Medicine and Health Sciences Commons^™

Suvorexant, A Novel Dual Orexin Receptor Antagonist, For The Management Of Insomnia., Andrew H. Han, Carolin R. Burroughs, Evan P. Falgoust, Jamal Hasoon, Grace Hunt, Juyeon Kakazu, Tim Lee, Adam M. Kaye, Alan D. Kaye, Latha Ganti

School of Pharmacy Faculty Articles

PURPOSE OF REVIEW: The present investigation is a comprehensive review regarding the use of Suvorexant for insomnia treatment. It covers the background, pathophysiology, and significance of addressing insomnia, the pharmaceutical details of Suvorexant, and its safety, efficacy, and implications in treating insomnia. We further discuss Suvorexant's role in targeting insomnia with other comorbidities.

RECENT FINDINGS: Insomnia refers to poor quality and/or quantity of sleep. While there are many existing treatments such as benzodiazepines, melatonin agonists, TCAs, and atypical antipsychotics used to target various receptors involved in normal induction and maintenance of sleep, Suvorexant is an antagonist that specifically targets orexin …

Trends And Patterns In Use Of Medications For Opioid Use Disorder In A Commercially Insured Population In The U.S., Catherine Serratore

Theses and Dissertations--Pharmacy

Opioid use disorder (OUD) and opioid overdose are pervasive public health problems in the U.S. Medications for opioid use disorder (MOUD) have been shown effective to reduce OUD morbidity and mortality. Two distinct approaches to MOUD are currently used: agonist therapy (methadone or buprenorphine) or antagonist therapy (naltrexone). Limited information is available about the patterns of use, adherence to therapy, and characteristics of those who use agonist vs. antagonist therapy. The objective of this study is to assess recent trends in MOUD, adherence in use of MOUD, and the characteristics of those who use agonist vs. antagonist therapy in a …

Design, Synthesis, And Biological Screening Of Selective Mu Opioid Receptor Ligands As Potential Treatments For Opioid Addiction, Samuel Obeng

Theses and Dissertations

Today, more Americans die each year because of drug overdoses than are killed in motor vehicle accidents. In fact, in 2015, more than 33,000 individuals died due to an overdose of heroin or prescription opioids. Sadly, 40-60 % of patients on current opioid addiction treatment medications relapse. Studies have shown that the addiction/abuse liability of opioids are abolished in mu opioid receptor (MOR) knock-out mice; this indicates that the addiction and abuse liability of opioids are mainly mediated through MOR. Utilizing the “message-address concept”, the our laboratory reported a novel non-peptide, reversible MOR selective ligand 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α (isoquinoline-3-carboxamido)morphinan (NAQ). Molecular modeling …

Antagonism Of Triazolam Self-Administration In Rhesus Monkeys Responding Under A Progressive-Ratio Schedule: In Vivo Apparent Pa2 Analysis, Bradford D. Fischer Phd, Donna M. Platt, Sundari K. Rallapalli, Ojas A. Namjoshi, James M. Cook, James K. Rowlett

Bradford Fischer

No abstract provided.

Pharmacokinetic Evaluation Of A Novel Compound, Sn79, A Putative Sigma-2 Receptor Antagonist, By Intravenous And Oral Administration In Rats, Harsha Vinnakota

Electronic Theses and Dissertations

Considering the alarming rates at which substance drug abuse, especially cocaine, is increasing in today's society, there is a lot of impetus on the development of medications that can effectively help alleviate its toxicity and addiction. The affinity of cocaine to sigma receptors (sigma-1 and sigma-2) rendered the hypothesis that blocking sigma receptors could be a possible mechanism to attenuate cocaine-induced toxicity and addiction. In this view, SN79, a synthetic compound with selectivity to both sigma-1 and sigma-2 receptors garnered our attraction for its use as an antagonist. This dissertation encompasses detailed investigation of SN79 from drug discovery and development …

Development Of Novel Ahr Antagonists, Hyosung Lee

University of Kentucky Doctoral Dissertations

Aryl hydrocarbon receptor (AHR) is a sensor protein, activated by aromatic chemical species for transcriptionally regulating xenobiotic metabolizing enzymes. AHR is also known to be involved in a variety of pathogenesis such as cancer, diabetes mellitus, cirrhosis, asthma, etc. The AHR signaling induced by xenobiotics has been intensively studied whereas its physiological role in the absence of xenobiotics is poorly understood. Despite a number of ligands of AHR have been reported thus far, further applications are still hampered by the lack of specificity and/or the partially agonistic activity. Thus, a pure AHR antagonist is needed for deciphering the AHR cryptic …

Transdemal Delivery Of Opioid Antagonist Prodrugs, Audra L. Stinchcomb, Peter W. Swaan

Pharmaceutical Sciences Faculty Patents

A composition, a method and an apparatus for transdermally delivering an effective amount of opioid antagonists derived from prodrugs for treatment of eating disorders, narcotic dependence and alcoholism. In addition, the present invention relates to a composition, a method and an apparatus for transdermally delivering an effective amount of an opioid and opioid antagonist derived from an opioid agonist and one of an opioid antagonist and a prodrug for treatment of pain.

Method Of Administering Narcotic Antagonists And Analgesics And Novel Dosage Forms Containing Same, Anwar A. Hussain

Pharmaceutical Sciences Faculty Patents

The invention provides a novel method of administering narcotic antagonists, narcotic analgesics and related compounds, and novel dosage forms containing those compounds which are adapted for nasal administration. The nasal dosage forms disclosed include solutions, suspensions, gels and ointments. Especially preferred compounds which can be advantageously administered in accordance with the invention include naloxone, naltrexone, nalbuphine, levorphanol, buprenorphine, butorphanol, Δ⁹-tetrahydrocannabinol (THC), cannabidiol (CBD) and levonantradol.