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102
result(s) for
"Prazosin - analogs "
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Bioequivalence study of two formulations of terazosin hydrochloride capsule in healthy Chinese subjects under fasting and fed conditions
by
Zhang, Pei-Wen
,
Mai, Gang
,
Gan, Chun-Yan
in
Adrenergic receptors
,
Area Under Curve
,
Bioequivalence
2022
This study was conducted to assess the pharmacokinetic and safety profiles between a new oral formulation of terazosin hydrochloride capsule compared with the brand-name drug.
A randomized, open-label, single-dose, 2-period crossover study under fasting or fed conditions was conducted in healthy Chinese subjects. 24 individuals were selected, respectively. Each subject was randomized at the beginning to receive a 2-mg capsule of the test or the reference terazosin during the first period and then received the alternate formulation during the second period following a 1-week washout period. Blood samples were collected at pre-dose and up to 60 hours after administration. Plasma terazosin was quantified by a validated LC-MS/MS method.
48 healthy subjects were enrolled, and 47 completed the study. C
, AUC
, and AUC
were similar and the 90% CIs for the geometric mean ratios of these parameters between the two groups were all bounded within the predefined bioequivalence criterion of 80 - 125% under both fasting and fed conditions. Throughout the study period, a total of 30 treatment-emergent adverse events (TEAEs) were reported under fasting condition. 35 TEAEs were observed under fed conditions. No serious adverse event was observed.
The test and reference formulations of terazosin were bioequivalent and well tolerated under both fasting and fed conditions.
Journal Article
Efficacy of combination terazosin and nifedipine therapy in postoperative treatment of distal ureteral stones after transurethral ureteroscopic lithotripsy
2020
Objective
To investigate the efficacy of combination terazosin and nifedipine therapy in postoperative treatment of distal ureteral stones after transurethral ureteroscopic lithotripsy.
Methods
This prospective single-blinded randomized study enrolled 165 patients undergoing transurethral ureteroscopic lithotripsy in our hospital. Patients were randomized into three groups: control, terazosin, and combination treatment (terazosin and nifedipine). Stone discharge rates and times were recorded, along with side effects and complications. Visual Analogue Scale (VAS) score was used to evaluate pain for 7 days postoperatively. International Prostatic Symptoms Score (IPSS) was used to evaluate prostatic function; quality of life (QOL) was evaluated preoperatively and at 7 days postoperatively.
Results
The stone discharge rate was significantly higher in the combination group than in other groups; moreover, mean discharge time was shorter in the combination group. Beginning at 3 days postoperatively, VAS scores were dramatically lower in the combination group than in other groups; IPSS and QOL scores were also lower in the combination group. Edema recurrence was significantly less common in combination and terazosin groups than in the control group. Side effects were similar among groups.
Conclusion
Combination terazosin and nifedipine therapy was safe and effective in postoperative treatment of distal ureteral stones after transurethral ureteroscopic lithotripsy.
Journal Article
A randomized controlled trial of levofloxacin, terazosin, and combination therapy in patients with category III chronic prostatitis/chronic pelvic pain syndrome
by
Yan, Dongliang
,
Liang, Kuixiang
,
Xu, Zhonghua
in
Administration, Oral
,
Adult
,
Anti-Bacterial Agents - administration & dosage
2016
Objective
To explore the efficacy of levofloxacin, terazosin, and their combination in patients with category III chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS).
Methods
A total of 115 patients with category III CP/CPPS receiving 6-week therapy were randomly divided into the levofloxacin group (
n
= 38), terazosin group (
n
= 38), and combination group (
n
= 39). The primary endpoint was the response rate (i.e., the change from baseline) in the total and domain scores of the National Institutes of Health Chronic Prostatitis Symptom Index (NIH-CPSI). Secondary endpoints were expressed as prostatic secretion-white blood cell (EPS-WBC) and International Index of Erectile Function-5 (IIEF-5).
Results
After 6 weeks, the response rate of NIH-CPSI scores was 45.1, 22.4, and 50.0 % in the levofloxacin group, terazosin group, and combination group, respectively. Furthermore, no significant difference in NIH-CPSI scores was observed between IIIA and IIIB patients in each arm. Levofloxacin alone or levofloxacin plus terazosin could significantly reduce EPS-WBC counts compared with terazosin alone. Finally, no significant difference was found between the three arms in terms of IIEF-5 scores.
Conclusion
A 6-week short-term treatment of levofloxacin or levofloxacin plus terazosin was more effective than terazosin alone in patients with category III CP/CPPS. Furthermore, levofloxacin treatment was not different from levofloxacin plus terazosin treatment in terms of treatment effect.
Journal Article
Enhancing glycolysis attenuates Parkinson’s disease progression in models and clinical databases
by
Fernandez-Carasa, Irene
,
Raya, Angel
,
Su, Wenting
in
Adenosine Triphosphate - metabolism
,
Aged
,
Aged, 80 and over
2019
Parkinson's disease (PD) is a common neurodegenerative disease that lacks therapies to prevent progressive neurodegeneration. Impaired energy metabolism and reduced ATP levels are common features of PD. Previous studies revealed that terazosin (TZ) enhances the activity of phosphoglycerate kinase 1 (PGK1), thereby stimulating glycolysis and increasing cellular ATP levels. Therefore, we asked whether enhancement of PGK1 activity would change the course of PD. In toxin-induced and genetic PD models in mice, rats, flies, and induced pluripotent stem cells, TZ increased brain ATP levels and slowed or prevented neuron loss. The drug increased dopamine levels and partially restored motor function. Because TZ is prescribed clinically, we also interrogated 2 distinct human databases. We found slower disease progression, decreased PD-related complications, and a reduced frequency of PD diagnoses in individuals taking TZ and related drugs. These findings suggest that enhancing PGK1 activity and increasing glycolysis may slow neurodegeneration in PD.
Journal Article
Symptomatic comparison in efficacy on patients with benign prostatic hyperplasia treated with two therapeutic approaches
by
Wang, Yongyan
,
Lu, Aiping
,
Li, Shao
in
Aged
,
Antineoplastic Agents - standards
,
Antineoplastic Agents - therapeutic use
2010
A randomised controlled trial was performed to compare the symptomatic effects on patients with benign prostatic hyperplasia (BPH) treated by two therapeutic approaches – the Western medicine (WM) and traditional Chinese medicine (TCM).
Four primary outcome measures, namely the quality of life (QOL), maximum urine flow ratio (UFR), International Prostate Symptom Score (IPSS) and prostate volumes, as well as four urethra-related and 35 non-urethra-related symptoms, were investigated to evaluate the effects on 31 BPH patients subjected to WM (Terazosin Hydrochloride Hytrin, THH) and 30 cases to TCM (herbal
Saxifrage tablet, HST). The effects of both treatments are compared by the two-sample Kolmogorov–Smirnov test. The contributions of symptoms for four assessments are analysed by the logistic regression model and the Chow test.
The effect of TCM is weaker than that of WM in the assessment of the IPSS score (
p
<
0.05), and both treatments are similar in the prostate volumes, the maximum UFR and the QOL assessments (
p
>
0.05), as well as in the effective number of urethra-related or non-urethra-related symptoms before and after treatment (
p
>
0.05). By comparing the linear regression models, different urethra-related and non-urethra-related symptom patterns associated with TCM and WM therapies are detected for four assessments, especially for the prostate volume assessment (
p
<
0.01).
TCM (HST) is a potentially effective treatment in improving the QOL, prostate volumes and maximum UFR for patients with BPH, though it is less effective in ameliorating the IPSS score when compared with WM (THH). The non-urethra-related symptoms experienced by BPH patients might be one of the parameters to further achieve the tailored diagnosis and treatment for BPH.
Journal Article
Effect of low‐dose terazosin on arterial stiffness improvement: A pilot study
2024
Arterial stiffness, a prominent hallmark of ageing arteries, is a predictor of all‐cause mortality. Strategies for promoting healthy vascular ageing are encouraged. Here we conducted a pilot study to evaluate the potential effects of low‐dose Terazosin on arterial stiffness. We enrolled patients aged over 40 with elevated arterial stiffness, defined as a brachial‐ankle pulse wave velocity (baPWV) ≥1400 cm/s, who were administered Terazosin (0.5 and 1.0 mg/day) from December 2020 to June 2023. Treatment responses were assessed every 3 months. Linear regression analysis was used to characterise the improvement. We matched cases who took Terazosin for 1 year with Terazosin‐free controls using propensity score matching (PSM). Our findings demonstrate that Terazosin administration significantly affected arterial stiffness. (1) Arterial stiffness significantly improved (at least a 5% reduction in baPWV) in 50.0% of patients at 3 months, 48.6% at 6 months, 59.3% at 9 months, and 54.4% at 12 months, respectively. (2) Those with higher baseline baPWV and hypertension exhibited a significantly reduced risk of non‐response. (3) Terazosin was associated with a reduction of baPWV at 1‐year follow‐up (linear regression: β = −165.16, p < 0.001). This pilot study offers valuable insights into the potential significance of Terazosin in improving arterial stiffness and paves the way for future randomised clinical trials in combating vascular ageing.
Journal Article
Terazosin in the Treatment of Premature Ejaculation: A Short-term Follow-up
by
Ferhat, Mehmet
,
Yılmaz, Erdal
,
Batislam, Ertan
in
Adrenergic alpha-Antagonists - pharmacology
,
Adrenergic alpha-Antagonists - therapeutic use
,
Adult
2005
The aim of the present study was to evaluate the efficacy of terazosine in patients with premature ejaculation and lower urinary tract symptoms (LUTS), after excluding other sexual disorders and chronic prostatitis.
A total of 90 patients with premature ejaculation and LUTS were enrolled to the study after excluding sexual disorders, prostatitis and benign prostatic hyperplasia. The patients were divided into two groups. Sixty patients in group 1 were treated with terazosine 5 mg daily for a month. Patients were followed monthly and questioned for their ejaculation problem. The results were classified as cure, improvement and ineffective. If patients showed improvement and ineffectiveness, the treatment was continued with 10 mg daily for the following month. Group 2 was included 30 patients, and placebo was applied for a month. At the end of this period, in patients who did not show any improvement, terazosine 10 mg was started.
In the treatment group, at the 1st month follow-up, 21 patients (35%) were cured, 20 (33.3%) showed improvement. In 19 (31.7%) patients, the treatment was ineffective. In group 2, 9 (30%) patients showed improvement and the rest had no-changes after one-month follow up. There was statistically significant difference between two groups (Pearson chi2 test = 0.000). Later, terazosine 10 mg was given to the patients in group 2 and to the patients who showed improvement or unsuccessful result with terazosine 5 mg. With terazosine 10 mg, 10 (14.5%) patients were cured, 29 (42.2%) patients were improved. Finally, terazosine treatment in patients with premature ejaculation was found to be effective in 60 patients (66.7%).
Alpha blockers seem to be physiological medical agents in the treatment of premature ejaculation since ejaculation is under sympathetic control. Moreover, these agents are effective in lower urinary tract and they should be used in patients with premature ejaculation and lower urinary tract symptoms.
Journal Article
Terazosin activates Pgk1 and Hsp90 to promote stress resistance
2015
The α1-adrenergic receptor antagonist terazosin protects flies and mammalian cells from stress and apoptosis through direct activation of the glycolytic enzyme phosphoglycerate kinase 1, which interacts with Hsp90 to promote ATP consumption.
Drugs that can protect against organ damage are urgently needed, especially for diseases such as sepsis and brain stroke. We discovered that terazosin (TZ), a widely marketed α1-adrenergic receptor antagonist, alleviated organ damage and improved survival in rodent models of stroke and sepsis. Through combined studies of enzymology and X-ray crystallography, we discovered that TZ binds a new target, phosphoglycerate kinase 1 (Pgk1), and activates its enzymatic activity, probably through 2,4-diamino-6,7-dimethoxyisoquinoline′s ability to promote ATP release from Pgk1. Mechanistically, the ATP generated from Pgk1 may enhance the chaperone activity of Hsp90, an ATPase known to associate with Pgk1. Upon activation, Hsp90 promotes multistress resistance. Our studies demonstrate that TZ has a new protein target, Pgk1, and reveal its corresponding biological effect. As a clinical drug, TZ may be quickly translated into treatments for diseases including stroke and sepsis.
Journal Article
Effects of branded versus generic terazosin hydrochloride in adults with benign prostatic hyperplasia: A randomized, open-label, crossover study in taiwan
by
Ou, Jiann-Hui
,
Lan, Shih-Kai
,
Tzai, Tzong-Shin
in
Adrenergic alpha-1 Receptor Antagonists
,
Aged
,
Biological and medical sciences
2007
Terazosin is an al-selective adrenoceptor blocking agent that has been reported in many clinical trials to be an effective choice for the treatment of benign prostatic hyperplasia (BPH). To improve cost-effectiveness, the development of an effective and well-tolerated generic formulation is needed.
The aim of this study was to compare the efficacy and tolerability of branded versus generic terazosin hydrochloride in adult patients with symptomatic BPH in Taiwan.
This randomized, open-label, 2-sequence, 2-period crossover study was conducted at the Urological Clinic, National Cheng Kung University Medical Center, Taman, Taiwan. Men newly diagnosed with symptomatic BPH who had not previously received treatment for BPH were recruited between August 2002 and April 2006. Patients were randomly assigned to 1 of 2 treatment sequences. Group A received generic terazosin during period 1 (6 weeks) and branded terazosin in period 2 (6 weeks); group B received the branded drug during period 1 and the generic during period 2. The 2 study periods were separated by a 1-week washout period. All treatments were given by mouth once daily (bedtime) at an initial dosage of 2 mg/d for the first 2 weeks. At the week-2 study visit in each treatment period, the dosage could be increased to 4 mg/d or decreased to 1 mg/d based on each patient's response and experience of adverse effects (AEs), based on the opinion of the investigator. Efficacy variables included the total score on the International Prostate Symptom Scale (IPSS), a 7-item instrument used to assess objective lower urinary tract symptoms, including quality of life. IPSS was measured at baseline and weeks 2 and 6 of each treatment period, and maximal and mean uroflow rates, measured at baseline and week 6. Tolerability was assessed at each time point using physical examination, including vital signs; laboratory analysis; and spontaneous reporting.
Fifty-three patients were randomized; 43 were included in the efficacy analysis (mean [SD] age, group A, 64.5 [7.7] years and group B, 62.9 [8.2] years; mean [SD] weight, group A, 66.4 [7.2] kg and group B, 67.1 [8.9] kg; all patients were Taiwanese). At 2 and 6 weeks, no significant between-product differences were found in mean (SD) decreases from baseline in IPSS total score (generic, 2.46 [0.84] and 2.46 [1.00], respectively; branded, 1.56 [0.60] and 2.87 [0.71]). At week 6, the between-product difference in mean increase from baseline in maximal uroflow rate was nonsignificant (generic, 2.36 [0.90] mL/s; branded, 2.03 [0.62] mL/s). A total of 86 treatment-emergent AEs were reported (45 with the generic drug; 41 with the branded drug), all of which were considered by the investigator as nonserious except for 1 case of acute epididymitis, which occurred with the generic drug. The most common AEs reported with the generic and branded formulations were dizziness (7/48 [14.6%] and 10/50 [20.0%], respectively) and peripheral edema (1/48 [2.1%] and 3/50 [6.0%]). No significant differences in the prevalences of AEs were found between the 2 treatments.
In this group of Taiwanese patients with symptomatic BPH, the efficacy and tolerability of generic terazosin were similar to those of branded terazosin.
Journal Article