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Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Nicergoline is a substrate of CYP2D6 (Bottiger et al. 1996). Nicergoline, an ergot derivative previously used as a vasodilator because of its α receptor blocking activity (Moretti et al. 1979), has been used in the treatment of senile dementia (Albus et al. 1986; Baskys and Hou 2007; Fioravanti and Flicker 2001). It decreases vascular resistance and increases arterial blood flow in the brain, improving the utilization of oxygen and glucose metabolism by brain cells. Nicergoline is rapidly hydrolyzed to an alcohol derivative, 1-methyl-10α-methoxy-9,10-dihydrolysergol (MMDL), which is further N-demethylated to form 10α-methoxy-9,10-dihydrolysergol (MDL) or hydroxylated to 1-OH-MMDL (Figure 3.47) (Arcamone et al. 1972). In healthy subjects, the plasma levels of MDL are much higher than those of MMDL. In PMs of CYP2D6, but not CYP2C19, the AUC of MDL is significantly lower than that in EMs but the AUC of MMDL is significantly higher than that in EMs (Bottiger et al. 1996).
Effects of Antithrombotic and Results of Drug Screening
Published in Josef Hladovec, Antithrombotic Drugs in Thrombosis Models, 2020
A very limited number of studies exists with ketanserin or other antiserotonins in thrombosis models. Some of these were not designed to explore the possible preventive effect of the drug, but rather the secondary consequences of an already existing thrombosis. Thus, Gautier et al.556 used methysergide, BC 105, and some ergot derivatives as effective inhibitors of white body formation in the cerebral microcirculation of rabbits. Using ketanserin, Humphrey and Aiken557 substantially decreased the transient platelet thrombus formation in stenosed canine coronary arteries (0.03 to 0.3 mg/kg i.v.). Bush et al.558 prevented by i.v. ketanserin (0.25 to 0.5 mg/kg) the cyclic flow reductions due to transient platelet aggregate formation. In their further studies even much lower doses were effective.559 Ashton et al.560, 561 in the same model confirmed the important role of 5-HT as a mediator and potentiating agent of other mediators of the phenomenon. They also confirmed the protective activity of ketanserin. De Clerck et al.562 prevented by ketanserin the inhibitory effect of platelets on the development of collateral circulation in cats with an occluding thrombus in the aorta and noted improved perfusion. Kordenat and Kezdi563 observed a protective effect of methysergide in an acute and chronic coronary thrombosis induced in dogs by the insertion of a thrombogenic wire via a catheter. A decreased accumulation of 5-HT in the myocardium and less severe necrotic changes were recorded. Sandler and Gerdin564 observed a preventive effect of methysergide pretreatment on a thrombin-induced DIC and pulmonary edema in rats. Cyproheptadine inhibited the development of occlusive thrombi in injured peripheral canine arteries30 and in primate AV-shunts.54 Cyproheptadine likewise protected pigs against endotoxin DIC.565 Der Agopian et al.566 inhibited with nicergoline (presented as an alpha- blocking agent, also possessing antiserotonin activity) traumatic thrombosis in the cortical microcirculation of rabbits. Bolli et al.567 noted inhibition of cyclic flow reductions in canine coronary arteries by the same agent. An interesting observation was a very specific antagonism of serotonin-induced platelet aggregation by 5-hydroxykynurenamide.568 A preventive effect of BOL-148, chlorpromazine, and other drugs was observed against an in vitro “thrombosis” in the Chandler apparatus by Michal and Penglis569 explained as an inhibition of 5-HT platelet uptake.
Use of Nicergoline as Adjunctive Treatment of Neurotrophic Keratitis in Routine Clinical Practice: A Case Series
Published in Ocular Immunology and Inflammation, 2022
L. Miguel-Escuder, C. Rocha-de-Lossada, N. Sabater-Cruz, José-María Sánchez-González, F. Spencer, S. Marín-Martínez, S. Batlle-Ferrando, X. Carreras Castañer, J. Torras, J. Peraza-Nieves
Nicergoline, (Sermion® [Biogenesis AntiAging, Fish Hock, South Africa]), is an ergot alkaloid derivative clinically available from the 1970s. Nicergoline has neurotrophic and antioxidant properties; it is widely used in the treatment of cognitive impairment secondary to ischemic stroke and other degenerative dementias, migraine or, dizziness.5 Nicergoline has been reported to accelerate wound healing in rat corneas.6 Likewise, recently a prospective study demonstrated with the off-label use of nicergoline a wound healing rate of 85% in patients with NK refractory to conventional therapy.7 In this series of cases, our aim is to describe the effectiveness and safety of the off-label use of nicergoline in patients with NK in real-life clinical practice, reinforcing previous outcomes.7
Neurotrophic keratopathy: current challenges and future prospects
Published in Annals of Medicine, 2022
Erin NaPier, Matthew Camacho, Timothy F. McDevitt, Adam R. Sweeney
Finally, nicergoline is an ergoline derivative that is used to treat cognitive impairment after dementia and stroke. Oral administration has been shown to increase NGF secretions in rat tears and lacrimal glands and lead to an increased rate of rat corneal healing [51]. A prospective non-comparative study of 27 eyes reported an 85% rate of complete healing of epithelial defects, and improved best-corrected visual acuity, increased corneal sensitivity, and tear nerve growth factor levels [52]. Comparative and randomized nicergoline formulations are needed.