A Review On Safety And Tolerability Of Telmisartan

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Dr. Kiran C. Mahajan
Mr. Sanket B. Gunjal
Mr. Sushant S. Gaikwad
Mr. Vinayak D. Gadge
Mr. Oasis P. Shelke
Dr. Ganesh Y. Dama

Abstract

Essential hypertension can be treated with telmisartan, a strong, long-acting nonpeptide antagonist of angiotensin II type-1 (AT1) receptor. Without influencing other receptor systems involved in the regulation of the cardiovascular system, it specifically blocks the activation of the AT1 receptor by angiotensin II. When combined with high volume of distribution and telmisartan’s distinctively high lipophilicity, the molecule provides the clinically significant benefit of strong tissue penetration. Additionally, it causes an increase in the protein level of adiponectin in adipocytes and activates peroxisome proliferator-activated receptor c (PPAR-c). They might increase insulin sensitivity in this way. According to the BCS classification, it is class II medication because of its high permeability and low solubility. To increase the telmisartan solid dispersion’s aqueous solubility and dissolution rate, various techniques were prepared and studied. One of the main issues with this medication is its low solubility in biological fluids, which leads to poor bioavailability after oral administration. Telmisartan’s solubility was shown to be enhanced when the medication was dispersed solidly utilizing carrier such poly vinyl pyrrolidonek30, poly ethylene glycol 6000, βeta-cyclodextrin, Gelucire 43/01, Poloxamer 407, PVP K30 and HPMC E4, PEG 6000, and NaHCO3.

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How to Cite
Dr. Kiran C. Mahajan, Mr. Sanket B. Gunjal, Mr. Sushant S. Gaikwad, Mr. Vinayak D. Gadge, Mr. Oasis P. Shelke, & Dr. Ganesh Y. Dama. (2024). A Review On Safety And Tolerability Of Telmisartan. Journal of Advanced Zoology, 45(4), 9–14. https://doi.org/10.53555/jaz.v45i4.4519
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Author Biographies

Dr. Kiran C. Mahajan

Department of Pharmaceutics, SGMSPM’s Sharadchandra Pawar College of Pharmacy, Dumbarwadi (Otur), Tal- Junnar, Dist.- Pune, 410504.

Mr. Sanket B. Gunjal

Department of Pharmaceutics, SGMSPM’s Sharadchandra Pawar College of Pharmacy, Dumbarwadi (Otur), Tal- Junnar, Dist.- Pune, 410504.

Mr. Sushant S. Gaikwad

Department of Pharmaceutics, SGMSPM’s Sharadchandra Pawar College of Pharmacy, Dumbarwadi (Otur), Tal- Junnar, Dist.- Pune, 410504.

Mr. Vinayak D. Gadge

Department of Pharmaceutics, SGMSPM’s Sharadchandra Pawar College of Pharmacy, Dumbarwadi (Otur), Tal- Junnar, Dist.- Pune, 410504.

Mr. Oasis P. Shelke

Department of Pharmaceutics, SGMSPM’s Sharadchandra Pawar College of Pharmacy, Dumbarwadi (Otur), Tal- Junnar, Dist.- Pune, 410504.

Dr. Ganesh Y. Dama

Department of Pharmacognosy, SGMSPM’s Sharadchandra Pawar College of Pharmacy, Dumbarwadi (Otur), Tal- Junnar, Dist.- Pune, 410504.

References

Sylvia Deppe, Rainer H Beoger, Johanna Weiss & Ralf A Benndorf, Telmisartan: a review of its pharmacodynamic and pharmacokinetic properties, Expert Opin. Drug Metab. Toxicol. 2010, 6(7):863- 871.

Ralf A. Benndorf4, Tanja Rudolph, Daniel Appel, Edzard Schwedhelm, Renke Maas, Friedrich Schulze, Elisabeth Silberhorn, Rainer H. Bfger, Telmisartan improves insulin sensitivity in nondiabetic patients with essential hypertension, Metabolism Clinical and Experimental 2006; 55: 1159– 1164.

Wolfgang Wienen, Michael Entzeroth, Jacobus C. A. van Meel, Joachim Stangier, Ulrich Busch, Thomas Ebner, Jochen Schmid, Horst Lehmann, Kandace Matzek, Joan Kempthorne-Rawson, Volker Gladigau, and Norbert H. Haul, A Review on Telmisartan: A Novel, Long-Acting Angiotensin II-Receptor Antagonist, Cardiovascular Drug Reviews Vol. 18, No. 2, pp. 127–154.

Mallion JM, Siche JP, Lacourcière Y and the Telmisartan Blood Pressure Monitoring Group.ABPM comparison of the antihypertensive profiles of the selective angiotensin II receptor antagonists telmisartan and losartan in patients with mild tomoderate hypertension. J Hum Hypertens 1999;13:657–664.

Jutta M. Nagel1, Anne B. Tietz1, Burkhard Gfke, Klaus G. Parhofer, The effect of telmisartan on glucose and lipid metabolism in nondiabetic, insulin-resistant subjects, Metabolism Clinical and Experimental, 2006; 55: 1149– 1154.

Burcu Barutcuoglui, Zuhal Parildari, M. Işıl Mutafi, Dilek Ozmen, Emin Alioglu, Sara Habif, Oya Bayindir,Effect of telmisartan on vascular endothelium in hypertensive and type 2 diabetic hypertensive patients, Turk J Med Sci 2010; 40 (2): 239-248.

Tatami S, Sarashina A , Yamamura N, Population pharmacokinetics of an angiotensinII

receptor antagonist, telmisartan, in healthy volunteers and hypertensive patients. Drug Metab

Pharmacokin 2003 ; 18 : 203 -11.

www.drugbank.com

Boehringer Ingelheim Pharma. Drug prescribing information: Micardis; 1998.

Stangier J, Schmid J , Turck D, Absorption, metabolism and excretion of intravenously and

orally administered telmisartan in health volunteers. J Clin Pharmacol 2000 ; 40 : 1312 -22.

Thomas GN, Chan P, Tomlinson B . The role of angiotensin II type 1 receptor antagonists in elderly patients with hypertension. Drugs Aging 2006 ; 23 : 131 -55.

Barbara H Rosario & Timothy James Hendra, Telmisartan in the treatment of hypertension,

Expert Opin. Drug Metab. Toxicol. 2008; 4(4):485- 492.

Stangier J, Schmid J, Turck D, et al. Absorption, metabolism, and excretion of intravenously and orally administered telmisartan in healthy volunteers. J Clin Pharmacol 2000;40:1312-22

Unger T, Kaschina E. Drug interactions with angiotensin receptor blockers: a comparison with other antihypertensives. Drug Saf 2003;26:707-20

Ishiguro N, Maeda K, Kishimoto W, et al. Predominant contribution of OATP1B3 to the hepatic uptake of telmisartan, an angiotensin II receptor antagonist, in humans. Drug Metab Dispos 2006;34:1109-15

Ishiguro N, Maeda K, Saito A, et al. Establishment of a set of double transfectants coexpressing organic anion transporting polypeptide 1B3 and hepatic efflux transporters for the characterization of the hepatobiliary transport of telmisartan acylglucuronide. Drug Metab Dispos 2008;36:796-805

Weiss J, Sauer A, Divac N, et al. Interaction of angiotensin receptor type 1 blockers with ATP-binding cassette transporters. Biopharm Drug Dispos 2010;31:150-61

Bajcetic M, Benndorf RA, Appel D, et al. Pharmacokinetics of oral doses of telmisartan and nisoldipine, given alone and in combination, in patients with essential hypertension. J Clin Pharmacol 2007;47:295-304

Yusuf S, Teo KK, Pogue J, et al. The ONTARGET investigators. Telmisartan, ramipril, or both in patients at high risk for vascular events. N Engl J Med 2008;358:1547-59

Ross SD, Akhras KS, Zhang S, et al. Discontinuation of antihypertensive drugs due to adverse events: a systematic review and meta-analysis. Pharmacotherapy 2001;21:940-53

Michel MC, Bohner H, Koster J, et al. Safety of telmisartan in patients with arterial hypertension: an open-label observational study. Drug Saf 2004;27:335-44

Petrovic J, Petrovic D, Vukovic N, et al. Ventricular and vascular remodelling: effects of the angiotensin II receptor blocker telmisartan and/or the angiotensin-converting enzyme inhibitor ramipril in hypertensive patients. J Int Med Res 2005;33:39-49A

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