This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antiepileptic agent. The chemical structure is similar to GABA, which acts as a braking mediator in the central nervous system. It is believed that the mechanism of action of gabapentin differs from other anticonvulsants acting through GABA synapses (including valproate, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA capture 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 the brain tissues of rats, including the hippocampus and the cerebral cortex, which may be related to the anticonvulsant activity of gabapentin and its derivatives. Gabapentin in clinically significant concentrations does not bind to other conventional drugs and neurotransmitter receptors in the brain, including.with GABA A -, GABA B -, benzodiazepine receptors, with NMDA receptors.
Finally, the mechanism of action of gabapentin is not established.
PHARMACOKINETICS
Gabapentin is absorbed from the digestive tract. After ingestion C max gabapentin in plasma is achieved after 2-3 hours. Absolute bioavailability is about 60%.Admission simultaneously with food (including high-fat) does not affect the pharmacokinetics of gabapentin.
Gabapentin does not bind to plasma proteins and has a V d of 57.7 liters. In patients with epilepsy, the concentration of gabapentin in the cerebrospinal fluid is 20% of the corresponding C ss in the plasma at the end of the dosing interval.
Gabapentin is excreted only by the kidneys. There are no signs of biotransformation of gabapentin in the human body. Gabapentin does not induce oxidases involved in the metabolism of drugs. The elimination of the drug is best described using a linear model. T 1/2 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 rate of elimination constant, plasma and renal clearance of gabapentin are directly proportional to the creatinine clearance.
Gabapentin is removed from the plasma during hemodialysis.
Values ​​of concentrations of gabapentin in plasma in children were similar to adults.
INDICATIONS
Treatment of neuropathic pain in adults over the age of 18; monotherapy of partial seizures with secondary generalization and without it in adults and children over 12 years of age; as an additional agent in the treatment of partial seizures with secondary generalization and without it in adults and children aged 3 years and older.
DOSING MODE
Individual, depending on the indications and treatment regimen.
SIDE EFFECT
From the side of the central nervous system and the peripheral nervous system: amnesia, ataxia, confusion, impaired coordination of movements, depression, dizziness, dysarthria, increased nervous excitability, nystagmus, drowsiness, thinking disorder, tremor, convulsions, amblyopia, diplopia, hyperkinesia, absence of reflexes, paresthesia, anxiety, hostility, violation of gait.
On the part of the digestive system: changing the staining of teeth, diarrhea, increased appetite, dry mouth, nausea, vomiting, flatulence, anorexia, gingivitis, abdominal pain, pancreatitis, changes in functional liver tests.
On the part of the hematopoiesis system: leukopenia, a decrease in the number of leukocytes, thrombocytopenic purpura.
On the part of the respiratory system: rhinitis, pharyngitis, cough, pneumonia.
From the musculoskeletal system: myalgia, arthralgia, fractures of bones.
From the cardiovascular system: arterial hypertension, manifestations of vasodilation.
From the urinary system: urinary tract infections, urinary incontinence.
Allergic reactions: erythema multiforme, Stevens-Johnson syndrome.
Dermatological reactions: skin maceration, acne, itching, rash.
Other: back pain, fatigue, peripheral edema, impotence, asthenia, malaise, puffiness of the face, weight gain, accidental trauma, asthenia, flu-like syndrome, fluctuations in blood glucose, in children - viral infection, otitis media.
CONTRAINDICATIONS
Increased sensitivity to gabapentin.
PREGNANCY AND LACTATION
Adequate and strictly controlled studies on the safety of gabapentin during pregnancy and lactation in humans have not been conducted. If you need to use during pregnancy and lactation, you should carefully weigh the expected benefit 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 the infant is not established.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with impaired renal function, as well as patients on hemodialysis, require a correction of the dosing regimen.
APPLICATION FOR CHILDREN
The efficacy and safety of therapy for neuropathic pain in patients under the age of 18 years have not been established.
The efficacy and safety of gabapentin monotherapy 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
APPLICATION IN ELDERLY PATIENTS
Older patients may need to adjust the dosage regimen gabapentin due to the fact that this category of patients may reduce renal clearance.
SPECIAL INSTRUCTIONS
A sharp cessation of therapy with anticonvulsants in patients with partial seizures can provoke a convulsive status. If necessary, reduce the dose, abolish gabapentin or replace it with an alternative remedy should be gradually over a minimum of 1 week.
GABAPENTIN is not an effective treatment for non-seizure seizures.
When combined with other anticonvulsants, false-positive results of the urine protein test were recorded. To determine the protein in the urine it is recommended to use a more specific method of precipitation of sulfosalicylic acid.
Patients with impaired renal function, as well as patients on hemodialysis, require a correction of the dosing regimen.
Older patients may need to adjust the dosage regimen gabapentin due to the fact that this category of patients may reduce renal clearance.
The efficacy and safety of therapy for neuropathic pain in patients under the age of 18 years have not been established.
The efficacy and safety of gabapentin monotherapy 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.
During the treatment period, do not drink alcohol.
Impact on the ability to drive vehicles and manage mechanisms
Before determining the individual response to treatment, the patient should refrain from potentially dangerous activities associated with the need for concentration and increased speed of psychomotor reactions.
DRUG INTERACTION
With simultaneous use with antacids, absorption of gabapentin from the digestive tract decreases.
When used simultaneously with felbamate, an increase in T 1/2 of felbamate is possible.
With simultaneous application, the case of increasing the concentration of phenytoin in the blood plasma has been described.
The information is provided for your information, do not self-medicate, it is dangerous for your health.
