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dosage form Capsules Composition Gabapentin 300 mg
The composition of the gelatin capsule: gelatin, colourant iron oxide red (E172), yellow iron oxide colorant (E172), titanium dioxide (E172). pharmachologic effect The antiepileptic drug. Gabapentin is similar in structure to the neurotransmitter gamma-aminobutyric acid (GABA). It is a lipophilic substance. However, its mechanism of action differs from that of some other drugs that interact with GABA-receptors, including valproic acid drugs, barbiturates, benzodiazepines, inhibitors of GABA-transferase reuptake inhibitors GABA, agonists GABA and prodrugs of GABA: it has no GABA-ergic properties and no effect on seizure metabolism and GABA. Preliminary studies suggest that gabapentin is associated with alpha2-gamma subunit of voltage-gated calcium channels and inhibits the flow of calcium ions, which plays an important role in the onset of neuropathic pain. Other mechanisms involved in the action of gabapentin for neuropathic pain are: glutamatzavisimoy decrease neuronal death, increasing the synthesis of GABA, inhibition of monoamine neurotransmitter release group. Gabapentin at clinically relevant concentrations does not bind to receptors of other common drugs or neurotransmitters including receptors GABAA and GABAV, benzodiazepine, glutamate, glycine, or NMDA.
Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro. Gabapentin partial agonist effects attenuated NMDA-glutamate receptors in some tests in vitro, but only at a concentration of more than 100 micromoles, which is not achieved in vivo. Gabapentin decreases somewhat monoamine neurotransmitter release activity and modifies the enzyme GABA-synthetase and glutamate synthase in vitro. Use of gabapentin in the rat resulted in an increase in GABA metabolism of certain areas of the brain; This effect was similar to that of valproic acid, although observed in other brain regions. The significance of these effects of gabapentin to its anticonvulsant activity is not established. Animals gabapentin easily penetrate brain tissue and prevents seizures induced by maximal electroshock, chemical agents, including inhibitors of the synthesis of GABA, as well as due to genetic factors. Pharmacokinetics Suction
At intake — fast absorption. Cmax is reached after 3 hours, regardless of the dose, received repeated doses at the time to reach Cmax Bioavailability 1 hour is not proportional to dose:. Declines with increasing dose.
The absolute bioavailability of gabapentin capsules is approximately 60%. Food intake (including high fat) has no significant effect on the pharmacokinetics, in such cases there is an increase in AUC and Cmax by 14%.
Before the drug at a dose of 300-4800 mg of mean values Cmax and AUC values increase with increasing dose. The deviation from linearity for both parameters is very low at doses not exceeding 600 mg; at high doses significantly less increase.
Gabapentin is almost bound to plasma proteins (less than 3%), Vd — 57.7 liters. concentration in CSF is 20% of the plasma Css.
It penetrates through the blood-brain barrier, excreted in breast milk.
Ggabapentin practically not metabolized in the human body and induces oxidative hepatic mixed function enzymes involved in the metabolism of drugs.
Elimination from the plasma after the / in the introduction is linear. T1 / 2 — 7.5 h, depending on the dose. The elimination rate constant, plasma clearance, and renal clearance are directly proportional to gabapentin QC. Gabapentin is excreted by the kidneys unchanged. Removed from plasma by hemodialysis.
Pharmacokinetics in special clinical situations
When receiving a single dose of gabapentin plasma concentration of the drug in children from 4 to 12 years is similar to that in adult patients. Repeated receptions saturation stage is reached after 1-2 days and is maintained throughout the course of treatment
Gabapentin plasma clearance is reduced in elderly patients and in patients with impaired renal function. When CC less than 30 ml / min, T1 / 2 is about 52 hours. In patients with impaired renal function and patients on hemodialysis, dose adjustment is recommended. Side effects In the treatment of partial seizures
From the central and peripheral nervous system: drowsiness, dizziness, headache, amnesia, ataxia, depression, emotional lability, increased nervous irritability, nystagmus (dose-dependent), tremor, muscle twitching, hyperkinesia, dysarthria, impaired coordination, hallucinations, movement disorders ( choreoathetosis, dyskinesia, dystonia), abnormal thinking, confusion, tics, paresthesia (dose-dependent), hyperkinesia, strengthening, weakening or absence of reflexes, anxiety, restlessness, hostility, insomnia. In addition, children under 12 years are marked hostility and hyperkinesia.
From the digestive system: nausea, vomiting, abdominal pain, dyspepsia, increased appetite, dry mouth or throat, constipation, diarrhea, destruction of teeth, pancreatitis, hepatitis, jaundice, elevated liver transaminases, flatulence, anorexia, gingivitis, color change tooth enamel.
Cardio-vascular system: palpitation, vasodilation symptoms. In the appointment of other drugs — increase in blood pressure.
From the Musculoskeletal System: arthralgia, myalgia, fractures.
The respiratory system: pharyngitis, rhinitis, the appointment with other antiepileptic drugs — cough, pneumonia.
From the senses: blurred vision (amblyopia, diplopia), tinnitus. sale Properties prescription Special conditions In the process of selecting the optimal therapeutic dose is not necessary in the measurement of drug concentrations in plasma.
The drug is ineffective in absence seizures.
In the application of gabapentin need to control blood glucose levels in diabetic patients; 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) should stop treatment with gabapentin. It is necessary to conduct a thorough examination of the patient (clinical and laboratory tests) for early diagnosis of acute pancreatitis.
If lactose intolerance should be noted that 1 caps. (100 mg) contains 22.14 mg of lactose, 1 caps. (300 mg) — 66.42 mg of lactose, and 1 caps. (400 mg) — 88.56 mg lactose.
Reduce the dose of the drug to cancel or replace the other alternative means should be phased in over at least 1 week. Abrupt discontinuation of treatment may provoke status epilepticus.
In the event of symptoms in adults somnolence, ataxia, dizziness, fatigue, nausea and / or vomiting, weight gain and drowsiness in children, hyperkinesia and hostility, you should stop taking the drug and consult a doctor.
Use in Pediatrics
Safety and efficacy of gabapentin in children aged up to 3 years up to 12 years as adjunctive therapy of epilepsy and in children have not been established as a monotherapy.
Safety and efficacy of treatment of neuropathic pain in patients under the age of 18 years have not been established.
Effects on ability to road management and operation mechanisms
During treatment, patients should refrain from driving motor vehicles and activities potentially hazardous activities that require high concentration and psychomotor speed reactions. testimony — Partial seizures with secondary generalization or without it in adults and children over 12 years as monotherapy or adjunctive therapy;
— Partial seizures with secondary generalization or without children from 3 to 12 years as an adjunctive therapy;
— Neuropathic pain in patients older than 18 years (effectiveness and safety in patients below the age of 18 years have not been established). Dosage When partial seizures in adults and children over 12 years of antiepileptic effect is provided when using the drug at a dose of 900-1200 mg / Optimum therapeutic benefit is achieved within a few days after the titration. Recommended dosage regimens: A. Day 1 — 300 mg of gabapentin (300 mg 1 time / 100 mg or 3). In the 2nd day — 600 mg of gabapentin (300 mg, 2 mg or 200 3). The 3rd day — 900 mg of gabapentin (300 mg 3). On the 4th day of the daily dose can be increased up to 1200 mg in 3 doses (400 mg 3) or B. In the 1st day initial dose — 300 mg 3 times, i.e. 900 mg / daily dose can then be increased to 1200 mg. Depending on the resulting effect of the dose can be increased to 300-400 mg / but not exceeding a total daily dose of 2400 mg (3 doses), which is due to insufficient data on the efficacy and safety of the drug in higher doses. As adjunctive therapy in children aged 3-12 years and a body weight more than 17 kg the recommended daily dose is 25-35 mg / kg / in 3 divided doses. Table 2 lists the recommended daily doses Tebantin® preparation depending on their body weight. The effective therapeutic dose titration is achieved as follows: Day 1 — 10 mg / kg / day 2 — 20 mg / kg / day 3 — 30 mg / kg / according to the method given in the table. Then, if necessary, the daily dose of the drug can be increased Tebantin® to 35 mg / kg / in 3 divided doses. These long-term clinical studies have confirmed the good tolerability Tebantin® drug in doses of 40-50 mg / kg /