Azilect

Rasagiline has a certain potential in neuroprotection and delaying the progression of Parkinson's disease (PD). However, the poor pharmacokinetics (PK) characteristics of conventional oral tablets and poor medication compliance limit the optimal efficacy of rasagiline. Based on this, we designed and optimized a sustained-release rasagiline in situ gel based on in vitro release and in vivo PK results. Among them, we found for the first time that aluminum hydroxide can effectively shorten the lag phase and promote early and late release, making the daily release more uniform...

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No abstract text is available yet for this article.

Parkinson's disease is a neurodegenerative disorder that manifests as motor deficits, tremors, rigidity, and postural instability. The most prominent pathological feature of this disease is reduced striatal dopamine concentration due to the loss of nigrodopaminergic neurons. Symptomatic dopamine replacement therapy is the standard management approach for Parkinson's disease. Treatment with monoamine oxidase B (MAO-B) inhibitors also improves Parkinson's disease symptoms by inhibiting the striatal dopamine metabolism and increasing the intracerebral dopamine concentration...

OBJECTIVE: Rasagiline is a second-generation potent selective inhibitor of monoamine oxidase-B. The aim of the study was to analyze the effectiveness of rasagiline in treatment of Parkinson's disease (PD), both as monotherapy and combination therapy. METHODS: Medline, Cochrane, EMBASE, and Google Scholar databases were searched until 9 March 2016 using the keywords: Rasagiline, Azilect, Parkinson's disease. Randomized controlled trials of patients with PD who were randomized to treatment with rasagiline or placebo were included...

BACKGROUND: We report a case of a patient with recurrent severe hypoglycemia after initiating the drug rasagiline (Azilect) for Parkinson disease. CASE PRESENTATION: A 25-year-old Emirati woman who had been diagnosed with Parkinson disease due to a genetic mutation since the age of 18 years presented to our hospital. She had been treated with a rotigotine patch 2 mg per day along with carbidopa + levodopa + entacapone 25 mg/100 mg/200 mg (Stalevo) over these years...

BACKGROUND: The Attenuation of Disease progression with Azilect GIven Once-daily (ADAGIO) delayed-start study demonstrated a benefit of early-start treatment with rasagiline 1 mg/day versus delayed-start treatment in PD. This follow-up study aimed to assess whether these benefits persist and the clinical progression rate during long-term naturalistic treatment. METHODS: The ADAGIO Follow-Up study was initiated approximately 26 months after completion of the ADAGIO study...

The present study aimed to investigate the protective effects of prolonged treatment with the selective, irreversible monoamine oxidase-B inhibitor, novel anti-parkinsonian drug, rasagiline (Azilect) in aged animals. Our findings from behavioral experiments demonstrated that long-term treatment of aged mice with rasagiline (0.2 mg/kg) exerted significant beneficial effects on mood-related dysfunction and spatial learning and memory functions. At this dose of rasagiline, chronic drug administration significantly inhibited monoamine oxidase-B activity and caused an increase in striatal dopamine and serotonin levels, while decreasing their metabolism...

BACKGROUND: The current cornerstone treatment of myocardial infarction (MI) is restoration of coronary blood flow by means of thrombolytic therapy or primary percutaneous coronary intervention. However, reperfusion of ischemic myocardium can actually provoke tissue damage, defined as "ischemia-reperfusion (I/R) injury." TVP1022 [the S-isomer of rasagiline (Azilect), FDA-approved anti-Parkinson's drug] was found to exert cardioprotective activities against various cardiac insults, such as chronic heart failure and I/R, in rat models...

IMPORTANCE: Depression, cognitive impairment, and other nonmotor symptoms (NMSs) are common early in Parkinson disease (PD) and may be in part due to disease-related dopamine deficiency. Many patients with PD are treated with antidepressants for NMSs, and the effect of the combination of PD medications that enhance dopamine neurotransmission and antidepressants on NMSs has not been studied. We report the effects of the addition of a monoamine oxidase B inhibitor, rasagiline, to antidepressant treatment in PD...

Rasagiline (Azilect(®)) is an oral, second-generation, selective, irreversible monoamine oxidase-B (MAO-B) inhibitor approved in the US for the treatment of Parkinson's disease. In randomized, controlled trials, oral rasagiline 1 mg once daily was superior to placebo in the symptomatic treatment of early Parkinson's disease, both as monotherapy or as an adjunct to dopamine agonists. Comparisons of early-start and delayed-start treatment suggested a disease-modifying effect for rasagiline, but the results were equivocal...

Increasing evidence suggests that dysregulation of brain insulin/insulin receptor (InsR) and insulin signaling cascade are associated with the pathogenesis of Alzheimer's disease (AD). Our group has designed and synthesized a series of multi-target iron chelating, brain permeable compounds for AD. One leading multi-target compound, M30 possesses the neuroprotective N-propargyl moiety of the anti-Parkinsonian, monoamine oxidase (MAO)-B inhibitor, rasagiline (Azilect®) and the antioxidant-iron chelating moiety of an 8-hydroxyquinoline derivative of the iron chelator, VK28...

Rasagiline (Azilect) is a highly selective and potent propargylamine inhibitor of monoamine oxidase (MAO) type B. Like other similar propargylamine inhibitors, rasagiline binds covalently to the N5 nitrogen of the flavin residue of MAO, resulting in irreversible inactivation of the enzyme. Therapeutic doses of the drug which inhibit brain MAO-B by 95% or more cause minimal inhibition of MAO-A, and do not potentiate the pressor or other pharmacological effects of tyramine. Metabolic conversion of the compound in vivo is by hepatic cytochrome P450-1A2, with generation of 1-aminoindan as the major metabolite...

Tremor is a common symptom of Parkinson's disease (PD). The underlying pathophysiology of parkinsonian rest tremor is not well understood. Rest tremor is less responsive to dopaminergic therapy than are symptoms of bradykinesia and rigidity. This paper reviews the effects of 1 mg daily oral rasagiline, as monotherapy and as adjunct therapy, on parkinsonian tremor. A literature search of the EMBASE database was conducted to identify relevant articles in English published between 2000 and October, 2012 using the search terms "rasagiline," or "Azilect®," or "Agilect®," and refined using the terms "Parkinson's disease" and "clinical trial...

Rasagiline (Azilect(®)) is a selective and irreversible monoamine oxidase B inhibitor, which is well tolerated, safe, improves motor symptoms, and prevents motor complications in Parkinson's disease (PD). Rasagiline is effective in monotherapy and as an adjunct to levodopa-therapy, with beneficial effects on quality-of-life parameters in early and late stages of PD. In this review, we compare the efficacy of rasagiline versus placebo for decreasing PD symptoms. Major databases (Medline, the Cochrane Library) were systematically searched to identify and select clinical randomized control trials of rasagiline...

INTRODUCTION: Rasagiline (Azilect, AGN 1135) is a selective irreversible inhibitor of monoamine oxidase B (MAO-B). MAO-B regulates the brain concentrations of important neurotransmitters that are related to movement, emotion, and cognition. Oral rasagiline, as monotherapy or as adjunctive therapy to levodopa, was effective in the symptomatic treatment of adult patients with Parkinson's disease participating in double-blind, placebo-controlled, international studies. AREAS COVERED: This article reviews the reported adverse effects of rasagiline...

Present anti-PD and -AD drugs have limited symptomatic activity and devoid of neuroprotective and neurorestorative property that is needed for disease modifying action. The complex pathology of PD and AD led us to develop several multi-target neuroprotective and neurorestorative drugs with several CNS targets with the ability for possible disease modifying activity. Employing the pharmacophore of our anti-parkinson drug rasagiline (Azilect, N-propagrgyl-1-R-aminoindan), we have developed a series of novel multi-functional neuroprotective drugs (A) [TV-3326 (N-propargyl-3R-aminoindan-5yl)-ethyl methylcarbamate)], with both cholinesterase-butyrylesterase and brain selective monoamine-oxidase (MAO) A/B inhibitory activities and (B) the iron chelator-radical scavenging-brain selective monoamine oxidase (MAO) A/B inhibitor and M30 possessing the neuroprotective and neurorescuing propargyl moiety of rasagiline, as potential treatment of AD, DLB and PD with dementia...

TVP1022, the S-enantiomer of rasagiline (Azilect®) (N-propargyl-1R-aminoindan), exerts cyto/cardio-protective effects in a variety of experimental cardiac and neuronal models. Previous studies have demonstrated that the protective activity of TVP1022 and other propargyl derivatives involve the activation of p42/44 mitogen-activated protein kinase (MAPK) signaling pathway. In the current study, we further investigated the molecular mechanism of action and signaling pathways of TVP1022 which may account for the cyto/cardio-protective efficacy of the drug...

Oral rasagiline (Azilect®) as monotherapy or as an adjunct to levodopa provides a useful option in the symptomatic treatment of adult patients with Parkinson's disease. In patients with early Parkinson's disease, monotherapy with rasagiline 1 mg/day improved symptoms of the disease relative to placebo. As adjunctive therapy to levodopa in patients with advanced Parkinson's disease, rasagiline 0.5 or 1 mg/day significantly reduces the total daily 'off' time. Rasagiline is generally well tolerated when administered as monotherapy or as adjunctive therapy...

This is a case report of a 69-year-old female with Parkinson's disease who developed an asymptomatic eruption on her legs bilaterally. Clinical and histologic examination was consistent with livedo reticularis, which was temporally associated with initiation of rasagiline. The pathogenesis of livedo reticularis is discussed along with the possible mechanisms for both rasagiline and amantidine causing drug-induced livedo reticularis in patients.