Basic Information Experimental Physicochemical Property Pharmacokinetic/Toxicokinetic Property Maximum Dosage Drug Property Radar Chart

Basic Information

Drug ID DDPD00297 ...
Drug Name Bupivacaine
Molecular Weight 288.4277
Molecular Formula C18H28N2O
CAS Number 38396-39-3
SMILES CCCCN1CCCCC1C(=O)NC1=C(C)C=CC=C1C
External Links
DRUGBANK DB00297
T3DB T3D2742
PubChem Compound 2474
PDR 1482
Drugs.com Drugs.com Drug Page

Experimental Physicochemical Property

Property Name Property Value Unit Raw Value Raw Unit Reference
Log P 3.41 - 3.41 - HANSCH,C ET AL. (1995)
Melting Point 107.5 ℃ 107-108 ℃ PhysProp
Water Solubility 2400.0 mg/L 2400 mg/L YALKOWSKY,SH & DANNENFELSER,RM 1992)
pKa 8.1 - 8.1 - DRUGBANK

Pharmacokinetic/ Toxicokinetic Property

Property Name Property Value Unit Raw Value Raw Unit Annotation Factor Reference
C Max 800.0 ng/ml 0.8 mcg/ml epidural administration; adults; patients; The Pharmacological Basis of Therapeutics
T Max 0.34 h 0.17-0.5 h epidural administration; adults; patients; The Pharmacological Basis of Therapeutics
Clearance 0.43 L/h/kg 7.1±2.8 ml/min/kg Total clearance; normal,healthy; Male, men; Children ↑ ;Elderly ↓ ; The Pharmacological Basis of Therapeutics
Clearance 0.26 L/h/kg 4.3 ml/min/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Volume of Distribution 0.90 L/kg 0.9±0.4 L/kg Steady state volume of distribution; normal,healthy; Male, men; Children ↑ ; The Pharmacological Basis of Therapeutics
Volume of Distribution 0.84 L/kg 0.84 L/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Half-life 2.7 h 2.7 h adults; DRUGBANK
Half-life 8.1 h 8.1 h Neonates; DRUGBANK
Half-life 2.4 h 2.4±1.2 h Children → ;Age → ; The Pharmacological Basis of Therapeutics
Half-life 3.1 h 3.1 h intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Toxicity LD50 7.0 mg/kg 6-8 mg/kg intravenous injection, IV; monkey; DRUGBANK
Toxicity LD50 41.5 mg/kg 38-45 mg/kg subcutaneous injection, SC; monkey; DRUGBANK
Toxicity LD50 7.0 mg/kg 6-8 mg/kg intravenous injection, IV; mouse; T3DB
Toxicity LD50 46.0 mg/kg 38-54 mg/kg subcutaneous injection, SC; mouse; T3DB
Toxicity Lethal Dose 4.4 mg/kg 4.4 mg/kg monkey; DRUGBANK
Toxicity Lethal Dose 4.5 mg/L 4.5 ug/ml monkey; DRUGBANK
Eliminate Route 6.0 % 6 % Urinary excretion; Unchanged drug; DRUGBANK
Eliminate Route 2.0 % 2±2 % Urinary excretion; Unchanged drug; The Pharmacological Basis of Therapeutics
Protein Binding 95.0 % 95 % DRUGBANK
Protein Binding 95.0 % 95±1 % Neonates ↓ ; The Pharmacological Basis of Therapeutics

Maximum Dosage

Property Name Property Value Unit Raw Value Raw Unit Annotation Brand Name Component Reference
Max dose for adults 266.0 mg 266 mg Transdermal preparations Exparel bupivacaine liposome PDR
Max dose for adults 133.0 mg 133 mg epidural administration Exparel bupivacaine liposome PDR
Max dose for geriatric 266.0 mg 266 mg Transdermal preparations Exparel bupivacaine liposome PDR
Max dose for geriatric 133.0 mg 133 mg epidural administration Exparel bupivacaine liposome PDR
Max dose for children 175.0 mg/dose 175 mg/dose Marcaine Spinal bupivacaine hydrochloride PDR
Max dose for children 400.0 mg/day 400 mg/day Marcaine Spinal bupivacaine hydrochloride PDR
Max dose for children 90.0 mg/procedure 90 mg/procedure Marcaine Spinal bupivacaine hydrochloride PDR
Max dose for children 75.0 mg 75 mg Marcaine Spinal bupivacaine 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