Yohimbine pharmacokinetics and interaction with the sympathetic nervous system in normal volunteers

@article{Hedner2005YohimbinePA,
  title={Yohimbine pharmacokinetics and interaction with the sympathetic nervous system in normal volunteers},
  author={Thomas Hedner and Boo Edgar and Lars Edvinsson and Jan Hedner and Bengt Persson and Anders Pettersson},
  journal={European Journal of Clinical Pharmacology},
  year={2005},
  volume={43},
  pages={651-656}
}
SummaryThe pharmacokinetics of yohimbine and its effects on sympathoadrenal function were studied in 13 young, healthy, male volunteers after an IV bolus dose of 0.25 or 0.5 mg · kg−1.Pharmacokinetic analysis showed that distribution was rapid, with a half life between 0.4 and IS min, and the elimination half life ranged between 0.25 and 2.5 h. The volume of distribution (Vss) was 741, (range 26 to 1271). Only 0.5 to 1 % of unchanged yohimbine was found in the urine, indicating that the major… Expand
The effects of yohimbine on the pharmacokinetic parameters of detomidine in the horse.
TLDR
The increased plasma concentrations in the presence of detomidine has the potential to cause untoward effects and therefore further studies to assess the physiologic effects of this combination of drugs are warranted. Expand
The antagonistic effects of atipamezole and yohimbine on stress-related neurohormonal and metabolic responses induced by medetomidine in dogs.
  • T. Ambrisko, Y. Hikasa
  • Medicine
  • Canadian journal of veterinary research = Revue canadienne de recherche veterinaire
  • 2003
TLDR
When medetomidine-induced sedation is antagonized in dogs, it is recommended to use atipamezole IM, from 2- to 6-fold the dose of medetamidine, unless otherwise indicated. Expand
Effects of three antagonists on selected pharmacodynamic effects of sublingually administered detomidine in the horse.
TLDR
At the doses administered in this study, the alpha2 -adrenergic antagonistic effects of tolazoline, yohimbine and atipamezole on cardiac and behavioral effects elicited by SL administration of detomidine are transient and incomplete. Expand
Yohimbine Attenuates Baroreflex-Mediated Bradycardia in Humans
TLDR
Yohimbine selectively attenuates baroreflex heart rate control in normotensive young men possibly through parasympathetic mechanisms as well as endogenous &agr;-2 adrenergic tone mediates a similar response. Expand
Oral Yohimbine as a New Probe Drug to Predict CYP2D6 Activity: Results of a Fixed-Sequence Phase I Trial
TLDR
Yohimbine is proposed to be a suitable probe drug to predict CYP2D6 activity and the microdose can be used in combination with microdosed midazolam to simultaneously evaluate CYP3A activity without any interaction between the probe drugs and because the microdoses exert no pharmacological effects. Expand
Cardiovascular reactivity to mental stress is not affected by alpha2-adrenoreceptor activation or inhibition
TLDR
Cardiovascular reactivity to mental stress is not related to pharmacologically manipulated tonic central sympathetic nervous system activity by alpha2-adrenergic agonists and antagonists, and these results do not support the assumption that cardiovascular reactivity is an index of toniccentral sympathetic nervous System activity. Expand
Yohimbine-Induced Amygdala Activation in Pathological Gamblers: A Pilot Study
TLDR
The present data support the hypothesis of brain sensitization to pharmacologically-induced stress in PG, and reveal significant left amygdala activation in response to yohimbine across all PG subjects. Expand
An Overview of Yohimbine in Sports Medicine
TLDR
Yohimbine is an α2-adrenoreceptor antagonist that has been popularized in various supplements and is often mixed with other ingredients and its effect must be regarded mainly as a stimulant and toxicity should be avoided with higher doses. Expand
The impact of Yohimbine-induced arousal on facets of behavioural impulsivity
TLDR
These results support the notion that impulsive behaviour is dependent upon state physiological arousal; however, distinct facets of impulsivity are differentially affected by physiological changes. Expand
Yohimbine Use for Physical Enhancement and Its Potential Toxicity
TLDR
Yohimbine is a naturally sourced pharmacological agent, which produces hyperadrenergic physiological effects, which may typically cause agitation, anxiety, hypertension, and tachycardia. Expand
...
1
2
3
...

References

SHOWING 1-10 OF 36 REFERENCES
The pharmacokinetics of yohimbine in man
TLDR
The results suggest that yohimbine is eliminated primarily through metabolism since the rapid plasma clearance of yohimine was not the result of renal elimination or sequestration by RBC. Expand
The pharmacokinetic properties of yohimbine in the conscious rat
TLDR
The rapid entry of yohimbine into the brain, the slow rate of elimination of yOHimbine from serum and brain and the linear relationship of brain yohimine concentration as a function of dose should be taken into consideration whenever yohIMine is to be used as a probe of α2-adrenoceptor function in vivo. Expand
Is yohimbine effective in the treatment of organic impotence? Results of a controlled trial.
TLDR
The response rate of organically impotent patients to yohimbine is at best marginal and the substance has shown modest effectiveness at the doses used in this trial (18 mg. per day). Expand
Oral yohimbine in human autonomic failure
TLDR
Yohimbine may be useful in the treatment of orthostatic hypotension associated with autonomic failure and enhances discharge of the patient's own sympathetic system, unique among current modes of therapy for this disorder. Expand
Ketanserin in essential hypertension: Effects during rest and exercise
TLDR
It is concluded that ketanserin lowers BP in essential hypertension without interference with cardiovascular reflexes during standing or exercise, and that the compound may offer an alternative approach in the treatment of hypertension. Expand
Assessment of α2 adrenergic autoreceptor function in humans: Effects of oral yohimbine
TLDR
Results indicate that determination of the plasma MHPG response to yohimbine may be of value in assessing alpha 2 adrenergic autoreceptor function in humans. Expand
Autonomic and psychic effects of yohimbine hydrochloride
TLDR
Central nervous system depressants, amobarbital and Ro 5–0690, reduced the degree of response to yohimbine, whilst the CNS stimulants imipramine and epinephrine potentiated the yohimine effect. Expand
Effect of yohimbine on blood pressure in patients with depression and orthostatic hypotension induced by clomipramine
TLDR
Yohimbine, a selective α2‐adrenoceptor antagonist, had a favorable effect in orthostatic hypotension and induced a significant increase in blood pressure and a pharmacodynamic and pharmacokinetic interaction between yohimbines and clomipramine or demethylclomipramsine was discussed. Expand
Effects of yohimbine in obsessive compulsive disorder
TLDR
The data suggest it is unlikely that abnormal noradrenergic function plays a primary role in the pathogenesis of OCD, and that OCD patients, like previous reports of depressed and panic disorders patients, had an increased cortisol response to yohimbine. Expand
α2‐Antagonist compounds and lipid mobilization: evidence for a lipid mobilizing effect of oral yohimbine in healthy male volunteers
Abstract. Investigations were carried out to analyse the interactions of α2‐antagonists (yohimbine, idazoxan, SK & F‐86,466) with human fat cell α2‐adrenoceptors. All the α2‐antagonists enhanced theExpand
...
1
2
3
4
...