Gabapentin, pregabalin

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Pharmacology

Summary

Gabapentin and pregabalin are narrow-spectrum antiepileptic drugs primarily employed in the management of refractory focal seizures, or seizures poorly controlled by other drugs. Gabapentin and pregabalin block voltage gated Ca2+ channels, thereby inhibiting calcium currents and subsequently reducing neurotransmitter release. This unique mechanism make them particularly effective in addressing neuropathic pain conditions, with notable success in managing postherpetic neuralgia and painful diabetic neuropathy.

Furthermore,In addition to their role in epilepsy and pain management, gabapentin and pregabalin are pivotal in alleviating pain associated with postherpetic neuralgia, a sequelae following herpes zoster infection. They are also used in conditions like fibromyalgia, marked by generalized pain in muscles, joints, and soft tissues without definitive laboratory or physical evidence. However, potential side effects, including dizziness, sedation, and ataxia, warrant caution, especially in the elderly.

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FAQs

What is the pharmacological action of gabapentin and pregabalin in managing specific types of seizures?

Gabapentin and pregabalin, both narrow-spectrum antiepileptic agents, are tailored for the treatment of focal seizures, with or without secondary generalization. Their therapeutic utility shines particularly for cases that remain refractory or are inadequately controlled by other antiepileptic medications. Their mechanism of action is anchored in their ability to inhibit voltage-gated Ca2+ channels, leading to reduced calcium influx and subsequent diminished neurotransmitter release.

For which pain-related conditions are gabapentin and pregabalin found to be beneficial?

Gabapentin and pregabalin are versatile in managing a spectrum of chronic pain conditions. Their efficacy extends to neuropathic pain, painful diabetic neuropathy, fibromyalgia, and postherpetic neuralgia, a painful condition ensuing from the reactivation of the varicella-zoster virus (VZV).

How do gabapentin and pregabalin modulate pain in conditions like diabetic neuropathy and postherpetic neuralgia?

Through their targeted action on voltage-gated Ca2+ channels, gabapentin and pregabalin effectively decrease calcium entry into neurons. This results in a curtailed release of excitatory neurotransmitters pivotal for pain perception, hence offering relief from conditions such as painful diabetic neuropathy and postherpetic neuralgia.

What central nervous system (CNS) side effects can be attributed to gabapentin and pregabalin?

The modulation of calcium channels within the CNS by gabapentin and pregabalin comes with various advers effects. Notably, patients may encounter CNS manifestations like ataxia, dizziness, and sedation when on these medications.