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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Following oral and intravenous dosing with [14C] eprosartan in human subjects, eprosartan was the only drug-related compound found in the plasma and faeces. In the urine, approximately 20% of the radioactivity excreted was an acyl glucuronide of eprosartan with the remaining 80% being unchanged eprosartan.
Classes of Drugs that can Cause Important Interactions
Published in Jerome Z. Litt, Neil H. Shear, Litt's Drug Eruption & Reaction Manual, 2017
Angiotensin II receptor antagonists (blockers)CandesartanEprosartanIrbesartanLosartanOlmesartanTelmisartanValsartan
Cardiovascular drugs
Published in Ann Richards, Nursing & Health Survival Guide, 2014
Candesartan, eprosartan, irbesartan, losartan, olmesartan, telmisartan, valsartanBlock the receptors for angiotensin II and thus vasodilate and have a small diuretic effect like ACE-inhibitors.Do not block ACE and so do not have the side effect of a dry cough.Used when patient cannot take ACE-inhibitors.
Selection of the candidate compound at an early stage of new drug development: retrospective pharmacokinetic and metabolic evaluations of valsartan using common marmosets
Published in Xenobiotica, 2022
Shogo Matsumoto, Shotaro Uehara, Hidetaka Kamimura, Naoki Cho, Hiroshi Ikeda, Satoshi Maeda, Kensuke Kagiyama, Atsunori Miyata, Hiroshi Suemizu, Kazumasa Fukasawa
The predicted t1/2 value of eprosartan in the present study was 4.7 h, whereas the t1/2, obs value of this drug was approximately 2 h following intravenous administration in a clinical study (Table 2). However, Tenero et al. (1998) reported that the terminal t1/2 value of eprosartan following oral administration was 5–7 h in humans. The longer t1/2, obs after oral administration than that after intravenous injection was considered to be due to the detection of an additional elimination phase or absorption rate-limited elimination. In the present study, the human CLt and Vss values of eprosartan were reasonably predicted (Figure 3(A,B)), and elimination t1/2 values after intravenous administration may be greater than 2 h. In fact, eprosartan is administered orally once or twice per day for the treatment of hypertension (Hedner and Himmelmann 1999).
Formulation and characterization of Phospholipon 90 G and tween 80 based transfersomes for transdermal delivery of eprosartan mesylate
Published in Pharmaceutical Development and Technology, 2018
Abdul Ahad, Abdulmohsen A. Al-Saleh, Abdullah M. Al-Mohizea, Fahad I. Al-Jenoobi, Mohammad Raish, Alaa Eldeen B. Yassin, Mohd Aftab Alam
With the above knowledge, we have developed transfersomes formulation of eprosartan mesylate using Phospholipon® 90 G (a lipid bilayer-forming substance) and Tween® 80 as an edge activator. Eprosartan mesylate is an angiotensin II receptor blocker used to treat hypertension. It has an oral bioavailability of 13% in humans and half-life of 5–9 h (Israili 2000; Dangre et al. 2016). The eprosartan mesylate has a log p value of 3.9. These features of the drug, distinguished it as a suitable candidate for transdermal delivery.
Formulation and characterization of eprosartan mesylate and β-cyclodextrin inclusion complex prepared by microwave technology
Published in Drug Delivery, 2022
Abdul Ahad, Yousef A. Bin Jardan, Mohd. Zaheen Hassan, Mohammad Raish, Ajaz Ahmad, Abdullah M. Al-Mohizea, Fahad I. Al-Jenoobi
Eprosartan mesylate (EM, Figure 1(A)) is considered a promising angiotensin II receptor antagonist (Ahad et al., 2018). EM is licensed for the management of hypertension in some more than 20 countries including the UK, Germany, and USA (Ahn et al., 2011).