Tebantin - instructions for use, analogs, reviews and release forms (capsules or tablets 100 mg, 300 mg and 400 mg) of the drug for the treatment of epilepsy, seizures, neuropathic pain in neuralgia in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Tebantin. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of experts on the use of Tebantin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues Tebantin in the presence of existing structural analogues. Use for the treatment of epilepsy, seizures,neuropathic pain in neuralgia and polyneuropathy in adults, children, as well as during pregnancy and breast-feeding. Composition of the preparation.

Tebantin antiepileptic drug. Gabapentin (the active substance of Tebantin) 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 indicate that gabapentin binds to the alpha2-omega subunit of potential-dependent calcium channels and suppresses 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 does not bind to receptors of other common drugs or transmitters, including GABAA and GABAB receptors, benzodiazepine, glutamate, Glycine or NMDA, at clinically significant concentrations.

Unlike phenytoin and carbamazepine, Tebantin does not interact with sodium channels. 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.

Composition

Gabapentin + auxiliary substances.

Pharmacokinetics

Absorption is fast. With repeated administration, Cmax 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 significantly affect the pharmacokinetics, in such cases, AUC and Cmax increase by 14%. When taking the drug at a dose of 300-4800 mg, the average values ​​of Cmax and AUC increase with increasing dose. 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. Gabapentin practically does not bind to plasma proteins (less than 3%). Concentration in cerebrospinal fluid is 20% of Css in plasma. Penetrates through the blood-brain barrier (GEB), excreted in breast milk. 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 from plasma after intravenous administration is linear. 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.

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 (with neuralgia and polyneuropathy) in patients older than 18 years.

Forms of release

Capsules 100 mg, 300 mg and 400 mg (sometimes mistakenly called tablets).

Instructions for use and dosing regimen

Teabanthine 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 per 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 once a day or 100 mg 3 times a day).

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

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

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

or

B. Alternative dosing regimen: the initial dose on the first day is 300 mg 3 times, i.e. 900 mg per 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 per day, but not exceeding the total daily dose of 2,400 mg (in 3 doses), which is due to the lack of data on the effectiveness 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 per day in 3 divided doses. The effective therapeutic dose is achieved by titration according to the following scheme:

• The 1st day - 10 mg / kg per day;
• The second day - 20 mg / kg per day;
• Day 3 - 30 mg / kg per day.

Then, if necessary, the daily dose of Tebantine can be increased to 35 mg / kg per day in 3 divided doses. Data from long-term clinical studies have confirmed the good tolerability of Tebantin in doses of 40-50 mg / kg per day.

In the treatment of neuropathic pain in adults (over 18 years), the optimal therapeutic dose of Tebantine is determined by titration, taking into account the effectiveness and tolerability. Depending on the individual reaction of the patient, the maximum dose can reach 3600 mg per day.

Recommended dosing regimens:

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

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

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

or

B. Alternative dosing regimen for intensive pain: the initial dose on day 1 is 300 mg 3 times, i.e. 900 mg per day. Then within 7 days the daily dose can be increased to 1800 mg per day.

In some cases, in order to achieve the desired analgesic effect, the dose can be increased to a maximum of 3600 mg per day, distributed to 3 doses. In clinical studies, during the first week, the dose was increased to 1800 mg, and in 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 per 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.

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, Tebantin should not be taken.

Side effect

• backache;
• chest pain;
• fever;
• increased fatigue;
• influenza-like syndrome;
• asthenia;
• accidental injury;
• malaise;
• drowsiness;
• dizziness;
• headache;
• amnesia;
• ataxia;
• depression;
• emotional lability;
• increased nervous excitability;
• nystagmus (dose-dependent);
• tremor;
• muscle twitching;
• hyperkinesis;
• dysarthria;
• lack of coordination;
• hallucinations;
• motor disorders (choreoathetosis, dyskinesia, dystonia);
• violation of thinking;
• confusion of consciousness;
• tics;
• paresthesia (dose-dependent);
• hyperkinesia;
• amplification, attenuation or absence of reflexes;
• anxiety;
• anxiety;
• hostility;
• insomnia;
• nausea, vomiting;
• abdominal pain;
• dyspepsia;
• increased appetite;
• dry mouth or throat;
• constipation, diarrhea;
• lesions of teeth;
• pancreatitis;
• hepatitis;
• jaundice;
• increased activity of hepatic transaminases;
• flatulence;
• anorexia;
• gingivitis;
• palpitation;
• symptoms of vasodilation;
• increased blood pressure;
• leukopenia, thrombocytopenia;
• arthralgia;
• myalgia;
• fractures;
• dyspnea;
• pharyngitis;
• rhinitis;
• when prescribed with other antiepileptic drugs - cough, pneumonia;
• impaired vision (amblyopia, diplopia);
• noise in ears;
• urinary incontinence;
• acute renal insufficiency;
• when prescribed with other antiepileptic drugs - urinary tract infection;
• impotence;
• an increase in the volume of mammary glands;
• gynecomastia;
• skin rash;
• itching;
• hives;
• fever;
• angioedema;
• multi-form exudative erythema (including Stevens-Johnson syndrome);
• purpura;
• increase in body weight;
• change in tooth enamel color;
• swelling of the face;
• peripheral edema;
• generalized edema;
• acne;
• alopecia;
• fluctuations in blood glucose concentration in patients with diabetes mellitus.

After abrupt abolition of gabapentin therapy, cancellation syndrome can develop for which the following symptoms are noted: anxiety, insomnia, nausea, pain of different localization, increased sweating.

Contraindications

• acute pancreatitis;
• monotherapy in children aged 3 to 12 years;
• children under 3 years;
• lactation period (breastfeeding);
• lactase insufficiency, lactose intolerance, glucose / galactose malabsorption (dosage form contains lactose);
• hypersensitivity to the components of the drug.

Application in 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 for 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 prescribed only if the benefit to the mother clearly outweighs the risk to the baby.

Use in children

Contraindicated in children under 3 years.

Contraindicated the use of Tebantine 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 hypoglycemic drug.

When the first signs of acute pancreatitis (prolonged pain in the abdominal cavity, nausea, repeated vomiting) should stop treatment with Tebantin.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, it should be noted that 1 capsule (100 mg) contains 22.14 mg of lactose, 1 capsule (300 mg) - 66.42 mg of lactose, and 1 capsule (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.

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

During the period of treatment, patients should refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Drug Interactions

Interactions between gabapentin and phenytoin, carbamazepine, valproic acid, and Phenobarbital have not been observed.The pharmacokinetics of gabapentin in the equilibrium state is the same in healthy people and patients receiving other antiepileptic drugs.

Gabapentin does not affect the pharmacokinetics and efficacy of oral contraceptives containing norethisterone and / or ethinylestradiol. However, the reduction / cessation of the contraceptive effect of these drugs is possible when combining Tebantine with other antiepileptic drugs that reduce the effectiveness of oral contraceptives.

Means that neutralize the acidity of the stomach, containing magnesium or aluminum, reduce the bioavailability of gabapentin by 24%. Capsules Tebantyn should be taken 2 hours after taking antacids.

With the combination of cimetidine with gabapentin, the excretion of the latter by the kidneys slightly decreases, which probably has no clinical significance.

Other drugs that affect the central nervous system, as well as ethanol (alcohol), can increase the side effects of Tebantin on the CNS (for example, drowsiness, ataxia).

Probenecid does not affect renal excretion of gabapentin.

With the joint administration of gabapentin and morphine,when morphine in the form of capsules with controlled release of 60 mg was taken 2 hours prior to gabapentin, an increase in AUC of gabapentin by 44% was observed, compared with monotherapy with gabapentin, which was accompanied by an increase in the pain threshold (cold pressor test). The clinical significance of these changes is not established. When gabapentin was administered 2 hours after morphine administration, there was no change in the pharmacokinetic parameters of morphine. The side effects of morphine when combined with gabapentin did not differ from those observed when taking morphine with placebo.

When gabapentin was added to other anticonvulsants, false positive results were recorded in determining the total protein in the urine using semi-quantitative tests. If positive results are obtained with such tests, it is recommended to use a more specific method of precipitation with sulfosalicylic acid or biuret breakdown.

Analogues of Tebantine

Structural analogs for the active substance:

• Gabagamma;
• Gabapentin;
• Gapentec;
• Caten;
• Convalis;
• Neuronthin;
• Egipentin;
• Eplorontin.

Analogues on the curative effect (antiepileptic drugs):

• Actinerval;
• Algerian;
• Acetazolamide;
• Benzobarbital;
• Benzon;
• Valparin;
• Valproate sodium;
• Valproic acid;
• Wimpat;
• Habitryl;
• Hexamidine;
• Depakin;
• Depamid;
• Diazepam;
• Diakarb;
• Diphenine;
• Zeptol;
• Zonegran;
• Inovevelon;
• Carbamazepine;
• Carbasan retard;
• Clonazepam;
• Convalis;
• Convulex;
• Convulsant;
• Lamyctal;
• Lamitor;
• Lamotrigine;
• Levetiracetam;
• Lethiram;
• Lyrics;
• Mazepine;
• Neuronthin;
• Pregabalin;
• Relium;
• Sibazon;
• Suxilep;
• Tegretol;
• Topiramate;
• Trileptal;
• Phenobarbital;
• Finlepsin;
• Finlepsin retard;
• Chloracon;
• Enkorat;
• Epimax;
• The epitope.

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