Background: Hydroxyzine hydrochloride is a piperazine derivative antihistamine that is used in the treatment of anxiety. Its tendency to cause somnolence makes it an attractive option for patients with anxiety-induced insomnia. Despite its antihistamine activity, hydroxyzine is noted to have alpha-adrenergic antagonism activity. Other alpha-adrenergic inhibitors have been implicated in medication-induced priapism, including risperidone. Risperidone is a second-generation antipsychotic that primarily blocks serotonin and dopamine receptors, while also inhibiting alpha-1 and alpha-2 receptors with high affinity. Objective: We report a case of a first-of-its-kind case report of a patient who was stable on risperidone and presented with priapism after taking hydroxyzine nightly for the previous 10 days. Results: A 35-year-old male with a past psychiatric history of depression, generalized anxiety disorder, schizoaffective disorder, presented to the emergency department with priapism for 15 hours that required intracaveronsal phenylephrine hydrochloride and manual drainage to achieve detumescence. The patient was on a stable dose risperidone but reported taking hydroxyzine 50 mg nightly for anxiety and insomnia 10 days prior to emergency department admission. Upon resolution of the priapism, the patient stopped hydroxyzine, but continued risperidone. The patient had another prolonged erection 10 days after stopping hydroxyzine; however, he reported that it resolved spontaneously without intervention after 4 hours. Conclusion: This case report demonstrates the risk of addition of hydroxyzine to antipsychotics which can result in an increased risk of priapism or prolonged episodes.

2022-12-01·Journal of affective disorders

Association of metformin and depression in patients with type 2 diabetes

Article

作者: Wang, Siyue ; Wu, Yiqun ; Hu, Yonghua ; Qin, Xueying ; Yang, Ruotong ; Wu, Tao ; Yu, Huan ; Wu, Junhui

BACKGROUND:

Emerging evidence showed metformin may have pleiotropic effects on ameliorating depression. However, whether metformin was associated with decreased risk of depression remains unclear.

METHODS:

A historical cohort study was conducted based on a medical claim database from 2010 to 2017 in Beijing, China. Patients newly diagnosed with T2D were classified into the metformin and non-metformin groups according to their initial antidiabetic prescription. The incidences of depression between the groups were compared using Cox proportional regression model.

RESULTS:

There were 193,624 (37.4 %) and 323,930 (62.6 %) T2D patients in the metformin and non-metformin groups. The mean age was 54.9 (SD: 13.1) years and 53.9% were females. With a median follow-up of 3.2 years, 64,963 patients developed depression. The adjusted incidence of depression in the metformin group (30.6, 95 % CI: 30.1, 31.0 per 1000 person-years) was significantly lower than in the non-metformin group (39.6, 95 % CI: 39.3, 40.0 per 1000 person-years, P < 0.001). The metformin group was significantly associated with a lower risk of depression compared with the overall non-metformin group (HR: 0.77, 95% CI: 0.75, 0.78), as well as compared with α-glucosidase inhibitors (HR: 0.73, 95 % CI: 0.71, 0.74), sulfonylureas (HR: 0.84, 95 % CI: 0.82, 0.86), and glinides (HR: 0.85, 95 % CI: 0.82, 0.88), except for thiazolidinediones (HR: 0.96, 95 % CI: 0.91, 1.01). The association between metformin and lower depression risk was significant in all the age and sex subgroups.

CONCLUSIONS:

Metformin was associated with a lower risk of depression compared with other oral hypoglycemic agents, indicating a potential pleiotropic effect on depression.

2022-08-01·Bioorganic & medicinal chemistry

Discovery of honokiol thioethers containing 1,3,4-oxadiazole moieties as potential α-glucosidase and SARS-CoV-2 entry inhibitors

Article

作者: Liu, Jia-Zheng ; Chu, Junyan ; Zhang, Qian ; Bai, Li-Ping ; Guo, Yong ; Meng, Jie-Ru ; Cheng, Wanqing ; Ma, Nannan ; Xu, Ting

Honokiol, isolated from a traditional Chinese medicine (TCM) Magnolia officinalis, is a biphenolic compound with several biological activities. To improve and broaden its biological activity, herein, two series of honokiol thioethers bearing 1,3,4-oxadiazole moieties were prepared and assessed for their α-glucosidase and SARS-CoV-2 entry inhibitory activities. Among all the honokiol thioethers, compound 7l exhibited the strongest α-glucosidase inhibitory effect with an IC₅₀ value of 18.9 ± 2.3 µM, which was superior to the reference drug acarbose (IC₅₀ = 24.4 ± 0.3 µM). Some interesting results of structure-activity relationships (SARs) have also been discussed. Enzyme kinetic study demonstrated that 7l was a noncompetitive α-glucosidase inhibitor, which was further supported by the results of molecular docking. Moreover, honokiol thioethers 7e, 9a, 9e, and 9r exhibited potent antiviral activity against SARS-CoV-2 pseudovirus entering into HEK-293 T-ACE2^h. Especially 9a displayed the strongest inhibitory activity against SARS-CoV-2 pseudovirus entry with an IC₅₀ value of 16.96 ± 2.45 μM, which was lower than the positive control Evans blue (21.98 ± 1.98 μM). Biolayer interferometry (BLI) binding and docking studies suggested that 9a and 9r may effectively block the binding of SARS-CoV-2 to the host ACE2 receptor through dual recognition of SARS-CoV-2 spike RBD and human ACE2. Additionally, the potent honokiol thioethers 7l, 9a, and 9r displayed relatively no cytotoxicity to normal cells (LO2). These findings will provide a theoretical basis for the discovery of honokiol derivatives as potential both α-glucosidase and SARS-CoV-2 entry inhibitors.

100 项与 Alpha-glucosidase inhibitor(Huadong Medicine) 相关的药物交易

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