Tebantin
Tebantin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Tebantin
ATX code: N03AX12
Active ingredient: Gabapentin (Gabapentin)
Manufacturer: JSC "Gedeon Richter". 1103, Budapest, Hungary
Description and photo update: 2019-12-08
Prices in pharmacies: from 705 rubles.
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Tebantin is an antiepileptic drug with analgesic activity (for neuropathy) and anxiolytic and neuroprotective effects.
Release form and composition
Tebantin's dosage form - Coni-Snap capsules: hard gelatinous, pinkish-brown cap, body color depends on the dose of the drug; capsules are filled with white or almost white crystalline powder (10 pieces in blisters, 5 or 10 blisters in a cardboard box):
- dose of 100 mg: capsule size No. 3, white body;
- dose of 300 mg: capsule size No. 1, light yellow body;
- dose 400 mg: capsule size No. 0, yellowish-orange body.
1 capsule contains:
- active substance: gabapentin - 100, 300 or 400 mg;
- auxiliary components: talc, lactose monohydrate, magnesium stearate, pregelatinized starch;
- capsule cap: iron dye red oxide (E172), iron dye yellow oxide (E172), titanium dioxide (E171), gelatin;
- capsule body: iron dye red oxide (E172) and iron dye yellow oxide (E172) - for doses of 300 and 400 mg, titanium dioxide (E171), gelatin.
Pharmacological properties
Pharmacodynamics
Gabapentin is a lipophilic substance whose structure is similar to that of the neutrotransmitter gamma-aminobutyric acid (GABA). At the same time, the mechanism of action of gabapentin differs from some other drugs interacting with GABA receptors: it does not exhibit GABA-ergic properties and does not affect the capture and metabolism of GABA.
According to preliminary studies, gabapentin is able to bind to the α2-δ subunit of voltage-gated calcium channels and inhibit calcium ion flux, which plays an important role in neuropathic pain. Gabapentin's action in neuropathic pain is also due to the following mechanisms:
- increased synthesis of GABA;
- decrease in glutamate-dependent neuronal death;
- suppression of the release of neurotransmitters of the monoamine group.
At clinically significant concentrations, gabapentin is unable to bind to receptors of other common drugs or transmitters (including receptors for GABA A and GABA B, N-methyl-D-aspartate, glycine, glutamate or benzodiazepines). Unlike carbamazepine and phenytoin, this substance is not capable of interacting with sodium channels in vitro.
Data from some in vitro tests indicate that gabapentin can partially attenuate the effects of the glutamate receptor agonist N-methyl-D-aspartate, but this pattern is only true for concentrations above 100 μmol, which cannot be achieved in vivo.
Gabapentin is able to slightly reduce the release of monoamine neurotransmitters and modify the activity of the enzymes glutamate synthetase and GABA synthetase in vitro. Experiments on rats indicate an increase in GABA metabolism in some parts of the brain, however, the significance of these effects for the anticonvulsant activity of gabapentin has not been established. In animals, this substance is able to easily penetrate into the brain tissue and prevent seizures that are caused by genetic factors or caused by chemical drugs (including inhibitors of GABA synthesis) or maximum electric shock.
Pharmacokinetics
The drug is rapidly absorbed, and the maximum plasma concentration is observed after 3 hours. After repeated administration, to achieve maximum concentration, it is necessary 1 hour less than with a single dose. The absolute bioavailability of gabapentin in capsules is approximately 60%. With an increase in the dose of the drug, the bioavailability of this substance decreases.
The simultaneous intake of Tebantin with food, including those containing a large amount of fat, increases the C max and AUC of gabapentin by about 14% and at the same time does not significantly affect the pharmacokinetics of the substance.
When taking 300–4800 mg of gabapentin, the average values of AUC and C max increase with increasing dose. At doses no more than 600 mg, the deviation from the linearity of both indicators is small, and at high doses, the increase is not so significant.
With a single oral dose, the plasma concentration of the drug in children 4–12 years of age is similar to that in adult patients. The equilibrium state with repeated doses was achieved after 1-2 days and was maintained during the entire course of therapy.
In the human body, gabapentin is practically not metabolized. In addition, this substance does not have the ability to induce mixed liver oxidative enzymes, which are involved in the metabolism of drugs.
Gabapentin is practically unable to bind to plasma proteins (less than 3%), and its volume of distribution is 57.7 liters. The concentration of gabapentin in the cerebrospinal fluid is 20% of the plasma concentration at equilibrium. This substance can cross the blood-brain barrier and pass into breast milk.
The elimination of Tebantine from plasma has a linear relationship. The half-life is independent of dose and ranges from 5 to 7 hours. Plasma clearance, renal clearance, and gabapentin clearance rate constant are directly proportional to creatinine clearance. Gabapentin is excreted unchanged through the kidneys and is also removed from plasma by hemodialysis.
In elderly patients and patients with impaired renal function, the clearance of gabapentin from plasma is reduced. With a creatinine clearance less than 30 ml / min, the half-life is approximately 52 hours. When treating patients with impaired renal function and those on hemodialysis, dose adjustment is recommended.
Indications for use
- partial epileptic seizures with secondary generalization (or without it) in children over 12 years of age and adult patients - monotherapy or additional treatment;
- partial epileptic seizures with secondary generalization (or without it) in children 3–12 years of age - additional treatment;
- neuropathic pain in adult patients over 18 years of age - relief and treatment.
Contraindications
Absolute:
- inflammation of the pancreas (pancreatitis) in acute form;
- lactation (breastfeeding period);
- children under 3 years of age (all types of therapy);
- children age 3–12 years (monotherapy);
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
- hypersensitivity to gabapentin and ancillary components of the drug.
The drug should be used with caution in patients with impaired renal function.
During pregnancy, Tebantin is used only if the intended benefit to the mother exceeds the possible risk to the fetus.
Instructions for the use of Tebantine: method and dosage
Tebantin capsules are taken orally, without chewing, with a sufficient amount of liquid. The effectiveness of the drug does not depend on the diet. When taking three doses, it is important to take into account that the interval between two doses should not be more than 12 hours.
Partial seizures in children over 12 years of age and adults
For children over 12 years of age and adult patients, a clinically significant desired antiepileptic effect is usually provided by a dose of 900–1200 mg / day, several days after the start of titration.
Recommended daily dose and basic dosing regimen (A):
- Day I: 300 mg - 1 time per day for 1 capsule of 300 mg or 3 times per day for 1 capsule of 100 mg;
- II day: 600 mg - 2 times a day, 1 capsule 300 mg, or 3 times a day, 2 capsules 100 mg;
- III day: 900 mg - 3 times a day, 1 capsule 300 mg, or 3 times a day, 3 capsules 100 mg;
- IV day and beyond: the dose can be increased to 1200 mg by dividing in equal doses into 3 doses (for example, 3 times a day, 1 capsule 400 mg).
Alternative dosage regimen (B): on the 1st day of therapy, a starting dose of 900 mg of gabapentin per day is taken, divided into 3 doses of 1 capsule 300 mg; the next day, the dose can be increased to 1200 mg per day and then (depending on the effect obtained) increased per day by 300-400 mg, but not exceeding the maximum daily dose of 2400 mg (with three doses). The efficacy and safety of using higher doses of the drug have not been studied enough.
Partial convulsions in children 3-12 years old with a body weight of more than 17 kg
Tebantin is used in children from 3 to 12 years old with a body weight> 17 kg for additional therapy, since there is insufficient data on the safety and efficacy of its use in this age group as a monotherapy.
The recommended daily dose of the drug is 25–35 mg / kg and is divided into 3 doses.
Scheme for choosing an effective dose using titration: 1st day - 10 mg / kg / day, 2nd day - 20 mg / kg / day, 3rd day - 30 mg / kg / day. If necessary, in the future, the daily dose of gabapentin can be increased to 35 mg / kg / day, divided into 3 doses. Long-term clinical studies confirm good tolerance of doses up to 40-50 mg / kg / day.
Initial dosing regimen before reaching therapeutic doses of gabapentin (recommended daily doses of gabapentin depending on body weight):
- children weighing 17-25 kg (600 mg per day): 1st day - 200 mg once a day, 2nd day - 200 mg 2 times a day, 3rd day - 200 mg 3 times a day;
- children weighing more than 26 kg (900 mg per day): 1st day - 300 mg once a day, 2nd day - 300 mg 2 times a day, 3rd day - 300 mg 3 times a day.
Maintenance doses of Tebantin (child's weight / dose): 17-25 kg - 600 mg / day, 26-36 kg - 900 mg / day, 37-50 kg - 1200 mg / day, 51-72 kg - 1800 mg / day.
Neuropathic pain
In the treatment of neuropathic pain, the attending physician determines the optimal therapeutic dose by titration based on the patient's individual response, drug tolerance and efficacy. The dose can be up to 3600 mg per day (maximum).
Recommended daily dose and basic dosing regimen (A):
- Day I: 300 mg - 1 time per day for 1 capsule of 300 mg or 3 times per day for 1 capsule of 100 mg;
- II day: 600 mg - 2 times a day, 1 capsule 300 mg, or 3 times a day, 2 capsules 100 mg;
- III day: 900 mg - 3 times a day, 1 capsule 300 mg, or 3 times a day, 3 capsules 100 mg.
An alternative dosing regimen for the treatment of intense pain (B): on the 1st day, a starting daily dose of 900 mg of gabapentin (divided into 3 doses) is taken, then the dose can be increased over 7 days to 1800 mg per day.
In order to achieve the required analgesic effect, in some cases, the dose can be increased to a maximum of 3600 mg per day, divided into 3 doses. In ongoing clinical studies, the dose was increased to 1800 mg during the 1st week, and to 2400 and 3600 mg, respectively, during the 2nd and 3rd weeks.
Weakened patients, patients with low body weight or after organ transplantation are allowed to increase the dose of Tebantin strictly by 100 mg per day.
In renal failure with creatinine clearance (CC) <80 ml / min, for hemodialysis patients and the elderly (due to age-related decrease in CC), the doctor selects the therapeutic dose individually.
Side effects
Partial seizure treatment
- general malaise: back / chest pain, increased fatigue, flu-like syndrome, fever, asthenia, feeling unwell;
- central nervous system (CNS): drowsiness / insomnia, headache, dizziness, ataxia, depression, emotional lability, increased nervous excitability, tremor, muscle twitching, hyperkinesis, dysarthria, impaired coordination, hallucinations, movement disorders (choreoathetosis, dyskinesia, dystonia), impaired thinking, confusion, paresthesia, nystagmus, tics (dose-dependent), hyperkinesia, increased, weakened or absent reflexes, anxiety, anxiety, hostility, amnesia;
- digestive system: nausea / vomiting, dyspepsia, abdominal pain, increased appetite, dry mouth or throat, diarrhea / constipation, dental lesions, hepatitis, jaundice, pancreatitis, increased liver transaminase activity, flatulence, gingivitis, anorexia;
- cardiovascular system: symptoms of vasodilation, palpitations, as part of complex therapy - increased blood pressure (BP);
- hematopoietic system: thrombocytopenia, leukopenia;
- musculoskeletal system: myalgia, arthralgia, fractures;
- respiratory system: rhinitis, pharyngitis; as part of complex therapy with other antiepileptic drugs - cough, pneumonia;
- sense organs: noise / ringing in the ears, visual impairment (diplopia, amblyopia);
- urinary system: impaired urinary control, acute renal failure; as part of complex therapy with other antiepileptic drugs - urinary tract infections;
- reproductive system: impotence, gynecomastia, an increase in the volume of the mammary glands;
- hypersensitivity reactions: urticaria, skin rash, pruritus, fever, angioedema, exudative erythema multiforme (including Stevens-Johnson syndrome);
- other reactions: weight gain, purpura, discoloration of tooth enamel, generalized edema, peripheral edema, facial edema, alopecia, acne, fluctuations in blood glucose concentration in diabetes mellitus.
Hyperkinesia and hostility have been reported with gabapentin as adjunctive therapy in children under 12 years of age.
Treating neuropathic pain
- general malaise: asthenia, infections, flu-like syndrome, headache, accidental injuries, pain of various localization, back pain;
- digestive system: dyspepsia, constipation / diarrhea, dry mouth, nausea / vomiting, flatulence, abdominal pain;
- nervous system: disorientation, gait disturbance, paresthesia, thought disorder, drowsiness, tremor;
- sense organs: amblyopia;
- respiratory system: shortness of breath, pharyngitis;
- metabolism: weight gain, peripheral edema;
- dermatological reactions: skin rash.
After a sharp withdrawal of Tebantin, the following are most often observed: nausea, insomnia, anxiety, pains of various localization, hyperhidrosis.
Overdose symptoms are: double vision, dizziness, speech impairment, diarrhea, drowsiness and lethargy. For the treatment of the condition, symptomatic therapy is recommended; in severe renal failure, hemodialysis may be indicated. Symptoms of acute life-threatening poisoning were not observed even after taking 49 g of the drug per day.
Overdose
Even after taking 49 g of Tebantine per day, no symptoms of life-threatening acute poisoning were observed.
In case of an overdose, speech impairment, double vision, dizziness, diarrhea, drowsiness and lethargy appear. Symptomatic treatment is recommended. When treating patients with severe renal failure, hemodialysis is possible.
special instructions
It is not necessary to measure the concentration of the drug in the plasma when selecting the optimal therapeutic dose.
Therapy for absence epilepsy with gabapentin is ineffective.
The use of gabapentin in patients with diabetes mellitus requires control of blood glucose levels and, in some cases, dose adjustment of the hypoglycemic drug.
With the appearance of prolonged abdominal pain, nausea, repeated vomiting (the first signs of acute pancreatitis), treatment with Tebantin must be discontinued. For early diagnosis of acute pancreatitis, a thorough examination (clinical and laboratory tests and tests) is required.
Patients with lactose intolerance should take into account its content in 1 Tebantin capsule, depending on the dose: 100 mg - 22.14 mg of lactose, 300 mg - 66.42 mg of lactose, 400 mg - 88.56 mg of lactose.
It is necessary to reduce the dose of the drug, stop treatment or replace gabapentin with an alternative drug gradually, for at least 1 week. With abrupt discontinuation, status epilepticus may develop.
The drug should be discontinued and seek medical advice if dizziness, drowsiness, ataxia, increased fatigue, nausea / vomiting, weight gain in adult patients appear, in children - hyperkinesia, drowsiness, hostility.
The efficacy and safety of Tebantin's use as a drug for adjunctive therapy of epilepsy in children under 3 years of age, as a drug for monotherapy in children under 12 years of age, and for the treatment of neuropathic pain in children and adolescents under 18 years of age have not been established.
During the period of treatment from engaging in potentially hazardous types of work that require speed of psychomotor reactions and increased concentration of attention, including from driving, it is necessary to refrain.
Application during pregnancy and lactation
There is no information on the use of Tebantin in the treatment of pregnant women, therefore, during this period, the drug is prescribed only for health reasons.
Gabapentin passes into breast milk, but there is no data on the effect of the substance on breastfed babies. During lactation, Tebantin is prescribed only in cases where the benefits to the mother outweigh the possible harm to the child.
Pediatric use
It is forbidden to use the drug in the treatment of children under 3 years of age and with monotherapy in children aged 3–12 years.
There are no data on the safety and efficacy of using Tebantine in the treatment of neuropathic pain in children under 18 years of age.
With impaired renal function
According to the instructions, Tebantin should be used with caution when treating patients with renal insufficiency. For patients with impaired renal function and those on hemodialysis, it is necessary to adjust the dose of the drug.
Use in the elderly
Due to the age-related decrease in creatinine clearance, the recommended dose of the drug for elderly patients should be selected individually.
Drug interactions
- phenytoin, valproic acid, carbamazepine, phenobarbital (antiepileptic drugs): no interaction with gabapentin was observed;
- oral contraceptives: gabapentin does not affect the effectiveness of oral contraceptives containing norethisterone / ethinyl estradiol and their pharmacokinetics, but deterioration / termination of their contraceptive effect is possible when Tebantin is used as part of complex therapy with other antiepileptic drugs that reduce the effect of oral contraceptives;
- antacids (magnesium or aluminum-containing agents that neutralize the acidity of the stomach): reduce the bioavailability of gabapentin by 24% (capsules should be taken 2 hours after antacids);
- cimetidine: the excretion of gabapentin by the kidneys decreases, which may not be of clinical significance;
- alcohol, other drugs that affect the central nervous system: can increase such unwanted side effects of gabapentin on the nervous system, such as drowsiness, ataxia;
- probenecid: no effect on renal excretion of gabapentin;
- morphine: when taking morphine in the form of 60 mg controlled-release capsules 2 hours before taking Tebantin, there was a 44% increase in gabapentin AUC compared with gabapentin monotherapy, as a result of which the pain threshold increased (cold pressor test), but the clinical significance of such changes not installed. Gabapentin administered 2 hours after morphine does not alter the pharmacokinetic characteristics of the latter, and the side effects do not differ from those observed with morphine and placebo.
Laboratory results for the determination of protein in urine: in the case of using the drug Tebantin as part of complex therapy with other anticonvulsants, false-positive results of determining the total protein in urine using semi-quantitative tests were noted; it is recommended to use a more specific precipitation method with a 20% sulfosalicylic acid solution or a biuret sample.
Analogs
Analogues of Tebantin are: Gabapentin, Gabagamma, Konvalis, Katena, Neurontin, Eplirontin, Egipentin, etc.
Terms and conditions of storage
Store out of the reach of children at room temperature.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tebantin
Reviews of Tebantin as a drug for combating neuropathic pain indicate its high effectiveness, but the main condition is compliance with the doctor's recommendations. The most common side effects are drowsiness and dizziness.
Reviews of patients who used the drug for the treatment of epileptic seizures are quite contradictory: some patients report a decrease in the severity and frequency of seizures, others do not observe any changes in their health.
The price of Tebantin in pharmacies
The price for Tebantin is about 900 rubles for a pack of 50 capsules and 1650-1780 rubles for a pack of 100 capsules.
Tebantin: prices in online pharmacies
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Drug name Price Pharmacy |
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Tebantine 300 mg capsule 50 pcs. 705 RUB Buy |
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Tebantin capsules 300mg 50 pcs. RUB 810 Buy |
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Tebantine 300 mg capsule 100 pcs. 1268 RUB Buy |
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Tebantin capsules 300mg 100 pcs. 1466 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
