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Adrenergic Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Alfuzosin (Fig. 4.4) has selective antagonistic action on α1 adrenoceptor having analogous selectivity to all the α1 receptor subtypes. Alfuzosin, being a quinazoline derivative performs its activity on α1 adrenoceptor by competitive binding there by alleviating the prostatic smooth muscles, rendering it useful in treating BPH but not preferred in treating hypertension (Brunton et al., 2011; Katzung, 2007; Gugger, 2011; Wilde et al., 1993). It shows 64% bioavailability succeeding oral administration. Literature reports the protein binding of alfuzosin to be 90% accompanied by a Vd of 2.5 L/kg. It is contraindicated by CYP3A4 inhibitors like clarithromycin, ketoconazole, ritonavir and so on due to CYP3A4 metabolism. Only 11% of alfuzosin is eliminated unaltered in urine; about 75–91% of metabolites remain inert and are eliminated in feces. It has a t½ of 3–5 h (Wilde et al., 1993). Most commonly observed adverse effects were postural hypotension, tachycardia, dizziness, and headache (Jardin A et al., 1991).
The prostate and seminal vesicles
Published in Professor Sir Norman Williams, Professor P. Ronan O’Connell, Professor Andrew W. McCaskie, Bailey & Love's Short Practice of Surgery, 2018
Professor Sir Norman Williams, Professor P. Ronan O’Connell, Professor Andrew W. McCaskie
Alfuzosin (2.5 mg b.d. to t.d.s., to a total maximum of 10 mg/ day), doxazosin (1 mg nocte, up to a maximum of 8 mg/day), indoramin (20 mg b.d., increased to a total maximum of 100 mg/day in divided doses), prazosin (500 mg b.d., maintenance up to 2 mg/day) and terazosin (1 mg nocte, to a total maximum of 10 mg/day), can be very useful, causing relaxation of the bladder neck. These drugs are not target specific, and patients must be warned of the possibility of postural hypotension, which is usually limited to the first few doses. They can be safely used in combination with anticholinergics to minimise the symptoms of bladder overactivity associated with BOO.
Saquinavir
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Matthew D. M. Rawlins, Martyn A. French
Alfuzosin and tamsulosin, alpha-blockers used for the treatment of benign prostatic hypertrophy, are both metabolized by CYP3A4 and combining them with saquinavir will increase adverse effects such as hypotension. Alfuzosin should not be used with saquinavir and tamsulosin should be used only with extreme caution (Roche, product information).
Alfuzosin hydrochloride-loaded low-density gastroretentive sponges: development, in vitro characterization and gastroretentive monitoring in healthy volunteers via MRI
Published in Pharmaceutical Development and Technology, 2020
Marwa Farrag Abd El-Aziz, Soha Ismail, Mina Ibrahim Tadros, Mohamed Ahmed Elnabarawi
Alfuzosin HCl (ALF) is an FDA approved selective alpha 1-adrenergic-receptor blocker. It is used for the treatment of benign prostate hyperplasia (BPH). It acts by relaxing the prostate smooth muscles and does not affect the prostate size that in order facilitates urine flow, improves weak urine stream, and decreases urination frequency (Liu and Fassihi 2008). Following oral administration, ALF possesses a short biological half-life of 3.8 h, a narrow absorption window (preferentially absorbed in the proximal part of the small intestine) and has a limited oral bioavailability under fasting conditions (25%); possibly due to the extensive first pass metabolism. Taking into consideration that the presence of food promotes the increase in drug bioavailability to 49%, the development of sustained release ALF-loaded gastroretentive systems like mucoadhesive floating beads (Fahmy 2012), compression-coated floating tablets (Gong et al. 2018), floating pellets (Pagariya and Patil 2013) and in situ gel (Shirguppe et al. 2018) were previously explored to combat these setbacks.
Design and optimization of gastric floating sustained-release mini-tablets of alfuzosin hydrochloride based on a factorial design: in vitro/in vivo evaluation
Published in Drug Development and Industrial Pharmacy, 2018
Ling Gong, Miao Yu, Yanyan Sun, Ying Gao, Tong An, Meijuan Zou, Gang Cheng
Alfuzosin hydrochloride was obtained from Shandong New Time Pharmaceutical Co., Ltd. (Shandong, China). Hydroxypropyl methylcellulose (HPMC K100M) was a gift from Shanghai Colorcon Co., Ltd. (Shanghai, China) and carbopol 971 P was also a gift from Beijing Fengli Jingqiu Pharmaceutical Co., Ltd. (Beijing, China). Sodium bicarbonate (NaHCO3) and stearyl alcohol were obtained from Tianjin Hengxing Chemical Preparation Co., Ltd. (Tianjin, China). Ethylcellulose (EC-N7 PHARM) was provided by Ashland Inc. (Shanghai, China) while anhydrous dicalcium phosphate was a kind gift from Shanghai Chineway Pharmaceutical Technology Co., Ltd. (Shanghai, China). Magnesium stearate (Mg stearate) was obtained from Anhui Shanhe Pharmaceutical Excipients Co., Ltd. (Anhui, China) and 1,1′-dioctadecyl-3,3,3′,3′-tetramethylindotricarbocyanine Iodide (DiR), used as NIRF imaging material, was obtained from Mellon Biological Technology Co., Ltd. (Dalian, China).Terazosin hydrochloride (internal standard) was obtained from Wuhan Shengtianyu Biotechnology Co., Ltd. (Hubei, China). Alfuzosin hydrochloride sustained-release tablets (10 mg, XATRAL®XL) were used as the reference preparation. All other chemicals used were of analytical grade.
Treatment of lower urinary tract symptoms/benign prostatic hyperplasia and erectile dysfunction
Published in The Aging Male, 2018
Aldo E. Calogero, Giovanni Burgio, Rosita A. Condorelli, Rossella Cannarella, Sandro La Vignera
Sildenafil was then studied in combination with an α-blocker in various trials. Sildenafil (25 mg once daily) or tadalafil (10 mg once daily) and the α1-adrenoceptor antagonist alfuzosin (10 mg once daily) for the treatment of LUTS were evaluated. Men with untreated LUTS (and concomitant ED) were randomized to either alfuzosin, sildenafil or tadalafil, or the combination of a α-blocker and a PDE5i. Study endpoints were changes from baseline in IPSS, Qmax, Qave, and residual urine volume. Improvement in IPSS was significant in all treatment arms, but it was more pronounced with the drug combinations. Residual urine volume, Qmax, frequency, and nocturia improved significantly with alfuzosin only and the combination regimen [40]. Improvements in the IPSS and IPSS-QoL were greater with the drug combination. A study evaluated the efficacy of sildenafil citrate (25 mg, four times per week for 8 weeks), tamsulosin (0.4 mg, once daily for 8 weeks) and the combination of both regimens in 60 men presenting with LUTS/BPH [41]. The authors found that the improvements in IPSS, Qmax and post-voiding residual volume (PRV) were significantly more pronounced in those patients who had received the combination therapy than in those who were on sildenafil citrate only. However, treatment with the drug combination did not enhance the improvements in IPSS and voiding symptoms seen in the tamsulosin group.