Effect of 3 weeks treatment with yohimbine on salivary secretion in healthy volunteers and in depressed patients treated with tricyclic antidepressants.

Abstract

The effect of yohimbine treatment (4 mg three times daily) for 3 weeks on salivary secretion was investigated. In healthy volunteers, acute administration of yohimbine increased salivary volume within 1 h to a similar extent before and at the end of the treatment period. In depressed patients treated with tricyclic antidepressants (and exhibiting a reduced salivary flow), yohimbine also acutely increased salivary volume. In contrast, the alpha 2‐adrenoceptor antagonist failed to modify resting values measured in the morning (i.e. 10 and 14 h after the last administration in healthy volunteers and depressed patients respectively). This result indicates that alpha 2‐adrenoceptor antagonists may have a potential therapeutic use in the treatment of dry mouth caused by tricyclic antidepressant drugs.

Pharmacokinetic study of yohimbine and its pharmacodynamic effects on salivary secretion in patients treated with tricyclic antidepressants.

“…The present trial first confirms that acute administration of yohimbine (10 mg) restores a normal salivary volume in patients suffering from dry mouth due to treatment with imipramine derivatives [8]. Secondly, the data show that the effects of yohimbine on plasma catecholamine concentrations occurred for at least 4 h in patients treated with tricyclic antidepressants.…”

“…Since the pharmacokinetics of yohimbine were mainly studied in healthy volunteers and showed considerable interindividual variations [9][10][11][12], the present study was performed in order to evaluate the time course of the effects of yohimbine in patients treated with tricyclic antidepressants: firstly, the pharmacokinetic and pharmacodynamic effects were investigated after oral administration of 10 mg yohimbine. However, the patients treated with tricyclic antidepressants in a previous trial [8] and in the present study exhibited more side effects than healthy volunteers after administration of 10 mg yohimbine. Thus, in a second protocol, the effect of a lower dose of yohimbine (4 mg) once at 07.00 h after overnight fasting.…”

“…In a previous paper, we found that salivary outflow measured 1 h after acute administration of yohimbine was significantly increased. Moreover, this effect was not subjected to tolerance during a 3 week treatment with yohimbine in depressed patients treated with tricyclic antidepressants [8]. Since the pharmacokinetics of yohimbine were mainly studied in healthy volunteers and showed considerable interindividual variations [9][10][11][12], the present study was performed in order to evaluate the time course of the effects of yohimbine in patients treated with tricyclic antidepressants: firstly, the pharmacokinetic and pharmacodynamic effects were investigated after oral administration of 10 mg yohimbine.…”

Salivary Secretory Disorders, Inducing Drugs, and Clinical Management

“…A number of preparations based on herbs, for instance jaborandi which contains pilocarpine, and yohimbine supplements (alkaloids) considered to be peripheral adrenergic α2 antagonists, may stimulate salivary secretion 61 , 62 . In addition, the betel nut, a widely used drug chewed by millions of people in Southeast Asia, contains arecoline a direct muscarinic agonist which can cause “betel nut drooling”, whilst both citric acid and red pepper can stimulate saliva flow (Table 5 ) 13 .…”

A Randomized, Double-Blind, Placebo-Controlled, Cross-Over Study to Evaluate the Efficacy of AqualiefTM Mucoadhesive Tablets in Head and Neck Cancer Patients Who Developed Radiation-Induced Xerostomia

“…One clinical trial has compared pilocarpine and cevimeline [46] and found a slightly, but statistically not significantly, greater efficacy of pilocarpine in increasing saliva flow in patients with xerostomia. Other compounds that have been reported to be of some efficacy in the treatment of xerostomia with residual salivary gland function are anethol trithione, which simulates the parasympathetic nervous system, leading to increased secretion of acetylcholine and, consequently, to the stimulation of saliva secretion [47], and yohimbine, an α2-adrenergic receptor antagonist which leads, indirectly, to an increase of peripheral cholinergic activity [48]. Non-pharmacologic approaches that are used episodically for the treatment of xerostomia in these patients are electrical stimulation of the salivary glands [49] and acupuncture [50].…”