Telmisartan

Profiles Drug Subst Excip Relat Methodol. 2015:40:371-429. doi: 10.1016/bs.podrm.2015.01.003. Epub 2015 Mar 31.

Abstract

Telmisartan is an angiotensin-II receptor antagonist (ARB) used in the treatment of hypertension. Generally, angiotensin-II receptor blockers such as telmisartan bind to the angiotensin-II type 1 receptors with high affinity, causing inhibition of the action of angiotensin II on vascular smooth muscle, ultimately leading to a reduction in arterial blood pressure. The present study gives a comprehensive profile of telmisartan, including detailed nomenclature, formulae, elemental analysis, and appearance of the drug are mentioned. The uses and applications and the several methods described for its preparation of the drug are outlined. The profile contains the physicochemical properties including: pKa value, solubility, X-ray powder diffraction, melting point, and methods of analysis (including compendial, electrochemical, spectroscopic, and chromatographic methods of analysis). Developed validated stability-indicating (HPLC and biodiffusion assay methods under accelerated acidic, alkaline, and oxidative conditions, in addition to effect of different types of light, temperature, and pH. Detailed Pharmacology also presented (Pharmacological actions, Therapeutic uses and Dosing, Interactions, and adverse effects and precautions). More than 80 references were given as a proof of the above-mentioned studies.

Keywords: Description; Method of analysis; Pharmacokinetics; Physical characteristics; Spectral properties; Stability; Synthesis; Telmisartan; Uses.

Publication types

  • Review

MeSH terms

  • Angiotensin II Type 1 Receptor Blockers / administration & dosage
  • Angiotensin II Type 1 Receptor Blockers / adverse effects
  • Angiotensin II Type 1 Receptor Blockers / chemistry*
  • Angiotensin II Type 1 Receptor Blockers / pharmacokinetics
  • Animals
  • Antihypertensive Agents / administration & dosage
  • Antihypertensive Agents / adverse effects
  • Antihypertensive Agents / chemistry*
  • Antihypertensive Agents / pharmacokinetics
  • Benzimidazoles / administration & dosage
  • Benzimidazoles / adverse effects
  • Benzimidazoles / chemistry*
  • Benzimidazoles / pharmacokinetics
  • Benzoates / administration & dosage
  • Benzoates / adverse effects
  • Benzoates / chemistry*
  • Benzoates / pharmacokinetics
  • Blood Pressure / drug effects
  • Chemistry, Pharmaceutical
  • Drug Interactions
  • Drug Stability
  • Humans
  • Hypertension / drug therapy
  • Hypertension / physiopathology
  • Molecular Structure
  • Technology, Pharmaceutical / methods
  • Telmisartan

Substances

  • Angiotensin II Type 1 Receptor Blockers
  • Antihypertensive Agents
  • Benzimidazoles
  • Benzoates
  • Telmisartan