Lisinopril is a third-generation angiotensin-converting enzyme inhibitor and a lysine derivative of enalapril. It was listed in the United States in 1987 for the treatment of hypertension and is a first-line drug for anti-hypertensive disease. The pharmacological action characteristics are similar to that of Enalapril. It has a strong inhibitory effect on angiotensin-converting enzyme. The inhibitory effect on ACE is 6 to 8 times that of captopril and 1 to 3 times that of benazepril. Total peripheral resistance and blood pressure can be significantly decreased, but not accompanied by reflex tachycardia. Lisinopril can reduce pulmonary wedge pressure, increase cardiac output, increase left ventricular ejection fraction, and improve cardiac function in patients with heart failure. Can increase renal blood flow, reduce renal vascular resistance, increase glomerular filtration rate. It can be used alone or in combination with other drugs to treat various degrees of hypertension and renal hypertension that are ineffective against other antihypertensive drugs, and can also be used alone or in combination with digitalis and diuretics to treat congestive heart failure. It can also be used as adjuvant therapy for hemodynamically stable patients after acute myocardial infarction.
Uses
For the treatment of hypertension, once a day, the initial dose is 10 mg each time; the maintenance dose is 20 mg orally each time; renal function impairment, renal hypertension, restricted water and sodium intake and some elderly people, the initial dose The dose is 2.5 to 5 mg each time to prevent symptomatic hypotension.
Pharmacokinetics
The oral absorption rate of this drug is 30%. Bioavailability is 25%. It takes effect 2 to 4 hours after oral administration, reaches the peak plasma concentration in 7 hours after oral administration, and lasts for 2 hours. Metabolites and drug prototypes are excreted from the kidneys. This product is carboxyl type, oral absorption is not affected by food, F is about 25% ~ 50%, Tmax is 6 ~ 8h, this product is not easily combined with plasma proteins, after oral administration of 10mg, the average Vd is 1.24L. T1/2 is 12.6h, and terminal T1/2 is about 30h. Take it once a day, 2 to 3 days up to Css. After absorption, it can be distributed in various tissues in the body, especially the kidney and heart with the highest concentration. The drug can exert an ACE inhibitory effect without being metabolized in the body, and is almost completely excreted from the kidney in its original form. Cl averaged 106ml/min and was mainly excreted through the kidneys. Renal insufficiency is easy to cause accumulation of poisoning, so the dose needs to be reduced.
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