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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, and generalized anxiety disorder (GAD). [13] [17] [18] Pregabalin also has antiallodynic properties.
Gabapentin at a low dose of 100 mg has a T max (time to peak levels) of approximately 1.7 hours, while the T max increases to 3 to 4 hours at higher doses. [1] The T max of pregabalin is generally less than or equal to 1 hour at doses of 300 mg or less. [1]
The effectiveness of pregabalin and its older relative gabapentin against pain syndromes of this kind (which tend to respond poorly to other analgesic drugs) has led to their widespread use, and these drugs have subsequently been found to be useful for many other medical applications, including as anticonvulsants, muscle relaxants, anxiolytics ...
As a result, the pharmacokinetics of gabapentin is dose-dependent, with diminished bioavailability and delayed peak levels at higher doses. [ 85 ] The oral bioavailability of gabapentin is approximately 80% at 100 mg administered three times daily once every 8 hours, but decreases to 60% at 300 mg, 47% at 400 mg, 34% at 800 mg, 33% at 1,200 mg ...
The maximum dose is used, rather than a lower dose, to reduce the number of test subjects (and, among other things, the cost of testing), to detect an effect that might occur only rarely. This type of analysis is also used in establishing chemical residue tolerances in foods. Maximum tolerated dose studies are also done in clinical trials.
The median effective dose is the dose that produces a quantal effect (all or nothing) in 50% of the population that takes it (median referring to the 50% population base). [6] It is also sometimes abbreviated as the ED 50, meaning "effective dose for 50% of the population". The ED50 is commonly used as a measure of the reasonable expectancy of ...
As a gabapentinoid, mirogabalin binds to the α 2 δ subunit of voltage-gated calcium channel (1 and 2), but with significantly higher potency than pregabalin. It has shown promising results in Phase II clinical trials for the treatment of diabetic peripheral neuropathic pain .
Bromazepam, sold under many brand names, is a benzodiazepine.It is mainly an anti-anxiety agent with similar side effects to diazepam.In addition to being used to treat anxiety or panic states, bromazepam may be used as a premedicant prior to minor surgery.