Peak plasma concentrations are seen within an hour as compared to 3 hours with gabapentin. 12 Oral bioavailability for pregabalin is more than 90% as compared to 30–60% for gabapentin. These differences can be explained by the mechanism of absorption. Pregabalin has advantages over gabapentin, including higher maximum concentration and faster absorption, which may lead to better patient outcomes. Gabapentin: Absorption is slow and follows a saturable process. Gabapentin doses do not have a linear relationship with blood concentration. Gabapentin is more slowly and variably absorbed, with peak plasma concentrations around 3 hours post-dose. Pregabalin is quickly absorbed, with the maximum rate of absorption being 3 times that of gabapentin. It reaches peak blood concentrations within an hour after ingestion. Gabapentin and pregabalin are similar drugs but differ in several distinct ways. The main differences are their indications—specific uses that the Food and Drug Administration (FDA) has approved them to treat—and their dosages. Pregabalin, sold under the brand name Lyrica among others, is an anticonvulsant, analgesic, and anxiolytic amino acid medication used to treat epilepsy, neuropathic pain, fibromyalgia, restless legs syndrome, opioid withdrawal, generalized anxiety disorder (GAD), and shingles. [13] [17] [18] [19] Pregabalin also has antiallodynic properties. Neuropathic pain is pain caused by a lesion or disease of the somatosensory system1 and is often described as sensations of burning, tingling, shooting, sharpness, stabbing, or like electrical shocks. It is associated with conditions seen in many hospice patients including cancer, diabetes, and stroke. Neuropathic pain may also be a complication of neuromuscular diseases [] Gabapentin and pregabalin are analogs of gamma-aminobutyric acid (GABA) and share a similar mechanism of action, although they differ in some aspects. Both drugs bind to the α2δ subunit of calcium channels in neurons, but pregabalin exhibits greater affinity and potency in its binding ( 5 , 6 ). The dose conversion used was gabapentin 3600 mg/day to pregabalin 600mg/day, gabapentin 1800 mg/day to pregabalin 300mg/day and gabapentin 900 mg/day to pregabalin 150 mg/day. Adverse effects Adverse effects are common with gabapentinoids resulting in a discontinuation rate of at least 11%, but First, gabapentin is primarily absorbed in the small intestine, while pregabalin is absorbed at multiple sites, the small intestine and the ascending portion of the colon. 6 Second, gabapentin’s absorption is saturable; meaning that as gabapentin doses increase, the rate of absorption and resulting bioavailability decreases. For neuropathic pain, a pregabalin dosage of 450 mg/day appears to reduce pain comparably to the predicted maximum effect of gabapentin. As an antiepileptic, pregabalin may be more effective than gabapentin, on the basis of the magnitude of the reduction in the seizure frequency. Gabapentin vs Seroquel for Sleep: Comparing Effectiveness and Side Effects provides further insight into how gabapentin compares to other sleep medications in terms of side effects and efficacy. The onset and duration of action is another important factor to consider when comparing these medications. Pregabalin bioavailability is ≥90% irrespective of clinical dose, whereas gabapentin’s bioavailability decreases from 60% to 33% as dose increases from 900 to 3600 mg/day. Both can be given without regard to food intake since the amount absorbed is unaffected by food. Pregabalin has a longer duration of action, with its therapeutic effects lasting between 8 to 12 hours [4]. Meanwhile, Gabapentin’s action lasts for about 5 to 7 hours [5]. The table below shows how long each drug takes to reach its maximum concentration in your blood. Pregabalin (Lyrica) and gabapentin (Neurontin) are both approved to treat nerve pain. How are they different, and which one is preferred? Compare both meds here. The particular NNTs for pregabalin and gabapentin were 7.71 and 7.16, respectively. 10 A more recent meta-analysis in 2022 specifically focused on post-herpetic neuralgia and found greater efficacy with pregabalin in alleviating pain and improving global perception of pain and sleep. 15 Another meta-analysis published in 2021 reported similar The site of action of pregabalin is the alpha2-delta subunits on voltage-gated calcium channels. It prevents the release of neurotransmitters responsible for pain, seizures, and neuronal excitability. Like gabapentin, the precise mechanism of action of pregabalin is unknown. 4 However, gabapentin differs from pregabalin because of the reduced binding affinity to voltage-gated calcium channels. 6 Pregabalin is six-times more potent than gabapentin in binding affinity to the alpha 2 -delta voltage-gated calcium channel. 9 The manufacturer Pregabalin showed superior results compared to gabapentin in the Visual Analog Scale (VAS) at various time intervals up to 12–14 weeks (SMD −0.47, 95% CI −0.74 to −0.19). Although pregabalin (Lyrica) might “kick in” slightly slower than gabapentin (Neurontin), the duration of action for standard pregabalin is longer (8 to 14 hours) than the duration of action for standard gabapentin (5 to 8 hours). Lyrica(Pregabalin) is a prescription medication used to treat nerve pain caused by diabetes, shingles, or spinal cord injury, as well as certain types of seizures. It works by reducing the number of pain signals sent out by damaged nerves. Side effects may include dizziness, drowsiness, and blurred vision.
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