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| http://linked.open...gbank/description
| - Trandolapril is a non-sulhydryl prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications. It is metabolized to its biologically active diacid form, trandolaprilat, in the liver. Trandolaprilat inhibits ACE, the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Trandolapril may be used to treat mild to moderate hypertension, to improve survival following myocardial infarction in clinically stable patients with left ventricular dysfunction, as an adjunct treatment for congestive heart failure, and to slow the rate of progression of renal disease in hypertensive individuals with diabetes mellitus and microalbuminuria or overt nephropathy. (en)
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| http://linked.open...y/drugbank/dosage
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| http://linked.open...generalReferences
| - # Berl T: Review: renal protection by inhibition of the renin-angiotensin-aldosterone system. J Renin Angiotensin Aldosterone Syst. 2009 Mar;10(1):1-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19286752 # Conen H, Brunner HR: Pharmacologic profile of trandolapril, a new angiotensin-converting enzyme inhibitor. Am Heart J. 1993 May;125(5 Pt 2):1525-31. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8480624 # Diaz A, Ducharme A: Update on the use of trandolapril in the management of cardiovascular disorders. Vasc Health Risk Manag. 2008;4(6):1147-58. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19337528 # Guay DR: Trandolapril: a newer angiotensin-converting enzyme inhibitor. Clin Ther. 2003 Mar;25(3):713-75. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12852701 # Jouquey S, Stepniewski JP, Hamon G: Trandolapril dose-response in spontaneously hypertensive rats: effects on ACE activity, blood pressure, and cardiac hypertrophy. J Cardiovasc Pharmacol. 1994;23 Suppl 4:S16-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/7527096 # Reynolds NA, Wagstaff AJ, Keam SJ: Trandolapril/verapamil sustained release: a review of its use in the treatment of essential hypertension. Drugs. 2005;65(13):1893-914. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16114984 # Rubio-Guerra AF, Vargas-Robles H, Vargas-Ayala G, Rodriguez-Lopez L, Escalante-Acosta BA: The effect of trandolapril and its fixed-dose combination with verapamil on circulating adhesion molecules levels in hypertensive patients with type 2 diabetes. Clin Exp Hypertens. 2008 Oct;30(7):682-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/18855271 # Sanbe A, Tanonaka K, Kobayasi R, Takeo S: Effects of long-term therapy with ACE inhibitors, captopril, enalapril and trandolapril, on myocardial energy metabolism in rats with heart failure following myocardial infarction. J Mol Cell Cardiol. 1995 Oct;27(10):2209-22. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8576937 # Torp-Pedersen C, Kober L: Effect of ACE inhibitor trandolapril on life expectancy of patients with reduced left-ventricular function after acute myocardial infarction. TRACE Study Group. Trandolapril Cardiac Evaluation. Lancet. 1999 Jul 3;354(9172):9-12. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/10406358 # Trandolapril: an ACE inhibitor for treatment of hypertension. Med Lett Drugs Ther. 1996 Nov 22;38(988):104-5. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8941256 # Wiseman LR, McTavish D: Trandolapril. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in essential hypertension. Drugs. 1994 Jul;48(1):71-90. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/7525196 # Zannad F: Trandolapril. How does it differ from other angiotensin converting enzyme inhibitors? Drugs. 1993;46 Suppl 2:172-81; discussion 182. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/7512472 (en)
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| http://linked.open...gy/drugbank/group
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| http://linked.open...drugbank/halfLife
| - The elimination half lives of trandolapril and trandolaprilat are about 6 and 10 hours, respectively, but, similar to all ACE inhibitors, trandolaprilat also has a prolonged terminal elimination phase that involves a small fraction of administered drug. This likely represents drug binding to plasma and tissue ACE. The effective half life of elimination for trandolaprilat is 16-24 hours. (en)
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| http://linked.open...ugbank/indication
| - For the treatment of mild to moderate hypertension, as an adjunct in the treatment of congestive heart failure (CHF), to improve survival following myocardial infarction (MI) in individuals who are hemodynamically stable and demonstrate symptoms of left ventricular systolic dysfunction or signs of CHF within a few days following acute MI, and to slow progression of renal disease in hypertensive patients with diabetes mellitus and microalbuminuria or overt nephropathy. (en)
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| http://linked.open...bank/manufacturer
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| http://linked.open...mechanismOfAction
| - There are two isoforms of ACE: the somatic isoform, which exists as a glycoprotein comprised of a single polypeptide chain of 1277; and the testicular isoform, which has a lower molecular mass and is thought to play a role in sperm maturation and binding of sperm to the oviduct epithelium. Somatic ACE has two functionally active domains, N and C, which arise from tandem gene duplication. Although the two domains have high sequence similarity, they play distinct physiological roles. The C-domain is predominantly involved in blood pressure regulation while the N-domain plays a role in hematopoietic stem cell differentiation and proliferation. ACE inhibitors bind to and inhibit the activity of both domains, but have much greater affinity for and inhibitory activity against the C-domain. Trandolaprilat, the active metabolite of trandolapril, competes with ATI for binding to ACE and inhibits and enzymatic proteolysis of ATI to ATII. Decreasing ATII levels in the body decreases blood pressure by inhibiting the pressor effects of ATII as described in the Pharmacology section above. Trandolaprilat also causes an increase in plasma renin activity likely due to a loss of feedback inhibition mediated by ATII on the release of renin and/or stimulation of reflex mechanisms via baroreceptors. (en)
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| http://linked.open...drugbank/packager
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| http://linked.open...y/drugbank/patent
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| http://linked.open...outeOfElimination
| - After oral administration of trandolapril, about 33% of parent drug and metabolites are recovered in urine, mostly as trandolaprilat, with about 66% in feces. (en)
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| http://linked.open.../drugbank/synonym
| - Mavik (en)
- Trandolaprilum (en)
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| http://linked.open...drugbank/toxicity
| - Most likely clinical manifestations of overdose are symptoms of severe hypotension. Most common adverse effects include cough, headache and dizziness. The oral LD<sub>50</sub> of trandolapril in mice was 4875 mg/kg in males and 3990 mg/kg in females. In rats, an oral dose of 5000 mg/kg caused low mortality (1 male out of 5; 0 females). In dogs, an oral dose of 1000 mg/kg did not cause mortality and abnormal clinical signs were not observed. (en)
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| http://linked.open...umeOfDistribution
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| http://linked.open.../drug/hasAHFSCode
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| http://linked.open...k/foodInteraction
| - Trandolapril may decrease the excretion of potassium. Salt substitutes containing potassium may increase the risk of hyperkalemia. (en)
- Take without regard to meals. (en)
- Herbs that may attenuate the antihypertensive effect of trandolapril include: bayberry, blue cohash, cayenne, ephedra, ginger, ginseng (American), kola and licorice. (en)
- High salt intake may attenuate the antihypertensive effect of trandolapril. (en)
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| http://linked.open.../drugbank/mixture
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| http://linked.open...nk/proteinBinding
| - Serum protein binding of trandolapril is ~ 80% (independent of concentration and not saturable) while that of trandolaprilat is 65 to 94% (concentration-dependent and saturable). (en)
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| http://linked.open...ynthesisReference
| - Narendra Joshi, Shekhar Bhirud, Buddhavarapu Ramam, Arjun Bodkhe, "Process for the preparation of intermediates of trandolapril and use thereof for the preparation of trandolapril." U.S. Patent US20060079698, issued April 13, 2006. (en)
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| http://linked.open...y/mesh/hasConcept
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| foaf:page
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| http://linked.open...ugbank/IUPAC-Name
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| http://linked.open...gy/drugbank/InChI
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| http://linked.open...Molecular-Formula
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| http://linked.open.../Molecular-Weight
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| http://linked.open...noisotopic-Weight
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| http://linked.open...y/drugbank/SMILES
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| http://linked.open.../Water-Solubility
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| http://linked.open...ogy/drugbank/logP
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| http://linked.open...ogy/drugbank/logS
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| http://linked.open...l/drug/hasATCCode
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| http://linked.open...nd-Acceptor-Count
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| http://linked.open...-Bond-Donor-Count
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| http://linked.open...drugbank/InChIKey
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| http://linked.open...urface-Area--PSA-
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| http://linked.open...nk/Polarizability
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| http://linked.open...bank/Refractivity
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| http://linked.open...atable-Bond-Count
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| http://linked.open...ugbank/absorption
| - ~ 40-60% absorbed; extensive first pass metabolism results in a low bioavailability of 4-14% (en)
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| http://linked.open.../affectedOrganism
| - Humans and other mammals (en)
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| http://linked.open...casRegistryNumber
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| http://linked.open...drugbank/category
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| http://linked.open...rugbank/clearance
| - * 52 L/h [After approximately 2 mg IV doses] (en)
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