Imidapril

Source: Wikipedia, the free encyclopedia.
Imidapril
Clinical data
Trade namesTanatril, others
AHFS/Drugs.comUK Drug Information
Routes of
administration
By mouth
ATC code
Legal status
Legal status
  • CA: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability42% (imidaprilat)
Protein binding85% (imidapril),
53% (imidaprilat)
MetabolitesImidaprilat (active metabolite)
Elimination half-life2 hrs (imidapril),
24 hrs (imidaprilat)
Excretion40% Kidney, 50% bile duct
Identifiers
  • (4S)-3-[(2S)-2-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]aminopropanoyl-1-methyl-2-oxoimidazolidine-4-carboxylic acid
JSmol)
Melting point139 to 140 °C (282 to 284 °F)
  • O=C(O)[C@H]2N(C(=O)[C@@H](N[C@H](C(=O)OCC)CCc1ccccc1)C)C(=O)N(C)C2
  • InChI=1S/C20H27N3O6/c1-4-29-19(27)15(11-10-14-8-6-5-7-9-14)21-13(2)17(24)23-16(18(25)26)12-22(3)20(23)28/h5-9,13,15-16,21H,4,10-12H2,1-3H3,(H,25,26)/t13-,15-,16-/m0/s1 ☒N
  • Key:KLZWOWYOHUKJIG-BPUTZDHNSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Imidapril, sold under the brand name Tanatril among others, is an

chronic heart failure.[1]

It was patented in 1982 and approved for medical use in 1993.[2]

Contraindications

Contraindications are hypersensitivity against ACE inhibitors, especially if it has resulted in

idiopathic or hereditary angioedema; kidney failure; the second and third trimesters in pregnancy; and combination with the drug aliskiren in people with diabetes.[3][4]

Adverse effects

Common adverse effects are similar to other antihypertensive drugs and include headache,

drowsiness. A dry cough is common as with all ACE inhibitors.[3][4] Other possible adverse effects are described at ACE inhibitor#Adverse effects
.

Interactions

No interaction studies have been conducted except with

hypoglycaemia (low blood glucose levels).[3][4]

Pharmacology

Mechanism of action

Pharmacokinetics

About 70% of the ingested imidapril is absorbed quickly from the gut; this percentage is reduced significantly when taken with a fatty meal. It reaches highest blood plasma concentrations after two hours and has a biological half-life of two hours. The substance is a prodrug and is activated to imidaprilat, which reaches highest plasma concentrations after 7 hours, has an initial half-life of 7 to 9 hours and a terminal half-life of more than 24 hours. The absolute bioavailability of imidaprilat is 42%.[3][4]

About 40% of the drug is excreted via the urine and 50% via the bile and faeces.[3][4]

Imidaprilat, the active metabolite

References

  1. S2CID 241327668
    .
  2. .
  3. ^ a b c d e Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag. 2019. Tanatril 10 mg-Tabletten.
  4. ^ .