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Trandolapril
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| Systematic (IUPAC) name | |
| (2S,3aR,7aS)-1-[(2S)-2-[[(1S)-1-ethoxycarbonyl-3-phenyl- propyl]amino]propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole- 2-carboxylic acid |
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| Identifiers | |
| CAS number | |
| ATC code | C09 |
| PubChem | |
| DrugBank | |
| 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. |
D(US) |
| 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.
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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.
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)
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Wikipedia content modification information:
- This page was last modified on 23 June 2008, at 11:19.
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