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Pakistan Journal of Medical Sciences 2022To study the therapeutic effects of combined tamsulosin hydrochloride and terazosin treatment for patients with chronic prostatitis Type-III b.
OBJECTIVES
To study the therapeutic effects of combined tamsulosin hydrochloride and terazosin treatment for patients with chronic prostatitis Type-III b.
METHODS
This study involved 180 patients with chronic prostatitis Type-III b treated between January 2018 and December 2020 conducted at Nanhua Hospital Affiliated to Nanhua University. Patients were randomly divided into two equal groups: one receiving oral terazosin hydrochloride tablets only (control group), and one orally receiving both tamsulosin hydrochloride sustained-release tablets and terazosin hydrochloride tablets (observation group). Outcome measurements included symptom scoring, inflammatory cytokine levels, as well as white blood cell and lecithin body counts in the prostatic fluid.
RESULTS
After 30 days of treatment, the observation group showed greater treatment effectiveness (86.67% vs. 73.33%, P<0.05). QLS, USS, PS, and NIH-CPSI symptom scores were lower in the observation group than the control group (P<0.05). No differences in adverse event distribution and incidence were noted. EPS IL-2 increased more in the observation group, while PGE-2, MIP-1α, and MIP-2 decreased more in the observation group. WBC levels decreased more in the observation group, while lecithin body levels increased more in the observation group.
CONCLUSION
The combination of tamsulosin hydrochloride and terazosin for the treatment of patients with chronic prostatitis Type-III b has a significant effect. This approach reduced patient symptoms, lowered inflammatory biomarkers, and generally improved quality of life. This approach appears to have clinical value worthy of future investigation.
PubMed: 35480502
DOI: 10.12669/pjms.38.3.4931 -
Deutsche Medizinische Wochenschrift... Apr 1998
Review
Topics: Adrenergic alpha-Antagonists; Humans; Hypertension; Male; Prazosin; Prostatic Hyperplasia
PubMed: 9581161
DOI: 10.1055/s-0029-1233226 -
Drug Delivery Dec 2021This study aimed to construct a transdermal iontophoresis delivery system for terazosin hydrochloride (IDDS-TEH), which included a positive and negative electrode...
This study aimed to construct a transdermal iontophoresis delivery system for terazosin hydrochloride (IDDS-TEH), which included a positive and negative electrode hydrogel prescription. Intact guinea pig skin was used as a model for the skin barrier function, and the current intensity, terazosin hydrochloride (TEH) concentration, pH, competitive salt, and transdermal enhancer properties were studied. The blood drug concentration was determined in Sprague-Dawley (SD) rats using HPLC, and the antihypertensive effects of IDDS-TEH were evaluated in spontaneously hypertensive rats (SHRs). The results showed that the steady-state penetration rate of TEH increased (from 80.36 µg·cm·h to 304.93 µg·cm·h), followed by an increase in the current intensity (from 0.10 mA·cm to 0.49 mA·cm). The pH values also had a significant influence on percutaneous penetration. The blood concentration of IDDS-TEH was significantly higher ( < .05) than with passive diffusion, which could not be detected. The main pharmacokinetic parameters of the high current group (0.17 mA·cm) and the low current group (0.09 mA·cm) were AUC: 5873.0 ng·mL·h and 2493.7 ng·mL·h, respectively. Meanwhile, the pharmacodynamic results showed that IDDS-TEH significantly decreased the blood pressure of SHRs compared with the TEH hydrogel without loading current. Therefore, TEH could be successfully delivered by the transdermal iontophoresis system and , and further clinical studies should be explored to develop a therapeutically useful protocol.
Topics: Administration, Cutaneous; Adrenergic alpha-1 Receptor Antagonists; Animals; Antihypertensive Agents; Area Under Curve; Blood Pressure; Chromatography, High Pressure Liquid; Drug Delivery Systems; Female; Guinea Pigs; Hypertension; Iontophoresis; Male; Prazosin; Rats; Rats, Inbred SHR; Rats, Sprague-Dawley; Skin Absorption
PubMed: 33620010
DOI: 10.1080/10717544.2021.1889719 -
Archivos Espanoles de Urologia Oct 2023This study aimed to explore the effect of terazosin hydrochloride combined with interventional embolisation on prostate volume and quality of life (QOL) of elderly...
OBJECTIVE
This study aimed to explore the effect of terazosin hydrochloride combined with interventional embolisation on prostate volume and quality of life (QOL) of elderly patients with prostatic hyperplasia (PH).
METHODS
The clinical data of 175 elderly patients with PH admitted to Central Hospital Affiliated to Shandong First Medical University from July 2020 to July 2022 were selected for retrospective analysis. Based on different treatment regimens, 89 patients who received interventional embolisation alone were included in the control group (CG), and 86 patients undergoing interventional embolisation combined with terazosin hydrochloride were included in the study group (SG). The prostate volume, serum indicators, adverse reactions and QOL of the two groups before and after treatment were compared between the two groups.
RESULTS
Before treatment, no significant difference in 36-item short-form health survey (SF-36) scores, serum tumour necrosis factor-α (TNF-α) and prostate-specific antigen (PSA) was observed in both groups ( > 0.05). After treatment, the SF-36 score in the SG was 78.20 ± 6.84 points, which was significantly higher than that in the CG (72.67 ± 5.94 points). In addition, the SG had remarkably lower residual urine volume and prostate volume, higher maximum flow rate and lower TNF-α and PSA levels compared with the CG ( < 0.05). The adverse reaction rate of the SG was only 4.65%, which was significantly lower than that of the CG (14.61%, < 0.05).
CONCLUSIONS
Terazosin hydrochloride combined with interventional embolisation overtly reduces the prostate volume and improves the clinical symptoms of patients with fewer side effects, which has a certain clinical application value.
Topics: Aged; Humans; Male; Adrenergic alpha-Antagonists; Prostate; Prostate-Specific Antigen; Prostatic Hyperplasia; Quality of Life; Retrospective Studies; Treatment Outcome; Tumor Necrosis Factor-alpha; Embolization, Therapeutic; Urological Agents
PubMed: 37960955
DOI: 10.56434/j.arch.esp.urol.20237608.70 -
The American Journal of Medicine May 1986Terazosin is a quinazoline antihypertensive agent that is chemically similar to prazosin. The saturated furan ring of terazosin distinguishes these two compounds.... (Comparative Study)
Comparative Study
Terazosin is a quinazoline antihypertensive agent that is chemically similar to prazosin. The saturated furan ring of terazosin distinguishes these two compounds. Terazosin (0.1 to 3.0 mg/kg) lowered blood pressure without increasing heart rate when given orally to spontaneously hypertensive rats. No tolerance was observed during five days of repeated oral administration. Although equally efficacious in spontaneously hypertensive rats as its congener prazosin, terazosin exhibited a more gradual onset of action than prazosin, a more uniform and linear dose-response curve, and a less variable duration of action. When administered intravenously to dogs, terazosin lowered blood pressure primarily by decreasing peripheral vascular resistance. Pretreatment with phenoxybenzamine but not with atropine or propranolol resulted in a greatly reduced hypotensive response to terazosin, demonstrating that this effect of terazosin is mediated by a sympatholytic mechanism of the alpha type. The nature of the alpha-blocking properties of terazosin was evaluated in vitro using both radioligand binding studies and functional tests in rabbit aorta and pulmonary artery. These studies demonstrated that terazosin is highly selective for alpha1 receptors. The affinity for alpha1 receptors was approximately one-third that of prazosin. Like prazosin, terazosin displayed minimal interaction with alpha2 receptors. Median lethal dose values in rats ranged from 0.255 to 0.270 g/kg for intravenous administration and from 5.5 to 6.0 g/kg, for oral administration. Oral administration of high doses of the compound to rats did not produce any gastrointestinal irritation and/or apparent abnormal behavioral effects. Comparison of the oral activity of terazosin in spontaneously hypertensive rats with the oral toxicity values in normal rats revealed a high efficacy/safety ratio. Terazosin given intravenously to rats and mice was 2.6 to 5.0 times less toxic than prazosin. The absorption of terazosin appeared to be slower than that of prazosin in rats. However, from eight to 16 hours after dosing, terazosin concentrations in plasma exceeded those of prazosin, suggesting the possibility of once-daily dosing with terazosin. In addition, terazosin exhibited statistically significant cholesterol lowering effects in gerbils.
Topics: Administration, Oral; Adrenergic alpha-Antagonists; Animals; Blood Pressure; Chemical Phenomena; Chemistry; Dogs; Dose-Response Relationship, Drug; Female; Gerbillinae; Hemodynamics; Hypertension; Lipoproteins; Male; Piperazines; Prazosin; Rabbits; Rats; Rats, Inbred Strains
PubMed: 2872801
DOI: 10.1016/0002-9343(86)90846-6 -
The American Journal of Medicine May 1986The pharmacokinetics of terazosin have been assessed in human volunteers, hypertensive patients, a limited number of elderly volunteers, and a small number of patients... (Comparative Study)
Comparative Study
The pharmacokinetics of terazosin have been assessed in human volunteers, hypertensive patients, a limited number of elderly volunteers, and a small number of patients with congestive heart failure. Terazosin was administered intravenously and orally in doses ranging up to 7.5 mg. Following intravenous administration, the disposition of terazosin is characteristic of a two-compartment, open model that is linear and independent of dose. Orally administered terazosin is rapidly, consistently, and almost completely absorbed into the bloodstream. Peak plasma drug levels occur within one to two hours after ingestion. Approximately 90 to 94 percent of the drug is bound to plasma proteins, with the volume of distribution estimated to be 25 to 30 liters. Terazosin undergoes extensive hepatic metabolism, and the major route of elimination is via the biliary tract. Small amounts of terazosin are excreted in the urine. Plasma and renal clearances are 80 and 10 ml per minute, respectively. The mean beta-phase half-life is approximately 12 hours. The pharmacokinetics of terazosin were not influenced by age, congestive heart failure, or hypertension (other than plasma clearance). In contrast to prazosin, terazosin is completely and consistently bioavailable and has a half-life that is three to four times longer than that of prazosin. The prolonged half-life of terazosin allows once-daily dosing, which may facilitate patient compliance with drug therapy for hypertension.
Topics: Administration, Oral; Adrenergic alpha-Antagonists; Aged; Animals; Blood Proteins; Chemical Phenomena; Chemistry; Female; Half-Life; Heart Failure; Humans; Hypertension; Infusions, Parenteral; Kinetics; Liver; Male; Middle Aged; Piperazines; Prazosin; Protein Binding; Rats
PubMed: 2872802
DOI: 10.1016/0002-9343(86)90847-8 -
International Journal of Clinical... Jan 2022This study was conducted to assess the pharmacokinetic and safety profiles between a new oral formulation of terazosin hydrochloride capsule compared with the brand-name... (Randomized Controlled Trial)
Randomized Controlled Trial
OBJECTIVE
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.
MATERIALS AND METHODS
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.
RESULTS
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.
CONCLUSION
The test and reference formulations of terazosin were bioequivalent and well tolerated under both fasting and fed conditions.
Topics: Area Under Curve; China; Chromatography, Liquid; Cross-Over Studies; Fasting; Healthy Volunteers; Humans; Prazosin; Tablets; Tandem Mass Spectrometry; Therapeutic Equivalency
PubMed: 34672254
DOI: 10.5414/CP204018 -
International Journal of Molecular... Dec 2021Gastrointestinal disease is the most common health concern that occurs due to environmental, infectious, immunological, psychological, and genetic stress. Among them,...
Gastrointestinal disease is the most common health concern that occurs due to environmental, infectious, immunological, psychological, and genetic stress. Among them, the most frequent diseases are gastric ulcer (GU) and ulcerative colitis (UC). DSS-induced UC and ethanol-stimulated GU models resemble the pathophysiology of human gastrointestinal disease. The current study was designed to explore the anti-oxidation, anti-inflammation, anti-cell death properties of terazosin, an α-adrenergic receptor antagonist, in vivo and in vitro. Our results indicate that terazosin dramatically activates Pgk1, and upregulates glycose metabolism, evidenced by the enhanced ATP production and higher LDH enzymatic activity. Also, terazosin significantly enhances p-AKT expression and inhibits NF-κB p65 activation through abrogating the phosphorylation of IKBα, as well as lowers Caspase-1 and GSDMD expression. The findings in this study demonstrate that terazosin exhibits anti-inflammatory effects by downregulating NF-κB-GSDMD signal pathway, along with enhancing glycolysis for gastrointestinal disease treatment. Meanwhile, we also find terazosin ameliorates ethanol-induced gastric mucosal damage in mice. Collectively, as a clinical drug, terazosin should be translated into therapeutics for gastrointestinal disease soon.
Topics: Apoptosis; Caco-2 Cells; Cell Survival; Colitis; Cytokines; Deoxyglucose; Dextran Sulfate; Gastric Mucosa; Gastrointestinal Diseases; Glucose; Humans; Hydrogen Peroxide; Inflammation Mediators; Lactic Acid; Malondialdehyde; Models, Biological; Peroxidase; Phosphoglycerate Kinase; Prazosin; Pyroptosis; Stomach Ulcer; Superoxide Dismutase
PubMed: 35008842
DOI: 10.3390/ijms23010416 -
Advanced Pharmaceutical Bulletin 2013Thermal analysis (TGA, DTG and DTA) and differential scanning calorimetry (DSC) have been used to study the thermal behavior of terazosin hydrochloride (TER).
PURPOSE
Thermal analysis (TGA, DTG and DTA) and differential scanning calorimetry (DSC) have been used to study the thermal behavior of terazosin hydrochloride (TER).
METHODS
Thermogravimetric analysis (TGA/DTG), differential thermal analysis (DTA) and differential scanning calorimetry (DSC) were used to determine the thermal behavior and purity of the used drug. Thermodynamic parameters such as activation energy (E*), enthalpy (∆H*), entropy (∆S*) and Gibbs free energy change of the decomposition (∆G*) were calculated using different kinetic models.
RESULTS
The purity of the used drug was determined by differential scanning calorimetry (99.97%) and specialized official method (99.85%) indicating to satisfactory values of the degree of purity. Thermal analysis technique gave satisfactory results to obtain quality control parameters such as melting point (273 ºC), water content (7.49%) and ash content (zero) in comparison to what were obtained using official method: (272 ºC), (8.0%) and (0.02%) for melting point, water content and ash content, respectively.
CONCLUSION
Thermal analysis justifies its application in quality control of pharmaceutical compounds due to its simplicity, sensitivity and low operational costs. DSC data indicated that the degree of purity of terazosin hydrochloride is similar to that found by official method.
PubMed: 24312828
DOI: 10.5681/apb.2013.025 -
The Cochrane Database of Systematic... 2002Lower urinary tract symptoms associated with benign prostatic obstruction (BPO) occur in up to 70% of men over the age of 60 years. To relieve these bothersome symptoms,... (Meta-Analysis)
Meta-Analysis Review
BACKGROUND
Lower urinary tract symptoms associated with benign prostatic obstruction (BPO) occur in up to 70% of men over the age of 60 years. To relieve these bothersome symptoms, treatment options include alpha-antagonists, also know as alpha-blockers.
OBJECTIVES
We conducted a systematic review to evaluate the effectiveness and adverse effects of the alpha-blocker, terazosin, for treatment of urinary symptoms associated with BPO.
SEARCH STRATEGY
Trials were searched in computerized general and specialized databases (MEDLINE, Cochrane Library), by checking bibliographies, and by contacting manufacturers and researchers.
SELECTION CRITERIA
Studies were included if they (1) were randomized trials of at least 1 month duration, and (2) included men with symptomatic BPO and compared terazosin with placebo or active controls.
DATA COLLECTION AND ANALYSIS
Study, patient characteristics and outcomes data were extracted in duplicate onto standardized forms utilizing a prospectively developed protocol. The main outcome measure for comparing the effectiveness of terazosin with placebo or other BPO medications was change in urological symptoms as measured by validated symptom scores. Secondary outcomes included urodynamic measures. The main outcome measure for adverse effects was the number of men reporting side effects. We also evaluated the number of men withdrawing from treatment and the number withdrawing due to adverse effects.
MAIN RESULTS
17 studies involving 5,151 subjects met inclusion criteria (placebo-controlled (10); alpha-blockers (7); finasteride alone or in combination with terazosin as well as placebo (1); microwave therapy (TUMT) (1). Study duration ranged from 4-52 weeks. Mean age was 65 years and 82% of men were white. Baseline urologic symptom scale scores and flow rates demonstrated that men had moderate BPO. Efficacy outcomes were rarely reported in a fashion that allowed for data pooling but indicated that terazosin improved symptom scores and flow rates more than placebo or finasteride and similarly to other alpha antagonists. The pooled mean percentage improvements for the Boyarsky symptom score was 37% for terazosin versus 15% for placebo (n=4 studies). The mean percentage improvement for the American Urological Association symptom score (AUA) was 38% compared to 17% and 20% for placebo and finasteride, respectively (n = 2 studies). The pooled mean improvement in the International Prostate Symptom Score (IPSS) (40%) was similar to tamsulosin (43%). Peak urine flow rates improved greater with terazosin (22%), than placebo (11%) and finasteride (15%) but did not differ significantly from the other alpha-blockers. The percentage of men discontinuing terazosin was comparable to men receiving placebo and finasteride but was greater then with other alpha-antagonists. Adverse effects were greater than placebo and included dizziness, asthenia, headache and postural hypotension.
REVIEWER'S CONCLUSIONS
The available evidence suggests that terazosin improves urinary symptoms and flow measures associated with BPO. Effectiveness is superior to placebo or finasteride, similar to other alpha-blockers but less than TUMT. Adverse effects were generally mild but more frequent than other alpha-blockers and associated with between a two-four fold increase in treatment discontinuation.
Topics: Adrenergic alpha-Antagonists; Aged; Antineoplastic Agents; Humans; Male; Middle Aged; Prazosin; Prostatic Hyperplasia
PubMed: 12519611
DOI: 10.1002/14651858.CD003851