Iii Other Third Generation Beta
Blocks the alpha-1, beta-1 and beta-2 receptors and alpha-1 receptor blokade is responsible for the vasodilator effect. It has a partial agonist effect and is metabolised mainly by the liver.
Bucindolol is a non-selective and lipophilic beta blocker with a higher affinity then beta receptors. Vasodilator effects seem to be due to direct alpha-1 blockade.
BEST failed to show any benefit of bucindolol for total mortality in Class III-IV heart failure patients when added to the usual care . In the Class IV patients bucindolol even increased the composite end point of death and heart failure hospitalisations in six-months follow-up. The annual mortality for Class IV patients in the placebo group of the BEST study was 28 % which was higher than CIBIS , COPERNICUS and MERIT-HF studies. It has been suggested that the Class IV patients in BEST study were much sicker than the other studies and this contributed to the less beneficial effect of bucindolol in the BEST study.
Celiprolol is a third generation beta blocker with a weak beta-2 agonist activity and weak alpha 2 blocker and direct smooth muscle relaxing properties. It reduces peripheral vascular resistance and has similar antihypertensive effects to metoprolol, propronalol, atenolol and pindolol. In a study on heart failure patients comparing metoprolol, placebo and celiprolol, both drugs were well tolerated but celiprolol did not show any additional benefit .
How To Cope With Side Effects Of Carvedilol
What to do about:
- feeling dizzy as your body gets used to carvedilol this side effect should wear off. If carvedilol makes you feel dizzy, stop what youre doing and sit or lie down until you feel better. Do not drive or operate machinery until you feel OK again. Try to avoid alcohol as it’ll make you feel worse.
- headaches make sure you rest and drink plenty of fluids. Ask your pharmacist to recommend a painkiller. Do not drink too much alcohol. Headaches usually go away after the first week of taking carvedilol. Talk to your doctor if the headaches last more than a week or are severe.
- feeling tired do not drive, ride a bike, or use tools or machinery if youre feeling tired. Do not drink any alcohol as this will make you feel more tired.
- feeling sick or being sick stick to simple meals and do not eat rich or spicy food. It might help to take your carvedilol after a meal or snack. If you’re being sick, try drinking small, frequent sips of water to avoid dehydration.
- cold fingers or toes put your hands or feet under warm running water, massage them, and wiggle your fingers and toes. Do not smoke or have drinks with caffeine, as this can make your blood vessels narrower and restrict your blood flow. Its best not to wear tight watches or bracelets as well. Try wearing mittens and warm socks. Speak to your doctor if this side effect bothers you.
Before Taking This Medicine
You should not take carvedilol if you are allergic to it, or if you have:
asthma, bronchitis, emphysema
severe liver disease or
a serious heart condition such as heart block, “sick sinus syndrome,” or slow heart rate .
To make sure carvedilol is safe for you, tell your doctor if you have:
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What Is Heart Failure
Heart failure is also known as weakened heart. It does not mean that your heart has stopped, but rather that your heart is not able to pump enough blood to all parts of your body.
- Your heart is a muscle that pumps blood. Blood carries oxygen to your cells. When your heart does not pump enough blood, your body doesnt get enough oxygen
- Because you are not getting enough oxygen, you may feel fatigue. Also, because your heart is not pumping strongly enough, blood may begin to back up in your lungs. This may also cause a build-up of fluid, causing your ankles, feet and legs to swell
- Heart failure occurs when the heart muscle has been damaged, often by conditions such as high blood pressure or heart attack
Carvedilol May Cause Hyperglycemia Call Your Doctor Immediately If You Have Any Of The Following Symptoms Of Hyperglycemia:
- difficulty breathing and swallowing
Carvedilol may cause other side effects. Tell your doctor if you experience any unusual problems while you are taking this medication.
If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration’s MedWatch Adverse Event Reporting program online or by phone .
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Warnings For Other Groups
For pregnant women: Carvedilol is a category C pregnancy drug. That means two things:
Tell your doctor if youre pregnant or plan to become pregnant. Carvedilol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
For women who are breastfeeding: It isnt known if carvedilol passes into breast milk. If it does, it may cause serious effects in a breastfeeding child. You and your doctor may need to decide if youll take carvedilol or breastfeed.
For seniors: Seniors may be more likely to experience dizziness while taking this drug.
For children: It has not been established that carvedilol is safe and effective for use in people under the age of 18 years.
This dosage information is for carvedilol oral tablets. All possible dosages and forms may not be included here. Your dose, form, and how often you take it will depend on:
- Strengths: 3.125 mg, 6.25 mg, 12.5 mg, and 25 mg
- Strengths: 3.125 mg, 6.25 mg, 12.5 mg, and 25 mg
Dosage For Heart Failure
- The recommended starting dosage is 3.125 mg taken twice per day for two weeks.
- It can be increased to 6.25 mg, 12.5 mg, and 25 mg taken twice per day over two-week intervals.
- When you first start the medication and during dosage increases, you might feel dizzy and lightheaded within the first hour of taking your dose. During this time, you shouldnt drive or do any similar activities that require alertness.
A safe and effective dosage hasnt been established for this age group.
- For people with kidney problems: If you have kidney problems, your doctor will closely monitor you during treatment. They may lower your dose or stop treatment if your kidney function gets worse.
Your doctor will monitor you closely during dosage increases.
Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this list includes all possible dosages. This information is not a substitute for medical advice. Always speak with your doctor or pharmacist about dosages that are right for you.
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Left Ventricular Dysfunction Following Myocardial Infarction
DOSAGE MUST BE INDIVIDUALIZED AND MONITORED DURING UP-TITRATION. Treatment with carvedilol tablets may be started as an inpatient or outpatient and should be started after the patient is hemodynamically stable and fluid retention has been minimized. It is recommended that carvedilol tablets be started at 6.25 mg twice daily and increased after 3 to 10 days, based on tolerability, to 12.5 mg twice daily, then again to the target dose of 25 mg twice daily. A lower starting dose may be used and/or the rate of up-titration may be slowed if clinically indicated . Patients should be maintained on lower doses if higher doses are not tolerated. The recommended dosing regimen need not be altered in patients who received treatment with an IV or oral -blocker during the acute phase of the myocardial infarction.
Cautions With Other Medicines
There are some medicines that can affect the way carvedilol works.
Tell your doctor if youre taking:
- other medicines for high blood pressure when taken together with carvedilol, they can sometimes lower your blood pressure too much
- other medicines that can lower your blood pressure these include some antidepressants, nitrates , baclofen , medicines for an enlarged prostate gland like tamsulosin, or levodopa
- medicines for an irregular heartbeat such as amiodarone or flecainide
- medicines for asthma or chronic obstructive pulmonary disease
- medicines for diabetes, particularly insulin carvedilol may make it more difficult to recognise the warning signs of low blood sugar. Speak to your doctor if you have low blood sugar levels without getting any warning signs. You should check your blood sugar after exercise, and follow usual advice about checking it before driving, or operating machinery.
- medicines that treat nose or sinus congestion, or other cold remedies
- medicines for allergies, such as ephedrine, noradrenaline or adrenaline
- non-steroidal anti-inflammatory medicines , such as ibuprofen, diclofenac and naproxen these medicines may increase your blood pressure
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Effects Of Carvedilol On Health Outcomes In Heart Failure
|The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details.
|First Posted : September 27, 2006Last Update Posted : September 27, 2006
The purpose of our study was to determine if a strategy of starting a heart medication before patients leave the hospital and then being seen by a nurse manager would reduce subsequent hospitalizations compared to usual care.
Hypothesis: A nurse-directed heart failure management program with inpatient initiation of beta blockers will improve health outcomes in a vulnerable, predominantly Hispanic and African American population.
|Drug: carvedilol plus nurse management
Comparison: Inpatient initiation of the beta-blocker carvedilol coupled with outpatient follow-up with a nurse manager was compared to usual care by internists and cardiologists.
The Carvedilol Or Metoprolol European Trial
In The Carvedilol Or Metoprolol European Trial two generations of beta-blockers were compared. Metoprolol, a second-generation beta-blocker was compared with the third-generation beta-blocker carvedilol . Both beta-blockers have been proven beneficial for use in a group of patients with heart failure . The aim of the trial from the outset was to study whether the extra effects of carvedilol mattered clinically and therefore the trial was designed to ensure as close as possible beta-1 blocking effect in the two study groups.
All cause mortality in the COMET trial. Copyright © 2003. Reproduced with permission from Poole-Wilson PA, Swedberg K, Cleland JG, et al. 2003. Comparison of carvedilol and metoprolol on clinical outcomes in patients withchronic heart failure in the Carvedilol Or Metoprolol European Trial :randomised controlled trial. Lancet, 362:713.
Abbreviations: COMET, The Carvedilol Or Metoprolol European Trial.
Abbreviations: COMET, The Carvedilol Or Metoprolol European Trial. *p=0.0022, p=0.034, p=0.0040.
The beta2-blocking effect affects the pre-synaptic release of NE, which reduces the amount of NE that can stimulate the beta1-receptors. carvedilol also exerts a more pronounced beta1-binding, and all together this reduces the deleterious effect of NE in heart failure .
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Carvedilol May Interact With Other Medications
Carvedilol oral tablet can interact with other medications, herbs, or vitamins you might be taking. Thats why your doctor should manage all of your medications carefully. If youre curious about how this drug might interact with something else youre taking, talk to your doctor or pharmacist.
Note: You can reduce your chances of drug interactions by having all of your prescriptions filled at the same pharmacy. That way, a pharmacist can check for possible drug interactions.
Examples of drugs that can cause interactions with carvedilol are listed below.
How Should This Medicine Be Used
Carvedilol comes as a tablet and an extended-release capsule to take by mouth. The tablet is usually taken twice a day with food. The extended-release capsule is usually taken once a day in the morning with food. Try to take carvedilol at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take carvedilol exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Swallow the extended-release capsules whole. Do not chew or crush the capsules, and do not divide the beads inside a capsule into more than one dose. If you are unable to swallow the capsules, you may carefully open a capsule and sprinkle all of the beads it contains over a spoonful of cool or room temperature applesauce. Swallow the entire mixture immediately without chewing.
Your doctor will probably start you on a low dose of carvedilol and gradually increase your dose to allow your body to adjust to the medication. Talk to your doctor about how you feel and about any symptoms you experience during this time.
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What If I Take Too Much
The amount of carvedilol that can lead to an overdose varies from person to person.
Taking too much carvedilol can lower your blood pressure, slow your heart rate, and make it difficult to breathe.
Urgent advice: Contact 111 for advice now if:
- you take too much carvedilol
Call 111 or go to 111.nhs.uk
If you need advice for a child under the age of 5 years, call 111.
Carcinogenesis Mutagenesis Impairment Of Fertility
In 2-year studies conducted in rats given carvedilol at doses up to 75 mg per kg per day or in mice given up to 200 mg per kg per day , carvedilol had no carcinogenic effect.
Carvedilol was negative when tested in a battery of genotoxicity assays, including the Ames and the CHO/HGPRT assays for mutagenicity and the in vitro hamster micronucleus and in vivo human lymphocyte cell tests for clastogenicity.
In a combined fertility/developmental/post-natal toxicity study, rats were given carvedilol orally by gavage for 2 weeks before mating and through mating, gestation, and weaning for females and for 62 days prior to and through mating for males. At a dosage of 300 mg per kg per day carvedilol was toxic to adult rats and was associated with a reduced number of successful matings, prolonged mating time, fewer corpora lutea and implants per dam, fewer live pups per litter, and delays in physical growth/development. The no-effect level for overt toxicity and impairment of fertility was 60 mg per kg per day .
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Perspective Of The Comet Trial
The perspective of COMET can be divided in 3 parts: the importance of beta-1 inhibition, the importance of other effects of carvedilol and the clinical consequence.
Three beta-blockers with beta-1 activity have been shown to reduce mortality in CHF. One interpretation of COMET is that a more effective inhibition by carvedilol, either because of a higher dose being given or because carvedilol has a higher affinity for the beta-1 receptor, explained the marked difference. Thus effective beta-1 inhibition with as high a dose as possible is clearly important for the treatment of CHF.
The mortality difference in COMET was marked even though the difference in resting pulse was small. Therefore, it is likely that other effects of carvedilol compared with metoprolol are important for the treatment of heart failure. Further research is necessary to clarify whether beta-2 inhibition, alpha-1 inhibition, antioxidative properties of, inhibition of endothelin-1biosynthesis, or yet another effect is beneficial .
What Should I Know About Storage And Disposal Of This Medication
Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture .
It is important to keep all medication out of sight and reach of children as many containers are not child-resistant and young children can open them easily. To protect young children from poisoning, always lock safety caps and immediately place the medication in a safe location â one that is up and away and out of their sight and reach.
Unneeded medications should be disposed of in special ways to ensure that pets, children, and other people cannot consume them. However, you should not flush this medication down the toilet. Instead, the best way to dispose of your medication is through a medicine take-back program. Talk to your pharmacist or contact your local garbage/recycling department to learn about take-back programs in your community. See the FDA’s Safe Disposal of Medicines website for more information if you do not have access to a take-back program.
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Glycemic Control In Type 2 Diabetes
In general, -blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia. Nonselective -blockers may potentiate insulin-induced hypoglycemia and delay recovery of serum glucose levels. Patients subject to spontaneous hypoglycemia or diabetic patients receiving insulin or oral hypoglycemic agents should be cautioned about these possibilities. In patients with heart failure and diabetes, carvedilol therapy may lead to worsening hyperglycemia, which responds to intensification of hypoglycemic therapy. It is recommended that blood glucose be monitored when carvedilol dosing is initiated, adjusted, or discontinued. Trials designed to examine the effects of carvedilol on glycemic control in patients with diabetes and heart failure have not been conducted. In a trial designed to examine the effects of carvedilol on glycemic control in a population with mild-to-moderate hypertension and well-controlled type 2 diabetes mellitus, carvedilol had no adverse effect on glycemic control, based on HbA1c measurements .