gabapentinoidok

Gabapentinoids are a class of prescription medicines that includes gabapentin and pregabalin. They are designed to modulate nerve activity by binding to the alpha-2-delta subunit of presynaptic voltage-gated calcium channels. A related compound, mirogabalin, has been developed and approved in some regions but is not universally available. In Hungarian usage, these drugs are often referred to as gabapentinoidok.

The drugs resemble GABA in structure but do not act on GABA receptors. By reducing calcium entry into neurons, they decrease the release of excitatory neurotransmitters, which lowers neuronal excitability. This mechanism underpins their use in neuropathic pain and as adjuncts in seizure management.

Common clinical uses include neuropathic pain conditions such as diabetic neuropathy and postherpetic neuralgia, and adjunctive therapy for focal seizures. Pregabalin is approved for fibromyalgia in several jurisdictions. Gabapentinoids are sometimes prescribed off-label for other conditions, including anxiety disorders and various chronic pain syndromes.

Pharmacokinetics vary between agents. Gabapentin shows saturable, nonlinear absorption with variable bioavailability; pregabalin has linear, dose-proportional pharmacokinetics. Both are largely excreted unchanged by the kidneys, with little hepatic metabolism, and require dose adjustment in renal impairment. They have relatively rapid onset but variable duration of effect.

Adverse effects commonly include dizziness, somnolence, ataxia, peripheral edema, and weight gain. Cognitive impairment and dry mouth can occur. There is potential for misuse and dependence, and abrupt withdrawal after long-term use can cause insomnia, nausea, or malaise. Caution is advised in elderly patients and during pregnancy.

Regulatory status and availability vary by country. Gabapentinoids are generally prescription-only medicines, with increasing regulatory attention in some jurisdictions due to misuse risk. Clinicians balance benefits in pain and seizures against potential adverse effects and misuse when determining the treatment plan.