Rasagiline is a selective, irreversible inhibitor of monoamine oxidase type-B (MAO-B) and has been used both as a monotherapy and in addition to levodopa in the treatment of Parkinson’s disease (PD). Rasagiline is metabolized by the cytochrome P450 (CYP) system, and the following three major me...

Sensorineural hearing losses (SNHLs; e.g., ototoxicant- and noise-induced hearing loss or presbycusis) are among the most frequent sensory deficits, but they lack effective drug therapies. The majority of recent therapeutic approaches focused on the trials of antioxidants and reactive oxygen spe...

A straightforward chemoenzymatic synthesis of rasagiline mesylate has been developed. The key steps for the introduction of chirality involved kinetic enzymatic resolution with lipases via acetylation of rac-indanol and an inversion configuration Mitsunobu reaction of the produced (S)-indanol. I...

Background(−)-Deprenyl and rasagiline are classified as selective inhibitors of B-type MAO. The DATATOP study revealed that the administration of (−)-deprenyl to untreated patients with Parkinson's disease (PD) significantly delays the need for levodopa therapy (Parkinson Study Group, 1989)...

Impulse control disorders (ICD) are increasingly recognized in patients with Parkinson’s disease (PD), particularly when treated with commonly used dopamine agonists such as pramipexole and ropinirole [1], [2], [3], [4], [5]. Less evident is the possible association between monoamine oxidase in...

In this work, the synthesis of several racemic derivatives of 1-pyrindane as rasagiline analogues is described. The 1-pyrindane moiety was functionalised at C-7 position to afford the respective propargyl and isobutyl ethers, propargyl, isopropyl, n-propyl, and cyclopropyl amines and N,N-dimethy...

BackgroundRasagiline is a monoamine oxidase type-B inhibitor in development in Japan for Parkinson's disease (PD). The objective of this Phase 3, randomized, double-blind study was to evaluate the efficacy and safety of rasagiline in Japanese patients with early PD (NCT02337725).

The title compound 1a was prepared from cyclopentadienylthallium in 11 steps. The key component of the pseudo-disaccharide 1a, (−)-allosamizoline 2, was synthesized in 2 steps starting from the known cyclopentene 4 by formation of the aminoimidate 5 followed by a mercury(II)trifluoroacetate medi...

The purpose of this study was to qualify and quantify the femoral artery blood flow by duplex Doppler ultrasonography (DDU) in healthy dogs, before and after the administration of a combination of acepromazine maleate and buprenorphine hydrochloride (ACP–BPN). Seven healthy adult mongrel dogs a...

BackgroundThere is evidence regarding the abuse potential of buprenorphine in prison settings. There is also emerging evidence from community settings that buprenorphine/naloxone is less amenable to abuse than the single preparation buprenorphine hydrochloride as evidenced by cost-differentials ...

A morphine alkaloid derivative, buprenorphine hydrochloride, induces apoptosis in NG108-15 cells. Apoptosis was detected mainly by apoptosis-specific DNA fragmentation and morphological changes. This apoptosis was dose-dependent and the time-course experiment indicated that DNA fragmentation occ...

ABSTRACTTramadol abuse is a critical and growing health concern in Asia. In Iran, tramadol abuse arises most commonly as a result of self-medicating that leads to tramadol dependence. Buprenorphine, a partial agonist of mu opioid receptors approved for the treatment of tramadol dependence, is ad...

For the first time, an ultrasensitive impedimetric buprenorphine hydrochloride (BN) biosensor based on immobilization of bovine serum albumin (BSA) onto multi-walled carbon nanotubes (MWCNTs)/glassy carbon electrode (BSA/MWCNTs/GCE) has been developed using initial characterization by computatio...

To control the minimum effective dose, and reduce the number and quantity of administered potent drugs are unique features of advanced drug delivery in situ forming gel formulation. The efficacy, consistency, and increasing the application of existing injection therapies can be enhanced through ...

A simple isocratic reversed-phase high-performance liquid chromatographic method (RP-HPLC) was developed for the simultaneous determination of buprenorphine hydrochloride, naloxone hydrochloride dihydrate and its major impurity, noroxymorphone, in pharmaceutical tablets. The chromatographic sepa...

IntroductionPsychosocial interventions are often recommended as part of buprenorphine treatment for patients with opioid use disorder, but little is known about prescriber perspectives on their use and how this varies across buprenorphine prescriber specialties.

ObjectiveThis study aims to evaluate the trends and risk factors of severe buprenorphine outcomes (SBO) reported to the U.S. Poison Centers (PCs).

BackgroundFacing an epidemic of opioid-related mortality, many government health departments, insurers, and treatment providers have attempted to expand patient access to buprenorphine in psychosocial substance use disorder (SUD) programs and medical settings.

Despite proven clinical utility, use of sublinugual buprenorphine is fraught with issues of potential diversion among patients with opioid dependence. Transdermal buprenorphine patches provide an alternative delivery model that can be utilized to reduce such diversion. This narrative review disc...

BackgroundBuprenorphine maintenance therapy (BMT) has been widely recognized as one of the most effective treatments for opioid use disorders (OUD). In the midst of the U.S. opioid overdose crisis, local, state, and federal authorities have attempted to increase the availability of BMT, yet few ...