Efficacy and Safety of Apomorphine Sl vs Placebo for Male Erectile Dysfunction (Med)

Padma‐Nathan, Harin; Auerbach, Stephen M.; Lewis, R. M.; Lewand, Michaelene; Perdok, Renee

doi:10.1097/00005392-199904010-00859

Cited by 29 publications

(8 citation statements)

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“…The sexual side effects do, however, point to an enhancing effect of dopamine on sexual response, which is in line with evidence from studies in animals. In addition, there is evidence for a positive effect of bupropion, which is primarily a dopamine uptake inhibitor, on sexual functioning in women (Crenshaw and Goldberg, 1996;Segraves et al, 2004), and for a facilitating effect of apomorphine, a dopamine agonist, on sexual functioning in women with female sexual desire and arousal problems (Russell, 2002), and on erection in healthy men and in men with erectile dysfunction (Lal et al, 1984;Padma-Nathan et al, 1999). The latter resulted in the use of apomorphine in the treatment for erectile dysfunction (Giuliano and Allard, 2001;Heaton, 2000).…”

Section: Introductionmentioning

confidence: 99%

Effect of a Single Dose of Levodopa on Sexual Response in Men and Women

Both

Everaerd

Laan

et al. 2004

Neuropsychopharmacol

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From animal research, there is ample evidence for a facilitating effect of dopamine on sexual behavior. In humans, little experimental research has been conducted on the inter-relation between dopamine and sexual response, even less so in women than in men. We investigated the effect of levodopa (100 mg) on sexual response in men and women following a double-blind, placebo-controlled crossover design. Genital and subjective sexual responses were measured as well as somatic motor system activity by means of Achilles tendon (T) reflex modulation. Genital and subjective sexual arousal were not affected by levodopa. However, the drug increased T reflex magnitude in response to sexual stimulation in men, but not in women. These results support the view that dopamine is involved in the energetic aspects of appetitive sexual behavior in men. The observed gender difference in the effect of levodopa is discussed in the perspective of possible dopamine-steroid interaction.

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Section: Introductionmentioning

confidence: 99%

Effect of a Single Dose of Levodopa on Sexual Response in Men and Women

Both

Everaerd

Laan

et al. 2004

Neuropsychopharmacol

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“…2,3 Apomorphine is a nonselective dopaminergic receptor agonist used in the treatment of ED. 4,5 The reported binding affinity (Ki) for D1-like receptors is: D1, 101 nM and D5, 10 nM, while for D2-like receptors is: D2, 32 nM; D3, 26 nM and D4, 2.6 nM. 6 The dopaminergic properties of apomorphine were first recognized in the mid-1960s, when it was used to suppress refractory motor oscillation in Parkinson disease.…”

Section: Introductionmentioning

confidence: 99%

Peripheral relaxant activity of apomorphine and of a D1 selective receptor agonist on human corpus cavernosum strips

et al. 2004

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Apomorphine is used in the erectile dysfunction therapy and its action has been ascribed to the stimulation of central dopamine receptor. At the present stage, very little is known about the peripheral action of apomorphine on human corpus cavernosum (HCC). We have investigated the peripheral action of apomorphine and the role of dopamine receptors in HCC. We here demonstrate that both D1 and D2 receptors were expressed in the HCC, D1 receptors were two-fold more abundant than D2 and that both receptors were mainly localized on the smooth muscle cell component. Apomorphine in vitro exerted an anti-a 1 adrenergic activity in human cavernosal strips since it prevented contraction induced by phenylephrine (PE), but not by U46619 or endothelin. Apomorphine elicited endothelium-independent and concentration-dependent relaxation of the strips contracted by PE, U46619 or endothelin. The EC 50 values (lM) for apomorphine, in the presence and absence of endothelium, were 51.0716 and 16.0714, 120719 and 150718, 59.0715 and 140750 on PE-, U46619-or endothelin-induced contraction, respectively. Selective dopamine receptor agonist A-68930 (D1-like), but not quinpirole (D2-like), caused concentration-dependent relaxation of the cavernosal strips, which was partially prevented by endothelium removal or by treatment with an inhibitor of nitric oxide (NO) synthase. In conclusion, we show that (1) apomorphine has a peripheral relaxant direct effect as well as an antiadrenergic activity, (2) HCC possesses more D1-like (D1 and D5) than D2-like (D2, D3 and D4) receptors, (3) both D1-and D2-like receptors are mainly localized on smooth muscle cells and (4) the relaxant activity is most probably mediated by D1-like receptor partially through NO release from endothelium.

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“…1,2 Apomorphine formulated in sub-lingual, slow release tablets has appeared as a promising pharmacological treatment for erectile dysfunction of various origins. 3,4 The proerectile activity of apomorphine is caused by stimulation of supraspinal central dopaminergic receptors and, in this view, the paraventricular nucleus of the hypothalamus (PVN) has been identi®ed as a key target. 5,6 Cytological data suggest that apomorphine may also act at the spinal level.…”

Section: Introductionmentioning

confidence: 99%

Spinal proerectile effect of apomorphine in the anesthetized rat

et al. 2001

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Considering the presence of dopaminergic receptors in the lumbosacral spinal cord, we tested whether apomorphine could exert a proerectile effect by acting at the spinal level. Intracavernous (ICP) and blood pressures (BP) were measured in anesthetized rats. ICP rises were quanti®ed (duration, percentage of ICPmaximumameanBP (ICPmaxaBP 6 100), area under ICP curve (AUCaBP) and sum of AUCaBP after intravenous (i.v.) and intrathecal (i.t.) injections of apomorphine alone or in presence of i.t. oxytocin (10 ng). Both 10 and 30 m mg i.v. apomorphine dosings elicited erectile events evidenced by ICP rises. Upon the 30 m mg i.v. injection, duration of ICP rises were increased from 25 AE 10 to 69 AE 18 s (P`0.001), ICPmaxaBP 6 100 from 21 AE 3 to 50 AE 14% (P 0.001), AUCaBP from 3 AE 1 to 14 AE 6 s (P 0.002) and sum of AUCaBP from 5 AE 7 to 34 AE 35 s (P 0.021). Upon 30 m mg i.t. injections of apomorphine at the lumbosacral level, the number of ICP rises was increased from 0.2 AE 0.4 to 3.0 AE 1.5, ICPmaxaBP 6 100 from 16 AE 9 to 43 AE 12 and sum of AUCaBP from 1 AE 3 to 31 AE 15 s compared to vehicle injection (P`0.05 for all parameters). Injection of 30 m mg i.v. or i.t. apomorphine non-signi®cantly enhanced the number and amplitude of the ICP rises induced by 10 ng i.t. oxytocin. However, the enhancement of the amplitude of the ICP rises elicited by i.t. oxytocin was more pronounced with i.t. apomorphine than with i.v. apomorphine. These results suggest the existence of a spinal site of action for apomorphine which may (1) participate to generation of erection and (2) exerts a facilitator effect on erection of supraspinal origin.

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Efficacy and Safety of Apomorphine Sl vs Placebo for Male Erectile Dysfunction (Med)

Cited by 29 publications

References 0 publications

Effect of a Single Dose of Levodopa on Sexual Response in Men and Women

Effect of a Single Dose of Levodopa on Sexual Response in Men and Women

Peripheral relaxant activity of apomorphine and of a D1 selective receptor agonist on human corpus cavernosum strips

Spinal proerectile effect of apomorphine in the anesthetized rat

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