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Nicardipine Hydrochloride and Sodium Chloride Injection

Function and Efficacy

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. 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. 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 blood pressure is lowered. This product increases cardiac ejection fraction and cardiac output, and the left ventricular end-diastolic pressure does not change much. This product can temporarily increase urinary sodium excretion. 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. Toxicological effects: When nicardipine hydrochloride injection was administered to pregnant rats at doses up to 5 mg/kg/day and to pregnant rabbits at doses up to 0.5 mg/kg/day, no embryotoxicity or teratogenicity was observed. Embryotoxicity was observed in rats at doses of 10 mg/kg/day and in rabbits at doses of 1 mg/kg/day, but no teratogenicity was observed at these doses. No adverse effects on the fetus were observed when New Zealand white rabbits were treated with doses of up to 100 mg nicardipine/kg/day (at this therapeutic dose, mortality was significantly increased) during organogenesis. Oral administration of nicardipine up to 100 mg/kg/day (50 times the maximum recommended human dose) to pregnant rats showed no signs of embryolethality or teratogenicity. However, dystocia, reduced birth weight, decreased neonatal survival, and reduced weight gain were noted.

Ingredients

Nicardipine Hydrochloride Sodium Chloride

Name Description Content CAS NO. Manufacturer
Nicardipine hydrochlorideIngredients

Calcium channel blockers inhibit the transmembrane calcium ion influx of the myocardium and vascular smooth muscle, have a high degree of vascular selectivity, dilate coronary vascular smooth muscle, reduce peripheral vascular resistance, lower blood pressure, increase cardiac ejection fraction and cardiac output, temporarily increase urinary sodium excretion, and do not affect fast sodium channels and atrioventricular conduction.

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54527-84-3 33
Sodium chlorideExcipients

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. 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. 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 blood pressure is lowered. This product increases cardiac ejection fraction and cardiac output, and the left ventricular end-diastolic pressure does not change much. This product can temporarily increase urinary sodium excretion. 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. Toxicological effects: When nicardipine hydrochloride injection was administered to pregnant rats at doses up to 5 mg/kg/day and to pregnant rabbits at doses up to 0.5 mg/kg/day, no embryotoxicity or teratogenicity was observed. Embryotoxicity was observed in rats at doses of 10 mg/kg/day and in rabbits at doses of 1 mg/kg/day, but no teratogenicity was observed at these doses. No adverse effects on the fetus were observed when New Zealand white rabbits were treated with doses of up to 100 mg nicardipine/kg/day (at this therapeutic dose, mortality was significantly increased) during organogenesis. Oral administration of nicardipine up to 100 mg/kg/day (50 times the maximum recommended human dose) to pregnant rats showed no signs of embryolethality or teratogenicity. However, dystocia, reduced birth weight, decreased neonatal survival, and reduced weight gain were noted.

More
7647-14-5 43

Appearance

This product is a colorless clear liquid.

Indication

This product is suitable for short-term treatment of hypertension patients who are not suitable or cannot be treated orally. In order to achieve long-term blood pressure control, patients should switch to oral treatment as long as the clinical situation allows.

Usage and Dosage

Intravenous drip method. Dilute the concentration of 0.1mg/ml with glucose injection or 0.9% sodium chloride injection before dripping and slowly and continuously infuse. The diluted solution can be placed stably for 24 hours at room temperature. It cannot be compatible with sodium bicarbonate (5%) injection or lactated Ringer's injection. When patients who have not used this drug start treatment, the time course of blood pressure reduction depends on the starting speed of infusion and the number of doses. In order to gradually lower blood pressure, drip at a rate of 50ml/hour (5.0mg/hour) when starting treatment. If a satisfactory antihypertensive effect is not obtained at this dose, the infusion rate can be increased by 25ml/hour (2.5mg/hour) every 15 minutes, up to a maximum of 150mg/hour (15.0mg/hour) until a satisfactory antihypertensive effect is obtained. In order to lower blood pressure faster, drip at a rate of 50ml/hour (5.0mg/hour) when starting treatment. If a satisfactory antihypertensive effect is not achieved at this dose, the infusion rate can be increased by 25 ml/hour (2.5 mg/hour) every 5 minutes, up to a maximum of 150 mg/hour (15.0 mg/hour), until a satisfactory antihypertensive effect is achieved. After the target blood pressure is achieved, the infusion rate should be reduced to 30 ml/hr (3.0 mg/hr).

Adverse Reactions

Common symptoms include: headache, hypotension, tachycardia, nausea, vomiting, etc. Rare symptoms include fever, neck pain, angina pectoris, atrioventricular block, ST segment depression, T wave inversion, deep vein thrombosis and phlebitis, indigestion, thrombocytopenia, hypophosphatemia, peripheral edema, confusion, intracranial hypertension, respiratory disorders, conjunctivitis, hearing impairment, tinnitus, frequent urination, etc.

Precautions

1. Patients allergic to nicardipine are contraindicated. 2. Patients with severe aortic stenosis are contraindicated. 3. Clinical experience with the use of nicardipine hydrochloride injection in hypertensive patients with pheochromocytoma is limited, so these patients should be treated with caution. 4. In order to minimize the risk of peripheral venous irritation, it is recommended to change the injection site every 12 hours. 5. Patients with liver damage or reduced liver blood flow should use the drug with caution. A lower dose is recommended. 6. Patients with mild to moderate hypertension and moderate renal impairment should use with caution. 7. For patients with congestive heart failure, caution should be used when nicardipine hydrochloride injection is used in combination with β-blockers.

Drug Interactions

1 When treated with nicardipine hydrochloride capsules, cimetidine increases the plasma concentration of nicardipine. The interaction with other histamine-2 receptor antagonists is not clear. 2 Co-administration of nicardipine hydrochloride injection and cyclosporine results in increased plasma concentrations of cyclosporine.

Storage

Keep away from light and store in a sealed container.

Packaging Specification

100ml: Nicardipine 0.02g and sodium chloride 0.9g

Manufacturer

Echo Group Jiangxi Dongya Pharmaceutical Co., Ltd.

  • Founded in:

    2005-08-10
  • Address:

    No. 6 Huiyingbi Road, Dongshan Industrial Park, Economic Development Zone, Dongxiang District, Fuzhou City, Jiangxi Province
  • Tax NO.:

    91361029778807964A
  • Registered Funds:

    73.333333 million yuan
  • Email:

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