Tramadol is a centrally acting synthetic
opioid analgesic that has a dual mechanism of action, binding to
mu-opioid receptors and weakly inhibiting the neuronal reuptake of
norepinephrine and
serotonin. Extended-release (ER)
tramadol tablets (
ULTRAM ER) are indicated for the management of moderate to moderately severe chronic (also referred to as persistent)
pain in adults who require around-the-clock treatment of
pain for an extended period of time. Because once-daily
tramadol ER results in less frequent fluctuations in plasma concentrations than equivalent daily doses of short-acting
tramadol, it may benefit patients experiencing
pain throughout the dosing interval. On the basis of computer-generated pharmacokinetic models, one can easily transition patients who are receiving short-acting
tramadol for chronic/persistent
pain to
tramadol ER, by calculating the current total daily dose of short-acting
tramadol and starting
tramadol ER at the nearest lower 100-mg-dose increment. In clinical studies,
tramadol ER significantly reduced
pain in patients with
chronic pain from
osteoarthritis and improved
pain-related sleep parameters, joint stiffness, and physical function.
Tramadol ER has been shown to be safe and well-tolerated and may be a suitable alternative for patients with inadequate
analgesic response or
contraindications (eg,
cardiovascular disease, gastrointestinal
ulcer) to use of nonsteroidal anti-inflammatory drugs (
NSAIDs) or
cyclooxygenase-2 (COX-2) inhibitors. The proven efficacy and safety profile--and the low potential for abuse--make
tramadol ER a viable therapeutic option for the management of chronic/persistent nonmalignant
pain in some patients. This article reviews the pharmacology, pharmacokinetics, pharmacodynamics, dosage, delivery system, administration,
analgesic efficacy, and safety and tolerability profile of
tramadol ER.