Basic Information

Drug ID DDPD00598 ...
Drug Name Labetalol
Molecular Weight 328.4055
Molecular Formula C19H24N2O3
CAS Number 36894-69-6
SMILES CC(CCC1=CC=CC=C1)NCC(O)C1=CC(C(N)=O)=C(O)C=C1
External Links
DRUGBANK DB00598
T3DB T3D3517
PubChem Compound 3869
PDR 1568
Drugs.com Drugs.com Drug Page

Experimental Physicochemical Property

Property Name Property Value Unit Raw Value Raw Unit Reference
Boiling Point 552.7 552.7 http://www.chemspider.com/Chemical-Structure.3734.html
Melting Point 188.0 188 U.S. Patent 4,012,444.
pKa 9.3 - 9.3 - https://pubchem.ncbi.nlm.nih.gov/compound/Labetalol#section=Caco2-Permeability

Pharmacokinetic/ Toxicokinetic Property

Property Name Property Value Unit Raw Value Raw Unit Annotation Factor Reference
Bioavailability 48.5 % 11-86 % PO, oral; Age; food; Age ↑ ;food ↑ ; DRUGBANK
T Max 0.67 h 0.33-1 h DRUGBANK
T Max 2.0 h 2 h DRUGBANK
Clearance 90.0 L/h ~1500 ml/min Plasma clearance; DRUGBANK
Clearance 66.0 L/h 1100.0 ml/min Total clearance; DRUGBANK
Clearance 1.4 L/h/kg 23 ml/min/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Volume of Distribution 805.0 L 805.0 L patients; DRUGBANK
Volume of Distribution 467.5 L 188-747 L hypertension; patients; DRUGBANK
Volume of Distribution 4.8 L/kg 4.8 L/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Half-life 3.9 h 1.7-6.1 h DRUGBANK
Half-life 4.4 h 4.4 h intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Toxicity LD50 600.0 mg/kg 600.0 mg/kg PO, oral; mouse; DRUGBANK
Toxicity LD50 2000.0 mg/kg >2 g/kg PO, oral; Rattus, Rat; DRUGBANK
Toxicity LD50 55.0 mg/kg 50-60 mg/kg intravenous injection, IV; mouse; Rattus, Rat; DRUGBANK
Toxicity LD50 66.0 mg/kg 66.0 mg/kg intravenous injection, IV; parenteral administration; Rattus, Rat; T3DB
Eliminate Route 57.5 % 55-60 % Urinary excretion; DRUGBANK
Eliminate Route 19.5 % 12-27 % Faeces excretion; DRUGBANK
Protein Binding 50.0 % ~50 % DRUGBANK

Maximum Dosage

Property Name Property Value Unit Raw Value Raw Unit Annotation Brand Name Component Reference
Max dose for children 1.0 mg/kg/dose 1 mg/kg/dose intravenous injection, IV Labetalol Hydrochloride Injection labetalol hydrochloride PDR
Max dose for children 40.0 mg/dose 40 mg/dose intravenous injection, IV Labetalol Hydrochloride Injection labetalol hydrochloride PDR
Max dose for children 72.0 mg/kg/day 3 mg/kg/hour intravenous infusion, iv in drop Labetalol Hydrochloride Injection labetalol hydrochloride PDR
Max dose for adolescents 1.0 mg/kg/dose 1 mg/kg/dose intravenous injection, IV Labetalol Hydrochloride Injection labetalol hydrochloride PDR
Max dose for adolescents 40.0 mg/dose 40 mg/dose intravenous injection, IV Labetalol Hydrochloride Injection labetalol hydrochloride PDR
Max dose for adolescents 0.125 mg/kg/day 3 mg/kg/hour intravenous infusion, iv in drop Labetalol Hydrochloride Injection labetalol hydrochloride PDR
Max dose for adults 2400.0 mg/day 2400 mg/day PO, oral Labetalol Hydrochloride Injection labetalol hydrochloride PDR
Max dose for adults 300.0 mg/day 300 mg/day intravenous injection, IV Labetalol Hydrochloride Injection labetalol hydrochloride PDR
Max dose for geriatric 2400.0 mg/day 2400 mg/day PO, oral Labetalol Hydrochloride Injection labetalol hydrochloride PDR
Max dose for geriatric 300.0 mg/day 300 mg/day intravenous injection, IV Labetalol Hydrochloride Injection labetalol hydrochloride PDR

Drug Property Radar Chart

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Note: Center: Q1-1.5*IQR, Edge: Q3+1.5*IQR; Q1: Quantile 1, Q3: Quantile 3, IQR: Q3-Q1