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an ACE inhibiting drug (trade names Prinival or Zestril) administered as an antihypertensive and after heart attacks (同)Prinival, Zestril

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/06/23 09:31:39」(JST)

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Lisinopril (/laɪˈsɪnəprɪl/ ly-SIN-ə-pril) is a drug of the angiotensin-converting enzyme (ACE) inhibitor class used primarily in treatment of hypertension, congestive heart failure, and heart attacks, and in preventing renal and retinal complications of diabetes. Its indications, contraindications, and side effects are as those for all ACE inhibitors.

Lisinopril was the third ACE inhibitor (after captopril and enalapril) and was introduced into therapy in the early 1990s.^[2] A number of properties distinguish it from other ACE inhibitors: It is hydrophilic, has a long half-life and tissue penetration, and is not metabolized by the liver.

Medical uses

Crystal Structure of Human Angiotensin Converting Enzyme in complex with lisinopril.

Lisinopril is typically used for the treatment of hypertension, congestive heart failure, acute myocardial infarction, and diabetic nephropathy.^[1]

Special populations

The dose must be adjusted in those with poor kidney function.^[3]

Contraindications

History of angioedema (hereditary or idiopathic)^[4]
Hypersensitivity reaction to lisinopril or any of other components found in its formulation^[5]
Concomitant use of aliskiren-containing drugs in patients with diabetes^[6]

Combination of aliskiren and lisinopril is contraindicated in patients with diabetes, and should be avoided in those with creatinine clearance less than 60ml/min. This combination may heighten the hyperkalemic, hypotensive, and nephrotoxic effects of lisinopril (and other ACE inhibitors). Therefore, serum potassium, blood pressure, and serum creatinine should be carefully monitored for all patients on this combination.

Adverse effects

Side effects, some of which are serious and require immediate medical attention, may include:^[7]

Chills, signs of infection
Dark urine (melanuria)
Decreased urination (oliguria)
Difficulty swallowing or breathing (signs of angioedema), allergic reaction (anaphylaxis)
Hoarseness
Itching
Yellowing of skin or eyes (jaundice)
Abdominal pain, bloating, vomiting
Chest pain or tightness, dizziness, lightheadedness, fainting
Dry cough
Fever
Joint pain
Rash
Diarrhea, nausea
Drowsiness, headache, tiredness
Muscle cramps
Dry mouth
Serious (possibly fatal) liver problems
Impotence^[8]
Dizziness
Faintness ^[9]

Lisinopril causes the kidneys to retain potassium, which may lead to hyperkalemia. From a study on eHealthMe of more than 1,000 patients with hyperkalemia when using it, the condition may happen more in older male users.^[10]

A rare but severe allergic reaction that affects the bowel wall and secondarily causes abdominal pain can occur. This "angioedema" reaction is very rare and must be given immediate medical attention.^[11]

Pregnancy and breastfeeding

Lisinopril has been assigned to pregnancy category D by the FDA for use during the second and third trimesters and to category C during the first trimester. Animal and human data have revealed evidence of embryolethality and teratogenicity associated with ACE inhibitors. No controlled data in human pregnancy are available. Congenital malformations have been reported with the use of ACE inhibitors during the first trimester of pregnancy, while fetal and neonatal toxicity, death, and congenital anomalies have been reported with their use during the second and third trimesters of pregnancy. If the patient becomes pregnant, lisinopril should be discontinued as soon as possible; it is considered contraindicated during pregnancy.

No data exist on the excretion of lisinopril into human milk. The manufacturer recommends, due to the potential for serious adverse reactions in nursing infants, a decision should be made to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. ^[12]

Lisinopril 40-mg oral tablet

Pharmacology

Lisinopril is the lysine-analog of enalapril. Unlike other ACE inhibitors, it is not a prodrug and is excreted unchanged in the urine. In cases of overdosage, it can be removed from circulation by dialysis.^[13]

Pharmacokinetics and metabolism

For adult patients, following oral administration of lisinopril, peak serum concentrations occur within about seven hours, although a trend to a small delay in time taken to reach peak serum concentrations in acute myocardial infarction patients was seen. Declining serum concentrations exhibit a prolonged terminal phase that does not contribute to drug accumulation. This terminal phase probably represents saturable binding to ACE and is not proportional to dose. Lisinopril does not appear to be bound to other serum proteins.

Lisinopril does not undergo metabolism and is excreted unchanged entirely in the urine. Based on urinary recovery, the mean extent of its absorption is approximately 25%, with large intersubject variability (6–60%) at all doses tested (5–80 mg). Lisinopril absorption is not influenced by the presence of food in the gastrointestinal tract. In patients with stable NYHA class II-IV congestive heart failure, its absolute bioavailability is reduced to about 16%, and the volume of distribution appears to be slightly smaller than that in normal subjects.

The oral bioavailability of lisinopril in patients with acute myocardial infarction is similar to that in healthy volunteers. Upon multiple dosing, it exhibits an effective half-life of accumulation of 12 hours.

Impaired renal function decreases elimination of lisinopril, which is excreted principally through the kidneys, but this decrease becomes clinically important only when the glomerular filtration rate is below 30 ml/min. Above this rate, the elimination half-life is little-changed. With greater impairment, however, peak and trough levels increase, time to peak concentration increases, and time to attain steady state is prolonged. Older patients, on average, have higher (around doubled) blood levels and area under the plasma concentration time curve than younger patients.

Brand names

Lisinopril was developed by Merck & Co., and is marketed worldwide as Prinivil or Tensopril, and by AstraZeneca as Zestril. In India, it is marketed by Micro Labs as Hipril. In the United States, a generic version is available. Like other ACE inhibitors, it is a synthetic functional and structural analog of a peptide derived from the venom of the jararaca, a Brazilian pit viper (Bothrops jararaca).^[14] Lisinopril can also be used in conjunction with the diuretic hydrochlorothiazide, and drugs that combine these two medications are available under the brand names Prinzide and Zestoretic.

References

^ ^a ^b "Lisinopril". The American Society of Health-System Pharmacists. Retrieved 3 April 2011.
^ Patchett A, Harris E, Tristram E, Wyvratt M, Wu M, Taub D, Peterson E, Ikeler T, ten Broeke J, Payne L, Ondeyka D, Thorsett E, Greenlee W, Lohr N, Hoffsommer R, Joshua H, Ruyle W, Rothrock J, Aster S, Maycock A, Robinson F, Hirschmann R, Sweet C, Ulm E, Gross D, Vassil T, Stone C (1980). "A new class of angiotensin-converting enzyme inhibitors". Nature 288 (5788): 280–3. doi:10.1038/288280a0. PMID 6253826.
^ "Lisinopril Dosage, Interactions, Side Effects, How to Use". HealthDigest.org.
^ Product Information: ZESTRIL(R) oral tablet, lisinopril oral tablet. AstraZeneca Pharmaceuticals LP, Wilmington, DE, 2005.
^ Product Information: ZESTRIL(R) oral tablet, lisinopril oral tablet. AstraZeneca Pharmaceuticals LP, Wilmington, DE, 2005.
^ Product Information: ZESTRIL(R) oral tablet, lisinopril oral tablet. AstraZeneca Pharmaceuticals LP, Wilmington, DE, 2005.
^ "Lisinopril Oral : Uses, Side Effects, Interactions, Pictures, Warnings & Dosing". WebMD. Retrieved 20 April 2010.
^ http://www.lisinopril.com/index.php?id=lisinopril_sideeffects
^ http://www.webmd.com/drugs/2/drug-6873/lisinopril-oral/details/list-sideeffects
^ "Hyperkalemia in the use of Lisinopril, who, when, how?". eHealthMe. Retrieved 31 August 2010.
^ http://www.ccjm.org/content/78/5/297.full
^ "Lisinopril". US Marketed Drugs www.drugsdb.eu.
^ AstraZeneca. "ZESTRIL (lisinopril) product insert" (PDF). accessdata.fda.gov. Retrieved 15 October 2011.
^ Patlak M (March 2004). "From viper's venom to drug design: treating hypertension". FASEB J. 18 (3): 421. doi:10.1096/fj.03-1398bkt. PMID 15003987.

External links

Prescribing information for Zestril
U.S. National Library of Medicine: Drug Information Portal – Lisinopril
Lisinopril.com – Lisinopril information

UpToDate Contents

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1. 糖尿病患者における高血圧治療 treatment of hypertension in patients with diabetes mellitus
2. アンギオテンシン変換酵素阻害剤およびアンギオテンシンII受容体拮抗剤の主な副作用 major side effects of angiotensin converting enzyme inhibitors and angiotensin ii receptor blockers
3. 原発性（本態性）高血圧における治療選択：臨床試験 choice of therapy in primary essential hypertension clinical trials
4. 収縮能障害による心不全におけるACE阻害剤：治療使用 ace inhibitors in heart failure due to systolic dysfunction therapeutic use
5. 原発性（本態性）高血圧における薬物療法の選択：推奨 choice of drug therapy in primary essential hypertension recommendations

English Journal

The cough reflex is upregulated by lisinopril microinjected into the caudal nucleus tractus solitarii of the rabbit.

Cinelli E1, Bongianni F1, Pantaleo T1, Mutolo D2.
Respiratory physiology & neurobiology.Respir Physiol Neurobiol.2015 Dec;219:9-17. doi: 10.1016/j.resp.2015.07.013. Epub 2015 Jul 30.
We have previously shown that cough potentiation induced by intravenous administration of the AT1 receptor antagonist losartan is lower than that induced by the ACE inhibitor lisinopril in anesthetized and awake rabbits. Since losartan and lisinopril cross the blood-brain barrier, their central acti
PMID 26234277

Automated Outreach for Cardiovascular-Related Medication Refill Reminders.

Harrison TN1, Green KR2, Liu IA1, Vansomphone SS3, Handler J4, Scott RD5, Cheetham TC1, Reynolds K1.
Journal of clinical hypertension (Greenwich, Conn.).J Clin Hypertens (Greenwich).2015 Nov 6. doi: 10.1111/jch.12723. [Epub ahead of print]
The objective of this study was to evaluate the effectiveness of an automated telephone system reminding patients with hypertension and/or cardiovascular disease to obtain overdue medication refills. The authors compared the intervention with usual care among patients with an overdue prescription fo
PMID 26542896

Treating hypertension in hemodialysis improves symptoms seemingly unrelated to volume excess.

Agarwal R1.
Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association.Nephrol Dial Transplant.2015 Nov 5. pii: gfv371. [Epub ahead of print]
BACKGROUND: Among hemodialysis patients, probing dry weight is an effective strategy for improving control of hypertension. Whether controlling hypertension improves or worsens symptoms among such patients remains unclear. The purpose of the study was to develop a tool to evaluate symptoms and exami
PMID 26546591

Japanese Journal

Lercanidipine Rescues Hippocampus Pyramidal Neurons from Mild Ischemia-Induced Delayed Neuronal Death in SHRSP.

Sakurai-Yamashita Yasuko,Harada Noboru,Niwa Masami
Cellular and molecular neurobiology 31(4), 561-567, 2011-05
… This study was designed to compare the effects of the antihypertensive drugs lercanidipine, nicardipine, lisinopril, valsartan, and hydralazine on occlusion-induced DND in SHRSPs. … Hydralazine and lisinopril were associated with the greatest reduction; …
NAID 120002835141

Complete remission of non-HIV collapsing glomerulopathy with deflazacort and lisinopril in an adult patient

VEGA Jorge,GUARDA Francisco Javier,GOECKE Helmuth,MENDEZ Gonzalo P.
Clinical and experimental nephrology 14(4), 385-388, 2010-08-01
NAID 10027706925

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★リンクテーブル★

リンク元	「アンジオテンシン変換酵素阻害薬」「リシノプリル」

「アンジオテンシン変換酵素阻害薬」

Lisinopril
	Chemical structure of lisinopril
Systematic (IUPAC) name
	N2-[(1S)-1-carboxy-3-phenylpropyl]-L-lysyl-L-proline
Clinical data
Trade names	Prinivil, Tensopril, Zestril, Hipril
AHFS/Drugs.com	monograph
MedlinePlus	a692051
Pregnancy; category	C (1st trimester) / D (2nd and 3rd trimester);
Legal status	℞ (Prescription only);
Routes of; administration	Oral
Pharmacokinetic data
Bioavailability	approx. 25%, but wide range between individuals (6 to 60%)
Protein binding	0
Metabolism	None
Biological half-life	12 hours
Excretion	Eliminated unchanged in urine
Identifiers
CAS Registry Number	83915-83-7
ATC code	C09AA03
PubChem	CID: 5362119
IUPHAR/BPS	6360
DrugBank	APRD00560
ChemSpider	4514933
UNII	7Q3P4BS2FD
KEGG	D00362
ChEBI	CHEBI:43755
ChEMBL	CHEMBL1237
Synonyms	(2S)-1-[(2S)-6-amino-2-{[(1S)-1-carboxy-3-phenylpropyl]amino}hexanoyl]pyrrolidine-2-carboxylic acid
PDB ligand ID	LPR (PDBe, RCSB PDB)
Chemical data
Formula	C21H31N3O5
Molecular mass	405.488 g/mol
	SMILES O=C(O)[C@H]2N(C(=O)[C@@H](N[C@H](C(=O)O)CCc1ccccc1)CCCCN)CCC2;
	InChI InChI=1S/C21H31N3O5/c22-13-5-4-9-16(19(25)24-14-6-10-18(24)21(28)29)23-17(20(26)27)12-11-15-7-2-1-3-8-15/h1-3,7-8,16-18,23H,4-6,9-14,22H2,(H,26,27)(H,28,29)/t16-,17-,18-/m0/s1 ; Key:RLAWWYSOJDYHDC-BZSNNMDCSA-N ;
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英: angiotensin-converting enzyme inhibitor angiotensin converting enzyme inhibitor , ACE inhibitor, ACEI
同: アンジオテンシン変換酵素阻害剤アンギオテンシン変換酵素阻害薬アンギオテンシン変換酵素阻害剤アンジオテンシン転換酵素阻害薬、ACE阻害薬 ACE阻害剤 ACE inhibitor、アンギオテンシン変換酵素拮抗薬, アンギオテンシン変換酵素拮抗薬, angiotensin-converting enzyme antagonist
関: アンジオテンシン, アンジオテンシン転換酵素 ACE, 1型アンジオテンシンII受容体拮抗薬アンジオテンシンII受容体拮抗薬 ARB