What Factors Affect a Sufficient Carvedilol Dose?

Carvedilol tablets, essential hypertension: Carvedilol is suitable for the treatment of essential hypertension and can be used alone or in combination with other antihypertensive drugs, especially thiazide diuretics. Treatment of symptomatic congestive heart failure: Carvedilol is used to treat symptomatic congestive heart failure to reduce mortality and hospitalization of cardiovascular files, improve the general condition of patients and slow disease progression, carvedilol Can be used as an additional treatment for standard treatments, and can also be used for patients who are intolerant to eight or who have not used digitalis, hydralazine, and nitrates.

Drug Name: Carvedilol
Drug type: Occupational injury medical insurance

Hanyu Pinyin: Ka Wei Di Luo Pian
Use classification: Other medications for congestive heart failure

Carvedilol tablets ingredients

The main ingredient of this product is carvedilol,
Its chemical name is: (±) -1- (9H--carbazole-4--oxy) -3- [2- (2-methoxyphenoxyethyl) -amino] -2-propanol Chemical Structure:

Molecular formula: C ₂₄ H ₂₆ N ₂ O ₄
Molecular weight: 406.48

Carvedilol traits

This product is white, off-white tablets or film-coated tablets.

Carvedilol tablets indications

Essential hypertension: Carvedilol is suitable for the treatment of essential hypertension and can be used alone or in combination with other antihypertensive drugs, especially thiazide diuretics.
Treatment of symptomatic congestive heart failure: Carvedilol is used to treat symptomatic congestive heart failure to reduce mortality and hospitalization of cardiovascular files, improve the general condition of patients and slow disease progression, carvedilol Can be used as an additional treatment for standard treatments, and can also be used for patients who are intolerant to eight or who have not used digitalis, hydralazine, and nitrates.

Carvedilol tablets specifications

6.25mg 12.5mg

Carvedilol dosage and dosage

Essential hypertension is recommended once a day.
Adults: The recommended dosage for the first 2 days is 12.5 mg once daily; thereafter, 25 mg each time, once daily. If the disease requires, you can increase the amount to 50 mg daily, 1 daily Take 2 or 2 times ^
Elderly: The initial dose is 12.5mg each time. Satisfactory results can be achieved in some patients once a day. If the effect is not good, the dose can be increased to the recommended maximum dose of 50mg per day after at least two weeks. Take once or daily.
The dose for the treatment of symptomatic congestive heart failure must be individualized, and doctors need to observe closely during the dose increase. Patients receiving digoxin. Diuretics and ACEI must first use these drugs to stabilize the treatment before using carvedilol. The recommended dose for the first two weeks is 3.125 mg each time, twice a day. Increase the dose once at least two weeks to 6.25 mg twice daily; then 12.5 mg twice daily; and then 25 mg twice daily. The dose must be increased to a level that the patient can tolerate. Ceiling. The weight is less than 85 kg, the maximum recommended dose is 25 mg twice daily, and the weight is more than 85 kg, the maximum recommended dose is 50 mg twice daily. Before each dose increase, the doctor needs to assess whether the patient has symptoms of exacerbation of heart failure or vasodilation. Exacerbation of heart failure or retention of water and sodium must be treated with increasing diuretic doses, sometimes reducing the dose of carvedilol or temporarily discontinuing carvedil Delox treatment. When Carvedilol is discontinued for more than two weeks, re-administration should start at 3.125 mg each time, twice a day, and then increase the dose in the recommended way above. Symptoms of vasodilation can be managed by reducing the dose of diuretics. If the symptoms persist, reduce the ACEI (if used) dose, and then reduce the carvedilol dose as needed. Before the symptoms of severe heart failure or vasodilatation stabilize Do not increase the dose of carvedilol.
There are no data on the safety and efficacy of patients under 18 years of age.
Carvedilol treatment generally requires long-term use. Treatment cannot be stopped suddenly and must be gradually reduced. This is particularly important for patients with coronary heart disease.
The method of administration is not related to meals, but patients with congestive heart failure must take carvedilol during meals to slow absorption and reduce the occurrence of orthostatic hypotension.

Carvedilol tablets adverse reactions

Carvedilol is used in the treatment of hypertension and angina pectoris, which is consistent with that observed during congestive heart failure. However, the former has a lower incidence of bad crotches. Some central nervous systems: occasional mild dizziness, headaches, and fatigue, especially in the early stages of treatment. Depression, sleep disturbances, and paresthesia are rare.
Cardiovascular system: early treatment of bradycardia, bradycardia, orthostatic hypotension, rarely syncope. Peripheral circulatory disorders (cold limbs) are uncommon and can exacerbate symptoms in patients with previous intermittent claudication or Raynaud's phenomenon. Edema is uncommon. Angina pectoris is uncommon. Individual patients have atrioventricular block and exacerbation of heart failure. Patients with heart failure may have dizziness and occasionally edema of varying degrees in different parts. Very few patients have complete atrioventricular block or progressive heart failure. I especially at increased doses.
Respiratory system: patients with asthma or dyspnea tend to develop the disease. Nasal congestion is rare.
Digestive system: gastrointestinal discomfort (such as abdominal pain, diarrhea, nausea, etc.) is rare, constipation and vomiting are not common.
Skin and accessories: skin reactions (such as allergic rashes are rare, individual patients may have urticaria, pruritus, lichen planus-like skin reactions. I may have psoriasis-like skin damage or exacerbate the original condition.
Biochemical and blood system: occasional changes in blood transaminase, thrombocytopenia, leukopenia, etc.
Metabolism: Due to the characteristics of -receptor blockers, this drug can cause lacrimal symptoms in patients with recessive diabetes, or exacerbate the symptoms of patients with existing diabetes, and inhibit the reverse glucose regulation mechanism. Patients with heart failure saw weight gain and hypercholesterolemia.
Other: occasional pain in the limbs. Dry mouth, dysuria, sexual dysfunction, visual impairment, and eye irritation are rare. May have dry eye symptoms. Patients with heart failure and diffuse cardiovascular disease and / or renal insufficiency may further aggravate renal damage, and renal failure may occur in individual cases.

Carvedilol taboos

Carvedilol is disabled in the following patients:
1. Those who are allergic to any ingredient of this product.
2. The New York Heart Association class IV decompensated heart failure requires intravenous positive inotropic drugs.
3. Asthma. Chronic obstructive pulmonary disease with bronchospasm (COPD, allergic rhinitis.
I abnormal liver function.
4- degree atrioventricular block, severe bradycardia (heart rate less than 50 beats / min), sick sinus syndrome (including sinoatrial block)
5.I cardiogenic shock.
6. Severe hypotension (systolic blood pressure less than 85mmHg)
7. Within 48 hours before surgery.

Carvedilol precautions

1. Carvedilol and digitalis can slow the atrioventricular conduction velocity, so Carvedil is used for patients with congestive heart failure who have been controlled by digitalis, diuretics and angiotensin converting enzyme inhibitor Be cautious when using dilo.
2. Carvedilol may mask or weaken the early symptoms and signs of acute hypoglycemia, so be careful when using carvedilol in diabetic patients Carvedilol is used in patients with congestive heart failure with diabetes It may make blood sugar difficult to control. Therefore, at the beginning of the use of this drug, blood glucose should be monitored regularly and the dosage of hypoglycemic drugs adjusted accordingly.
3. Carvedilol can cause reversible renal dysfunction in patients with congestive heart failure associated with hypotension (systolic blood pressure less than 100 mmHg), ischemic heart disease, diffuse vascular disease, and / or renal insufficiency In such patients, renal function should be closely monitored when increasing the amount of carvedilol. If renal failure occurs, the use or withdrawal of carvedilol should be reduced.
4. Patients with hemorrhagic heart failure may increase heart failure and sodium and sodium retention during the increase in the dose of carvedilol. At this time, the amount of diuretics should be increased, and carvedilol will not be increased until the above situation recovers. In the rare cases, it may be necessary to reduce the amount of carvedilol or temporarily discontinue the drug. The above conditions usually do not affect the increase of the dose of carvedilol in the future.
5. Carvedilol can only be used in patients with chronic obstructive pulmonary disease who do not require oral or inhaled bronchospasmicide treatment, unless the benefits outweigh the disadvantages. Patients with a tendency to bronchospasm may experience increased respiratory resistance, thereby As a result of respiratory distress, the patient's breathing should be closely observed during the initial phase of carvedilol use and during the increase of dose. If any evidence of bronchospasm is found during treatment, the dose of carvedilol should be reduced in time.
6. Contact lens wearers should be aware that this medicine may cause dry eyes.
7. When stopping carvedilol treatment, do not stop the drug suddenly. People with ischemic heart disease should especially pay attention. Such patients should gradually reduce the dosage and then stop the drug (1-2 weeks).
8. Like other beta-blockers, carvedilol may mask symptoms of hyperthyroidism.
9. Because beta-blockers may increase the chance of allergies in patients or cause exacerbations of allergic reactions, patients with a history of severe allergies and undergoing desensitization treatment should be careful with carvedilol.
10. Pros and cons should be considered in patients with beta-blocker-associated psoriasis before applying carvedilol.
11. Beta-blockers should be used in patients with pheocytoma before using carvedilol. Although carvedilol has pharmacological effects of alpha and beta receptor blockade, there is no clinical experience with this type of patient. Therefore, patients with suspected echinocytoma should be used with caution.
12Prinzmetalis patients with variant angina pectoris may cause chest pain when using non-selective beta blockers. Although the beta blocker of carvedilol may prevent angina pectoris, it has not been used in such patients. Clinical Experience. Therefore, patients with suspected angina pectoris should be used with caution.
13. Carvedilol should be used with caution in patients with peripheral vascular disease, as beta-blockers can worsen arterial insufficiency.
14. Carvedilol may be aggravated in patients with peripheral vascular disorders (such as Raynaud's phenomenon).
15. Carvedilol should be used with caution in surgical patients. Carvedilol and anesthetics have synergistic negative muscle strength and hypotension.
16. Carvedilol can induce bradycardia. If the heart rate is less than 55 beats / min, carvedilol must be reduced.
17. When Carvedilol is used with calcium channel blockers such as verapamil and diltiazem or other combinations, the patient's ECG and blood pressure should be closely monitored.
18. Due to lack of clinical experience, patients with unstable or secondary hypertension should be used with caution.
Impact on drivers and operators:
Carvedilol reduces alertness (such as the ability to drive and operate machines), and this effect varies from person to person. It is more obvious at the beginning of the medication, the dose change and the combined drinking.
19. Use with caution by athletes.

Carvedilol tablets for pregnant and lactating women

Carvedilol does not have sufficient clinical experience in pregnant women. Animal reproduction experiments did not find carvedilol teratogenic. Beta receptor blocker reduces placental perfusion, which may lead to fetal death, intrauterine abortion and premature birth. In addition, side effects can also occur on the fetus and the newborn (especially hypoglycemia and bradycardia can increase the risk of cardiopulmonary complications in the newborn. Therefore, carvedilol should not be used by pregnant women or women who may become pregnant.
Carvedilol and / or its metabolites can be secreted through breast milk, so breastfeeding women should avoid taking this product, and breastfeeding should be stopped if the drug is really needed.

Carvedilol tablets for children

There are no data on the safety and efficacy of patients under 18 years of age.

Carvedilol tablets for elderly

This drug is mainly metabolized in the liver. People with severe liver dysfunction may experience a continuous rise in blood concentration, and elderly patients are often accompanied by low liver function. Therefore, elderly patients should start medication at a low dose (10mg) and pay close attention to it. .

Carvedilol tablets drug interactions

Like other beta-blockers, carvedilol can also enhance the effects of other antihypertensive drugs (such as alpha-receptor antagonists) used in combination, or produce hypotension.
When carvedilol and diltiazem are administered orally, individual patients develop cardiac conduction disorders (the effect on hemodynamics is rarely the same as other drugs with beta receptor blockade, carvedilol, verapamil, and diltiazem, etc. When calcium channel blockers or Class I antiarrhythmic drugs are used in combination, the patient's ECG and blood pressure should be closely monitored, and the combined use of such drugs is strictly prohibited.
In patients with hypertension, the combination of carvedilol and digoxin can increase the steady-state trough concentration of digoxin by 16%. Therefore, it should be used at the beginning of administration, adjustment of the agent, and when the carvedilol is stopped. Strengthen the monitoring of blood concentration of digoxin.
When discontinuing the combination of carvedilol and clonidine, stop carvedilol for a few days before gradually reducing clonidine.
Carvedilol may enhance the effects of insulin or oral hypoglycemic agents, and symptoms and signs of hypoglycemia (especially tachycardia) may be masked or weakened and not easily detected, so regular monitoring of blood glucose levels is recommended.
When Carvedilol is used in patients receiving a rifampicin-mixed functional oxidase inducer, the blood concentration of carvedilol may decrease. When used for patients receiving mixed function oxidase inhibitors such as cimetidine, the blood concentration of carvedilol may increase, so attention should be paid.
When patients use carvedilol during anesthesia, they should closely observe the negative muscle effect and hypotension caused by the cooperation of carvedilol and anesthetics.
Carvedilol in combination with a strong heart type may extend atrioventricular conduction time.

Carvedilol overdose

When severe sinus bradycardia is caused by overdose, first atropine sulfate <0.25-1mg> is given intravenously. Later, isoproterenol hydrochloride (started with a 25ug slow intravenous injection) or m-hydroxisosulfate may be given according to the need -adrenaline (0.5 mg slow intravenous injection) and other beta receptor agonists. If you must increase the amount of beta agonists, take care to avoid high blood pressure.

Carvedilol tablets pharmacology and toxicology

Carvedilol is a neurohumoral antagonist with multiple effects, with non-selective beta-blocking, alpha-blocking and antioxidant properties. Dilate blood vessels by selectively blocking the alpha ₁ adrenergic receptor. Carvedilol reduces peripheral resistance through vasodilation and inhibits the renin-angiotensin-aldosterone system through beta-blocking. Plasma renin activity is reduced and fluid retention is rare. Carvedilol has no intrinsic sympathomimetic activity, and similar to propranolol, it has membrane-stabilizing properties.
Carvedilol is a racemic mixture of a pair of enantiomers. In animal models, both isomers have alpha adrenergic blockade properties. Carvedilol has a non-selective ₁ and ₂ adrenergic receptor blockade, and its effect is related to the L-body of carvedilol.
Carvedilol is a strong antioxidant and a strong reactive oxygen free radical scavenger. Carvedilol and its metabolites have been shown to have anti-oxidant properties in vivo and in vitro in animal tests and in vitro human cell tests.
A two-year study was conducted in rats and mice. Carvedilol was administered at 75 mg / kg / day and 200 mg / kg / day (calculated as mg / m ² , respectively. 12, 16 times, the results showed no carcinogenic effect.
Multiple genotoxicity tests have not shown that carvedilol is mutagenic.
At doses 200mg / kg / day (in mg / m2, is 32 times the most recommended human dose), carvedilol has toxic effects (sedation, weight loss) in adult rats, no significant The dose of toxic and fertility damage is 60mg / kg / day (calculated as mg / m ² is 10 times the maximum recommended human dose)

Carvedilol tablets pharmacokinetics

Carvedilol tablets are quickly absorbed after oral administration, and the maximum blood radon concentration can be reached in about 1 hour, and the first pass effect is obvious. The absolute bioavailability is about 25%. When taken with food, its absorption is slowed, but it has no significant effect on bioavailability, and it can reduce the risk of orthostatic hypotension. Carvedilol is a lipophilic compound, approximately 98% to 99%. Carvedilol binds to plasma proteins and has a volume of distribution of approximately 2 L / kg, which increases in patients with cirrhosis. Carvedilol is widely broken down into various metabolites. The hydroxylation and methylation on the benzene ring can produce 3 metabolites with -blocking activity, which has a weak vasodilator effect. The beta-blocking effect of hydroxyphenol metabolites is approximately 13 times stronger than carvedilol. The elimination half-life of carvedilol is about 6 to 10 hours, and the plasma clearance is about 590ml / min. Elimination is mainly through the biliary tract, excreted by feces, and a small part is excreted by the kidneys as metabolites.
In patients with impaired liver function, due to reduced first-pass effects, the bioavailability of carvedilol increased to 80%.

Carvedilol tablets storage

Shaded and sealed.

Carvedilol tablets packaging

Aluminum plastic packaging, 14 pieces / board / box.

Carvedilol tablet expiration date

36 months

Carvedilol Tablets

2005 Supplement of Chinese Pharmacopoeia

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