BLACK BOX WARNING
- abrupt withdrawal
carvedilol
Brand: Coreg
⚠ BBW Prototype Drug
Drug Class: beta-blocker
Drug Family: antihypertensive
Subclass: non-selective beta-blocker + alpha-1 blocker
Organ Systems: cardiovascular
Mechanism of Action
Non-selective beta-blocker with alpha-1 blockade; vasodilation offsets peripheral vasoconstriction; antioxidant properties.
beta-1 receptorbeta-2 receptoralpha-1 receptor
Indications
- heart failure (HFrEF)
- hypertension
- post-MI LV dysfunction
Contraindications
- decompensated HF
- cardiogenic shock
- severe bradycardia
- reactive airway disease (relative)
- severe hepatic impairment
Adverse Effects
Common
- dizziness
- fatigue
- hypotension (alpha-1)
- bradycardia
- weight gain
Serious
- bronchospasm
- heart block
Pharmacokinetics (ADME)
| Absorption | 25-35% bioavailability (extensive first-pass); food increases absorption |
| Distribution | highly lipophilic; large Vd |
| Metabolism | extensive hepatic CYP2D6, CYP2C9 |
| Excretion | fecal (>60%) |
| Half-life | 7-10 hours |
| Onset | 1-2 hours |
| Peak | 1-2 hours |
| Duration | 12 hours |
| Protein Binding | 98% |
| Vd | 115 L |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| CYP2D6 inhibitors (amiodarone, fluoxetine) | increased carvedilol levels | moderate |
| digoxin | additive bradycardia; carvedilol increases digoxin levels | moderate |
| clonidine | rebound hypertension risk on withdrawal | major |
Nursing Considerations
- Administer with food to slow absorption and reduce orthostatic hypotension
- Take apical pulse 1 min before; hold if <50 bpm
- CARVEDILOL (US Carvedilol) and COPERNICUS trials: mortality benefit in HFrEF
- Titrate dose slowly (double every 2 weeks as tolerated)
- Monitor for orthostatic hypotension (alpha-1 effect)
Clinical Pearls
- US Carvedilol trials + COPERNICUS: reduced mortality in HFrEF
- Alpha-1 blockade causes vasodilation — more hypotension than cardioselective beta-blockers
- Take with food to avoid first-dose hypotension
Safety Profile
Pregnancy use-with-caution
Lactation avoid
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.