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

Basic Information

Drug ID DDPD00343 ...
Drug Name Diltiazem
Molecular Weight 414.518
Molecular Formula C22H26N2O4S
CAS Number 42399-41-7
SMILES COC1=CC=C(C=C1)[C@@H]1SC2=C(C=CC=C2)N(CCN(C)C)C(=O)[C@@H]1OC(C)=O
External Links
DRUGBANK DB00343
T3DB T3D2758
PubChem Compound 39186
PDR 1387
Drugs.com Drugs.com Drug Page

Experimental Physicochemical Property

Property Name Property Value Unit Raw Value Raw Unit Reference
Caco-2 Permeability -4.38 - -4.38 - ADME Research, USCD
Log P 2.8 - 2.8 - Human Metabolome Database (HMDB)
Melting Point 187.5 ℃ 187-188 ℃ Kugita, H., Inoue, H., Ikezaki, M. and Takeo, S.; U.S. Patent 3,562,257; assigned to Tanabe Seiyaku Co.,Ltd., Japan.
Water Solubility 465.0 mg/L 465 mg/L MCFARLAND,JW ET AL. 2001)

Pharmacokinetic/ Toxicokinetic Property

Property Name Property Value Unit Raw Value Raw Unit Annotation Factor Reference
Bioavailability 40.0 % 40(24-74) % PO, oral; DRUGBANK
Bioavailability 38.0 % 38±11 % PO, oral; The Pharmacological Basis of Therapeutics
C Max 151.0 ng/ml 151±46 ng/ml Oral single dose; adults; normal,healthy; The Pharmacological Basis of Therapeutics
T Max 14.5 h 11-18 h PO, oral; DRUGBANK
T Max 4.0 h 4.0±0.4 h Oral single dose; adults; normal,healthy; The Pharmacological Basis of Therapeutics
Clearance 65.0 L/h ~65 L/h Total clearance; intravenous injection, IV; normal,healthy; Male, men; DRUGBANK
Clearance 48.0 L/h 48.0 L/h Total clearance; intravenous infusion, IV in drop; normal,healthy; Male, men; DRUGBANK
Clearance 0.71 L/h/kg 11.8±2.2 ml/min/kg Multiple dose; Elderly → ;RD, renal impairment, Renal disease，including uremia ↓ ; The Pharmacological Basis of Therapeutics
Clearance 0.78 L/h/kg 13 ml/min/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Volume of Distribution 305.0 L ~305 L Apparent volume of distribution; intravenous injection, IV; normal,healthy; Male, men; DRUGBANK
Volume of Distribution 3.3 L/kg 3.3±1.2 L/kg Elderly → ;RD, renal impairment, Renal disease，including uremia ↓ ; The Pharmacological Basis of Therapeutics
Volume of Distribution 4.1 L/kg 4.1 L/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Half-life 3.8 h ~3.0-4.5 h elimination half-life; Oral single dose; Oral multiple dose; hepatopathy，LD ↑ ;increasing doses ↑ ; DRUGBANK
Half-life 7.5 h 6-9 h elimination half-life; Single dose; Multiple dose; extended release formulation; DRUGBANK
Half-life 3.4 h 3.4 h elimination half-life; DRUGBANK
Half-life 4.4 h 4.4±1.3 h PO, oral; RD, renal impairment, Renal disease，including uremia → ;Age → ; The Pharmacological Basis of Therapeutics
Half-life 9.0 h 9±2 h Active metabolite; The Pharmacological Basis of Therapeutics
Half-life 7.5 h 7.5±1 h Active metabolite; The Pharmacological Basis of Therapeutics
Half-life 5.6 h 5.6 h intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Toxicity LD50 577.5 mg/kg 415-740 mg/kg PO, oral; mouse; DRUGBANK
Toxicity LD50 685.0 mg/kg 560-810 mg/kg PO, oral; Rattus, Rat; DRUGBANK
Toxicity LD50 50.0 mg/kg >50 mg/kg PO, oral; dog; DRUGBANK
Toxicity LD50 60.0 mg/kg 60.0 mg/kg intravenous injection, IV; mouse; DRUGBANK
Toxicity LD50 38.0 mg/kg 38.0 mg/kg intravenous injection, IV; Rattus, Rat; DRUGBANK
Toxicity LD50 740.0 mg/kg 740.0 mg/kg PO, oral; mouse; T3DB
Toxicity Lethal Dose 360.0 mg/kg 360.0 mg/kg monkey; DRUGBANK
Eliminate Route 3.0 % 2-4 % Urinary excretion; Unchanged drug; DRUGBANK
Eliminate Route 4.0 % <4 % Urinary excretion; Unchanged drug; The Pharmacological Basis of Therapeutics
Protein Binding 75.0 % ~70-80 % plasma proteins; DRUGBANK
Protein Binding 40.0 % ~40 % DRUGBANK
Protein Binding 30.0 % ~30 % DRUGBANK
Protein Binding 78.0 % 78±3 % The Pharmacological Basis of Therapeutics

Maximum Dosage

Property Name Property Value Unit Raw Value Raw Unit Annotation Brand Name Component Reference
Max dose for children 6.0 mg/kg/day 6 mg/kg/day PO, oral Cardizem CD diltiazem hydrochloride PDR
Max dose for children 360.0 mg/day 360 mg/day PO, oral Cardizem CD diltiazem hydrochloride PDR
Max dose for adolescents 6.0 mg/kg/day 6 mg/kg/day PO, oral Cardizem CD diltiazem hydrochloride PDR
Max dose for adolescents 360.0 mg/day 360 mg/day PO, oral Cardizem CD diltiazem hydrochloride PDR
Max dose for adults 480.0 mg/day 480 mg/day PO, oral Cardizem CD diltiazem hydrochloride PDR
Max dose for adults 540.0 mg/day 540 mg/day PO, oral Cardizem CD diltiazem hydrochloride PDR
Max dose for elderly 480.0 mg/day 480 mg/day PO, oral Cardizem CD diltiazem hydrochloride PDR
Max dose for elderly 540.0 mg/day 540 mg/day PO, oral Cardizem CD diltiazem 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