Selegiline MAO inhibitor
Selegiline (L-deprenyl) is an irreversible MAO-B inhibitor created in Joseph Knoll's Budapest laboratory in the 1960s and prescribed for Parkinson's disease and, as a skin patch, for major depression. In early Parkinson's disease 10 mg a day delayed the need for levodopa by about nine months, though whether that was protection or symptom relief was never settled; the patch beat placebo modestly in adult depression and not at all in adolescents. It is broken down to l-methamphetamine and l-amphetamine. Its reputation as an anti-aging drug rests on rat longevity studies that replicated inconsistently, and a Cochrane review found no clinically meaningful benefit in Alzheimer's disease.
Established1984 · other · L-deprenyl plus L-phenylalanine in the treatment of depression. 1988 · preclinical · The striatal dopamine dependency of life span in male rats. Longevity study with (-)deprenyl. 1988 · clinical trial · Enhanced pressor sensitivity to oral tyramine challenge following high dose selegiline treatment. 1989 · RCT · Effect of deprenyl on the progression of disability in early Parkinson's disease. 1989 · clinical trial · A controlled study of the antidepressant efficacy and side effects of (-)-deprenyl. A selective monoamine oxidase inhibitor. 1993 · RCT · Effects of tocopherol and deprenyl on the progression of disability in early Parkinson's disease. 1993 · preclinical · Chronic treatment of aged mice with L-deprenyl produces marked striatal MAO-B inhibition but no beneficial effects on survival, motor performance, or nigral lipofuscin accumulation. 1993 · preclinical · Chronic treatment of (-)deprenyl prolongs the life span of male Fischer 344 rats. Further evidence. 1994 · review · Pharmacokinetic aspects of l-deprenyl (selegiline) and its metabolites. 1994 · RCT · High-dose selegiline in treatment-resistant older depressive patients. 1994 · clinical trial · Slow recovery of human brain MAO B after L-deprenyl (Selegeline) withdrawal. 1994 · preclinical · Multiple, small dose administration of (-)deprenyl enhances catecholaminergic activity and diminishes serotoninergic activity in the brain and these effects are unrelated to MAO-B inhibition. 1995 · RCT · Comparison of therapeutic effects and mortality data of levodopa and levodopa combined with selegiline in patients with early, mild Parkinson's disease. Parkinson's Disease Research Group of the United Kingdom. 1995 · RCT · Selegeline hydrochloride treatment in narcolepsy. A double-blind, placebo-controlled study. 1995 · preclinical · Enhanced catecholaminergic and serotoninergic activity in rat brain from weaning to sexual maturity: rationale for prophylactic (-)deprenyl (selegiline) medication. 1996 · RCT · Selegiline in adults with attention deficit hyperactivity disorder: clinical efficacy and safety. 1996 · RCT · A controlled trial of deprenyl in children with Tourette's syndrome and attention deficit hyperactivity disorder. 1996 · preclinical · L-deprenyl treatment in aged mice slightly increases life spans, and greatly reduces fecundity by aged males. 1996 · preclinical · (-)Deprenyl and (-)1-phenyl-2-propylaminopentane, [(-)PPAP], act primarily as potent stimulants of action potential-transmitter release coupling in the catecholaminergic neurons. 1996 · RCT · Tyramine pressor sensitivity in healthy subjects during combined treatment with moclobemide and selegiline. 1997 · RCT · A controlled trial of selegiline, alpha-tocopherol, or both as treatment for Alzheimer's disease. The Alzheimer's Disease Cooperative Study. 1997 · preclinical · Chronic treatment of Syrian hamsters with low-dose selegiline increases life span in females but not males. 1997 · preclinical · Long-term treatment of male F344 rats with deprenyl: assessment of effects on longevity, behavior, and brain function. 1997 · preclinical · Treatment with L-deprenyl prolongs life in elderly dogs. 1997 · review · Clinical pharmacokinetics and pharmacodynamics of selegiline. An update. 1997 · other · Metabolism of selegiline in humans. Identification, excretion, and stereochemistry of urine metabolites. 1997 · observational · Autonomic effects of selegiline: possible cardiovascular toxicity in Parkinson's disease. 1997 · observational · Serotonin syndrome and the combined use of deprenyl and an antidepressant in Parkinson's disease. Parkinson Study Group. 1998 · RCT · Mortality in DATATOP: a multicenter trial in early Parkinson's disease. Parkinson Study Group. 1998 · meta-analysis · Effect of selegiline on mortality in patients with Parkinson's disease: a meta-analysis. 1998 · preclinical · Long-term administration of (-)-deprenyl increases mortality in male Wistar rats. 1999 · preclinical · (-)1-(Benzofuran-2-yl)-2-propylaminopentane, [(-)BPAP], a selective enhancer of the impulse propagation mediated release of catecholamines and serotonin in the brain. 2001 · review · Antiaging compounds: (-)deprenyl (selegeline) and (-)1-(benzofuran-2-yl)-2-propylaminopentane, [(-)BPAP], a selective highly potent enhancer of the impulse propagation mediated release of catecholamine and serotonin in the brain. 2002 · RCT · Transdermal selegiline in major depression: a double-blind, placebo-controlled, parallel-group study in outpatients. 2003 · meta-analysis · Selegiline for Alzheimer's disease. 2003 · RCT · A double-blind, placebo-controlled trial of the safety and efficacy of selegiline transdermal system without dietary restrictions in patients with major depressive disorder. 2003 · RCT · Selegiline in the treatment of attention deficit hyperactivity disorder in children: a double blind and randomized trial. 2003 · RCT · A new formulation of selegiline: improved bioavailability and selectivity for MAO-B inhibition. 2003 · review · Neuroprotection by deprenyl and other propargylamines: glyceraldehyde-3-phosphate dehydrogenase rather than monoamine oxidase B. 2003 · preclinical · Enhancer substances: selegiline and R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane [(-)-BPAP] enhance the neurotrophic factor synthesis on cultured mouse astrocytes. 2004 · meta-analysis · Monoamine oxidase type B inhibitors in early Parkinson's disease: meta-analysis of 17 randomised trials involving 3525 patients. 2004 · RCT · Zydis selegiline reduces off time in Parkinson's disease patients with motor fluctuations: a 3-month, randomized, placebo-controlled study. 2004 · RCT · Selegiline in comparison with methylphenidate in attention deficit hyperactivity disorder children and adolescents in a double-blind, randomized clinical trial. 2004 · clinical trial · Transdermal selegiline and intravenous cocaine: safety and interactions. 2005 · RCT · Double-blind, placebo-controlled, multicenter trial of selegiline augmentation of antipsychotic medication to treat negative symptoms in outpatients with schizophrenia. 2005 · preclinical · Dose-dependency of life span prolongation of F344/DuCrj rats injected with (-)deprenyl. 2005 · RCT · A comprehensive assessment of the safety of intravenous methamphetamine administration during treatment with selegiline. 2006 · RCT · Selegiline transdermal system for the treatment of major depressive disorder: an 8-week, double-blind, placebo-controlled, flexible-dose titration trial. 2006 · RCT · Selegiline transdermal system in the prevention of relapse of major depressive disorder: a 52-week, double-blind, placebo-substitution, parallel-group clinical trial. 2006 · RCT · Placebo-controlled study examining effects of selegiline in children with attention-deficit/hyperactivity disorder. 2006 · RCT · Double-blind, placebo-controlled trial of selegiline transdermal system (STS) for the treatment of cocaine dependence. 2006 · clinical trial · Tyramine pressor sensitivity during treatment with the selegiline transdermal system 6 mg/24 h in healthy subjects. 2007 · RCT · Pharmacokinetics and absolute bioavailability of selegiline following treatment of healthy subjects with the selegiline transdermal system (6 mg/24 h): a comparison with oral selegiline capsules. 2010 · RCT · A double-blind, placebo-controlled, randomized clinical trial of oral selegiline hydrochloride for smoking cessation in nicotine-dependent cigarette smokers. 2012 · RCT · Selegiline transdermal system (STS) as an aid for smoking cessation. 2014 · RCT · A double-blind, placebo-controlled study of selegiline transdermal system in depressed adolescents. 2015 · clinical trial · Evidence that formulations of the selective MAO-B inhibitor, selegiline, which bypass first-pass metabolism, also inhibit MAO-A in the human brain. 2016 · review · The significance of selegiline/(-)-deprenyl after 50 years in research and therapy (1965-2015). 2016 · preclinical · Longevity study with low doses of selegiline/(-)-deprenyl and (2R)-1-(1-benzofuran-2-yl)-N-propylpentane-2-amine (BPAP). 2016 · review · A simple practice guide for dose conversion between animals and human. 2021 · case report · Detection of l-Methamphetamine and l-Amphetamine as Selegiline Metabolites. 2022 · preclinical · Enhancer Regulation of Dopaminergic Neurochemical Transmission in the Striatum. 2023 · meta-analysis · Efficacy and safety of selegiline across different psychiatric disorders: A systematic review and meta-analysis of oral and transdermal formulations. 2023 · meta-analysis · Efficacy and safety of selegiline for the treatment of Parkinson's disease: A systematic review and meta-analysis. 2023 · preclinical · Striking Neurochemical and Behavioral Differences in the Mode of Action of Selegiline and Rasagiline.