{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,2,27]],"date-time":"2026-02-27T16:49:27Z","timestamp":1772210967636,"version":"3.50.1"},"reference-count":11,"publisher":"Institute of Physiology of the Czech Academy of Sciences","content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Physiol Res"],"published-print":{"date-parts":[[2018,12,30]]},"abstract":"<jats:p>Telmisartan is an angiotensin receptor blocker (ARB) and a selective peroxisome proliferator activated receptor gamma (PPARG) modulator. Recently, we tested metabolic effects of telmisartan (5 mg\/kg body weight) in spontaneously hypertensive rats (SHR) fed a diet containing 60 % fructose, a widely used model of the metabolic syndrome. Surprisingly, we observed acute toxic effects of telmisartan. Rats lost body weight rapidly and died within 2 to 3 weeks due to bleeding into the upper gastrointestinal tract. SHR fed a high fructose diet and treated with telmisartan exhibited rapid decrease in blood pressure when compared to the SHR fed a high fructose diet and treated with valsartan. Concentrations of both unconjugated telmisartan and telmisartan glucuronide in the liver of SHR rats fed a high fructose diet were approximately 4 fold higher when compared to Brown Norway (BN) rats fed the same diet. Plasma concentrations of unconjugated telmisartan in the SHR were about 5 fold higher when compared to BN rats while plasma levels of telmisartan glucuronide were similar between the strains. Testing of other rat strains, diets, and the ARB valsartan showed that toxic effects of telmisartan in combination with high fructose diet are specific for the SHR. These results are consistent with the possibility that in some circumstances, SHR are predisposed to telmisartan toxicity possibly because of a genetically determined disturbance in telmisartan metabolism.<\/jats:p>","DOI":"10.33549\/physiolres.933951","type":"journal-article","created":{"date-parts":[[2019,8,8]],"date-time":"2019-08-08T12:58:03Z","timestamp":1565269083000},"page":"851-856","source":"Crossref","is-referenced-by-count":5,"title":["Acute Toxic Effects of Telmisartan in Spontaneously Hypertensive Rats Fed a High Fructose Diet"],"prefix":"10.33549","author":[{"given":"J.","family":"\u0160ILHAV\u00dd","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"P.","family":"MLEJNEK","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"M.","family":"\u0160IM\u00c1KOV\u00c1","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"I.","family":"VAN\u011a\u010cKOV\u00c1","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"M.","family":"BEHULIAK","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"O.","family":"KUDA","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"E.","family":"STICOV\u00c1","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"M.","family":"JIRSA","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"M.","family":"PRAVENEC","sequence":"additional","affiliation":[{"name":"Institute of Physiology of the Czech Academy of Sciences, Prague, Czech Republic"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"19169","published-online":{"date-parts":[[2018,12,9]]},"reference":[{"key":"ref0","doi-asserted-by":"publisher","unstructured":"BENSON SC, PERSHADSINGH HA, HO CI, CHITTIBOYINA A, DESAI P, PRAVENEC M, QI N, WANG J, AVERY MA, KURTZ TW: Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma-modulating activity. Hypertension 43: 993-1002, 2004.","DOI":"10.1161\/01.hyp.0000123072.34629.57"},{"key":"ref1","unstructured":"DrugInformer a: www.druginformer.com\/search\/side_effect_details\/Telmisartan\/chronic%20gastrointestinal%20bleeding.html"},{"key":"ref2","unstructured":"DrugInformer b: www.druginformer.com\/search\/side_effect_details\/Telmisartan\/abdominal%20pain.html"},{"key":"ref3","unstructured":"eHealthMe: www.ehealthme.com\/ds\/telmisartan\/ulcer-stomach"},{"key":"ref4","unstructured":"FDA Drug Approval Package: http:\/\/www.accessdata.fda.gov\/drugsatfda_docs\/nda\/98\/20850_Micardis.cfm"},{"key":"ref5","unstructured":"Patientsville.com: http:\/\/patientsville.com\/telmisartan\/gastrointestinal-haemorrhage.htm"},{"key":"ref6","doi-asserted-by":"crossref","unstructured":"PRAVENEC M, K\u0158EN V, LANDA V, MLEJNEK P, MUSILOV\u00c1 A, \u0160ILHAV\u00dd J, \u0160IM\u00c1KOV\u00c1 M, Z\u00cdDEK V: Recent progress in the genetics of spontaneously hypertensive rats. Physiol Res 63 (Suppl 1): S1-S8, 2014.","DOI":"10.33549\/physiolres.932622"},{"key":"ref7","doi-asserted-by":"publisher","unstructured":"RABIE EM, HEEBA GH, ABOUZIED MM, KHALIFA MM: Comparative effects of Aliskiren and Telmisartan in high fructose diet-induced metabolic syndrome in rats. Eur J Pharmacol 760: 145-153, 2015.","DOI":"10.1016\/j.ejphar.2015.04.019"},{"key":"ref8","doi-asserted-by":"publisher","unstructured":"SENGUPTA P, DAS A, IBRAHIM F, MANDAL UK, CHATTERJEE B, MAHMOOD S, DAS SK, KIFAYATULLAH M: Safety profiling of pioglitazone and telmisartan combination by sub-chronic toxicity study in rat. Regul Toxicol Pharmacol 81: 155-161, 2016.","DOI":"10.1016\/j.yrtph.2016.08.009"},{"key":"ref9","doi-asserted-by":"publisher","unstructured":"SHAHATAA MG, MOSTAFA-HEDEAB G, ALI EF, MAHDI EA, MAHMOUD FA: Effects of telmisartan and pioglitazone on high fructose induced metabolic syndrome in rats. Can J Physiol Pharmacol 94: 907-917, 2016.","DOI":"10.1139\/cjpp-2016-0090"},{"key":"ref10","doi-asserted-by":"publisher","unstructured":"YAN T, LI H, DENG L, GUO Y, YU W, FAWCETT JP, ZHANG D, CUI Y, GU J: Liquid chromatographic-tandem mass spectrometric method for the simultaneous quantitation of telmisartan and hydrochlorothiazide in human plasma. J Pharm Biomed Anal 48: 1225-1229, 2008.","DOI":"10.1016\/j.jpba.2008.08.021"}],"container-title":["Physiological Research"],"original-title":[],"language":"en","deposited":{"date-parts":[[2021,1,16]],"date-time":"2021-01-16T08:44:28Z","timestamp":1610786668000},"score":1,"resource":{"primary":{"URL":"http:\/\/www.biomed.cas.cz\/physiolres\/pdf\/67\/67_851.pdf"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2018,12,9]]},"references-count":11,"URL":"https:\/\/doi.org\/10.33549\/physiolres.933951","relation":{},"ISSN":["1802-9973","0862-8408"],"issn-type":[{"value":"1802-9973","type":"electronic"},{"value":"0862-8408","type":"print"}],"subject":[],"published":{"date-parts":[[2018,12,9]]}}}