Chronic pain is a condition affecting a vast patient population and resulting in billions of dollars in associated health care costs annually. Sufferers from severe chronic pain often require [correction of requite] twenty-four hour drug treatment through intrusive means and/or repeated oral dosing. Although the oral route of administration is most preferred, conventional immediate release oral dosage forms lead to inconvenient and suboptimal drug therapies for the treatment of chronic pain. Effective drug therapies for the management of chronic pain therefore require advanced formulation design to optimize the delivery of potent analgesic agents. Ideally, these advanced delivery systems provide efficacious pain therapy with minimal side effects via a simple and convenient dosing regime. In this article, currently commercialized and developing drug products for pain management are reviewed with respect to dosage form design as well as clinical efficacy. The drug delivery systems reviewed herein represent advanced formulation designs that are substantially improving analgesic drug therapies.
"Morphine in the MS Contin® slow-release tablet is embedded in a complex dual matrix of hydroxyethyl cellulose and cetostearyl alcohol, designed to release the drug over 12 h . Crushing the tablet disrupts this matrix, allowing the rapid extraction of morphine. "
[Show abstract][Hide abstract] ABSTRACT: Injections of mixtures prepared from crushed tablets contain insoluble particles which can cause embolisms and other complications. Although many particles can be removed by filtration, many injecting drug users do not filter due to availability, cost or performance of filters, and also due to concerns that some of the dose will be lost.
Injection solutions were prepared from slow-release morphine tablets (MS Contin) replicating methods used by injecting drug users. Contaminating particles were counted by microscopy and morphine content analysed by liquid chromatography before and after filtration.
Unfiltered tablet extracts contained tens of millions of particles with a range in sizes from < 5 microm to > 400 microm. Cigarette filters removed most of the larger particles (> 50 microm) but the smaller particles remained. Commercial syringe filters (0.45 and 0.22 microm) produced a dramatic reduction in particles but tended to block unless used after a cigarette filter. Morphine was retained by all filters but could be recovered by following the filtration with one or two 1 ml washes. The combined use of a cigarette filter then 0.22 microm filter, with rinses, enabled recovery of 90% of the extracted morphine in a solution which was essentially free of tablet-derived particles.
Apart from overdose and addiction itself, the harmful consequences of injecting morphine tablets come from the insoluble particles from the tablets and microbial contamination. These harmful components can be substantially reduced by passing the injection through a sterilizing (0.22 microm) filter. To prevent the filter from blocking, a preliminary coarse filter (such as a cigarette filter) should be used first. The filters retain some of the dose, but this can be recovered by following filtration with one or two rinses with 1 ml water. Although filtration can reduce the non-pharmacological harmful consequences of injecting tablets, this remains an unsafe practice due to skin and environmental contamination by particles and microorganisms, and the risks of blood-borne infections from sharing injecting equipment.
[Show abstract][Hide abstract] ABSTRACT: This ongoing column is dedicated to the challenging clinical interface between psychiatry and primary care-two fields that are inexorably linked.Tramadol (Ultram(®)) is a commonly prescribed analgesic because of its relatively lower risk of addiction and better safety profile in comparison with other opiates. However, two significant adverse reactions are known to potentially occur with tramadol-seizures and serotonin syndrome. These two adverse reactions may develop during tramadol monotherapy, but appear much more likely to emerge during misuse/overdose as well as with the coadministration of other drugs, particularly antidepressants. In this article, we review the data relating to tramadol, seizures, and serotonin syndrome. This pharmacologic intersection is of clear relevance to both psychiatrists and primary care clinicians.
[Show abstract][Hide abstract] ABSTRACT: Management of chronic noncancer pain (CNCP) requires a comprehensive assessment of the patient, the institution of a structured treatment regimen, an ongoing reassessment of the painful condition and its response to therapy, and a continual appraisal of the patient's adherence to treatment. For many patients with CNCP, the analgesic regimen will include opioids. Physicians should consider the available evidence of efficacy, the routes of administration, and the pharmacokinetics and pharmacodynamics of the various formulations as they relate to the temporal characteristics of the patient's pain. When making initial decisions, physicians should decide whether to prescribe a short-acting opioid (SAO) with a relatively quick onset of action and short duration of analgesic activity, a long-acting opioid (LAO) with a longer duration of analgesic action but a potentially longer onset of action, or both. Studies suggest that SAOs and LAOs are both effective for most types of CNCP. A review of published studies found no data to suggest that either SAOs or LAOs are generally more efficacious for treating any particular CNCP condition. The LAOs may provide more stable analgesia with less frequent dosing; however, opioid therapy should be tailored to the pain state and the individual patient, and SAOs may be appropriate for some patients with CNCP. MEDLINE and PubMed searches were conducted to locate relevant studies published from January 1975 to April 2008 using the following search terms: opioids, short-acting opioids, long-acting opioids, chronic pain, chronic pain AND opioids, and narcotics. English-only randomized controlled trials and nonrandomized studies were considered.
Mayo Clinic Proceedings 08/2009; 84(7):602-12. DOI:10.1016/S0025-6196(11)60749-0 · 6.26 Impact Factor
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