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At least 19 recordsLinked to original sources
PubMed1983

Mechanism of relaxant action of papaverine. II. Differences between modes of relaxant effects of papaverine and amytal in guinea-pig taenia coli.

Mode of relaxant effect of papaverine on guinea-pig taenia coli was compared with that of amytal, especially in regard to their actions on the calcium movements. The present results provided evidence that the mode of relaxant effect of papaverine differs from that of amytal. Papaverine relaxed the taenia coli even in the Na-free solution although its relaxant activity was markedly reduced, while amytal failed to reveal relaxant activity in the same condition. Reintroduction of a small amount of sodium ion to the Na-free solution restored the relaxant activities of papaverine and amytal but their sodium ion dependencies of the restoration were not equal. Amytal was more sensitive to sodium ion than papaverine. Papaverine induced the muscle relaxation with synchronous acceleration of 45Ca-efflux, while the relaxation in response to amytal was not accompanied by acceleration of 45Ca-efflux. The cellular 45Ca-uptake was inhibited by papaverine, but not by amytal. In these experiments, both papaverine and amytal were used at sufficient doses to inhibit the mitochondrial respiration. From these findings, it is concluded that papaverine relaxes the smooth muscle through different mechanism from that of amytal and thus the relaxant effect of papaverine may not be related to its inhibitory action on the mitochondrial respiration.

Amobarbital↗
PubMed1990

Toxicity assessment of papaverine hydrochloride and papaverine-derived metabolites in primary cultures of rat hepatocytes.

The present study was undertaken to assess and compare the toxic effects of papaverine hydrochloride and its metabolites. Primary cell cultures of rat hepatocytes were treated with papaverine (papaver), 3'-O-desmethyl (3'-OH), 4'-O-desmethyl (4'-OH), and 6-O-desmethyl (6-OH) papaverine at 1 x 10(-5), 1 x 10(-4), and 1 x 10(-3) M for 4, 8, 12, and 24-h periods. Cell injury was determined by: a) cell viability using the trypan blue exclusion test; b) cytosolic enzyme leakage of lactate dehydrogenase and aspartate aminotransferase; c) morphologic alterations; and d) lactate:pyruvate (L:P) ratios. Cell cultures showed concentration- and time-dependent toxic responses. For example, a decrease in cell viability and an increase in enzyme leakage were observed after cell treatment with 1 x 10(-4) and 1 x 10(-3) M papaver for 8 h; 1 x 10(-3) M 6-OH papaverine for 8 h and 1 x 10(-4) M for 24 h; and 1 x 10(-3) M 4'-OH papaverine for 24 h (P less than 0.05). Furthermore, changes in morphology correlated to cell viability and enzyme release in those cultures treated with papaver, 4'-OH and 6-OH papaverine. Some of these changes included size deformation, cell detachment from the dishes, and cell necrosis. On the other hand, an increase in L:P ratios (P less than 0.05) was detected with papaver as early as 8 h with 1 x 10(-4) and 1 x 10(-3) M and 12 h with 1 x 10(-5) M; 6-OH showed an increase in L:P ratios at 8 h with 1 x 10(-3) M and 12 h with 1 x 10(-4) M; these changes were evident with with 4'-OH at 12 h with 1 x 10(-3) M. In contrast, cells treated with 3'-OH papaverine did not show significant damage with any time period and concentration used in this study. The results of this study indicate that papaverine-derived metabolites are less cytotoxic than its parent compound, papaver. The toxicity was ranked as follows: papaver greater than 6-OH greater than 4'-OH greater than -3'-OH.

Animals↗
PubMed1991

Intracavernous injection of prostaglandin E1 in combination with papaverine: enhanced effectiveness in comparison with papaverine plus phentolamine and prostaglandin E1 alone.

We compared the erectile response to intracavernous injection of a combination of papaverine and prostaglandin E1 with that of a combination of papaverine and phentolamine (49 patients), and prostaglandin E1 alone (38). The degree of erection achieved was significantly better with papaverine plus prostaglandin E1 than with papaverine plus phentolamine and the duration of erection was less, although the incidence of prolonged erections (greater than 5 hours) was similar with both combinations. Papaverine with prostaglandin E1 likewise resulted in a significantly better degree of erection than prostaglandin E1 alone (prolonged erections occurred only after the drug combination). All erections subsided spontaneously and none required medical intervention throughout the study. Pain was noted only after injection of prostaglandin E1. The incidence was clearly lower (7 of 38 versus 13 of 38) after the injection of only 5 micrograms. prostaglandin E1 in combination with papaverine (although the difference is not statistically significant). Subjectively, the side effects caused by the drug combination were described as much less dramatic by the patients than after prostaglandin E1 alone. The combination of papaverine and prostaglandin E1 shows a clearly synergistic effect and might suitably replace papaverine plus phentolamine or prostaglandin E1 alone in patients who do not respond well or suffer side effects after high single doses.

Adult↗
PubMed1989

Treatment of impotence by intrapenile injections. A comparison of papaverine versus papaverine and phentolamine: a double-blind, crossover trial.

The efficacy of papaverine, and a combination of papaverine and phentolamine as a pharmacological treatment of impotence was compared in a double-blind, crossover trial. A total of 40 impotent men received intracavernous injections of papaverine (40 mg.) or a combination of papaverine (20 mg.) and phentolamine (0.5 mg.) at monthly intervals. Observations at 20 minutes after injection demonstrated that papaverine caused full erections in 27 per cent of the men and partial erections in 65 per cent. The combined injection resulted in full erections in 48 per cent of the men and 52 per cent had partial erections. The difference was significant (Z equals 2.29, p less than 0.05).

Adult↗
PubMed1983

Mechanism of relaxant action of papaverine. III. Comparison of sodium ion dependencies on the relaxant effects of papaverine, Aspaminol and benactyzine in guinea-pig taenia coli.

The role of sodium ion on the relaxant action of papaverine in guinea-pig taenia coli contracted by hypertonic 40 mM KCl were studied by manipulating the external sodium ion concentration and compared with those of its allied antispasmodics, Aspaminol and benactyzine. Whereas all of the three antispasmodics relaxed the taenia in all media used herein, their relaxant activities were declined by eliminating sodium ion from the bathing media. The declined relaxant activities were restored by re-introducing sodium ion to the solution depending on the amount of sodium ion but sodium ion dependencies of the restoration were not equal for each. In a solution containing 20 mM sodium ion, almost complete restoration was encountered with papaverine, while displayed only a slight restoration with Aspaminol and benactyzine. When a small amount of sodium ion was applied to the taenia before or after the treatment with the antispasmodics, the relaxation in response to papaverine was augmented, but those in response to Aspaminol and benactyzine were not affected. All of the three antispasmodics inhibited the cellular 45Ca-uptake in all media. While, their inhibitory activities were reduced by eliminating sodium ion from the media and were not restored so markedly by re-introducing 20 mM sodium ion to the solution. From these findings, it is suggested that papaverine may induce the smooth muscle relaxation not only by inhibiting the Ca-influx independently of the presence of sodium ion but also by other mechanisms sensitive to sodium ion, by contrast, Aspaminol and benactyzine may evoke the relaxation through mechanisms less sensitive to the presence of sodium ion, which include the inhibition of Ca-influx.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1995

Papaverine-phentolamine and prostaglandin E1 versus papaverine-phentolamine alone for intracorporeal injection therapy: a clinical double-blind study.

PURPOSE: A study was designed to compare intracorporeal injections of papaverine plus phentolamine (2-drug solution) and papaverine plus phentolamine and prostaglandin E1 (3-drug solution) for the treatment for impotence. MATERIALS AND METHODS: A total of 20 impotent patients received intracorporeal injections of the 2-drug or 3-drug solution alternately during 2 sessions, and the quality and duration of erections were assessed. RESULTS: Of the patients 73% achieved a full erection with the 3-drug solution compared to 28% with the 2-drug solution. The average duration of erections was 57 minutes and 33.6 minutes, respectively. The complication rate was similar for the 2 treatments. CONCLUSIONS: Papaverine plus phentolamine and prostaglandin E1 is superior to papaverine plus phentolamine alone for the treatment of impotence.

Adult↗
PubMed1986

Papaverine: the ideal coronary vasodilator for investigating coronary flow reserve? A study of timing, magnitude, reproducibility, and safety of the coronary hyperemic response after intracoronary papaverine.

A potent, short-acting vasodilator that induces a maximal hyperemic response of the coronary vascular bed is needed to determine coronary flow reserve. In 12 patients, we measured coronary sinus blood flow by thermodilution over a period of 2 min during which a bolus of 10 mg papaverine was given into the left main coronary artery. This was repeated after 5 min to assess the reproducibility of the changes. The maximal hyperemic response lasted from 24 until 37 sec after papaverine administration. There was no significant difference between the two consecutive hyperemic responses (Student's t-test for paired observations). The mean difference between first and second hyperemic responses at 30 sec was 7.0% (SD +/- 6.2%). In conclusion, 10 mg of intracoronary papaverine is a short-lasting and reproducible means of inducing a maximal hyperemic response in the coronary vascular bed and therefore appears to be the ideal agent for investigating coronary flow reserve.

Aged↗
PubMed1981

Papaverine-insensitive and papaverine-sensitive drug-induced contractions of chick smooth muscle.

The mechanisms by which acetylcholine (ACh) and noradrenaline (NA) induce muscle contraction were examined in the chick expansor secundariorum muscle in early life, because responsiveness to ACh disappeared and responsiveness to NA persisted during development. ACh-induced contractions decreased with lowered temperature, while NA-induced contractions increased between 30 and 20 degrees C. Papaverine depressed and antagonized NA-induced contractions, but did not depress ACh-induced contractions. The second application of ACh in Ca2+-free solution produced a negligible contraction. In contrast, even the third application of NA in Ca2+-free solution still evoked a contraction of more than 50% of the response in normal solution. These results suggest that the pathway from cholinergic receptor activation to contraction is mainly mediated through a papaverine-insensitive and external Ca2+-dependent process, whereas the pathway from adrenergic receptor activation to contraction is mainly mediated through a papaverine-sensitive and external Ca2+-independent process.

Animals↗
PubMed1982

Papaverine degradation with papaverine mutants of a Nocardia sp.

Nocardia mutants, capable of utilizing papaverine as a sole source of carbon and nitrogen, were induced with N-methyl-N'-nitro-N-nitrosoguanidine and mitomycin C. The isolated mutants were divided in four groups, depending on the accumulated papaverine metabolites: 4 = 2-(2-hydroxy-4,5-dimethoxyphenyl)ethanol; 5 = 3,4-dimethoxyphenylacetic acid; 6 = 2-hydroxy-4,5-dimethoxyphenylacetic acid; 10 = 3-(3,4-dimethoxybenzyl)-2-hydroxy-5,6-dimethoxy-1-indenone; 11 = 4-(3,4-dimethoxybenzyl)-6,7-dimethoxyisocoumarin. The degrading pathway of metabolites 5 and 6 was investigated. Studies of the cell wall and membrane fraction of the mutants and wild-type show two inducible, particle-bound proteins with the molecular mass of 29 000 and 60 000 Da involved in papaverine degradation.

Bacterial Proteins↗
PubMed1978

Metabolism of papaverine IV. Urinary elimination of papaverine metabolites in man.

1. A gas chromatographic method is described for the quantitative determination of the metabolites of papaverine in urine. 2. The urinary excretion of papaverine metabolites was studied in man. About 50% of the metabolites of papaverine are excreted in the urine within 48 h. 6-Desmethylpapaverine is the major metabolite in the urine. The metabolites are excreted almost completely in conjugated form.

Biotransformation↗
PubMed1992

[Prospective study of the effectiveness and side effects of intracavernous prostaglandin E1 versus papaverine or papaverine phentolamine in the diagnosis and treatment of erection dysfunction. Review of the literature].

E1 prostaglandins (E1-PG) by intracavernous injection has been given for diagnostic purposes to 70 randomly selected patients visiting the practice with erectile dysfunction (ED). Sixty-one were suggested to begin a weekly intracavernous self-injection (WICSI) according to the established protocol. Fifty-one patients (83.6%) started the therapy and within an 18-months follow-up interval only 2 (3.27%) preferred to return to papaverine, since 20 patients had previously undergone the papaverine test and 6 were on WICSI with this preparation. Fifty-three patients (75%) achieved complete erection, 8 (11.4%) enough erection to penetrate without manual help, representing a total efficacy of 87%. E1-PG dosage varied from 10 to 40 mcg based on diagnosis, and was readjusted in 6 of the 9 patients which in the initial tests had not obtained sufficient erection, therefore bringing about a final 91.4% erections of sufficient characteristics for intercourse to be considered normal. During the year and a half follow-up a total of 2,880 E1-PG self-injections were injected without during this time cases of priapism, systemic reactions, cavernous bodies infections, arteriovenous fistulae, fibrosis of the cavernous bodies, etc, being observed. Two patients showed prolonged erections of 3-5 hours during the E1-PG tests which remitted spontaneously without sequelae and now continue the WICSI programme after dosage readjustment. In our experience, E1-PG intracavernous injection has proven to be more effective than papaverine in the treatment of erectile dysfunction and therefore, added to its safety and degree of acceptance, we consider it a first choice approach in the diagnosis and treatment of erectile dysfunction in males.

Adult↗
PubMed1977

The inhibitory effect of papaverine on respiration-dependent contracture of guinea pig taenia coli in high-K medium. III. The differential effect of papaverine and rotenone on DT diaphorase.

The differential effects of papaverine (Pap) and rotenone (Rot) were studied on the highly respiration-dependent contracture of guinea pig taenia coli in 40 mM potassium (40-K) medium, on isolated DT diaphorase activity and on mitochondrial respiration. The inhibition of guinea pig taenia coli to the 40-K induced tension by Rot (5 x 10(-7)M) was fully reversed by the addition of a water soluble vitamin K3 (VK3) derivative or menadione sodium bisulfite (MSB). A low concentration (10(-7)--10(-6)M) of Pap which had no effect on the 40-K induced tension inhibited the VK3 restored tension from the Rot suppression, corresponding to a Pap inhibition of the isolated DT diaphorase. Inhibition of the effective concentration of Pap to the 40-K induced tension development was never reversed by addition of VK3 or MSB. In taenia coli, both MSB and VK3 established a bypass of the Rot sensitive site on the mitochondrial respiratory chain by means of the DT diaphorase system. The difference in washout-efficacy between Pap and Rot on the inhibition of 40-K induced tension was ascribed to a difference in their mitochondrial binding properties.

Animals↗