How does pregabalin work?

How does pregabalin work?

As a gabapentinoid, pregabalin 300 mg is an analogue of gamma-aminobutyric acid or GABA (the main neurotransmitter of the nervous system). The mechanism of analgesic action of this medication, with regard to the nerves, is well known but the role in postoperative pain is unfamiliar.

The effects of this GABA analogue may be attributed to an array of mechanisms concerning depression of the sensitivity of the dorsal horn (the area at the back of the spinal cord containing sensory neurons).

Mechanisms directly related to release of the neurotransmitter at the dorsal horn:

  • Calcium-mediated inhibition of the release of neurotransmitters through action on the alpha-2-delta subunits
  • Inhibition of trafficking of the alpha-2-delta subunit 1 from the cluster of neurons at the root of a spinal nerve (dorsal root)
  • Recycling from endosomal compartments
  • Processes mediated by thrombosporin
  • Stimulation of the uptake of glutamate by the excitory amino acids (EAAs)

Mechanisms not directly related to release of the neurotransmitter at the dorsal horn:

  • Inhibition of descending serotonergic facilitation
  • Descending inhibition stimulation
  • An influence on the affective component of pain
  • Anti-inflammatory actions

How Long Does Pregabalin Take to Work?

Medications which are effective for seizures and depression can sometimes be useful for neuropathic pain (nerve pain). The efficacy of this therapeutic is related to the optimal level of pain relief without the onset of adverse effects. It is widely known that the intensity of nerve pain can make it difficult to sleep well. Pregabalin is often used as a painkiller to get better sleep when neuropathic pain makes it difficult to do so.

Peak levels of this medicine in the blood may be detected two to three hours after administration, but the therapeutic benefits may only be visible after a longer period of time.

For sleep, when experiencing pain associated with damaged nerves (this can be a result of diabetes, a spinal cord injury or an infection by the herpes zoster virus), these effects can be observed after a week of using the medication.

For the relief of the symptoms associated with neuropathic pain, as described above, it may take at least two weeks to notice visible results. This duration is increase to a few weeks with regard to a reduction in the frequency of seizures.

It has been reported, in some cases, that those using this medication for varying reasons have noticed immediate benefits.

Can I Take Two Pregabalin Tablets?

The amount of pregabalin tablets you take depends on the reason you are using it for and your response to the medication. It is not important how many tablets you take but rather the strength of the medicine as using too much of the active ingredient can lead to harmful effects.

These tablets and capsules (and oral solutions) come in varying strengths from 25 mg to 300 mg.

For instance, you may able to take three 50 mg tablets a day when using this medication for the management of diabetic nerve pain. But these three tablets would not be sufficient when using this medication for partial onset seizures. In this case you can use two 300 mg tablets twice a day so as to not exceed the maximum daily limit of 600 mg.

If you use more than the recommended amount of this pharmaceutical, you become prone to an increased chance of experiencing side effects. Furthermore, you can also develop a dependence on or tolerance to the medicine. Even though this gabapentinoid has the potential for abuse, it has been demonstrated as well tolerated and relatively safe in comparison to other psychotic substances such as opioids.

Never Mix Pregabalin and Alcohol

Never Mix Pregabalin and Alcohol

Pregabalin works by affecting the brain. This is the same for the effects of alcohol. When used together, the consequences may be dire. The combined effect of these substances is known as a 'negative' synergistic effect.

In addition to resulting in certain adverse events, any underlying mental conditions you may have can become worsened. The effectiveness of the medicine is also reduced when treatment includes the use of alcohol.

Consuming alcohol whilst on this medication causes an intense depression of the central nervous system resulting in:

  • Increased drowsiness
  • Increased dizziness
  • Increased concentration issues

Other side effects which involve combining alcohol and Lyrica can include:

  • Itchiness
  • Hives
  • Rashes
  • Reduced level of alertness
  • Angioedema symptoms (swelling of the lips, eyes and tongue)
  • Breathing problems

According to the Substance Abuse and Mental Health Services Administration (SAMHS), the concomitant use of alcohol and medications is a regular practice. SAMHS and other sources, such as the National Institute on Drug Abuse (NIDA), reports the effects of mixing these substances (and the severity thereof) will largely depend on the action of the medicine.

Is Pregabalin Safe During Pregnancy

In a study conducted to investigate the safety of pregabalin during pregnancy, the details involved:

  • A research period from 2004 to 2013
  • The study areas included the Netherlands, France, Switzerland, Finland, Italy, Turkey and the United Kingdom.
  • 163 trial patients received the medication and 656 women were part of the control group (not administered ant medication)
  • 115 women were using the medication for nerve pain, 5 for epileptic attacks, 1 for restless leg syndrome and 39 for psychiatric conditions
  • The administered dosages ranged from 75 mg to 300 mg, with an average 150 mg of the main ingredient

The results of the above study indicated that the rate of birth defects was higher for the test group than the control group. Birth deformities with major effects were observed in 6% of the trial patients (this was in comparison to the 2.1% of the control group). The full term pregnancies of the women using the medication were fewer than those not using the medications. The rate of live births was also reduced for the test group. Both groups did not show any risk of spontaneous abortion.

When evaluating the results of the above study, the risks seem quite high. However, if the benefits of painkillers far outweigh the risk, it would be appropriate to administer during pregnancy. When using this medication, a higher dose of folic acid is recommended as it helps the baby grow in a healthy way.

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Updated: 27th January 2021
Review Due: January 2022



Fueled with a passion to try and help people less fortunate than himself Steve immersed himself in the medical industry. By researching new and innovative medical advancements and regularly sharing important information on social media Steve intends to make a difference where it matters most, people's health. His wealth of knowledge and keen eye for detail will help keep our readers informed and contribute towards improved health.

Lindsay Taylor – Feb 27, 2021
Hello Steve, this blog has given me so much valuable information about my condition that I just had to write and say thank you. I regularly suffer from seizures and was really struggling to manage them before I read your blog. Now that I have all the information i need and a medication i can trust, I no longer fear these dreaded seizures. Thank you Lindsay Taylor

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