What Is Benazepril Hydrochloride?

[Chinese name]: Benazepril hydrochloride

Benazepril hydrochloride

[Chinese name]: Benazepril hydrochloride

[Simplified Pinyin]: YSBNPL

[English name]: Benazepril Hydrochloridec

category:

Chinese name: Benazepril hydrochloride Chinese alias:

[Alias] Benazepril hydrochloride,

1. Occasionally dizziness, fatigue, symptomatic hypotension, gastrointestinal upset, rash, itching,

[Indications] 1. Hypertension (can be used alone or combined with other antihypertensive drugs such as diuretics) 2.

Benazepril hydrochloride

[Drug name] Benazepril Hydrochloride

[Drug alias] Benazepril, Lotensin, Lotensin, Benazepril Hydrochloride

Structural formula:

[Formulation specifications] Tablets: 5mg, 10mg, 20mg, 40mg.

[Pharmacology and toxicology] This product is a strong angiotensin-converting enzyme inhibitor, which can reduce peripheral vascular resistance, but does not cause compensatory fluid retention. It can reduce afterload, but does not produce counterregulation. Glucose tolerance in diabetic patients

Pharmacology

(1) Antihypertensive: This product hydrolyzes to benazepril in the liver, and becomes a competitive angiotensin-converting enzyme inhibitor, preventing the conversion of angiotensin I to angiotensin II, reducing vascular resistance, Decreased aldosterone secretion and increased plasma renin activity. Benazepril also inhibits the degradation of bradykinin, which also reduces vascular resistance and produces a hypotensive effect.

(2) Reduce heart load: This product expands arteries and veins, reduces peripheral vascular resistance or post-cardiac load, reduces pulmonary capillary entrapment or pre-cardiac load, and reduces pulmonary vascular resistance, thereby improving cardiac output and exercise tolerance. And time extension.

2. Toxicology

Rats and mice continued to take benazepril for 2 years at a dose of 150 mg / kg per day. No carcinogenicity was found. (The dose is calculated as mg / kg, which is 110 times the maximum human consumption; calculated as mg / m, it is 18 and 9 times the maximum human consumption).

This product has not been found to be mutagenic in bacterial tests or in mammalian cell tests in vitro.

Female and male rats take benazepril orally at a dose of 50 to 150 mg / kg per day, and this product has not been found to affect reproduction. (The dosage is calculated as mg / kg, which is 37 to 375 times the maximum dosage for humans; calculated as mg / m, it is 6 to 60 times the maximum dosage for humans).

[Pharmacokinetics] The oral Tmax is about 1 to 1.5 hours, and the active metabolite Tmax is about 1.5 to 2 hours. Both PB are about 95%. The effect is about 2 to 6 hours, and the maximum antihypertensive effect can be achieved for 2 weeks. Intrahepatic benazepril is converted to active benazepril, which is mainly excreted by the kidneys. Benazepril T1 / 2 is about 0.6h, and Benazepril T1 / 2 is about 11h.

Oral absorption of benazepril is rapid, peak time is 0.5 to 1 hour, and benazepril is 1 to 1.5 hours. Oral absorption of at least 37%, eating does not affect absorption. The protein binding rate of this product is as high as 96.7%, and that of benazepril is 95.3%. This product is hydrolyzed in the liver to form benazepril after absorption. Its inhibitory effect on angiotensin converting enzyme is stronger than this product. The half-life of this product is 0.6 hours, and that of benazepril is 10 to 11 hours. After 2 to 3 days, it reaches a steady state. This product is mainly cleared by the kidneys. Less than 1% of benazepril is excreted in the original form, 20% is benazepril and the combination of benazepril and benazepril's acetyl-glucuronide Excretion; 11% to 12% are excreted from the biliary tract. Mild to moderate renal dysfunction (creatinine clearance> 30ml / min), liver dysfunction caused by cirrhosis, and age did not affect pharmacokinetics. During hemodialysis, a small amount of this product can be removed by dialysis

Indications

1. Hypertension (can be used alone or in combination with other antihypertensive drugs such as diuretics)

2. Cardiac insufficiency (can be used alone or in combination with cardiotonic diuretics)

[Adverse reactions] headache, dizziness, fatigue, worsening cough, sore throat, rash, flushing, tachycardia, palpitations, nausea, diarrhea, nervousness, ataxia, hypotension, edema. There are also sexual dysfunction, elevated blood urea nitrogen or creatinine.

1. Common are: headache, dizziness, fatigue, lethargy, nausea, and cough. The most common are headaches and coughs.

2. Rarely: symptomatic hypotension, orthostatic hypotension, syncope, palpitations, peripheral edema, rash, dermatitis, constipation, gastritis, anxiety, insomnia, paresthesia, joint pain, myalgia, asthma, etc. Angioedema is rare.

[Taboo]

1. People who are allergic to benazepril or other angiotensin-converting enzyme inhibitors.

2. History of angioedema.

3. Solitary kidney, transplanted kidney, bilateral renal artery stenosis and renal dysfunction.

[Interaction] Thiazine diuretics, calcium antagonists or beta blockers can enhance the effect of this product. Non-steroidal anti-inflammatory analgesics can reduce the effect of this product. This product can increase the blood concentration of lithium preparations.

1. Combined with diuretics, the antihypertensive effect is enhanced, which may cause severe hypotension. Therefore, the original diuretics should be discontinued or reduced. This product started with a small dose and gradually adjusted the dose.

2. Combination with other vasodilators may cause hypotension. If combined, start with a small dose.

3. Combined with potassium diuretics (such as spironolactone, ampicillin, amiloride) can cause hyperkalemia

4. Combination with non-steroidal anti-inflammatory analgesics can reduce the antihypertensive effect of this product by inhibiting prostaglandin synthesis and sodium and sodium retention.

5. Combined with other antihypertensive drugs, the antihypertensive effect is strengthened. Among them, it has a large additive effect with a drug that causes renin release or affects sympathetic activity, and a combined use with a beta-blocker has a smaller additive effect.

[Drug overdose] First of all, hypotension should be corrected. Expanding blood volume by intravenous infusion of normal saline is an effective measure to restore blood pressure. Benazepril can be partially removed by dialysis.

[Usage and Dosage] The dosage should be individualized. Adult dosage

(1) Antihypertensive: For those who have not taken diuretics, the recommended starting dose is 10 mg orally once a day; those who have taken diuretics (except for severe and malignant hypertension) should stop using diuretics for 2 to 3 days. In small doses, carefully increase the dose under observation. If the blood pressure can not be controlled once a day, the dose can be increased or divided into two doses, the maintenance amount can reach 20mg 40mg / day. Patients with renal dysfunction or lack of water and sodium started to use 5mg once a day.

(2) Cardiac insufficiency: The recommended starting dose is 5 mg orally once a day. Blood pressure should be monitored for the first dose. The maintenance amount can be used once a day from 5mg to 10mg. Severe cardiac insufficiency requires a smaller dose than mild and moderate cardiac insufficiency.

Child dosage

No research data available.

Precautions

1. Angioedema: Lip or facial edema has occurred after taking this product. If this symptom occurs, the drug should be stopped immediately and the patient should be monitored until the edema disappears. Edema of the glottis, tongue, and throat may cause airway obstruction. The drug should be discontinued and appropriate treatment immediately, such as subcutaneous injection of a 1: 1000 adrenaline solution (0.3ml to 0.5ml).

2. Hypotension: Hypotension may occur when taking this product for people with severe hyponatremia and hypovolemia (such as those receiving a lot of diuretics or dialysis). Diuretics should be discontinued or other measures taken to replenish body fluids a few days before starting this product. Those who may have severe hypotension (such as patients with cardiac insufficiency) should be closely monitored after taking the first dose until the blood pressure is stable. If hypotension occurs, the patient should be placed in a supine position and intravenous saline solution if necessary.

3. Granulocytopenia: Leukocytes or granulocytopenia are more likely to occur in patients with autoimmune diseases and renal insufficiency. For patients with renal insufficiency or leukopenia, the white blood cell count and classification are checked every 2 weeks for the first 3 months, and then regularly checked.

4. Renal insufficiency: A small number of patients may temporarily increase blood urea nitrogen and creatinine after taking this product. After stopping this product and / or diuretics, they can recover. For patients with renal insufficiency, renal function should be closely monitored in the weeks before treatment, and renal function should be checked regularly in the future. When using this product, if the creatinine clearance rate is <30ml / min or blood urea nitrogen and creatinine are increased, the dose of this product must be reduced and / or diuretics should be stopped.

5. Others: Occasionally, serum potassium is elevated, especially when renal insufficiency and drugs for hypokalemia are used in combination. Occasionally elevated aminotransferases. Insufficient blood supply to the brain or coronary arteries can worsen blood pressure. Metabolism of this product in the liver is reduced during liver dysfunction.

[Medication for pregnant and lactating women]

This product should not be taken during pregnancy. This product can be taken through the placenta in the second and third trimesters of pregnancy, which can cause fetal damage and even death. If pregnancy is found, the drug should be stopped immediately.

This product and benazepril can be secreted into breast milk, but benazepril can reach the infant's systemic circulation.

[Child medication]

Inadequate research in children. In newborns and infants, oliguria and neurological abnormalities occur.

[Medication for elderly patients]

Elderly patients have better efficacy and tolerance when taking this product, but elderly patients and patients with heart dysfunction, coronary and cerebral arteriosclerosis should pay attention to blood pressure when taking this product. A sudden drop in blood pressure will cause blood supply to important organs insufficient.