Nicardipine Hydrochloride Tablets
Function and Efficacy
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 the peripheral vascular resistance of the human body, lowers blood pressure, and can reduce the systolic and diastolic blood pressure of 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 lowering blood pressure. 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 showed that this product dilates coronary arteries and increases local myocardial blood flow, but does not affect atrioventricular conduction. Carcinogenicity, mutagenicity and reproductive toxicity Rats were given nicardipine 5, 15 or 45 mg/kg daily, and the results after two years showed that thyroid hyperplasia and neoplasia (follicular adenomas/tumors) increased with increasing doses. Studies on 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. A slow increase in TSH can cause high thyroid excitement. Rats with iodine-deficient diets were given nicardipine for one month and thyroid hyperplasia occurred, which could be prevented by supplementing T4. Mice were given nicardipine 100 mg/kg daily, and no tumor formation or thyroid changes in any tissue were found after 18 months. Dogs were given nicardipine 25 mg/kg daily, and no thyroid pathological changes were found after 1 year; nicardipine was not found to affect human thyroid function (plasma T4 and TSH). In the reproductive toxicity test on microbial indicator bacteria, the micronucleus test on mice and hamsters, or the sister chromatid exchange test on hamsters, no mutagenicity of nicardipine was found. No reproductive impairment was observed in male and female rats after oral administration of nicardipine at 100 mg/kg.
Ingredients
Nicardipine Hydrochloride
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| Nicardipine hydrochlorideIngredients |
Calcium channel blockers inhibit the transmembrane calcium ion influx of the myocardium and vascular smooth muscle without changing the blood calcium concentration; they have high vascular selectivity, dilate the coronary vascular smooth muscle, increase the exercise tolerance of patients with chronic stable angina pectoris, and reduce the frequency of angina attacks; they reduce the body's peripheral vascular resistance, lower blood pressure, and can lower the systolic and diastolic blood pressure in patients with mild to moderate hypertension; they increase the cardiac ejection fraction and cardiac output, with little change in left ventricular end-diastolic pressure; they temporarily increase urinary sodium excretion; and they block slow calcium channels without affecting fast sodium channels. More |
54527-84-3 | 33 |
Appearance
This product is brown or tan granules; it tastes sweet and slightly bitter.
Indication
Essential hypertension. Cerebrovascular diseases such as cerebral arteriosclerosis, cerebral thrombosis and sequelae of cerebral hemorrhage. Coronary heart disease and various types of angina pectoris.
Usage and Dosage
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.
Adverse Reactions
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 aggravated angina pectoris. Reduce the dose or increase the dosage.
Precautions
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.
Drug Interactions
1. It is well tolerated 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. The blood concentration of digoxin has not been increased when used in combination with digoxin, but the blood concentration of digoxin must be measured. 4. The blood concentration of cyclosporine increases when used in combination with cyclosporine, so the blood concentration of cyclosporine must be closely monitored and the dose of cyclosporine must 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.
Storage
Keep sealed.
Packaging Specification
10mg
Validity Period
24 months
Manufacturer
Shanghai Worldbest Anhui JINHUI Pharmaceutical Co., Ltd.
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Founded in:
1989-11-27 -
Address:
No. 160 Lianhua Road, Yingzhou District, Fuyang City, Anhui Province -
Tax NO.:
91341200151860120M -
Registered Funds:
93 million yuan -
Website:
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Email: