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  1. Simple and high sample throughput LC/ESI-MS/MS method for bioequivalence study of prazosin, a drug with risk of orthostatic hypotension
    Loh GOK, Wong EYL, Tan YTF, Wee HC, Ng RS, Syed HK, et al.
    Drug Dev Ind Pharm, 2022 Sep;48(9):470-479.
    PMID: 36111737 DOI: 10.1080/03639045.2022.2125985
    OBJECTIVE: The study aimed to develop a rapid, simple and sensitive LC/ESI-MS/MS method to measure prazosin concentration in human plasma and apply bedside sampling in bioequivalence study of two prazosin tablets to resolve the adverse effect of orthostatic hypotension.

    SIGNIFICANCE: The LC/ESI-MS/MS prazosin method was highly sensitive and selective. Bedside sampling reduced the orthostatic hypotension incidence and subject dropout rate.

    METHODS: After sample preparation, prazosin and terazosin (IS) were detected on mass spectrometer operating in multiple reaction monitoring mode using positive ionization. Mobile phase flow rate was set at 0.40 mL/min with sample run time of 1.75 min. The bioanalytical method was validated as per EMEA and FDA guidelines. Bedside sampling was performed in bioequivalence study for the first 4 h after dosing. The three primary pharmacokinetic parameters, Cmax, AUC0-t and AUC0-∞ and 90% confidence interval were determined.

    RESULTS: The small injection volume of 1 μL minimized instrumentation contamination and prolonged the analytical column lifespan. Linearity was obtained between 0.5 and 30.0 ng/mL, with coefficient of determination, r2 ≥ 0.99. The mean extraction recovery of prazosin and IS was >92%, with precision value (CV, %) ≤ 10.3%. Only two orthostatic hypotension adverse events were reported. The two prazosin formulations were found to be bioequivalent.

    CONCLUSION: The LC/ESI-MS/MS method has shown robustness and reliability exemplified by the incurred sample re-analysis result. Bedside sampling should be proposed for bioequivalence or pharmacokinetic studies of drugs demonstrating adverse event of orthostatic hypotension.

    Matched MeSH terms: Prazosin/adverse effects
  2. Fulltext Urinary incontinence caused by prazosin
    Rachagan SP, Mathews A
    Singapore Med J, 1992 Jun;33(3):308-9.
    PMID: 1631598
    Urinary incontinence is a common problem in elderly women. However, urinary incontinence secondary to the commonly used antihypertensive, prazosin, is a rare phenomenon. The possible mechanism of this drug in causing incontinence is described in this case report. The possibility of an exaggerated response to the drug by women suffering from borderline stress incontinence is highlighted.
    Matched MeSH terms: Prazosin/adverse effects*
  3. Improved high-performance liquid chromatographic analysis of terazosin in human plasma
    Cheah PY, Yuen KH, Liong ML
    J Chromatogr B Biomed Sci Appl, 2000 Aug 18;745(2):439-43.
    PMID: 11043762
    A simple, sensitive and reproducible high-performance liquid chromatography (HPLC) method was developed for the determination of terazosin in human plasma. The method involves a one-step single solvent extraction procedure using dichloromethane with a 0.25 ml plasma sample. Recovery values were all greater than 90% over the concentration range 0.25-100 ng/ml. Terazosin was found to adsorb to glass or plastic tubes, but this could be circumvented by using disposable plastic tubes. Also, rinsing the injector port with methanol after each injection helped to prevent any carry-over effect. The internal standard, prazosin, did not exhibit this problem. The method has a quantification limit of 0.25 ng/ml. The within- and between-day coefficient of variation and accuracy values were all less than 7% over the concentration range 0.25-100 ng/ml and hence the method is suitable for use in pharmacokinetic studies of terazosin.
    Matched MeSH terms: Prazosin/analogs & derivatives*; Prazosin/blood*; Prazosin/pharmacokinetics
  4. Simple and fast LC-MS/MS method for quantification of terazosin in human plasma and application to bioequivalence study
    Loh GOK, Wong EYL, Tan YTF, Ong LM, Ng RS, Wee HC, et al.
    J Chromatogr B Analyt Technol Biomed Life Sci, 2021 Jan 15;1163:122517.
    PMID: 33429127 DOI: 10.1016/j.jchromb.2020.122517
    A simple, fast and sensitive LC-MS/MS method was developed to quantify terazosin in human plasma. The mobile phase consisted of acetonitrile-0.1% (v/v) formic acid (70:30, v/v). Prazosin was used as internal standard (IS). As deproteinization agent, acetonitrile produced a clean sample. A higher response intensity with more symmetrical peak was obtained using Agilent Poroshell 120 EC-C18 - Fast LC column (100 × 2.1mmID, 2.7 μm) compared with Kinetex XB-C18 (100 × 2.1 mm, 2.6 µm) column. The response of terazosin and IS were approximately two times in citrate phosphate dextrose (CPD) plasma compared with dipotassium ethylenediaminetetraacetic acid (K2EDTA) plasma. Plasma calibration curve was linear from 1.0 to 100.0 ng/mL, with coefficient of determination r2 ≥ 0.99. The within-run and between-run precision values (CV, %) were <5.2% and <7.8%, while accuracy values were 102.8-112.7% and 103.4-112.2%. The extended run accuracy was 98.6-102.8% and precision (CV, %) 4.3-10.4%. The recovery of analyte was >98% and IS >94%. Terazosin in plasma kept at benchtop was stable for 24 h, in autosampler tray for 48 h, in instrumentation room for 48 h, for 7 freeze-thaw cycles and in freezer for 140 days. Terazosin and IS stock standard solutions were stable for 140 days at room temperature and in the chiller. The high throughput method was successfully utilized to measure 935 samples in a bioequivalence study of terazosin.
    Matched MeSH terms: Prazosin/administration & dosage; Prazosin/analogs & derivatives*; Prazosin/blood; Prazosin/pharmacokinetics
  5. Fulltext Prazosin and priapism
    Segasothy M
    Med J Malaysia, 1982 Dec;37(4):384.
    PMID: 7167095
    Matched MeSH terms: Prazosin/adverse effects*
  6. Terazosin therapy for patients with female lower urinary tract symptoms: a randomized, double-blind, placebo controlled trial
    Low BY, Liong ML, Yuen KH, Chee C, Leong WS, Chong WL, et al.
    J Urol, 2008 Apr;179(4):1461-9.
    PMID: 18295277 DOI: 10.1016/j.juro.2007.11.060
    PURPOSE: We determined the clinical efficacy and safety of terazosin in the treatment of patients with female lower urinary tract symptoms.
    MATERIALS AND METHODS: A total of 100 females 20 to 70 years old who met the inclusion criteria of total International Prostate Symptom Score 8 or greater, symptom duration 1 or more months, and did not meet any exclusion criteria were entered into the study. Subjects were randomized to receive terazosin or placebo in titrated dose from 1 mg od, 1 mg twice daily to 2 mg twice daily during 14 weeks. Successful treatment outcomes use primary end point of International Prostate Symptom Score quality of life 2 or less and secondary end point of total International Prostate Symptom Score 7 or less. Other outcome measures included International Prostate Symptom Score individual item scores, King's Health Questionnaire quality of life domains, objective assessment parameters of 24-hour frequency volume chart, maximum flow rate and post-void residual urine.
    RESULTS: Using a primary end point, 32 of 40 (80%) evaluable terazosin subjects responded in contrast to 22 of 40 (55%) evaluable placebo subjects (p <0.02). The secondary end point revealed a successful outcome in 85% of terazosin subjects vs 55% in placebo (p <0.01). Of the 7 International Prostate Symptom Score individual item scores, only item scores of frequency and straining showed statistically significant reductions with terazosin (p <0.01). All King's Health Questionnaire quality of life domains except domain of severity measures showed statistically significant improvement with terazosin (p <0.05). There were no differences between treatment groups in all objective assessment parameters. Of all evaluable subjects 23 of 40 (58%) on placebo experienced adverse events vs 16 of 40 (40%) on terazosin (p >0.05).
    CONCLUSIONS: Terazosin proved to be more effective and safe than placebo in patients with female lower urinary tract symptoms.
    Matched MeSH terms: Prazosin/analogs & derivatives*; Prazosin/therapeutic use
  7. Terazosin therapy for chronic prostatitis/chronic pelvic pain syndrome: a randomized, placebo controlled trial
    Cheah PY, Liong ML, Yuen KH, Teh CL, Khor T, Yang JR, et al.
    J Urol, 2003 Feb;169(2):592-6.
    PMID: 12544314 DOI: 10.1097/01.ju.0000042927.45683.6c
    PURPOSE: We evaluate terazosin therapy for chronic prostatitis/chronic pelvic pain syndrome.
    MATERIALS AND METHODS: The study included 100, 20 to-50-year-old subjects who met the consensus criteria for chronic prostatitis/chronic pelvic pain syndrome and had not received previous alpha-blockers. Subjects were randomized to receive terazosin with dose escalation from 1 to 5 mg. daily or placebo for 14 weeks. The primary criterion for response was scoring 2 or less ("delighted-to-mostly satisfied") on the National Institutes of Health Chronic Prostatitis Symptom Index (NIH-CPSI) quality of life item. The secondary criterion for response was greater than 50% reduction in NIH-CPSI pain score at 14 weeks. Other outcomes included total and NIH-CPSI domain scores, International Prostate Symptom Score, peak urinary flow rate, post-void residual urine and adverse effects.
    RESULTS: Using the primary criterion 24 of 43 evaluable subjects (56%) responded in the terazosin group compared to 14 of 43 (36%) in the placebo group (p = 0.03). Using the secondary criterion 26 of 43 subjects (60%) responded in the terazosin group compared to 16 of 43 (37%) in the placebo group (p = 0.03). The terazosin group had greater reductions (p <0.05) in NIH-CPSI total score, individual domain scores and International Prostate Symptom Score than the placebo group. There was no difference in peak urinary flow rate or post-void residual. In the terazosin group 18 patients (42%) had side effects compared to 9 (21%) in the placebo group (p = 0.04).
    CONCLUSIONS: Terazosin proved superior to placebo for patients with chronic prostatitis/chronic pelvic pain syndrome who had not received alpha-blockers previously.
    Matched MeSH terms: Prazosin/analogs & derivatives*; Prazosin/therapeutic use*
  8. The fate of prazosin and levonorgestrel after electrochemical degradation process: Monitoring by-products using LC-TOF/MS
    Al-Qaim FF, Mussa ZH, Yuzir A, Latip J, Othman MR
    J Environ Sci (China), 2018 Dec;74:134-146.
    PMID: 30340667 DOI: 10.1016/j.jes.2018.02.019
    Prazosin (PRZ) and levonorgestrel (LNG) are widely used as an anti-disease drugs due to their biological activity in the human body. The frequent detection of these compounds in water samples requires alternative technologies for the removal of both compounds. After electrochemical degradation of PRZ and LNG, the parent compounds could be completely removed after treatment, but the identification and characterization of by-products are necessary as well. In this study, the effects of NaCl concentration and applied voltage were investigated during the electrochemical degradation process. The results revealed that the increase of NaCl concentration and applied voltage could promote the generation of hypochlorite OCl- and then enhance the degradation of PRZ and LNG. After initial study, 6V and 0.2g NaCl were selected for further experiments (96% and 99% removal of PRZ and LNG after 40min, respectively). Energy consumption was also evaluated and calculated for PRZ and LNG at 3, 6 and 8V. Solid phase extraction (SPE) method plays an important role in enhancing the detection limit of by-products. Furthermore, characterization and identification of chlorinated and non-chlorinated by-products were conducted using an accurate liquid chromatography-time of flight/mass spectrometry LC-TOF/MS instrument. The monitoring of products during the electrochemical degradation process was performed at 6V and 0.2g NaCl in a 50mL solution. The results indicated that two chlorinated products were formed during the electrochemical process. The toxicity of by-products toward E. coli bacteria was investigated at 37°C and 20hr incubation time.
    Matched MeSH terms: Prazosin/toxicity; Prazosin/chemistry*
  9. Initial, long-term, and durable responses to terazosin, placebo, or other therapies for chronic prostatitis/chronic pelvic pain syndrome
    Cheah PY, Liong ML, Yuen KH, Teh CL, Khor T, Yang JR, et al.
    Urology, 2004 Nov;64(5):881-6.
    PMID: 15533470 DOI: 10.1016/j.urology.2004.06.041
    OBJECTIVES: To evaluate the initial, long-term, and durable response rates to terazosin, placebo, or other therapies in patients with chronic prostatitis/chronic pelvic pain syndrome.
    METHODS: A total of 100 subjects, aged 20 to 50 years, who met the National Institutes of Health criteria for chronic prostatitis/chronic pelvic pain syndrome and had not previously been treated with alpha-blockers, were entered in a 14-week, double-blind comparison of terazosin or placebo therapy. Nonresponders and responders with subsequent relapse were treated with terazosin or other medications (open label). The criterion for response was a score of 0 to 2 on the National Institutes of Health Chronic Prostatitis Symptom Index quality-of-life item. The initial response was evaluated at week 14, and the long-term response was evaluated after a median of 38 weeks (range 34 to 42), regardless of any additional treatment. A durable response was defined as an initial response without additional treatment.
    RESULTS: Of the 43 patients in the terazosin group, 24 (56%) had an initial response compared with 14 (33%) of 43 subjects in the placebo group (P = 0.03). Long-term responses were noted in 23 (56%) of 41 assessable subjects treated with terazosin initially compared with 12 (32%) of 38 assessable subjects treated with placebo (P = 0.03). Of the nonresponders and initial responders with relapse, 7 (41%) of 17 subjects responded to terazosin compared with 7 (21%) of 34 given other treatment (P = 0.12). Durable responses occurred in 18 (44%) of the 41 assessable patients treated initially with terazosin and in 6 (16%) of 38 treated initially with placebo (P = 0.01).
    CONCLUSIONS: Patients treated with terazosin were more likely to have initial, long-term, and durable responses than those treated with placebo.
    Matched MeSH terms: Prazosin/analogs & derivatives*; Prazosin/therapeutic use
  10. Fulltext Biphasic Effects of α-Asarone on Immobility in the Tail Suspension Test: Evidence for the Involvement of the Noradrenergic and Serotonergic Systems in Its Antidepressant-Like Activity
    Chellian R, Pandy V, Mohamed Z
    Front Pharmacol, 2016;7:72.
    PMID: 27065863 DOI: 10.3389/fphar.2016.00072
    Alpha (α)-asarone is one of the main psychoactive compounds, present in Acorus species. Evidence suggests that the α-asarone possess an antidepressant-like activity in mice. However, the exact dose-dependent effect of α-asarone and mechanism(s) involved in the antidepressant-like activity are not clear. The present study aimed to investigate the dose-dependent effect of α-asarone and the underlining mechanism(s) involved in the antidepressant-like activity of α-asarone in the mouse model of tail suspension test (TST). In this study, the acute effect of α-asarone per se at different doses (10-100 mg/kg, i.p.) on immobility in the TST was studied. Additionally, the possible mechanism(s) involved in the antidepressant-like effect of α-asarone was studied using its interaction with noradrenergic and serotonergic neuromodulators in the TST. The present results reveal that the acute treatment of α-asarone elicited biphasic responses on immobility such that the duration of the immobility time is significantly reduced at lower doses (15 and 20 mg/kg, i.p.) but increased at higher doses (50 and 100 mg/kg, i.p.) in the TST. Besides, α-asarone at higher doses (50 and 100 mg/kg, i.p.) significantly decreased the spontaneous locomotor activity. Moreover, pretreatment of mice with noradrenergic neuromodulators such as AMPT (100 mg/kg, i.p., a catecholamine synthesis inhibitor), prazosin (1 mg/kg, i.p., an α1-adrenoceptor antagonist), yohimbine (1 mg/kg, i.p., an α2-adrenoceptor antagonist) and with serotonergic neuromodulators such as PCPA (100 mg/kg, i.p., once daily for four consecutive days, a serotonin synthesis inhibitor,) and WAY100635 (0.1 mg/kg, s.c., a selective 5-HT1A receptor antagonist) significantly reversed the anti-immobility effect of α-asarone (20 mg/kg, i.p.). Taken together, our results suggest that the acute treatment with α-asarone elicited biphasic actions in the TST in which antidepressant-like effect was seen at relatively lower doses (15 and 20 mg/kg, i.p.) and depressive-like activity at relatively higher doses (50 and 100 mg/kg, i.p.). Furthermore, it has been revealed that the antidepressant-like effect of α-asarone could be mediated through both noradrenergic (α1 and α2 adrenoceptors) and serotonergic (particularly, 5-HT1A receptors) systems.
    Matched MeSH terms: Prazosin
  11. Fulltext Zerumbone Modulates α2A-Adrenergic, TRPV1, and NMDA NR2B Receptors Plasticity in CCI-Induced Neuropathic Pain In Vivo and LPS-Induced SH-SY5Y Neuroblastoma In Vitro Models
    Chia JSM, Izham NAM, Farouk AAO, Sulaiman MR, Mustafa S, Hutchinson MR, et al.
    Front Pharmacol, 2020;11:92.
    PMID: 32194397 DOI: 10.3389/fphar.2020.00092
    Zerumbone has shown great potential in various pathophysiological models of diseases, particularly in neuropathic pain conditions. Further understanding the mechanisms of action is important to develop zerumbone as a potential anti-nociceptive agent. Numerous receptors and pathways function to inhibit and modulate transmission of pain signals. Previously, we demonstrated involvement of the serotonergic system in zerumbone's anti-neuropathic effects. The present study was conducted to determine zerumbone's modulatory potential involving noradrenergic, transient receptor potential vanilloid type 1 (TRPV1) and N-methyl-D-aspartate (NMDA) receptors in chronic constriction injury (CCI)-induced in vitro and lipopolysaccharide (LPS)-induced SH-SY5Y in vitro neuroinflammatory models. von Frey filament and Hargreaves plantar tests were used to assess allodynia and hyperalgesia in the chronic constriction injury-induced neuropathic pain mouse model. Involvement of specific adrenoceptors were investigated using antagonists- prazosin (α1-adrenoceptor antagonist), idazoxan (α2-adrenoceptor antagonist), metoprolol (β1-adrenoceptor antagonist), ICI 118,551 (β2-adrenoceptor antagonist), and SR 59230 A (β3-adrenoceptor antagonist), co-administered with zerumbone (10 mg/kg). Involvement of excitatory receptors; TRPV and NMDA were conducted using antagonists capsazepine (TRPV1 antagonist) and memantine (NMDA antagonist). Western blot was conducted to investigate the effect of zerumbone on the expression of α2A-adrenoceptor, TRPV1 and NMDA NR2B receptors in CCI-induced whole brain samples of mice as well as in LPS-induced SH-SY5Y neuroblastoma cells. Pre-treatment with α1- and α2-adrenoceptor antagonists significantly attenuated both anti-allodynic and anti-hyperalgesic effects of zerumbone. For β-adrenoceptors, only β2-adrenoceptor antagonist significantly reversed the anti-allodynic and anti-hyperalgesic effects of zerumbone. β1-adrenoceptor antagonist only reversed the anti-allodynic effect of zerumbone. The anti-allodynic and anti-hyperalgesic effects of zerumbone were both absent when TRPV1 and NMDA receptors were antagonized in both nociceptive assays. Zerumbone treatment markedly decreased the expression of α2A-adrenoceptor, while an up-regulation was observed of NMDA NR2B receptors. Expression of TRPV1 receptors however did not significantly change. The in vitro study, representing a peripheral model, demonstrated the reduction of both NMDA NR2B and TRPV1 receptors while significantly increasing α2A-adrenoceptor expression in contrast to the brain samples. Our current findings suggest that the α1-, α2-, β1- and β2-adrenoceptors, TRPV1 and NMDA NR2B are essential for the anti-allodynic and antihyperalgesic effects of zerumbone. Alternatively, we demonstrated the plasticity of these receptors through their response to zerumbone's administration.
    Matched MeSH terms: Prazosin
  12. Fulltext Utility of alpha-blockade in a hypotensive pheochromocytoma patient with myocardial infarction
    Wahab NA, Zainudin S, AbAziz A, Kamaruddin NA
    Med Princ Pract, 2015;24(1):96-8.
    PMID: 25428406 DOI: 10.1159/000369021
    OBJECTIVE: The aim of this case study is to emphasize the importance of α-blockade in managing a rare complication of an untreated pheochromocytoma.

    CLINICAL PRESENTATION AND INTERVENTION: A 41-year-old man with previous bilateral pheochromocytoma presented with chest pain. He was suffering from cardiac failure and persistent hypotension requiring an inotrope. Cardiac markers, an electrocardiogram and an echocardiogram confirmed acute myocardial infarct with poor ejection fraction and global hypokinesia. An (18)F-fluorodeoxyglucose PET/CT scan showed progressive left suprarenal and organ of Zuckerkandl pheochromocytomas. Blood pressure stabilisation proved challenging but was achieved by titrating an incremental dose of α-blocker against a tapering inotropic dose.

    CONCLUSION: This case showed the efficacy of an α-blocker despite persistent hypotension in a patient with pheochromocytoma-induced cardiomyopathy.

    Matched MeSH terms: Prazosin/administration & dosage*
  13. Hyperthermic effects of Durio zibethinus and its interaction with paracetamol
    Chua YA, Nurhaslina H, Gan SH
    Methods Find Exp Clin Pharmacol, 2008 Dec;30(10):739-43.
    PMID: 19271022 DOI: 10.1358/mf.2008.30.10.1316830
    Because durian (Durio zibethinus), which is known in Southeast Asia as "the king of fruits", is thought to have special body-warming properties, it should not be consumed with paracetamol due to a risk of toxic effects. The claim of warming properties, however, has not been scientifically proven. This study was conducted to investigate durian's hyperthermic effect and its toxicity when consumed together with paracetamol in rats. Five groups of rats (n=6) were fed with: 1) distilled water (4 ml/250 g), 2) homogenized durian (4 g/250 g), 3) paracetamol solution (2400 mg/kg), 4) durian (4 g/250 g) followed by paracetamol solution (2400 mg/kg), or 5) prazosin solution (15 mg/kg, pregavaged) followed 1 h later by durian (4 g/250 g) and paracetamol solution (2400 mg/kg). Rectal temperature, systolic blood pressure and serum alanine aminotransferase (ALT) levels were taken from each rat at baseline and after the various administrations at 1, 2 and 5 h. Our results showed that the body temperature of rats in the durian-treated group was not significantly elevated when compared to the control. However, there was a significant decrease in body temperature over time in animals from groups 4 and 5. We did not, however, observe a consistent pattern of blood pressure change. Serum chemical analysis for ALT also did not show any significant change in any of the groups. In conclusion, contrary to what some believe, even though durian was found to increase body temperature in some rats, this increment was not significant. Rats receiving the durian-paracetamol combination showed a significant drop in body temperature, which may explain the belief that the two mixtures are toxic. However, the exact mechanism of toxicity is still unknown.
    Matched MeSH terms: Prazosin/pharmacology
  14. Fulltext Elucidation of prazosin biodegradation by isolated Bacillus spp. from the tropical environment
    Mohd Mohsi NF, Apandi A, Megat Mohd Noor MJ, Md Akhir FN, Sugiura N, Utsumi M, et al.
    J Gen Appl Microbiol, 2020 Apr 13;66(1):8-14.
    PMID: 31281138 DOI: 10.2323/jgam.2019.04.001
    Prazosin (PRZ), a drug used to treat hypertensive patients, is an emergent contaminant in water systems. PRZ is an alpha-adrenergic receptor blocker used to treat anxiety, and is believed to reach the environment through human excretion, irresponsible disposal of unused medicine, and waste products from manufacturing plants. The purpose of this research was to isolate and characterize potential microbes for PRZ biodegradation and to identify the degradation pathway. After screening, isolated strain STP3 showed a capability for PRZ degradation and was chosen for further analysis. Resting cell assays with PRZ were conducted to identify the intermediate metabolites formed from biodegradation by Fourier transform ion cyclotron resonance mass spectrometer (FT-ICR MS) analysis. Two metabolites degraded from PRZ by STP3 were successfully found, and as these metabolites are derived from the main structure of PRZ, their presence proved PRZ degradation. Draft genome sequencing analysis of STP3 was performed to identify potential enzymes for PRZ biodegradation based on the metabolites found.
    Matched MeSH terms: Prazosin
  15. Fulltext Data on the mechanisms of antidiarrhoeal activity of methanol leaf extract of Combretum hypopilinum Diels (Combretaceae): Involvement of opioidergic and (α1 and β)-adrenergic pathways
    Ahmad MH, Zezi AU, Anafi SB, Alhassan Z, Mohammed M, Danraka RN
    Data Brief, 2021 Jun;36:107155.
    PMID: 34041327 DOI: 10.1016/j.dib.2021.107155
    This article describes the dataset for the elucidation of the possible mechanisms of antidiarrhoeal actions of methanol leaves extract of Combretum hypopilinum (Diels) Combretaceae in mice. The plant has been used in traditional medicine to treat diarrhoea in Nigeria and other African countries. We introduce the data for the antidiarrhoeal activity of the methanol leaf extract of Combretum hypopilinum at 1,000 mg/kg investigated using charcoal meal test in mice with loperamide (5 mg/kg) as the standard antidiarrhoeal agent. To elucidate the possible mechanisms of its antidiarrhoeal action, naloxone (2 mg/kg), prazosin (1 mg/kg), yohimbine (2 mg/kg), propranolol (1 mg/kg), pilocarpine (1 mg/kg) and isosorbide dinitrate (150 mg/kg) were separately administered to different groups of mice 30 minutes before administration of the extract. Each mouse was dissected using dissecting set, and the small intestine was immediately removed from pylorus to caecum, placed lengthwise on moist filter paper and measured the distance travelled by charcoal relative to the length of the intestine using a calibrated ruler in centimetre. Besides, the peristaltic index and inhibition of charcoal movement of each animal were calculated and recorded. The methods for the data collection is similar to the one used to investigate the possible pathways involved in the antidiarrhoeal action of Combretum hypopilinum in mice in the research article by Ahmad et al. (2020) "Mechanisms of Antidiarrhoeal Activity of Methanol Leaf Extract of Combretum hypopilinum Diels (Combretaceae): Involvement of Opioidergic and (α1 and β)-Adrenergic Pathways" (https://doi.org/10.1016/j.jep.2020.113750) [1]. Therefore, this datasets could form a basis for in-depth research to elucidate further the pharmacological properties of the plant Combretum hypopilinum and its bioactive compounds to develop standardized herbal product and novel compound for management of diarrhoea. It could also be instrumental for evaluating the plant's pharmacological potentials using other computational-based and artificial intelligence approaches, including predictive modelling and simulation.
    Matched MeSH terms: Prazosin
  16. Fulltext Cost-effectiveness of antihypertensive treatment in Malaysia
    Qais Alefan, M. Izham M. Ibrahim, Tariq Abdul Razak, Azizi Ayub
    Malaysian Journal of Pharmaceutical Science, 2009;7(2):137-152.
    MyJurnal
    Hypertension is a prevalent chronic disease, which is strongly related to the development of cerebrovascular and cardiovascular diseases. The prevalence of hypertension in Malaysia in subjects aged 15 years and above was estimated to be 27.8%. Cost-effectiveness analysis (CEA) compares treatment options with different effectiveness and safety profiles. The utilisation of antihypertensive drugs has raised some concerns about the balance between its costs and benefits. This study was conducted to describe the healthcare costs for hypertensive subjects and to examine the cost-effectiveness of different classes of antihypertensive drugs used in Malaysia. Retrospective and prospective data analysis of a cohort of uncomplicated hypertensive patients was conducted to determine ambulatory health care costs among hypertensive patients groups. The total direct and
    indirect costs of controlled and uncontrolled blood pressure (BP) were described. The health care
    costs ($) / clinical outcome (AC/E ratio) was calculated. Mean total direct costs per patient per month was higher in uncontrolled blood pressure groups compared to the controlled blood pressure groups. The cost-effectiveness relationship was more favourable for diuretics (1.9), angiotensin converting enzyme inhibitors (ACEIs) (2.0), prazosin (2.4) and beta blockers (2.5), more than the diuretics and beta blockers combination theraphy (3.0), calcium channel blockers (CCBs) (3.4) and other combinations (6.1). Antihypertensive drugs used to treat hypertensive patients were different
    in their cost-effectiveness ratios. Such results will allow health care professionals and/or decision
    makers to make better decisions on how to select treatment options for hypertensive patients in
    Malaysia and how to distribute and allocate scarce health care resources. Pharmacoeconomic
    evaluations can help in making difficult choices rationally and allocate scarce resources efficiently.
    Matched MeSH terms: Prazosin
  17. Fulltext Involvement of monoaminergic system in the antidepressant-like effect of aqueous extract of Channa striatus in mice
    Saleem AM, Taufik Hidayat M, Jais AM, Fakurazi S, Moklas MA, Sulaiman MR, et al.
    Eur Rev Med Pharmacol Sci, 2013;17(15):2019-22.
    PMID: 23884821
    BACKGROUND: In our previous study, the aqueous extract of Channa striatus (family: Channidae) fillet (AECSF) showed an antidepressant-like effect in mice. However, the mechanism of the antidepressant-like effect is unknown.
    AIM: The objective of this study was to explore the involvement of monoamines in the antidepressant-like effect of AECSF in mice.
    MATERIALS AND METHODS: AECSF was prepared by steaming the fillets of C. striatus. The male ICR mice were pretreated with various monoaminergic antagonists viz., p-chlorophenylalanine (100 mg/kg, i.p.), prazosin (1 mg/kg, i.p.) and yohimbine (1 mg/kg, i.p.), SCH23390 (0.05 mg/kg, s.c.) and sulpiride (50 mg/kg, i.p.) followed by treatment with AECSF and tested in tail suspension test (TST). Two-way ANOVA with Tukey test were used at p < 0.05 for significance.
    RESULTS: The pretreatments with p-chlorophenylalanine, prazosin and yohimbine, but not with SCH23390 and sulpiride, were able to reverse the antidepressant-like effect of AECSF in TST.
    CONCLUSIONS: The antidepressant-like effect of AECSF may be mediated through the serotonergic and noradrenergic systems and not through the dopaminergic system.
    Matched MeSH terms: Prazosin/pharmacology
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