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an ACE inhibiting drug (trade name Mavik) used in some patients after a heart attack or to treat hypertension (同)Mavik

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/06/22 19:33:18」(JST)

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Trandolapril is an ACE inhibitor used to treat high blood pressure, it may also be used to treat other conditions. It is marketed by Abbott Laboratories with the brand name Mavik.

Pharmacology

Trandolapril is a prodrug that is de-esterified to trandolaprilat. It is believed to exert its antihypertensive effect through the renin-angiotensin-aldosterone system. Trandolapril has a half-life of about 6 hours, and trandolaprilat has a half life of about 10 h. Trandolaprilat has about eight times the activity of its parent drug. About one-third of trandolapril and its metabolites are excreted in the urine, and about two-thirds of trandolapril and its metabolites are excreted in the feces. Serum protein binding of trandolapril is about 80%.

Mode of action

Trandolapril acts by competitive inhibition of angiotensin converting enzyme (ACE), a key enzyme in the renin-angiotensin system which plays an important role in regulating blood pressure.

Side effects

Side effects reported for trandolapril include nausea, vomiting, diarrhea, headache, dry cough, dizziness or lightheadedness when sitting up or standing, hypotension, or fatigue.

Possible drug interactions

Patients also on diuretics may experience an excessive reduction of blood pressure after initiation of therapy with trandolapril. It can reduce potassium loss caused by thiazide diuretics, and increase serum potassium when used alone. Therefore, hyperkalemia is a possible risk. Increased serum lithum levels can occur in patients who are also on lithium.

Contraindications and precautions

Pregnancy and lactation

Trandolapril is teratogenic (US: pregnancy category D) and can cause birth defects and even death of the developing fetus. The highest risk to the fetus is during the second and third trimesters. When pregnancy is detected, trandolapril should be discontinued as soon as possible. Trandolapril should not be administed to nursing mothers.

Additional effects

Combination therapy with paricalcitol and trandolapril has been found to reduce fibrosis in obstructive uropathy.^[1]

References

^ Tan, X; He, W; Liu, Y (2009). "Combination therapy with paricalcitol and trandolapril reduces renal fibrosis in obstructive nephropathy". Kidney international 76 (12): 1248–57. doi:10.1038/ki.2009.346. PMID 19759524.

External links

Mavik (PDF from manufacturer's website)
Tarka (PDF from manufacturer's website)
Trandolapril Information - rxlist.com (Rxlist.com, The Internet Drug Index)

UpToDate Contents

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1. ACE阻害剤、アンギオテンシン受容体遮断剤、および心房細動 ace inhibitors angiotensin receptor blockers and atrial fibrillation
2. 急性心筋梗塞におけるアンギオテンシン変換酵素阻害剤および受容体遮断剤：臨床試験 angiotensin converting enzyme inhibitors and receptor blockers in acute myocardial infarction clinical trials
3. アテローム性心血管疾患患者における血圧マネージメント blood pressure management in patients with atherosclerotic cardiovascular disease
4. 原発性（本態性）高血圧における治療選択：臨床試験 choice of therapy in primary essential hypertension clinical trials
5. 黒人における高血圧治療 treatment of hypertension in blacks

English Journal

Impurity profiling of trandolapril under stress testing: Structure elucidation of by-products and development of degradation pathway.

Dendeni M, Cimetiere N, Amrane A, Hamida NB.SourceLaboratoire de Chimie Analytique et Electrochimie, Faculté des Sciences de Tunis, Campus universitaire de Tunis El Manar, 2092 Tunis, Tunisia; Ecole Nationale Supérieure de Chimie de Rennes, CNRS, UMR 6226, Av. du Général Leclerc, CS 50837, 35708 Rennes Cedex 7, France; Université européenne de Bretagne, 35000 Rennes, France.
International journal of pharmaceutics.Int J Pharm.2012 Nov 15;438(1-2):61-70. doi: 10.1016/j.ijpharm.2012.08.048. Epub 2012 Sep 1.
Various regulatory authorities like International Conference on Harmonization (ICH), US Food and Drug Administration, Canadian Drug and Health Agency are emphasizing on the purity requirements and the identification of impurities in active pharmaceutical drugs. Qualification of the impurities is the
PMID 22960502

Glomerular Hyperfiltration and Renal Disease Progression in Type 2 Diabetes.

Ruggenenti P, Porrini EL, Gaspari F, Motterlini N, Cannata A, Carrara F, Cella C, Ferrari S, Stucchi N, Parvanova A, Iliev I, Dodesini AR, Trevisan R, Bossi A, Zaletel J, Remuzzi G; for the GFR Study Investigators.SourceCorresponding author: Piero Ruggenenti, pruggenenti@ospedaliriuniti.bergamo.it.
Diabetes care.Diabetes Care.2012 Oct;35(10):2061-2068. Epub 2012 Jul 6.
OBJECTIVE To describe the prevalence and determinants of hyperfiltration (glomerular filtration rate [GFR] ≥120 mL/min/1.73 m(2)), GFR decline, and nephropathy onset or progression in type 2 diabetic patients with normo- or microalbuminuria. RESEARCH DESIGN AND METHODS We longitudinally studied 6
PMID 22773704

Japanese Journal

Changes of Matrix Metalloproteinase-9 Level Is Associated With Left Ventricular Remodeling Following Acute Myocardial Infarction Among Patients Treated With Trandolapril, Valsartan or Both

MIYAZAKI Sakiko,KASAI Takatoshi,MIYAUCHI Katsumi,MIYAZAKI Tadashi,AKIMOTO Yoshinori,TAKAGI Atsutoshi,AIHARA Kouichiro,KAWAMURA Masaki,SUWA Satoru,KOJIMA Satoshi,SUMIYOSHI Masataka,DAIDA Hiroyuki
Circulation journal : official journal of the Japanese Circulation Society 74(6), 1158-1164, 2010-05-25
… trandolapril, valsartan or a combination of both (half-dose-trandolapril plus half-dose-valsartan). … In comparison, across groups, it was found that MMP-9, LVEDVI and LVESVI at 12 months were significantly lower in the combination therapy group than in the trandolapril group. … There were no significant differences between the valsartan group and combination therapy group, or between the valsartan group and the trandolapril group. …
NAID 10026474742

心疾患を合併する高血圧 JMIC-B,INVEST (大規模臨床試験--循環・代謝系を中心に) -- (高血圧)

由井芳樹
日本臨床 66(-) (945), 130-134, 2008-10
NAID 40016297580

Related Pictures

★リンクテーブル★

リンク元	「トランドラプリル」

「トランドラプリル」

Trandolapril
Systematic (IUPAC) name
	(2S,3aR,7aS)-1-[(2S)-2-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}propanoyl]-octahydro-1H-indole-2-carboxylic acid
Clinical data
Trade names	Mavik
AHFS/Drugs.com	monograph
MedlinePlus	a697010
Pregnancy; category	US: D (Evidence of risk);
Legal status	℞ (Prescription only);
Routes of; administration	Oral
Pharmacokinetic data
Protein binding	Trandolapril 80%; (independent of concentration); Trandolaprilat 65 to 94%; (concentration-dependent)
Metabolism	Hepatic
Biological half-life	6 hours (trandolapril); 10 hours (trandolaprilat)
Excretion	Fecal and renal
Identifiers
CAS Registry Number	87679-37-6
ATC code	C09AA10
PubChem	CID: 5484727
IUPHAR/BPS	6453
DrugBank	DB00519
ChemSpider	4588590
UNII	1T0N3G9CRC
KEGG	D00383
ChEMBL	CHEMBL1519
Chemical data
Formula	C24H34N2O5
Molecular mass	430.537 g/mol
	SMILES O=C(OCC)[C@@H](N[C@H](C(=O)N1[C@H](C(=O)O)C[C@H]2CCCC[C@H]12)C)CCc3ccccc3;
	InChI InChI=1S/C24H34N2O5/c1-3-31-24(30)19(14-13-17-9-5-4-6-10-17)25-16(2)22(27)26-20-12-8-7-11-18(20)15-21(26)23(28)29/h4-6,9-10,16,18-21,25H,3,7-8,11-15H2,1-2H3,(H,28,29)/t16-,18+,19-,20-,21-/m0/s1 ; Key:VXFJYXUZANRPDJ-WTNASJBWSA-N ;
Physical data
Melting point	119 to 123 °C (246 to 253 °F)
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　　[★]

英: trandolapril
商: オドリック、トラントーワ、プレドリック、プレラン

[1] Tan, X; He, W; Liu, Y (2009). "Combination therapy with paricalcitol and trandolapril reduces renal fibrosis in obstructive nephropathy". Kidney international 76 (12): 1248–57. doi:10.1038/ki.2009.346. PMID 19759524.

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案内

trandolapril