It has recently been reported that both norepinephrine and dopamine elicit antidiuresis when given intracerebroventricularly. But no inference has been made as to their mechanisms. As dopamine is the immediate precursor of norepinephrine in the biosynthesis of catecholamine, it might be possible that dopamine might act indirectly through increased level of norepinephrine in the brain tissue. To certify whether the dopamine-induced antidiuresis is related to norepinephrine, the influence of phentolamine, a specific alpha-adrenergic blocking agent, on the centrally induced antidiuresis of both norepinephrine and dopamine was investigated in this study. Norepinephrine and dopamine given intraventricularly elicited maximal antidiuresis in doses of 10ug and 500ug, respectively. Phentolamine, administered intravenously in dose of 2mg/kg, abolished the renal effect of norepinephrine given intraventricularly, but did not influence the antidiuresis induced by dopamine. It is suggested that both norepinephrine and dopamine produce antidiuresis when given intracerebroventricularly but their actions are mediated by different mechanisms, and that norepinephrine does not participate in the renal action of dopamine.
Brain ; Dopamine* ; Norepinephrine* ; Phentolamine*

An in vitro pharmacologic study was conducted to investigate the effect of phentolamine on norepinephrine induced contraction of human corpus cavernosum. The isometric muscle tension of corpus cavernosum from 4 potent volunteers were recorded after stimulation with various concentrations of norepinephrine and phentolamine. The results are summarized as follows. Contractile response of corpus cavernosum was observed to begin in the concentration of 10(-6) M and to reach maximal level in the concentration of 10(-4)M norepinephrine. Compared to it, contractile activity of corpus cavernosum to norepinephrine was observed to be gradually decreased in response to pretreatment with phentolamine from 10(-6)M to 10(-4)M. These indicate that norepinephrine causes a dose dependent contraction of corpus cavernosum and phentolamine had a relaxant effect on norepinephrine-induced contraction of corpus cavernosum in dose dependent manner.
Humans ; Muscle Tonus ; Norepinephrine* ; Phentolamine* ; Volunteers

The effects of intraventricular atropine on the heart rate was investigated in the rabbit. Intraventricular administration of atropine in a dose of 10, 30, 100, or 300 ug produced dose dependant bradycardia. Atropine (100 ug) induced bradycardia was abolished by bilateral vagotomy or intravenous atropine, and inhibited by intravenous propranolol but not by intravenous Regitine. Intraventricular Ecolid or regitine pretreatment diminished the bradycardia induced by intraventricular atropine. From the above results, it is suggested that a central adrenergic mechanism as well as vagal activity plays an important role in the intraventricular atropine-induced bradycardia.
Atropine* ; Bradycardia ; Chlorisondamine ; Heart Rate* ; Heart* ; Phentolamine ; Propranolol ; Vagotomy

PURPOSE: To compare the efficacy of Bimix solution (27.3 mg/ml papaverine and 0.9 mg/ml phentolamine) versus Trimix solution (18.8 mg/ml papaverine, 0.6 mg/ml phentolamine and 6.3ug/ml prostaglandin El) in terms of erectile response and complications. MATERIALS AND METHODS: We comparatively analyzed the erectile response and the incidence of pain, prolonged erection (>4 hours), and corporal fibrosis of either medication in the 155 impotent patients who used Bimix solution for intracavernous pharmacotherapy (mean duration: 15 months) and thereafter used Trimix solution (mean 12 months). RESULTS: Erectile response to Trimix solution was significantly better than Bimix solution (p<0.01). The mean dose of Bimix solution was higher than Trimix solution (0.43 ml. vs. 0.34 ml, p<0.05). The severe pain enough for impediment to ntercourse occurred in 6.5% of the Trimix group, while no patient of the Bimix group experienced (p<0.01). The corporal fibrosis was noted in 8.4% of the Trimix group and 16.1% of the Bimix group. However, there was no significant difference between the two groups (p=0.08). The incidence of prolonged erection was significantly lower (p<0.05) in the Trimix group (2.6%) than in the Bimix group (12.3%). A total of 139 patients (89.7%) finally selected Trimix solution. CONCLUSIONS: The Trimix solution was more effective and safer than Bimix solution for the treatment of erectile dysfunction.
Drug Therapy ; Erectile Dysfunction* ; Fibrosis ; Humans ; Incidence ; Male ; Papaverine ; Phentolamine

PURPOSE: This study was aimed to compare the erectile response when phentolamine of intracavernous trimix(papaverine, phentolamine, alprostadil) was replaced with chlorpromazine. MATERIALS AND METHODS: A total of 65 patients with erectile dysfunction(63.3+/-9.19 years of age) who had already used intracavernous injection with trimix(4.5+/-2.12 years) were recruited for this study. The erection quality and adverse reactions of chlorpromazine solution were compared with those of trimix. RESULTS: Among 65 patients, the erection quality of the intracavernous chlorpromazine solution compared to that of trimix was worse in 26 patients(40%), better in 8(12.3%) and similar in 31(47.7%) when injected at the clinic. Among 45 patients who used the chlorpromazine solution for intracavernous self-injection at home for more than 3 months, however, the erection quality was worse in 13(28.9%), better in 8(17.8%) and similar in 24(53.3%). Intracavernous chlorpromazine solution-either injected at the clinic or self-injected-showed no significant adverse reaction. CONCLUSIONS: Chlorpromazine could be a safe and effective substitude of phentolamine of trimix.
Alprostadil* ; Chlorpromazine* ; Erectile Dysfunction ; Humans ; Male ; Papaverine* ; Phentolamine

1. It was attempted to clarify the mechanism of the pressor response to raised intracranial pressure in urethane-anesthetized rabbits. 2. Intraventricular clonidine markedly inhibited the pressor response to raised intracranial pressure. 3. Intraventricular regitine antagonized the above mentioned inhibitory effect of clonidine on the pressor response. 4. In reserpine-treated rabbits the pressor response to raised intracranial pressure was not observed, whereas after the intraventricular administration of norepinephrine the pressor response was observed. 5. Intraventricular clonidine inhibited the pressor response that could be observed in the reserpine-treated rabbits after the intraventricular norepinephrine. 6. It is inferred that raised intracranial pressure stimulated some part of the brain to cause the increase of norepinephrine release, resulting in the increase of the sympathetic outflow and the elevation of blood pressure.
Blood Pressure ; Brain ; Clonidine* ; Intracranial Pressure* ; Norepinephrine ; Phentolamine* ; Rabbits*

A total or 76 patients of erectile dysfunction were treated with intracorporeal self-injection of Papaverine hydrochloride(30mg/ml) and Phentolamine mesylate(1mg/ml) from Feb. 1986 to Aug. 1988. The results were obtained as follows: 1. The average patient age was 48.1 years, with a range of 26 to 72 years. The etiology of impotence were psychogenic in dosages patients (47.4 %), vasculogenic in 32 (42.1 %) and neurogenic in 4 (5.3%). 2. The average effective dosages were 0.44ml in psychogenic impotence, 0.69ml in vasculogenic and 0.16ml in neurogenic. 3. The erection time was 60 minutes in 14 (70.0%) out of 20 psychogenic impotence, 30-60minutes in 8 (50.0% ) out of 16 vasculogenic and 90-120 minutes in all neurogenic. 4. The durations of treatment were 1-3months in 12 patients (33.3% ) and 12-24months in 7(19. 5%). The average duration of treatment was 6.9months. 5. Complications included priapism in 7 patients, subcutaneous hematoma in 2, induration of injection site in 1 and fibrous plaque on cavernosal body in 1. 6. Of the 76 patients, 40 patients discontinued injection due to improved potency in 14 patients, penile prosthesis in 4, refusal of treatment in 3 and failure to follow-up in 19. Therefore, intracorporeal self-injection of Papaverine hydrochloride and Phentolamine mesylate seems to be safe and effective primary choice of treatment for selective impotence.
Erectile Dysfunction* ; Follow-Up Studies ; Hematoma ; Humans ; Male ; Papaverine* ; Penile Prosthesis ; Phentolamine* ; Priapism ; Treatment Refusal

PURPOSE: To evaluate the efficacy and safety of an intracavernous injection of lyophilized papaverine/phentolamine/alprostadil (Standro(R)) for the treatment of erectile dysfunction (ED) in Koreans. MATERIALS AND METHODS: 249 men (>20 years old), with ED (>6 month duration), were enrolled from 14 clinical centers. The intracavernous 'TMs' were titrated in a stepwise fashion at the clinic, from 0.05-0.25ml (17.64mg papaverine, 0.6mg phentolamine, and 6mug alprostadil per ml), with increment of 0.02-0.05ml, according to the etiology and severity of the ED and the patients' ages. RESULTS: Of the 249 men, 238 completed the dose titration, and progressed to home treatment of 3 months duration. Of these 238, 193 (psychogenic 13.0%, organic 75.5%, mixed 11.5%) completed the home treatment (4 or more self-injections), with the other 45 dropping out (lost to follow-up in 24, patient refusal in 9, no chance to have intercourse in 7 and omitted recording of patient diary in 2). The success rate per trial (a total number of sufficient erection for vaginal intromission/a total number of injections) and per patient (number of patients who had one or more sufficient erections for vaginal intromission/the enrolled patients at beginning or 193 patients), and the satisfaction rate per patient (number of patients who had both patient and partner satisfaction with erection/193 patients) were 74.1, or 91.2 and 75.1%, respectively. The adverse reactions were prolonged erections in 3, urethral pain in 1 and penile skin edema in 2. Three patients complained of penile pain during an erection, but there was no dropout due to the pain. No significant changes in laboratory tests were found after the home treatment. CONCLUSIONS: A 'TM' seems to be effective and safe for an intracavernous injection for the treatment of men with erectile dysfunction.
Alprostadil ; Disulfiram ; Edema ; Erectile Dysfunction* ; Follow-Up Studies ; Humans ; Male ; Papaverine ; Patient Dropouts ; Phentolamine ; Skin

Recent reports suggest that the responses of the detrusor muscle to the hypogastric nerve stimulation and some autonomic drugs may not be identical among various species. In this study, the responses of the isolated detrusor muscle strips of the Amyda Japonica and the rabbit to catecholamines were compared, and the type of the adrenergic-receptors was investigated. The results obtained were as follows : 1. Catecholamines (norepinephrine and epinephrine) evoked only contraction in the isolated detrusor muscle of the Amyda Japonica and relaxation in the preparation of the rabbit. 2. The contraction-response in the Amyda Japonica was blocked in the presence of regitine, an adrenergic alpha-receptor blocking agent. 3. The relaxation-response in the rabbit was abolished by pre-treatment with propranolol, an adrenergic beta-receptor blocking agent. 4. Acetylcholine elicited contraction in both of the isolated detrusor muscle strips of the Amyda japonica and the rabbit, and the response was completely blocked in the presence of atropine. 5. The results described above suggest that catecholamines exert excitatory effect on the detrusor muscle of the Amyda japonica as it contains adrenergic alpha-receptors and inhibitory effect on the same preparation of the rabbit as it contains the adrenergic beta-receptors. Key Word : amyda japonica,alpha receptor, beta receptor.
Acetylcholine ; Atropine ; Autonomic Agents* ; Catecholamines ; Phentolamine ; Propranolol ; Receptors, Adrenergic, alpha ; Receptors, Adrenergic, beta ; Relaxation

PURPOSE: Glucocorticoid contribute to the pathogenesis of hypertension through intracellular signals that stimulate vascular smooth muscle contraction. However, some in vitro and in vivo studies have shown that glucocorticoid has the potential role of vasorelaxation. Therefore, we tried to investigate the effect of short acting glucocorticoid (hydrocortisone; HCS) on the isolated rabbit cavernosal smooth muscle for evaluation of the possibility of using this material as a pharmacoerecting agent. MATERIALS AND METHODS: Strips of rabbit corpus cavernosum were mounted in organ chambers. On the precontracted muscle strips with phenylephrine(PHE; 5x10-6M), HCS was treated with increasing concentration from 10microgram/mL. The relaxing activity of ACh(10-7M), phentolamine(10-8M), papaverine(10-8M), verapamil(10-6M), PGE1(10-2M), SNAP(5x10-5M) were observed with the preparation of HCS. Depolarization by KCl were observed with HCS to investigate the relationship of HCS effects to K+. RESULTS: Pretreatment of muscle strips with low dose of HCS caused concentration-related increase of a PHE induced contraction. On muscle strips submaximally precontracted with PHE, HCS(10microgram/mL to 100microgram/mL) showed no relaxations. Pretreatment of muscle strips with 10microgram/mL dose of HCS caused a potentiation of a relaxation effects of ACh, papaverine, verapamil, SNAP, PGE1 and 50microgram/mL dose of HCS caused a potentiation of a relaxation effects of ACh, phentolamine. However, 100microgram/mL dose of HCS did not produce changes of these potentiating responses to relaxation. Also, HCS did not influenced the depolarization with any concentrations of KCl. CONCLUSIONS: HCS has the potentiating effect of both the PHE-induced contraction, and the relaxation of the ACh, phentolamine, papaverine, verapamil, SNAP, PGE1 at 10-50microgram/mL concentration on the cavernosal smooth muscle.
Alprostadil ; Hypertension ; Muscle, Smooth* ; Muscle, Smooth, Vascular ; Papaverine ; Phentolamine ; Relaxation ; Vasodilation ; Verapamil