Nicardipine Hydrochloride Tablets

Pharmacological action 1 This product is a calcium channel blocker (slow channel blocker or calcium ion antagonist), which can inhibit the transmembrane calcium ion influx of myocardial and vascular smooth muscle without changing the blood calcium concentration. This product has a high degree of vascular selectivity, and its calcium ion antagonist effect on vascular smooth muscle is stronger than that on myocardium. 2 In animal experiments, this product dilates coronary vascular smooth muscle. This product can increase the exercise tolerance of patients with chronic stable angina pectoris and reduce the frequency of angina attacks. 3 This product reduces human peripheral vascular resistance, lowers blood pressure, and can reduce systolic and diastolic blood pressure in patients with mild and moderate hypertension, but does not change the circadian rhythm of blood pressure. This effect is greater in patients with hypertension than in those with normal blood pressure, and there is a reflex increase in heart rate and increased myocardial contractility when blood pressure is lowered. 4 This product increases cardiac ejection fraction and cardiac output, and the left ventricular end-diastolic pressure does not change much. 5 It can temporarily increase urinary sodium excretion. 6 This product blocks slow calcium channels without affecting fast sodium channels. Experiments on anesthetized dogs show that this product dilates coronary arteries and increases local myocardial blood flow, but does not affect atrioventricular conduction. Carcinogenicity, Mutagenesis and Reproductive Toxicity Rats were given nicardipine at 5, 15 or 45 mg/kg daily, and results after two years showed that thyroid hyperplasia and neoplasia (follicular adenomas/tumors) increased with increasing doses. Studies in rats showed that these results were associated with a nicardipine-induced decrease in plasma thyroxine (T4) levels, accompanied by an increase in plasma thyrotropin (TSH) levels. The slow increase in TSH can cause hyperexcitation of the thyroid gland. Rats with iodine-deficient diets given nicardipine for one month developed thyroid hyperplasia, which could be prevented by supplementation with T4. Mice were given nicardipine at 100 mg/kg daily, and no neoplasia or thyroid changes were found in any tissue after 18 months. Dogs were given nicardipine at 25 mg/kg daily, and no thyroid pathology was found after one year; nicardipine was not found to affect human thyroid function (plasma T4 and TSH). Nicardipine was not found to be mutagenic in reproductive toxicity tests with microbial indicator bacteria, micronucleus tests in mice and hamsters, or sister chromatid exchange tests in hamsters. No impairment of reproductive capacity was observed in male and female rats after oral administration of 100 mg/kg of nicardipine.

The main component of this product and its chemical name are: 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dihydroxy acid, 3-[beta;-(N-benzyl-N-methylamino)]ethyl ester-5-methyl ester acid salt. Its structural formula is: Molecular formula: C26H29N3O6HCL Molecular weight: 515.99

This product is slightly yellow tablet or sugar-coated tablet.

1. Hypertension. 2. Exertional angina pectoris.

Oral administration for hypertension, starting dose 20 mg/time, 3 times a day, the dose can be adjusted to 40 mg/time, 3 times a day depending on the response. Administer the drug continuously for at least 3 days before increasing the dose to ensure that the steady-state blood concentration is reached. It can be used in combination with anti-hypertensive drugs such as diuretics and beta-blockers. Oral administration for angina pectoris, starting dose 20 mg/time, 3 times a day, the dose can be adjusted to 40 mg/time, 3 times a day depending on the response. Administer the drug continuously for at least 3 days before increasing the dose to ensure that the steady-state blood concentration is reached. It can be used in combination with anti-anginal drugs such as nitrates and beta-blockers.

1. Common symptoms include edema of the ankles, dizziness, headache, and facial flushing. 2. Elevated levels of alanine aminotransferase (GPT) and aspartate aminotransferase (GOT) may occur. 3. Less common symptoms include palpitations, tachycardia, and worsening angina pectoris, which can be corrected by reducing the dose or adding beta-receptor blockers. 4. Rare symptoms include nausea, dry mouth, constipation, fatigue, and rash. 5. Occasionally, bilirubin, lactate dehydrogenase, cholesterol, urea nitrogen, and creatinine may increase; granulocytopenia may occur.

1. Patients with allergic reaction to this product. 2. Patients with severe aortic stenosis. 3. Patients with intracranial hemorrhage that has not yet completely stopped. 4. Patients with increased intracranial pressure in the acute stage of cerebral stroke.

Precautions for children: Not clear yet. Precautions for pregnancy and lactation: There is still a lack of well-controlled studies on the use of this product in pregnant women. Some animal experiments have adverse effects, so the use of this product in humans must weigh the pros and cons. This product may be excreted into breast milk. After rats took this product orally, high concentrations of nicardipine were detected in breast milk, so it is recommended that lactating women do not use this drug. Precautions for the elderly: No differences were found in the pharmacokinetic studies of this product in the elderly (≥65 years old) and young and middle-aged people, so the medication for the elderly is the same as that for young and middle-aged people.

1. Good tolerance when used in combination with adrenergic beta-receptor blockers. 2. The plasma concentration of this product can be increased when used in combination with cimetidine, so it should be monitored carefully. 3. No increase in digoxin blood concentration was observed when used in combination with digoxin, but the digoxin blood concentration must be measured. 4. When used in combination with cyclosporine, the blood concentration of cyclosporine increased, so the blood concentration of cyclosporine must be closely monitored and the dose of cyclosporine should be reduced accordingly. 5. The addition of therapeutic concentrations of furosemide, propranolol, dimethoprim, warfarin, quinidine, and naproxen to human plasma in vitro does not change the protein binding rate of this product.

Keep sealed.

10 mg

24 months

Shenyang Kangzhi Pharmaceutical Co., Ltd.

• Founded in:

  1979-11-08

• Address:

  No. 7A1, Kaifa Road, Shenyang Economic and Technological Development Zone

• Tax NO.:

  912101001179954513

• Registered Funds:

  12.678899 yuan

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