Trandolapril

Trandolapril
Clinical data
Trade names Mavik
AHFS/Drugs.com Monograph
MedlinePlus a697010
Pregnancy
category
  • US: D (Evidence of risk)
    Routes of
    administration    		 Oral
    ATC code
    Legal status
    Legal status
    • In general: ℞ (Prescription only)
    Pharmacokinetic data
    Protein binding Trandolapril 80%
    (independent of concentration)
    Trandolaprilat 65 to 94%
    (concentration-dependent)
    Metabolism Hepatic
    Elimination half-life 6 hours (trandolapril)
    10 hours (trandolaprilat)
    Excretion Fecal and renal
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    ECHA InfoCard 100.108.532 Edit this at Wikidata
    Chemical and physical data
    Formula C24H34N2O5
    Molar mass 430.537 g/mol
    3D model (JSmol)
    Melting point 119 to 123 °C (246 to 253 °F)
      (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 under the brand name Mavik.

    Pharmacology

    Trandolaprilat — the active metabolite of trandolapril

    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

    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

    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

    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

    Pregnancy and lactation

    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 administered to nursing mothers.

    Additional effects

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

    References

    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.
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