Category:Antihypertensive, Vasodilator. (PDR 2002)Composition:Each tablet contains lisinopril 5 or 10 mg.Chemistry:Lisinopril, a synthetic peptide derivative, is an oral long-acting angiotensin converting enzyme inhibitor. Lisinopril is chemically described as (S)-1-[N2-(1- carboxy-3-phenylpropyl) -L-lysyl] -L-proline dihydrate.(C21H31N3o5. 2H2O)Molecular weight= 441.52 (PDR 2002)Mechanism of Action: Lisinopril inhibits angiotensin converting enzyme (ACE). ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. Angiotensin II also stimulates aldostrone secretion by the adrenal cortex. (PDR 2002) Pharmacokinetics:Absorption: Approximately 25% but widely variable between individuals (6 to 60%) not affected by the presence of food.Protein binding: None.Half Life: 12 hours, increased in renal failure.Onset of action: 1hour.Duration of action: Approximately 24 hours.Elimination: Renal; 100% unchanged. (USP DI 2004)Indications:Hypertension, (Lisinopril may be used alone as initial therapy or concomitantly with other classes of antihypertensive agents).Heart failure, Acute myocardial infarction. (PDR 2002) Contraindications:Lisinopril 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. (PDR 2002) Precaution:- Aortic stenosis/ Hypertrophic cardiomyopathy (As with all vasodilators)- Impaired renal function- Cough- Surgery/ Anesthesia (PDR 2002) Pregnancy: Category C (first trimester) and D (second and third trimesters). ACE inhibitors can cause fetal and neonatal morbidity and death when administered to pregnant women. (PDR 2002)Breast - feeding: It is not known whether Lisinopril is distributed into breast milk, and because of the potential for serious adverse reactions in nursing infants from ACE inhibitors, a decision should be made whether to discontinue Lisinopril, taking into account the importance of the drug to the mother. (USP DI 2004)Drug interaction:- Hypotension-producing medications (Like diuretics).- Non-steroidal anti-inflammatory agents.Concurrent use of these agents may reduce the antihypertensive effects of ACE inhibitors. Indomethacin and possibly other NSAIDs may antagonize the antihypertensive effect by inhibiting renal prostaglandin synthesis and / or causing sodium and fluid retention. (USP DI 2004)- Agents increasing serum potassium.Lisinopril attenuates potassium loss caused by thiazide type diuretics. Use of Lisinopril with potassium-sparing diuretics (e.g.spironolactone, triamterene, or amiloride, potassium supplements, or potassium-containing salt substitutes may lead to significant increase in serum potassium.- Lithium: Lithium toxicity has been reported in patients receiving lithium concomitantly with drugs which cause elimination of sodium, including ACE inhibitors. (PDR 2002)Side / Adverse effect:Those indicating need for medical attention:• Incidence less frequentHypotension, skin rash with or without itching, fever or joint pain.• Incidence rareAngioedema of the extremitities, face, lips, mucous-membranes...Those indicating need for medical attention only if they continue or are bothersome:• Incidence more frequent:Cough, dry persistent, headache(Cough usually occurs within the first week of therapy (onset varies from 24 hours to several weeks after initiation) persists throughout therapy, and disappears within a few day after withdrawal of the ACE inhibitor.• Incidence less frequentDiarrhea, dysgeusia (loss of taste), fatigue, nausea.(USP DI 2004)Administration and dosage:Usual adult and adolescent doseAntihypertensiveInitial:Oral, 10mg once a day, the dosage being adjusted according to clinical response.Maintenance:Oral, 20 to 40mg once a day.Note: An initial dose of 5mg should be used in patients who are sodium - and water depleted as a result of prior diuretic therapy, or patients with renal failure (creatinine clearance less than or equal to 30ml per minute). An initial dose of 2.5mg should be used in patients with a creatinine clearance less than 10cc per minute. Such patients should be kept under medical supervision for at additional hour after blood pressure has stabilized) to watch for excessive hypotension.• Vasodilator, congestive heart failure:Initial:Oral 5mg per day, the dosage being adjusted according to clinical response.Maintenance:Oral, 5 to 20mg per day.Note: An initial dose of 2.5mg per day should be used in patients with hyponatremia or who have moderate to severe renal impairment (creatinine clearance less than or equal to 30cc per minute). Acute myocardial infarction:Initial:Oral, 5mg within 24 hours of onset of an acute myocardial infarction. Followed by 5mg after 24 hours, 10mg after 48 hours then 10mg per day.Maintenance:10mg per day.Note: In patients with low systolic blood pressure (≤120mmHg) an initial dose of 2.5mg should be used when treatment begins, or during the first three days after the infarction if hypotention occurs (systolic blood pressure is less than or equal to 100mmHg) a daily maitenance dose of 5mg may be given with temporary reduction to 2.5mg if needed. If prolonged hypotension occurs (systolic blood pressure ≤90mmHg for more than 1 hour) Lisinopril should be withdrawn.Usual pediatric dose:Safety and efficacy have not been established.(USP DI 2004)Packaging and storage:Store below 40°C. Preferably between 20˚C and 25°C, in a well- closed container. (USP DI 2004)References:• (USP DI 2004) • (PDR 2002)
Use logical operators AND, OR, NOT (In Upper case) for Advance Search.
Ex : Niro AND Tehran , Iran OR Investment