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A lack of hepatic metabolism makes gabapentin an attractive option for patients on multiple antiepileptic drugs and patients with impaired hepatic function. Although gabapentin is relatively well tolerated, patients should be counseled on and monitored for CNS-related adverse effects, including somnolence, dizziness, ataxia, and asthenia. How Is Gabapentin Metabolized? Gabapentin is a tablet, capsule, extended-release (long-acting), and oral solution (liquid) to take by mouth. It is a lipid-soluble drug. The liver does not break down Gabapentin into metabolites, unlike most of the other drugs. Gabapentin's elimination involves renal clearance, with minimal metabolism by the liver. Its half-life is typically 5-7 hours, but can vary based on renal function. Clinical factors like dosage, individual metabolism, and renal impairment can influence its clearance. Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication primarily used to treat neuropathic pain and also for partial seizures [10][7] of epilepsy. It is a commonly used medication for the treatment of neuropathic pain caused by diabetic neuropathy, postherpetic neuralgia, and central pain. [11] It is moderately effective: about 30–40% of those given Pharmacodynamics Mechanisms of action Gabapentin and pregabalin do not bind to GABA receptors despite their structural similarity but have a high affinity for the α2δ-1 subunit of voltage-gated The pharmacokinetic (PK) properties of gabapentin, including absorption, distribution, metabolism, and excretion (ADME), were investigated during the development of Neurontin®, an immediate-release (IR) formulation of gabapentin that is orally administered three-times daily. As a drug, gabapentin was formerly considered as a structural analogue of the inhibitory neurotransmitter γ-aminobutyric acid (GABA). However, preliminary studies proposed that gabapentin did not bind to either GABA-A or GABA-B receptors 11, nor was it transform metabolically into GABA. 12. Absorption of gabapentin is solely dependent on LAT that are easily saturable, resulting in dose-dependent pharmacokinetics. As the dose of gabapentin increases, the area under the plasma concentration–time curve (AUC) does not increase proportionally. All pharmacological actions following gabapentin administration are due to the activity of the parent compound; gabapentin is not appreciably metabolized in humans. Gabapentin is a new antiepileptic drug (AED) with an attractive pharmacokinetic profile. It is absorbed by an active and saturable transport system, and has a high volume of distribution. Gabapentin is not bound to plasma proteins, does not induce hepatic enzymes and is not metabolized. At steady st Gabapentin: Gabapentin is indicated for postherpetic neuralgia and serves as adjunctive therapy for managing partial seizures (with or without secondary generalization) in adults and pediatric patients aged 3 or older. Impact on Other Organs While gabapentin primarily targets the CNS, its effects ripple through other organ systems as well. The kidneys, liver, and gastrointestinal tract all play roles in how gabapentin is metabolized and eliminated from the body. Effects on the Kidneys Gabapentin is primarily excreted unchanged by the kidneys. Gabapentin isn’t known to harm the liver. It’s not metabolized (broken down) by your liver. While there have been some individual reports of liver damage from gabapentin, it’s considered extremely rare. One uncommon risk with gabapentin is a reaction called DRESS (drug reaction with eosinophilia and systemic symptoms) syndrome. Gabapentin is not appreciably metabolized. Gabapentin enacarbil, the prodrug of gabapentin, is rapidly and efficiently converted to gabapentin by first-pass hydrolysis following oral administration. Gabapentin is not protein-bound. A high volume of distribution indicates greater concentration in tissue than in plasma. It is not metabolized and does not induce hepatic enzymes or inhibit metabolism of other antiepileptic drugs. Gabapentin (Trade name: Neurontin) is an anticonvulsant. It is commonly also used off-label for anxiety disorders, restless leg syndrome, and in alcohol use disorder. It is structurally similar to GABA but does not directly bind to GABA receptors. Gabapentin (Neurontin) Overview Brand name: Neurontin Structure and Mechanism 1- (aminomethyl)cyclohexaneacetic acid (C9H17NO2) It is structurally related to gamma-aminobutyric acid (GABA). However, does not modify GABA binding, is not converted into a GABA agonist, and does not inhibit GABA uptake/degradation By inhibiting the voltage-gated calcium channels in the CNS, gabapentin reduces the release of excitatory neurotransmitters (mostly noradrenaline, dopamine and serotonin), and therefore decreases epileptogenesis. Gabapentin is an anticonvulsant medication used in the management of peripheral neuropathic pains, postherpetic neuralgia, and partial-onset seizures.
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