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Unique pain management compounds

Andrei H Iagaru, Erik Mittra, Patrick M Colletti, Hossein Jadvar
Although selective metabolic and receptor-based molecular agents will surely be included in the future of prostate cancer diagnosis and therapy, currently available inorganic compounds-such as (18)F-NaF for the diagnosis of bony disease and (223)RaCl2 for the therapy of bone metastases-were recently shown to be superior to standard (99m)Tc-phosphonates for diagnosis and (153)Sm-ethylenediaminetetramethylene phosphonate or (89)SrCl2 for therapy. The advantages of (18)F-NaF include improved lesion detection and, when used in combination with CT, improved diagnostic confidence and specificity...
October 2016: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
John P McNulty, George Muller
A compounded preparation is needed when no commercially manufactured medication is available to adequately address a patient's medical needs. Among the greatest therapeutic challenges faced by both patients and caregivers is the treatment required by individuals who have a terminal condition. It is difficult to find evidence-based studies on the management of end-of-life situations because each patient's medical case is unique. In addition, maintaining a controlled environment for such patients is difficult...
May 2014: International Journal of Pharmaceutical Compounding
Connie Y Chang, Chaitanya K Challa, Janki Shah, Jean Daniel Eloy
Gabapentin (1-aminomethyl-cyclohexaneacetic acid) is an amino acid that has the structure of the neurotransmitter γ -aminobutyric acid (GABA). It is a novel drug used for the treatment of postoperative pain with antihyperalgesic properties and a unique mechanism of action. Gabapentin and the related, more potent compound pregabalin have been shown to be beneficial in the treatment of neuropathic pain as well as postoperative pain following spinal surgery and hysterectomy. This study reviews five aspects of gabapentin: (1) chemical and structural characteristics; (2) pharmacokinetics and pharmacodynamics; (3) application in acute pain management; (4) adverse effects; and (5) drug safety...
2014: BioMed Research International
David G Soergel, Ruth Ann Subach, Brian Sadler, John Connell, Alan S Marion, Conrad L Cowan, Jonathan D Violin, Michael W Lark
TRV130 is a G protein-biased ligand at the µ-opioid receptor. In preclinical studies it was potently analgesic while causing less respiratory depression and gastrointestinal dysfunction than morphine, suggesting unique benefits in acute pain management. A first-in-human study was conducted with ascending doses of TRV130 to explore its tolerability, pharmacokinetics, and pharmacodynamics in healthy volunteers. TRV130 was well-tolerated over the dose range 0.15 to 7 mg administered intravenously over 1 hour...
March 2014: Journal of Clinical Pharmacology
Vince Vadurri
Pikes Peak Hospice and Palliative Care, Inc., provides care for more than 200 patients with terminal disease who reside at home, in long-term care facilities, in assisted living facilities, or in its acute-care Inpatient Unit. Over the past 4 years, its pharmacy has evolved to provide individualized compounded preparations to meet the unique and complex needs of these patients. An integral part of this evolution was development and implementation of topical treatment for pain. These patients often have multiple medical conditions and complicated health issues...
May 2008: International Journal of Pharmaceutical Compounding
Joel Christiansen
Compounding pharmacists can provide a great therapeutic service to pain management patients who have overcome an addiction to prescribed or illegal drugs or alcohol. By collaborating with the physician and the patient, the compounder can develop an effective analgesic formulation with no addictive potential; a preparation that can be safely adjusted to meet changing medical needs. In this report, we present a personal account of the value of two compounded preparations that relieve severe musculoskeletal pain without producing mood-altering effects, as well as information about how those compounds are prepared...
July 2010: International Journal of Pharmaceutical Compounding
Gordon Munro, Rikke R Hansen, Naheed R Mirza
GAB(A) (γ-aminobutyric acid) is abundantly expressed within the brain, and spinal cord pain circuits where it acts as the principal mediator of fast inhibitory neurotransmission. However, drugs that target GABA(A) receptor function such as the classical benzodiazepines have not been optimised to promote analgesia, are limited by side effects and are not routinely used for this purpose in humans. Compounds such as NS11394, L-838,417, HZ166 and TPA023 all bind to the same benzodiazepine site on the GABA(A) receptor to allosterically modulate receptor function and enhance the actions of GABA...
September 15, 2013: European Journal of Pharmacology
Marilyn N Bulloch, Amber M Hutchison
Fentanyl pectin nasal spray is a novel intranasal formulation for the management of breakthrough cancer pain in patients taking and tolerant to opioids for persistent cancer pain. The pectin-based delivery modulates the product's transmucosal absorption. Nasal delivery allows fentanyl pectin nasal spray to achieve a greater maximum plasma concentration than oral transmucosal fentanyl products and at a much faster rate. Compared with intranasal fentanyl compounded with aqueous solutions, the pectin-based system decreases the maximum plasma concentration and prolongs exposure to more closely match the time course of a typical breakthrough cancer pain episode...
January 2013: Expert Review of Clinical Pharmacology
Jonathan Daitch, Michael E Frey, David Silver, Carol Mitnick, Danielle Daitch, Joseph Pergolizzi
BACKGROUND: Sublingual buprenorphine-naloxone (buprenorphine SL) is a preparation that is used to treat opioid dependence. In addition, the Drug Enforcement Administration (DEA) has acknowledged the legality of an off-label use to treat pain with a sublingual buprenorphine preparation. Buprenorphine SL is unique among the opioid class of analgesics; this compound has a high affinity for the mu-receptor, yet only partially activates it. Thus, buprenorphine SL can provide analgesia, yet minimize opioid side effects...
July 2012: Pain Physician
Qiu-Yu Tong, Wen Ma, Wei-Dong Shen
In view of the characteristics of different analgesic methods applied to nasal operation, the principle of point selection in acupuncture anesthesia, the frequency of electroacupuncture and the assessment of operation, it was stated that the compound acupuncture anesthesia not only prevented from incomplete analgesia of local anesthesia, but also avoided the adverse reactions of general anesthesia in this paper. Moreover, by reducing the dose of narcotics, the unique advantage of acupuncture anesthesia could be displayed...
May 2012: Zhongguo Zhen Jiu, Chinese Acupuncture & Moxibustion
Christopher D Rosenbaum, Stephanie P Carreiro, Kavita M Babu
Despite their widespread Internet availability and use, many of the new drugs of abuse remain unfamiliar to health care providers. The herbal marijuana alternatives, like K2 or Spice, are a group of herbal blends that contain a mixture of plant matter in addition to chemical grade synthetic cannabinoids. The synthetic cathinones, commonly called "bath salts," have resulted in nationwide emergency department visits for severe agitation, sympathomimetic toxicity, and death. Kratom, a plant product derived from Mitragyna speciosa Korth, has opioid-like effects, and has been used for the treatment of chronic pain and amelioration of opioid-withdrawal symptoms...
March 2012: Journal of Medical Toxicology: Official Journal of the American College of Medical Toxicology
Steven D Stockton, Lakshmi A Devi
Morphine and other opiates are among the most widely prescribed and clinically useful medications for the treatment of chronic pain. However, the applicability of these compounds has been severely hampered by the rapid development of tolerance and physical dependence that typically accompanies their repeated use. A growing body of evidence has implicated the regulated functioning of μ-δ opioid receptor heteromers in both the modulation of morphine-mediated antinociception, and in the limitation of undesirable side effects resulting from chronic opiate exposure...
March 1, 2012: Drug and Alcohol Dependence
Simon Barrett
This article examines the role of a unique dressing-Mepilex Ag--that incorporates the rapid and sustained antimicrobial action of ionic silver with the benefits of Safetac soft silicone adhesive technology. The combined attributes of each component of this dressing allow both the control of pain and infection to be achieved simultaneously. This dual approach to the management of wounds is of significance since the evidence suggests that wound infection and the release of pro-inflammatory modulators result in both local pain and delayed healing...
November 12, 2009: British Journal of Nursing: BJN
Pao-Luh Tao, Ping-Yee Law, Horace H Loh
The myriad of side effects that associate with morphine has been problematic in the clinical use to manage moderate to severe pain. It has been the holy grail of the pharmacologists to develop a compound, or treatment paradigm that could retain the analgesic effect of the drug as eliminating or reducing the side effects, mainly the tolerance and addiction development associates with chronic usage of the drug. In our earlier receptor structure/activities studies, we discovered an unique mutation of a conserved Ser in the fourth transmembrane domain of the opioid receptor that the alkaloid antagonist could activate the receptor...
February 2010: IUBMB Life
Elfatih Elzein, Jeff Zablocki
BACKGROUND: The challenges in developing any A(1) adenosine receptor (A(1)-AdoR) agonist involve having the desired effect on target tissue while avoiding side effects due to activation of A(1)-AdoR on other tissues. A(1)-AdoR de-sensitization leading to tachyphylaxis is also another challenge. OBJECTIVES: The major goal of this review is twofold: to highlight the structure affinity relationships (SAR) of A(1)-AdoR agonists, starting with initial lead compounds that were the genesis for second-generation compounds with high selectivity, affinity, and partial agonism; and to give an overview of the A(1)-AdoR agonists under development for various indications...
December 2008: Expert Opinion on Investigational Drugs
Anthony J Windebank, Wolfgang Grisold
Neurotoxic side effects of cancer therapy are second in frequency to hematological toxicity. Unlike hematological side effects that can be treated with hematopoietic growth factors, neuropathies cannot be treated and protective treatment strategies have not been effective. For the neurologist, the diagnosis of a toxic neuropathy is primarily based on the case history, the clinical and electrophysiological findings, and knowledge of the pattern of neuropathy associated with specific agents. In most cases, toxic neuropathies are length-dependent, sensory, or sensorimotor neuropathies often associated with pain...
March 2008: Journal of the Peripheral Nervous System: JPNS
C Richard Chapman, Robert P Tuckett, Chan Woo Song
UNLABELLED: This paper advances a psychophysiological systems view of pain in which physical injury, or wounding, generates a complex stress response that extends beyond the nervous system and contributes to the experience of pain. Through a common chemical language comprising neurotransmitters, peptides, endocannabinoids, cytokines, and hormones, an ensemble of interdependent nervous, endocrine, and immune processes operates in concert to cope with the injury. These processes act as a single agent and comprise a supersystem...
February 2008: Journal of Pain: Official Journal of the American Pain Society
Laura S Stone, Kelley F Kitto, James C Eisenach, Carolyn A Fairbanks, George L Wilcox
Agonists acting at alpha2-adrenergic receptors (alpha2ARs) produce antinociception and synergize with opioids. The alpha2ARs are divided into three subtypes, alpha(2A)AR, alpha(2B)AR, and alpha(2C)AR. Most alpha2AR agonists require alpha(2A)AR activation to produce antinociception and opioid synergy. The same subtype also mediates the side effect of sedation, which limits the clinical utility of these compounds. Identification of a non-alpha(2A)AR-mediated antinociceptive agent would enhance the therapeutic utility of alpha2AR agonists in pain management...
December 2007: Journal of Pharmacology and Experimental Therapeutics
Stephen J Farr, Babatunde A Otulana
Pulmonary opioid delivery, on the basis of the fact that small molecular entities can be rapidly and completely absorbed from the peripheral lung, poses a unique opportunity for the treatment of severe (breakthrough) pain, which currently is treated with intravenous therapy. Early clinical studies involving inhaled opioids were focused on treatment of dyspnoea and not pain management, but they showed that inhalation of various opioid compounds is safe, even in severely ill patients. The advent of specialized and efficient pulmonary drug delivery systems has facilitated the evaluation of inhaled opioids, such as morphine and fentanyl, for management of severe pain associated with surgery or malignant disease...
October 31, 2006: Advanced Drug Delivery Reviews
Susan Carter
Postoperative ileus (POI) is defined as the impairment of bowel motility that occurs almost universally after major open abdominal procedures, as well as other abdominal and nonabdominal procedures. For the majority of affected patients, POI generally lasts approximately three to five days, but longer duration is not uncommon. The causes of POI are multifactorial, but can be broadly categorized into two groups: those related to the surgical procedure and those related to pharmacologic interventions (opioids)...
April 2006: Journal of Perianesthesia Nursing: Official Journal of the American Society of PeriAnesthesia Nurses
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