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14-September-2008 18:02:41 - Trandolapril Trandolapril Systematic IUPAC name 2S,3aR,7aS-1-2S-2-1S-1-ethoxycarbonyl-3-phenyl- propylaminopropanoyl-2,3,3a,4,5,6,7,7a-octahydroindole- 2-carboxylic acid Identifiers CAS number 87679-37-6 ATC code C09AA10 PubChem 5484727 DrugBank APRD01269 Chemical data Formula C24H34N2O5 Mol. mass 430.537 g/mol Pharmacokinetic data Bioavailability ? Protein binding Trandolapril 80% independent of concentration Trandolaprilat 65 to 94% concentration-dependent Metabolism Hepatic Half life 6 hours trandolapril 10 hours trandolaprilat Excretion Fecal and renal Therapeutic considerations Pregnancy cat. DUS Legal status ℞ Prescription only Routes Oral 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. Contents 1 Pharmacology 2 Mode of action 3 Side effects 4 Possible Drug Interactions 5 Contraindications and Precautions 6 Pregnancy and Lactation 6.1 Category D 7 External links 8 References Pharmacology Trandolapril is a prodrug that is deesterified to trandolaprilat. It is believed to exert its antihypertenive 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. Trandolaprilat has about 8 times the activity of its parent drug. Approximately 1/3 of Trandolapril and its metabolites are excreted in the urine, and about 2/3 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 RAS pathway which plays an important role in regulating blood pressure. See ACE inhibitors for more information. Side effects Side effects reported for Trandolapril include nausea, vomiting, or 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. Trandolapril 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. For more information see angiotensin converting enzyme ACE inhibitors. Contraindications and Precautions See ACE inhibitors for more information. Pregnancy and Lactation Category D Trandolapril is teratogenic and can cause birth defects and even death of the developing fetus. The highest risk to the fetus is during the second and third trimester. When pregnancy is detected, Trandolapril should be discontinued as soon as possible. Trandolapril should not be administed to nursing mothers. Main article: ACE inhibitor External links Mavik PDF from manufacturer's website Tarka PDF from manufacturer's website Trandolapril patient information Trandolapril Information - rxlist.com Rxlist.com, The Internet Drug Index References Trandolapril Information - rxlist.com Rxlist.com, The Internet Drug Index v d e Agents acting on the renin-angiotensin system C09 ACE inhibitors Alacepril Benazepril Captopril Cilazapril Delapril Enalapril Fosinopril Imidapril Lisinopril Moexipril Perindopril Quinapril Ramipril Rentiapril Spirapril Temocapril Trandolapril Zofenopril Angiotensin II receptor antagonists AIIRA Azilsartan Candesartan Eprosartan Irbesartan Losartan Olmesartan Tasosartan Telmisartan Valsartan Renin inhibitors Aliskiren Remikiren Retrieved from http://en..org/wiki/Trandolapril Categories: ACE inhibitors | Prodrugs Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Hrvatski Italiano Magyar This page was last modified on 23 June 2008, at 11:19
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