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Urapidil Hydrochloride Injection

Function and Efficacy

Urapidil is uracil substituted with benzoxazosin. This product has both peripheral and central hypotensive effects. Peripherally, it mainly blocks postsynaptic α1 receptors, causing vasodilation and significantly reducing peripheral resistance. It also has a weaker presynaptic α2 blocking effect, blocking the vasoconstrictive effect of catecholamines (different from the peripheral effect of prazosin); the central effect is mainly through stimulating serotonin-1A (5-HT1a) receptors, reducing the sympathetic feedback regulation of the medullary cardiovascular center and lowering blood pressure (different from the central effect of clonidine). While lowering blood pressure, this product generally does not cause reflex tachycardia. In open clinical studies, single anesthesia can reduce systolic and diastolic blood pressure by 3.1% and 2.1%, respectively, and for hypertensive patients, it can reduce them by 12% and 6.7%, respectively.

Ingredients

Ingredients: Urapidil hydrochloride. Chemical name: 6-[[3-[4-(2-methoxyphenyl)-1-piperazinyl]propyl]amino]-1,3-dimethyl-2,4(1H,3H)-pyrimidinedione hydrochloride.

Name Description Content CAS NO. Manufacturer
Urapidil hydrochlorideIngredients

Urapidil is a benzoxazosin-substituted uracil, which has both peripheral and central hypotensive effects. The periphery mainly blocks postsynaptic α1 receptors, causing vasodilation and significantly reducing peripheral resistance. It also has a weak presynaptic α2 blocking effect, blocking the vasoconstriction effect of catecholamines; the central effect is mainly through stimulating serotonin-1A (5-HT1a) receptors, reducing sympathetic feedback regulation of the medullary cardiovascular center and lowering blood pressure. While lowering blood pressure, it generally does not cause reflex tachycardia. In clinical open studies, single anesthesia can reduce systolic and diastolic blood pressure by 3.1% and 2.1%, respectively, and for hypertensive patients, it can reduce them by 12% and 6.7%, respectively.

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Indication

1. Hypertensive crisis (such as a sudden increase in blood pressure) 2. Severe and extremely severe hypertension 3. Refractory hypertension; 4. Control of perioperative hypertension.

Usage and Dosage

Urapidil injection should be given intravenously or by intravenous drip, and the patient should lie down. Single and repeated intravenous injections and long-term intravenous drips are both possible. It can also be continued intravenously after intravenous injection. Intravenous injection: Slowly inject 10-50 mg of urapidil injection, monitor blood pressure changes, and the antihypertensive effect should be shown within 5 minutes. If the effect is not satisfactory, the drug can be repeated. Continuous intravenous drip or use of infusion pump: After intravenous injection, in order to maintain its antihypertensive effect, this product can be continuously intravenously dripped. The liquid is prepared as follows: Usually 250 mg of urapidil is added to a suitable liquid, such as normal saline, 5% or 10% glucose, 5% fructose plus normal saline. If an infusion pump is used to maintain the dose, 20 ml of injection solution (equivalent to 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 as appropriate according to the patient's blood pressure. The recommended initial rate is 2 mg per minute and the maintenance rate is 9 mg per hour. (If 250 mg of urapidil is dissolved in 500 ml of liquid, 1 mg of urapidil is equivalent to 44 drops or 2.2 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 reduction is determined by the dose of the drug infused in the first 15 minutes, and then maintained with a low dose.

Adverse Reactions

1. After using urapidil, some cases may experience headache, dizziness, nausea, vomiting, sweating, irritability, fatigue, palpitations, arrhythmia, upper facial pressure or dyspnea. The reason is that the blood pressure drops too quickly. Usually, it disappears within a few minutes. The patient does not need to stop taking the drug. If the blood pressure drops too much, you can raise the lower limbs and replenish blood volume to improve. 2. Allergic reactions are rare (such as itching, skin redness, rash, etc.). 3. In very rare cases, the platelet count decreases when taking this drug orally, but serum immunology studies have not yet confirmed the causal relationship.

Precautions

1. Patients with aortic stenosis or arteriovenous shunt (except hemodynamically ineffective dialysis shunt). 2. Breastfeeding women.

Special Population Medication

Precautions for children: This drug is rarely used in children, and there is currently a lack of data on this aspect. Precautions for pregnancy and lactation: There is no data on the safety of urapidil injection in the first 6 months of pregnancy, and the data on its use in the last three months of pregnancy is also incomplete. For pregnant women, this drug should only be used when absolutely necessary. There is no data for breastfeeding women, so it is not suitable for use. Precautions for the elderly: This product should be used with caution in elderly patients, and the initial dose should be small. The sensitivity of elderly patients to drugs is sometimes difficult to estimate.

Drug Interactions

1. Urapidil injection cannot be mixed with alkaline liquids, as its acidic nature may cause turbidity or floc formation. 2. The antihypertensive effect of this product can be enhanced when used with antihypertensive drugs or drinking alcohol. 3. The blood concentration of this product can be increased by 15% when used with cimetidine. 4. There is currently insufficient information to indicate that this product can be used with angiotensin-converting enzyme inhibitors, so it is not recommended to use it with angiotensin-converting enzyme inhibitors. If other antihypertensive drugs are used at the same time, drinking alcohol, or the patient has hypovolemia, such as diarrhea and vomiting, the antihypertensive effect of urapidil injection can be enhanced.

Storage

Keep away from light and keep in airtight container.

Packaging Specification

5ml:25mg (based on urapidil)

Manufacturer

HE BEI YI PIN Pharmaceutical Co., Ltd.

  • Founded in:

    2013-05-29
  • Address:

    Sanxia Road, Shijiazhuang Economic and Technological Development Zone
  • Tax NO.:

    911300000694342458
  • Registered Funds:

    68.68 million yuan
  • Email:

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