Carvedilol Tablets

Carvedilol has both (1) and non-selective (2) receptor blocking effects within the therapeutic dose range, and has no intrinsic sympathomimetic activity. This product blocks the (1) receptors on the postsynaptic membrane, thereby dilating blood vessels and reducing peripheral vascular resistance; it blocks the (2) receptors, inhibits the secretion of renin by the kidneys, blocks the renin-angiotensin-aldosterone system, and produces a hypotensive effect. Carvedilol lowers blood pressure rapidly and can maintain its hypotensive effect for a long time. It has no effect on left ventricular ejection fraction, cardiac function, renal function, renal blood perfusion, peripheral blood flow, plasma electrolytes and blood lipid levels, does not affect the heart rate or slightly slows it down, and rarely produces water and sodium retention.

The main ingredient of this product is carvedilol.

Active ingredient: One tablet of carvedilol contains 6.25 mg of carvedilol. The tablet is for oral use. The tablet is a film-coated tablet and appears white or off-white after the coating is removed.

1. Essential hypertension: It can be used alone or in combination with other antihypertensive drugs, especially thiazide diuretics. 2. Heart failure: Mild or moderate heart failure (NYHA grade II or III), combined with digitalis, diuretics and angiotensin converting enzyme inhibitors (ACEI). It can also be used for patients with heart failure who are intolerant to ACEI and who are treated with or without digitalis, hydralazine or nitrates.

The dosage must be individualized and needs to be increased under the close supervision of the physician. 1 The recommended starting dose for hypertension is 6.25 mg/time, taken orally twice a day. If tolerated, the standing systolic blood pressure 1 hour after taking the drug is used as a guide to maintain this dose for 7 to 14 days, and then increased to 12.5 mg/time, twice a day, if necessary, based on the blood pressure at the trough concentration. Similarly, the dose can be increased to 25 mg/time, twice a day. Generally, a complete antihypertensive effect is achieved within 7 to 14 days. The total amount should not exceed 50 mg/day. This product must be taken with food to slow absorption and reduce the occurrence of orthostatic hypotension. Adding a diuretic to this product or adding this product to a diuretic is expected to produce an additive effect and expand the orthostatic effect of this product. 2 Heart failure: Before using this product, the doses of digitalis, diuretics, and ACEI (if used) must be stable. The recommended starting dose is 3.125 mg/time, twice a day orally for 2 weeks, and if tolerated, it can be increased to 6.25 mg/time, twice a day. Thereafter, the dose can be doubled every 2 weeks to the maximum dose that the patient can tolerate. Each time a new dose is applied, the patient should be observed for 1 hour for dizziness or mild headache. The recommended maximum dose: 25 mg/time, twice a day for patients <85 kg; 50 mg/time, twice a day for patients >85 kg. This product must be taken with food to slow absorption and reduce the occurrence of orthostatic hypotension. Before each dose increase, assess the condition of cardiac insufficiency, such as worsening cardiac function, vasodilation (dizziness, mild headache, symptomatic hypotension) or bradycardia symptoms to determine tolerance to carvedilol. Transient worsening of cardiac insufficiency can be treated by increasing the dose of diuretics, and occasionally a reduction in carvedilol or temporary discontinuation of the drug is required. Symptoms of vasodilation respond to diuretics or ACEI dose reduction. If symptoms do not improve, carvedilol dose reduction may be required. The dose of this product can be increased only after the heart failure worsens or the symptoms of vasodilation stabilize. If bradycardia (pulse < 55 beats/min) occurs in patients with heart failure, the dose must be reduced.

1. Hypertension: incidence ≥ 1%, adverse events without causal relationship: fatigue, bradycardia, postural hypotension, postural-dependent edema, lower limb edema, dizziness, insomnia, somnolence, abdominal pain, diarrhea, thrombocytopenia, hyperlipidemia, back pain, viral infection, rhinitis, pharyngitis, dyspnea, urinary tract infection. Incidence 0.1%, 2%, adverse events without causal relationship: sweating, fatigue, chest pain, pain, edema, fever, lower limb edema, bradycardia, hypotension, syncope, atrioventricular block, worsening angina, dizziness, headache, diarrhea, nausea, abdominal pain, vomiting, thrombocytopenia, weight gain, gout, increased urea nitrogen, hyperlipidemia, dehydration, hypervolemia, back pain, arthralgia, myalgia, upper respiratory tract infection, infection, sinusitis, tracheitis, pharyngitis, urinary tract infection, hematuria, visual abnormality. Incidence 1%, <2%: allergy, sudden death, malaise, hypovolemia, postural hypotension, hypoesthesia, dizziness, melena, periodontitis, elevated ALT and AST, hyperuricemia, hypoglycemia, hyponatremia, increased alkaline phosphatase, positive urine glucose, purpura, lethargy, abnormal renal function, albuminuria. Rare reports of aplastic anemia, which only occurred when other drugs related to the event were used in combination.

1. Patients with NYHA grade IV decompensated heart failure who require intravenous inotropic drugs; 2. Patients with bronchospasm (two cases of patients with persistent asthma died after taking a single dose of carvedilol) or related bronchospasm; 3. Second or third degree atrioventricular block; 4. Sick sinus syndrome; 5. Cardiogenic shock; 6. Severe bradycardia. 7. Patients with clinically severe liver dysfunction. 8. Patients who are allergic to this product are contraindicated. 9. Diabetic ketoacidosis and metabolic acidosis.

Precautions for children: The safety and efficacy of carvedilol for children under 18 years of age are not yet clear. Precautions for pregnancy and lactation: Human studies are insufficient, and carvedilol can only be used in pregnant women when the benefits to the fetus outweigh the risks. It is unclear whether it is secreted into human breast milk. Many other beta-blockers can be secreted into breast milk, as well as potential serious adverse reactions such as bradycardia, so by weighing the importance of the drug to the mother, it is determined that breastfeeding women should stop taking the drug or stop breastfeeding. Precautions for the elderly: There is no difference in the efficacy and incidence of adverse events between elderly and young patients with heart failure and hypertension.

1. CYP2D6 inhibitors There are no studies on the interaction between carvedilol and CYP2D6 inhibitors (such as quinidine, fluoxetine, paroxetine), but it is expected that this type of drug will increase the concentration of carvedilol dextrorotatory body. Retrospective analysis shows that the incidence of dizziness is high in patients with poor 2D6 metabolizers during the dosage increase period, which is speculated to be due to the vasodilatory effect of the dextrorotatory body with alpha-blocking activity due to the increased concentration. 2. Drugs that deplete catecholamines When carvedilol is taken with drugs that deplete catecholamines (such as reserpine, monoamine oxidase inhibitors), the patient must be closely observed for hypotension and/or severe bradycardia symptoms. 3. Digoxin When carvedilol and digoxin are taken at the same time, the blood digoxin concentration can be increased by 15%. 4. When clonidine is taken at the same time as carvedilol, it may enhance the effect of lowering blood pressure and slowing heart rate. Carvedilol should be discontinued a few days before clonidine is discontinued, and then clonidine should be gradually reduced to discontinuation. 5. Cyclosporine increases the trough concentration of cyclosporine in the blood, and the dose of cyclosporine needs to be reduced to maintain it within the therapeutic concentration. It is recommended to closely monitor the concentration of cyclosporine after starting carvedilol treatment and adjust the dose of cyclosporine appropriately. 6. The liver metabolism inducer and inhibitor remifentanil reduces the plasma concentration of carvedilol by 70%. Cimetidine increases the AUC of carvedilol by 30%, but the Cmax does not change. 7. There are reports of conduction disorders when calcium antagonists are used in combination with diltiazem. It is recommended that, like other beta-receptor blockers, electrocardiograms and blood pressure should be monitored when used in combination with verapamil or diltiazem-type calcium antagonists. 8. Insulin or oral hypoglycemic drugs with beta-receptor blocking activity may enhance the blood sugar-lowering effect of insulin or oral hypoglycemic drugs, so blood sugar needs to be monitored.

Validity period if stored in a light-proof and airtight container: three years.

6.25mg

36 months

Fuan Pharmaceutical Group Ningbo Team Pharmaceutical Co., Ltd.

• Founded in:

  1992-08-12

• Address:

  No. 366, Anping Road, Zhaobaoshan Street, Zhenhai District, Ningbo City, Zhejiang Province

• Tax NO.:

  91330211144072003N

• Registered Funds:

  415 million yuan

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