Carvedilol is a non-selective beta blocker without a sympathomimetic activity. It is one of the three beta-blockers that have been proven to reduce cardiovascular mortality in patients with heart failure.
Bisoprolol, carvedilol, or extended-release metoprolol succinate are the only beta-blockers that have been shown to lower mortality.
It is recommended for the treatment of the following conditions:
- Ischemia or cardiomyopathic-related mild to severe chronic heart failure with a lowered ejection fraction.
- Treatment of Hypertension (although not a first-line of therapy)
- Left ventricular dysfunction after myocardial infarction in patients who are clinically stable
Off Label Uses of Carvedilol in Adults include:
- Acute myocardial infarction
- Atrial fibrillation
- Chronic stable angina
- For the prophylaxis of Gastroesophageal variceal hemorrhage in patients with cirrhosis
- Ventricular arrhythmias
Carvedilol Dose in Adults
If the heart rate falls to less than 55 beats per minute, reduce the dosage.
Use as an alternative agent in the treatment of Hypertension:
- Immediate-release tablets:
- 6.25 mg twice day. Adjust the dosage as necessary every one to two weeks, up to a maximum of 25 mg twice daily.
- Extended-release tablets:
- Once a day, 20 mg. Depending on how the patient responds to an 80 mg once daily maximum dose, the dose should be adjusted at intervals of one or two weeks.
- Once a day, 20 mg. Depending on how the patient responds to an 80 mg once daily maximum dose, the dose should be adjusted at intervals of one or two weeks.
Use in the treatment of Heart failure with reduced ejection fraction:
It should be used with caution in patients with NYHA class IV heart failure. Before initiating therapy, patients should be off inotropic support, intravenous diuretics and vasodilators.
- Immediate- release formulations:
- 3.125 mg, taken twice day for two weeks. If the patient is tolerating the dose after two weeks, raise it to 6.25 mg twice daily.
- Up until the maximum acceptable dose, the dose may be further raised every two weeks.
- The Maximum recommended dose is:
- Patients under 85 kg should take 25 mg twice day.
- Patients who weigh more over 85 kg should take 50 mg twice daily.
- Extended-release formulation:
- Once daily for two weeks at 10 mg. To reach the highest tolerable dose, titrate the dose higher by 20 mg, 40 mg, and 80 mg every two weeks.
- The daily dose cap is set at 80 mg.
Use in treatment of Left ventricular dysfunction after a Myocardial infarction:
It should be initiated in patients who are hemodynamically stable
- Immediate- release:
- 2.125 mg to 6.25 mg twice daily. Depending on the patient's tolerance, gradually increase the dose to 12.5 mg twice a day at intervals of 3–10 days, with a target dose of 25 mg twice a day.
- The AHA advises a maximum dose of 50 milligrammes administered twice daily.
- Extended-release:
- 10–20 mg, used once daily. Depending on tolerance, increase the dose gradually every 3 to 10 days until you reach the goal dose of 80 mg once per day.
- 10–20 mg, used once daily. Depending on tolerance, increase the dose gradually every 3 to 10 days until you reach the goal dose of 80 mg once per day.
Off-label use in the treatment of Angina pectoris:
- Immediate-release:
- Two doses of 25 to 50 mg per day
- Two doses of 25 to 50 mg per day
Off-label use in the treatment of rate control Atrial fibrillation:
- Usual maintenance dose:
- 2.25 to 3.125 mg twice daily. Patients with heart failure may have their medication increased to a target dose of 25 mg twice day at intervals of two weeks (or 50 mg twice daily in patients weighing more than 85 kg).
- 2.25 to 3.125 mg twice daily. Patients with heart failure may have their medication increased to a target dose of 25 mg twice day at intervals of two weeks (or 50 mg twice daily in patients weighing more than 85 kg).
Off-label use as an alternative agent in the prophylactic treatment of Gastroesophageal variceal hemorrhage in patients with cirrhosis :
-
- If you want to have a resting heart rate of 55 to 60 bpm, use 3.125 mg twice daily or 6.25 mg once daily (if heart rate used for titration).
- After three to seven days, the dose may be increased to a maximum of 6.25 mg twice daily or 12.5 mg once daily.
- Patients with recurrent variceal hemorrhage and those with refractory ascites should not exceed doses greater than 12.5 mg/day.
Off label use in the treatment of Ventricular arrhythmias:
- Immediate release:
- 3.125 to 25 mg two times a day
- 3.125 to 25 mg two times a day
- Conversion from immediate-release to extended-release (Coreg CR) tablets:
- 3.125 mg immediate-release tablets two times a day: Convert to 10 mg extended-release capsules once a day
- 6.25 mg immediate-release tablets two times a day: Convert to 20 mg extended-release capsules once a day.
- 12.5 mg immediate-release tablets two times a day: Convert to 40 mg extended-release capsules once a day.
- 25 mg immediate-release tablets two times a day: Convert to 80 mg extended-release capsules once a day.
Carvedilol Dose in children:
Note: On a mg:mg basis, immediate-release and extended-release medicines are not interchangeable.
Use in the treatment of Heart failure:
- Infants, Children, and Adolescents less than 17 years of age:
- Immediate-release tablets:
- 0.075-0.08 mg/kg/dose twice a day. Titrate the dose at two weeks intervals by 50% to the usual target dose of 0.3-0.75 mg/kg/dose twice a day
- The maximum daily dose is 50 mg/day.
- Immediate-release tablets:
- Adolescents 18 years of age or older:
- Immediate-release tablets:
- 3.125 mg twice a day for 2 weeks. Titrate the dose at 2 weeks intervals to the highest recommended dose
- The Maximum recommended dose:
- Mild to moderate heart failure:
- Less than 85 kg: 25 mg twice a day
- More than 85 kg: 50 mg twice a day
- Severe heart failure:
- 25 mg twice a day
- Mild to moderate heart failure:
- Extended-release capsules:
- 10 mg once a day for 2 weeks. Double the dose at two weeks intervals (eg, 20 mg, 40 mg) to a maximum dose of 80 mg once a day.
- 10 mg once a day for 2 weeks. Double the dose at two weeks intervals (eg, 20 mg, 40 mg) to a maximum dose of 80 mg once a day.
- Immediate-release tablets:
Carvedilol dose in Hypertension:
- Adolescents 18 years of age or older:
- Immediate-release tablets:
- 6.25 mg twice a day to a maximum daily dose of 50 mg/day. (Titrate the dose at two weeks intervals by 50%)
- Extended-release capsules:
- 20 mg once a day to a maximum daily dose of 80 mg/day. Titrate the dose to 40 mg once a day at 2 weeks intervals.
- 20 mg once a day to a maximum daily dose of 80 mg/day. Titrate the dose to 40 mg once a day at 2 weeks intervals.
- Immediate-release tablets:
Use in treatment of Left ventricular dysfunction following Myocardial Infarction:
- Adolescents older than18 years:
Note: Therapy shouldn't start until the patient's hemodynamics are stable and fluid retention has been kept to a minimum.
-
- Immediate-release tablets:
- 3.125–6.25 mg twice per day, with a target dose of 25 mg twice per day. If tolerated, the dose should be increased every 3–10 days.
- Extended-release capsules:
- Once daily, 10–20 mg. To reach the goal dose of 80 mg once per day, increase the dose gradually at 3- to 10-day intervals..
- Once daily, 10–20 mg. To reach the goal dose of 80 mg once per day, increase the dose gradually at 3- to 10-day intervals..
- Immediate-release tablets:
Conversion from immediate-release to extended-release (Coreg CR) tablets:
- Adolescents older than18 years:
- Tablets for immediate release 3.125 mg twice daily should be changed to 10 mg once daily for extended-release capsules.
- 2.25 mg of immediate-release pills per day: Use extended-release capsules instead once daily 20 mg
- 12.5 mg pills for immediate release, taken twice daily: Change to 40 mg once-daily extended-release capsules.
- Taking two 25 mg immediate-release pills each day: Use extended-release capsules instead
Pregnancy Risk Factor C
- It is preferable to utilise medications that are not beta-blockers even though beta-blockers can be used during pregnancy to treat hypertension or heart failure.
- There have been adverse effects observed in animal studies. These include hypoglycemia and fetal/neonatal bradycardia.
Carvedilol use during breastfeeding:
- It is unknown whether carvedilol can be found in breastmilk. The benefits of breastfeeding should be balanced against the risk of adverse neonatal outcomes such as bradycardia.
- Patients with heart disease should not breastfeed because of the demands.
Carvedilol Dose in Renal:
Dose adjustment has not been recommended by the manufacturer. It is not cleared via hemodialysis.
Carvedilol Dose in liver disease:
In patients with advanced decompensated liver disease, carvingilol is not advised. However, patients with mild to moderate hepatic impairment and portal hypertension routinely utilise it.
Common Side Effects Of Carvedilol Include:
- Cardiovascular:
- Hypotension
- Orthostatic hypotension
- Central nervous system:
- Dizziness
- Fatigue
- Endocrine & metabolic:
- Weight gain
- Hyperglycemia
- Gastrointestinal:
- Diarrhea
- Neuromuscular & skeletal:
- Asthenia
Less Common Side Effects Of Carvedilol Include:
- Cardiovascular:
- Bradycardia
- Syncope
- Peripheral edema
- Angina pectoris
- Edema
- Atrioventricular block
- Cerebrovascular accident
- Exacerbation of angina pectoris
- Hypertension
- Lower extremity edema
- Palpitations
- Peripheral vascular disease
- Peripheral ischemia
- Tachycardia
- Central nervous system:
- Headache
- Depression
- Drowsiness
- Hypoesthesia
- Hypotonia
- Malaise
- Vertigo
- Paresthesia
- Insomnia
- Abnormality in thinking
- Emotional lability
- Exacerbation of depression
- Lack of concentration
- Nervousness
- Nightmares
- Sleep disorder
- Dermatologic:
- Diaphoresis
- Erythematous rash
- Maculopapular rash
- Pruritus
- Psoriasiform eruption
- Skin photosensitivity
- Endocrine & metabolic:
- Increased nonprotein nitrogen
- Dependent edema
- Hypercholesterolemia
- Albuminuria
- Diabetes mellitus
- Glycosuria
- Gout
- Hyperkalemia
- Hyperuricemia
- Hypervolemia
- Hypoglycemia
- Hyponatremia
- Hypovolemia
- Impotence
- Increased gamma-glutamyltransferase
- Weight loss
- Decreased libido
- Hypertriglyceridemia
- Hypokalemia
- Gastrointestinal:
- Nausea
- Vomiting
- Melena
- Periodontitis
- Gastrointestinal pain
- Xerostomia
- Genitourinary:
- Hematuria
- Urinary frequency
- Hematologic & oncologic:
- Hypoprothrombinemia
- Nonthrombocytopenic purpura
- Thrombocytopenia
- Leukopenia
- Hepatic:
- Increased serum alanine aminotransferase
- Increased serum alkaline phosphatase
- Increased serum aspartate aminotransferase
- Hyperbilirubinemia
- Increased liver enzyme
- Hypersensitivity:
- Hypersensitivity reaction
- Neuromuscular & skeletal:
- Arthralgia
- Arthritis
- Muscle cramps
- Hypokinesia
- Ophthalmic:
- Visual disturbance
- Blurred vision
- Otic:
- Tinnitus
- Renal:
- Increased blood urea nitrogen
- Increased serum creatinine
- Renal insufficiency
- Respiratory:
- Increased cough
- Nasopharyngitis
- Rales
- Dyspnea
- Flu-like symptoms
- Nasal congestion
- Paranasal sinus congestion
- Asthma
- Miscellaneous:
- Fever
Contraindication to Carvedilol include:
- Severe allergic reactions to carvedilol and any component of the formulations
- Inotropic support and intravenous vasopressors are required for decompensated cardiac failure
- Allergy bronchial asthma
- Second- or third-degree block of AV,
- Sinusitis, and
- Bradycardia severe
- Cardiogenic shock
- Advanced liver impairment
- Hypotension severe
- Primary obstructive valve heart disease
- Patients suffering from severe Alzheimer disease, addiction, or drug abuse should be closely monitored.
Warnings and Precautions
- Anaphylactic reactions
- It should not be used by those who have a known allergy to beta-blockers.
- Patients who experience a drug hypersensitivity reaction should be advised to stop using it and treated accordingly.
- Furthermore, people who have had an allergic reaction to a beta-blocker may not respond well to epinephrine.
- Bradycardia
- If the heart rate falls below 55 beats per hour, you should reduce the dose.
- Floppy iris syndrome:
- Patients who have had cataract surgery may be affected by intraoperative floppy-iris syndrome.
- Hypotension and syncope:
- Symptomatic hypotension can occur after carvedilol is administered for the first 30 days.
- To avoid side effects such as syncopal attacks or symptomatic hypotension, increase the dose slowly.
- Angina
- Prinzmetal variant of angina patients should be avoided.
- Asthma, and other bronchospastic conditions:
- Beta-blockers should not be prescribed to patients with asthma or any other disorder that affects the reactive airways.
- Diabetes:
- It can increase hypoglycemia, mask its clinical symptoms like anxiety, sweating, and tachycardia.
- Hypoglycemia can be a major problem for diabetic patients who have been on beta-blockers or carvedilol since their heart failure.
- Heart failure:
- Patients with heart disease who take beta-blockers are at greater risk of developing kidney dysfunction, especially if they have diffuse atherosclerotic diseases and a systolic pressure of less 100 mmHg.
- You should start it at a lower dose, and gradually increase the dosage over 2 to 3 weeks.
- Beta-blockers can temporarily be stopped if there is renal dysfunction
- Hepatic impairment
- It should not be used in cases of severe liver disease.
- Myasthenia gravis:
- Patients with myasthenia Gravis should use it with caution.
- Peripheral Vascular Disease (PVD).
- Patients with peripheral arterial disease should use caution.
- Pheochromocytoma:
- Patients with pheochromocytoma should be prescribed beta-blockers after using alpha-blockers.
- Psoriasis:
- It can worsen the symptoms of psoriasis.
- Thyroid disease:
- It can mask hyperthyroidism symptoms. Patients with hyperthyroidism may experience a thyroid storm or crisis if they stop taking beta-blockers abruptly.
Carvedilol: Drug Interaction
Note: Drug Interaction Categories:
- Risk Factor C: Monitor When Using Combination
- Risk Factor D: Consider Treatment Modification
- Risk Factor X: Avoid Concomitant Use
Risk Factor C (Monitor therapy). |
|
| Acetylcholinesterase inhibitors | Beta-Blockers may increase the bradycardic effects. |
| Ajmaline | High risk of Inhibitors increasing serum concentrations of CYP2D6 Substrates |
| Alfuzosin | Might increase the hypotensive effects of Blood Pressure Lowering Agents. |
| Alpha1-Blockers | Beta-Blockers can increase the orthostatic hypotensive effects of Alpha1Blockers. Ophthalmic products are less likely to be a risk than systemic ones. |
| Aminoquinolines (Antimalarial) | May reduce the metabolism of Beta-Blockers. |
| Amiodarone | Beta-Blockers may increase bradycardic effects. Possible to cause cardiac arrest. Amiodarone could increase serum Beta-Blockers. |
| Amphetamines | May decrease the antihypertensive effects of Antihypertensive Drugs. |
| Antipsychotic Agents (Phenothiazines) | Beta-Blockers may increase hypotensive effects. Beta-Blockers can decrease the metabolism Antipsychotic Agents (Phenothiazines). The metabolism of Beta-Blockers may be affected by Antipsychotic Agents (Phenothiazines). |
| Antipsychotic Agents, Second Generation (Atypical) | Blood Pressure Lowering Agents can increase the hypotensive effects of Antipsychotic Agents (Second Gen [Atypical]). |
| Barbiturates | May lower the serum level of Beta-Blockers. |
| Barbiturates | Might increase the hypotensive effects of Blood Pressure Lowering Agents. |
| Benperidol | Might increase the hypotensive effects of Blood Pressure Lowering Agents. |
| Bradycardia-Causing Agents | May increase the bradycardic effects of Bradycardia-Causing agents. |
| Brentuximab Vedotin | Brentuximab P-glycoprotein/ABCB1 inhibitors may lead to a rise in vedotin. The monomethyl auristatin E component (MMAE) concentrations could rise. |
| Bretylium | Bradycardia Causing Agents may have more bradycardic effects. Patients taking AV blockers might notice less AV blockage after taking Bretylium. |
| Brigatinib | May decrease the antihypertensive effects of Antihypertensive Drugs. Brigatinib could increase the bradycardic effects of Antihypertensive Drugs. |
| Brimonidine (Topical) | Might increase the hypotensive effects of Blood Pressure Lowering Agents. |
| Bupivacaine | Beta-Blockers can increase serum Bupivacaine concentrations. |
| Calcium Channel Blockers (Nondihydropyridine) | The hypotensive effects of betablockers can be amplified. Bradycardia and indications of heart illness have also been recorded. Nondihydropyridine, a calcium channel blocker, may raise the level of beta-blockers in the blood. Bepridil is an exception. |
| Cardiac Glycosides | Cardiac Glycosides' bradycardic effects can be exacerbated by beta-blockers. |
| Celiprolol | P-glycoprotein/ABCB1 inhibitors may enhance the serum levels of Celiprolol. |
| Cholinergic Agonists | Beta-Blockers might make Cholinergic Agonists more toxic or harmful. Possible bronchoconstriction or aberrant cardiac conduction are of particular concern. Administration: Use these medications with extreme caution and keep an eye out for conduction issues. Methacholine plus any beta-blocker should be avoided due to the potential for additive bronchoconstriction. |
| Cimetidine | May increase serum Carvedilol concentration. |
| CloBAZam | High risk of Inhibitors increasing serum concentrations of CYP2D6 Substrates |
| Cobicistat | High risk of Inhibitors increasing serum concentrations of CYP2D6 Substrates |
| Moderate CYP2C9 Inhibitors | Increased serum Carvedilol concentrations may occur. Particularly, the concentrations of S-carvedilol may increase. |
| Moderate CYP2D6 inhibitors | Might decrease metabolism of CYP2D6 substrates (High Risk with Inhibitors). |
| Darunavir | High risk of Inhibitors increasing serum concentrations of CYP2D6 Substrates |
| Dexmethylphenidate | Antihypertensive agents may have a less therapeutic effect. |
| Diazoxide | May intensify blood pressure lowering medications' hypotensive effects. |
| Digoxin | The bradycardic effects could be worsened by carvingilol. Carvedilol may raise the serum levels of digoxin. |
| Dipyridamole | Beta-Blockers may increase the bradycardic effects. |
| Disopyramide | Beta-Blockers may increase the bradycardic effects. Disopyramide may have a negative inotropic effect that Beta-Blockers can enhance. |
| DULoxetine | DULoxetine may increase hypotensive effects by lowering blood pressure. |
| EPINEPHrine (Nasal) | The therapeutic effects of epinephrine can be lessened by beta-blockers (with alpha blocking properties). |
| EPINEPHrine (Oral Inhalation) | It is possible that beta-blockers with alpha-blocking properties will lessen the therapeutic benefits of oral inhalation of epinephrine. |
| Epinephrine (Racemic) | Epinephrine's therapeutic effects can be diminished by beta-blockers (with alpha blocking properties). |
| EPINEPHrine Systemic | Beta-blockers (with Alpha Blocking Properties) can lessen EPINEPHRINE Systemic's therapeutic benefits. |
| Erdafitinib | It's conceivable to have higher serum levels of P-glycoprotein/ABCB1 Substrates. |
| Everolimus | P-glycoprotein/ABCB1 inhibitors may raise the levels of everolimus in the blood |
| Herbs (Hypertensive Properties) | May lessen the effects of antihypertensive medications in treating hypertension. |
| Herbs (Hypotensive properties) | May intensify blood pressure lowering medications' hypotensive effects. |
| Hypotension-Associated Agents | The hypotensive action of hypotension-associated agents may be strengthened by blood pressure lowering medications. |
| Imatinib | High likelihood that inhibitors will raise serum levels of CYP2D6 substrates |
| Insulins | Beta-Blockers can enhance insulin's hypoglycemic effects. |
| Ivabradine | Ivabradine's bradycardic effects may be exacerbated by substances that cause bradycardia. |
| Lacosamide | Lacosamide's AV-blocking effects can be exacerbated by substances that cause bradycardia. |
| Larotrectinib | P-glycoprotein/ABCB1 inhibitors may raise the serum levels of Larotrectinib. |
| Levodopa-Containing Products | Levodopa-Containing Products' hypotensive effects may be amplified by blood pressure-lowering medications. |
| Lidocaine (Systemic) | Beta-Blockers can raise the level of lidocaine in the serum (Systemic). |
| Lidocaine (Topical) | The serum concentrations of lidocaine (Topical) can rise when taking beta-blockers. |
| Lormetazepam | May intensify blood pressure lowering medications' hypotensive effects. |
| Lumacaftor | May reduce the levels of P-glycoprotein/ABCB1 Substrates in the serum. P-glycoprotein/ABCB1 Substrates serum levels may rise in response to lumacaftor. |
| Lumefantrine | Mepivacaine serum levels may rise in response to beta-blockers. |
| Mepivacaine | P-glycoprotein/ABCB1 inhibitors may raise the serum concentrations of naldemedine. |
| Methoxyflurane | May increase the hypotensive effects of Beta-Blockers. |
| Methylphenidate | May decrease the antihypertensive effects of Antihypertensive Drugs. |
| Midodrine | May increase the bradycardic effects of Bradycardia Causing Agents. |
| Molsidomine | Might increase the hypotensive effects of Blood Pressure Lowering Agents. |
| Naftopidil | Might increase the hypotensive effects of Blood Pressure Lowering Agents. |
| Naloxegol | Naloxegol serum concentrations may rise in response to P-glycoprotein/ABCB1 inhibitors. |
| NiCARdipine | The consequences of hypotension may be amplified with carvingol. Patients using Carvedilol may experience heart failure after taking NiCARdipine. NiCARdipine may elevate serum Carvedilol levels. |
| Nicergoline | May intensify blood pressure lowering medications' hypotensive effects. |
| Nicorandil | May intensify blood pressure lowering medications' hypotensive effects. |
| NIFEdipine | May intensify beta-blockers' hypotensive effects. The unfavourable inotropic effects of beta-blockers could be exacerbated by NIFEdipine. |
| Nitroprusside | Blood pressure lowering medications may intensify Nitroprusside's hypotensive effects. |
| Nonsteroidal Anti-Inflammatory Drugs | BetaBlockers may have a lower antihypertensive impact. |
| Opioids (Anilidopiperidine) | Beta-Blockers may increase the bradycardic effects. Anilidopiperidine and other opioids may increase the hypotensive effects of Beta-Blockers. |
| Panobinostat | High likelihood that inhibitors will raise serum levels of CYP2D6 substrates |
| Peginterferon Alfa-2b | Inhibitors carry a high danger. may reduce the level of CYP2D6 substrates in serum. Serum levels of CYP2D6 Substrates may rise after administration of peginterferon Alf-2b. |
| Pentoxifylline | May intensify blood pressure lowering medications' hypotensive effects. |
| Perhexiline | CYP2D6 Substrates may lead to an increase in perhexiline. The serum concentrations of CYP2D6 substrates can rise in response to perhexiline (High Risk with Inhibitors). |
| P-glycoprotein/ABCB1 Inducers | Pglycoprotein/ABCB1 Substrates' serum concentrations could drop. P-glycoprotein inducers may restrict distribution to specific cells, tissues, and organs where p-glycoprotein is present in high concentrations (such as the brain, T-lymphocytes, and testes). |
| P-glycoprotein/ABCB1 Inhibitors | Increases the level of ABCB1 substrates in the serum. Additionally, p-glycoprotein inhibitors can improve the distribution of pglycoprotein substrates to specific cells, tissues, and organs where large levels of p-glycoprotein are present (e.g. brain, T-lymphocytes and testes). |
| P-glycoprotein/ABCB1 Substrates | Inhibitors of P-glycoprotein/ABCB1 may lead to higher serum concentrations of P-glycoprotein/ABCB1 Substrates. Additionally, p-glycoprotein inhibitors can expand the distribution of pglycoprotein substrates in particular cells, tissues, and organs that have high quantities of p-glycoprotein (e.g. brain, T-lymphocytes and testes). Exceptions: Loperamide. |
| Pholcodine | By reducing blood pressure, pholocdine may exacerbate hypotension. |
| Phosphodiesterase 5 Inhibitors | Might increase the hypotensive effects of Blood Pressure Lowering Agents. |
| Propafenone | May increase serum Beta-Blockers. Propafenone has some beta-blocking activity on its own. |
| Prostacyclin Analogues | Might increase the hypotensive effects of Blood Pressure Lowering Agents. |
| Prucalopride | The serum concentrations of Prucalopride may be increased by P-glycoprotein/ABCB1 inhibitors. |
| Quinagolide | Might increase the hypotensive effects of Blood Pressure Lowering Agents. |
| QuiNINE | High risk of Inhibitors increasing serum concentrations of CYP2D6 Substrates |
| Ranolazine | Inhibitors of P-glycoprotein/ABCB1 may augment the effects of ranolazine. |
| Ranolazine | It's conceivable to have higher serum levels of P-glycoprotein/ABCB1 Substrates. |
| Regorafenib | The consequences of bradycardia could be amplified by beta-blockers. |
| Reserpine | May intensify beta-blockers' hypotensive effects. |
| Rifamycin Derivatives | The serum level of beta-blockers might be decreased. The exception is rifabutin. |
| RifAXIMin | P-glycoprotein/ABCB1 inhibitors may raise the serum quantities of RifAXIMin. |
| Ruxolitinib | Bradycardia-Causing Agents' bradycardic effects might be amplified. Management: The Canadian product labels for roxolitinib advise against using any medication that can cause bradycardia. |
| Selective Serotonin Reuptake inhibitors | May raise serum levels of beta-blockers. Citalopram, Escitalopram, and FluvoxaMINE are exceptions. |
| Silodosin | P-glycoprotein/ABCB1 inhibitors may raise the serum level of Silodosin. |
| Sulfonylureas | Sulfonylureas' hypoglycemic effects can be enhanced by beta-blockers. Beta blockers that are not cardioselective may be more harmful than those that are. All beta-blockers appear to be able to conceal tachycardia as the early indication of hypoglycemia. In comparison to systemic medications, ophthalmic beta blockers are probably associated with a decreased risk. |
| Terlipressin | Bradycardia Causing Agents may have more bradycardic effects. |
| Tofacitinib | Bradycardia Causing Agents may have more bradycardic effects. |
| Yohimbine | May lessen the effects of antihypertensive medications in treating hypertension. |
Risk Factor D (Consider therapy modifications) |
|
| Abiraterone Acetate | High chance that inhibitors will raise serum levels of CYP2D6 substrates. Avoid using abiraterone and CYP2D6 Substrates with a restricted therapeutic index together whenever possible. If concurrent usage cannot be avoided, constantly watch patients for symptoms/signs and administer therapy as necessary. |
| Afatinib | P-glycoprotein/ABCB1 inhibitors may raise the serum concentrations of Afatinib. Reduce the dose by 10 mg if afatinib is not tolerated. According to Canadian labelling, it is advisable to stay away from any drug combinations. If you must use the P-gp inhibitor, take afatinib right after or concurrently. |
| Alpha2-Agonists | Beta-Blockers may have an AV-blocking effect that is greater. It is possible to increase the risk of sinus node dysfunction. Beta-Blockers can increase the rebound hypertensive effect Alpha2Agonists. This can happen if the Alpha2-Agonist abruptly withdraws. Treatment: Monitor your heart rate closely while you are taking clonidine and beta blockers. When possible, stop taking beta blockers a few days before you begin clonidine withdrawal. Also, monitor your blood pressure carefully. Other alpha2-agonists will not be recommended. Exceptions: Apraclonidine. |
| Amifostine | The hypotensive effects of amifostine may be strengthened by blood pressure reducing medications. Treatment: Stop taking blood pressure medications at least 24 hours before taking amifostine. In the absence of blood pressure reducing medicine, amifostine should be avoided. |
| Asunaprevir | High risk of Inhibitors increasing serum concentrations of CYP2D6 Substrates |
| Betrixaban | P-glycoprotein/ABCB1 inhibitors may raise the serum levels of betrixaban. Treatment: If betrixaban is administered in combination with a Pglycoprotein inhibitor, reduce the initial dose to 80 mg, then reduce it to 40 mg daily. |
| Bilastine | Inhibitors of P-glycoprotein/ABCB1 may cause an increase in blastine. Patients on p-glycoprotein inhibitors who have severe or moderate renal impairment should look into alternative treatments. |
| Ceritinib | Bradycardia-inducing substances may intensify the bradycardic effects of ceritinib. Management: If the combination is not possible, keep a close eye out for bradycardia symptoms in patients, and closely monitor blood pressure and heart rate throughout treatment. Various monographs will go through the exceptions. |
| Colchicine | P-glycoprotein/ABCB1 inhibitors may raise the serum Colchicine levels. Colchicine may be more widely distributed in some tissues, such the brain. Colchicine shouldn't be administered to people who simultaneously take a p-glycoprotein inhibitor and have compromised renal and hepatic function. Colchicine dosage should be decreased for people with healthy liver or kidney function. For information, see the entire monograph. |
| CycloSPORINE Systemic | Carvedilol may elevate CycloSPORINE levels in the blood. Systemic P-glycoprotein/ABCB1 inhibitors may raise DOXOrubicin serum levels (Conventional). Treatment: If you are receiving doxorubicin, you may want to think about using different P-glycoprotein inhibitors. One American company, Pfizer Inc., advises against using certain combos. |
| Strong CYP2D6 inhibitors | Might decrease metabolism of CYP2D6 substrates (High Risk with Inhibitors). |
| Dabigatran Etexilate | The serum concentrations may be increased by P-glycoprotein/ABCB1 inhibitors. Treatment: Dabigatran dosage reductions may be necessary. Particular recommendations can vary depending on the labeling of the US and Canada, specific Pgp inhibitors, renal function, indications for dabigatran therapy, and other factors. Refer to the full monograph and dabigatran labeling. |
| Dacomitinib | High risk of Inhibitors causing an increase in serum concentrations of CYP2D6 substrates. Management: Do not use dacomitinib concurrently with CYP2D6 Substrates that have a narrow therapeutic Index. |
| DOXOrubicin (Conventional) | Beta-blockers may intensify the consequences of bradycardia. Dronedarone may elevate serum levels of beta-blockers. This is most likely accurate only for substances that use CYP2D6 for metabolism. Treatment: It is advised to start taking beta-blockers at lower doses. The patient's ability to tolerate the combination should be confirmed by the results of the ECG. |
| Edoxaban | The serum concentrations of Edoxaban may be increased by P-glycoprotein/ABCB1 inhibitors. Management: See full monograph for details. Patients receiving edoxaban to treat venous embolism are advised to take lower doses when taking it with P-gp inhibitors. For patients with atrial fibrillation, edoxaban should not be adjusted in the same way. |
| Ergot Derivatives | The vasoconstrictive effects of ergot derivatives can be enhanced by beta-blockers. The exception is Nicergoline. |
| Fingolimod | Fingolimod may increase the bradycardic effects of beta-blockers. If possible, avoid the use of beta-blockers and fingolimod together. Patients who require coadministration should be monitored for ECG changes overnight. Patients should be monitored for bradycardia. |
| Grass Pollen Allergen Extract (5 Grass Extract) | Beta-Blockers could increase the toxic/adverse effect of Grass Pollen Extract (5 Grass) Beta-Blockers can also inhibit the effectiveness of epinephrine to treat severe allergic reactions to Grass Pollen Allergen Extract (5 Grass Extract). Other effects of epinephrine might not be affected or even increased by Beta-Blockers. |
| Obinutuzumab | This may increase the hypotensive effects of Blood Pressure Lowering Agents. Management: You may temporarily withhold blood pressure lowering medication beginning 12 hours before obinutuzumab injection and continuing for 1 hour after infusion. |
| Siponimod | Bradycardia-Causing Drugs can increase Siponimod's bradycardic effects. Management: Siponimod should not be taken with bradycardia-causing drugs. |
| Talazoparib | Carvedilol can increase serum Talazoparib concentrations. Management: Reduce the daily dose of talazoparib to 0.75 mg if concurrent use is impossible. Increase the talazoparib dosage to the same level as before you started carvedilol. |
| Theophylline Derivatives | Beta-Blockers (Nonselective), may decrease the bronchodilatory effects of Theophylline Derivates. |
| Venetoclax | Venetoclax may be increased by P-glycoprotein/ABCB1 inhibitors. Treatment: Patients who are concomitantly treated with P-glycoprotein inhibitors (P-gp), should consider a venetoclax dose decrease of at least 50%. |
Risk Factor X (Avoid Combination) |
|
| Beta2-Agonists | Beta-Blockers (Nonselective), may decrease the bronchodilatory effects of Beta2Agonists. |
| Bromperidol | Bromperidol's hypotensive effects may be enhanced by Blood Pressure Lowering agents. Bromperidol could decrease the hypotensive effects of Blood Pressure Lowering agents. |
| Floctafenine | Beta-Blockers may have an adverse/toxic effect that can be increased. |
| Methacholine | Beta-Blockers can increase the toxic/adverse effects of Methacholine. |
| PAZOPanib | ABCB1/P-glycoprotein inhibitors may raise PAZOPanib levels in the bloodstream. |
| Rivastigmine | Beta-Blockers may increase the bradycardic effects. |
| Topotecan | P-glycoprotein/ABCB1 inhibitors may raise topotecan serum concentrations |
| VinCRIStine (Liposomal) | P-glycoprotein/ABCB1 inhibitors have the potential to raise the serum concentration of VinCRIStine (Liposomal). |
Monitoring parameters:
Monitor the following parameters while on carvedilol treatment:
- Heart rate
- Blood pressure (Target blood pressure should be less than 130/80)
- Renal functions
- Liver functions
- Plasma glucose in diabetics.
How to take Carvedilol?
- To reduce the risk of syncope and orthostatic hypotension, it can be given with food.
- Crushing, chewing, or dividing extended-release capsules is not advised.
- For immediate usage, they can be opened and the contents sprinkled over applesauce.
Mechanism of action of Carvedilol:
- Carvedilol, a non-selective Beta & Alpha receptor blocking drug, is also known as Carvedilol.
- It is not sympathetically evoking. It lessens reflex orthostatic tachycardia, exercise-induced tachycardia, and tachycardia brought on by beta-agonists. Vasodilation and a reduction in peripheral blood vascular resistance are the results.
- In patients with congestive heart failure, it also reduces the pulmonary capillary pressure and pulmonary arterial pressure.
Carvedilol's antihypertensive effects can be seenWithin 30 minutes, the maximum is reached in one to two hoursBeta-blockade is given within one hour of being administered. It isRapidly absorbedIt is then subject to the first pass metabolism. The blood levels of patients with advanced liver disease or the elderly are 50% higher and 4-7 times higher, respectively. When taken with meals, absorption can be delayed.
It is easily available and 98% are in stock. protein-bound.It isMetabolizedIt is converted (98%) into three active metabolites by the liver. It is abioavailabilityThe range is between 25% and 35%. Patients with heart disease and patients who have consumed fatty meals increase bioavailability. The half-life elimination ranges from 2 to 5 hours. The Time to reach peak plasma concentration of the extended-release tablets is about 5 hours. It is excreted primarily via the feces.
International brands of Carvedilol:
- APO-Carvedilol
- Auro-Carvedilol
- DOM-Carvedilol
- JAMP-Carvedilol
- MYLAN-Carvedilol
- NOVO-Carvedilol
- NU-Carvedilol
- PMS-Carvedilol
- RAN-Carvedilol
- TEVA-Carvedilol
- Alvelol
- Arlec
- Artist
- Avernol
- Avidol
- Betacard
- Betaplex
- Bloquedil
- Blorec
- Cadil
- Caraca-12.5
- Caraten
- Carbloxal
- Carca-3
- Carca-6
- Cardilol
- Cardine
- Cardiol
- Cardipres
- Cardivas
- Cardoz
- Cargen
- Carloc
- Carlov
- Carsantin
- Carved
- Carvedexxon
- Carvedil
- Carvediteg
- Carvelmed
- Carvelol
- Carvena
- Carvepen
- Carveta
- Carvid
- Carvidex
- Carvidil
- Carviditeg
- Carvidol
- Carvil
- Carvilar
- Carvo
- Cavel
- Coreg
- Coronis
- Coropres
- Corubin
- Coryol
- Dicarz
- Dilabloc
- Dilapress
- Dilatrend
- Dilatrend SR
- Dilbloc
- Dilgard
- Dimitone
- Duobloc
- Epicarve
- Gladycor
- Glovedol
- Ictus
- Karter
- Karvedil
- Karvex
- Kredex
- Longcardio
- Normotride
- Querto
- Scodilol
- Syntrend
- Talliton
- Udilol
- V-Bloc
- Vasodilren
- Vedilol
- Volirop
- Xetin
- Ziclar
Cavedilol Brands in Pakistan:
|
Carvedilol [Tabs 12 mg] |
|
| ARVEDA | PHARMAFIVE (PVT) LTD |
|
Carvedilol [Tabs 25 mg] |
|
| CADILOL | ALLIANCE PHARMACEUTICALS (PVT) LTD. |
| CARLOV | HILTON PHARMA (PVT) LIMITED |
| CARPRO | NABIQASIM INDUSTRIES (PVT) LTD. |
| CARVEDA | FEROZSONS LABORATOIES LTD. |
| CARVILOL | STANDPHARM PAKISTAN (PVT) LTD. |
| CAVIDOL | INDUS PHARMA (PVT) LTD. |
| CEZAR | AMBROSIA PHARMACEUTICALS |
| CUORE | WEBROS PHARMACEUTICALS |
| CURALOV | Curatech Pharma (Pvt) Ltd |
| DELAWARE | EFROZE CHEMICAL INDUSTRIES (PVT) LTD. |
| DILATREND | ROCHE PAKISTAN LTD. |
| DIMITONE | ROCHE PAKISTAN LTD. |
| HART | MACTER INTERNATIONAL (PVT) LTD. |
| HIDILOL | HELIX PHARMA (PRIVATE) LIMITED |
| NORMIDILOL | NABIQASIM INDUSTRIES (PVT) LTD. |
| TACAR | BRYON PHARMACEUTICALS (PVT) LTD. |
| VADIL | TABROS PHARMA |
| VASOCARE | HEAL PHARMACEUTICALS PVT LTD |
| VEDICAR | BARRETT HODGSON PAKISTAN (PVT) LTD. |
|
Carvedilol [Tabs 12.5 mg] |
|
| ARVEDA | PHARMAFIVE (PVT) LTD |
| CARLOV | HILTON PHARMA (PVT) LIMITED |
| CARPRO | NABIQASIM INDUSTRIES (PVT) LTD. |
| CARVEDA | FEROZSONS LABORATOIES LTD. |
| CARVOLOC | CARAWAY PHARMACEUTICALS |
| CAVIDOL | INDUS PHARMA (PVT) LTD. |
| CAVIDOL | INDUS PHARMA (PVT) LTD. |
| CUORE | WEBROS PHARMACEUTICALS |
| CUORE | WEBROS PHARMACEUTICALS |
| CUORE | WEBROS PHARMACEUTICALS |
| DELAWARE | EFROZE CHEMICAL INDUSTRIES (PVT) LTD. |
| DELAWARE | EFROZE CHEMICAL INDUSTRIES (PVT) LTD. |
| DILATREND | ROCHE PAKISTAN LTD. |
| DIMITONE | ROCHE PAKISTAN LTD. |
| HART | MACTER INTERNATIONAL (PVT) LTD. |
| HIDILOL | HELIX PHARMA (PRIVATE) LIMITED |
| NORMIDILOL | NABIQASIM INDUSTRIES (PVT) LTD. |
| OTELLO | WILSHIRE LABORATORIES (PVT) LTD. |
| TACAR | BRYON PHARMACEUTICALS (PVT) LTD. |
| VADIL | TABROS PHARMA |
| VEDICAR | BARRETT HODGSON PAKISTAN (PVT) LTD. |
| VEDICAR | BARRETT HODGSON PAKISTAN (PVT) LTD. |
|
Carvedilol [Tabs 6.25 mg] |
|
| ARVEDA | PHARMAFIVE (PVT) LTD |
| CADILOL | ALLIANCE PHARMACEUTICALS (PVT) LTD. |
| CARLOV | HILTON PHARMA (PVT) LIMITED |
| CARPRO | NABIQASIM INDUSTRIES (PVT) LTD. |
| CARVEDA | FEROZSONS LABORATOIES LTD. |
| CARVEL | CANDID PHARMACEUTICALS |
| CARVOLOC | CARAWAY PHARMACEUTICALS |
| CUORE | WEBROS PHARMACEUTICALS |
| CURALOV | Curatech Pharma (Pvt) Ltd |
| DELAWARE | EFROZE CHEMICAL INDUSTRIES (PVT) LTD. |
| DILATREND | ROCHE PAKISTAN LTD. |
| DIMITONE | ROCHE PAKISTAN LTD. |
| HART | MACTER INTERNATIONAL (PVT) LTD. |
| HIDILOL | HELIX PHARMA (PRIVATE) LIMITED |
| NORMIDILOL | NABIQASIM INDUSTRIES (PVT) LTD. |
| TACAR | BRYON PHARMACEUTICALS (PVT) LTD. |
| VADIL | TABROS PHARMA |
| VASOCARE | HEAL PHARMACEUTICALS PVT LTD |
| VEDICAR | BARRETT HODGSON PAKISTAN (PVT) LTD. |
|
Carvedilol [Tabs 62.5 mg] |
|
| CARVILOL | STANDPHARM PAKISTAN (PVT) LTD. |
|
Carvedilol [Tabs 3.125 mg] |
|
| DELAWARE | EFROZE CHEMICAL INDUSTRIES (PVT) LTD. |
| VADIL | TABROS PHARMA |
| XICARD | GETZ PHARMA PAKISTAN (PVT) LTD. |
