Carvedilol

Carvedilol Uses, Dosage, Side Effects, Food Interaction and all others data.

(Carvedilol) is a cardiovascular drug whose main pharmacological action is non-selective antagonism of β-adrenergic receptors but which also possesses appreciable α-adrenergic antagonistic activity. It also has antiproliferative properties and is a scavenger of reactive free oxidant radicals. It is used in the treatment of hypertension, angina pectoris and congestive heart failure.

Carvedilol reduces tachycardia through beta adrenergic antagonism and lowers blood pressure through alpha-1 adrenergic antagonism. It has a long duration of action as it is generally taken once daily and has a broad therapeutic index as patients generally take 10-80mg daily. Patients taking carvedilol should not abruptly stop taking this medication as this may exacerbate coronary artery disease.

Trade Name Carvedilol
Availability Prescription only
Generic Carvedilol
Carvedilol Other Names Carvedilol, Carvédilol, Carvedilolum
Related Drugs amlodipine, aspirin, lisinopril, metoprolol, losartan, furosemide, hydrochlorothiazide, propranolol, spironolactone, warfarin
Weight 25mg, , 6.25mg, 3.125mg, 3, 125mg
Type Tablet
Formula C24H26N2O4
Weight Average: 406.4742
Monoisotopic: 406.18925733
Protein binding

Carvedilol is 98% protein bound in plasma. 95% of carvedilol is bound to serum albumin.

Groups Approved, Investigational
Therapeutic Class Alpha adrenoceptor blocking drugs, Beta-adrenoceptor blocking drugs, Beta-blockers
Manufacturer Mylan, Pratapa Nirmala, Darya Varia, Ecomed Pharma Limited
Available Country United Kingdom, United States, Indonesia, Netherlands, Nigeria
Last Updated: September 19, 2023 at 7:00 am
Carvedilol
Carvedilol

Uses

(Carvedilol) is used for the treatment of mild or moderate {NYHA (New York Heart Association) class II or III} heart failure of ischemic or cardiomyopathic origin, in conjunction with digitalis, diuretics and ACE inhibitor, to reduce the progression of disease as evidenced by cardiovascular death, cardiovascular hospitalization, or the need to adjust other heart failure medications. Carvista (Carvedilol) may be used in patients unable to tolerate an ACE inhibitor. Carvista (Carvedilol) may be used in patients who are not receiving digitalis, hydralazine or nitrate therapy.

Carvedilol is also used to associated treatment for these conditions: Atrial Fibrillation, Chronic Stable Angina Pectoris, High Blood Pressure (Hypertension), LVEF ≤40% Left ventricular dysfunction, NYHA Class I or II heart failure, Chronic heart failure with reduced ejection fraction (NYHA Class III), Chronic heart failure with reduced ejection fraction (NYHA Class IV)

How Carvedilol works

Carvedilol inhibits exercise induce tachycardia through its inhibition of beta adrenoceptors. Carvedilol's action on alpha-1 adrenergic receptors relaxes smooth muscle in vasculature, leading to reduced peripheral vascular resistance and an overall reduction in blood pressure. At higher doses, calcium channel blocking and antioxidant activity can also be seen. The antioxidant activity of carvedilol prevents oxidation of low density lipoprotein and its uptake into coronary circulation.

Dosage

Carvedilol dosage

In heart failure, initially 3.125 mg twice daily (with food) may be given, dose may be increased at intervals of at least 2 weeks to 6.25 mg twice daily, then to 12.5 mg twice daily, then to 25 mg twice daily. The dose may be increased to highest dose tolerated, maximum 25 mg twice daily in patients less than 85 kg body-weight and 50 mg twice daily in patients over 85 kg.In hypertension initially 12.5 mg once daily, increased after 2 days to usual dose of 25 mg once daily; if necessary the dose may be further increased at intervals of at least 2 weeks to maximum 50 mg daily in single or divided doses.In elderly patients the initial dose of 12.5 mg daily may provide satisfactory control.In angina pectoris the recommended dose for initiation of therapy is 12.5 mg twice daily for the first 2 days. Thereafter, the recommended dosage is 25 mg twice daily. For elderly patients, the maximum daily dose is 50 mg daily in divided doses.

Side Effects

Postural hypotension, dizziness, headache, fatigue, gastro-intestinal disturbances, bradycardia; occasionally diminished peripheral circulation, peripheral oedema and painful extremities, dry mouth, dry eyes, eye irritation or disturbed vision, impotence, disturbances of micturition, influenza-like symptoms, rarely angina, AV block, exacerbation of intermittent claudication or Raynaud's phenomenon, allergic skin reactions, exacerbation of psoriasis, nasal stuffiness, wheezing, depressed mood, sleep disturbances, paresthesia, heart failure, changes in liver enzymes, thrombocytopenia, leukopenia are also reported.

Toxicity

Patients experiencing an overdose may present with hypotension, bradycardia, cardiac insufficiency, cardiogenic shock, and cardiac arrest. Patients should remain in a supine position and may be given atropine for bradycardia and glucagon followed by sympathomimetics to support cardiovascular function.

Precaution

Take caution in hepatic impairment and in heart failure monitor clinical status for 2-3 hours after initiation and after increasing each dose. Before increasing dose ensure that the renal function and heart failure are not deteriorating.

Interaction

Drug interactions have been seen with co-administration of carvedilol and digoxin, resulting in an increased bioavailability of digoxin. This increase is not clinically significant and does not correlate with pharmacologic response. Pharmacokinetics studies demonstrated a lack of drug interaction between carvedilol and hydrochlorothiazide, cimetidine, torsemide and warfarin

Food Interaction

  • Take with food. Food slows the absorption and reduces the incidence of adverse effects.

Carvedilol Alcohol interaction

[Moderate]

Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.

Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.

Caution and close monitoring for development of hypotension is advised during coadministration of these agents.

Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.

Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.

Carvedilol Cholesterol interaction

[Moderate] Beta-adrenergic receptor blocking agents (aka beta-blockers) may alter serum lipid profiles.

Increases in serum VLDL and LDL cholesterol and triglycerides, as well as decreases in HDL cholesterol, have been reported with some beta-blockers.

Patients with preexisting hyperlipidemia may require closer monitoring during beta-blocker therapy, and adjustments made accordingly in their lipid-lowering regimen.

Carvedilol multivitamins interaction

[Moderate] ADJUST DOSING INTERVAL: Concurrent administration with calcium salts may decrease the oral bioavailability of atenolol and possibly other beta-blockers.

The exact mechanism of interaction is unknown.

In six healthy subjects, calcium 500 mg (as lactate, carbonate, and gluconate) reduced the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of atenolol (100 mg) by 51% and 32%, respectively.

The elimination half-life increased by 44%.

Twelve hours after the combination, beta-blocking activity (as indicated by inhibition of exercise tachycardia) was reduced compared to that with atenolol alone.

However, during a 4-week treatment in six hypertensive patients, there was no difference in blood pressure values between treatments.

The investigators suggest that prolongation of the elimination half-life induced by calcium coadministration may have led to atenolol cumulation during long-term dosing, which compensated for the reduced bioavailability.

It may help to separate the administration times of beta-blockers and calcium products by at least 2 hours.

Patients should be monitored for potentially diminished beta-blocking effects following the addition of calcium therapy.

Volume of Distribution

Carvedilol has a volume of distribution of 1.5-2L/kg or 115L.

Elimination Route

Carvedilol has a bioavailability of 25-35%. Carvedilol has a Tmax of 1 to 2 hours. Taking carvedilol with a meal increases Tmax without increasing AUC. Carvedilol doses of 50mg lead to a Cmax of 122-262µg/L and an AUC of 717-1600µg/L*h. Carvedilol doses of 25mg lead to a Cmax of 24-151µg/L and an AUC of 272-947µg/L*h. Carvedilol doses of 12.5mg lead to a Cmax of 58-69µg/L and an AUC of 208-225µg/L*h.

Half Life

The half life of carvedilol is between 7-10 hours, though significantly shorter half lives have also been reported.

Clearance

The plasma clearance of carvedilol has been reported as 0.52L/kg or 500-700mL/min.

Elimination Route

16% of carvedilol is excreted in the urine with 4 Carvedilol is primarily excreted in the bile and feces.

Pregnancy & Breastfeeding use

Carvedilol should not be used during breast-feeding, since no studies have been performed in lactating women and animal studies have shown that carvedilol is excreted in breast milk. Safety and efficacy in children have not been established with carvedilol. Carvedilol should not be used during pregnancy as no studies have been performed in this group. Animal studies have shown that carvedilol crosses the placental barrier. No information is available on safety and efficacy of Carvedilol use in neonates.

Contraindication

Carvedilol is contraindicated in patients with severe chronic cardiac failure requiring intravenous inotropic therapy, bronchial asthma or related bronchospastic conditions, second or third-degree AV block, sick sinus syndrome (unless a permanent pacemaker is in place), cardiogenic shock, or severe bradycardia. Use of carvedilol in patients with clinically manifested hepatic impairment is not recommended. Carvedilol is contraindicated in patients with hypersensitivity to the drug.

Special Warning

The safety and efficacy of carvedilol in paediatric patients have not been established.

Acute Overdose

Symptoms: Severe hypotension, bradycardia, heart failure, cardiogenic shock and cardiac arrest. Resp problems, bronchospasms, vomiting, lapses of consciousness and generalised seizures. 

Management: Symptomatic and supportive treatment. Consider use of atropine for excessive bradycardia, IV glucagon or sympathomimetics to support ventricular function. Consider using norfenephrine or noradrenaline if vasodilation dominates the intoxication profile and IV inj of diazepam or clonazepam for seizures.

Interaction with other Medicine

Digoxin : In normal healthy volunteers a single dose of carvedilol taken together with a single dose of digoxin resulted in significantly increased levels of digoxin 24 hour later. Patients with congestive heart failure stabilized on digoxin have been given carvedilol concomitantly without any adverse effects. Increased monitoring of digoxin is recommended when initiating, adjusting, or discontinuing the dose of carvedilol.

Rifampin : Pretreatment with rifampin resulted in a 60% decrease in Cmax and AUC.

Warfarin : Carvedilol did not alter the in vitro plasma protein binding of warfarin.

Clonidine : b-receptor antagonists potentiate the pressor reaction which may follow sudden withdrawal of treatment with clonidine although, in theory, the a-blocking action of carvedilol should modify the pressure rise.

Storage Condition

Store in a cool and dry place. Protect from light and moisture.

Innovators Monograph

You find simplified version here Carvedilol

Carvedilol contains Carvedilol see full prescribing information from innovator Carvedilol Monograph, Carvedilol MSDS, Carvedilol FDA label

FAQ

What is Carvedilol used for?

Carvedilol is a medication used to treat high blood pressure, congestive heart failure, and left ventricular dysfunction in people who are otherwise stable. For high blood pressure, it is generally a second-line treatment.

How safe is Carvedilol?

For people with low blood pressure, Carvedilol can cause dangerously low blood pressure that may cause you to lose consciousness. For people with chronic bronchitis or emphysema, You shouldn't take Carvedilol or other beta-blockers. This drug can affect not only your heart but also your lungs.

How does Carvedilol work?

Carvedilol works by slowing down your heart rate and making it easier for your heart to pump blood around your body.

What are the common side effects of Carvedilol?

Common side effects of Carvedilol are include :

  • Dizziness
  • Fatigue
  • Low blood pressure (hypotension)
  • Weight gain
  • High blood sugar (hyperglycemia)
  • Diarrhea
  • Slow heart rate
  • Nausea
  • Cough
  • Headache
  • Atrioventricular block, edema
  • Chest pain (angina)
  • Hypercholesterolemia
  • Hypertriglyceridemia
  • Vomiting
  • Indigestion
  • Lightheadedness/fainting
  • Runny nose

Is Carvedilol safe during pregnancy?

This Carvedilol should be used during pregnancy only if the benefit outweighs the risk. There are no concerns that beta blockers cause birth defects, stillbirth or preterm birth.

Is Carvedilol safe during breastfeeding?

There is no published experience with Carvedilol during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant. This Carvedilol should not be used during breastfeeding unless the benefit outweighs the risk. The effects in the nursing infant are unknown; however, the possibility of the consequences of alpha and beta blockade should be considered.

Can I drink alcohol with Carvedilol?

Alcohol is generally toxic to the heart. The combined effect of alcohol and Carvedilol may cause excessive dizziness or fainting.

Can I drive after taking Carvedilol ?

Do not drive, use machinery, or do anything that needs alertness until you can do it safely.

When should be taken of Carvedilol?

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(s) every day.

How often can I take Carvedilol?

Adults, at first, 6.25 milligrams (mg) two times a day. Some patients may start at 3.125 mg two times a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 25 mg two times a day.

How should I take Carvedilol?

Swallow the tablets whole with a drink of water. Do not chew or crush them. However, if you are taking Carvedilol for heart failure, it's best to take the tablets with food.

How long does Carvedilol take to work?

Carvedilol usually starts to work after about 1 hour.

How long does Carvedilol take to work?

It usually takes between 4 and 5 half-lives for your system to clear a drug. So it may take between 28 hours and 50 hours for Carvedilol to be completely removed from your system after a dose is taken.

Can I take Carvedilol for a long time?

If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure.

Who should not take Carvedilol?

You should not take Carvedilol 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 (unless you have a pacemaker).

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention. Overdose symptoms may include uneven heartbeats, shortness of breath, bluish-colored fingernails, dizziness, weakness, fainting, and seizure (convulsions).

What happen If I suddenly stop taking Carvedilol?

If you suddenly stop taking Carvedilol, you may experience serious heart problems such as severe chest pain, a heart attack, or an irregular heartbeat. Your doctor will probably want to decrease your dose gradually over 1 to 2 weeks.

Can Carvedilol affect fertility?

Carvedilol are generally considered safe for use during pregnancy in helping to reduce high blood pressure and aren't thought to affect your ability to get pregnant.

Does Carvedilol cause heart problems?

If you suddenly stop taking Carvedilol, you may experience serious heart problems such as severe chest pain, a heart attack, or an irregular heartbeat.

Can Carvedilol affects my liver?

Carvedilol may cause pruritus and elevated liver function test results.

Can Carvedilol raise blood pressure?

Carvedilol can cause dangerously low blood pressure, which may cause you to lose consciousness. This risk is highest after your first doses and during dosing increases.

*** Taking medicines without doctor's advice can cause long-term problems.
Share