If paracetamol, ibuprofen, and aspirin are appropriate for you to consume along with pregabalin, that is fine. When combined with pregabalin, potent painkillers like codeine, co-codamol, and dihydrocodeine can make you feel more tired.
Pregabalin (PGB), also known as (S)-3-(aminomethyl)-5-methylhexanoic acid, has been available on the U.S. market since 2005. It is used to treat epilepsy/partial seizures, neuropathic pain, especially diabetic peripheral neuropathy, post-herpetic neuralgia, and fibromyalgia. It is a comparatively more potent analogue of gabapentin. PGB is authorised for the treatment of generalised anxiety disorder in Europe (GAD). PGB has received numerous off-label prescriptions for psychiatric disorders such bipolar disorder, alcohol/narcotic withdrawal symptoms, and ADHD.
PGB does not bind GABAA, GABAB, or benzodiazepine receptors despite being a gamma-aminobutyric acid (GABA) analogue. Moreover, short-term PGB treatment had little effect on blood GABA levels. The alpha-2-delta subunit of voltage-gated calcium channels is highly affinified by PGB. As a result, after ingesting PGB, calcium influx is decreased, and substance P, glutamate, and noradrenaline—neurotransmitters involved in pain pathways—have less calcium-dependent release.
PGB’s pharmacokinetics are predictable. No matter the dose or frequency of administration, it has an oral bioavailability of more than 90%. Up to 98% of it is eliminated through the kidneys unaltered. It barely interacts to serum proteins and has no known pharmacokinetic drug interactions.
1.5 hours after injection, plasma PGB concentrations reach their peak. PGB has relatively fewer negative side effects and easily passes the blood-brain barrier. PGB is a fantastic option for clinical usage due to the pharmacological and pharmacokinetic characteristics listed above. For all of the aforementioned medical disorders, it is frequently prescribed. PGB saw annual sales growth of 2.8% in 2017 and ranked tenth in terms of gross sales (5.1 billion USD), according to Pharma Marketing (2018).
Pregabalin Abuse Potential
In 2006, the first reports of PGB usage and dependence were patients from Turkey, Germany, and Italy. Since 2008, the Scandinavian, British, French, and German pharmaco vigilance systems have received several reports of PGB abuse, the majority of which included patients who are currently or have previously been dependent on other similar drugs.
In 2010, data from the European Monitoring Centre for Drugs and Drug Addiction (EMCDDA) for the first time identified PGB misuse. PGB was added to the list of psychoactive substances under evaluation by the 41st Expert Committee on Drug Dependency of the WHO in November 2018 due to its propensity for abuse and dependence as well as its potential to impair social and public health. PGB was categorized as possessing a high “abuse liability.”
PGB transitioned from being a prescription medicine to a recreational drug over the previous ten years. On the underground market or through online sources, access to it grew over time. In an effort to increase the overall psychogenic impact, PGB is frequently combined with alcohol, BZDs, zopiclone, and gabapentin. Additionally, it has been mixed with mephedrone, heroin, opiates, amphetamines, LSD, and cannabis. PGB and opiates used together are known to significantly increase mortality and may have a potentially fatal effect. Concerns concerning higher risks of respiratory depression and death when combined with opioids or other CNS depressants have also been raised due to PGB’s potential for abuse.
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