Pharmacological action Gabapentin 300 mg
Antiepileptic drug. On the chemical structure is similar to GABA, inhibitory neurotransmitter function executes in the CNS. It is believed that the mechanism of action of gabapentin is different from other anticonvulsants acting through synapses GABA (including valproate, barbiturates, benzodiazepines, GABA-transaminase inhibitors, inhibitors of the capture of GABA, GABA agonists and prodrugs of GABA). In in vitro studies showed that gabapentin is characterized by a new peptide binding sites in rat brain tissues, including the hippocampus and cerebral cortex, which may be relevant to the anticonvulsant activity of gabapentin and its derivatives. Gabapentin in clinically relevant concentrations is not associated with other conventional drugs, and neurotransmitter receptors in the brain, including with GABAA-, GABAB-, benzodiazepine receptors, with NMDA-receptors.
Finally, the mechanism of action of gabapentin is not installed.
Pharmacokinetics Gabapentin 300 mg
Gabapentin is absorbed from the gastrointestinal tract. After oral administration of gabapentin in plasma Cmax achieved within 2-3 h. The absolute bioavailability of approximately 60%. Reception in conjunction with diet (including high-fat diet) has no effect on the pharmacokinetics of gabapentin.
Gabapentin is not bound to plasma proteins and has Vd 57.7 l. In patients with epilepsy gabapentin concentration in the cerebrospinal fluid of 20% from the corresponding plasma Css at the end of the dosing interval.
Gabapentin is displayed only by the kidneys. Signs of the biotransformation of gabapentin in humans have been found. Gabapentin does not induce the oxidases involved in the metabolism of drugs. Withdrawal of the drug is best described by a linear model. T1 / 2 is independent of dose and amounts to an average of 5-7 hours
Gabapentin clearance is reduced in the elderly and in patients with impaired renal function. Constant rate of excretion, plasma and renal clearance of gabapentin is directly proportional to creatinine clearance.
Gabapentin is removed from plasma by hemodialysis.
The concentrations of gabapentin in the plasma of children were similar to adults.
Statement Gabapentin 300 mgGabapentin 300 mg
Treatment of neuropathic pain in adults over the age of 18 years of partial seizures with monotherapy with secondary generalization, and without her children and adults older than 12 years as an adjunct in the treatment of partial seizures with secondary generalization, and without her children and adults at the age of 3 years and older.
Dosage regimen Gabapentin 300 mg
Individual, depending on the indications and treatment regimens.
Side effect Gabapentin 300 mg
From the central and peripheral nervous system: Amnesia, ataxia, confusion, impaired coordination, depression, dizziness, dysarthria, increased nervous irritability, nystagmus, drowsiness, impaired thinking tremors, convulsions, amblyopia, diplopia, hyperkinesia, strengthening, weakening or lack of reflexes, paresthesia, anxiety, hostility, impaired gait.
From the digestive system: the change of teeth staining, diarrhea, increased appetite, dry mouth, nausea, vomiting, flatulence, anorexia, gingivitis, abdominal pain, pancreatitis, changes in liver function tests.
From the hemopoietic system: leucopenia, decrease the number of leukocytes, thrombocytopenic purpura.
The respiratory system: rhinitis, pharyngitis, cough, pneumonia.
With the Musculoskeletal System: myalgia, arthralgia, bone fractures.
Cardio-vascular diseases: hypertension, manifestations of vasodilation.
The urinary system: urinary tract infections, urinary incontinence.
Allergic reactions: erythema multiforme, Stevens-Johnson syndrome.
Dermatological reactions: maceration of the skin, acne, pruritus, rash.
Other: back pain, fatigue, peripheral edema, impotence, fatigue, malaise, swelling of the face, weight gain, accidental injury, asthenia, flu-like symptoms, fluctuations in blood glucose in children – a viral infection, otitis media.
Contraindications Gabapentin 300 mg
Hypersensitivity to gabapentin.
Pregnancy and breastfeeding Gabapentin 300 mg
Adequate and well controlled studies on the safety of gabapentin during pregnancy and lactation in humans has not been carried out. If necessary, use during pregnancy and lactation should carefully weigh the potential benefits of therapy for the mother and the potential risk to the fetus or infant.
Gabapentin is excreted in breast milk. When used in lactation of gabapentin on the nature of the infant is not installed.
Cautions Gabapentin 300 mg
The abrupt cessation of therapy, anticonvulsant drugs in patients with partial seizures can induce convulsive status. If necessary, reduce the dose of gabapentin or cancel replace it with an alternative means should be phased in over at least 1 week.
Gabapentin is not an effective treatment for absansnyh seizures.
In a joint application with other anticonvulsant drugs have been reported false-positive test results determination of protein in the urine. To determine the protein in the urine is recommended to use a specific method of sulfosalicylic acid precipitation.
Patients with impaired renal function, as well as patients on hemodialysis require adjustment of dosing regimen.
Elderly patients may require adjustment of dosage regimen of gabapentin due to the fact that such patients may decrease the renal clearance.
Efficacy and safety of treatment of neuropathic pain in patients under the age of 18 is not installed.
Efficacy and safety of gabapentin monotherapy for the treatment of partial seizures in children under the age of 12 years and adjunctive therapy in the treatment of gabapentin partial seizures in children under 3 years of age have not been established.
In the period of treatment to avoid alcohol.
Effects on ability to drive and control mechanisms
Prior to determining individual response to treatment the patient should refrain from potentially dangerous activities associated with the need to focus and increased speed of psychomotor reactions.
Drug Interactions Gabapentin 300 mg
While the use of antacids reduce the absorption of gabapentin from the gastrointestinal tract.
While the use of felbamate may increase the T1 / 2 of felbamate.
With simultaneous application described a case raising the concentration of phenytoin in blood plasma.
