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Drugs Affecting the Central Nervous System
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: It should be used with caution because the pregnancy experience in humans is limited, and the reproduction studies in animals have shown the risk of fetal toxicity associated with the use of Rasagiline.
Neurotransmitters and pharmacology
Published in Mark J. Ashley, David A. Hovda, Traumatic Brain Injury, 2017
Ronald A. Browning, Richard W. Clough
NE is degraded intraneuronally by the enzyme MAO as indicated previously. Inhibiting this enzyme should eventually increase the concentration of NE in the synaptic cleft. Several nonselective MAO inhibitors are used clinically as antidepressants. These include tranylcypromine (Parnate), phenelzine (Nardil®), and isocarboxazid (Marplan®). Selegiline marketed as a transdermal patch (Emsam®) is a selective MAO-B inhibitor that is FDA-approved for the treatment of depression. Selegiline marketed as Eldepryl® is also used for Parkinson’s disease (but not depression). Rasagiline (Azilect®) is another MAO-B inhibitor used for the treatment of Parkinson’s disease. Patients on MAO inhibitors, particularly those that contain MAO-A, cannot eat foods containing tyramine, a potent NE releaser. Normally, tyramine is metabolized by MAO in the intestine, but this enzyme is inactive in patients on an MAO-A inhibitor. Tyramine reaching the circulation causes a hypertensive crisis with very dangerous consequences. Thus, individuals taking MAO inhibitors must avoid foods containing tyramine, such as wine, beer, cheese, and other fermented products.
Movement Disorders
Published in John W. Scadding, Nicholas A. Losseff, Clinical Neurology, 2011
Two selective monoamine oxidase B inhibitors (MAOBIs), selegiline and rasagiline, are licensed for PD. They are so-called ‘suicide inhibitors’ which inactivate MAOB by irreversible binding so that recovery of full enzyme activity only occurs when sufficient new enzyme has been manufactured, 6 weeks or more after stopping the drug. Both have a mild symptomatic effect and can prolong the duration of action of levodopa doses in some patients. Selegiline (usual dose 10 mg in the morning) is partly metabolized to methamphetamine, so can cause insomnia. Another, buccally absorbed, formulation of selegiline called Zelapar (usual dose 1.25 mg in the morning) avoids hepatic first-pass metabolism, so is devoid of this effect. A putative neuroprotective effect on nigral neurones (selegiline and rasagiline block MPTP toxicity in non-human primates) is unproven in humans. Delayed-start studies of rasagiline (usual dose 1 mg in the morning) suggested a possible disease-modifying effect, but this was absent at 2 mg in the morning, so is controversial.
Safety review of current pharmacotherapies for levodopa-treated patients with Parkinson’s disease
Published in Expert Opinion on Drug Safety, 2023
Angela M Richmond, Kelly E Lyons, Rajesh Pahwa
LARGO and PRESTO demonstrated that adjunctive rasagiline is generally well tolerated, with similar rates of AEs between treatment and placebo groups [52,53]. Dyskinesia was the most common TEAE reported in patients taking rasagiline in PRESTO (18%) compared to placebo (10%), but in LARGO, its incidence was similar to patients taking placebo (5% vs 4%) [52,53]. Other common TEAEs occurring in < 5% of patients, and in some cases less than placebo, included balance difficulties, nausea, vomiting, weight loss, dizziness, depression, and sleep difficulties. Incidence of serious AEs (e.g. worsening PD symptoms, melanoma) in patients taking rasagiline was similar to, and again in some cases, less than placebo [52,53]. TEAEs led to treatment discontinuation in 3% of patients in LARGO [53]. There was no significant increase in TEAEs regarding age older or younger than 70 years [53].
Privileged multi-target directed propargyl-tacrines combining cholinesterase and monoamine oxidase inhibition activities
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Zofia Chrienova, Eugenie Nepovimova, Rudolf Andrys, Rafael Dolezal, Jana Janockova, Lubica Muckova, Lenka Fabova, Ondrej Soukup, Patrik Oleksak, Martin Valis, Jan Korabecny, José Marco-Contelles, Kamil Kuca
Rasagiline is an irreversible inhibitor of MAO-B used as a monotherapy to treat symptoms of early Parkinson’s disease (PD) or as an adjunct therapy in more advanced cases of PD21. Findings of structure–activity relationship (SAR) studies of rasagiline provided an evidence that particularly N-propargyl moiety is responsible for the promotion of neuronal survival, highlighting its importance in the design of our compounds22. However, sequential studies revealed that rasagiline’s neuroprotective activity is not dependent on MAO-B inhibition via the interaction of N-propargyl moiety with FAD co-factor of the enzyme, but on the ability of rasagiline to regulate the non-amyloidogenic processing of amyloid precursor protein23,24. Apart from N-propargyl moiety of rasagiline (8 − 15; Chart 1), we have also utilised N-allyl motif (1 − 7; Chart 1) for comparative purposes.
Design, synthesis, and evaluation of novel O-alkyl ferulamide derivatives as multifunctional ligands for treating Alzheimer’s disease
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Gaofeng Zhu, Ping Bai, Keren Wang, Jing Mi, Jing Yang, Jiaqi Hu, Yujuan Ban, Ran Xu, Rui Chen, Changning Wang, Lei Tang, Zhipei Sang
Ferulic acid (FA) is a polyphenol that is abundant in vegetables and maize bran. Several lines of evidence have displayed that FA would be hopeful for treating AD because of its scavenging free radicals, Aβ aggregation inhibition properties, anti-inflammatory properties, and neuroprotective effects13,14. However, the low bioavailability of FA limits its clinical uses in AD. Based on this, many groups have developed the FA derivative to treat AD14. Rasagiline, a selective MAO-B inhibitor, which has been approved for treating symptoms of Parkinson’s disease, is in Phase II clinical trial with mild to moderate AD, the data showed that Rasagiline improved blood flow in a separate small study of 11 people with AD treated for a median of 1.7 years with 1 mg per day, along with donepezil6. The propargyl group has been confirmed as the pharmacophore of rasagiline. In addition, evidences show that introducing benzyl derivatives and alkyl fragment into the skeleton could increase MAO-B inhibitory potency15. Thus, we plan to introduce the propargyl, benzyl, and alkyl fragment into the FA skeleton based on the MTDLs strategy and create novel O-alkyl ferulamide derivatives as multifunctional agents (Figure 2).