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Chemical Compound Review

Cordanum     1-cyclohexyl-3-[4-[2-hydroxy- 3-(tert...

Synonyms: Talinolol, Talinololum, SureCN78047, CHEMBL152067, AG-K-15103, ...
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Disease relevance of Cordanum


Psychiatry related information on Cordanum

  • In experiments on male Wistar rats, we studied the effects of some beta-adrenoceptor blockers: nonselective-propranolol, pindolol and 3b (a new aminotetraline derivative); and cardioselective (beta 1)-acebutolol and talinolol, on avoidance learning [4].

High impact information on Cordanum


Biological context of Cordanum

  • Grapefruit juice ingestion significantly reduces talinolol bioavailability [6].
  • SUBJECTS AND METHODS: In a randomized, crossover placebo-controlled study, oral pharmacokinetics of talinolol (50 mg) after concomitant administration of single doses of R-verapamil (120 mg) or placebo were investigated in 9 healthy volunteers [7].
  • However, multiple comparisons with combinations of putative functional SNPs did not confirm a significant influence of the MDR1 genotype on talinolol disposition [8].
  • RESULTS: A single glass of grapefruit juice decreased the talinolol area under the serum concentration-time curve (AUC), peak serum drug concentration (Cmax), and urinary excretion values to 56% (P < .001), 57% (P < .001), and 56% (P < .001), respectively, of those with water [6].
  • OBJECTIVE: To examine the relevance of site-dependent small intestinal absorption for incomplete intestinal absorption of the poorly metabolized beta 1-adrenergic receptor antagonist talinolol [9].

Anatomical context of Cordanum


Associations of Cordanum with other chemical compounds


Gene context of Cordanum

  • Carbamazepine regulates intestinal P-glycoprotein and multidrug resistance protein MRP2 and influences disposition of talinolol in humans [16].
  • METHODS: The disposition of talinolol after intravenous (30 mg) and single or repeated oral administration (100 mg daily) was monitored before and after chronic treatment with simvastatin (40 mg daily) in 18 healthy subjects (10 males, eight females, body mass index 19.0-27.0 kg m(-2)) genotyped for ABCB1, ABCC2 and SLCO1B1 polymorphisms [14].
  • In conclusion, the stereoselectivity of talinolol disposition is of minor importance, and most likely caused by presystemic biotransformation via CYP3A4 [17].
  • It is postulated that the effect of P-gp on the rate and extent of oral absorption should be more pronounced for those more slowly or incompletely absorbed drugs (i.e., drugs with relatively low permeabilities) as illustrated by talinolol in humans [18].
  • Talinolol was confirmed to bind to beta-adrenoceptors with moderate affinity but to act as a highly selective and efficient beta 1-adrenoceptor antagonist in terms of the relative degree and duration of its ergometric effects [19].

Analytical, diagnostic and therapeutic context of Cordanum

  • There was a direct correlation between the perfusion rate of talinolol and its transport rate for both regions and in all subjects investigated [9].
  • Moreover, the disposition of the probe drug talinolol was evaluated in 55 subjects after oral administration (100 mg) and in 23 subjects after intravenous administration(30 mg) [8].
  • Concentrations of talinolol were also measured in urine by HPLC [7].
  • Quantitation of talinolol and other beta-blockers by capillary electrophoresis for in vitro drug absorption studies [20].
  • METHODS: Talinolol immediate-release (Cordanum((R)), 100mg), one controlled-release (100mg) and two controlled-release tablets (200mg) were administered as single doses to fasting healthy volunteers in a crossover design with a 1 week washout period between treatments [21].


  1. Anti-anginal and anti-ischemic effects of the selective beta-blocker talinolol in patients with stable angina pectoris. Faulhaber, H.D., Weigmann, I., Lang, U., Weinsberg, F., Terhaag, B. International journal of clinical pharmacology and therapeutics. (2005) [Pubmed]
  2. The actions of talinolol, a beta 1-selective beta blocker, in cardiac arrhythmia and acute myocardial infarction. Assmann, I. Current medical research and opinion. (1995) [Pubmed]
  3. Pharmacokinetics of oral talinolol following a single dose and during steady state in patients with chronic renal failure and healthy volunteers. Krueger, M., Achenbach, H., Terhaag, B., Haase, H., Richter, K., Oertel, R., Preiss, R. International journal of clinical pharmacology and therapeutics. (2001) [Pubmed]
  4. Effects of some beta-adrenoceptor blockers on avoidance learning in rats. Staneva-Stoytcheva, D., Astrug, A., Ivanov, D. Methods and findings in experimental and clinical pharmacology. (1989) [Pubmed]
  5. P-glycoprotein and surfactants: effect on intestinal talinolol absorption. Bogman, K., Zysset, Y., Degen, L., Hopfgartner, G., Gutmann, H., Alsenz, J., Drewe, J. Clin. Pharmacol. Ther. (2005) [Pubmed]
  6. Grapefruit juice ingestion significantly reduces talinolol bioavailability. Schwarz, U.I., Seemann, D., Oertel, R., Miehlke, S., Kuhlisch, E., Fromm, M.F., Kim, R.B., Bailey, D.G., Kirch, W. Clin. Pharmacol. Ther. (2005) [Pubmed]
  7. Unexpected effect of verapamil on oral bioavailability of the beta-blocker talinolol in humans. Schwarz, U.I., Gramatté, T., Krappweis, J., Berndt, A., Oertel, R., von Richter, O., Kirch, W. Clin. Pharmacol. Ther. (1999) [Pubmed]
  8. The effects of the human MDR1 genotype on the expression of duodenal P-glycoprotein and disposition of the probe drug talinolol. Siegmund, W., Ludwig, K., Giessmann, T., Dazert, P., Schroeder, E., Sperker, B., Warzok, R., Kroemer, H.K., Cascorbi, I. Clin. Pharmacol. Ther. (2002) [Pubmed]
  9. Direct demonstration of small intestinal secretion and site-dependent absorption of the beta-blocker talinolol in humans. Gramatté, T., Oertel, R., Terhaag, B., Kirch, W. Clin. Pharmacol. Ther. (1996) [Pubmed]
  10. Intestinal secretion of intravenous talinolol is inhibited by luminal R-verapamil. Gramatté, T., Oertel, R. Clin. Pharmacol. Ther. (1999) [Pubmed]
  11. Induction of P-glycoprotein by rifampin increases intestinal secretion of talinolol in human beings: a new type of drug/drug interaction. Westphal, K., Weinbrenner, A., Zschiesche, M., Franke, G., Knoke, M., Oertel, R., Fritz, P., von Richter, O., Warzok, R., Hachenberg, T., Kauffmann, H.M., Schrenk, D., Terhaag, B., Kroemer, H.K., Siegmund, W. Clin. Pharmacol. Ther. (2000) [Pubmed]
  12. Intestinal drug efflux: formulation and food effects. Wagner, D., Spahn-Langguth, H., Hanafy, A., Koggel, A., Langguth, P. Adv. Drug Deliv. Rev. (2001) [Pubmed]
  13. Oral bioavailability of digoxin is enhanced by talinolol: evidence for involvement of intestinal P-glycoprotein. Westphal, K., Weinbrenner, A., Giessmann, T., Stuhr, M., Franke, G., Zschiesche, M., Oertel, R., Terhaag, B., Kroemer, H.K., Siegmund, W. Clin. Pharmacol. Ther. (2000) [Pubmed]
  14. Simvastatin does not influence the intestinal P-glycoprotein and MPR2, and the disposition of talinolol after chronic medication in healthy subjects genotyped for the ABCB1, ABCC2 and SLCO1B1 polymorphisms. Bernsdorf, A., Giessmann, T., Modess, C., Wegner, D., Igelbrink, S., Hecker, U., Haenisch, S., Cascorbi, I., Terhaag, B., Siegmund, W. British journal of clinical pharmacology. (2006) [Pubmed]
  15. The talinolol double-peak phenomenon is likely caused by presystemic processing after uptake from gut lumen. Weitschies, W., Bernsdorf, A., Giessmann, T., Zschiesche, M., Modess, C., Hartmann, V., Mrazek, C., Wegner, D., Nagel, S., Siegmund, W. Pharm. Res. (2005) [Pubmed]
  16. Carbamazepine regulates intestinal P-glycoprotein and multidrug resistance protein MRP2 and influences disposition of talinolol in humans. Giessmann, T., May, K., Modess, C., Wegner, D., Hecker, U., Zschiesche, M., Dazert, P., Grube, M., Schroeder, E., Warzok, R., Cascorbi, I., Kroemer, H.K., Siegmund, W. Clin. Pharmacol. Ther. (2004) [Pubmed]
  17. Stereoselective disposition of talinolol in man. Zschiesche, M., Lemma, G.L., Klebingat, K.J., Franke, G., Terhaag, B., Hoffmann, A., Gramatté, T., Kroemer, H.K., Siegmund, W. Journal of pharmaceutical sciences. (2002) [Pubmed]
  18. Apparent lack of effect of P-glycoprotein on the gastrointestinal absorption of a substrate, tacrolimus, in normal mice. Chiou, W.L., Chung, S.M., Wu, T.C. Pharm. Res. (2000) [Pubmed]
  19. Dose-effect and kinetic-dynamic relationships of the beta-adrenoceptor blocking properties of various doses of talinolol in healthy humans. de Mey, C., Schroeter, V., Butzer, R., Jahn, P., Weisser, K., Wetterich, U., Terhaag, B., Mutschler, E., Spahn-Langguth, H., Palm, D. J. Cardiovasc. Pharmacol. (1995) [Pubmed]
  20. Quantitation of talinolol and other beta-blockers by capillary electrophoresis for in vitro drug absorption studies. Awadallah, B., Schmidt, P.C., Holzgrabe, U., Wahl, M.A. Electrophoresis (2003) [Pubmed]
  21. Effects of controlled-release on the pharmacokinetics and absorption characteristics of a compound undergoing intestinal efflux in humans. Tubic, M., Wagner, D., Spahn-Langguth, H., Weiler, C., Wanitschke, R., B??cher, W.O., Langguth, P. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. (2006) [Pubmed]
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