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ACE inhibitors

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ACE inhibitors

  • block bradykinin kinase as well as ACE and increase the concentration of bradykinin (potent vasodilator)
  • do not cause reflex tachycardia. Distinct advantage over direct vasodilators

Clinical uses

  • hypertension. Particularly effective in renovascular hypertension but also effective in anephric patients and in low renin hypertension; probably the result of local effects on tissue ACE
  • chronic heart failure: results in improved prognosis as well as improved symptom control
  • post MI in all patients who have had pulmonary oedema in association with MI, however transient. Thought to relate to an effect on ventricular remodelling

Contraindications

  • bilateral renal artery stenosis or stenosis in a solitary kidney

Captopril

  • contains as sulphydryl group that interacts with Zn2+ of ACE binding site with greater affinity than angiotensin I
  • given sublingually has an onset of action in 20-30 min with maximum effect after approx 50 min and duration of action of about 4 h
  • adverse effects include agranulocytosis, Stevens-Johnson

Enalapril

  • sulphydryl group of captopril substituted by phenylalanine
  • pro-drug which is metabolized in liver to enalaprilat

Enalaprilat

  • active metabolite of enalapril
  • available as an IV preparation
  • IV dose 1-5 mg. Decrease in patients with renal impairment, renovascular hypertension and those on diuretics
  • onset of action 15 min after IV administration with duration of 6-12 h
  • hypotensive response is variable and is partly dependent on intravascular volume
  • excreted by kidney

Further reading

Chui PT, Low JM. Acute hypertension and vasodilators. In Oh TE (ed), Intensive Care Manual, 4th Ed., Butterworth Heinemann, Oxford, 1997, pp 153-62


© Charles Gomersall December 1999

 

©Charles Gomersall, April, 2014 unless otherwise stated. The author, editor and The Chinese University of Hong Kong take no responsibility for any adverse event resulting from the use of this webpage.
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