Interní Med. 2004; 6(7): 373

Farmakologický profil losartanu

MUDr. Tomáš Doležal
Ústav farmakologie 3. LF UK, Praha

Published: December 31, 2004  Show citation

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Doležal T. Farmakologický profil losartanu. Interní Med. 2004;6(7):373.

Losartan je nepeptidový antagonista angiotenzinu II. Farmakologické in vitro a in vivo studie ukázaly, že se losartan kompetitivně váže na AT1 receptor bez vnitřní agonistické aktivity. Losartan je v organizmu metabolizován na 5-karboxylovou kyselinu (E-3174), která má silnější vazbu (10-40 násobně) na AT1 receptor než vlastní losartan, pomalejší disociaci a také delší dobu působení...

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    References

    1. Zaidenstein R, Soback S, Gips M et al. Effect of grapefruit juice on the pharmacokinetics of losartan and its active metabolite E3174 in healthy volunteers. Ther. Drug Monit. 2001; 23: 369-373. Go to original source... Go to PubMed...
    2. Ohtawa M, Takayama F, Saitoh K, Yoshinaga T, Nakashima M. Pharmacokinetics and biochemical efficacy after single and multiple oral administration of losartan, an orally active nonpeptide angiotensin II receptor antagonist, in humans. Br.J Clin Pharmacol. 1993; 35: 290-297. Go to original source... Go to PubMed...
    3. Conlin PR, Spence JD, Williams B et al. Angiotensin II antagonists for hypertension: are there differences in efficacy? Am. J Hypertens. 2000; 13: 418-426. Go to original source... Go to PubMed...
    4. Nakao N, Yoshimura A, Morita H, Takada M, Kayano T, Ideura T. Combination treatment of angiotensin-II receptor blocker and angiotensin-converting-enzyme inhibitor in non-diabetic renal disease (COOPERATE): a randomised controlled trial. Lancet 2003; 361: 117-124. Go to original source... Go to PubMed...
    5. Chan P, Tomlinson B, Huang TY, Ko JT, Lin TS, Lee YS. Double-blind comparison of losartan, lisinopril, and metolazone in elderly hypertensive patients with previous angiotensin-converting enzyme inhibitor-induced cough. J Clin Pharmacol. 1997; 37:253-257. Go to original source... Go to PubMed...
    6. Weber MA. Clinical experience with the angiotensin II receptor antagonist losartan. A preliminary report. Am. J Hypertens. 1992; 5: 247S-251S. Go to original source... Go to PubMed...
    7. Grossman E, Messerli FH, Neutel JM. Angiotensin II receptor blockers: equal or preferred substitutes for ACE inhibitors? Arch. Intern. Med. 2000; 160: 1905-1911. Go to original source... Go to PubMed...
    8. Grossman E, Messerli FH, Neutel JM. Angiotensin II receptor blockers: equal or preferred substitutes for ACE inhibitors? Arch. Intern. Med. 2000; 160: 1905-1911. Go to original source... Go to PubMed...
    9. Dahlof B, Devereux RB, Kjeldsen SE, et al. Cardiovascular morbidity and mortality in the Losartan Intervention For Endpoint reduction in hypertension study (LIFE): a randomised trial against atenolol. Lancet 2002; 359: 995-1003. Go to original source... Go to PubMed...
    10. Pitt B, Segal R, Martinez FA, et al. Randomised trial of losartan versus captopril in patients over 65 with heart failure (Evaluation of Losartan in the Elderly Study, ELITE). Lancet 1997; 349: 747-752. Go to original source... Go to PubMed...
    11. Pitt B, Poole-Wilson PA, Segal R et al. Effect of losartan compared with captopril on mortality in patients with symptomatic heart failure: randomised trial-the Losartan Heart Failure Survival Study ELITE II. Lancet 2000; 355: 1582-1587. Go to original source... Go to PubMed...
    12. Zaidenstein R, Soback S, Gips M et al. Effect of grapefruit juice on the pharmacokinetics of losartan and its active metabolite E3174 in healthy volunteers. Ther. Drug Monit. 2001; 23: 369-373. Go to original source... Go to PubMed...
    13. Ohtawa M, Takayama F, Saitoh K, Yoshinaga T, Nakashima M. Pharmacokinetics and biochemical efficacy after single and multiple oral administration of losartan, an orally active nonpeptide angiotensin II receptor antagonist, in humans. Br.J Clin Pharmacol. 1993; 35: 290-297. Go to original source... Go to PubMed...
    14. Conlin PR, Spence JD, Williams B et al. Angiotensin II antagonists for hypertension: are there differences in efficacy? Am. J Hypertens. 2000; 13: 418-426. Go to original source... Go to PubMed...
    15. Nakao N, Yoshimura A, Morita H, Takada M, Kayano T, Ideura T. Combination treatment of angiotensin-II receptor blocker and angiotensin-converting-enzyme inhibitor in non-diabetic renal disease (COOPERATE): a randomised controlled trial. Lancet 2003; 361: 117-124. Go to original source... Go to PubMed...
    16. Chan P, Tomlinson B, Huang TY, Ko JT, Lin TS, Lee YS. Double-blind comparison of losartan, lisinopril, and metolazone in elderly hypertensive patients with previous angiotensin-converting enzyme inhibitor-induced cough. J Clin Pharmacol. 1997; 37:253-257. Go to original source... Go to PubMed...
    17. Weber MA. Clinical experience with the angiotensin II receptor antagonist losartan. A preliminary report. Am. J Hypertens. 1992; 5: 247S-251S. Go to original source... Go to PubMed...
    18. Grossman E, Messerli FH, Neutel JM. Angiotensin II receptor blockers: equal or preferred substitutes for ACE inhibitors? Arch. Intern. Med. 2000; 160: 1905-1911. Go to original source... Go to PubMed...
    19. Grossman E, Messerli FH, Neutel JM. Angiotensin II receptor blockers: equal or preferred substitutes for ACE inhibitors? Arch. Intern. Med. 2000; 160: 1905-1911. Go to original source... Go to PubMed...
    20. Dahlof B, Devereux RB, Kjeldsen SE, et al. Cardiovascular morbidity and mortality in the Losartan Intervention For Endpoint reduction in hypertension study (LIFE): a randomised trial against atenolol. Lancet 2002; 359: 995-1003. Go to original source... Go to PubMed...
    21. Pitt B, Segal R, Martinez FA, et al. Randomised trial of losartan versus captopril in patients over 65 with heart failure (Evaluation of Losartan in the Elderly Study, ELITE). Lancet 1997; 349: 747-752. Go to original source... Go to PubMed...
    22. Pitt B, Poole-Wilson PA, Segal R et al. Effect of losartan compared with captopril on mortality in patients with symptomatic heart failure: randomised trial-the Losartan Heart Failure Survival Study ELITE II. Lancet 2000; 355: 1582-1587. Go to original source... Go to PubMed...

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