Opiate analgesics: the effect of agonist-antagonist character on prolactin secretion

Brown, Barry L.; Dettmar, P W; Dobson, Pauline R.M.; Lynn, Andrew; Metcalf, G.; Morgan, Barry A.

doi:10.1111/j.2042-7158.1978.tb13348.x

Cited by 25 publications

(2 citation statements)

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“…Acute bupre¬ norphine administration failed to induce the sup¬ pression of serum LH values observed by Mendelson et al (1982) after long-term treatment of heroin addicts with large doses of this opiod. Fur¬ thermore, we did not confirm the experimental data demonstrating a decrease in serum Prl levels recorded after buprenorphine administration in rats (Brown et al 1978). This probably reflects species differences, already observed after admini¬ stration of other opiod drugs, including nalorphine (Lien et al 1979;Rolandi et al 1981) and naloxone (Gold et al 1979;Rolandi et al 1982).…”

Section: Discussioncontrasting

confidence: 51%

Changes in pituitary secretion induced by an agonist-antagonist opioid drug, buprenorphine

Rolandi

Marabini

Franceschini

et al. 1983

Acta Endocrinologica

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The im administration in 6 healthy subjects of buprenorphine, a derivative of the morphine alkaloid thebaine with agonist-antagonist properties, resulted in a significant rise of serum Prl within 45\p=n-\240 min, a small and transient increase in serum GH and a significant fall in serum cortisol values. Conversely, no appreciable changes in the serum levels of the other hormones studied were found. The observed hormonal effects indicate that, in man, buprenorphine exerts an opiate agonist rather than an opiate antagonist effect.

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Section: Discussioncontrasting

confidence: 51%

Changes in pituitary secretion induced by an agonist-antagonist opioid drug, buprenorphine

Rolandi

Marabini

Franceschini

et al. 1983

Acta Endocrinologica

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“…Studies in several species report both exogenous and endogenous opioids stimulate prolactin acutely [131][132][133] . This effect is reversed by naloxone [134][135][136][137] , stimulated by serotoninergic pathways, and inhibited by dopaminergic pathways [138][139][140] . All opioid receptors at the hypothalamus have been implicated, especially µ-receptors 141,142 .…”

Section: Evidence In Animalsmentioning

confidence: 99%

The effect of opioid analgesics on pituitary function and quality of life

Lamprecht¹

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Objective: To evaluate pituitary function, sexual function and quality of life (QoL) in patients on oral or transdermal opioids for chronic non-cancer pain.Introduction and Literature Review: Opioid medication prescribing for chronic pain is on the rise in Australia. Despite its widespread use throughout history, many details about exogenous opioids remain poorly understood including its adverse effects. Research continues into the relationship between opioid use and the endocrine system. Of hormones under control of the anterior pituitary there is some evidence for opioid-induced adrenal insufficiency in some users, strong evidence of suppression of the hypothalamic-pituitary-gonadal axis, and weak evidence around the effects of chronic oral or transdermal opioids on the thyroid, growth hormone, and prolactin systems. Design and Methods: Cross-sectional study comparing pituitary function, QoL and sexual function in people on long-term opioid therapy (n = 40) versus an age and sex-matched control group (n = 25). Baseline pituitary function was assessed on blood samples collected prior to 0900h. Further testing with corticotropin (250μg IV) and metyrapone (30mg/kg) stimulation tests was undertaken on participants with serum cortisol <250nmol/L. Validated questionnaires were completed to assess QoL, fatigue and sexual function.Results: Secondary adrenal insufficiency (SAI) was identified on the basis of a failed stimulation test in 22.5% of opioid users versus no controls (P = 0.01). Opioid users with SAI had a higher median morphine equivalent daily dose (MEDD), P = 0.037 -50% with MEDD >200mg and 0% with MEDD <60mg had SAI. Among male participants, testosterone was inversely associated with body mass index (BMI) (P = 0.001) but not opioid use. A non-significant trend to low testosterone <8nmol/L in male opioid users (11/24 opioid users vs 2/14 control, P = 0.08) suggests a small sub-group with opioid-induced androgen deficiency. Opioid users had greater fatigue, reduced quality of life in all subsections of the SF-36 and impaired sexual function in both males and females (all scores P < 0.001 compared to controls). While opioid users with lower morning cortisol reported poorer bodily pain, questionnaires were otherwise not predictive of hormone deficiency.Conclusion: Long-term opioid therapy was associated with dose-related SAI in over 20% of chronic pain patients and is associated with poor quality of life, fatigue and sexual dysfunction.Elevated BMI may contribute to low testosterone in male opioid users. The most striking finding of the study is the rate of SAI, which raises important questions requiring further research about Publications included in this thesisNo publications included.

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Central Actions of Opiates and Opioid Peptides

Wood¹,

Iyengar²

1988

The Opiate Receptors

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Opiate analgesics: the effect of agonist-antagonist character on prolactin secretion

Cited by 25 publications

References 10 publications

Changes in pituitary secretion induced by an agonist-antagonist opioid drug, buprenorphine

Changes in pituitary secretion induced by an agonist-antagonist opioid drug, buprenorphine

The effect of opioid analgesics on pituitary function and quality of life

Central Actions of Opiates and Opioid Peptides

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