Lisinopril
(British Approved Name, US Adopted Name, rINN)
Drug Nomenclature
International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):
Pharmacopoeias. In Europe, Japan, and US.
European Pharmacopoeia, 6th ed., 2008 and Supplements 6.1 and 6.2 (Lisinopril Dihydnate). Awhite or almost white crystalline powder. Soluble in water; practically insoluble in dehydrated alcohol and in acetone; sparingly soluble in methyl alcohol.
The United States Pharmacopeia 31, 2008, and Supplements 1 and 2 (Lisinopril). A white crystalline powder. Soluble 1 in 10 of water and 1 in 70 of methyl alcohol; practically insoluble in alcohol, in acetone, in acetonitrile, in chloroform, and in ether.
Suspension. The US licensed prescribing information provides the following method for making 200 mL of a suspension containing lisinopril 1 mg/mL. Add 10 mL of purified water to a polyethylene terephthalate bottle containing ten 20-mg tablets (Prinivil, Merck or Zestril, AstraZeneca) and shake for at least 1 minute. Add 30 mL of Bicitra (Alza USA) and 160mL of Ora-Sweet SF (Paddock, USA) to the bottle and gently shake for several seconds. The suspension should be stored at or below 25° and can be stored for up to 4 weeks. Studies of the characteristics of this and other liquid dosage forms of lisinopril have been published.
Adverse Effects, Treatment, and Precautions
As for ACE inhibitors.
Porphyria. Lisinopril has been associated with acute attacks of porphyria and is considered unsafe in porphyric patients.
Interactions
As for ACE inhibitors.
Pharmacokinetics
Lisinopril is slowly and incompletely absorbed after oral doses. About 25% of a dose is absorbed on average, but the absorption varies considerably between individuals, ranging from about 6 to 60%. It is already an active diacid and does not need to be metabolised in vivo. Peak concentrations in plasma are reported to occur after about 7 hours. Lisinopril is reported not to be significantly bound to plasma proteins. It is excreted unchanged in the urine. The effective half-life for accumulation after multiple doses is 12 hours in patients with normal renal function. Lisinopril is removed by haemodialysis.
Uses and Administration
Lisinopril is an ACE inhibitor. It is used in the treatment of hypertension and heart failure, prophylactically after myocardial infarction, and in diabetic nephropathy (see Kidney Disorders).
The haemodynamic effects of lisinopril are seen within 1 to 2 hours of a single oral dose and the maximum effect occurs after about 6 hours, although the full effect may not develop for several weeks during chronic dosing. The haemodynamic action lasts for about 24 hours after once-daily dosing. Lisinopril is given orally as the dihydrate, but doses are expressed in terms of the anhydrous substance. Lisinopril 2.72 mg as the dihydrate is equivalentto about2.5 mg of anhydrous lisinopril. The dose of lisinopril should be reduced in patients with renal impairment (see below).
In the treatment of hypertension, the usual initial dose is 10 mg daily. Since there may be a precipitous fall in blood pressure in some patients when starting therapy with an ACE inhibitor, the first dose should preferably be given at bedtime. Hypotension is particularly likely in patients with renovascular hypertension, volume depletion, heart failure, or severe hypertension and such patients should be given a lower initial dose of 2.5 to 5 mg once daily. Patients taking diuretics should have the diuretic withdrawn 2 or 3 days before lisinopril is started and resumed later if required; if this is not possible, an initial dose of 5 mg once daily should be given. The usual maintenance dose is 20 mg given once daily, though up to 80 mg daily may be given if necessary.
In the management of heart failure, severe first-dose hypotension on introduction of an ACE inhibitor is common in patients on loop diuretics, but their temporary withdrawal may cause rebound pulmonary oedema. Thus treatment should be started with a low dose under close medical supervision. Lisinopril is given in an initial dose of 2.5 mg daily. In the USA an initial dose of 5 mg daily is suggested. Usual maintenance doses range from 5 to 40 mg daily. After myocardial infarction, treatment with lisinopril may be started within 24 hours of the onset of symptoms in an initial dose of 5 mg once daily for two days, then increased to 10 mg once daily. An initial dose of 2.5 mg once daily is recommended for patients with a low systolic blood pressure.
In the management of diabetic nephropathy, hypertensive type 2 diabetics with microalbuminuria may be given a dose of 10 mg once daily, increased if necessary to 20 mg once daily to achieve a sitting diastolic blood pressure below 90 mmHg.
Administration in children. Lisinopril has been reported to be an effective and well-tolerated antihypertensive in children 6 years of age and older, although it has been used successfully in younger children. US licensed product information recommends an oral starting dose for lisinopril of 70 micrograms/kg (up to 5 mg) once daily for children 6 years of age and older (but see also Administration in Renal Impairment, below). The BNFC recommends similar doses for children aged 6 to 12 years and states that this dose may be increased at intervals of 1 to 2 weeks to a maximum of 600 micrograms/kg or 40 mg once daily. For children between 12 and 18 years of age the BNFC recommends an initial dose of 2.5 mg daily increased as necessary to a maximum of 40 mg daily.
In the treatment of heart failure in children between 12 and 18 years of age the BNFC recommends an initial dose of 2.5 mg daily increased as necessary to a usual maintenance dose of 5 to 20 mg daily.
Administration in renal impairment. In adult patients with renal impairment, the initial dose of lisinopril should be reduced depending on the creatinine clearance (CC) as follows:
• CC 31 to 80 mL/minute: 5 to 10 mg once daily
• CC 10 to 30 mL/minute: 2.5 to 5 mg once daily
• CC less than 10 mL/minute or on dialysis: 2.5 mg once daily The dose should be adjusted according to response, to a maximum of 40 mg once daily.
US licensed prescribing information states that lisinopril should not be given to children with a glomerular filtration rate of less than 30 mL/minute per 1.73 m2 but gives no guidance on dosage in other children with renal impairment.
Preparations
British Pharmacopoeia, 2008: Lisinopril Tablets;
The United States Pharmacopeia 31, 2008, and Supplements 1 and 2: Lisinopril Tablets.
Single-ingredient Preparations
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.
Argentina: Doxapril; Lisinal; Sedotensil; Tensopril; Tersif; Zestril; Australia: Fibsol; Liprace; Lisinobell; Lisodur; Prinivil; Zestril; Austria: Acemin; Acetan; Hypomed¤; Lisihexal; Lisinostad; Lisinotyrol; Prinivil; Belgium: Novatec; Zestril; Brazil: Linopril¤; Listril; Novral¤; Prinivil; Vasojet; Zestril; Zinopril; Canada: Prinivil; Zestril; Chile: Acerdil; Lipreren; Presokin; Tonotensil; Zestril; Czech Republic: Dapril; Diroton; Irumed; Listril; Prinivil; Denmark: Acepril; Lanatin; Lisinogen; Vivatec; Zestril; Finland: Lisipril; Vivatec; Zestril; France: Prinivil; Zestril; Germany: Acerbon; Coric; Lisi Lich; Lisi-Puren; Lisi; Lisibeta; Lisigamma; Lisihexal; Lisodura; Greece: Adicanil; Axelvin; Gnostoval; Icoran; Landolaxin¤; Leruze; Lisinospes; Nafordyl; Perenal; Press-12; Pressuril; Prinivil; Terolinal; Thriusedon; Tivirlon; Vercol; Veroxil; Z-Bec; Zestril; Hong Kong: Acepril; Prinivil; Zestril; Hungary: Conpres; Lisopress; India: Biopril; Cipril; Linoril; Linvas; Lipril; Lisoril; Normopril; Ireland: Carace; Lisopress; Lispril; Zesger; Zestan; Zestril; Israel: Tensopril; Italy: Alapril; Prinivil; Zestril; Malaysia: Prinivil¤; Ranopril; Zestril; Mexico: Alfaken; Priniser; Prinivil; Zestril; Netherlands: Novatec; Zestril; Norway: Vivatec; Zestril; New Zealand: Prinivil; Zestril¤; Portugal: Ecapril; Farpresse; Lipril; Prinivil; Zestril; Russia: Dapril (Даприл); Diroton (Диротон); Lisoril (Лизорил); Sinopril (Синоприл); South Africa: Prilosin; Prinivil; Renotens; Sinopren; Zestomax¤; Zestril; Zetomax; Singapore: Dapril; Lisdene; Lisoril; Prinivil; Zestril; Spain: Doneka; Iricil; Likenil; Prinivil; Secubar¤; Tensikey; Zestril; Sweden: Vivatec; Zestril; Switzerland: Lisitril; Lisopril; Prinil; Zestril; Thailand: Lisdene; Lispril; Zestril; United Kingdom: Carace; Zestril; United States: Prinivil; Zestril; Venezuela: Lisilet; Prinivil; Rantex; Tonoten
Multi-ingredient Preparations
Argentina: Tensopril D; Zestoretic; Austria: Acecomb; Co-Acetan; Prinzide¤; Zestoretic; Belgium: Novazyd; Zestoretic; Brazil: Lisinoretic; Lisoclor; Lisonotec; Prinzide; Zestoretic; Canada: Prinzide; Zestoretic; Chile: Acerdil-D; Tonotensil D; Zestoretic¤; Denmark: Vivazid; Zestoretic; Finland: Acercomp; Lisipril Comp; Vivatec Comp; France: Prinzide; Zestoretic; Germany: Acercomp; Coric Plus; Greece: Prinzide; Zestoretic; Hong Kong: Zestoretic; India: Amlopres L; Amlosafe-LS; Biopril-AM; Calchek L; Cipril-H; Lisoril-5HT; Ireland: Carace Plus; Lispril-hydrochlorothiazide; Zestoretic; Italy: Nalapres; Prinzide; Zestoretic; Mexico: Prinzide; Zestoretic; Netherlands: Lisidigal HCT; Novazyd; Zestoretic; Norway: Vivatec Comp; Zestoretic; New Zealand: Prinzide¤; Zestoretic¤; Portugal: Ecamais; Prinzide; Zestoretic; South Africa: Zestoretic; Spain: Doneka Plus; Iricil Plus; Prinivil Plus; Secubar Diu; Tensikey Complex; Zestoretic; Sweden: Zestoretic; Switzerland: Prinzide; Zestoretic; United Kingdom: Carace Plus; Caralpha; Lisicostad; Zestoretic; United States: Prinzide; Zestoretic
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