Antiepileptics, antidepressants, and local anesthetic drugs
Harald Breivik, William I Campbell, Michael K Nicholas in Clinical Pain Management, 2008
Pregabalin is quite similar to gabapentin in effects and side effects, but onset of pain relief is more rapid and its anxiolytic effects may be of additional benefit in some patients. Pregabalin can be started with a daily dose of 150 mg (in two or three divided doses) or 75 mg at bedtime in elderly patients and in patients prone to side effects. Upward titration can reach 300 mg per day within one to two weeks and the maximum benefits occur often after two weeks of treatment at target dosages of 300–600 mg/day. The linear pharmacokinetics (90 percent oral bioavailability, excreted unchanged in urine), the more rapid onset of pain relief, and the potential for twice daily dosing of pregabalin contribute to the relative greater ease of use compared to gabapentin. In patients with reduced kidney function, doses must be reduced accordingly.1
Pain and Its Management in Older Adults
K. Rao Poduri in Geriatric Rehabilitation, 2017
Anticonvulsants. This class of medications is used in treatment of neuropathic pain conditions, fibromyalgia, and migraines. These should be started at a low dose and titrated slowly as tolerated in older adults due to a significant risk of cognitive side effects. Gabapentin is used for the treatment of diabetic neuropathic pain, postherpetic neuralgia, and in the treatment of spinal stenosis and postlaminectomy pain syndrome with a dose range from 1800 to 3600 mg per day, in three divided doses. The recommended starting dose for gabapentin is 100 mg at night, increasing in 100 mg increments every 3 days as tolerated. Pregabalin is FDA approved for treatment of pain related to diabetic neuropathy, spinal cord injury, postherpetic neuralgia, and fibromyalgia. Dosing is 150–600 mg per day in two or three divided doses. The recommended starting dose in older population is 50 mg at night and titrating by 50 mg increments every 3–4 days as tolerated. These medications are thought to work on alpha2 delta subunit of voltage gated calcium channels. Weight gain, edema, ataxia, and dizziness are common side effects associated with the use of gabapentinoids.
Development of palliative medicine in the United Kingdom and Ireland
Eduardo Bruera, Irene Higginson, Charles F von Gunten, Tatsuya Morita in Textbook of Palliative Medicine and Supportive Care, 2015
In the medically ill patient, gabapentin should be initiated at a daily dose of 100-300mg at bedtime; the lower dose should be used in the setting of significant frailty or renal insufficiency. The starting dose of pregabalin usually is 50-75mg/ day, and 25mg/ day may be appropriate in those with severe frailty or renal impairment. The dose can be increased every few days. In the absence of a demonstrable analgesic ceiling dose or the development of treatment-limiting adverse effects, upward dose titration should continue until the gabapentin dose is 2700-3600 mg/day in two-three divided doses and the pregabalin dose is 300-600mg/ day in two divided doses. The drug should be stopped if there are no demonstrable benefits.
An update on the pharmacological management of pain in patients with multiple sclerosis
Published in Expert Opinion on Pharmacotherapy, 2020
Clara G. Chisari, Eleonora Sgarlata, Sebastiano Arena, Emanuele D’Amico, Simona Toscano, Francesco Patti
Pregabalin is an anticonvulsivant medication used to treat epilepsy, neuropathic pain, fibromyalgia, restless leg syndrome, and generalized anxiety disorder. Pregabalin acts as a gabapentinoid, inhibiting several calcium channels [51]. In regards to MS pain, pregabalin has been used in an open-label pilot study evaluating 16 MS patients and paroxysmal pain reached a mean treatment dosage of 154 mg daily. In this study, pregabalin demonstrated to be effective in reducing pain symptoms in almost 50% of patients [52]. In this study, three patients discontinued treatment because of adverse effects, in particular dizziness and general malaise. In another report on two patients, the occurrence of delirium, at a daily dose of 75 mg of pregabalin, was described. However, both patients were older than 60 and were also treated with specific CNS medications (benzodiazepine, baclofen, and/or tramadol) [53]. Thus, the Authors concluded that possible drug interactions particularly in older patients should be carefully considered. Moreover, in a recent, prospective, open-label, pilot study five patients with trigeminal neuralgia secondary to MS were successfully treated by a combination treatment of pregabalin plus lamotrigine [54]. Common adverse events possibly associated to pregabalin are weight gain, sleepiness, and fatigue, dizziness, leg swelling, disturbed vision, loss of coordination, and euphoria [55–57].
Is there a role for combined use of gabapentin and pregabalin in pain control? Too good to be true?
Published in Current Medical Research and Opinion, 2018
Helen Senderovich, Geetha Jeyapragasan
Gabapentin was originally approved in the United Kingdom in 1993. It is currently used for treatment of epilepsy and neuropathic pain disorders. In the US, it is also used as an adjunctive treatment for partial seizures, and for post-herpetic neuralgia. Pregabalin was approved in 2004 in Europe for peripheral neuropathic pain control, and as an adjunctive therapy for partial seizures. Subsequent approval was granted for neuropathic pain of all types, and for generalized anxiety disorder. In the US, the FDA approved pregabalin in 2005 for neuropathic pain associated with diabetic peripheral neuropathy, post-herpetic neuralgia in adults and as an adjunctive therapy for partial seizures. In June 2007, pregabalin was also approved for the treatment of fibromyalgia, insomnia and anxiety. It is important to recognize that in the United States pregabalin is used to treat epilepsy, diabetic neuropathy pain and post-herpetic neuralgia. The European Union also uses pregabalin to treat generalized anxiety disorder, whereas other drugs are used for this condition in the US4. The number needed to treat (NNT) for gabapentin in post-herpetic neuralgia is 8.0, and in painful diabetic neuropathy it is 5.95. The NNT for pregabalin is 3.96. For individuals with neuropathic pain associated with a spinal injury, 75 mg of pregabalin orally twice per day is recommended. The dose may be increased to 150 mg of pregabalin twice within 1 week. Patients who don’t feel a reduction in pain are able to take 300 mg twice daily. As such, the maximum dosage per day is 600 mg7.
New frontiers in the pharmacological treatment of social anxiety disorder in adults: an up-to-date comprehensive overview
Published in Expert Opinion on Pharmacotherapy, 2023
Alice Caldiroli, Enrico Capuzzi, Ilaria Tagliabue, Luisa Ledda, Massimo Clerici, Massimiliano Buoli
Pregabalin is a valid alternative for clinicians. It is a second-generation antiepileptic, which decreases glutamate release by binding the α2δ subunit of voltage-dependent calcium channels [67]. Similarly, pregabalin mitigates excessive noradrenaline neurotransmission associated with the somatic manifestation of acute anxiety [68,69]. This compound presents the strongest evidence of efficacy in subjects affected by SAD, especially at higher doses (450–600 mg/day), as shown by three large-sample high-quality studies [42–44] (Figure 2). In contrast, although pregabalin is well tolerated overall, it presents a non-negligible risk of abuse and dependence [70]. Moreover, providers need to be mindful of tapering the medication to prevent withdrawal and monitor prescription to individuals with substance use disorders [71]. In addition, this compound should be used with caution in subjects with renal impairment or those taking medications that alter kidney function (for example, diuretics) [72].
Related Knowledge Centers
- Allodynia
- Anxiolytic
- Generalized Anxiety Disorder
- Epilepsy
- Anticonvulsant
- Fibromyalgia
- Analgesic
- Restless Legs Syndrome
- Opioid Withdrawal
- Focal Seizure