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Molecular Aspects of the Activity and Inhibition of the FAD-Containing Monoamine Oxidases
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
The pharmacological exploitation of MAO inhibitors as drugs began with the serendipitous discovery that the tubercular drug iproniazid had antidepressant effects (reviewed in Tipton, 2018). Despite the cheese effect of the non-selective irreversible inhibitors, the most effective MAO inhibition is still achieved by irreversible inhibition. Drugs such as pargyline and tranylcypromine are underused in psychiatry, yet the reversible MAO A-selective antidepressant drug, moclobemide, works only in some cases of depression. MAO B-selective reversible inhibitors have been slow to appear but safinamide (Ki for MAO B 450 nM) has now been approved by the FDA for use as adjunct therapy in Parkinson’s disease. The therapeutic potential of MAOI is clearly recognized (Youdim et al., 2006), with recent efforts yielding patents for new reversible inhibitors or for inhibitors that also target other features of degenerative disease (multi-target compounds) as will be discussed below.
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
Safinamide is available as 50 and 100 mg tablets [125]. The recommended starting dose is 50 mg daily, which can be increased to 100 mg daily after 2 weeks to achieve an optimal clinical response [125]. It is rapidly absorbed, with a Tmax between 2–3 h and steady state attainment within 5–6 d [125]. Safinamide is almost completely absorbed, with a bioavailability of 95%, yielding > 90% MAO-B inhibition [121,125]. Safinamide is metabolized via three different pathways; reduced dosing is required with moderate liver dysfunction, and avoidance recommended with severe hepatic dysfunction. The majority is renally excreted, with a T½ of 20–30 h [121].
Efficacy and safety evaluation of safinamide as an add-on treatment to levodopa for parkinson’s disease
Published in Expert Opinion on Drug Safety, 2022
Kanako Kurihara, Takayasu Mishima, Shinsuke Fujioka, Yoshio Tsuboi
At present, safinamide has been shown to be effective as a drug added to levodopa for patients with wearing off, but it is expected that data will be accumulated as a therapeutic drug for Parkinson’s disease at an earlier stage in the future.