Imidapril


Generic Medicine Info
Indications and Dosage
Oral
Hypertension
Adult: Initially, 5 mg once daily. 1st dose preferably given at bedtime to avoid precipitous fall in BP. Maintenance: 10 mg/day. Max: 20 mg/day. Patients on diuretics: 2.5 mg daily.
Elderly: Initially, 2.5 mg daily. Max Dose: 10 mg daily.
Renal Impairment
Initially, 2.5 mg/day.
Hepatic Impairment
Initially, 2.5 mg/day.
Administration
Should be taken on an empty stomach. Take 15 min before meals. However, when initiating therapy, 1st dose should be given at bedtime.
Contraindications
History of angioneurotic oedema related w/ previous ACE inhibitor therapy. Hereditary or idiopathic angioedema. Pregnancy.
Special Precautions
Renal artery stenosis; collagen vascular disease, heart failure; at risk for hypotension (e.g. volume-depleted patients). Renal and hepatic impairment. Lactation.
Adverse Reactions
Dizziness, headache, fatigue, somnolence, GI and taste disturbances, persistent dry cough and other upper resp tract symptoms, hyperkalaemia, hyponatraemia, blood disorders (e.g. neutropenia, agranulocytosis, anaemia, thrombocytopenia).
Potentially Fatal: Severe hypotension, which could result in MI or stroke in patients w/ ischaemic heart disease or cerebrovascular disease. Rarely, fulminant hepatic necrosis.
MonitoringParameters
Assess renal function before and during the 1st wk of therapy. Monitor serum electrolytes and creatinine levels frequently.
Overdosage
Symptoms: Severe hypotension, bradycardia, shock, stupor, electrolyte disturbances and renal failure. Management: Perform haemodialysis and gastric lavage. Administer adsorbents and Na sulfate w/in 30 min of ingestion.
Drug Interactions
Marked hypotension w/ diuretics, other antihypertensives, and vasodilators, TCAs, neuroleptics. Additive hyperkalaemic effects w/ K-sparing diuretics, K supplements, and K-containing salt substitutes. Reduced antihypertensive effects or additive nephrotoxic effects w/ NSAIDs, rifampicin, sympathomimetics. Increased lithium levels and toxicity. May cause nitritoid reactions w/ injectable gold (Na aurothiomalate).
Action
Description: Imidapril, a prodrug of imidaprilat, inhibits ACE from converting angiotensin I to angiotension II (a potent vasoconstrictor) resulting in increased plasma renin activity and reduced aldosterone (a hormone that causes water and Na retention) secretion. This promotes vasodilation and BP reduction. It may also inhibit the degradation of bradykinin.
Pharmacokinetics:
Absorption: Rapidly but incompletely absorbed (approx 70%) from the GI tract. Reduced absorption w/ food. Absolute bioavailability: Approx 42% (imidaprilat). Time to peak plasma concentration: Approx 7 hr (imidaprilat).
Distribution: Plasma protein binding: 85% (imidapril); 53% (imidaprilat).
Metabolism: Hepatically hydrolysed to imidaprilat (active metabolite).
Excretion: Via urine (approx 40%); faeces (approx 50%). Terminal half-life: >24 hr.
Storage
Store below 30°C.
References
Anon. Imidapril: International Drug Information. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 21/11/2013.

Buckingham R (ed). Imidapril. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/11/2013.

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