Gabapentin VS pregabalin, which is the best choice for pain relief?
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Gabapentin types include gabapentin and pregabalin, which have similar structures and mechanisms of action. Gabapentin class drugs are structurally similar to gamma aminobutyric acid (GABA), but have no affinity for GABA receptors. They bind to the presynaptic membrane calcium channel α 2 δ subunit, inhibit calcium ion influx, and reduce the release of painful substances; It can also inhibit the activity of N-methyl-D-aspartate (NMDA) receptors, reduce Ca2+, Na+influx and K+efflux, thereby reducing abnormal neuronal discharges induced by high calcium conductivity and the resulting seizures and neuropathic pain.
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| 60142-96-3 gabapentin | 148553-50-8 pregabalin |
1: What are the differences in clinical applications?
Gabapentin and Pregabalin were launched in 1993 and 2004 respectively. Gabapentin drugs were originally used as adjuvant therapy for epileptic seizures and are currently mainly used for the treatment of various types of pain.
The indications approved by gabapentin in China include adjuvant treatment of partial seizures, post herpetic neuralgia, and in Europe, gabapentin is also approved for the treatment of diabetes peripheral neuropathic pain.
The indications of pregabalin approved in China are post herpetic neuralgia and fibromyalgia, and it is also approved in Europe and America for the treatment of diabetes peripheral neuropathic pain, fibromyalgia, spinal cord injury related neuralgia, adult peripheral and central neuropathic pain, and adult generalized anxiety disorder.
Although the approved indications are limited at present, gabapentin drugs are commonly used beyond the instructions for various pain situations. Clinically, it is used for the treatment of postherpetic neuralgia, neuropathic pain, and generalized anxiety disorder. It is also commonly used for bipolar disorder, alcohol/anesthetic withdrawal, attention deficit/hyperactivity disorder, restless leg syndrome, trigeminal neuralgia, sciatica, and other conditions. However, there are multiple indications for the use of drugs beyond the instructions.
2:Which medication works faster?
In terms of pharmacokinetics, gabapentin has slow absorption and blood drug concentration does not increase proportionally with the increase of drug dose, exhibiting nonlinear pharmacokinetic characteristics; In contrast, pregabalin absorbs faster and blood drug concentration increases proportionally with increasing dose.
In terms of pharmacodynamics, both pregabalin and gabapentin showed a clear dose-response relationship in the treatment of postherpetic neuralgia (PHN), and the pain relief effect of pregabalin at 450mg/d was comparable to the maximum expected effect of gabapentin. Overall, Pregabalin seems to have more pharmacokinetic advantages, which may translate into improved pharmacodynamics.
3: Is there a difference in security between the two?
Gabapentin drugs were initially considered safer drugs, with common adverse reactions including dizziness, drowsiness, and gait abnormalities, as well as peripheral edema, dry mouth, vomiting, diarrhea, increased body weight, increased appetite, and constipation.
According to researchers' comparison, pregabalin and gabapentin have differences in safety:
The adverse reactions of Pregabalin are mainly systemic, neurological, and ocular, among which drowsiness, weight gain, visual blurring, and peripheral edema are serious adverse reactions described in the instructions.
The adverse reactions of gabapentin are mainly neurological adverse reactions and kidney damage, among which drug allergy, drowsiness, and suicidal ideation belong to the serious adverse reactions described in the instructions.
The reason why there are more reports of gabapentin related kidney injury is speculated to be as follows: Gabapentin is often used clinically to treat pruritus, peripheral neuropathy, and restless leg syndrome in patients with kidney disease. Chronic kidney disease patients themselves have renal dysfunction, and gabapentin is mainly excreted in the form of the original drug through the kidneys, which increases the accumulation and toxicity risk of gabapentin in the kidneys.
4: Be alert to the risk of gabapentin abuse!
Since 1994, multiple countries including the United States, United Kingdom, Germany, Finland, India, South Africa, France, and Canada have reported on the abuse of gabapentin. In the first investigation conducted by the Swedish Adverse Event Reporting System in 2010 after the listing of Pregabalin, it was found that there was an increasing trend of abuse.
In recent years, the abuse of gabapentin drugs has continued to increase, and its specific mechanism is not yet clear. It may be related to GABA mediation, as some GABA regulating drugs are also prone to abuse, such as alcohol, benzodiazepines, and sleeping pills. There are also cases of high-dose medication among abused patients.
There are reports that some patients take Pregabalin at doses 20 times higher than the recommended maximum dose. Abuse can increase the risk of adverse events such as dizziness, falls, drowsiness, and ataxia, especially when combined with opioid drugs, which not only increases the risk of respiratory depression but may also increase mortality by 60%.
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