BLACK BOX WARNING
- abrupt withdrawal
labetalol
Brand: Trandate, Normodyne
⚠ BBW Prototype: carvedilol
Drug Class: beta-blocker
Drug Family: antihypertensive
Subclass: non-selective beta-blocker + alpha-1 blocker
Organ Systems: cardiovascular
Mechanism of Action
Combined alpha-1 and non-selective beta-blockade; 3:1 beta:alpha oral, 7:1 IV; rapid vasodilation with maintained cardiac output.
beta-1 receptorbeta-2 receptoralpha-1 receptor
Indications
- hypertensive urgency/emergency (IV)
- hypertension
- hypertension in pregnancy
- pheochromocytoma (after adequate alpha block)
Contraindications
- asthma/COPD
- cardiogenic shock
- severe bradycardia
- high-degree AV block
- decompensated HF
Adverse Effects
Common
- dizziness
- fatigue
- hypotension
Serious
- bronchospasm
- severe hypotension with IV
- hepatotoxicity
Pharmacokinetics (ADME)
| Absorption | 25% oral bioavailability (first-pass) |
| Distribution | moderate lipophilicity |
| Metabolism | hepatic (conjugation) |
| Excretion | renal |
| Half-life | 5-8 hours |
| Onset | 5-10 min IV; 20-120 min oral |
| Peak | 2-4 hours oral |
| Duration | 8-12 hours |
| Protein Binding | 50% |
| Vd | 3-16 L/kg |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| cimetidine | increases labetalol bioavailability | moderate |
| halothane | additive hypotension | moderate |
Nursing Considerations
- IV used for hypertensive emergency — keep patient supine (orthostatic hypotension)
- Drug of choice for hypertension in pregnancy (IV)
- Monitor for bronchospasm in pulmonary disease
- IV infusion: titrate by 2 mg/min; maximum 300 mg total bolus
- Rare hepatotoxicity — monitor LFTs in long-term use
Clinical Pearls
- Preferred IV agent for hypertensive emergency in pregnancy
- Non-selective beta-blockade — avoid in asthma/COPD
- Unique in maintaining cardiac output due to alpha-1 vasodilation
Safety Profile
Pregnancy safe
Lactation use-with-caution
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.