• 한국임상약학회지
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• 제30권1호
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• pp.59-64
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• 2020

The emergence of phosphodiesterase (PDE) 5 inhibitors gave rise to the solution for erectile dysfunction, starting with the development of sildenafil. Although their efficacy in treating erectile dysfunction has been shown, the side effects of PDE5 inhibitors, especially sildenafil, must be taken into consideration. A 64-year-old man received 100 mg of sildenafil and experienced blue vision in both eyes; however, after a day or so, his symptoms improved. The symptoms disappeared when he stopped administering sildenafil, but reappeared when the medication was re-administered. Therefore, he discontinued sildenafil treatment and was prescribed udenafil instead. After that, visual adverse events no longer occurred. Causality assessment showed that in this case, sildenafil-induced cyanopsia was "certain" under the World Health Organization-Uppsala Monitoring Center (WHO-UMC) criteria and Korean causality assessment algorithm (Ver.2), and was "probable" according to the Naranjo scale. In addition, sildenafil also led to abnormal visual reactions in other cases. Sildenafil can also inhibit PDE6, which is present in retinal cells, unlike other PDE5 inhibitors. Thus, visual adverse reactions, such as blue vision, are the unique results of sildenafil, and other PDE5 inhibitors may be used to prevent them.

• 약학회지
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• 제49권4호
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• pp.260-267
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• 2005

[ $PGE_1$ ] is an endogenous substance of potent vasodialator as well as inhibitor of platelet aggregation. It has been used therapeutically in peripheral arterial occlusive disease and impotence. Intracavernous injection of $PGE_1$ for erectile dysfunction has been established for several years as a treatment option for erectile dysfunction of diverse etiologies, but this mode of administration is limited by penile discomfort, pain at the injection site, inconvenience and noncompliance. As the matter of worse, the $\beta-hydroxy$ moiety of $PGE_1$ is extremely susceptible to dehydration in solution to give inactive $PGA_1$ and $PGB_1$. For the improvement of stability, rapid absorption at action site and the convenience of application, $PGE_1$ was formulated as urethral suppositories of three types of formulations, such as PEG, witepsol, and the mixture of PEG and witepsol. The stability test of $PGE_1$ and the release test in urinary suppositories were performed. Futhermore, the effect of enhancers and vehicle composition on the penetration of $PGE_1$ through excised rat skin was evaluated by permeability coefficient and enhancement ratio.

• 대한한방내과학회지
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• 제19권1호
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• pp.452-465
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• 1998

Rosae laevigatae Fructus extract (RLF) was tested for the effects on the urethral nitric oxide synthase (NOS) activity and Antioxidation in streptozotocin (STZ) induced diabetic rats. RLF was treated firstly into samples, and then STZ induced diabetic rats were set with them. In vitro, the urethral NOS activity was not noted but the type O activity and type conversion ratio of xanthine oxidase and the level of urethral lipid peroxide were decreased in the level of Dose of extract prepared from RLF. In vivo, after the extract was administered to the animal model for fifteen days, the urethral NOS activity increased in STZ induced diabetic rats to the level of normal rats. The content of urethral nitrite and glutathione followed by RLF pre-medicating administration, increased as highly as normal group in compare with the group treated with STZ. The type O activity and type conversion ratio of xanthine oxidase and the level of urethral lipid peroxide followed by RLF pre-medicating administration, decreased as lowly as normal group in compare with the group treated with STZ. In conclusion, the extract of RLF will be able to restore erectile dysfunction of STZ induced diabetic rats.

• 동의생리병리학회지
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• 제32권1호
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• pp.24-29
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• 2018

In order to define the effect of Torilis Fructus(TF) extract which has been used for the treatment of erectile dysfunction, experiments were carried out by organ bath study, histochemical and immunohistochemical methods. First, in the organ bath study, when TF extract was administered to the maxillary contracted corpus cavernosum by PE ($10^{-6}M$), there was a significant relaxation effect on corpus cavernosum at concentration of 1, $3mg/m{\ell}$. Compared with the absence of $\text\tiny{L}$-NNA pretreatmen, pretreatment of $\text\tiny{L}$-NNA was inhibited the relaxation effect of penile corpus cavernosum. In the immunohistochemical study, the eNOS positive reaction was significantly increased, and the PDE5 positive reaction was significantly decreased due to the administration of TF extract. Therefore, it show that the TF enhances the production of eNOS and NO, inhibits PDE5 which blocks the action of increased cGMP, relaxes the corpus cavernosum. So TF relaxes the corpus cavernosum and it can be used as a safer erectile dysfunction treatment.

• International Journal of Industrial Entomology and Biomaterials
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• 제5권1호
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• pp.123-126
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• 2002

More than three hundred million men in the world are suffering from erectile dysfunction. Korean ancient medical records say that the unmated male silkworm moth is effective in strengthening men's vitality, but no scientific examination has preyed its clinical efficacy. Currently, silkworm moths are not allowed for food-stuff. Thus, we selected silkworm of 14-days-after-metamorphosis, at which external morphology possesses that of pupae, but internal component is that of moths. To obtain the reliable source of unmated male silkworm moth, we used the sex-limited silkworm breed with larval marking. The body marker allows casual separation of sex during larval period, preventing mating right after emergence from cocoon. Using the extract prepared with the pupae of 14-days-after-metamorphosis, we investigated the tonic effect of the extract on the rat fed the extract for three weeks. The results showed that the testosterone levels in serum increased maximum by 19%, that of testicle increased maximum by 200%, and athletic endurance of the rats rose by 6%, suggesting positive tonic effect of the pupae prepared at the stage of 14 days after metamorphosis.

• Journal of Pharmaceutical Investigation
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• 제37권5호
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• pp.291-295
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• 2007

Prostaglandin $E_1\;(PGE_1)$ was formulated as two self-microemulsifying drug delivery systems (SMEDDS) composed of Cremophor $EL^{(R)}$ or Cremophor $ELP^{(R)}$ as a surfactant, ethanol as a cosurfactant and Labrafac $CC^{(R)}$ as an oil to develop liquid preparation for the treatment of erectile dysfunction. In pseudo-ternary phase diagram, viscous gel area and microemulsion area were defined. In the measurement of viscosity, the viscosity of two formulations increased gradually upon the addition of water and it decreased from the water contents over 40%. With excessive water, the present systems formed a microemulsion spontaneously. From these results, rte could expect that the present liquid $PGE_1$ SMEDDS formulations might stay within the urethra in the viscous state when contacting the moisture of the urethra and can be easily eliminated by urination. In long-term stability study, we could select one formulation more stable at the shelf storage condition of $4^{\circ}C$.

• 대한한의학회지
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• 제19권2호
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• pp.112-124
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• 1998

The purpose of this study was to investigate the effect of Brousson etiae fructus (BF) on the urethral nitrite level and the urethral nitric oxide synthase (NOS) activity in streptozotocin (STZ) induced diabetic rats. In vitro, the urethral NOS activity was not noted in the level of Dose of extract prepared from BF. In vivo, the urethral NOS activity was increased in normal rats and STZ induced diabetic rats by dose and term of extract prerared from BF. The the NOS activity decreased in STZ induced diabetic rats was increased as highly as norma1 group by the extract of BF The level of urethral nitrite and glutathione was increased too. But the level of urethral lipid peroxide increased in STZ induced diabetic rats was decreased as lowly as normal group by the extract of BF. In conclusion, the extract of BF can restore erectile dysfunction of STZ induced diabetic rats.

• Archives of Pharmacal Research
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• 제23권5호
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• pp.471-476
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• 2000

DA-8159, a new phosphodiesterase 5 inhibitor, was assessed for its erectogenic potential by a penile erection test in rats, the relaxation of isolated rabbit corpus cavernosum (CC), and estimation of the intracavernous pressure (ICP) in the anesthetized dog. Oral administration of DA-8159 (0.3 to 1 ${\mu}g/kg$ ) increased the number of erections in rats with increasing dosage, with the highest penile erection index at 10 ${\mu}g/kg$ DA-8159 induced the relaxation of phenylephrine (PHE)-induced contractions in the rabbit CC and decreased the $IC_{50}$ of the nitric oxide donor sodium nitroprusside (SNP) in a dose-dependent fashion. In pentobarbital-anesthetized dogs, the intravenous administration of DA-8159 (1~300 ${\mu}g/kg$ ) potentiated the increase in ICP induced by the intracavernosal SNP in a dose-related manner. These findings suggest that DA-8159 has significant therapeutic potential in the treatment of erectile dysfunction.

• Biomolecules & Therapeutics
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• 제11권4호
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• pp.232-237
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• 2003

The present study examined functional effects of a new selective phosphodiesterase type 5 inhibitor, 1-[4-ethoxy-3-(6,7-dihydro-1-methyl-7-thioxo-3-propyl-1H-pyrazolo[ 4,3]pyrimidin-5-yl)phenylsulphonyl]-4-methyl piperazine (KJH-1002), in the isolated rabbit corpus cavernosum (RCC). Relaxing effects of KJH-1002 were also compared with those of sildenafil, which is currently used as an oral therapy for penile erectile dysfunction. In the isolated RCC precontracted with phenylephrine, both KJH-1002 and sildenafil in the concentration range of 1 to 1000 nM, produced a comparable potentiation of the electical field stimulation-induced relaxation in a concentration-dependent manner. In the sodium nitroprusside (SNP)-induced relaxation, the $IC_{50}$/ values, concentrations of SNP required to produce a 50％ relaxation of the phenylephrine-induced contraction, were significantly decreased to the similar extent by treatments with KJH-1002 and sildenafil. The results suggest that a new selective phosphodiesterase type 5 inhibitor, KJH-1002, has an augmentative effect on penile erection comparable to that of sildenafil and can be useful for the treatment of erectile dysfunction.

• Clinical and Experimental Reproductive Medicine
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• 제43권1호
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• pp.26-30
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• 2016

Objective: We aimed to investigate the prevalence of erectile dysfunction (ED) and the usage of phosphodiesterase type 5 (PDE5) inhibitors for ED treatment in infertile couples. Methods: A total of 260 male partners in couples reporting infertility lasting at least 1 year were included in this study. In addition to an evaluation of infertility, all participants completed the International Index of Erectile Function (IIEF)-5 questionnaire to evaluate their sexual function. The participants were asked about their use of PDE5 inhibitors while trying to conceive during their partner's ovulatory period and about their concerns regarding the risks of PDE5 inhibitor use to any eventual pregnancy and/or the fetus. Results: Based on the IIEF-5 questionnaire, 41.5% of the participants (108/260) were classified as having mild ED (an IIEF-5 score of 17-21), while 10.4% of the participants (27/260) had greater than mild ED (an IIEF-5 score of 16 or less). The majority (74.2%, 193/260) of male partners of infertile couples had a negative perception of the safety of using a PDE5 inhibitor while trying to conceive. Only 11.1% of men (15/135) with ED in infertile couples had used a PDE5 inhibitor when attempting conception. Conclusion: ED was found to be common in the male partners of infertile couples, but the use of PDE5 inhibitors among these men was found to be very low. The majority of male partners were concerned about the risks of using PDE5 inhibitors when attempting to conceive. Appropriate counseling about this topic and treatment when necessary would likely be beneficial to infertile couples in which the male partner has ED.