scholarly journals The In vitro Effects of Atenolol and Zinc Chloride on the Protein Binding of Amlodipine in Aqueous Medium

1970 ◽  
Vol 7 (1) ◽  
pp. 15-21 ◽  
Author(s):  
Md Shah Amran ◽  
Sheikh Niaz Morshed ◽  
Md Jahangir Alam Khandakar ◽  
Md Masudur Rahman ◽  
Md Mosiur Rahman ◽  
...  

An in vitro study of protein binding has been carried out to observe the influence of atenolol and zinc chloride on the protein binding of amlodipine by equilibrium dialysis method at 37±1 0C and at physiological pH (7.4). It has been found that zinc chloride lowered the affinity and percentage of protein binding of amlodipine to bovine serum albumin but atenolol has no such effect. The Scatchard plots were prepared to reveal the number of binding sites and the affinity for protein binding. It was seen that the highest percentage binding of amlodipine was 91% and the lowest was 74%. In the presence of atenolol, the highest and the lowest value of percentage of protein binding was 90% and 72%, respectively. In the presence of zinc chloride these values were 84% and 65% respectively. It is, thus, inferred that atenolol or its complex with amlodipine has no significant effect on percentage of protein binding of amlodipine. While zinc chloride or its complex with amlodipine can cause a decrease in percentage of protein binding of amlodipine. Complexation of amlodipine with zinc chloride might, therefore, displace the drug from the plasma and the displaced drugs may be redistributed, thus , increasing the free drug in plasma and tissue systems. This may change the pharmacokinetic properties of the drug and may affect the pharmacological and toxic effects. It is thus inferred that care and monitoring must be taken during combination therapy of amlodipine and zinc chloride. Key words: Amlodipine, protein binding, binding site, equilibrium dialysis, Scatchard plot, atenolol, zinc chloride, combination therapy  DOI = 10.3329/dujps.v7i1.1202Dhaka Univ. J. Pharm. Sci. 7(1): 15-21, 2008 (June)

2005 ◽  
Vol 25 (1_suppl) ◽  
pp. S58-S58
Author(s):  
Megumi Watanabe ◽  
Ken-ichiro Katsura ◽  
Genki Mizukoshi ◽  
Ikuroh Ohsawa ◽  
Sadamitsu Asoh ◽  
...  

2022 ◽  
Vol 74 ◽  
pp. 101684
Author(s):  
Akram Mirzaei ◽  
Mohammad Reza Akbari ◽  
Seyed Saeed Tamehri Zadeh ◽  
Fatemeh Khatami ◽  
Rahil Mashhadi ◽  
...  

2016 ◽  
Vol 131 ◽  
pp. 464-472 ◽  
Author(s):  
Lucas M.M. Marques ◽  
Daniel R. Callejon ◽  
Larissa G. Pinto ◽  
Michel L. de Campos ◽  
Anderson R.M. de Oliveira ◽  
...  

2017 ◽  
Vol 92 (2) ◽  
pp. 184-190 ◽  
Author(s):  
Kazuhiro Torii ◽  
Noriaki Maeshige ◽  
Michiko Aoyama-Ishikawa ◽  
Makoto Miyoshi ◽  
Hiroto Terashi ◽  
...  

2019 ◽  
Vol 74 (10) ◽  
pp. 2930-2933 ◽  
Author(s):  
Hannelore I Bax ◽  
Corné P de Vogel ◽  
Johan W Mouton ◽  
Jurriaan E M de Steenwinkel

Abstract Background Despite intensive treatment regimens, the outcome of Mycobacterium abscessus infections is extremely poor and thus novel treatment regimens are needed. Although tigecycline seems to be one of the best options currently available, its long-term use is hampered by severe toxic side effects as well as the need for intravenous administration and the relatively high concentrations required for efficacy. Objectives To assess the in vitro activity of omadacycline against M. abscessus and compare it with the activity of tigecycline. Methods The concentration- and time-dependent killing capacities of omadacycline and tigecycline against M. abscessus subspecies abscessus were determined using a time–kill kinetics assay. Time–kill curves as well as concentration–effect curves were generated. Results Time–kill curves showed strong concentration-dependent antimicrobial activity for both omadacycline and tigecycline. Omadacycline showed inhibition of mycobacterial growth at 4 mg/L and mycobacterial killing at concentrations ≥16 mg/L. Tigecycline showed mycobacterial killing at concentrations ≥4 mg/L, achieving elimination at concentrations ≥16 mg/L. The concentration–effect curves after 7 days of exposure showed stasis, 1 log mycobacterial killing and 2 log mycobacterial killing at 3.3, 4.0 and 4.8 mg/L for omadacycline and 2.2, 2.7 and 3.4 mg/L for tigecycline, respectively. Conclusions The results of this in vitro study on omadacycline activity, together with its favourable (pharmacokinetic) properties, suggest that omadacycline is a potential new agent for the treatment of M. abscessus infections.


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