Trandolapril

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Trandolapril
Trandolapril.svg
Systematic (IUPAC) name
(2S,3aR,7aS)-1-[(2S)-2-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}propanoyl]-octahydro-1H-indole-2-carboxylic acid
Clinical data
Trade names Mavik
AHFS/Drugs.com monograph
MedlinePlus a697010
Pregnancy cat.
Legal status
  • Prescription only
Routes Oral
Pharmacokinetic data
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
Identifiers
CAS number 87679-37-6 YesY
ATC code C09AA10
PubChem CID 5484727
DrugBank DB00519
ChemSpider 4588590 YesY
UNII 1T0N3G9CRC YesY
KEGG D00383 YesY
ChEMBL CHEMBL1519 YesY
Chemical data
Formula C24H34N2O5 
Mol. mass 430.537 g/mol
Physical data
Melt. point 119–123 °C (246–253 °F)
 YesY (what is this?)  (verify)

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.

Pharmacology[edit]

Trandolapril is a prodrug that is de-esterified to trandolaprilat. It is believed to exert its antihypertensive 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 h. Trandolaprilat has about eight times the activity of its parent drug. About one-third of trandolapril and its metabolites are excreted in the urine, and about two-thirds of trandolapril and its metabolites are excreted in the feces. Serum protein binding of trandolapril is about 80%.

Mode of action[edit]

Main article: ACE inhibitor

Trandolapril acts by competitive inhibition of angiotensin converting enzyme (ACE), a key enzyme in the renin-angiotensin system which plays an important role in regulating blood pressure.

Side effects[edit]

Side effects reported for trandolapril include nausea, vomiting, diarrhea, headache, dry cough, dizziness or lightheadedness when sitting up or standing, hypotension, or fatigue.

Possible drug interactions[edit]

Patients also on diuretics may experience an excessive reduction of blood pressure after initiation of therapy with trandolapril. It 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.

Contraindications and precautions[edit]

Pregnancy and lactation[edit]

Trandolapril is teratogenic (US: pregnancy category D) and can cause birth defects and even death of the developing fetus. The highest risk to the fetus is during the second and third trimesters. When pregnancy is detected, trandolapril should be discontinued as soon as possible. Trandolapril should not be administed to nursing mothers.

Additional effects[edit]

Combination therapy with paricalcitol and trandolapril has been found to reduce fibrosis in obstructive uropathy.[1]

References[edit]

  1. ^ Tan, X; He, W; Liu, Y (2009). "Combination therapy with paricalcitol and trandolapril reduces renal fibrosis in obstructive nephropathy". Kidney international 76 (12): 1248–57. doi:10.1038/ki.2009.346. PMID 19759524. 

External links[edit]