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PubMed2005

Determination of the molecular complexation constant between alprostadil and alpha-cyclodextrin by conductometry: implications for a freeze-dried formulation.

The binding constant between alprostadil (PGE1) and alpha-cyclodextrin (alpha-CD) was determined at four temperatures using conductance measurements. Alpha-cyclodextrin is an excipient material in Caverject dual chamber syringe (DCS) that was added to enhance stability. The binding constant was used to calculate the amount of PGE1 free upon reconstitution and injection, since only the free drug is clinically active. The conductivity measurement is based on a decrease in specific conductance as alprostadil is titrated with alpha-CD. The change in conductivity was plotted versus free ligand concentration (alpha-CD) to generate a binding curve. As the value of the binding constant proved to be dependent on substrate concentration, it is really a pseudo binding constant. A value of 742+/-60 M(-1) was obtained for a 0.5 mM solution of alprostadil at 27 degrees C and a value of 550+/-52 M(-1) at 37 degrees C. These results compare favorably to values previously obtained by NMR and capillary electrophoresis. Calculation of the fraction PGE1 free upon reconstitution and injection show it to approach the desired outcome of one. Hence, the amount of drug delivered by Caverject DCS is nominally equivalent to that delivered by Caverject S. Po., a predecessor product that contains no alpha-cyclodextrin.

Algorithms↗
PubMed2006

Metabolism of eicosanoids and their action on renal function during ischaemia and reperfusion: the effect of alprostadil.

Eicosanoids, active metabolites of arachidonic acid (AA), play an important role in the regulation of renal haemodynamics and glomerular filtration. Our study verified the hypothesis on the positive action of exogenously administered PGE(1) on renal function during an operation with temporary ischaemia of the lower half of the body. Also the effect of alprostadil (prostaglandin E(1) analogue) administered during the operation of an abdominal aorta aneurysm on the postoperative systemic metabolism of AA and the glomerular filtration rate (GFR) was investigated. The study included 42 patients with a diagnosed abdominal aorta aneurysm who have been qualified for the operation of implantation of the aortic prosthesis. The patients were randomly assigned to two groups: the study group (I) receiving alprostadil and the control group (II) without alprostadil. The levels of hydroxyeicosatetraenoic acids (15-HETE, 12-HETE, 5-HETE) were determined by RP-HPLC and the level of thromboxane B(2) (TxB(2)) was determined by ELISA in the plasma of the blood drawn from vena cava superior immediately before aortic clamping (A) and 5 min after aortic declamping (B). The administration of PGE(1) affects the metabolism of 15-HETE in a manner dependent on the baseline value of GFR but does not significantly change the postoperative renal function. The metabolism of 15-HETE is affected by the baseline value of GFR1 and a longer period of ischaemia is correlated with lower concentrations of 5-HETE during reperfusion. The results of our studies indicate that TxB(2) influences the postoperative function of kidneys.

12-Hydroxy-5,8,10,14-eicosatetraenoic Acid↗
PubMed1984

Quantitative determination of alprostadil (PGE) in bulk drug and pharmaceutical formulations by high-performance liquid chromatography.

An adsorption high-performance liquid chromatographic method suitable for the quantitative determination of the purity of alprostadil (prostaglandin E1) bulk drug and of the concentration of alprostadil in Prostin V.R. Pediatric Sterile Solution is described. A variety of isomers and related compounds including 8-iso-PGE1, 11-epi-PGE1, 15-epi-PGE1, PGE2, 5,6-trans-PGE2, and 8-iso-PGE2 are separated from alprostadil and are quantifiable. The 2-naphthacyl ester derivatives are employed and derivatization conditions providing maximum response are described.

Alprostadil↗
PubMedDate not supplied

The use of alprostadil sterile powder in a home self-injection study of Asian men with erectile dysfunction.

This study evaluated the individual optimal dose of alprostadil in the office setting that could be used as the basis for effective home self-injection therapy. The study included 150 Asian men with erectile dysfunction (ED). The mean age of study participants was 48.3 years (range, 21 to 74 years), and the mean duration of ED was 3.6 years. The most common cause of ED was venogenic (24%), psychogenic (21%), arteriogenic (13%), neurogenic (0.7%), or a combination of these (41%). An optimal response was seen in 72% of patients (n = 108) in the office and 96% of patients (n = 100) at home. The mean +/- SD office dose of alprostadil was 19.4 +/- 12.8 micrograms versus 18.0 +/- 12.2 micrograms at home. More than half of the patients (57% in an office setting and 53% at home) achieved an optimal response at a dose between 5 and 15 micrograms. By the 20-micrograms dose, 82% of patients had achieved an optimal dose at home compared with 70% of patients in the office. An optimal response was seen at the same dose in the office and home in 75% of patients; the dose at home decreased from the office dose for 16% of the patients and increased for 9%. There were 24 patients who experienced adverse events: penile pain after injection (18 patients), cold sweating (2 patients), pediculosis (1 patient), broken leg (1 patient), ankle pain (1 patient), and prolonged erection (1 patient). One patient discontinued the study because of penile pain. Alprostadil sterile powder offered safe and effective treatment of ED for home self-injection therapy. Once an optimal dose response had been established in the physician's office, further home adjustments were needed in 25% of patients. Penile pain, usually mild, was the most common, possibly related adverse effect reported.

Adult↗
PubMed2002

A synthetic prostaglandin E1 analog, alprostadil alfadex, relaxes sphincter of Oddi in humans.

It is well established that prostaglandins (PGs) exert potent pharmacological actions on vascular and nonvascular smooth muscle, although their effects on the sphincter of Oddi (SO) remain to be elucidated. The aim of this study was to investigate the effect of PGE1 on motility of the human SO. Twenty patients appearing for routine endoscopic retrograde cholangiopancreatography (ERCP) examination were studied. Each patient was randomly allocated to receive an intravenous infusion of normal saline (six patients), or alprostadil alfadex, a synthetic PGE1 analog, at a dose of either 0.05 or 0.1 microg/kg/min (seven patients for each condition). Endoscopic biliary manometry was done with a recording of basal SO pressure, amplitude of SO phasic contractions, and phasic contractile frequency before and 5 min after intravenous infusions, using a 4-French microtransducer catheter. There was no significant change in SO motor variables following application of normal saline. Alprostadil alfadex significantly decreased basal SO pressure at a dose of 0.05 microg/kg/min, and significantly decreased all parameters at a dose of 0.1 microg/kg/min. A synthetic PGE1 analog, alprostadil alfadex, effectively inhibits motility of the human SO. This drug may be of clinical application as a SO-relaxing agent.

Adult↗
PubMed1997

A dose-response study of alprostadil sterile powder (S.Po.) (Caverject) for the treatment of erectile dysfunction in Korean and Indonesian men.

This open-label, dose-escalation study investigated the efficacy and safety of alprostadil (PGE1, prostaglandin E1) Sterile Powder (S.Po.) (Caverject) for treatment of erectile dysfunction (ED) in 84 men with ED of various etiologies lasting > or = 4 months. Doses started with 2.5 micrograms, then 5 micrograms, 10, 15, 20, 30, up to a 40 micrograms maximum. Eligible patients received single alprostadil injections in the physician's office until an erection occurred. Ten minutes after injection, the patient's erection was clinically evaluated. Optimal response was defined as erection sufficient to permit vaginal penetration and lasting 30-60 min. The patient also reported his own evaluation of response and any side effects. Patients were 24-65 y old (mean: 43.7 y), had ED of psychogenic, vascular, or neurogenic origin lasting 4 months-30 y (mean: 3.75 y). Of 84 patients enrolled, 82 completed the study. In the 82 patients who completed the study 78 (92.9%) achieved an optimal response; 18/78 patients (23.1%) had an optimal response at 2.5 micrograms, 9/78 (11.5%) at 5 micrograms, 21/78 (26.9%) at 10 micrograms, 12/ 78 (15.4%) at 15 micrograms, and 11/78 (14.1%) at 20 micrograms. Only 5/78 (6.4%) at 30 micrograms and 2/78 (2.6%) at 40 micrograms achieved an optimal response. Mean optimal alprostadil dose was 11.9 micrograms, and the mean minimal effective dose was 9.9 micrograms. Mean onset of erection was 11.2 min; mean duration of erection was 50.5 min. Penile pain in five patients (6%) was the only reported side effect.

Adult↗
PubMed1998

Intracavernous Alprostadil Alfadex--an effective and well tolerated treatment for erectile dysfunction. Results of a long-term European study.

Long-term efficacy and safety of Alprostadil-Alfadex (EDEX/VIRIDAL) in intracavernous self-injection therapy for chronical erectile failure was investigated in a four year running multicenter European trial. Of the 16,886 protocolled injections 93% (15,713) resulted in rigid erections followed by successful sexual intercourse. Reported side effects by patients were prolonged erections > 6 h only occurring during the first year in 1.2% (2 out of 162), painful erections in 29% (47 out of 162) during the first year and decreasing to 12.1% by year 4, hematomas, neither requiring therapeutic measures nor impeding sexual performance in 33.3% (54 out of 162) in year 1 with a decrease to 12.1% by year 4, fibrotic penile alterations such as nodules, plaques or deviations in 11.7% (19 out of 162) with spontaneous healing in 48% (9 out of 19). Of the 162 patients involved in this trial 54 completed the 4 y. Of the 54 completers 91.4% considered the tolerability good or very good and were satisfied or very satisfied with self-injection therapy with Alprostadil-Alfadex. The respective rates of the female partners were 51.7% very satisfied and 39.7% satisfied. These data of the world-wide longest running prospective trial with a vasoactive drug in self-injection therapy provided impressive proof that Alprostadil-Alfadex represents a very effective and safe treatment for erectile dysfunction of both psychogenic and organogenic origin.

Adult↗
PubMed2002

Comparison of a needle-free high-pressure injection system with needle-tipped injection of intracavernosal alprostadil for erectile dysfunction.

Patients identified from hospital records as using alprostadil injections for erectile dysfunction were invited to take part in this open crossover study. On alternate weeks eight patients were given intracavernosal needle injections and transdermal needle-free injection of alprostadil in a randomized order. Efficacy of injection and associated pain were assessed and compared for the two methods. Pain produced during injection was significantly greater with the needle-free system than with the needle-tipped injection whilst efficacy was significantly less. Bruising was reported in all except one patient following needle-free injection only. Patient ratings of the needle-free injector were significantly lower than ratings for needle-tipped alprostadil delivery and when asked to express a preference, every patient chose the needle-tipped injection over the needle-free device.

Adult↗
PubMed2003

The efficacy and safety of a topical alprostadil cream, Alprox-TD, for the treatment of erectile dysfunction: two phase 2 studies in mild-to-moderate and severe ED.

In two multicenter, placebo controlled, phase 2 studies, patients with mild-to-moderate (n=161, Study 1) or severe (n=142, Study 2) erectile dysfunction (ED) were randomized to receive placebo, 0.05, 0.1, or 0.2 mg (Study 1) or placebo, 0.1, 0.2, or 0.3 mg (Study 2) of topically applied alprostadil (containing a proprietary skin permeation enhancer). The primary efficacy end point in both studies was the change in erectile function (EF) score from baseline to final visit. The changes from baseline for EF scores were -0.8+/-1.1, 1.8+/-1.1, 0.7+/-1.2, and 3.7+/-1.2 (P<0.01; Study 1) and 2.7+/-1.3, 6.29+/-1.4, 6.49+/-1.5, and 9.44+/-1.5 (P<0.001; Study 2) for ascending dose groups in each study. Topical alprostadil was well tolerated with the most common adverse event being urogenital pain. These results suggest this topical alprostadil formulation may be a potentially useful agent for the treatment of ED.

Administration, Topical↗
PubMedDate not supplied

Topical alprostadil in the treatment of Female Sexual Arousal Disorder: a pilot study.

This study evaluated the efficacy and safety of three doses of topical alprostadil USP (prostaglandin E1) cream in 8 patients with Female Sexual Arousal Disorder (FSAD). Each patient was administered a single intravaginal dose of placebo followed by escalating intravaginal doses of the active drug at 2-week intervals. Alprostadil's effectiveness in enhancing subjective and physiological arousal during visual sexual stimulation was supported by patient ratings and physician assessments of vaginal erythema and transudate volume. Photoplethysmography measurement of vaginal pulse amplitude was not able to demonstrate treatment sensitivity in the present study. Adverse events included mild cases of vaginal itching and burning. The data support further investigation of the use of alprostadil for FSAD.

Administration, Topical↗
PubMed2000

Thalassaemic men affected by erectile dysfunction treated with transurethral alprostadil: case report.

The aim of this controlled clinical study, performed in a specialized institutional unit for thalassaemic men, was to consider the possibility of restoring erection in beta-thalassaemic patients with erectile dysfunction by administering E(1) prostaglandins (alprostadil) transurethrally. Four patients affected by beta-thalassaemia, aged between 32 and 52 years, and having an erectile dysfunction were included in the study. Each patient was given 500 microg alprostadil in the distal urethra. Response was evaluated by the erection assessment scale. The main outcome measures were: (i) the clinical study; (ii) FSH, LH, total and free testosterone plasma concentrations; and (iii) basal and dynamic Doppler sonography of cavernous arteries. The treatment produced a response of 3-4 on the erection assessment scale. Average minimum response time was 20 min, while average maximum response time was about 60 min. There was no evidence of significant side effects. Our hypothesis is that the delayed reaction was due to organ damage induced by iron load, causing a reduction or absence of elasticity in the interstitial tissue of the corpora cavernosa. Thus, we believe that treatment with alprostadil can be considered an effective, non-invasive therapy for thalassaemic patients with erectile dysfunction.

Adult↗
PubMed2000

Clinical experience with intraurethral alprostadil (MUSE) in the treatment of men with erectile dysfunction. A retrospective study. Medicated urethral system for erection.

OBJECTIVE: The Food and Drug Administration (USA) approved the transurethral administration of prostaglandin (alprostadil in January 1997), which had an efficacy of approximately 50% in clinical trials. We studied its effectiveness in clinical practice. METHODS: Patient and partner education was followed by an initial office trial of a medicated urethral system for erection (MUSE) after other medical risk factors were corrected during a 2- to 4-month period. The initial titration dose of alprostadil was usually 125 or 250 microg. Further titration, if needed, was instituted by the patient at home. Success was determined as the satisfactory completion of sexual intercourse in more than 66% of attempts, with a minimum of two being required. RESULTS: Two hundred and seventy patients entered the trials, and follow-up information was available in 229 (85%). The overall success rate was 56%. The dose required was 500 microg in 49.2% and 1,000 microg in 42.2%. Of the 44% in whom treatment failed, 61.4% did so because of lack of efficacy and 38.6% because of side effects (genital pain or urethral bleeding). Minor urogenital symptoms, which did not interfere with treatment, occurred in an additional 40% of patients. CONCLUSIONS: The efficacy of transurethral administration of alprostadil (56%) is higher than the initial published clinical trial data and higher than recent reported clinical experiences, although higher doses were required in our study. Men over 50 years of age, having an organic cause for erectile dysfunction, had better responses. Patient and partner education is important for successful treatment, and the in-office initial titration is an integral part of this success. Prior correction of medical risk factors may enhance the success rate.

Adult↗
PubMed1995

[The therapeutic and diagnostic potentials of the intra-corpora cavernosa use of alprostadil, Edex, in patients with erectile dysfunction].

The paper presents the results of diagnostic and therapeutic use of intracavernous injections of alprostadil edex (prostaglandin E1) of Schwartz Pharma AG production (Germany) in 14 patients with functional, compensated and subcompensated organic erectile dysfunction. Pharmacological test with alprostadil modelling cavernous body function extends diagnostic efficacy of doppler scanning of the penis and cavernosography. A complete effect (100% sexual rehabilitation) was achieved in 1 and partial in 3 males. Alprostadil edex kits are advocated as safe and convenient.

Adult↗
PubMed1992

Influence of alprostadil on pulmonary dysfunction after a cardiac operation.

To test the effects of alprostadil on pulmonary dysfunction after cardiac operations, we studied 24 male patients undergoing aortocoronary bypass. Twelve were given an intravenous infusion of alprostadil (synthetic prostaglandin E1), 20 ng.kg-1.min-1, in a double-blind manner during operation; the other 12 were controls. Duration of artificial respirator use and frequent blood gas analyses were used to assess postoperative pulmonary function. Use of the artificial respirator postoperatively was significantly lower in the prostaglandin group (mean time. 5.25 +/- 1.81 hours) compared with the controls (mean time, 8.34 +/- 4.35 hours) (p = 0.047). The proportion of patients with hypercapnia and with hypoxia determined every 4 hours for the first 24 hours after extubation was significantly lower in the prostaglandin group compared with the controls (p less than 0.0001). These results indicate that synthetic prostaglandin E1 may play a role in protecting lung tissue during extracorporeal circulation.

Adult↗
PubMed1999

Intraurethral alprostadil for treatment of erectile dysfunction in patients with spinal cord injury.

OBJECTIVES: To assess the efficacy of intraurethral prostaglandin E1 (alprostadil, MUSE) in treating erectile dysfunction in patients with spinal cord injury (SCI). METHODS: Intraurethral alprostadil was tested in 15 patients with SCI to evaluate its effectiveness in treating SCI-associated erectile dysfunction. All patients were at least 1 year after injury, and all had previously used intracavernosal injections successfully (Schramek's grade 5 erection). The intraurethral drug was administered in the office, in the presence of a physician, with monitoring of blood pressure. If effective, the patient was then able to use MUSE at home. The first 3 patients underwent gradual dose escalation starting with 125 microg, without the use of a constriction ring. Because of hypotension, the remaining 12 patients all used a penile constriction ring prior to intraurethral drug administration using 1000 microg. The quality of the erection was compared with that achieved with intracavernosal injections using Schramek's grading. RESULTS: The dose escalation (titration) in the first 3 patients demonstrated that the 1000-microg dose was the most effective in creating an erectile response. Transient hypotension was noted in these first 3 patients in whom the constricting band was not used. The highest dose of MUSE (1000 microg) was, therefore, used in the remaining 12 patients, with the constriction band. The quality of the erection varied and appeared to be less rigid in all patients (12 patients with grade 1 to 3; 3 patients with grade 4) than that noted with intracavernosal injection therapy (1 5 patients with grade 5). There was no incidence of priapism. The 3 patients with grade 4 erections tried the MUSE at home. All 3 patients were dissatisfied with the quality of the erection and did not continue to use the MUSE at home and returned to intracavernosal injection therapy. CONCLUSIONS: MUSE appears to be somewhat effective in creating erections; however, these were less rigid erections than those obtained with intracavernosal therapy and provided less overall satisfaction. It should always be used in the patient with SCI after placement of a constriction ring to prevent hypotension. Its ultimate use depends on the patient's level of satisfaction with the quality of the erection compared with intracavernosal injections.

Adult↗
PubMed1998

Quality of life effects of alprostadil therapy for erectile dysfunction: results of a trial in Europe and South Africa.

OBJECTIVES: Quality of life (QOL) data were used to evaluate the effects of self-administered intracavernosal injection of alprostadil for erectile dysfunction, when used for up to 18 months during a 13 country Phase III clinical trial. METHODS: The Duke Health Profile was used to measure patients' physical and psychosocial QOL at baseline, 3, 6, 12 and 18 months. Changes from baseline were measured using paired t-tests, with additional analyses by cause of dysfunction, starting dosage, and prior treatment. RESULTS: Patients displayed significant improvements in mental and social health and self-esteem at six months (P < 0.01, n = 570), with greater improvements at 12 and 18 months. Anxiety and depression measures also improved significantly at 12 and 18 months, as did the summary general health score. Worse pain scores were observed in the first year but not at 18 months. Those with a starting dosage of 10-20 micrograms, those with psychogenic causes of dysfunction, and those with no prior treatment for erectile dysfunction generally showed the greatest improvements. CONCLUSION: In this study, the clinical improvements in erectile function due to intracavernosal alprostadil therapy were complemented by QOL improvements, particularly in the mental health, of many patients.

Adult↗
PubMed2002

Deep venous thrombosis and venous thrombophlebitis associated with alprostadil treatment for erectile dysfunction.

We report a patient who developed deep vein thrombosis of the calf and thrombophlebitis after treatment with intracorporeal alprostadil (Viridal). The reaction recurred on rechallenge with Viridal. This adverse effect has not been reported in the literature but six patients have been reported to the Medicines Control Agency in Great Britain. The history of deep venous thrombosis or thrombophlebitis may not be a formal contraindication to treatment with alprostadil, but the patient should be made aware of this possible complication before embarking on this form of treatment.

Alprostadil↗
PubMedDate not supplied

Clitoral hemodynamic changes after a topical application of alprostadil.

We performed duplex ultrasonography of the clitoris to assess the local hemodynamic changes after a topical application of alprostadil. Color duplex ultrasonography was used to evaluate 18 women before and after the application of 1 g of 0.2% alprostadil gel. The peak systolic velocity and end diastolic velocity showed a statistically significant difference after the application. All women showed labial and clitoral engorgement, 72% reported a pleasant sensation of warmth, and no systemic side effects were found. These findings are similar to the values reported after sexual stimulation, indicating that topical vasoactive drugs might help in the differential diagnosis of the vascular component of female sexual dysfunction.

Administration, Topical↗