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Chemical Compound Review

Cardizem     [(4R,5R)-2-(2- dimethylaminoethyl)-5-(4...

Synonyms: Altiazem, Deltazen, Aldizem, Dilacor, diltiazem, ...
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Disease relevance of diltiazem


Psychiatry related information on diltiazem


High impact information on diltiazem


Chemical compound and disease context of diltiazem


Biological context of diltiazem


Anatomical context of diltiazem

  • Diltiazem in the prevention of coronary artery disease in heart-transplant recipients [24].
  • Diltiazem and internal anal sphincter [25].
  • LN-induced neurite growth, like that induced by N-cadherin, is insensitive to diltiazem and conotoxin, but is highly sensitive to Ni2+ inhibition [26].
  • K+ depolarization experiments suggest that voltage-dependent Ca2+ influx pathways in CG neurons (cell bodies and growth cones) are largely blocked by the combination of diltiazem and Ni2+ [26].
  • The increase in LVSR during administration of diltiazem did not appear to be mediated by changes in contractility or regional myocardial blood flow, but were probably mediated in part by afterload reduction and possibly by a reduction in calcium entry into ischemic myocardium [27].

Associations of diltiazem with other chemical compounds

  • INTERVENTION: Diltiazem (mean dose, 392 +/- 27 mg/d) or nifedipine (mean dose, 83 +/- 9 mg/d) was used to decrease blood pressure to less than 140/90 mm Hg [28].
  • Ca(2+) channel blockers such as 1,4-dihydropyridines, phenylalkylamines, diltiazem and mibefradil exert their anti-arrhythmic and anti-hypertensive action by restricting Ca(2+) entry into myocardial cells and smooth muscle cells [29].
  • Treadmill exercise tests were done according to a randomized double-blind protocol 90 minutes after administration of placebo, 80 mg propranolol, or 120 mg diltiazem, each at both -8 degrees and 20 degrees C. Eight of the patients were classified by history as cold-sensitive before the study [30].
  • Change in luminal area after acute administration of a calcium antagonist (diltiazem or nicardipine), during exercise, and after sublingual nitroglycerin (percent change compared with rest = 100%) was assessed by biplane quantitative coronary arteriography [31].
  • Cardiovascular responses to handgrip, diltiazem, their combination, and nitroglycerin were assessed by hemodynamic and electrocardiographic measurements and by computer-assisted measurements of normal and diseased segments of epicardial coronary arteries [32].

Gene context of diltiazem

  • In contrast to these findings, the IL-6 plasma concentrations were comparable in both groups, whereas the serum concentration of soluble IL-2 receptors was decreased in patients treated with diltiazem [33].
  • Both, CsA and high doses of diltiazem caused an increase of IL-6 mRNA [33].
  • Role of CYP3A4 in human hepatic diltiazem N-demethylation: inhibition of CYP3A4 activity by oxidized diltiazem metabolites [34].
  • AIMS: To determine the effect of diltiazem on intestinal CYP3A activity and protein and mRNA expression in vivo in healthy subjects [35].
  • It has earlier been shown that the isoenzymes CYP2D6 and CYP3A4 are involved in O- and N-demethylation of diltiazem (DTZ), respectively [36].

Analytical, diagnostic and therapeutic context of diltiazem


  1. Life-threatening ventricular arrhythmias in patients with silent myocardial ischemia due to coronary-artery spasm. Myerburg, R.J., Kessler, K.M., Mallon, S.M., Cox, M.M., deMarchena, E., Interian, A., Castellanos, A. N. Engl. J. Med. (1992) [Pubmed]
  2. Diltiazem and reinfarction in patients with non-Q-wave myocardial infarction. Results of a double-blind, randomized, multicenter trial. Gibson, R.S., Boden, W.E., Theroux, P., Strauss, H.D., Pratt, C.M., Gheorghiade, M., Capone, R.J., Crawford, M.H., Schlant, R.C., Kleiger, R.E. N. Engl. J. Med. (1986) [Pubmed]
  3. Diltiazem and subacute cutaneous lupus erythematosus-like lesions. Crowson, A.N., Magro, C.M. N. Engl. J. Med. (1995) [Pubmed]
  4. Diltiazem prophylaxis in refractory migraine. Smith, R., Schwartz, A. N. Engl. J. Med. (1984) [Pubmed]
  5. Retinitis pigmentosa: rod photoreceptor rescue by a calcium-channel blocker in the rd mouse. Frasson, M., Sahel, J.A., Fabre, M., Simonutti, M., Dreyfus, H., Picaud, S. Nat. Med. (1999) [Pubmed]
  6. Diltiazem and akathisia. Jacobs, M.B. Ann. Intern. Med. (1983) [Pubmed]
  7. Interactions between diltiazem and ethanol: differences from those seen with dihydropyridine calcium channel antagonists. Watson, W.P., Little, H.J. Psychopharmacology (Berl.) (1994) [Pubmed]
  8. The effects of diltiazem on hemodynamics and seizure duration during electroconvulsive therapy. Wajima, Z., Yoshikawa, T., Ogura, A., Imanaga, K., Shiga, T., Inoue, T., Ogawa, R. Anesth. Analg. (2001) [Pubmed]
  9. A new extended-release formulation of diltiazem HCl for the treatment of mild-to-moderate hypertension. Frishman, W.H. Journal of clinical pharmacology. (1993) [Pubmed]
  10. Diltiazem as augmentation therapy in patients with treatment-resistant bipolar disorder: a retrospective study. Silverstone, P.H., Birkett, L. Journal of psychiatry & neuroscience : JPN. (2000) [Pubmed]
  11. Single-drug therapy for hypertension in men. A comparison of six antihypertensive agents with placebo. The Department of Veterans Affairs Cooperative Study Group on Antihypertensive Agents. Materson, B.J., Reda, D.J., Cushman, W.C., Massie, B.M., Freis, E.D., Kochar, M.S., Hamburger, R.J., Fye, C., Lakshman, R., Gottdiener, J. N. Engl. J. Med. (1993) [Pubmed]
  12. A preliminary study of diltiazem in the prevention of coronary artery disease in heart-transplant recipients. Schroeder, J.S., Gao, S.Z., Alderman, E.L., Hunt, S.A., Johnstone, I., Boothroyd, D.B., Wiederhold, V., Stinson, E.B. N. Engl. J. Med. (1993) [Pubmed]
  13. Do the results of randomized clinical trials of cardiovascular drugs influence medical practice? The SAVE Investigators. Lamas, G.A., Pfeffer, M.A., Hamm, P., Wertheimer, J., Rouleau, J.L., Braunwald, E. N. Engl. J. Med. (1992) [Pubmed]
  14. Excretion of diltiazem in human milk. Okada, M., Inoue, H., Nakamura, Y., Kishimoto, M., Suzuki, T. N. Engl. J. Med. (1985) [Pubmed]
  15. An assessment of diltiazem and hydrochlorothiazide in hypertension. Application of factorial trial design to a multicenter clinical trial of combination therapy. Burris, J.F., Weir, M.R., Oparil, S., Weber, M., Cady, W.J., Stewart, W.H. JAMA (1990) [Pubmed]
  16. Randomised, double-blind trial of intravenous diltiazem versus glyceryl trinitrate for unstable angina pectoris. Göbel, E.J., Hautvast, R.W., van Gilst, W.H., Spanjaard, J.N., Hillege, H.L., DeJongste, M.J., Molhoek, G.P., Lie, K.I. Lancet (1995) [Pubmed]
  17. Effects of diltiazem or lisinopril on massive proteinuria associated with diabetes mellitus. Bakris, G.L. Ann. Intern. Med. (1990) [Pubmed]
  18. Treatment of angina pectoris and hypertension with sustained-release calcium channel-blocking drugs. Klein, M.D., Weiner, D.A. Circulation (1987) [Pubmed]
  19. Termination of paroxysmal supraventricular tachycardia with a single oral dose of diltiazem and propranolol. Yeh, S.J., Lin, F.C., Chou, Y.Y., Hung, J.S., Wu, D. Circulation (1985) [Pubmed]
  20. Association of diltiazem therapy with increased insulin resistance in a patient with type I diabetes mellitus. Pershadsingh, H.A., Grant, N., McDonald, J.M. JAMA (1987) [Pubmed]
  21. Coregulation of calcium channels and beta-adrenergic receptors in cultured chick embryo ventricular cells. Marsh, J.D. J. Clin. Invest. (1989) [Pubmed]
  22. Smooth muscle calcium and endothelium-derived relaxing factor in the abnormal vascular responses of acute renal failure. Conger, J.D., Robinette, J.B., Schrier, R.W. J. Clin. Invest. (1988) [Pubmed]
  23. Pharmacokinetics and pharmacodynamics of intravenous diltiazem in patients with atrial fibrillation or atrial flutter. Dias, V.C., Weir, S.J., Ellenbogen, K.A. Circulation (1992) [Pubmed]
  24. Diltiazem in the prevention of coronary artery disease in heart-transplant recipients. Pollak, R., Fabrega, A.J. N. Engl. J. Med. (1993) [Pubmed]
  25. Diltiazem and internal anal sphincter. Jonard, P., Essamri, B. Lancet (1987) [Pubmed]
  26. Ca2+ influx and neurite growth in response to purified N-cadherin and laminin. Bixby, J.L., Grunwald, G.B., Bookman, R.J. J. Cell Biol. (1994) [Pubmed]
  27. Effect of diltiazem and propranolol on left ventricular segmental relaxation during temporary coronary arterial occlusion and one month reperfusion in conscious dogs. Tilton, G.D., Bush, L.R., Apprill, P.G., Buja, L.M., Willerson, J.T. Circulation (1985) [Pubmed]
  28. Effects of sodium intake on albumin excretion in patients with diabetic nephropathy treated with long-acting calcium antagonists. Bakris, G.L., Smith, A. Ann. Intern. Med. (1996) [Pubmed]
  29. beta-Subunits: fine tuning of Ca(2+) channel block. Hering, S. Trends Pharmacol. Sci. (2002) [Pubmed]
  30. Exercise-induced myocardial ischemia in a cold environment. Effect of antianginal medications. Juneau, M., Johnstone, M., Dempsey, E., Waters, D.D. Circulation (1989) [Pubmed]
  31. Normalization of abnormal coronary vasomotion by calcium antagonists in patients with hypertension. Frielingsdorf, J., Seiler, C., Kaufmann, P., Vassalli, G., Suter, T., Hess, O.M. Circulation (1996) [Pubmed]
  32. Diltiazem-induced blockade of sympathetically mediated constriction of normal and diseased coronary arteries: lack of epicardial coronary dilatory effect in humans. Hossack, K.F., Brown, B.G., Stewart, D.K., Dodge, H.T. Circulation (1984) [Pubmed]
  33. Effects of diltiazem upon metabolism and immunosuppressive action of cyclosporine in kidney graft recipients. Kunzendorf, U., Walz, G., Brockmoeller, J., Neumayer, H.H., Jochimsen, F., Roots, I., Offermann, G., Strom, T.B. Transplantation (1991) [Pubmed]
  34. Role of CYP3A4 in human hepatic diltiazem N-demethylation: inhibition of CYP3A4 activity by oxidized diltiazem metabolites. Sutton, D., Butler, A.M., Nadin, L., Murray, M. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  35. Diltiazem inhibits human intestinal cytochrome P450 3A (CYP3A) activity in vivo without altering the expression of intestinal mRNA or protein. Pinto, A.G., Horlander, J., Chalasani, N., Hamman, M., Asghar, A., Kolwankar, D., Hall, S.D. British journal of clinical pharmacology. (2005) [Pubmed]
  36. Desacetyl-diltiazem displays severalfold higher affinity to CYP2D6 compared with CYP3A4. Molden, E., Asberg, A., Christensen, H. Drug Metab. Dispos. (2002) [Pubmed]
  37. Characterization of antihypertensive therapy by whole-day blood pressure monitoring. Weber, M.A., Cheung, D.G., Graettinger, W.F., Lipson, J.L. JAMA (1988) [Pubmed]
  38. Diltiazem in acute myocardial infarction treated with thrombolytic agents: a randomised placebo-controlled trial. Incomplete Infarction Trial of European Research Collaborators Evaluating Prognosis post-Thrombolysis (INTERCEPT). Boden, W.E., van Gilst, W.H., Scheldewaert, R.G., Starkey, I.R., Carlier, M.F., Julian, D.G., Whitehead, A., Bertrand, M.E., Col, J.J., Pedersen, O.L., Lie, K.I., Santoni, J.P., Fox, K.M. Lancet (2000) [Pubmed]
  39. Coronary arterial spasm and Prinzmetal's variant form of angina induced by hyperventilation and Tris-buffer infusion. Yasue, H., Nagao, M., Omote, S., Takizawa, A., Miwa, K., Tanaka, S. Circulation (1978) [Pubmed]
  40. Short- and long-term efficacy of high-dose oral diltiazem for angina due to coronary artery disease: a placebo-controlled, randomized, double-blind crossover study. Petru, M.A., Crawford, M.H., Sorensen, S.G., Chaudhuri, T.K., Levine, S., O'Rourke, R.A. Circulation (1983) [Pubmed]
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