Universal reference book for medicines
Product name: TEBANTIN ® (TEBANTIN ® )

Active substance: gabapentin

Type: Anticonvulsant drug

Manufacturer: GEDEON RICHTER (Hungary)
Composition, form of production and packaging
Hard
gelatin capsules, Coni-Snap ® , size 3, with a pinkish-brown lid and a white body;
the contents of the capsules are a white or almost white crystalline powder.
1 caps.

gabapentin 100 mg

[PRING] magnesium stearate, pregelatinized starch, talc, lactose monohydrate.

Composition of the cap of the gelatin capsule: iron oxide red (E172), iron oxide yellow (E172), titanium dioxide (E171), gelatin.

The composition of the gelatin capsule body: titanium dioxide (E171), gelatin.

10 pieces.
- blisters (5) - packs of cardboard.
10 pieces.
- blisters (10) - packs of cardboard.
Hard gelatin capsules, Coni-Snap ® , size 1, with a pinkish-brown lid and a light yellow body;
the contents of the capsules are a white or almost white crystalline powder.
1 caps.

gabapentin 300 mg

[PRING] magnesium stearate, pregelatinized starch, talc, lactose monohydrate.

Composition of the cap of the gelatin capsule: iron oxide red (E172), iron oxide yellow (E172), titanium dioxide (E171), gelatin.

The composition of the gelatin capsule body: iron dye red oxide (E172), iron oxide yellow (E172), titanium dioxide (E171), gelatin.

10 pieces.
- blisters (5) - packs of cardboard.
10 pieces.
- blisters (10) - packs of cardboard.
Hard gelatin capsules, Coni-Snap ® , size No. 0, with a pinkish-brown lid and a yellowish-orange body;
the contents of the capsules are a white or almost white crystalline powder.
1 caps.

gabapentin 400 mg

[PRING] magnesium stearate, pregelatinized starch, talc, lactose monohydrate.

Composition of the cap of the gelatin capsule: iron oxide red (E172), iron oxide yellow (E172), titanium dioxide (E171), gelatin.

The composition of the gelatin capsule body: iron dye red oxide (E172), iron oxide yellow (E172), titanium dioxide (E171), gelatin.

10 pieces.
- blisters (5) - packs of cardboard.
10 pieces.
- blisters (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2016.

PHARMACHOLOGIC EFFECT

Antiepileptic drug.
Gabapentin is similar in structure to the neurotransmitter gamma-aminobutyric acid (GABA). Is a lipophilic substance. However, its mechanism of action is different from that of some other drugs interacting with GABA receptors, including valproic acid preparations, barbiturates, benzodiazepines, GABA transferase inhibitors, GABA-capture inhibitors, GABA agonists and prodrugs of GABA: it does not possess GABA -ergic properties and does not affect the capture and metabolism of GABA. Preliminary studies suggest that gabapentin binds to? 2 -? subunit of potential-dependent calcium channels and inhibits the flow of calcium ions, which plays an important role in the occurrence of neuropathic pain. Other mechanisms involved in the action of gabapentin in neuropathic pain are: reduction of glutamate-dependent death of neurons, an increase in GABA synthesis, suppression of the release of neurotransmitters of the monoamine group. Gabapentin at clinically significant concentrations does not bind to receptors of other common drugs or transmitters, including the GABA A and GABA B receptors ,benzodiazepine, glutamate, glycine, or NMDA.
Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro.
Gabapentin partially attenuated the effects of the glutamate NMDA receptor agonist in some in vitro tests, but only at a concentration of more than 100 μmol, which is not achieved in vivo. Gabapentin somewhat reduces the release of monoamine neurotransmitters and modifies the activity of GABA synthetase and glutamate synthetase in vitro. The use of gabapentin in rats resulted in increased GABA exchange 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

Suction

Absorption is fast.
After ingestion, C max is achieved after 3 hours. With repeated administration, C max is achieved approximately 1 h faster than with a single dose.The bioavailability of gabapentin is not proportional to the dose: it decreases with increasing dose.
Absolute bioavailability of gabapentin in capsules is about 60%.
Food intake (including high-fat) does not have a significant effect on the pharmacokinetics, in such cases, AUC and C max increase by 14%.
When taking the drug at a dose of 300-4800 mg, the average values ​​of C max and AUC increase as the dose increases.
The deviation from linearity for both indices is very small at doses not exceeding 600 mg; at high doses, the increase is not so significant.
The pharmacokinetic parameters of gabapentin for repeated administration of the drug every 8 hours are given in Table 1.

Index 300 mg (n = 7) 400 mg (n = 11)

C max (μg / ml) 4.02 5.50 (21)

T max (h) 2.7 2.1 (47)

T 1/2 (h) 5.2 6.1 (not specified)

AUC (μg / hr / mL) 24.8 33.3 (20)

The amount of gabapentin excreted in the urine (%) None 63.6 (14)

Distribution

Gabapentin practically does not bind to plasma proteins (less than 3%), V d - 57.7 l.
Concentration in the cerebrospinal fluid is 20% of the C ss in the plasma.
Penetrates through the BBB, excreted in breast milk.

Metabolism

Gabapentin is practically not metabolized in the human body and does not induce oxidative liver enzymes with a mixed function involved in the metabolism of drugs.

Excretion

Excretion from the plasma after intravenous administration is linear.
T 1/2 - 5-7 hours, does not depend on the dose. The rate of elimination constant, plasma clearance and renal clearance of gabapentin are directly proportional to QC. Gabapentin is excreted by the kidneys unchanged. It is removed from the plasma during hemodialysis.
Pharmacokinetics in special clinical cases

After ingestion of gabapentin, the single-dose plasma concentration of the drug in children aged 4 to 12 years is similar to that in adult patients.
With repeated administration of the equilibrium state was achieved after 1-2 days and persisted throughout the course of treatment.
The plasma clearance of gabapentin decreases in elderly patients and in patients with impaired renal function.
When QC is less than 30 ml / min, T 1/2 is about 52 hours. In patients with impaired renal function and patients on hemodialysis, dose adjustment is recommended.
INDICATIONS

- partial seizures with secondary generalization or without it in adults and children over 12 years of age as monotherapy or complementary therapy;

- partial seizures with secondary generalization or without it in children from 3 to 12 years of age as adjunctive therapy;

- Neuropathic pain in patients older than 18 years (efficacy and safety in patients under the age of 18 years are not established).

DOSING MODE

Teabantin ® is administered internally, regardless of food intake or with food.
Capsules should be taken without chewing with a sufficient amount of liquid. With a three-fold administration, it should be borne in mind that the time between two doses should not exceed 12 hours.
With partial seizures in adults and children over 12 years of antiepileptic effect is provided when the drug at a dose of 900-1200 mg / day.
The optimal therapeutic effect is achieved within a few days after titration.
Recommended dosing regimens:

A. On the 1st day - 300 mg gabapentin per day (300 mg 1 time / day or 100 mg 3 times / day).

On the second day - 600 mg gabapentin per day (300 mg 2 times / day or 200 mg 3 times / day).

On the third day - 900 mg gabapentin per day (300 mg 3 times / day).

On the 4th day, the daily dose can be increased to 1200 mg, distributed to 3 doses per day (400 mg 3 times / day).

or

B. Alternative dosing regimen: the initial dose on the first day is 300 mg 3 times, i.e.
900 mg / day. Then the daily dose can be increased to 1200 mg.
Depending on the effect obtained, the dose can be increased by 300-400 mg / day, but not exceeding the total daily dose of 2,400 mg (in 3 doses), which is due to the lack of data on efficacy and safety of the drug at higher doses.

The use of the drug as an additional therapy in children aged 3-12 years and body weight of more than 17 kg

Due to insufficient data on efficacy and safety, the drug is not recommended for children under 3 years of age and is not recommended for children aged 3 to 12 years as a monotherapy.

The recommended daily dose of the drug is 25-35 mg / kg / day in 3 divided doses.
Table 2 presents the recommended daily doses of Tebantin ® , depending on the weight of the child. The effective therapeutic dose is achieved by titration according to the following scheme:
1st day - 10 mg / kg / day

2nd day - 20 mg / kg / day

Day 3 - 30 mg / kg / day, according to the method given in the table.
Then, if necessary, the daily dose of Tebantin® can be increased to 35 mg / kg / day in 3 divided doses. Data from long-term clinical trials have confirmed the good tolerability of Tebantin® in doses of 40-50 mg / kg / day.
Table 2. Initial doses of gabapentin for children aged 3-12 years and a body weight of more than 17 kg.

Body weight (kg) Daily dose First day Second day Third day

17-25 600 mg 200 mg (1 time / day) 200 mg (2 times / day) 200 mg (3 times / day)

> 26 900 mg 300 mg (1 time / day) 300 mg (2 times / day) 300 mg (3 times / day)

Table 3. Supportive doses of gabapentin for children aged 3-12 years and body weight of more than 17 kg.

Body weight (kg) Total daily dose (mg)

17-25 600

26-36,900

37-50,200

51-72 1800

In the treatment of neuropathic pain in adults (over 18 years), the optimal therapeutic dose of Tebantin® is determined by titration, taking into account efficacy and tolerability.
Depending on the individual reaction of the patient, the maximum dose can reach 3600 mg / day.
Recommended dosing regimens:

A. On the 1st day - 300 mg gabapentin per day (300 mg 1 time / day or 100 mg 3 times / day).

On the second day - 600 mg gabapentin per day (300 mg 2 times / day or 200 mg 3 times / day).

On the third day - 900 mg gabapentin per day (300 mg 3 times / day).

or

B. Alternative dosing regimen for intensive pain: the initial dose on day 1 is 300 mg 3 times, i.e.
900 mg / day. Then within 7 days the daily dose can be increased to 1800 mg / day.
In some cases, to achieve the desired analgesic effect, the dose can be increased to a maximum of 3600 mg / day, distributed to 3 doses.
In clinical studies, during the first week, the dose was increased to 1800 mg, and for the second and third weeks, respectively, to 2,400 mg and 3600 mg.
Weakened patients, patients with low body weight or undergoing organ transplantation dose can be increased strictly by 100 mg / day.

Elderly patients in accordance with the age-related decrease in QC, patients with renal insufficiency (CC less than 80 ml / min), as well as patients on hemodialysis , the therapeutic dose should be selected individually (Table 4).

Table 4. Recommended doses of gabapentin for renal dysfunction.

Creatinine clearance (ml / min) Daily dose of gabapentin (mg) *

? 80 ml / min. 900-2400

50-79 600-1800

30-49 300-900

15-29 150 ** - 600

<15 150 ** - 300

* The daily dose should be divided into 3 divided doses

** Take 100 mg of the drug every other day 3 times / day.

Patients who are on hemodialysis and who have not previously taken gabapentin, it is recommended to appoint a saturating dose equal to 300-400 mg, then every 4 h of hemodialysis session, appoint 200-300 mg of the drug.
In days that are free of dialysis, Teabantin ® can not be taken.
SIDE EFFECT

When treating partial seizures

Common: back pain, chest pain, fever, fatigue, flu-like syndrome, asthenia, malaise.

From the side of the nervous system: drowsiness, dizziness, headache, amnesia, ataxia, depression, emotional lability, increased nervous excitability, nystagmus (dose-dependent), tremor, muscle twitching, hyperkinesia, dysarthria, coordination disorder, hallucinations, motor disorders (choreoathetosis, dyskinesia , dystonia), impaired thinking, confusion, tics, paresthesia (dose-dependent), hyperkinesia, strengthening, weakening or lack of reflexes, anxiety, anxiety, hostility, insomnia.

On the part of the digestive system: nausea, vomiting, abdominal pain, dyspepsia, increased appetite, dry mouth or throat, constipation, diarrhea, dental lesions, pancreatitis, hepatitis, jaundice, hepatic transaminase activity, flatulence, anorexia, gingivitis.

From the cardiovascular system: palpitation, symptoms of vasodilation.
When appointed with other drugs - increased blood pressure.
On the part of the hematopoiesis system: leukopenia, thrombocytopenia.

From the musculoskeletal system: arthralgia, myalgia, fractures.

On the part of the respiratory system: pharyngitis, rhinitis, when prescribed with other antiepileptic medicines - cough, pneumonia.

From the sense organs: visual impairment (amblyopia, diplopia), tinnitus.

From the urinary system: urinary incontinence, acute renal failure, with the appointment of other antiepileptic drugs - urinary tract infection.

On the part of the reproductive system: impotence, an increase in the volume of the mammary glands, gynecomastia.

Allergic reactions: skin rash, itching, urticaria, fever, angioedema, multi-form exudative erythema (including Stevens-Johnson syndrome).

Other: purpura, weight gain, discoloration of the tooth enamel, facial edema, peripheral edema, generalized edema, acne, alopecia, fluctuations in blood glucose concentration in patients with diabetes mellitus.

In the treatment of neuropathic pain

Common: accidental injuries, asthenia, back pain, flu-like syndrome, headache, infections, pain of different localization.

From the digestive system: constipation, diarrhea, indigestion, dry mouth, flatulence, nausea, vomiting, abdominal pain.

From the side of the nervous system: gait disturbance, disorientation, paresthesia, drowsiness, disturbance of thinking, tremor.

From the respiratory system: shortness of breath, pharyngitis.

Dermatological reactions: skin rash.

From the sense organs: amblyopia.

From the side of metabolism: peripheral edema, increase in body weight.

In addition, children under 12 years of age were noted for hostility and hyperkinesia when taking gabapentin as adjunctive therapy.

After the abrupt withdrawal of gabapentin therapy, anxiety, insomnia, nausea, pains of various locations, increased sweating were most often noted.

CONTRAINDICATIONS

acute pancreatitis;

- monotherapy in children aged 3 to 12 years;

- children's age till 3 years;

- the period of lactation (breastfeeding);

- Lactase insufficiency, lactose intolerance, glucose / galactose malabsorption (dosage form contains lactose);

- Hypersensitivity to the components of the drug.

Caution should be given to patients with renal insufficiency.

PREGNANCY AND LACTATION

Data on the use of the drug in pregnant women are not available, therefore Tebantin® should be used during pregnancy only if the intended benefit to the mother exceeds the possible risk to the fetus.

Gabapentin is excreted in breast milk.
The effect of gabapentin on infants who are breastfed is unknown, so during breastfeeding Tebantin® should be given only if the benefit to the mother clearly outweighs the risk to the baby.
APPLICATION FOR FUNCTIONS OF THE LIVER

Caution should be given to patients with renal insufficiency.
In patients with impaired renal function and patients on hemodialysis, dose adjustment is recommended.
APPLICATION FOR CHILDREN

Contraindicated in children under 3 years.

Contraindicated the use of Teabantin ® as a monotherapy in children aged 3 to 12 years.

The safety and efficacy of therapy for neuropathic pain in patients under the age of 18 years have not been established.

APPLICATION IN ELDERLY PATIENTS

Patients in the elderly in accordance with the age-related decrease in QC dose should be selected individually.

SPECIAL INSTRUCTIONS

In the process of selecting the optimal therapeutic dose, there is no need to measure the concentration of the drug in the plasma.

The drug is ineffective for the treatment of absent epileptic seizures.

When gabapentin is used, it is necessary to monitor the blood glucose level in patients with diabetes mellitus;
sometimes there is a need to change the dose of a hypoglycemic drug.
When the first signs of acute pancreatitis (prolonged pain in the abdominal cavity, nausea, repeated vomiting) should stop treatment with gabapentin.
A thorough examination of the patient (clinical and laboratory tests) should be carried out for the purpose of early diagnosis of acute pancreatitis.
When lactose intolerance should be taken into account that 1 caps.
(100 mg) contains 22.14 mg of lactose, 1 caps. (300 mg) - 66.42 mg lactose, and 1 caps. (400 mg) - 88.56 mg of lactose.
Reduce the dose, cancel the drug or substitute for another alternative means should be gradually over a minimum of 1 week.
A sharp cessation of therapy can provoke an epileptic status.
In case of adult drowsiness, ataxia, dizziness, fatigue, nausea and / or vomiting, weight gain in adults, drowsiness, hyperkinesia and hostility in children, stop taking the drug and consult a doctor.

Use in Pediatrics

The safety and efficacy of gabapentin in children under 3 years of age as an additional therapy for epilepsy and in children under 12 years of age have not been established as monotherapy.

The safety and efficacy of therapy for neuropathic pain in patients under the age of 18 years have not been established.

Influence on the ability to manage motor vehicles and work with mechanisms

During treatment, patients should refrain from driving motor vehicles and activities potentially hazardous activities that require high concentration and psychomotor speed reactions.
OVERDOSE

Symptoms: dizziness, double vision, impaired speech, drowsiness, lethargy and diarrhea. Symptoms of acute poisoning threatens life is not observed even after a daily intake of 49 grams of the drug.
Treatment: symptomatic therapy. Patients with severe renal insufficiency, hemodialysis may be indicated.
DRUG INTERACTION

Interactions between gabapentin and phenytoin, carbamazepine, valproic acid, phenobarbital were observed. The pharmacokinetics of gabapentin in the equilibrium state is the same in healthy people and patients receiving other antiepileptic drugs.
Gabapentin has no effect on the pharmacokinetics and efficacy of oral contraceptive preparations containing norethisterone and / or ethinyl estradiol. However, the reduction / cessation of contraceptive effect of these drugs is possible by combining the drug Tebantin ® with other antiepileptic drugs, which reduce the effectiveness of oral contraceptives.
Means of neutralizing gastric acidity, containing magnesium or aluminum, gabapentin reduced bioavailability by 24%. Capsules Tebantin ®It should be taken 2 hours after ingestion of antacids.
In combination with cimetidine gabapentin decreases somewhat kidney excretion last, which probably has no clinical significance.
Other drugs that affect the central nervous system, as well as ethanol, capable of increasing the side effects of gabapentin on central nervous system (e.g. somnolence, ataxia).
Probenecid does not affect the renal excretion of gabapentin.
When co-administered gabapentin and morphine when morphine in the form of capsules with controlled release 60 mg was passed for 2 hours before taking gabapentin, an increase AUC of gabapentin 44%, compared to a monotherapy gabapentin, which was accompanied by an increase in pain threshold (cold-pressor test). The clinical significance of these changes has been established. In applying gabapentin 2 hours after administration of morphine no change morphine pharmacokinetic parameters. Side effects of morphine, when used together with gabapentin did not differ from those observed with morphine when receiving placebo.
When adding gabapentin to other anticonvulsant agents false positive results were reported in the determination of total protein in urine using semiquantitative tests.Upon receipt of the positive results with such tests, it is recommended to use a specific precipitation method sulfosalicylic acid or biuret assay.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children at a temperature of no higher than 25 ° C.
Shelf life - 5 years.
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