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Lisinopril capsule

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Indications: This product is used for the treatment of essential hypertension and renal vascular hypertension. It can be used alone or in combination with other types of antihypertension such as diuretics. In patients with congestive heart failure, this product can be added when digitalis or diuretics are not effective.

Approval date: January 05, 2007

Revised date: June 24, 2009 October 01, 2010 July 10, 2012 December 01, 2015

Please read the instructions carefully and use under the guidance of a physician.

Allergic to this product or other angiotensin-converting enzyme inhibitors, patients with hyperkalemia

【Drug Name】

Generic name: lisinopril capsule

Product Name: Di Yiluo

English name: Lisinopril Capsules

Phonetic script (Hanyu Pinyin): Lainuopuli Jiaonang

【ingredient】

The main ingredient of this product is lisinopril.

Chemical name: 1- [N 2 -[(S) -1-carboxy-3-phenylpropyl] -L-lysyl] -L-proline dihydrate.

Molecular formula: C 21 H 31 N 3 O 5 · 2H 2 O

Molecular weight: 441.52

[Properties] This product is a capsule, and the content is white or off-white particles or powder.

[Specification] 5mg; 10mg (calculated based on lisinopril anhydrous).

[Usage and Dosage] The absorption of this product is not affected by food. It can be taken before, during or after meals, once a day.

Essential hypertension

For patients with essential hypertension, it is generally recommended that the starting dose should be 2.5 to 5 mg (5 mg: half to 1 capsule; 10 mg: 1/4 to half), and the effective maintenance dose is 10 to 20 mg (5 mg: 2 daily). ~ 4 capsules; 10mg: 1-2 capsules). The dose should be adjusted according to the change in blood pressure. The highest daily dose is 40mg (5mg: 8 capsules; 10mg: 4 capsules). Patients with kidney injury, patients who cannot interrupt diuretic therapy, patients with reduced blood volume and / or reduced sodium for various reasons, and patients with renal vascular hypertension should take lower starting doses.

Patients treated with diuretics may develop symptomatic hypotension when starting treatment with this product, and patients with diuretics are more likely to develop symptomatic hypotension. Because these patients have reduced blood volume and / or sodium loss, they should be cautious Combination therapy. Diuretics should be discontinued 2 to 3 days before starting treatment with this product. For patients whose diuretics cannot be stopped, the treatment of this product should start with 5mg (5mg: 1 capsule; 10mg: half capsule), and the subsequent dose adjustment should be based on blood pressure. Diuretics can be reused if needed.

Dose adjustment when renal function is impaired

Patients with renal impairment should adjust the dose according to the definition of creatinine clearance listed in Table 1 (including those on dialysis). Dosage and frequency should be adjusted according to blood pressure. Gradually increase the dose until blood pressure is controlled or to a maximum daily dose of 40 mg (5 mg: 8 capsules; 10 mg: 4 capsules).

Creatinine clearance (ml / min)

Starting dose (mg / hour)

<10

2.5mg

10≤creatinine clearance≤30

5mg

Table 1

2. Renal vascular hypertension

For some patients with renal vascular hypertension, especially those with bilateral renal artery stenosis or single renal artery stenosis, it may produce a large response when taking this product for the first time, so 2.5mg (5mg: half capsule; 10mg: 1 is recommended) / 4 capsules) or 5 mg (5 mg: 1 capsule; 10 mg: half capsule) at a lower starting dose, and then adjust the dose based on blood pressure.

3. Congestive heart failure

For patients who cannot be properly controlled with diuretics and / or digitalis, this product can be added. The starting dose is 2.5 mg (5 mg: half a capsule; 10 mg: 1/4 capsules) once a day, usually the effective dose range is 5 ~ 20mg (5mg: 1 to 4 capsules; 10mg: half to 2 capsules).

【Adverse reactions】

Controlled clinical trials have shown that this product is generally well tolerated. In most cases, adverse reactions are mild in nature and transient. In controlled clinical trials, the most common adverse reactions shown by this product are: dizziness (6.5%), headache (5.4%), diarrhea (3.8%) and fatigue (2.9%). Other adverse reactions that occurred above 1% were cough, nausea, rash, symptomatic hypotension, orthostatic hypotension, palpitations, chest pain, and asthma. The most common reasons for withdrawal are headache and cough. Rare adverse reactions are: syncope, peripheral edema, dermatitis, constipation, gastritis, anxiety, insomnia, paresthesia, joint pain, myalgia, asthma, etc.

Allergic / angioneuronic edema Facial, limb, lips, tongue, glottis and / or throat, neuroedema are rare (see precautions) and should be discontinued immediately.

Abnormal laboratory tests Rarely, significant changes have occurred in the standard laboratory test parameters associated with taking this product. After discontinuation of this product, hematuria and plasma creatinine increase, this change is usually reversible. Hemoglobin and hematocrit were slightly reduced. In clinical trials, serum potassium concentrations in individual cases were> 5.7mEq / L, but they were usually transient. The incidence of proteinuria was 0.7%.

[Contraindications] Those who are allergic to this product or other angiotensin-converting enzyme inhibitors are contraindicated. Disable hyperkalemia patients.

【Precautions】

1. Rare symptomatic hypotension in patients with uncomplicated hypertension. If patients already have reduced blood volume (such as diuretics, salt-restricted diets, dialysis, diarrhea, or vomiting), hypotension is more likely to occur with this product. Patients with congestive heart failure may have symptomatic hypotension regardless of whether they are associated with renal insufficiency. Patients with severe heart failure are more likely to develop symptomatic hypotension. These patients should start treatment under the supervision of a doctor, and close adjustments must be made when adjusting the dose of lisinopril and / or diuretics.

If hypotension occurs, the patient may lie supine, and intravenous saline may be administered if necessary. Transient hypotension is not necessary to contraindicate taking this product again. After expanding blood volume to increase blood pressure, it is no problem to take it again.

In normotensive or hypotensive patients with congestive heart failure, lisinopril can cause further reductions in blood pressure, and this effect is expected, usually without interruption of treatment. If symptoms of hypotension occur, it is necessary to reduce the dose or discontinue this product.

2. For patients with renal impairment

In patients with congestive heart failure, hypotension following initial treatment with an ACE inhibitor may cause some degree of further damage to renal function, and this condition may present with acute renal failure (usually reversible). For some patients with bilateral renal artery stenosis or single renal artery stenosis, the use of ACE treatment increases blood urea nitrogen and plasma creatinine, and returns to normal after stopping treatment. This is especially true in patients with renal insufficiency. In some patients with hypertension without renal vascular disease, blood urea nitrogen and increased plasma creatinine are generally mild and temporary. They are more common when used together with diuretics. Patients with pre-existing renal impairment are more likely to have increased blood urea nitrogen and plasma creatinine, and may need to reduce or discontinue this product and / or diuretics.

Solitary kidney, transplanted kidney, bilateral renal artery stenosis and renal dysfunction are contraindicated.

3. Allergies / Angioedema

Patients treated with ACE inhibitors (including: this product) have rare facial, limb, lip, tongue, glottic, and / or throat, neuroedema In these cases, medication should be stopped promptly and the patient should be carefully observed until the swelling disappears. Although antihistamines can relieve symptoms, swelling of the face and lips usually disappears without treatment.

Laryngeal angioedema may be fatal. Such edema (including tongue, glottis, and throat edema) may cause airway obstruction. In this case, an epinephrine solution 1: 1000 (0.3ml ~ 0.5ml) and other treatments.

4. Surgery / Application of Anesthetic

This product can block the formation of angiotensin II in patients undergoing major surgical operations or anesthesia with anesthesia that can cause hypotension, which can cause substitute renin release. If hypotension occurs and is considered to be caused by the above mechanism, it can be corrected by increasing blood volume.

When using this product, there may be ① increased blood urea nitrogen and creatinine concentrations, which are usually temporary, and are easy to occur when there is renal disease or severe hypertension and blood pressure drops rapidly; ② occasionally increased serum liver enzymes; ③ slightly increased potassium, Especially in those with renal dysfunction.

5. Use this product with caution in the following situations: ① Autoimmune diseases such as severe systemic lupus erythematosus, at this time, the chance of white blood cells or granulocytes is increased. ② bone marrow suppression. ③ Insufficient blood supply to the brain or coronary arteries may increase ischemia due to decreased blood pressure. ④ Hyperkalemia. ⑤ Renal dysfunction can cause blood potassium to increase, reduce white blood cells and granulocytes, and keep the product. ⑥ Strict dietary restrictions on sodium salts or dialysis treatment, the first dose of this product may occur sudden and severe hypotension.

6. Follow-up inspection during the use of this product: ① For patients with renal dysfunction or patients with a history of white blood cell deficiency, check the white blood cell count and classified count every 2 weeks for the first 3 months, and then check regularly; ② urine protein test, Once a month.

[Medication for pregnant and lactating women]

1. The application of this product to pregnant women has not been studied. Use in pregnant women only if the potential benefits to pregnant women outweigh the potential risks to the fetus.

2. It is unclear whether this product is secreted into human milk. Because many drugs are secreted into human milk, lactating women should take this product with caution.

[Children's medication] Inadequate research in children. In newborns and infants, there is a risk of oliguria and neurological abnormalities, which may be related to renal and cerebral ischemia caused by lowering blood pressure caused by this product.

[Medicine for the elderly] In clinical studies, there is no age-related change in the effectiveness or safety of this product. However, elderly patients with impaired renal function should determine the starting dose of this product according to the principles in Table 1. Thereafter, according to blood pressure The response adjusts the dose.

【medicine interactions】

1. Combined use with diuretics. Patients receiving this product are usually treated with diuretics and their antihypertensive effect is usually enhanced. For patients who have been treated with diuretics and especially recently with diuretics, excessive reduction in blood pressure may occur when this product is added. By discontinuing diuretics before beginning treatment with this product, the likelihood of symptomatic hypotension can be greatly reduced. This product starts with a small dose and gradually adjusts the dose.

2. The antihypertensive effect is strengthened when used together with other antihypertensive drugs. Among them, it has a large additive effect with drugs that cause renin release or affect sympathetic activity, and it has a lesser additive effect with beta blockers.

3. Used together with sylvite potassium diuretics such as spironolactone, ampicillin, and amiloride may cause hyperkalemia.

4. Non-steroidal anti-inflammatory and analgesic drugs, especially indomethacin, can inhibit the prostaglandin synthesis and cause water and sodium retention. When used with this product, it can reduce the hypotensive effect of this product.

[Drug overdose] The usual treatment method is infusion of normal saline. This product can be removed by hemodialysis.

[Pharmacology and toxicology] lisinopril is a synthetic peptide derivative, which is an oral long-acting angiotensin-converting enzyme inhibitor, which makes the concentration of angiotensin II (a strong vasoconstrictor) and aldosterone Decreased, resulting in peripheral vasodilation and reduced vascular resistance, which lowers blood pressure. Research data show that long-term use of this product will not diminish the effect, and immediate withdrawal will not cause blood pressure rebound. In patients with congestive heart failure, lisinopril reduces the pre- and post-load of the heart and increases cardiac output by dilating the arteries and veins, without reflex tachycardia. This product rarely produces hypokalemia and hyperuricemia caused by thiazine drugs.
The literature reports that the LD 50 value of lisinopril in mice is greater than 9100 mg / 100, the LD 50 value of rats in oral administration is greater than 8500 mg / ㎏, and the LD 50 value of dogs in oral administration is greater than 6000 mg / ㎏.

Application of lisinopril in the second and third stages of pregnancy can cause fetal damage and even death, so it should not be applied at this time. It has not been found to have mutagenic and carcinogenic effects.

[Pharmacokinetics] About 25% (6% ~ 60%) of the drug is absorbed after oral administration, and the absorption is not affected by food. After a single oral dose, the blood concentration reached a peak 7 hours, the half-life was about 12.6 hours, and the drug was taken once a day. After 3 days, the blood concentration reached a steady state. It works within 1 hour after a single oral dose, peaks at 6 hours, and the effect is maintained for about 24 hours. Lisinopril has no obvious metabolism in the liver, and is mainly eliminated by the kidneys as a prototype, and t 1/2 is prolonged in renal failure. There are very few lisinopril drugs that bind to plasma proteins. After oral administration of 10mg of this product, the average distribution volume is 1.24L, and the average renal clearance is 106ml / min. Lisinopril can be removed by hemodialysis.

[Storage] shading and sealed.

[Packing] 5mg: aluminum plastic, 7 tablets / board or 14 tablets / board, 1 plate / box;

10mg: aluminum plastic, 7 tablets / board or 14 tablets / board, 1 plate / box;

[Validity] 24 months

[Executive Standards] 2015 Chinese Pharmacopoeia

[Approval number] 5mg: National Medicine Standard H20020427

10mg: National Medicine Standard H20000110

【manufacturer】