Carvedilol dispersible tablets
Function and Efficacy
Carvedilol is a neurohumoral antagonist with multiple actions, including non-selective beta-blocking, alpha-blocking and antioxidant properties. The vasodilatory effect is a selective alpha1-adrenergic receptor blocking action. Carvedilol reduces peripheral resistance by vasodilation and inhibits the renin-angiotensin-aldosterone system by beta-blockade. Plasma renin activity is reduced and fluid retention rarely occurs. Carvedilol does not have the intrinsic sympathomimetic activity of propranolol and it has membrane stabilizing properties. Carvedilol is a racemic mixture of two stereoisomers. In animal models, both isomers have alpha-adrenergic receptor blocking properties. The beta-adrenergic receptor blocking effect is a non-selective beta1 and beta2 adrenergic receptor blocking effect, and its action is related to the levorotatory form of carvedilol. Carvedilol is a strong antioxidant and a strong reactive oxygen free radical scavenger. The antioxidant properties of carvedilol and its metabolites have been confirmed by in vivo and in vitro animal studies and in vitro various human cell studies.
Ingredients
Molecular weight: C24H26N2O4
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| CarvedilolIngredients |
Carvedilol is a neurohumoral antagonist with multiple actions, including non-selective beta-blocking, alpha-blocking and antioxidant properties. The vasodilatory effect is a selective alpha1-adrenergic receptor blocking action. Carvedilol reduces peripheral resistance by vasodilation and inhibits the renin-angiotensin-aldosterone system by beta-blockade. Plasma renin activity is reduced and fluid retention rarely occurs. Carvedilol does not have the intrinsic sympathomimetic activity of propranolol and it has membrane stabilizing properties. Carvedilol is a racemic mixture of two stereoisomers. In animal models, both isomers have alpha-adrenergic receptor blocking properties. The beta-adrenergic receptor blocking effect is a non-selective beta1 and beta2 adrenergic receptor blocking effect, and its action is related to the levorotatory form of carvedilol. Carvedilol is a strong antioxidant and a strong reactive oxygen free radical scavenger. The antioxidant properties of carvedilol and its metabolites have been confirmed by in vivo and in vitro animal studies and in vitro various human cell studies. More |
72956-09-3 | 52 |
Appearance
Dispersible tablets.
Indication
Essential hypertension: It can be used alone or in combination with other antihypertensive drugs, especially thiazide diuretics. 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.
Usage and Dosage
Essential hypertension. It is recommended to take the drug once a day. Adults: The recommended dose for the first two days is 12.5 mg (i.e. 1 tablet) once a day, and then 25 mg (i.e. 2 tablets) once a day. If the condition requires, the dose can be increased to the maximum recommended dose of 50 mg (i.e. 4 tablets) per day after two weeks, taken once a day or in two divided doses. Elderly: An initial dose of 12.5 mg (i.e. 1 tablet) once a day can achieve satisfactory results in some patients. If the effect is not good, the dose can be increased to the maximum recommended dose of 50 mg (i.e. 4 tablets) per day after an interval of at least two weeks, taken once a day or in divided doses. The dose for treating symptomatic congestive heart failure must be individualized, and the doctor needs to observe closely during the dose increase. Patients receiving digoxin, diuretics, and ACEI treatment
Adverse Reactions
The adverse events that occur when carvedilol is used to treat hypertension and angina pectoris are consistent with those observed in congestive heart failure, but the incidence of adverse reactions in the former is lower. 1. Central nervous system - Mild dizziness, headache, and fatigue occasionally occur, especially in the early stages of treatment. - Depression, sleep disorders, and paresthesias are rare. 2. Cardiovascular system - Bradycardia and postural hypotension occasionally occur in the early stages of treatment, and syncope is rare. - Peripheral circulation disorders (cold limbs) are uncommon and may aggravate symptoms in patients with existing intermittent claudication or Raynaud's phenomenon. - Edema is uncommon. - Angina pectoris is uncommon. - Some patients experience atrioventricular conduction block and worsening of heart failure. - Patients with heart failure may experience dizziness, occasional edema of varying degrees in different parts, and complete atrioventricular conduction.
Precautions
1. Patients with NYHA grade IV decompensated heart failure who need intravenous inotropic drugs are contraindicated; 2. Patients with bronchospasm (two cases of patients with persistent asthma died after taking a single dose of carvedilol) or related bronchospasm are contraindicated; 3. Patients with second-degree or third-degree atrioventricular block or sick sinus syndrome are contraindicated; 4. Patients with cardiogenic shock and severe bradycardia are contraindicated; 5. Patients with clinically severe liver dysfunction are contraindicated; 6. Patients who are allergic to this product are contraindicated; 7. Patients with diabetic ketoacidosis and metabolic acidosis are contraindicated; 8. Lactating women are contraindicated.
Special Population Medication
Precautions for children: There is no research data on the safety and efficacy of patients under 18 years old. Precautions for pregnancy and lactation: There is no sufficient clinical experience in the use of carvedilol in pregnant women. Animal reproduction experiments have not found carvedilol to be teratogenic. Beta-blockers reduce placental perfusion, which may lead to intrauterine fetal death, miscarriage and premature birth. In addition, side effects may occur on the fetus and newborn (especially hypoglycemia and bradycardia). It also increases the risk of cardiopulmonary complications in newborns. Pregnant women should not use carvedilol unless the benefits outweigh the risks. Carvedilol and/or its metabolites can be secreted through breast milk, so breastfeeding is not recommended during carvedilol treatment. Precautions for the elderly: See [Usage and Dosage].
Drug Interactions
1. Like other beta-blockers, carvedilol can also enhance the effects of other antihypertensive drugs (such as alpha-blockers) used in combination, or produce hypotension. When carvedilol is used in combination with diltiazem, some patients experience heart conduction block (the effect on hemodynamics is rare). However, like other drugs with beta-blocking effects, when carvedilol is used in combination with calcium channel blockers such as verapamil and diltiazem, the patient's electrocardiogram and blood pressure should be closely monitored, and intravenous co-use of such drugs is strictly prohibited. 2. When carvedilol and digoxin are used in combination in hypertensive patients, the steady-state blood concentration of digoxin will increase by about 16%. Therefore, the monitoring of digoxin blood concentration should be strengthened at the beginning stage of carvedilol use, the dose adjustment stage and when carvedilol is discontinued. 3.
Storage
Keep sealed.
Packaging Specification
6.25mg
Validity Period
24 months
Manufacturer
Zhejiang Jingxin Pharmaceutical Co., Ltd.
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Founded in:
1999-02-13 -
Address:
No. 800, Xinchang Avenue East Road, Yulin Street, Xinchang County, Zhejiang Province -
Tax NO.:
91330000704503984N -
Registered Funds:
861.02914 million yuan -
Website:
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Email: