Lisipril - General Information
One of the angiotensin-converting enzyme inhibitors (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure. [PubChem]
Pharmacology of Lisipril
Lisipril, an angiotensin-converting enzyme (ACE) inhibitor, is used to treat hypertension, congestive heart failure (CHF), postmyocardial infarction, and diabetic nephropathy or retinopathy. Although it is the lysine ester of enalaprilat, the active form of the prodrug enalapril, lisinopril is active unchanged.
Lisipril for patients
Angioedema: Angioedema, including laryngeal edema, may occur at any time during treatment with
angiotensin converting enzyme inhibitors, including lisinopril. Patients should be so advised
and told to report immediately any signs or symptoms suggesting angioedema (swelling of face,
extremities, eyes, lips, tongue, difficulty in swallowing or breathing) and to take no more
drug until they have consulted with the prescribing physician.
Symptomatic Hypotension: Patients should be cautioned to report lightheadedness especially during
the first few days of therapy. If actual syncope occurs, the patients should be told to discontinue
the drug until they have consulted with the prescribing physician. All patients should be cautioned
that excessive perspiration and dehydration may lead to an excessive fall in blood pressure because
of reduction in fluid volume. Other causes of volume depletion such as vomiting or diarrhea may
also lead to a fall in blood pressure; patients should be advised to consult with their physician.
Hyperkalemia: Patients should be told not to use salt substitutes containing potassium without
consulting their physician.
Leukopenia/Neutropenia: Patients should be told to report promptly any indication of infection
(e.g., sore throat, fever) which may be a sign of leukopenia/neutropenia.
Pregnancy: Female patients of childbearing age should be told about the consequences of second-
and third-trimester exposure to ACE inhibitors, and they should also be told that these consequences
do not appear to have resulted from intrauterine ACE-inhibitor exposure that has been limited to the
first trimester. These patients should be asked to report pregnancies to their physicians as soon as
NOTE: As with many other drugs, certain advice to patients being treated with PRINIVIL is warranted.
This information is intended to aid in the safe and effective use of this medication. It is not a
disclosure of all possible adverse or intended effects.
Hypotension - Patients on Diuretic Therapy: Patients on diuretics, and especially those in whom diuretic therapy was recently instituted, may occasionally experience an excessive reduction of blood pressure after initiation of therapy with PRINIVIL. The possibility of hypotensive effects with PRINIVIL can be minimized by either discontinuing the diuretic or increasing the salt intake prior to initiation of treatment with PRINIVIL. If it is necessary to continue the diuretic, initiate therapy with PRINIVIL at a dose of 5 mg daily, and provide close medical supervision after the initial dose until blood pressure has stabilized. When a diuretic is added to the therapy of a patient receiving PRINIVIL, an additional antihypertensive effect is usually observed. Studies with ACE inhibitors in combination with diuretics indicate that the dose of the ACE inhibitor can be reduced when it is given with a diuretic.
Non-steroidal Anti-inflammatory Agents: In some patients with compromised renal function who are being treated with non-steroidal anti-inflammatory drugs, the co-administration of lisinopril may result in a further deterioration of renal function. These effects are usually reversible.
Reports suggest that NSAIDs may diminish the antihypertensive effect of ACE inhibitors, including lisinopril. This interaction should be given consideration in patients taking NSAIDs concomitantly with ACE inhibitors.
In a study in 36 patients with mild to moderate hypertension where the antihypertensive effects of PRINIVIL alone were compared to PRINIVIL given concomitantly with indomethacin, the use of indomethacin was associated with a reduced antihypertensive effect, although the difference between the two regimens was not significant.
Other Agents: PRINIVIL has been used concomitantly with nitrates and/or digoxin without evidence of clinically significant adverse interactions. This included post myocardial infarction patients who were receiving intravenous or transdermal nitroglycerin. No clinically important pharmacokinetic interactions occurred when PRINIVIL was used concomitantly with propranolol or hydrochlorothiazide. The presence of food in the stomach does not alter the bioavailability of PRINIVIL.
Agents Increasing Serum Potassium: PRINIVIL attenuates potassium loss caused by thiazide-type diuretics. Use of PRINIVIL with potassium-sparing diuretics (e.g., spironolactone, triamterene, or amiloride), potassium supplements, or potassium-containing salt substitutes may lead to significant increases in serum potassium. Therefore, if concomitant use of these agents is indicated because of demonstrated hypokalemia, they should be used with caution and with frequent monitoring of serum potassium. Potassium sparing agents should generally not be used in patients with heart failure who are receiving PRINIVIL.
Lithium: Lithium toxicity has been reported in patients receiving lithium concomitantly with drugs which cause elimination of sodium, including ACE inhibitors. Lithium toxicity was usually reversible upon discontinuation of lithium and the ACE inhibitor. It is recommended that serum lithium levels be monitored frequently if PRINIVIL is administered concomitantly with lithium.
PRINIVIL is contraindicated in patients who are hypersensitive to this product and in patients with a history of angioedema related to previous treatment with an angiotensin converting enzyme inhibitor and in patients with hereditary or idiopathic angioedema.
Additional information about Lisipril
Lisipril Indication: For the treatment of hypertension, heart failure and acute myocardial infarction. It may be used alone or in combination with thiazide diuretics
Mechanism Of Action: Lisipril competes with angiotensin I for its binding site on the angiotensin-converting enzyme (ACE), an enzyme which converts angiotensin I to angiotensin II. As angiotensin II is a vasoconstrictor and a negative feedback mediator for renin activity, lower angiotensin II plasma levels result in decreased blood pressure and increased plasma renin activity. Baroreceptor reflex mechanisms, stimulated by the fall in blood pressure, release kininase II, an enzyme identical to ACE that degrades bradykinin, a vasodilator.
Drug Interactions: Amiloride Increased risk of hyperkaliemia
Triamterene Increased risk of hyperkaliemia
Spironolactone Increased risk of hyperkaliemia
Potassium Increased risk of hyperkaliemia
Drospirenone Increased risk of hyperkaliemia
Clozapine Increases the effect and toxicity of clozapine
Lithium The ACE inhibitor increases serum levels of lithium
Tizanidine Tizanidine increases the risk of hypotension with the ACE inhibitor
Food Interactions: Avoid alcohol.
Avoid excess salt/sodium unless otherwise instructed by your physician.
Avoid salt substitutes containing potassium.
Avoid natural licorice.
Take without regard to meals.
Generic Name: Lisinopril
Synonyms: Not Available
Drug Category: Cardiotonic Agents; Antihypertensive Agents; Angiotensin-converting Enzyme Inhibitors
Drug Type: Small Molecule; Approved
Other Brand Names containing Lisinopril: Acercomp; Inhibril; Linopril; Lisinopril Dihydrate; Lisipril; Lysinopril; Noperten; Presiten; Prinivil; Prinzide; Renacor; Sinopril; Zestoretic; Zestril;
Absorption: Approximately 25%, but widely variable between individuals (6 to 60%)
Toxicity (Overdose): hypotension, LD50= 2000 mg/kg(orally in rat)
Protein Binding: Lisinopril does not appear to be bound to other serum proteins
Biotransformation: Lisinopril does not undergo metabolism and is excreted unchanged entirely in the urine
Half Life: 12 hours
Dosage Forms of Lisipril: Tablet Oral
Chemical IUPAC Name: (2S)-1-[(2S)-6-amino-2-[[(2S)-1-hydroxy-1-oxo-4-phenylbutan-2-yl]amino]hexanoyl]pyrrolidine-2-carboxylic acid
Chemical Formula: C21H31N3O5
Lisinopril on Wikipedia: https://en.wikipedia.org/wiki/Lisinopril
Organisms Affected: Humans and other mammals