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Active ingredients
Gabapentin
Release form
Capsules
Composition
Gabapentin 300 mg.; Excipients: lactose monohydrate, corn starch, talc.; Capsule shell composition: titanium dioxide (E171), iron dye yellow oxide (E172), gelatin.
Pharmacological effect
Antiepileptic drug. The chemical structure is similar to GABA, which serves as a brake mediator in the central nervous system. The mechanism of action of gabapentin is believed to be different from other anticonvulsant drugs acting through GABA synapses (including valproate, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA trapping inhibitors, GABA agonists and GABA prodrugs). In vitro studies have shown that gabapentin is characterized by the presence of a new peptide binding site in rat brain tissues, including the hippocampus and cerebral cortex, which may be related to the anticonvulsant activity of gabapentin and its derivatives. At clinically relevant concentrations, gabapentin does not bind to other conventional drugs and neurotransmitter receptors in the brain, incl. with GABAA-, GABAB-, benzodiazepine receptors, with NMDA-receptors.; Finally, the mechanism of action of gabapentin is not installed.
Pharmacokinetics
Gabapentin is absorbed from the gastrointestinal tract. After oral ingestion, Cmax gabapentin in plasma is reached in 2–3 hours. Absolute bioavailability is about 60%. Reception simultaneously with food (including those with a high content of fat) does not affect the pharmacokinetics of gabapentin.; Gabapentin does not bind to plasma proteins and has a Vd of 57.7 liters. In patients with epilepsy, the concentration of gabapentin in the cerebrospinal fluid is 20% of the corresponding Css in plasma at the end of the dosing interval.; Gabapentin is excreted only by the kidneys. No signs of gabapentin biotransformation were detected in humans. Gabapentin does not induce oxidases involved in drug metabolism. Removal of the drug is best described using a linear model. T1 / 2 does not depend on the dose and averages 5-7 hours. The clearance of gabapentin decreases in the elderly and in patients with impaired renal function. The removal rate constant, plasma and renal clearance of gabapentin is directly proportional to creatinine clearance.; Gabapentin is removed from plasma by hemodialysis.; The values of gabapentin plasma concentrations in children were similar to adults.
Indications
Treatment of neuropathic pain in adults (18 years and older).Efficacy and safety in patients under the age of 18 years have not been established; monotherapy of partial seizures with epilepsy with secondary generalization and without it in adults and children over the age of 12 years. The efficacy and safety of monotherapy in children under the age of 12 years have not been established; as an additional tool in the treatment of partial seizures with epilepsy with secondary generalization and without it in adults and children aged 3 years and older. The safety and efficacy of additional gabapentin therapy in children less than 3 years old has not been established.
Contraindications
children up to 3 years; hypersensitivity to gabapentin or auxiliary components of the drug. With caution should be prescribed the drug for renal failure; Application for violations of renal function; Precautions should be prescribed the drug for renal failure .; Patients on hemodialysis who have not previously taken gabapentin, the drug is recommended to be prescribed in a saturating dose of 300-400 mg, and then apply it to 200-300 mg every 4 hours of hemodialysis.
Use during pregnancy and lactation
Adequate and strictly controlled studies on the safety of gabapentin during pregnancy and lactation in humans have not been conducted. If necessary, use during pregnancy and lactation should carefully weigh the expected benefits of therapy for the mother and the potential risk to the fetus or infant.; Gabapentin is excreted in breast milk. When applied during lactation, the nature of the action of gabapentin on an infant has not been established.
Dosage and administration
The drug Katena; prescribed inside, regardless of the meal. If it is necessary to reduce the dose, discontinue the drug or replace it with an alternative means, this should be done gradually over at least one week .; Neuropathic pain in adults; The initial daily dose is 900 mg (in 3 doses in equal doses); if necessary, depending on the effect, the dose is gradually increased to the maximum - 3.6 g / day. Treatment can begin immediately with a dose of 900 mg / day (300 mg 3 times / day) or during the first 3 days the dose can be increased gradually to 900 mg per day according to the following scheme: Day 1: 300 mg 1 time / day; 2nd day: 300 mg 2 times / day; 3rd day: 300 mg 3 times / day; Partial seizures; Adults and children over the age of 12; Effective dose - from 900 mg to 3.6 g per day. Therapy can be started with a dose of 300 mg 3 times / day on day 1 or gradually increased to 900 mg according to the scheme described above (seesection Neuropathic pain in adults). Subsequently, the dose may be increased to the maximum - 3.6 g / day in 3 doses in equal doses. The maximum interval between doses when taking the drug three times should not exceed 12 hours in order to avoid the resumption of seizures. Good tolerability of the drug in doses up to 4.8 g / day was noted; Children aged 3-12 years; The initial dose of the drug varies from 10 to 15 mg / kg / day, which is prescribed in equal doses 3 times / day and increased to effective for approximately 3 days. The effective dose of gabapentin in children aged 5 years and older is 25-35 mg / kg / day in equal doses in 3 doses. The effective dose of gabapentin in children aged 3 to 5 years is 40 mg / kg / day in equal doses of 3 doses. There was a good tolerability of the drug in doses up to 50 mg / kg / day with prolonged use. The maximum interval between doses of the drug should not exceed 12 hours in order to avoid the resumption of seizures .; There is no need to control the concentration of gabapentin in plasma. The drug Katena; can be used in combination with other anticonvulsants without taking into account changes in its plasma concentration or concentration of other anticonvulsant drugs in serum .; Selection of doses for renal failure; Patients with renal insufficiency are recommended to reduce the dose of gabapentin according to the table .; Creatinine clearance (ml / min) Daily dose (mg / day) *;> 80 900-3600; 50-79 600-1800; 30-49 300-900; 15-29 150 ** - 600; 150 ** - 300 ; * The daily dose should be prescribed in 3 doses .; ** Assign 300 mg every other day .; Patients on hemodialysis who have not previously taken gabapentin, the drug is recommended to be prescribed in a saturating dose of 300-400 mg, and then apply it to 200-300 mg every 4 hours of hemodialysis.
Side effects
Since the cardiovascular system: the symptoms of vasodilation, hypertension .; On the part of the digestive system: dyspepsia, flatulence, nausea, vomiting, abdominal pain, constipation, diarrhea, dry mouth or throat, anorexia, gingivitis, dental disease, increased appetite, increased activity of hepatic transaminases .; On the part of the musculoskeletal system: myalgia, arthralgia, back pain, increased bone fragility .; Nervous system disorders: drowsiness, dizziness, ataxia, amnesia, confusion, incoordination,fatigue, impaired thinking, tremor, hypoesthesia, depression, dysarthria, insomnia, nervousness, nystagmus, strengthening, weakening or absence of reflexes, asthenia, anxiety, hostility, hyperkinesia, emotional lability .; On the part of the respiratory system: pharyngitis, rhinitis, shortness of breath, cough, pneumonia, bronchitis, respiratory infections .; On the part of the genitourinary system: urinary tract infections, impotence .; From the senses: blurred vision, amblyopia, diplopia .; On the part of the blood-forming organs: leukopenia, purpura (most often it is described as bruises that occurred during physical trauma) .; Allergic reactions: skin rash, itching, acne .; Other: fever, viral infection, weight gain, pain of different localization, peripheral edema, swelling of the face, headache .; Post-registration application experience; There have been cases of sudden unexplained death, whose connection with treatment with gabapentin has not been established .; Other adverse effects: acute renal failure, allergic reactions, including urticaria, alopecia, angioedema, generalized edema; fluctuations in blood glucose concentrations in patients with diabetes mellitus, chest pain, an increase in the volume of the mammary glands, gynecomastia, increased liver function, exudative erythema multiforme (including Stevens-Johnson syndrome), hallucinations, movement disorders such as choreoathetosis , dyskinesia and dystonia, palpitations, pancreatitis, tinnitus, thrombocytopenia, urinary incontinence, myoclonus.
Overdose
Currently, no cases of overdose have been reported.
Interaction with other drugs
With simultaneous use with antacids, the absorption of gabapentin from the gastrointestinal tract decreases.; With simultaneous use with felbamate, an increase in T1 / 2 of felbamate is possible.; With simultaneous use, a case of increasing the concentration of phenytoin in plasma is described.
special instructions
Abrupt cessation of anticonvulsant therapy in patients with partial seizures may provoke a convulsive status. If necessary, reduce the dose, cancel gabapentin or replace it with an alternative means should be gradually for at least 1 week.; Gabapentin is not effective for the treatment of absence convulsive seizures. When used together with other anticonvulsants, false-positive results of the test were recorded protein in the urine.To determine the protein in the urine, it is recommended to use a more specific method of precipitation of sulfosalicylic acid. this category of patients may have reduced renal clearance.; The efficacy and safety of the treatment of neuropathic pain in patients under the age of 18 years have not been established. and the safety of monotherapy with gabapentin in the treatment of partial seizures in children under 12 years of age and additional therapy with gabapentin in the treatment of partial seizures in children under 3 years of age have not been established; and control mechanisms; Until an individual response to treatment is determined, the patient should refrain from potentially hazardous activities associated with the need for concentration and increased speed sihomotornyh reactions.