Urapidil Injection

Urapidil is a selective alpha 1 receptor blocker, and has both peripheral and central hypotensive effects. The peripheral vasodilator effect is mainly through blocking postsynaptic alpha 1 receptors, which significantly reduces peripheral resistance and dilates blood vessels. The central effect is through activating 5-hydroxytryptamine-1A receptors, reducing the sympathetic feedback of the cardiovascular regulation center of the medulla oblongata and playing a hypotensive role. This product has the effect of blocking postsynaptic alpha 1 receptors and blocking peripheral alpha 2 receptors, but the former is dominant. This product has a greater dilating effect on venous blood vessels than on arterial blood vessels, and can reduce renal vascular resistance. It has no hypotensive effect on people with normal blood pressure and has no significant effect on heart rate. Toxicological effects Acute toxicology studies have shown that the ratio of the LD50 of animals (mice, rats, rabbits, dogs) after the application of this product to the daily therapeutic dose of humans is 70 to 180 times after intravenous injection; 100 to 840 times after intravenous drip; and 610 to 870 times after oral administration. Chronic toxicology studies have not found teratogenic, carcinogenic and mutagenic effects. Experiments on rats and mice have shown that this product can increase the level of animal prolactin and stimulate the growth of breast tissue. However, humans do not have the above effects after using the recommended therapeutic dose. According to the study of the drug's mechanism of action, this product will not cause abnormal hormone regulation in humans.

The main ingredient of this product is urapidil. Chemical name: 6-[[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyl-2,4(1H,3H)-pyrimidinedione.

This product is a colorless clear liquid.

1. Used to treat hypertensive crisis (such as a sharp increase in blood pressure), severe and extremely severe hypertension, and refractory hypertension. 2. Used to control perioperative hypertension.

Intravenous injection. Slowly inject 10-15 mg intravenously, monitor blood pressure changes, and the antihypertensive effect should appear within 5 minutes. If the effect is not satisfactory, the drug can be repeated, continuous intravenous drip or infusion pump can be used. After intravenous injection, in order to maintain its antihypertensive effect, this product can be continuously intravenously dripped, and the liquid is prepared as follows; usually 250 mg of urapidil (equivalent to 10 urapidil injections) is added to a suitable liquid, such as normal saline, 5% or 10% glucose, 5% fructose solution. If an infusion pump is used to maintain the dose, 20 ml of injection (= 100 mg of urapidil) can be added and then diluted to 50 ml with the above liquid. The maximum drug concentration of intravenous infusion is 4 mg of urapidil per milliliter. The infusion rate is adjusted according to the patient's blood pressure. The recommended initial rate is 2 mg/min and the maintenance rate is 9 mg/h. (If 250 mg of urapidil is dissolved in 500 ml of liquid, 1 mg of urapidil is equivalent to 44 drops or 2.21 ml of infusion liquid). Intravenous drip or infusion with an infusion pump should be used after intravenous injection to maintain blood pressure stability. The degree of blood pressure drop is determined by the dose of the drug infused within the first 15 minutes, and then maintained with a low dose. The course of treatment generally does not exceed 7 days.

After using this product, patients may experience headache, dizziness, nausea, vomiting, sweating, irritability, fatigue, palpitations, arrhythmia, upper chest oppression or dyspnea, etc., which are mostly caused by too rapid a drop in blood pressure and usually disappear within a few minutes. Patients do not need to stop taking the drug. Allergic reactions are rare (such as itching, skin redness, rash, etc.). In very rare cases, platelet counts decrease when taking this drug orally, but serum immunology studies have not yet confirmed the causal relationship.

It is contraindicated in patients with aortic stenosis or arteriovenous shunts (except for hemodynamically ineffective dialysis shunts).

If the patient is using other antihypertensive drugs, drinking alcohol or has hypovolemia (such as diarrhea, vomiting) at the same time, the antihypertensive effect of this product may be enhanced. The simultaneous use of cimetidine may increase the blood concentration of this product by up to 15%.

Seal and store in a cool place.

5ml:25mg

Tonghua Golden-Horse Pharmaceutical Industey Co., Ltd.

• Founded in:

  1993-02-26

• Address:

  No. 999, Jinma Road, Erdaojiang District, Tonghua City, Jilin Province

• Tax NO.:

  91220501244575134M

• Registered Funds:

  966.494707 yuan

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