Lisinopril

trade name: Zestril; drug class: angiotensin-converting enzyme (ACE) inhibitor; action: selectively suppresses renin-angiotensin-aldosterone system; inhibits ACE, which prevents conversion of angiotensin I to angiotensin II; uses: mild to moderate hypertension, post myocardial infarction if hemodynamically stable.

Brand names: Prinivil®Zestril®

Chemical formula:

Español:
• Lisinopril, Tableta oral

Lisinopril Oral tablet

What is this medicine?

LISINOPRIL is an ACE inhibitor. This medicine is used to treat high blood pressure and heart failure. It is also used to protect the heart immediately after a heart attack.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•diabetes
•heart or blood vessel disease
•immune system disease like lupus or scleroderma
•kidney disease
•low blood pressure
•previous swelling of the tongue, face, or lips with difficulty breathing, difficulty swallowing, hoarseness, or tightening of the throat
•an unusual or allergic reaction to lisinopril, other ACE inhibitors, insect venom, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on your prescription label. You may take this medicine with or without food. Take your medicine at regular intervals. Do not stop taking this medicine except on the advice of your doctor or health care professional.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed. While this drug may be prescribed for children as young as 6 years of age for selected conditions, precautions do apply.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

•diuretics
•lithium
•NSAIDs, medicines for pain and inflammation, like ibuprofen or naproxen
•over-the-counter herbal supplements like hawthorn
•potassium salts or potassium supplements
•salt substitutes

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular check ups. Check your blood pressure as directed. Ask your doctor what your blood pressure should be, and when you should contact him or her. Call your doctor or health care professional if you notice an irregular or fast heart beat.

Women should inform their doctor if they wish to become pregnant or think they might be pregnant. There is a potential for serious side effects to an unborn child. Talk to your health care professional or pharmacist for more information.

Check with your doctor or health care professional if you get an attack of severe diarrhea, nausea and vomiting, or if you sweat a lot. The loss of too much body fluid can make it dangerous for you to take this medicine.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this drug affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol can make you more drowsy and dizzy. Avoid alcoholic drinks.

Avoid salt substitutes unless you are told otherwise by your doctor or health care professional.

Do not treat yourself for coughs, colds, or pain while you are taking this medicine without asking your doctor or health care professional for advice. Some ingredients may increase your blood pressure.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•abdominal pain with or without nausea or vomiting
•allergic reactions like skin rash or hives, swelling of the hands, feet, face, lips, throat, or tongue
•dark urine
•difficulty breathing
•dizzy, lightheaded or fainting spell
•fever or sore throat
•irregular heart beat, chest pain
•pain or difficulty passing urine
•redness, blistering, peeling or loosening of the skin, including inside the mouth
•unusually weak
•yellowing of the eyes or skin

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•change in taste
•cough
•decreased sexual function or desire
•headache
•sun sensitivity
•tiredness

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Protect from moisture. Keep container tightly closed. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

An angiotensin-converting enzyme inhibitor, similar to captopril, but with longer duration of activity. Used in the treatment of heart disease in dogs.

The noun has one meaning:

Meaning #1: an ACE inhibiting drug (trade names Prinivil or Zestril) administered as an antihypertensive and after heart attacks
  Synonyms: Prinivil, Zestril

Lisinopril
Systematic (IUPAC) name
N2-[(1S)-1-carboxy-3-phenylpropyl]-L-lysyl-L-proline
Identifiers
CAS number	83915-83-7
ATC code	C09AA03
PubChem	5362119
DrugBank	APRD00560
ChemSpider	4514933
Chemical data
Formula	C21H31N3O5
Mol. mass	405.488 g/mol
SMILES	eMolecules & PubChem
Synonyms	(2S)-1-[(2S)-6-amino-2-{[(1S)-1-carboxy-3-phenylpropyl]amino}hexanoyl]pyrrolidine-2-carboxylic acid
Pharmacokinetic data
Bioavailability	approx. 25%, but wide range between individuals (6 to 60%)
Protein binding	0
Metabolism	None
Half life	12 hours
Excretion	Eliminated unchanged in Urine
Therapeutic considerations
Pregnancy cat.	D - teratogenic
Legal status	℞ Prescription only
Routes	PO

Lisinopril (lye-SIN-o-pril) is a drug of the angiotensin converting enzyme (ACE) inhibitor class that is primarily used in treatment of hypertension, congestive heart failure, heart attacks and also in preventing renal and retinal complications of diabetes. It has been compared with omapatrilat which is of similar function.

Historically, lisinopril was the third ACE inhibitor, after captopril and enalapril, and was introduced into therapy in the early 1990s.^[1] Lisinopril has a number of properties that distinguish it from other ACE inhibitors: it is hydrophilic, has long half-life and tissue penetration and is not metabolized by the liver.

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 derived from the venom of the jararaca, a Brazilian pit viper (Bothrops jararaca)^[2]. Lisinopril can also be used in conjunction with the diuretic Hydrochlorothiazide and also goes by the brand names Prinizide and Zestoretic.

Contents 1 Pharmacology 2 Pharmacokinetics and metabolism 3 Drug dosage 4 Clinical use 5 Adverse effects 6 See also 7 References 8 Footnotes 9 External links

Pharmacology

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

Pharmacokinetics and metabolism

Adult patients: Following oral administration of lisinopril, peak serum concentrations occur within about 7 hours, although there was a trend to a small delay in time taken to reach peak serum concentrations in acute myocardial infarction patients. Declining serum concentrations exhibit a prolonged terminal phase which 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 absorption of lisinopril is approximately 25 percent, with large inter-subject variability (6-60 percent) at all doses tested (5-80 mg). Lisinopril absorption is not influenced by the presence of food in the gastrointestinal tract. The absolute bioavailability of lisinopril is reduced to about 16 percent in patients with stable NYHA Class II-IV congestive heart failure, 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, lisinopril 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 glomerular filtration rate, the elimination half-life is little changed. With greater impairment, however, peak and trough lisinopril levels increase, time to peak concentration increases and time to attain steady state is prolonged. Older patients, on average, have (approximately doubled) higher blood levels and area under the plasma concentration time curve (AUC) than younger patients

creatinine clearance ≥ 10 mL/min ≤ 30 mL/min (serum creatinine ≥ 3 mg/dL), the first dose is 5 mg once daily. For patients with creatinine clearance < 10 mL/min (usually on hemodialysis)

Drug dosage

Dosage Adjustment in Renal Impairment: The usual dose of PRINIVIL (10 mg) is recommended for patients with a creatinine clearance > 30 mL/min (serum creatinine of up to approximately 3 mg/dL). For patients with chronic renal impairment the recommended initial dose is 2.5 mg. The dosage may be titrated upward until blood pressure is controlled or to a maximum of 40 mg daily.

Renal Status Creatinine-Clearance mL/min Initial Dose mg/day Normal Renal Function to Mild Impairment > 30 mL/min 10 mg Moderate to Severe Impairment ≥ 10 ≤ 30 mL/min 5 mg Dialysis Patients** < 10 mL/min 2.5 mg***

**See WARNINGS, Anaphylactoid reactions during membrane exposure

*** Dosage or dosing interval should be adjusted depending on the blood pressure response.

Dosage adjustment in patients with myocardial infarction with renal impairment: In acute myocardial infarction, treatment with PRINIVIL should be initiated with caution in patients with evidence of renal dysfunction, defined as serum creatinine concentration exceeding 2 mg/dL. No evaluation of dosage adjustment in myocardial infarction patients with severe renal impairment has been performed.

Clinical use

Its indications, contraindications and side effects are as those for all ACE inhibitors. Its long half-life allows for once a day dosing which aids patient compliance. The usual daily dose in all indications ranges from 2.5 mg in sensitive patients to 40 mg. Some patients have been treated with 80 mg daily and have tolerated this high dose well. Lower dosages must be used in patients with higher grade renal impairment (glomerular filtration rate (GFR) lower than 30 ml/min).

Adverse effects

Serious side effects that would require immediate medical attention include:

• Chills, infection
• Dark urine, decreased urination (oliguria)
• Difficulty swallowing or breathing (signs of angioedema), allergic reaction (anaphylaxis)
• Hoarseness
• Itching
• Rapid weight gain, stomach pain
• Yellowing of skin or eyes (jaundice)

• Abdominal pain, bloating, vomiting
• Chest pain or tightness, dizziness, lightheadedness, fainting (syncope)
• Dry cough
• Fever
• Joint pain
• Rash

• Diarrhea, loss of taste, nausea
• Drowsiness, headache, tiredness
• Change in mood/irrational behaviour
• Blurred vision
• Muscle cramps
• Fainting/blackouts
• Sexual dysfunction
• Death

Lisinopril causes the kidneys to retain potassium, which may lead to hyperkalemia.

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

See also

• Omapatrilat

References

• Bussien JP, Waeber B, Nussberger J, Gomez HJ, Brunner HR. Once-daily lisinopril in hypertensive patients: Effect on blood pressure and the renin-angiotensin system. Curr Therap Res 1985;37:342-51.
• Lisinopril info - rx-list.com
• Goodman & Gilman's : The pharmacological basis of therapeutics, 10th. ed., 2001
• Lisinopril.com - Lisinopril information

Footnotes

1. ^ 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. 
2. ^ http://www.fasebj.org/cgi/content/full/18/3/421

External links

• Prescribing information for ZESTRIL

This antihypertensive-related article is a stub. You can help Wikipedia by expanding it. v • d • e

v • d • e Antihypertensives: agents acting on the renin-angiotensin system (C09) ACE inhibitors ("-pril") Sulfhydryl-containing: Captopril • Zofenopril Dicarboxylate-containing: Enalapril# • Ramipril • Quinapril • Perindopril • Lisinopril • Benazepril Phosphonate-containing: Fosinopril Other/ungrouped: Alacepril • Cilazapril • Delapril • Imidapril • Moexipril • Rentiapril • Spirapril • Temocapril • Trandolapril AIIRAs/ ("-sartan") Azilsartan • Candesartan • Eprosartan • Irbesartan • Losartan • Olmesartan • Tasosartan • Telmisartan • Valsartan Renin inhibitors/ ("-kiren") Aliskiren • Remikiren #WHO-EM. ‡Withdrawn from market. CLINICAL TRIALS: †Phase III. §Never to phase III

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