Spirapril
ACE Inhibitor (angiotensin Converting Enzyme Inhibitor); Prodrug (esterified Dipeptide Mimetic)Rx: PrescriptionCompound: Approved
Also known as: Renormax, SCH-33861
Summary
Spirapril is an ACE inhibitor prodrug used in the treatment of hypertension. It is converted in vivo to its active diacid form, spiraprilat. It has a long duration of action and is excreted via both renal and hepatic routes, making it potentially useful in patients with renal impairment.
Mechanism of Action
Spirapril is a prodrug hydrolyzed to spiraprilat, which competitively inhibits angiotensin-converting enzyme (ACE), blocking conversion of angiotensin I to angiotensin II. This reduces vasoconstriction and aldosterone secretion, lowering blood pressure.
Routes of Administration
Oral
Goals & Uses
- Heart failureCardiovascularLow
- Hypertension managementCardiovascularHigh
- Renoprotection in chronic kidney diseaseNephrologyLow
Contraindications
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- History of ACE inhibitor-induced angioedemaImmunologic/AllergicHigh
- Severe hypersensitivity to spirapril or excipientsAllergyHigh
- Concurrent use of aliskiren in diabetic patientsDrug InteractionHigh
- Bilateral renal artery stenosisVascular/RenalHigh
Adverse Effects
- Hypotension (first-dose effect)CardiovascularCommon
- Renal impairmentRenalUncommon
- HyperkalemiaElectrolyte ImbalanceUncommon
- Dry coughRespiratoryCommon
- AngioedemaImmunologicRare
- Dizziness/headacheNeurologicalCommon
Drug Interactions
- Potassium-sparing diuretics (e.g., spironolactone, amiloride)High
- AliskirenHigh
- NSAIDsModerateMay increase renal risk in susceptible patients
- Antidiabetic agents (insulin, sulfonylureas)Moderate
- LithiumHigh
Population Constraints
- Pediatric patientsAgeRelative
- Patients with severe renal artery stenosisRenalAbsolute
- Patients with severe hepatic impairmentHepaticRelative
- Elderly patientsAgeRelative
- Pregnant womenReproductiveAbsolute
Regulatory Status
- European UnionApprovedApproved: HypertensionApproved in select EU member states (e.g., Scandinavia, some Eastern European countries) under brand name Renormax.
- United StatesUnapprovedNot approved by the FDA; no NDA filed or approved.
- United KingdomUnknownLimited availability data post-Brexit; not a commonly listed product in MHRA databases.
Approved in several European countries for hypertension. Not approved by the FDA in the United States. Available in limited markets.
Evidence & Sources
No sources recorded yet.