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Pregabalin
  • Pregabalin

Pregabalin

Item No.: CAS 148553-50-8
Product Name:Pregabalin,Lyrica
CAS No: 148553-50-8
MF: C8H17NO2
MW:159.23
Purity: 99%
Application: Anti-Epileptic Drug Pharmaceutical Intermediates
Appearance: White or Almost White Crystalline Powder
Function: Blood System Agents
Grade Standard:
INQUIRY
Pregabalin (Lyrica) is a medication in the gabapentinoid class. It has anticonvulsant, anxiolytic, and analgesic properties. As such, it's used for epilepsy, neuropathic pain, anxiety, and other conditions. Despite being a GABA derivative, it doesn't appear to be operating through a GABA-related mechanism. The substance is also used recreationally due to its euphoric, anxiolytic, and pro-social effects.
 

1. Dose

1.1 Medical

Range: 150 - 600 mg/d
Typically it's started at ~150 mg/d (split into multiple doses) and that dose increases weekly until an ideal response is achieved.

1.2 Non-medical
Light: 150 - 300 mg
Common: 300 - 600 mg
Strong: 600 - 900 mg
While some people report using over 1 gram, it's not a great idea. We know less about its safety at that dose and the severity of negatives is known to increase.

2. Timeline

Oral

Total: 6 - 10 hours (though some effects can persist for another 5 hours)
Onset: 30 - 60 minutes
Even though the onset should be under an hour, a lot of people in recreational settings report a delay. The effects could take 1.5 - 2.5 hours to really become apparent.

3. Effects

3.1. Medical

It's primarily used for neuropathic pain, fibromyalgia, seizures, and anxiety. Though it does have other applications.
Some of the reasons for its widespread use are its fast onset of efficacy, low drug-drug interaction potential, and its relatively high safety level.
Along with helping people's core condition (e.g. neuropathic pain), it can improve secondary insomnia and anxiety.
There have been criticisms of its widespread use, however. Part of the critique comes from those who are worried about its abuse potential.

3.1.1. Seizures

Pregabalin is mainly used as an adjunct therapy for partial seizures, meaning it's given to people who aren't receiving adequate benefit from their existing medications.
Studies have found it can reduce the frequency of partial seizures, particularly at 300 - 600 mg/d. According to (Kalviainen, 2008), it may aggravate myoclonus and myoclonic seizures, so it should be avoided in those populations.
Compared to other adjunct treatments, it might be superior to gabapentin and is similar in efficacy to levetiracetam.
As a monotherapy, it may be inferior to lamotrigine and topiramate.

3.1.2. Neuropathic pain

Pregabalin is effective for certain kinds of neuropathic pain, including postherpetic neuralgia, diabetic neuropathy, and central neuropathic pain. A lack of impact was found on HIV-associated neuropathy.
The most reliable benefits are seen with 200 - 600 mg/d.
Compared to gabapentin, there's at least a trend towards superior responses with pregabalin.

3.1.3. Fibromyalgia

It appears effective at improving pain and sleep in fibromyalgia, with a potentially less reliable or significant impact on fatigue. (Crofford, 2005) report it could improve sleep and pain.

3.1.4. Generalized anxiety disorder

Research has found it's more effective than placebo, but it's not yet clear if it should be a first-line treatment. When it works, it has a relatively fast onset of efficacy and a similar level of impact on psychic and somatic symptoms.
Some studies have found benzodiazepines aren't really superior to a higher dose of pregabalin and that it also comes close to SSRIs/SNRIs. While other research has found a pretty small clinical effect on certain scales.
It's approved in Europe, but not the US, for this condition.
There are some patients who benefit from pregabalin while being resistent to other treatments.

3.1.5. Postoperative pain

Variable effects of pregabalin have been seen on postoperative pain. It might be able to reduce opioid use and pain, but more research is needed. Even when it does offer some level of change, it might not be clinically significant.
Given it can raise the chance of some side effects (e.g. sedation), it may or may not be useful. Certain populations, like the elderly, may be better off avoiding it.
Some reports suggest it can reduce the risk of nausea and vomiting.
Positive reports exist for its administration prior to tonsillectomy, nasal surgery, and lumbar spinal surgery.

3.1.6. Social anxiety

Like with GAD, 150 mg doesn't appear very effective, but 300  - 600 mg/d might be effective.

3.1.7. Insomnia

It often has a positive impact on sleep across conditions.
Both healthy and treatment populations have reported improved sleep from the substance.
It can increase slow-wave sleep, improve sleep maintenance, reduce Stage 1 sleep, and potentially improve sleep onset. Though it does reduce REM.

3.1.8. PTSD

Very little research exists other than a little bit of evidence in favor of its use as an adjunct therapy.

3.2. Non-medical

3.2.1 Positives
  • Euphoria
  • Mood lift
  • Sedation
  • Analgesia
  • Muscle relaxation
  • Anxiolysis
  • Light to moderate entactogen effects (pro-social, greater empathy, greater appreciation)
  • Light to moderate dissociation
  • Physical euphoria (Pleasant sensations. Feelings of warmth and/or energy. Altered tactile perception.)
  • Increased self-confidence
  • Calmness
3.2.2. Negatives
  • Dizziness
  • Drowsiness
  • Amnesia - [Typically just minor and not prominent at common doses. Actual anterograde amnesia, like is possible with ethanol and benzodiazepines, isn't a notable effect.]
  • Impaired motor control
  • Cognitive impairment
  • Nausea
  • Muscle twitches - [Unclear occurrence. Not really reported in medical settings.]

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