, gabapentin AUC was 30% lower than in children aged 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 QC. The average T 1/2 is about 4.7 h and is similar between the specified 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 with the latter taking a dose of 30 mg / kg / day.
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.
Because 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;

- monotherapy of partial seizures with secondary generalization and without it in adults and children over the age of 12;

- 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.

DOSING MODE

Neuronthin ® is administered internally regardless of food intake.
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.
Neuropathic pain in adults

The initial dose is 900 mg / day in 3 divided doses;
if necessary, depending on the effect, the dose is gradually increased to a maximum of 3600 mg / day. It should be taken into account that no additional efficacy is observed when using Neurontin ® at a dose above 1800 mg / day.
Treatment can begin immediately with a dose of 900 mg / day (300 mg 3 times / day) or you can increase the dose gradually to 900 mg / day for the first 3 days according to the following scheme: 1st day - 300 mg of the drug 1 time / day ;
The second day - 300 mg 2 times / day; The third day - 300 mg 3 times / day.
Partial cramps

In adults and children over the age of 12, the effective dose is from 900 to 3600 mg / day.
Therapy can begin with a dose of 300 mg 3 times / day on the first day or increase gradually to 900 mg according to the scheme described above (see subsection "Neuropathic pain in 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 three-time intake of the drug should not exceed 12 hours in order to avoid the resumption of seizures.
In 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 / day and increased to an effective dose for approximately 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. The effective dose of gabapentin in children aged 3 to 5 years is 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.
Patients with renal failure are recommended to reduce the dose of gabapentin according to Table 1:

Creatinine clearance (ml / min) Daily dose (mg / day) A

? 80 900-3600

50-79 600-1800

30-49 300-900

15-29 150 B- 600

<15 150 B -300

A daily dose should be given in three divided doses.

B Assign 300 mg every other day.

Patients who are on hemodialysis who have not previously taken gabapentin, it is recommended to prescribe the drug at a saturating dose of 300-400 mg, and then apply it at 200-300 mg after every 4 hours of hemodialysis.

SIDE EFFECT

In the treatment of neuropathic pain

The main side effects that arose on the background of treatment in at least 1% of patients:

On the part of the digestive system: constipation, diarrhea, dryness of the oral mucosa, dyspepsia, flatulence, nausea, vomiting, abdominal pain.

From the side of the nervous system: gait disturbance, coordination disorder, amnesia, ataxia, confusion, dizziness, hypoesthesia, drowsiness, disturbance of 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, infection, pain of different localization, peripheral edema, weight gain, hyperglycemia.

When treating partial seizures

The safety of gabapentin as an additional agent has been studied in more than 2000 patients;
its tolerability was good. GABAPENTIN is most commonly used in combination with other anticonvulsants, so it is impossible to determine which drug (s) cause side effects (if such a link exists at all).
The main side effects that arose on the background of treatment in at least 1% of patients:

From the cardiovascular system: symptoms of vasodilation or hypertension.

On the part of the digestive system: constipation, dental diseases, diarrhea, dyspepsia, increased appetite, dryness of the oral mucosa or pharynx, nausea and / or vomiting, abdominal pain, flatulence, anorexia, gingivitis.

On the part of the organs of hematopoiesis: leukopenia, 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 side of the nervous system: amnesia, ataxia, confusion, coordination disorder, depression, dysarthria, emotional lability, insomnia, nervousness, nystagmus, drowsiness, disturbance of thinking, tremor, muscle twitching, dizziness, hyperkinesia;
strengthening, weakening or lack of reflexes, paresthesia, anxiety, hostility, headache.
On the part of the respiratory system: cough, pharyngitis, rhinitis, pneumonia, bronchitis, respiratory tract infections.

From the skin: abrasions, acne, skin itching, skin rash.

From the sense organs: amblyopia, diplopia, impaired vision, vertigo.

From the genitourinary system: infection of the urinary tract, impotence.

Other: back pain, fatigue, fever, viral infection, peripheral edema, weight gain, asthenia, general malaise, face edema, erectile dysfunction.

These side effects were mild or moderate.
The side effects observed in elderly patients did not differ from those of younger people.
Against the background of monotherapy, no new or unexpected side effects were noted.
When comparing the tolerability of the drug at doses of 300 and 3600 mg / day, the dependence on the dose of such phenomena as dizziness, ataxia, drowsiness, paresthesia and nystagmus is noted.
Children

The following side effects observed with additional therapy in children aged 3-12 years 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.

On the part of the respiratory system: bronchitis, respiratory infection.

Other: viral infection, fever, weight gain, fatigue.

Other adverse events observed in more than 2% of children whose frequency in the placebo group were similar or higher: pharyngitis, upper respiratory tract infection, headache, rhinitis, convulsions, diarrhea, anorexia, cough and otitis media.

Termination of treatment due to adverse events

Side effects, which most often led to the abolition 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, whose association with treatment with gabapentin has not been established.
Other undesirable phenomena registered during the post-marketing use of the drug included an increase in the concentration of creatine phosphokinase in the blood plasma, rhabdomyolysis, acute renal failure, allergic reactions, including hives, alopecia, angioedema, 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 eosinophilia and systemic reactions; gynecomastia, an increase in liver function indicators, hepatitis, jaundice, exudative erythema multiforme, incl. Stevens-Johnson syndrome, hallucinations, hypersensitivity, including systemic reactions, motor disorders such as choreoathetosis, dyskinesia and dystonia, myoclonus, palpitation, pancreatitis, thrombocytopenia, tinnitus, urinary incontinence.
After abrupt abolition of gabapentin therapy, the most common side effects were: anxiety, insomnia, nausea, pain of varying localization and increased sweating.

CONTRAINDICATIONS

- use as a monotherapy of partial seizures with secondary generalization and without it in children under 12 years of age;

- use as an additional agent in the treatment of partial seizures with secondary generalization and without it in children under 3 years of age;

- 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.

With caution should prescribe the drug for kidney failure.

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 effect on the infant is unknown, therefore, during breastfeeding, Neuronthin ® should be given only if the benefit to the mother clearly outweighs the risk to the infant.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution should prescribe the drug for kidney failure.

Patients who are on hemodialysis who have not previously taken gabapentin, it is recommended to prescribe the drug at a saturating dose of 300-400 mg, and then apply it at 200-300 mg after every 4 hours of hemodialysis.

APPLICATION FOR CHILDREN

Contraindicated for use in monotherapy of partial seizures with secondary generalization and without children under the age of 12 years; as an adjunct in the treatment of partial seizures with secondary generalization and without children under the age of 3 years; for the treatment of neuropathic pain in children and adolescents under the age of 18 years.
SPECIAL INSTRUCTIONS

Antiepileptic drugs, including gabapentin, may increase the risk of suicidal thoughts or behavior. Therefore, patients receiving these drugs should be closely monitored for the emergence or worsening of depression, the emergence of suicidal thoughts or behavior, as well as for any changes in behavior.
In the case of acute pancreatitis in patients receiving gabapentin should assess the possibility of withdrawal of the drug.
Although the syndrome of "cancellation", accompanied by the development of seizures in the treatment of gabapentin is not checked, abrupt discontinuation of therapy with anticonvulsants in patients with epilepsy could provoke the development of status epilepticus (see. Section "Dosage and administration").
Gabapentin is not considered as an effective means for the treatment of absence epilepsy.
When applied simultaneously with morphine may experience increasing concentrations of gabapentin in plasma. In this regard, the patient needs to be closely monitored for signs of depression of the central nervous system (CNS) disorders such as drowsiness. The dose of gabapentin or morphine should adequately reduce (see. The section "Interaction with other drugs").
While taking antiepileptic drugs, including gabapentin reported cases of severe life-threatening hypersensitivity reactions, such as drug rash with eosinophilia and systemic concomitant symptoms. It must be remembered that the early signs of hypersensitivity reactions such as fever, lymphadenopathy, may develop even in the absence of skin rash. In the event of such symptoms, you need an immediate examination of the patient. If no other reason other than the use of gabapentin, the use of the drug should be discontinued.
Gabapentin is recommended to take about 2 hours after administration of the antacid. Effect of long-term treatment (more than 36 weeks) gabapentin on learning, intelligence, and development of the child is not sufficiently studied. It is necessary to weigh the possible risks and benefits when prescribing long-term therapy.
As with other antiepileptic drugs, against application of gabapentin can be marked increase in frequency of seizures or other type of appearance of convulsions.
When the joint application of gabapentin and other anticonvulsants false positive results were reported at the determination of protein in urine using test strips N-Multistix Ames SG ®. For determination of protein in urine it is recommended to use a specific precipitation method sulfosalicylic acid.
Impact on the ability to drive vehicles and manage mechanisms

During the administration of the drug to patients is not recommended to drive a car or use potentially dangerous technique to confirm the absence of the negative impact of the drug on the performance of these functions.
OVERDOSE

In single dose of gabapentin should be observed at a dose of 49 g of symptoms: dizziness, double vision, impaired speech, drowsiness, lethargy and mild diarrhea.
Treatment: symptomatic therapy;
patients with severe renal insufficiency, hemodialysis may be indicated.
DRUG INTERACTION

When applying 600 mg of gabapentin at 2 h after administration of morphine in the form of sustained release capsules 60 mg marked increase in the mean AUC of gabapentin by 44% compared to a monotherapy gabapentin that is associated with an increase in pain threshold (cold pressor test). The clinical significance of this change is not established, the pharmacokinetic characteristics of morphine is not changed. Side effects of morphine during coadministration with gabapentin did not differ from those of reception of morphine together with placebo. The degree of interaction of these drugs in other doses unknown.
Interactions between gabapentin and phenobarbital, phenytoin, carbamazepine and valproic acid were 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, is not accompanied by changes in the pharmacokinetics of the two components.
The simultaneous use of gabapentin with antacids that contain aluminum and magnesium, followed by reduction of gabapentin bioavailability by approximately 20% (see. The "Special instructions").
Probenecid does not affect the renal excretion of gabapentin.
A slight decrease (14%) Renal excretion of gabapentin while receiving cimetidine probably has no clinical significance.
With simultaneous use of naproxen (250 mg) and gabapentin (125 mg) was an increase in absorption of gabapentin from 12% to 15%. Gabapentin has no influence on the pharmacokinetic parameters of naproxen. Given the minimum dose of drugs is less than therapeutic. The simultaneous use of these drugs has not been studied in large doses.
With simultaneous use of gabapentin and hydrocodone marked dose-dependent decrease in C max and AUC hydrocodone versus monotherapy with hydrocodone.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored in reach of children at a temperature not higher than 25 ° C.
Shelf life - 3 years.
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