TEBANTIN

Active material: Gabapentin
When ATH: N03AX12
CCF: Anticonvulsants
ICD-10 codes (testimony): G40, R52.2
When CSF: 02.05.10
Manufacturer: GEDEON RICHTER Ltd. (Hungary)

DOSAGE FORM, COMPOSITION AND PACKAGING

Capsules hard gelatin, size №3, Cones-Snap, with pinkish-brown cap and white body; contents of capsules – white or almost white crystalline powder.

Excipients: lactose monohydrate, pregelatinized starch, talc, magnesium stearate.

Composition of a gelatin capsule: iron oxide red, iron oxide yellow, Titanium dioxide, gelatin.

10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Capsules hard gelatin, size №1, Cones-Snap, with pinkish-brown cap and pale yellow body; contents of capsules – white or almost white crystalline powder.

Excipients: lactose monohydrate, pregelatinized starch, talc, magnesium stearate.

Composition of a gelatin capsule: iron oxide red, iron oxide yellow, Titanium dioxide, gelatin.

10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Capsules hard gelatin, size №0, Cones-Snap, with pinkish-brown cap and yellowish orange body; contents of capsules – white or almost white crystalline powder.

Excipients: lactose monohydrate, pregelatinized starch, talc, magnesium stearate.

Composition of a gelatin capsule: iron oxide red, iron oxide yellow, Titanium dioxide, gelatin.

10 PC. – blisters (5) – packs cardboard.
10 PC. – blisters (10) – packs cardboard.

Pharmacological action

The antiepileptic drug. Its structure is similar to gabapentin neurotransmitter gamma-aminobutyric acid (GABA). It is a lipophilic substance. At therapeutic concentrations does not bind to GABA receptors_A, GABA_IN, benzodiazepine, glutamate, glycine and N-methyl-d-aspartate. It shows high activity against receptors in the brain, associated with the α- and δ-structures of the voltage-sensitive calcium channels.

In vitro identified novel peptide receptors in brain tissue, which can mediate the anticonvulsant activity of gabapentin and its derivatives (structure and function of receptors gabapentinovyh not fully understood).

Pharmacokinetics

Absorption

The time to reach C_max is 3 no, irrespective of dose, when receiving repeated doses of the time to reach C_max is reduced to 1 no. Bioavailability is not proportional to the dose: decreases with increasing dose and after repeated receptions 300-600 mg gabapentin 3 times / day is about 60%, and after receiving 1600 mg – about 30%. Eating (incl. rich in fats) did not significantly affect the bioavailability of, in this case the increased AUC and C_max on 14%.

Before the drug at a dose of 300-4800 With averages mg_max and AUC values ​​increase with increasing dose. The deviation from linearity for both parameters is very low at doses, not exceeding 600 mg.

Distribution

Gabapentin is not bound to plasma proteins, V_d – 57.7 l. Concentration in cerebrospinal fluid is 20% from C_ss plasma.

The drug crosses the blood-brain barrier, excreted in breast milk.

Metabolism

Symptoms biotransformation of gabapentin in the human liver inconsequential. Gabapentin does not cause induction of liver enzymes, involved in oxidative processes.

Deduction

Withdrawal from the plasma after the / in the introduction is linear. T_1/2 – 5-7 no. T_1/2 and renal clearance independent of dose and after repeated administration remain unchanged. 80% of the administered dose is excreted in the urine and 20% – with stool. Once inside 400 mg gabapentin 63.6% of the dose excreted in urine.

Obtained at steady state average pharmacokinetic parameters are listed in Table (Tebantinprimenyalsya on 300 mg or 400 mg every 8 no).

Table 1

Pharmacokinetics in special clinical situations

When receiving a single dose of gabapentin plasma concentration of the drug in children 4 to 12 s is similar to that in adults. Repeated receptions stage of saturation is achieved through 1-2 day and is maintained throughout the course of treatment. Children between the ages of 1 months before 5 years AUC value approximately 30% less, than in the older age group with the single dose of the drug at a dose of 10 mg / kg body weight, and when receiving a daily dose of 10-65 mg / kg, razdelennoy of 3 admission.

Age impaired renal function in elderly patients, and kidney diseases, manifested in the reduction QC, lead to a reduction of the plasma clearance of gabapentin and increase the time of excretion. QC reduced proportionally reduce the constant rate of excretion of gabapentin, plasma and renal clearance.

Testimony

- Epilepsy: for the treatment of partial seizures, incl. proceeding with secondary generalization (in adults and children older than 12 years – as monotherapy or in combination therapy; in children 3 to 12 years – in a combination therapy);

- Neuropathic pain: treatment in adults 18 and older (efficacy and safety in patients aged 18 years have not been established).

Dosage regimen

At epilepsy adults and children over 12 years the drug is prescribed in high doses 900-1200 mg / day. The initial dose (first day) is 300 mg 3 times / day. The maximum daily dose – 3600 mg (for 3 equal reception). The maximum interval between doses of the drug doses in the appointment 3 times / day should not exceed 12 no.

Desired therapeutic level of drug in the blood can be achieved within a few days, using the following dosing regimen:

A. First day – 300 mg gabapentin:

(by 300 mg 1 time / day or 100 mg 3 times / day).

On the second day – 600 mg gabapentin:

(by 300 mg 2 times / day, or 200 mg 3 times / day).

On the third day – 900 mg gabapentin:

(by 300 mg 3 times / day).

On the fourth day, increase the dose to 1200 mg for 3 admission, ie. by 400 mg 3 times / day.

or

B. On the first day can be started with the reception at 300 mg 3 times, ie. 900 mg / day. Then, the daily dose can be increased to 1200 mg.

Depending on the resulting effect of the dose can be increased on a daily basis 300-400 mg to a maximum daily dose, Distributed on 3 admission. In long-term clinical studies, doses up to 2400 mg / day were well tolerated. In short-term studies doses up to 3600 mg / day were assigned to a small number of patients, are well tolerated these doses.

When treating epilepsy in children aged 3 to 12 years The recommended daily dose older children 5 years is 25-35 mg / kg, to children 3-4 years – 40 mg / kg. The daily dose is distributed over 3 admission. The effective dose is determined for 3 so days, the first day of the calculation of the dose administered 10 mg / kg / day, on the second day - 20 mg / kg / day and the third day – 30 mg / kg / day. The maximum daily dose in this age range 35-40 mg / kg.

Table 2. The initial dose of gabapentin for children 3-12 years.

Table 3. Maintenance doses of gabapentin for children 3-12 years.

The drug is used for a long time (2-3 year), then the dose is gradually reduced.

When treating neuropathic pain adult, given the resulting effect and tolerability, optimal therapeutic dose is determined by titration. Depending on the individual response of the patient may reach the maximum dose 3600 mg / day.

Recommended modes prescribing:

A. First day 300 mg gabapentin:

(by 300 mg 1 time / day or 100 mg 3 times / day).

On the second day 600 mg gabapentin:

(by 300 mg 2 times / day, or 200 mg 3 times / day).

On the third day 900 mg gabapentin:

(by 300 mg 3 times / day).

or

B. With very intense pain in the first day, you can take 300 mg 3 times, ie. 900 mg / day. Then for one week daily dose may be increased to 1800 mg.

In some cases, it may require a further increase in dose. The maximum daily dose 3600 mg is distributed to 3 admission.

Debilitated patients, patients with low body weight or organ transplant dose can be increased strongly at 100 mg / day.

Elderly patients according to age-related decrease QC, patients with renal insufficiency (CC less than 80 ml / min), and patients, hemodialysis, the dose should be selected individually as follows.

Table 4. The recommended dose of gabapentin at the kidney function

* take in a day at 100 mg 3 times / day.

Patients, hemodialysis, and earlier did not take gabapentin, recommended that a loading dose, equal 300-400 mg, then every 4 h hemodialysis appoint 200-300 mg. In days, free of dialysis, can not take gabapentin.

The course of treatment is from 1 weeks before 1 month, depending on the severity of pain. The duration of treatment depends on the clinical response to therapy.

The capsules should be taken orally, liquid squeezed the necessary amount of liquid, regardless of the meal.

Side effect

From the central and peripheral nervous system: drowsiness (10.6%), dizziness (10.2%), dystaxia (ataxia), nistagmo, visual impairment (diplopia, amblyopia), headache, tremor, dysarthria, amnesia, aphronia, depression, anxiety, emotional lability, disturbances of consciousness, irritability, increased nervous irritability, asthenia, insomnia, tics, Hypo- or arefleksiya, decreased sensitivity, tinnitus, in children under 12 years – hostility and hyperkinesis.

Cardio-vascular system: increased or decreased blood pressure, feeling flares, Warming the extremities.

From the digestive system: nausea, vomiting, anorexia, pancreatolysis, constipation, diarrhea, stomach ache, increased appetite, dryness in the throat, gingivitis, destruction of tooth enamel or changing their colors, flatulence, increase in liver transaminases.

From the hematopoietic system: leukopenia.

On the part of the musculoskeletal system: arthralgia, increased fragility of bones, mialgii, back pain.

The respiratory system: cough, pharyngitis, breathlessness, rhinitis.

Allergic reactions: erythema multiforme exudative, Stevens-Johnson syndrome.

Dermatological reactions: acne, itch, purpura.

With the genitourinary system: urinary incontinence, impotence.

On the part of the endocrine system: changes in blood glucose levels within clinically relevant (blood glucose <3.3 or >7.8 mmol / l at a rate 3.5-5.5 mmol / l), weight gain.

Other: peripheral edema, swelling of the face, fever, fever, flu-like symptoms.

Contraindications

- Acute pancreatitis;

- Children up to age 3 years;

- Hypersensitivity to any component of the drug.

FROM caution should be prescribed in patients with renal insufficiency, Pregnancy and lactation.

Pregnancy and lactation

Due to the lack of sufficient clinical experience on the use of gabapentin during pregnancy Tebantin use in this period is only possible after a thorough evaluation of a possible correlation of risks and benefits of therapy.

Gabapentin is excreted in breast milk. Because of impossibility to avoid the danger of serious adverse effects in infants preparation can be administered during lactation only, when the intended benefits to the mother outweighs the potential risk to the baby.

Cautions

In the process of selecting the optimal therapeutic dose is not necessary to measure the concentration of drug in plasma.

The drug is ineffective in primary generalized seizures, eg, during absences.

When using gabapentin requires monitoring of blood glucose levels in patients with diabetes; sometimes there is a need to change the dose of hypoglycemic medication.

At the first signs of acute pancreatitis (prolonged abdominal pain, nausea, repeated vomiting) discontinue treatment with gabapentin. Should conduct a thorough examination of the patient (clinical and laboratory tests) for early diagnosis of acute pancreatitis.

If lactose intolerance should be considered, what 1 caps. (100 mg) It contains 22.14 Lactose mg, 1 caps. (300 mg) – 66.42 mg, and 1 caps. (400 mg) – 88.56 Lactose mg.

Cancelling preparation, to change the dose, or replaced by other alternative means should be phased in over at least 1 of the week. Abrupt discontinuation of treatment may provoke status epilepticus.

In the case of symptoms of sleepiness in adults, ataksii, dizziness, fatigue, nausea and / or vomiting, weight gain, and the children of sleepiness, hyperkinesia and hostility, should stop taking the drug and consult a doctor.

During gabapentin in qualitative analysis for the presence of protein in the urine with litmus paper possible false positive result. In such cases, you should confirm the result using another method of analysis.

Use in Pediatrics

Safety and efficacy of treatment of neuropathic pain in patients aged 18 years not set.

Effects on ability to drive vehicles and operate machinery

During the period of treatment should refrain from driving vehicles and Occupation potentially hazardous activities, require high concentration and speed of psychomotor reactions.

Overdose

Symptoms: dizziness, double vision, drowsiness, dysarthria and diarrhea.

Treatment: gastric lavage, administration of activated charcoal, simptomaticheskaya therapy. Withdrawal of gabapentin from the body by hemodialysis possible.

Drug Interactions

At simultaneous application with other antiepileptic drugs (phenytoin, karʙamazepinom, valproic acid and phenobarbital) Tebantin not they can increase the level of blood plasma.

Gabapentin has no influence on the action of norethindrone- and / or oral contraceptives etinilestradiolosoderzhaschih, However, when his appointment in combination with other antiepileptic drugs, It is known for its ability to reduce the effect of oral contraceptives, should expect a decrease in contraceptive effectiveness.

Antacids, containing aluminum or magnesium, MAY 24% reduce the bioavailability of gabapentin. Tebantin should be taken no earlier, than after 2 hours after taking antacids.

Cimetidine snizhaet pochechnuyu эliminatsiyu gabapentin.

Ethanol and preparations, affecting the CNS, can increase the side effects of gabapentin CNS.

Conditions of supply of pharmacies

The drug prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 30 ° C. Shelf life - 3 year.