In in vitro studies using radiolabeled gabapentin, gabapentin binding sites were found in rat brain

Jump to: Feature substance Pharmacology identi Gabapentin Gabapentin Contraindications Use of the substance use during pregnancy and breast-feeding Side Effects Interactions Overdose Dosage and Administration Precautions substance Gabapentin Cautions Further reading interactions with other active ingredients Russian name Latin name Gabapentin Gabapentin Gabapentin substance Chemical Name
1 - (aminomethyl) cyclohexane acid molecular formula C 9 H 17 NO 2 Therapeutic substances gabapentin Antiepileptic agents nosological classification (ICD-10) G40.0 localized (focal) (partial) identi idiopathic epilepsy and epileptic syndromes with seizures starting with a focal G40.1 localized (focal) (partial) symptomatic epilepsy and epileptic syndromes with simple identi partial seizures G40.2 localized (focal) (partial) symptomatic epilepsy and epileptic syndromes with complex partial identi seizures G53.0 neuralgia after herpes zoster (B02.2 +) Code CAS 60142-96-3 Characteristics substance Gabapentin
White to off-white crystalline solid, readily soluble in water and in acidic and basic water solutions. The molecular weight of 171.24. Pharmacology of drugs - an anticonvulsant, analgesic.
Prevents the occurrence of seizures in the induction identi of maximal electroshock seizures and pentylenetetrazole mice and rats as well as in other preclinical models (e.g., lines of genetically induced epilepsy, etc.). Relevance of these models to human epilepsy is unknown.
Gabapentin has structural similarity to the neurotransmitter GABA but does not change the radioligand binding of GABA to GABA A or GABA receptors, is not metabolized in the GABA agonist or GABA-receptors and inhibit the seizure or destruction of GABA. In a study using the method of radioligand binding at concentrations identi of gabapentin to 100 uM showed no affinity for a number of other receptors including benzodiazepine, identi glutamate, N-methyl-D-aspartate, kviskvalatnye, kainate, glycine (strychnine-insensitive and strychnine-sensitive), alpha 1 -, alpha 2 -, and beta-adrenergic, adenosine A 1 and A 2, muscarinic and nicotinic cholinergic, dopamine D 1 and D 2, H 1-histamine, serotonin identi 5-HT 1 and 5-HT 2, the mu-opiate, identi delta and kappa, cannabinoid identi 1 as well as binding sites for the voltage-sensitive calcium channels (or labeled nitrendipine diltiazem) or voltage-sensitive sodium channels (20-labeled alpha-benzoate batrahotoksininom A). Additionally, gabapentin does not affect the cellular uptake of dopamine, noradrenaline and serotonin.
In in vitro studies using radiolabeled gabapentin, gabapentin binding sites were found in rat brain tissue, including the neocortex and hippocampus. Protein in the brain tissue of animals with high affinity to gabapentin identified as voltazhaktivirovannogo Additional calcium channel subunit. The clinical significance of this fact is binding until set.
In experimental identi studies, gabapentin prevents hyperalgesia and allodynia, especially painful identi response to various models of neuropathic pain in rats and mice (model streptozocin-induced diabetes, spinal cord injury, etc.). Besides, reduces pain response model of peripheral inflammation, but does not affect the behavior directly caused by pain. Relevance of these models for pain in humans has not been established.
The effectiveness of gabapentin as adjuvant antiepileptic therapy in adults and children (3 years and older) with refractory partial seizures set in the multi-center, placebo-controlled, double-blind clinical trials with parallel groups.
Confirm the performance identi were obtained in three studies conducted with the participation of 705 patients (aged 12 years and older) and in one study involving 247 children (aged 3 to 12 years). All these are included in the study patients had a history of at least four partial seizures per month in spite of the use of one or more antiepileptic drugs at therapeutic doses, and in the mode set it antiepileptic therapy seizures observed during the 12-week baseline period (for children - within 6 weeks). Patients with continuing seizures (at least 2, and in some studies - 4 attack per month) was added to the ongoing treatment gabapentin or placebo for 12 weeks. identi Efficacy was evaluated by the number of patients who decreased the frequency of seizures in more than 50% compared to baseline and the expected "response factor" identi with the formula (T-B) / (T + B), where - the base h