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Cureus Mar 2023Intracavernosal injection of Trimix (a combination of phentolamine, papaverine, and alprostadil) is used for the treatment of erectile dysfunction. A rare but serious...
Intracavernosal injection of Trimix (a combination of phentolamine, papaverine, and alprostadil) is used for the treatment of erectile dysfunction. A rare but serious side effect of Trimix is priapism, a persistent erection lasting for more than four hours. Penoscrotal decompression is a newer technique being used to treat refractory and persistent ischemic priapism. Here, we report a unique case of priapism treated with penoscrotal decompression in a patient following an unmeasured injection of Trimix. A 36-year-old male presented to the emergency room complaining of a persistent painful erection over the previous five days following a Trimix injection and illicit methamphetamine use. At bedside, aspiration and irrigation were attempted without any improvement. Phenylephrine injection was contraindicated due to sinus tachycardia. The patient then underwent bilateral penoscrotal decompression on day six post-Trimix injection. The procedure was successful with a resolution of the erection, though some moderate corporal fibrosis was noted. At a 10-day follow-up, the patient reported moderate pain in his penis but had regained complete potency. Misuse of Trimix can cause persistent ischemic priapism. Penoscrotal decompression is a novel technique used to treat persistent ischemic priapism and has been shown to have positive efficacy in the resolution of priapism as well as in salvaging erectile function. To our knowledge, treatment of persistent priapism with penoscrotal decompression after using Trimix has not yet been reported in the literature. Given the rarity of this, our report highlights a unique case that has potential benefit for future practitioners who are faced with this clinical scenario.
PubMed: 37123749
DOI: 10.7759/cureus.36757 -
Molecules (Basel, Switzerland) Mar 2023The pharmacological actions of benzylisoquinoline alkaloids are quite substantial, and have recently attracted much attention. One of the principle benzylisoquinoline... (Review)
Review
The pharmacological actions of benzylisoquinoline alkaloids are quite substantial, and have recently attracted much attention. One of the principle benzylisoquinoline alkaloids has been found in the unripe seed capsules of L. Although it lacks analgesic effects and is unrelated to the compounds in the morphine class, it is a peripheral vasodilator and has a direct effect on vessels. It is reported to inhibit the cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) phosphodiesterase in smooth muscles, and it has been observed to increase intracellular levels of cAMP and cGMP. It induces coronary, cerebral, and pulmonary artery dilatation and helps to lower cerebral vascular resistance and enhance cerebral blood flow. Current pharmacological research has revealed that papaverine demonstrates a variety of biological activities, including activity against erectile dysfunction, postoperative vasospasms, and pulmonary vasoconstriction, as well as antiviral, cardioprotective, anti-inflammatory, anticancer, neuroprotective, and gestational actions. It was recently demonstrated that papaverine has the potential to control SARS-CoV-2 by preventing its cytopathic effect. These experiments were carried out both in vitro and in vivo and require an extensive understanding of the mechanisms of action. With its multiple mechanisms, papaverine can be considered as a natural compound that is used to develop therapeutic drugs. To validate its applications, additional research is required into its precise therapeutic mechanisms as well as its acute and chronic toxicities. Therefore, the goal of this review is to discuss the major studies and reported clinical studies looking into the pharmacological effects of papaverine and the mechanisms of action underneath these effects. Additionally, it is recommended to conduct further research via significant pharmacodynamic and pharmacokinetic studies.
Topics: Humans; Papaverine; Opium; COVID-19; SARS-CoV-2; Alkaloids; Benzylisoquinolines
PubMed: 37049912
DOI: 10.3390/molecules28073149 -
Foods (Basel, Switzerland) Apr 2023Morphine and codeine are the two principal opiates found in the opium poppy ( L.) and are therapeutically used for pain management. Poppy seeds with low opiates are...
Morphine and codeine are the two principal opiates found in the opium poppy ( L.) and are therapeutically used for pain management. Poppy seeds with low opiates are primarily used for culinary purposes due to their nutritional and sensory attributes. Intentional adulteration of poppy seeds is common, often combined with immature, less expensive, exhausted, or substituted with morphologically similar seeds, viz., amaranth, quinoa, and sesame. For a safer food supply chain, preventive measures must be implemented to mitigate contamination or adulteration. Moreover, the simultaneous analysis of and its adulterants is largely unknown. Pre- and post-processing further complicate the alkaloid content and may pose a significant health hazard. To address these issues, two independent methods were investigated with eight botanically verified and fifteen commercial samples. Microscopical features were established for the authenticity of raw poppy seeds. Morphine, codeine, and thebaine quantities ranged from 0.8-223, 0.2-386, and 0.1-176 mg/kg, respectively, using LC-QToF. In most cases, conventional opiates have a higher content than papaverine and noscapine. The analytical methodology provided a chemical profile of 47 compounds that can be effectively applied to distinguish poppy seeds from their adulterants and may serve as an effective tool to combat ongoing adulteration.
PubMed: 37048333
DOI: 10.3390/foods12071510 -
African Health Sciences Sep 2022Drotaverine, a spasmolytic, has been found to have potential to achieve a reduction in the duration of labour and prevent prolonged labour. (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Drotaverine, a spasmolytic, has been found to have potential to achieve a reduction in the duration of labour and prevent prolonged labour.
OBJECTIVE
To compare the effects of intravenous drotaverine hydrochloride with placebo for shortening the duration of active phase of labour in primigravidas.
METHODS
A double-blind, placebo-controlled randomized trial of 246 primigravidas in active phase of labour at term was conducted. They were randomly (1:1 ratio) administered intravenous 2 ml (40mg) of drotaverine hydrochloride or 2 ml of Vitamin B complex as placebo. The primary outcome measure was the duration of active phase of labour. The secondary outcome measures were cervical dilatation rate, oxytocin augmentation rate, incidence of prolonged labour, labour pain scores, mode of delivery, maternal and neonatal outcomes.
RESULTS
The mean duration of active phase of labour (hour) was significantly lower in the drotaverine group compared to the control (drotaverine; 6.22 ± 2.41 vs placebo; 8.33 ± 3.56; p <0.001). Also, the cervical dilatation rate (cm/hr) was significantly faster in the drotaverine arm (drotaverine; 1.68 ± 1.02 versus placebo; 1.06 ± 0.53, p <0.001). There was a significantly higher probability of faster delivery among women who were given drotaverine (log-rank test, p < 0.001). The oxytocin augmentation rate, incidence of prolonged labour, labour pain scores, mode of delivery, maternal and neonatal outcomes were not significantly different among the groups.
CONCLUSIONS
Drotaverine hydrochloride is effective in shortening the duration of active phase of labour without adverse maternal and neonatal outcomes. However, more evidence is needed to explore its role in active phase of labour among primigravid women. Trial registration number: PACTR201810902005232.
Topics: Pregnancy; Infant, Newborn; Female; Humans; Oxytocin; Labor Pain; Labor, Obstetric; Papaverine; Double-Blind Method
PubMed: 36910347
DOI: 10.4314/ahs.v22i3.13 -
Scientific Reports Feb 2023In this paper, we present the results of toxicological analyses of preserved brain tissue and bone samples from the remains of the seventeenth century patients of the...
In this paper, we present the results of toxicological analyses of preserved brain tissue and bone samples from the remains of the seventeenth century patients of the Ospedale Maggiore, the main hospital in Milan and one of the most innovative hospitals in Europe from the Renaissance period. Beneath it, the crypt functioned as the burial place for the deceased of the hospital. In this multidisciplinary study of the remains, toxicological analyses in particular were performed with HPLC-MS/MS on different biological samples from nine individuals. Anthropological, paleopathological, histological, radiological examinations and radiocarbon dating were also carried out. As a result, archeotoxicological analyses revealed the presence of codeine, morphine, noscapine and papaverine, derived from Papaver somniferum, a plant present in the hospital pharmacopeia used as a narcotic, analgesic, astringent, coagulant, and antitussive agent. Such analyses have shed light on the pharmacological therapies administered to the patients near the time of death and have implemented our knowledge of medical treatment and drug administration in the 1600's.
Topics: Humans; Papaver; Tandem Mass Spectrometry; Brain; Italy; Hospitals; Narcotics
PubMed: 36854677
DOI: 10.1038/s41598-023-27953-1 -
Molecules (Basel, Switzerland) Feb 2023Bioconversion of biosynthetic heterocyclic compounds has been utilized to produce new semisynthetic pharmaceuticals and study the metabolites of bioactive drugs used...
Bioconversion of biosynthetic heterocyclic compounds has been utilized to produce new semisynthetic pharmaceuticals and study the metabolites of bioactive drugs used systemically. In this investigation, the biotransformation of natural heterocyclic alkaloid papaverine via filamentous fungi was explored. Molecular docking simulations, using protein tyrosine phosphatase 1B (PTP1B), α-glucosidase and pancreatic lipase (PL) as target enzymes, were performed to investigate the antidiabetic potential of papaverine and its metabolites in silico. The metabolites were isolated from biotransformation of papaverine with NRRL 2310, NRRL y1592, ATCC 10002 and NRRL 1369 via reduction, demethylation, -oxidation, oxidation and hydroxylation reactions. Seven metabolites were isolated: namely, 3,4-dihydropapaverine (metabolite ), papaveroline (metabolite ), 7-demethyl papaverine (metabolite ), 6,4'-didemethyl papaverine (metabolite ), papaverine-3-ol (metabolite ), papaverinol (metabolite ) and papaverinol N-oxide (metabolite ). The structural elucidation of the metabolites was investigated with 1D and 2D NMR and mass spectroscopy (EI and ESI). The molecular docking studies showed that metabolite exhibited better binding interactions with the target enzymes PTP1B, α-glucosidase and PL than did papaverine. Furthermore, papaverinol--oxide () also displayed inhibition of α-glucosidase and lipase enzymes comparable to that of their ligands (acarbose and orlistat, respectively), as unveiled with an in silico ADMET profile, molecular docking and molecular dynamics studies. In conclusion, this study provides evidence for enhanced inhibition of PTP1B, α-glucosidase and PL via some papaverine fungal transformation products and, therefore, potentially better antidiabetic and antiobesity effects than those of papaverine and other known therapeutic agents.
Topics: Hypoglycemic Agents; Papaverine; Molecular Docking Simulation; alpha-Glucosidases; Biotransformation; Lipase; Oxides
PubMed: 36838572
DOI: 10.3390/molecules28041583 -
Oxidative Medicine and Cellular... 2022The genus is highly esteemed in the pharmacy industry, in the culinary field, and as ornamental plants. These plants are also valued in traditional medicine. Among all... (Review)
Review
The genus is highly esteemed in the pharmacy industry, in the culinary field, and as ornamental plants. These plants are also valued in traditional medicine. Among all species, L. (opium poppy) is the most important species in supplying phytochemicals for the formulation of drugs, mainly alkaloids like morphine, codeine, rhoeadine, thebaine, and papaverine. In addition, plants present other types of phytochemicals, which altogether are responsible for its biological activities. Therefore, this review covers the phytochemical composition of r plants, including alkaloids, phenolic compounds, and essential oils. The traditional uses are reviewed along with their pharmacological activities. Moreover, safety aspects are reported to provide a deep overview of the pharmacology potential of this genus. An updated search was carried out in databases such as Google Scholar, ScienceDirect, and PubMed to retrieve the information. Overall, this genus is a rich source of alkaloids of different types and also contains interesting phenolic compounds, such as anthocyanins, flavonols, and the characteristic indole derivatives nudicaulins. Among other pharmacological properties, numerous preclinical studies have been published about the analgesic, anticancer, antimicrobial, antioxidant, and antidiabetic activities of plants. Although it highlights the significant impact of this genus for the treatment of a variety of diseases and conditions, as a future prospect, characterization works accompanying preclinical studies are required along with clinical and toxicology studies to establish a correlation between the scientific and traditional knowledge.
Topics: Papaver; Anthocyanins; Alkaloids; Phytochemicals; Medicine, Traditional
PubMed: 36824615
DOI: 10.1155/2022/2041769 -
Indian Journal of Urology : IJU :... 2023The most common reason for constructing an arteriovenous fistula (AVF) is chronic kidney disease. Various factors are associated with nonmaturation or failure of AVF,...
INTRODUCTION
The most common reason for constructing an arteriovenous fistula (AVF) is chronic kidney disease. Various factors are associated with nonmaturation or failure of AVF, which can be evaluated using color Doppler/duplex ultrasound (DUS). We carried out this study to evaluate the role of pre- and postoperative DUS for the prediction of outcomes of wrist radiocephalic (RC) AVF.
METHODS
In our prospective observational study, dialysis-dependent patients between 20 and 70 years of age undergoing primary RC-AVF from May 2019 to July 2020 were included. All patients underwent pre- and postoperative DUS examination after obtaining consent.
RESULTS
Among 104 participants, 87 (83.7%) were male and 17 (16.3%) were female. Successful maturation was seen in 68 (65.4%) participants, whereas 90 (86.53%) had functional maturation. Radial artery diameter (RAD) ≥1.6 mm, cephalic vein diameter (CVD) ≥2.0 mm, vein distensibility (VD) ≥0.5 mm, and peak systolic velocity (PSV) RAD ≥30 cm/s were associated with higher successful maturation of AVF with statistically significant results ( < 0.05). RAD ≥1.6 mm, CVD ≥2.0 mm, VD ≥0.5 mm, and PSV RAD ≥30 cm/s were related to a greater probability of RC-AVF maturation. Among them, VD and PSV-RA were the most influencing factors predicting RC-AVF successful maturation.
CONCLUSIONS
If we consider the rule of six for AVF maturation, then the results will be much less than the actual fistulas which are dialyzable with adequate blood flow as per functional maturation criteria. Thus, more randomized studies are needed to define maturation criteria for the Indian population and to identify the effect of papaverine on successful AVF maturation.
PubMed: 36824103
DOI: 10.4103/iju.iju_190_22 -
International Journal of Impotence... May 2024Peyronie's disease (PD) is a debilitating pathology which is associated with penile curvature and erectile dysfunction due to the formation of fibrotic plaques in the...
Peyronie's disease (PD) is a debilitating pathology which is associated with penile curvature and erectile dysfunction due to the formation of fibrotic plaques in the penile tunica albuginea. In the present study, we developed a novel rabbit model of PD via subtunical injection of recombinant transforming growth factor (TGF)-β1 protein and characterized erectile function and histopathological endpoints following plaque formation. Ten adult male, New Zealand white rabbits were randomized into 3 experimental groups including nonsurgical controls (NSC, N = 3) and those receiving subtunical injections of vehicle (N = 3) or TGF-β1 protein (0.5 µg/50 µl; N = 4). Following 1 month post-op, focal fibrous plaques composed of disorganized collagen type I and III bundles as well as fragmented elastin fibers at TGF-β1 injection sites were observed in contrast to control groups. Cavernosometric and cavernosographic evaluations revealed no significant differences in maximum intracorporal pressures or substantial curvature during papaverine-induced erection in either the vehicle or TGF-β1 cohorts. Immunohistochemical and histomorphometric analyses demonstrated significant increases in elastase 2B expression in TGF-β1-induced plaques as well as significant declines in matrix metalloproteinase (MMP)-2 and -9 expression relative to control levels. Our results demonstrate that PD-like fibrotic plaques can be created in the rabbit penile tunica albuginea following TGF-β1 injection.
PubMed: 36782023
DOI: 10.1038/s41443-023-00671-y -
Frontiers in Surgery 2022Abnormal contraction of uterus and vascular smooth muscle lead to the formation of hypoxia environment in uterus. Abnormal contraction may be the basis of dysmenorrhea,...
OBJECTIVE
Abnormal contraction of uterus and vascular smooth muscle lead to the formation of hypoxia environment in uterus. Abnormal contraction may be the basis of dysmenorrhea, endometriosis, infertility and other diseases. Phloroglucinol is a non-atropine and non-papaverine smooth muscle spasmolytic agent, which can reduce the abnormal contraction of uterine smooth muscle. This study investigated the effect of phloroglucinol on frozen embryo transfer in patients with endometriosis.
METHODS
The data of patients with endometriosis who underwent a frozen embryo transfer in Shanghai Changzheng Hospital from August 2018 to August 2021, comprising a total of 453 cycles, were retrospectively analyzed. The patients for whom phloroglucinol was included over 217 cycles were administered intramuscully 40 mg phloroglucinol starting on the day of progesterone administration, then once daily up to day 7 after the embryo transfer. Those for whom phloroglucinol was not administered over 236 cycles were used as the control group. The age of 35 years was used as a boundary in this study to observe the pregnancy outcomes of patients in the two different age groups.
RESULTS
The biochemical pregnancy rate (63.13% vs. 51.27%), embryo implantation rate (44.64% vs. 33.60%), clinical pregnancy rate (59.64% vs. 48.30%), and live birth rate (52.99% vs. 36.86%) after the administration of phloroglucinol were higher than for patients in the control group, and the early abortion rate (7.75% vs. 20.18%) was also lower. The differences were statistically significant ( < 0.05). In particular, in the age group <35 years old, the embryo implantation rate (51.81% vs. 39.38%), clinical pregnancy rate (69.34% vs. 57.55%), and the live birth rate (63.50% vs. 44.60%) after phloroglucinol intervention rose significantly, and the abortion rate dropped (6.32% vs. 17.5%), indicating a statistically significant difference ( < 0.05). However, pregnancy outcomes showed no difference in the age group ≥35 years old ( > 0.05).
CONCLUSION
Continuous low-dose phloroglucinol pretreatment before and after frozen embryo transfer can improve both the clinical pregnancy and live birth rates and reduce the risk of abortion in younger infertile patients with endometriosis.
PubMed: 36684314
DOI: 10.3389/fsurg.2022.994775