OBJECTIVESTo supply clinical data for drug selextion in the treatment of erectile dysfunction through intracavernosal injection.

METHODSFifty-six ED patients were randomly classified into 2 groups and received phentolamine along with papaverine (for group 1) or phentolamine, papaverine and ligustrazin hydrochloride(for group 2).

RESULTSPatients in group 2 enjoyed a longer time of erection. More patients in group 2 succeeded in having enough erection time and hardness to complete sexual intercourse (P < 0.05).

CONCLUSIONSThe extrainjection of ligustrazin hydrochloride injection can help prolong erection duration and hardness and reduce tubercles that might occur in the corpus carvernosal. Therefore it is a safe and inexpensive drug in the intracarvernous injection treatment.

Adult ; Erectile Dysfunction ; drug therapy ; Humans ; Injections ; Male ; Middle Aged ; Papaverine ; administration & dosage ; Phentolamine ; administration & dosage ; Pyrazines ; administration & dosage

Administration, Topical ; Female ; Humans ; Intracranial Aneurysm ; complications ; Middle Aged ; Papaverine ; administration & dosage ; Vasospasm, Intracranial ; complications ; drug therapy

PURPOSE: To investigate the chemical stability of papaverine/phentolamine/alprostadil (Standro(R)) used for intracaver nous injection in patients with erectile dysfunction. MATERIALS AND METHODS: Samples of lyophilized Standro(R) were stored at room temperature (25+/-2 degrees C) or in the refrigerator (4+/-2 degrees C). The pH and concentration of papaverine HCl, phentolamine mesylate, and alprostadil were measured at intervals by high-performance liquid chromatography. RESULTS: At 24 months, the concentrations of papaverine, phentolamine, and alprostadil stored in the refrigerator and at room temperature were 99.7%, 98.9%, and 98.7% and 98.4%, 96.3%, and 93.3% of the original concentrations, respectively. When the product was stored in solution in the refrigerator for 19 weeks, the concentrations of the three drugs were 98.7%, 97.2%, and 88.0%, respectively. In 5 days at room temperature, the concentration of alprostadil dropped to 86.4%, which is below the minimum concentration for the product specified by the Korean Food and Drug Administration, although the concentrations of papaverine and phentolamine remained stable (99.6%, 98.4%). The pH of the three agents did not change significantly regardless of the storage conditions (temperature, duration, lyophilized or dissolved). CONCLUSIONS: Lyophilized papaverine/phentolamine/alprostadil (Standro(R)) is chemically stable for at least 2 years at room temperature, although solutions need to be kept in the refrigerator and become less effective with prolongation of storage.
Alprostadil ; Chromatography, Liquid ; Erectile Dysfunction ; Humans ; Hydrogen-Ion Concentration ; Male ; Papaverine ; Phentolamine ; United States Food and Drug Administration

OBJECTIVETo evaluate the application of intracavernous pressure (ICP) monitoring in the electrophysiologic and pharmacologic induction of penile erection.

METHODSThe penile dorsal nerves (DN) of 8 anesthetized adult male rats were isolated and the corpora cavernosa exposed. A heparinized 25-gauge angiocath (intravenous catheter) was inserted into the right corpus cavernosum to monitor the ICP and a 30-gauge needle was inserted into the left corpus cavernosum for intracavernosal drug administration. Penile erection was induced by electrical stimulation of the dorsal nerve (16 Hz frequency, 0.5 ms pulse width, 20 s duration, 4 volts) and intracavernous papaverine hydrochloride injection (0.4 mg). ICP was recorded with the SMUP-PC biological signal process system.

RESULTSIn the anesthetized rats, the baseline level of ICP was (12.3 +/- 3.1) mm Hg and the electrical stimulation of the DN significantly increased ICP[(36.4 +/- 2.3) mm Hg, P < 0.05], which slowly returned to baseline pressure after termination of the electrical stimulation. The intravavernosal administration of papaverine also induced a significant increase in ICP [(28.4 +/- 6.1) mm Hg, P < 0.05].

CONCLUSIONICP monitoring in rats provides a useful scientific tool for in vivo studies of penile erection in experimental rat models. It is of great significance for further studying the physiology of penile erection and the pathogenesis of erectile dysfunction as well as for evaluating the efficacy of novel therapies for erectile dysfunction.

Animals ; Electric Stimulation ; Injections ; Male ; Papaverine ; administration & dosage ; pharmacology ; Penile Erection ; drug effects ; physiology ; Penis ; innervation ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo evaluate the effect of external use of papaverine cream on enhancement of tissue expansion.

METHODS8 mini pigs were randomly divided into 4 groups. During inflation, papaverine was given externally in group A, through a delivery system in group B, though intramuscular injection in group C. Papaverine was not given in group D. The time of inflation, the expansion rate, the surviving length of expanded flaps and the papaverine concentration in the fibrous capsule in each group were examined. Histologic and electroscope examinations of the expanded tissue were made.

RESULTSThe average inflation time was 28.9 +/- 4.5 days in group A, 34.0 +/- 2.6 days in group B, 37.6 +/- 4.8 days in group C and 38.5 +/- 3.5 days in group D. There was significant difference between each group(P < 0.05). The average surviving length of expanded flaps in group A was 13.67 +/- 1.28 cm, 11.07 +/- 0.88 cm in group B, 10.79 +/- 0.49 cm in group C, and 9.49 +/- 0.77 cm in group D. There was significant difference between each group (P < 0.01). Histologic examinations of the expanded tissue suggested that there were no significant differences in thickness of epidermis, derma and fibrous capsule among the four groups. Electroscope examinations of the myofibroblast in fibrous capsule showed that there were smaller nuclei, fewer microfilaments and fewer mitochondrias and rougher endoplastic reticulume in group A than those in other groups. The concentration of papaverine in fibrous capsule of group A was 3.5 +/- 1.2 micrograms/g. Papaverine was detected neither in the skin of other groups nor in the blood of all groups.

CONCLUSIONS1. Papaverine cream can permeate through skin and maintain high concentration and continuous effect in local tissue. 2. External use of papaverine cream can inhabit the function of myofibroblast in fibrous capsule, increase inflation rate, accelerate expansion process, and improve microcirculation of the expanded skin with a result of prolongation of surviving length of expanded flaps. 3. The technique of enhancing tissue expansion with external use of papaverine has the advantages of convenient delivery, cheapness, no more injury and infection, and no side effects etc. It is a safe, effective, simple, and reliable method for accelerating tissue expansion.

Animals ; Papaverine ; administration & dosage ; pharmacokinetics ; Skin ; drug effects ; Surgical Flaps ; Swine ; Swine, Miniature ; Time Factors ; Tissue Expansion ; Vasodilator Agents ; administration & dosage

Administration, Oral ; Animals ; Chromatography, High Pressure Liquid ; Feces ; chemistry ; Female ; In Vitro Techniques ; Male ; Microsomes, Liver ; metabolism ; Papaverine ; administration & dosage ; metabolism ; pharmacokinetics ; Rats ; Rats, Wistar ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry ; Vasodilator Agents ; administration & dosage ; metabolism ; pharmacokinetics

The corporeal blood gas changes in accordance with the duration of the prolonged erection which developed after intracorporeal pharmacotherapy with papaverine and phentolamine were investigated in 62 impotence patients. The picture of the corporeal blood taken from 15 psychogenic impotence patients (a control group) at 10 minutes after intracavernous injection when they showed full erections was arterial but there was pCO2 rise and pH drop compared to femoral artery blood taken simultaneously. As the erection lasted longer, significant gas changes of the cavernous blood began to appear (p<0.0001): increase in pCO2 and decrease in pO2 from 4 hours, decrease in pH from 5 hours, decrease in O2 saturation from 6 hours. Erections lasting for more than 16 hours showed significantly worse hypoxia (p<0.05). Therefore, to prevent hypoxia and metabolic acidosis, drug-induced prolonged erection would be better decompressed before it lasts for more than 4 hours.
Adult ; Carbon Dioxide/*blood ; Erectile Dysfunction/*blood/drug therapy ; Femoral Artery ; Humans ; Hydrogen-Ion Concentration ; Male ; Middle Aged ; Oxygen/*blood ; Papaverine/administration & dosage/therapeutic use ; Penile Erection/*drug effects ; Phentolamine/administration & dosage/therapeutic use ; Time Factors

ObjectiveTo investigate the application value of Toshiba 320-row dynamic volumetric CT angiography in the diagnosis of venous erectile dysfunction (VED).

METHODSWe enrolled in this study 33 patients diagnosed with ED by audiovisual sexual stimulation screening in the outpatient department. Penile erection was induced in the patients by injection of 2 mg phentolamine plus 30 mg papaverine into the corpus cavernosum, followed by that of contrast agent of iobitridol through the vein and corpus cavernosum successively. Then 320-row dynamic volumetric CT angiography was performed and the images of the corpus cavernosum in the arterial and venous phases were collected and processed.

RESULTSDifferent degrees of abnormal venous drainage were observed in 29 of the patients, including 7 cases (24.1%) of back deep venous leakage, 6 cases (20.7%) of foot venous leakage, 3 cases (10.3%) of dorsal superficial venous leakage, 1 case (3.5%) of intervertebral venous leakage, 2 cases (6.9%) of cavernous venous leakage, and 10 cases (34.5%) of mixed venous leakage. Ten of the patients underwent surgery, dorsal deep penile vein ligation in 2 cases, dorsal deep vein embedding plus foot vein ligation in 4, and foot vein ligation in the other 4. Eight of the patients were followed up for 3－12 months post-operatively, during which 2 achieved obvious erectile improvement, while the other 6 gained normal penile erection.

CONCLUSIONSToshiba 320-row dynamic volumetric CT angiography is a reliable method for the diagnosis of VED, which displays the precise location of venous leakage for clinical treatment, with the advantages of clearer images, lower doses of contrast agent and radiation, and faster examination than X-ray penile angiography.

Adult ; Arteries ; diagnostic imaging ; Computed Tomography Angiography ; Contrast Media ; Drug Combinations ; Erectile Dysfunction ; diagnostic imaging ; Humans ; Injections ; Iohexol ; analogs & derivatives ; Ligation ; Male ; Middle Aged ; Papaverine ; administration & dosage ; Penile Erection ; Penis ; diagnostic imaging ; physiopathology ; Phentolamine ; administration & dosage ; Veins ; diagnostic imaging ; surgery

The paper is to establish a method for simultaneous determination of 5 kinds of alkaloids in ephedra and poppy which are in Kechuanning tablets. Solid-phase extraction (SPE) was adopted in pretreatment, and a UPLC method with 2 different wavelengths had been developed: 210 nm for the detection of morphine, codeine phosphate, ephedrine hydrochloride and pseudoephedrine hydrochloride, and 251 nm for papaverine hydrochloride. The column used was Acquity UPLC BEH C18 (100 mm x 2.1 mm ID, 1.7 microm) with linear gradient elution using acetonitrile and 0.1% phosphoric acid. The flow rate was 0.4 mL.min-1, and the column temperature was 30 degrees C. The linear response range was 0.375 0 - 12.50 microg.mL-1 for morphine, 0.064 32 - 2.144 microg.mL-1 for codeine phosphate, 0.030 06 - 1.002 microg.mL-1 for papaverine hydrochloride, 1.126 - 37.52 microg.mL-1 for ephedrine hydrochloride, 0.287 8 - 9.592 microg.mL-1 for pseudoephedrine hydrochloride (r = 0.999 7). The average recoveries of these compounds were 99.26%, 100.6%, 95.29%, 100.1% and 97.48%, respectively. This is a more reasonable and credible method of quality control for Kechuanning tablets.
Alkaloids ; analysis ; Chromatography, High Pressure Liquid ; Codeine ; analysis ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; isolation & purification ; Ephedra ; chemistry ; Ephedrine ; analysis ; Morphine ; analysis ; Papaver ; chemistry ; Papaverine ; analysis ; Plants, Medicinal ; chemistry ; Pseudoephedrine ; analysis ; Quality Control ; Solid Phase Extraction ; Tablets