Trandolapril

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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. weight	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®.

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

[edit] 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%.

[edit] 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.

[edit] 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.

[edit] 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.

[edit] Contraindications and Precautions

See ACE inhibitors for more information.

[edit] Pregnancy and Lactation

[edit] 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

[edit] 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)

[edit] References

• Trandolapril Information - rxlist.com (Rxlist.com, The Internet Drug Index)

ACE inhibitors (C09A) edit
Benazepril, Captopril, Enalapril, Fosinopril, Lisinopril, Perindopril, Quinapril, Ramipril, Spirapril, Trandolapril