Labetalol
Labetalol
Trandate, Normodyne (discontinued in US)
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Summary
Pharmacy
Starting dose
Oral: 100 mg PO BID, titrate to 400 mg BID. IV: 20 mg over 2 minutes, repeat 40-80 mg every 10 minutes as needed (maximum cumulative 300 mg); continuous infusion 2 mg/minute
Preparations
Tablets 100, 200, 300 mg; injection 5 mg/mL
US FDA Max
2400 mg/day (oral); 300 mg total per IV bolus dosing series
Pharmacology
Routes
Oral, intravenous
Onset
BP effect within hours (oral); 5-10 minutes (IV)
Duration
8-12 hours (oral); 4-6 hours (IV)
Half-life
~6-8 hours[1]
Bioavailability
~25% (oral; extensive first-pass)[1]
Pregnancy
Among the safest antihypertensives in pregnancy, recommended for chronic hypertension during pregnancy and first-line for severe hypertension in preeclampsia and eclampsia[1]
Legal status
Rx-only in US
Purported mechanism
Combined α1-adrenergic and non-selective β-adrenergic receptor antagonist with approximately 1:3 α:β ratio orally and 1:7 IV. The combined α and β blockade lowers blood pressure through two complementary mechanisms: reduced cardiac output and renin secretion (the β effect, shared with all β-blockers) plus reduced peripheral vascular resistance via vasodilation (the α effect, distinguishing labetalol from selective β-blockers).0 The favorable pregnancy safety profile and the dual mechanism support its first-line role in pregnancy-associated hypertension and in hypertensive emergencies where rapid, controllable BP reduction is needed[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Trandate (labetalol hydrochloride), Prometheus/Bausch, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/018716s022lbl.pdf