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Diphenidol Hydrochloride

What Is Diphenidol Hydrochloride?

Diphenidol hydrochloride is an organic compound with the chemical formula C21H27NO-HCl and a molecular weight of 345.91. It serves as an antidiarrheal agent, primarily used to treat vertigo associated with inner ear disorders, Meniere’s disease, vestibular neuritis, and symptoms related to vestibular dysfunction.

Uses of Diphenidol Hydrochloride

Diphenidol hydrochloride, administered orally as a tablet or capsule, is taken three to four times daily. It effectively treats vertigo and alleviates symptoms of motion sickness, nausea, and vomiting, particularly post-surgery. Common side effects include mild and transient drowsiness, headache, dry mouth, and gastrointestinal symptoms like nausea, vomiting, and constipation.

Due to potential serious side effects and allergic reactions, patients should promptly report any unusual symptoms to their physician. Caution is advised when administering diphenidol hydrochloride to patients with glaucoma, obstructive urinary tract diseases, or gastrointestinal tract obstructions.

Properties of Diphenidol Hydrochloride

Diphenidol hydrochloride, with a molecular formula C21H27NO・HCl and molecular weight of 345.91, is a white crystalline powder almost insoluble in diethyl ether, slightly soluble in water, and soluble in ethanol and methanol. It decomposes at approximately 217°C.

Structure of Diphenidol Hydrochloride

The chemical name of diphenidol hydrochloride is “1,1-diphenyl-4-piperidin-1-ylbutan-1-ol monohydrochloride.” It contains two phenyl groups, a hydroxyl group at its benzyl position, and is classified as a tertiary alcohol. The planar arrangement of the molecule is characterized by the two phenyl groups, while the piperidine ring and hydroxyl group contribute to its unique three-dimensional structure.

Other Information on Diphenidol Hydrochloride

1. Production Process

Synthesized in 1946 by Miescher et al., diphenidol hydrochloride is commonly manufactured through total synthesis. In Japan, it is marketed under the name “Cefadol Tablets” by Nippon Shinyaku Co.

2. Mechanism of Action

Although not entirely clear, diphenidol hydrochloride is believed to alleviate vasoconstriction of the vertebral artery, increasing blood flow to improve the excitability imbalance between the left and right vestibular systems. It blocks abnormal impulses from the peripheral vestibular system at the vestibular nucleus and hypothalamus, correcting imbalances in the equilibrium system. Administered orally, it reaches peak blood levels in approximately 1.6 hours and has a half-life of about 6.5 hours.

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