Trandolapril

Source: Wikipedia, the free encyclopedia.
"Mavik" redirects here. Not to be confused with Mavic.
Trandolapril
Clinical data
Trade namesMavik, others
AHFS/Drugs.comMonograph
MedlinePlusa697010
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Protein bindingTrandolapril 80%
(independent of concentration)
Trandolaprilat 65 to 94%
(concentration-dependent)
MetabolismLiver
Elimination half-life6 hours (trandolapril)
10 hours (trandolaprilat)
ExcretionFecal and Kidney
Identifiers
  • (2S,3aR,7aS)-1-[(2S)-2-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}propanoyl]-octahydro-1H-indole-2-carboxylic acid
JSmol)
Melting point119 to 123 °C (246 to 253 °F)
  • O=C(OCC)[C@@H](N[C@H](C(=O)N1[C@H](C(=O)O)C[C@H]2CCCC[C@H]12)C)CCc3ccccc3
  • InChI=1S/C24H34N2O5/c1-3-31-24(30)19(14-13-17-9-5-4-6-10-17)25-16(2)22(27)26-20-12-8-7-11-18(20)15-21(26)23(28)29/h4-6,9-10,16,18-21,25H,3,7-8,11-15H2,1-2H3,(H,28,29)/t16-,18+,19-,20-,21-/m0/s1 checkY
  • Key:VXFJYXUZANRPDJ-WTNASJBWSA-N checkY
  (verify)

Trandolapril is an ACE inhibitor used to treat high blood pressure. It may also be used to treat other conditions. It is similar in structure to another ramipril but has a cyclohexane group. It is a prodrug that must be metabolized into its active form. It has a longer half-life when compared to other agents in this class.

It was patented in 1981 and approved for medical use in 1993.[1] It is marketed by Abbott Laboratories under the brand name Mavik.

Side effects

fatigue
.

Possible drug interactions

Patients also on

thiazide diuretics and increase serum potassium when used alone. Therefore, hyperkalemia
is a possible risk. Increased serum lithium levels can occur in patients who are also on lithium.

Contraindications and precautions

Main article: ACE inhibitor § 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.[2]

Pharmacology

Trandolaprilat — the active metabolite of trandolapril

Trandolapril is a

renin–angiotensin–aldosterone system
. Trandolapril has a half-life of about six hours, while trandolaprilat has a half life of about ten hours. 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

Main article: ACE inhibitor

Trandolapril acts by

angiotensin converting enzyme (ACE), a key enzyme in the renin–angiotensin system
. which plays an important role in regulating blood pressure.

References

  1. ISBN 9783527607495
    .
  2. PMID 19759524
    .

External links
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