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Development of Inhaled GABA Receptor Modulators to Improve Airway Function in Bronchoconstrictive Disorders.
ACS Pharmacol Transl Sci
February 2022
Department of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee, Milwaukee, Wisconsin 53211, United States.
We report the modification of MIDD0301, an imidazodiazepine GABA receptor (GABAR) ligand, using two alkyl substituents. We developed PI310 with a 6-(4-phenylbutoxy)hexyl chain as used in the long-acting β2-agonist salmeterol and PI320 with a poly(ethylene glycol) chain as used to improve the brain:plasma ratio of naloxegol, a naloxone analogue. Both imidazodiazepines showed affinity toward the GABAR binding site of clonazepam, with IC values of 576 and 242 nM, respectively.
View Article and Find Full Text PDFEvolution of drug delivery systems: From 1950 to 2020 and beyond.
J Control Release
February 2022
Akina, Inc., West Lafayette, IN 47906, United States of America; Purdue University, Departments of Biomedical Engineering and Pharmaceutics, West Lafayette, IN 47907, United States of America. Electronic address:
Modern drug delivery technology began in 1952 with the advent of the Spansule® sustained-release capsule technology, which can deliver a drug for 12 h after oral administration through an initial immediate dose followed by the remaining released gradually. Until the 1980s, oral and transdermal formulations providing therapeutic durations up to 24 h for small molecules dominated the drug delivery field and the market. The introduction of Lupron Depot® in 1989 opened the door for long-acting injectables and implantables, extending the drug delivery duration from days to months and occasionally years.
View Article and Find Full Text PDF[Opioid-induced constipation in oncologic patient: a clinical case treated with naloxegol].
Recenti Prog Med
March 2019
Oncologic patients on opioid therapy due to pain may have several side effects, including respiratory depression (in about 1% of cases), pruritus (up to 10% of cases), nausea (in 25-32% of cases), sedation (in 20- 60% of cases); but the most far-reaching side effect (up to 95% of cases) that can occur is constipation. The socalled "opioid-induced constipation" (OIC) can develop at the start of opioid therapy and can last as long as continued use. The OIC is a real change in intestinal habits that occurs when opioid treatment is started; it is noted with a reduced frequency of episodes of defecation, with a development or worsening of the effort to defecation, with a feeling of incomplete emptying and a perception on the part of the patient to live in a stressful way the act of defecation.
View Article and Find Full Text PDFConsumption of Movantik™ (Naloxegol) results in detection of naloxone in the patient's urine evaluated by confirmatory urine drug testing.
Clin Biochem
May 2019
Elite Medical Laboratory Solutions, Tomball, TX, United States of America.
Background: Many patients on chronic opioid therapy suffer from constipation, one of the most common side effect of opioids. Movantik™ (naloxegol) is an opioid antagonist that is recently introduced in the market to treat opioid-induced constipation and contains naloxegol as the active ingredient. Naloxegol is a pegylated (polyethylene glycol-modified) derivative of α-naloxol.
View Article and Find Full Text PDF[Treatment of persistent opioid-induced constipation in patients with hematological malignancies: case report].
Recenti Prog Med
November 2018
Opioid-induced bowel dysfunction wich comprises several other gastrointestinal complaints; could be highly debilitating, thus significantly deteriorating patients' quality of life. In particular, opioid-induced constipation (OIC) is the most frequent symptom. Therefore patients with haematological malignances need special attention of these disabling symptoms, which should be prevented by a correct evaluation of diet, age, intestinal habits, history of prior bowel disorders as well as constipating effects of other concomitant medication.
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