Zestril
Buy ZestrilZestril Information
Brand Name: Zestril
Generic Name: Lisinopril
Zestril Indications:
Hypertension
Zestril is indicated for the treatment of hypertension. Zestril may be used alone as initial therapy or concomitantly with other classes of antihypertensive agents.
Heart Failure
Zestril is indicated as adjunctive therapy in the management of heart failure in patients who are not responding adequately to diuretics and digitalis.
Acute Myocardial Infarction
Zestril is indicated for the treatment of hemodynamically stable patients within 24 hours of acute myocardial infarction, to improve survival. Patients should receive, as appropriate, the standard recommended treatments such as thrombolytics, aspirin and beta-blockers.
In using Zestril, consideration should be given to the fact that another angiotensin-converting enzyme inhibitor, captopril, has caused agranulocytosis, particularly in patients with renal impairment or collagen vascular disease, and that available data are insufficient to show that Zestril does not have a similar risk.
In considering the use of Zestril, it should be noted that in controlled clinical trials ACE inhibitors have an effect on blood pressure that is less in Black patients than in non-Blacks. In addition, ACE inhibitors have been associated with a higher rate of angioedema in Black than in non-Black patients.
Zestril Ingredients and Composition
How Does Zestril Work?
Mechanism of Action
Lisinopril, the active ingredient in Zestril inhibits angiotensin-converting enzyme (ACE) in human subjects and animals. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex. The beneficial effects of lisinopril in hypertension and heart failure appear to result primarily from suppression of the renin-angiotensin-aldosterone system. Inhibition of ACE results in decreased plasma angiotensin II which leads to decreased vasopressor activity and to decreased aldosterone secretion. The latter decrease may result in a small increase of serum potassium. In hypertensive patients with normal renal function treated with Zestril alone for up to 24 weeks, the mean increase in serum potassium was approximately 0.1 mEq/L; however, approximately 15% of patients had increases greater than 0.5 mEq/L and approximately 6% had a decrease greater than 0.5 mEq/L. In the same study, patients treated with Zestril and hydrochlorothiazide for up to 24 weeks had a mean decrease in serum potassium of 0.1 mEq/L; approximately 4% of patients had increases greater than 0.5 mEq/L and approximately 12% had a decrease greater than 0.5 mEq/L. (See PRECAUTIONS.) Removal of angiotensin II negative feedback on renin secretion leads to increased plasma renin activity.
ACE is identical to kininase, an enzyme that degrades bradykinin. Whether increased levels of bradykinin, a potent vasodepressor peptide, play a role in the therapeutic effects of Zestril remains to be elucidated.
While the mechanism through which Zestril lowers blood pressure is believed to be primarily suppression of the renin-angiotensin-aldosterone system, Zestril is antihypertensive even in patients with low-renin hypertension. Although Zestril was antihypertensive in all races studied, Black hypertensive patients (usually a low-renin hypertensive population) had a smaller average response to monotherapy than non-Black patients.
Concomitant administration of Zestril and hydrochlorothiazide further reduced blood pressure in Black and non-Black patients and any racial differences in blood pressure response were no longer evident.
How To Take Zestril and Zestril Dosage and Administration
Hypertension
Initial Zestril Therapy: In patients with uncomplicated essential hypertension not on diuretic therapy, the recommended initial dose is 10 mg once a day. Zestril Dosage should be adjusted according to blood pressure response. The usual Zestril dose range is 20 to 40 mg per day administered in a single daily dose. The antihypertensive Zestril effect may diminish toward the end of the dosing interval regardless of the administered dose, but most commonly with a dose of 10 mg daily. This can be evaluated by measuring blood pressure just prior to Zestril dosing to determine whether satisfactory control is being maintained for 24 hours. If it is not, an increase in Zestril dose should be considered. Zestril doses up to 80 mg have been used but do not appear to give greater effect. If blood pressure is not controlled with Zestril alone, a low dose of a diuretic may be added. Hydrochlorothiazide, 12.5 mg has been shown to provide an additive effect. After the addition of a diuretic, it may be possible to reduce the dose of Zestril.
Diuretic Treated Patients: In hypertensive patients who are currently being treated with a diuretic, symptomatic hypotension may occur occasionally following the initial dose of Zestirl. The diuretic should be discontinued, if possible, for two to three days before beginning therapy with Zestril to reduce the likelihood of hypotension. The dosage of Zestril should be adjusted according to blood pressure response. If the patient's blood pressure is not controlled with Zestril alone, diuretic therapy may be resumed as described above.
If the diuretic cannot be discontinued, an initial Zestril dose of 5 mg should be used under medical supervision for at least two hours and until blood pressure has stabilized for at least an additional hour.
Concomitant administration of Zestril with potassium supplements, potassium salt substitutes, or potassium-sparing diuretics may lead to increases of serum potassium.
Dosage Adjustment in Renal Impairment: The usual dose of Zestril (10 mg) is recommended for patients with creatinine clearance > 30 mL/min (serum creatinine of up to approximately 3 mg/dL). For patients with creatinine clearance ≥ 10 mL/min ≤ 30 mL/min (serum creatinine < 3 mg/dL), the first Zestril dose is 5 mg once daily. For patients with creatinine clearance < 10 mL/min (usually on hemodialysis) the recommended initial Zestril dose is 2.5 mg. Zestril dosage may be titrated upward until blood pressure is controlled or to a maximum of 40 mg daily.
Heart Failure
Zestril is indicated as adjunctive therapy with diuretics and (usually) digitalis. The recommended starting dose is 5 mg once a day. When initiating treatment with Zestril (lisinopril) in patients with heart failure, the initial dose should be administered under medical observation, especially in those patients with low blood pressure (systolic blood pressure below 100 mmHg). The mean peak blood pressure lowering occurs six to eight hours after dosing. Observation should continue until blood pressure is stable. The concomitant diuretic dose should be reduced, if possible, to help minimize hypovolemia which may contribute to hypotension. The appearance of hypotension after the initial dose of Zestril does not preclude subsequent careful dose titration with the drug, following effective management of the hypotension.
The usual effective Zestril dosage range is 5 to 40 mg per day administered as a single daily dose. The dose of Zestril can be increased by increments of no greater than 10 mg, at intervals of no less than 2 weeks to the highest tolerated dose, up to a maximum of 40 mg daily. Dose adjustment should be based on the clinical response of individual patients.
Dosage Adjustment in Patients with Heart Failure and Renal Impairment or Hyponatremia: In patients with heart failure who have hyponatremia (serum sodium < 130 mEq/L) or moderate to severe renal impairment (creatinine clearance ≤ 30 mL/min or serum creatinine > 3 mg/dL), therapy with Zestril should be initiated at a dose of 2.5 mg once a day under close medical supervision.
Acute Myocardial Infarction
In hemodynamically stable patients within 24 hours of the onset of symptoms of acute myocardial infarction, the first dose of Zestril is 5 mg given orally, followed by 5 mg after 24 hours, 10 mg after 48 hours and then 10 mg of Zestril once daily. Dosing should continue for six weeks. Patients should receive, as appropriate, the standard recommended treatments such as thrombolytics, aspirin, and beta-blockers.
Patients with a low systolic blood pressure (≤ 120 mmHg) when treatment is started or during the first 3 days after the infarct should be given a lower 2.5 mg oral dose of Zestril. If hypotension occurs (systolic blood pressure ≤ 100 mmHg) a daily maintenance dose of 5 mg may be given with temporary reductions to 2.5 mg if needed. If prolonged hypotension occurs (systolic blood pressure < 90 mmHg for more than 1 hour) Zestril should be withdrawn.
Dosage Adjustment in Patients With Myocardial Infarction with Renal Impairment: In acute myocardial infarction, treatment with Zestril should be initiated with caution in patients with evidence of renal dysfunction, defined as serum creatinine concentration exceeding 2 mg/dL. No evaluation of Zestril dosing adjustments in myocardial infarction patients with severe renal impairment has been performed.
If you suspect a Zestril Overdose
Following a single oral Zestril dose of 20 g/kg no lethality occurred in rats, and death occurred in one of 20 mice receiving the same dose. The most likely manifestation of Zestril overdose would be hypotension, for which the usual treatment would be intravenous infusion of normal saline solution.
Lisinopril can be removed by hemodialysis.
Zestril Side Effects
Zestril Warnings
Zestril Precautions and Contraindications
Zestril 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.
Taking Zestril during Pregnancy or Breast-feeding
Female patients of childbearing age should be told about the consequences of second- and third-trimester exposure to ACE inhibitors such as Zestril, 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 possible.
Zestril Clinical Trials and Studies
Storing Zestril
Store Zestril at controlled room temperature, 20-25°C (68-77°F). Protect Zestril from moisture, freezing and excessive heat. Dispense in a tight container.
Buy Zestril
