Pregabalin: Uses, side effects and painkiller compatibility
Pregabalin is a prescription medication that belongs to a class of drugs known as anticonvulsants. It was first synthesised in 1990 as an anticonvulsant agent and is a structural derivative of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter[1, 2]. It is available in various forms like a capsule, a solution, and an extended-release tablet, all taken orally [3].
The exact working mechanism of action of pregabalin has yet to be fully understood. Still, it is known to bind to the alpha2delta 1 subunit of voltage-gated calcium channels in the central nervous system (CNS). This binding modulates the calcium channels, reducing the release of several excitatory neurotransmitters, including glutamate, norepinephrine, substance P, and calcitonin gene-related peptide [1, 2, 4].
This modulation, as discussed before, helps regulate the reduction of the excessive neurotransmitter release that is observed in certain neurologic and psychotic disorders. It is believed to work by calming the damaged or overactive nerves in your body that may cause pain or seizures [3].
Pregabalin has analgesic (pain-relieving), anticonvulsant, and anxiolytic (anti-anxiety) activity. It has shown efficacy in the management of neuropathic pain related to diabetic peripheral neuropathy and postherpetic neuralgia and as adjuvant therapy for adult patients who deal with partial onset seizures [1].
Uses of Pregabalin
As an Anticonvulsant: Pregabalin is a versatile drug with a wide range of applications in the management of various health conditions. One of its primary uses is as an anticonvulsant for treating epilepsy [4, 5, 6, 4]. It has been shown to be effective as an adjunctive therapy for refractory partial-onset seizures, with up to 51% of patients showing a 50% reduction in seizure frequency [6, 4].
As an Analgesic: Another significant use of pregabalin is in the treatment of neuropathic pain, which is a type of chronic pain caused by damage to the nerves. It has also been effective in reducing pain in several other conditions, including diabetic neuropathy, postherpetic neuralgia, and fibromyalgia [1, 7, 8, 9, 4, 5, 10, 11].
Reducing anxiety: Pregabalin is also used to manage general anxiety-related disorders, displaying similar efficacy to benzodiazepines and venlafaxine [12, 13]. It has been found to have anxiolytic, or anxiety-reducing, properties and may also have beneficial effects on sleep [12, 13].
Aiding relapse prevention and withdrawal phases: In addition, pregabalin has been suggested as a potential therapeutic agent for the treatment of alcohol abuse, both in the withdrawal phase and in relapse prevention [4]. However, it's important to note that there are reports of pregabalin being misused, particularly among drug users and patients with substance use disorders [5].
Side effects of Pregabalin
Common side effects: Pregabalin is known to have several side effects. Common side effects include:
Other side effects can include:
- tiredness,
- headache,
- dry mouth, vomiting, nausea, constipation, gas, bloating,
- speech problems,
- difficulty concentrating or paying attention, forgetfulness, anxiety,
- lack of coordination, loss of balance or unsteadiness, uncontrollable shaking or jerking of a part of the body, muscle twitching, weakness, [15].
Serious side effects: In a few cases, pregabalin can cause more severe side effects. These include blurred vision, double vision, hives, rash, blisters, itching, swelling of the eyes, face, throat, mouth, lips, gums, tongue, head or neck, hands, feet, ankles, or lower legs, swelling of the arms, shortness of breath, wheezing, muscle pain, tenderness, soreness, or weakness, especially if it comes along with fever, chest pain, and difficulty breathing [15].
Rare side effects: Pregabalin can also cause rare side effects such as acute psychosis, epileptiform EEG changes [14], visual hallucinations [16], and urticarial rash and neutropenia [17].
In some cases, pregabalin can exacerbate heart failure, especially if patients have a history of cardiac issues [18].
What painkillers can you take with pregabalin?
Many studies have been conducted to determine pregabalin's interactions with various painkillers. It's important to note that the interactions can vary depending on the dosage and the specific painkiller used.
Tramadol: When combined with tramadol, a study found that the pain-blocking effect of pregabalin and tramadol increased significantly when a non-analgesic dose of pregabalin was combined with a low analgesic dose of tramadol. However, when non-analgesic doses of both drugs were combined, the effect was sub-additive, which means the combined effect was less than the sum of their individual effects [19].
Morphine: Pregabalin also showed a synergistic interaction with morphine, a potent opioid painkiller. The combined dose of pregabalin and morphine produced significantly more antinociceptive effects than either drug alone, especially at lower doses [20].
Synthetic Cannabinoid: In another study, pregabalin was combined with the synthetic cannabinoid WIN 55,212-2 mesylate. The combination resulted in a synergistic interaction, meaning the combined effect was more significant than the sum of their individual effects [21].
Tapentadol: Pregabalin and tapentadol also show a synergistic interaction. The combination of pregabalin and tapentadol resulted in a more significant antinociceptive effect than either drug alone [22].
Naproxen: Finally, a synergistic interaction was also found between Pregabalin and Naproxen, a non-steroidal anti-inflammatory drug (NSAID), to reverse thermal hyperalgesia associated with peripheral inflammation [23].
In conclusion, pregabalin can interact synergistically with various painkillers, potentially enhancing their analgesic effects. However, the nature of these interactions can depend on the specific painkiller and the doses used. Therefore, it is essential to consult your physician before using a particular combination.