Terazosin

Terazosin is an antagonist of α1-adrenergic receptor [1].

Terazosin is a long acting and selective α1-adrenergic-antagonist drug. The major use of it is the treatment for benign prostatic hyperplasia since it can relax the prostatic smooth muscle. Terazosin is proved to be a safe and effective treatment and has few adverse effects [1].

Besiedes, terazosin is also used to treat for hypertension. It is found to significantly decrease blood pressure in patients with uncomplicated hypertension. It is also found to effect blood lipids beneficially. Terazosin modestly lowers blood total cholesterol, low density lipoprotein cholesterol and triglycerides as well as increases high density lipoprotein. The beneficial effects make terazosin more potent to prevent coronary heart disease [2].

References:
[1] Lepor H, Williford W O, Barry M J, et al. The efficacy of terazosin, finasteride, or both in benign prostatic hyperplasia. New England Journal of Medicine, 1996, 335(8): 533-540.
[2] Grimm R H. alpha 1-antagonists in the treatment of hypertension. Hypertension, 1989, 13(5 Suppl): I131.

Highly Sensitive Fluorescence Methods for the Determination of Alfuzosin, Doxazosin, Terazosin and Prazosin in Pharmaceutical Formulations, Plasma and Urine.[Pubmed:27396658]

Anal Sci. 2016;32(7):763-8.

Polymeric ionic liquid-coated magnetic nanoparticles have been successfully prepared as adsorbents for the magnetic solid-phase extraction of four drugs, namely alfuzosin, doxazosin, Terazosin and prazosin, from pharmaceutical preparations, urine samples and plasma samples. The four drugs were detected by fluorescence spectrophotometer. Several extraction parameters, including the pH of the solution; the type, ratio and volume of the desorbing reagent; the amount of adsorbent; the time of the extraction and desorption processes; and the addition of NaCl, were investigated and optimized. Linear responses were determined for the four drugs in the concentration range of 0.5 - 45 ng mL(-1). The limit of detection values for alfuzosin, doxazosin, Terazosin and prazosin, which were defined as three times the standard deviation of a blank sample, were determined to be 0.035, 0.034, 0.027 and 0.028 ng mL(-1) (n = 11), respectively. Furthermore, this new method gave preconcentration factors of 114.5, 111.3, 111.1 and 108.5 for these four drugs.

Renewal of an old European Pharmacopoeia method for Terazosin using modeling with mass spectrometric peak tracking.[Pubmed:27987393]

J Pharm Biomed Anal. 2017 Feb 20;135:8-15.

An older method for Terazosin was reworked in order to reduce the analysis time from 90min (2x45min) to below 5min. The method in European Pharmacopoeia (Ph.Eur.) investigates the specified impurities separately. The reason of the different methods is that the retention of two impurities is not adequate in reversed phase, not even with 100% water. Therefore ion-pair-chromatography has to be applied and since that two impurities absorb at low UV-wavelength they had to be analyzed by different method than the other specified impurities. In our new method we could improve the retention with pH elevation using a new type of stationary phases available for high pH applications. Also a detection wavelength could be selected that is appropriate for the detection and quantification of all impurities. The method development is the bottleneck of liquid chromatography even today, when more and more fast chromatographic systems are used. Expert knowledge with intelligent programs is available to reduce the time of method development and offer extra information about the robustness of the separation. Design of Experiments (DoE) for simultaneous optimization of gradient time (tG), temperature (T) and ternary eluent composition (tC) requires 12 experiments. A good alternative way to identify a certain peak in different chromatograms is the molecular mass of the compound, due to its high specificity. Liquid Chromatography-Mass Spectrometry (LC-MS) is now a routine technique and increasingly available in laboratories. In our experiment for the resolution- and retention modeling the DryLab4 method development software (Version 4.2) was used. In recent versions of the software the use of (m/z)-MS-data is possible along the UV-peak-area-tracking technology. The modelled and measured chromatograms showed excellent correlations. The average retention time deviations were ca. 0.5s and there was no difference between the predicted and measured Rs,crit -values.

Utility of Hantzsch reaction for development of highly sensitive spectrofluorimetric method for determination of alfuzosin and terazosin in bulk, dosage forms and human plasma.[Pubmed:28303653]

Luminescence. 2017 Sep;32(6):1066-1071.

A highly sensitive, cheap, simple and accurate spectrofluorimetric method has been developed and validated for the determination of alfuzosin hydrochloride and Terazosin hydrochloride in their pharmaceutical dosage forms and in human plasma. The developed method is based on the reaction of the primary amine moiety in the studied drugs with acetylacetone and formaldehyde according to the Hantzsch reaction, producing yellow fluorescent products that can be measured spectrofluorimetrically at 480 nm after excitation at 415 nm. Different experimental parameters affecting the development and stability of the reaction products were carefully studied and optimized. The fluorescence-concentration plots of alfuzosin and Terazosin were rectilinear over a concentration range of 70-900 ng ml(-1) , with quantitation limits 27.1 and 32.2 ng ml(-1) for alfuzosin and Terazosin, respectively. The proposed method was validated according to ICH guidelines and successfully applied to the analysis of the investigated drugs in dosage forms, content uniformity test and spiked human plasma with high accuracy.

Myocardial infarction induced by oral terazosin in a patient with predisposing structural cardiomyopathy: case report.[Pubmed:27392141]

Medwave. 2016 Jun 28;16(5):e6480.

We describe a 71-year-old male patient who developed acute myocardial infarction (AMI) due to a dynamic left ventricular outflow tract obstruction induced by Terazosin. After receiving Terazosin, the patient had a syncope followed by angina. The electrocardiogram showed Q waves and ST segment elevation in the precordial and inferior leads. Coronary angiography evidenced a chronically occluded left anterior descending artery. Doppler-echocardiography revealed apical akinesia, hyperdynamic basal segments, systolic anterior motion of the mitral valve (SAM) and dynamic left ventricular outflow tract obstruction. Therapy with intravenous fluids and atenolol resulted in marked clinical improvement. Acute myocardial infarction resulted from low coronary perfusion pressure in a patient with a chronically diminished coronary reserve.

Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.

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