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Trandolapril



Trandolapril
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
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.

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®.

Additional recommended knowledge

Contents

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

References

  • Trandolapril Information - rxlist.com (Rxlist.com, The Internet Drug Index)
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Trandolapril". A list of authors is available in Wikipedia.
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