Coreg 25 mg Tablets

Brand Name

This medication is sold under the trade name Coreg, a label well-regarded in medical practice for its cardiovascular applications.

International Nonproprietary Name (INN)

The active ingredient is known worldwide as carvedilol, providing a universal identifier across healthcare settings.

Form of Release

The drug is available as tablets, formulated for oral use with various strengths to meet individual patient requirements. This tablet design ensures convenience and stability under typical storage conditions.

Composition

Carvedilol is the primary active substance, developed to target specific bodily functions. Supporting ingredients include lactose monohydrate, colloidal silicon dioxide, crospovidone, and magnesium stearate, which maintain tablet structure and aid disintegration. Some versions feature a film coating of hypromellose and polyethylene glycol, improving durability and ease of swallowing. These components are selected to enhance therapeutic effects without altering potency.

Pharmacologic Properties

Pharmacodynamics

This medication acts as a non-selective beta-blocker with alpha-1 antagonism, offering a comprehensive approach to cardiovascular control. It blocks beta-1 and beta-2 receptors, slowing heart rate and reducing myocardial effort, thus lowering oxygen demand. Alpha-1 blockade relaxes blood vessels, decreasing resistance and blood pressure. This combined action suits conditions needing heart and vascular adjustments. Effects begin within an hour, with full benefits emerging over days to weeks. Carvedilol’s antioxidant traits may also reduce oxidative damage in heart tissues.

Pharmacokinetics

After oral administration, the drug absorbs well from the digestive tract, with food boosting bioavailability by limiting initial liver breakdown. Carvedilol peaks in plasma within one to two hours. It undergoes significant hepatic metabolism via cytochrome P450 enzymes, yielding active metabolites that extend its duration. Highly lipophilic, it spreads to tissues like the heart and lungs, binding 98% to plasma proteins. Elimination occurs mostly through bile and feces, with about 25% exiting via urine as metabolites. The half-life ranges from six to ten hours, potentially increasing with liver issues, necessitating dose adjustments.

Indications for Use

The medication treats multiple cardiovascular disorders requiring precise management. It effectively lowers high blood pressure through its receptor-blocking properties. It’s also used for chronic heart failure, enhancing left ventricular performance and survival, especially in reduced ejection fraction cases. Following myocardial infarction, it stabilizes cardiac function in those with left ventricular issues, preventing further decline. Its dual impact on heart rate and vessel tone makes it valuable in these contexts, often part of broader treatment strategies.

Contraindications

Certain conditions prevent the use of this drug to avoid severe risks. Hypersensitivity to carvedilol or tablet components rules it out, as reactions might range from rashes to anaphylaxis. Severe asthma or chronic obstructive pulmonary disease with bronchospasm prohibits it due to beta-blockade effects. It’s not suitable for decompensated heart failure needing IV inotropes, nor for severe bradycardia, advanced atrioventricular block, or sick sinus syndrome without a pacemaker, where heart rate suppression could worsen outcomes. Significant liver impairment also bars its use due to metabolic reliance.

Method of Administration and Dosage

How to Take

Tablets are taken orally, preferably with food to improve absorption and reduce sudden blood pressure drops. Swallowing them whole with water ensures proper delivery. A regular daily schedule maintains consistent levels in the body.

Dosage for Adults and Children

Adults with hypertension often begin at 6.25 mg twice daily, increasing to 12.5 mg or 25 mg twice daily as needed, up to 50 mg daily maximum. For heart failure, 3.125 mg twice daily is typical, slowly raised to 25 mg twice daily if tolerated, based on stability. Post-myocardial infarction, 6.25 mg twice daily may adjust to 25 mg twice daily. Pediatric dosing is rare, starting at 0.1 mg per kilogram twice daily, with careful increases under specialist care.

Dose Adjustment in Specific Conditions

Renal impairment usually needs no change, as kidney excretion is minimal, though fluid status monitoring is wise. Liver dysfunction requires lower doses or avoidance, as slowed metabolism can raise drug levels. Elderly or low-weight patients may start lower to avoid excessive pressure or heart rate effects. Regular checks ensure dosing fits individual needs.

Side Effects

The medication may cause various unintended effects, varying in frequency. Dizziness or fatigue, often from blood pressure decreases, is common early on. Bradycardia might lead to weakness or cold hands and feet, especially in those with low baseline pulses. Some heart failure patients experience fluid retention or worsening symptoms, needing close oversight. Nausea, diarrhea, or stomach discomfort can occur but are usually mild. Rare serious reactions, like bronchospasm in susceptible people or notable liver enzyme rises, require urgent attention. Patient reports and check-ups manage these effectively.

Overdose

Symptoms of Overdose

Taking too much can cause severe hypotension, leading to dizziness, fainting, or circulatory failure from excessive vessel relaxation. Extreme bradycardia or heart block might result, risking cardiac arrest. Respiratory issues, such as wheezing or breathlessness, could affect vulnerable patients due to beta-blockade. Symptoms typically start within hours and worsen without care, showing the drug’s strong cardiovascular influence.

First Aid Measures

Stop the medication immediately in an overdose and seek urgent medical help. Recent ingestion may call for gastric lavage or charcoal under supervision to limit absorption. IV fluids and atropine can treat low pressure and slow heart rate, while bronchodilators like albuterol ease breathing issues. Continuous heart monitoring stabilizes the patient until recovery, focusing on normal pressure and rhythm.

Drug Interactions

Effects on Other Medications

This drug alters other medications’ effects when combined. It may boost antihypertensive actions, risking steep pressure drops, needing dose tweaks. With digoxin, it can raise levels, increasing toxicity odds, requiring plasma checks. Calcium channel blockers like verapamil or diltiazem might worsen bradycardia or heart block, needing careful use. It may also slow metabolism of cytochrome P450 2D6-processed drugs, like some antidepressants, affecting their performance. Adjustments and monitoring reduce these risks.

Compatibility with Alcohol and Food

Alcohol might heighten dizziness or drowsiness with the medication, especially from added pressure drops, so moderation is advised. Food enhances absorption, lessening sudden pressure changes, though high-fat meals may slightly delay peak effects. No major dietary limits apply, but balance aids results.

Special Precautions

Use During Pregnancy and Breastfeeding

The drug isn’t advised in pregnancy unless benefits outweigh risks, as animal data suggest fetal harm, though human evidence is scarce. It enters breast milk minimally, so nursing mothers should consult their doctor, possibly choosing alternatives to limit infant exposure.

Impact on Driving and Machinery Operation

Dizziness or fatigue, particularly at the start or dose adjustments, may affect driving or machinery use. Patients should test their response before such activities, ensuring safety.

Considerations for Elderly and Pediatric Populations

Older adults might need lower initial doses due to greater sensitivity to pressure and heart rate shifts, with regular tolerance checks. In children, use is uncommon and specialist-managed, with weight-based dosing monitored for developmental effects. Tailored care ensures safety and efficacy.