Extended-release Tramadol (ULTRAM ER): a pharmacotherapeutic, pharmacokinetic, and pharmacodynamic focus on effectiveness and safety in patients with chronic/persistent pain.

Abstract

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.

• Authors: Robert L Barkin
• Journal: American journal of therapeutics (Am J Ther) 2008 Mar-Apr Vol. 15 Issue 2 Pg. 157-66 ISSN: 1536-3686 [Electronic] United States
• PMID: 18356636 (Publication Type: Journal Article, Review)

Chemical References

• Analgesics, Opioid
• Delayed-Action Preparations
• Tramadol

Topics

• Analgesics, Opioid (administration & dosage, adverse effects, pharmacokinetics, therapeutic use)
• Chronic Disease
• Delayed-Action Preparations
• Humans
• Pain (drug therapy)
• Tramadol (administration & dosage, adverse effects, pharmacokinetics, therapeutic use)