Peringatan Keamanan

Most likely clinical manifestations of overdose are symptoms of severe hypotension. Most common adverse effects include cough, headache and dizziness. The oral LD50 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.

Trandolapril

DB00519

small molecule approved

Deskripsi

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.

Struktur Molekul 2D

Berat 430.5372
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 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.
Volume Distribusi * 18 L
Klirens (Clearance) * 52 L/h [After approximately 2 mg IV doses]

Absorpsi

~ 40-60% absorbed; extensive first pass metabolism results in a low bioavailability of 4-14%

Metabolisme

Cleavage of the ester group of trandolapril, primarily in the liver, is responsible for conversion to trandolaprilat, the active metabolite. Seven other metabolites, including diketopiperazine and glucuronide conjugated derivatives of trandolapril and trandolaprilat, have been identified.

Rute Eliminasi

After oral administration of trandolapril, about 33% of parent drug and metabolites are recovered in urine, mostly as trandolaprilat, with about 66% in feces.

Interaksi Makanan

4 Data
  • 1. Avoid hypertensive herbs (e.g. bayberry, blue cohosh, cayenne, ephedra, and licorice).
  • 2. Avoid potassium-containing products. Potassium products increase the risk of hyperkalemia.
  • 3. Limit salt intake. Salt may attenuate the antihypertensive effect.
  • 4. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

848 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Trandolapril is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Trandolapril is combined with Levodopa.
Risperidone Trandolapril may increase the hypotensive activities of Risperidone.
Alfuzosin Alfuzosin may increase the hypotensive activities of Trandolapril.
Amifostine Trandolapril may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Trandolapril.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Trandolapril.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Trandolapril.
Obinutuzumab Trandolapril may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Trandolapril.
Rituximab Trandolapril may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Trandolapril.
Phentermine Phentermine may decrease the antihypertensive activities of Trandolapril.
Midodrine Midodrine may decrease the antihypertensive activities of Trandolapril.
Eletriptan Eletriptan may decrease the antihypertensive activities of Trandolapril.
Isoetharine Isoetharine may decrease the antihypertensive activities of Trandolapril.
Methysergide Methysergide may decrease the antihypertensive activities of Trandolapril.
Cabergoline Cabergoline may decrease the antihypertensive activities of Trandolapril.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Trandolapril.
Etomidate Etomidate may decrease the antihypertensive activities of Trandolapril.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Trandolapril.
Dihydroergotamine Dihydroergotamine may decrease the antihypertensive activities of Trandolapril.
Amitriptyline Amitriptyline may decrease the antihypertensive activities of Trandolapril.
Protriptyline Protriptyline may decrease the antihypertensive activities of Trandolapril.
Methylergometrine Methylergometrine may decrease the antihypertensive activities of Trandolapril.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Trandolapril.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Trandolapril.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Trandolapril.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Trandolapril.
Promazine Promazine may decrease the antihypertensive activities of Trandolapril.
Droperidol Droperidol may decrease the antihypertensive activities of Trandolapril.
Buspirone Buspirone may decrease the antihypertensive activities of Trandolapril.
Nortriptyline Nortriptyline may decrease the antihypertensive activities of Trandolapril.
Amoxapine Amoxapine may decrease the antihypertensive activities of Trandolapril.
Doxapram Doxapram may decrease the antihypertensive activities of Trandolapril.
Atropine Atropine may decrease the antihypertensive activities of Trandolapril.
Lisuride Lisuride may decrease the antihypertensive activities of Trandolapril.
Metaraminol Metaraminol may decrease the antihypertensive activities of Trandolapril.
Trazodone Trazodone may decrease the antihypertensive activities of Trandolapril.
Epinephrine Epinephrine may decrease the antihypertensive activities of Trandolapril.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Trandolapril.
Ergotamine Ergotamine may decrease the antihypertensive activities of Trandolapril.
Nicergoline Nicergoline may decrease the antihypertensive activities of Trandolapril.
Methoxamine Methoxamine may decrease the antihypertensive activities of Trandolapril.
Trimipramine Trimipramine may decrease the antihypertensive activities of Trandolapril.
Propiomazine Propiomazine may decrease the antihypertensive activities of Trandolapril.
Alfentanil Alfentanil may decrease the antihypertensive activities of Trandolapril.
Fentanyl Fentanyl may decrease the antihypertensive activities of Trandolapril.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Trandolapril.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Trandolapril.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Trandolapril.
Dobutamine Dobutamine may decrease the antihypertensive activities of Trandolapril.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Trandolapril.
Benzphetamine Benzphetamine may decrease the antihypertensive activities of Trandolapril.
Ritodrine Ritodrine may decrease the antihypertensive activities of Trandolapril.
Terbutaline Terbutaline may decrease the antihypertensive activities of Trandolapril.
Flupentixol Flupentixol may decrease the antihypertensive activities of Trandolapril.
Bitolterol Bitolterol may decrease the antihypertensive activities of Trandolapril.
Quinidine Quinidine may decrease the antihypertensive activities of Trandolapril.
Almotriptan Almotriptan may decrease the antihypertensive activities of Trandolapril.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Trandolapril.
Salmeterol Salmeterol may decrease the antihypertensive activities of Trandolapril.
Naratriptan Naratriptan may decrease the antihypertensive activities of Trandolapril.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Trandolapril.
Formoterol Formoterol may decrease the antihypertensive activities of Trandolapril.
Dopamine Dopamine may decrease the antihypertensive activities of Trandolapril.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Trandolapril.
Albuterol Salbutamol may decrease the antihypertensive activities of Trandolapril.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Trandolapril.
Ergoloid mesylate Ergoloid mesylate may decrease the antihypertensive activities of Trandolapril.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Trandolapril.
Arbutamine Arbutamine may decrease the antihypertensive activities of Trandolapril.
Dutasteride Dutasteride may decrease the antihypertensive activities of Trandolapril.
Doxepin Doxepin may decrease the antihypertensive activities of Trandolapril.
Nefazodone Nefazodone may decrease the antihypertensive activities of Trandolapril.
Desipramine Desipramine may decrease the antihypertensive activities of Trandolapril.
Pergolide Pergolide may decrease the antihypertensive activities of Trandolapril.
Finasteride Finasteride may decrease the antihypertensive activities of Trandolapril.
Ergometrine Ergometrine may decrease the antihypertensive activities of Trandolapril.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Trandolapril.
Paliperidone Paliperidone may decrease the antihypertensive activities of Trandolapril.
Arformoterol Arformoterol may decrease the antihypertensive activities of Trandolapril.
Fenoterol Fenoterol may decrease the antihypertensive activities of Trandolapril.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Trandolapril.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Trandolapril.
Ephedrine Ephedrine may decrease the antihypertensive activities of Trandolapril.
Mephentermine Mephentermine may decrease the antihypertensive activities of Trandolapril.
Procaterol Procaterol may decrease the antihypertensive activities of Trandolapril.
Yohimbine Yohimbine may decrease the antihypertensive activities of Trandolapril.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Trandolapril.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Trandolapril.
Bambuterol Bambuterol may decrease the antihypertensive activities of Trandolapril.
MMDA MMDA may decrease the antihypertensive activities of Trandolapril.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Trandolapril.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Trandolapril.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Trandolapril.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Trandolapril.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Trandolapril.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Trandolapril.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Trandolapril.

Target Protein

Angiotensin-converting enzyme ACE

Referensi & Sumber

Synthesis reference: 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.
Artikel (PubMed)
  • PMID: 19286752
    Berl T: Review: renal protection by inhibition of the renin-angiotensin-aldosterone system. J Renin Angiotensin Aldosterone Syst. 2009 Mar;10(1):1-8. doi: 10.1177/1470320309102747.
  • PMID: 8480624
    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.
  • PMID: 19337528
    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.
  • PMID: 12852701
    Guay DR: Trandolapril: a newer angiotensin-converting enzyme inhibitor. Clin Ther. 2003 Mar;25(3):713-75.
  • PMID: 7527096
    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.
  • PMID: 16114984
    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.
  • PMID: 18855271
    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. doi: 10.1080/10641960802251941.
  • PMID: 8576937
    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.
Menampilkan 8 dari 12 artikel.

Contoh Produk & Brand

Produk: 114 • International brands: 0
Produk
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