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

Basic Information

Drug ID DDPD00440 ...
Drug Name Trimethoprim
Molecular Weight 290.3177
Molecular Formula C14H18N4O3
CAS Number 738-70-5
SMILES COC1=CC(CC2=CN=C(N)N=C2N)=CC(OC)=C1OC
External Links
DRUGBANK DB00440
PubChem Compound 5578
PDR 800
Drugs.com Drugs.com Drug Page

Experimental Physicochemical Property

Property Name Property Value Unit Raw Value Raw Unit Reference
Log P 0.91 - 0.91 - HANSCH,C ET AL. (1995)
Melting Point 201.0 ℃ 199-203 ℃ PhysProp
Water Solubility 400.0 mg/L 400 mg/L YALKOWSKY,SH & DANNENFELSER,RM 1992)
pKa 7.12 - 7.12 - PERRIN,DD (1972)
Log S -2.86 - -2.86 - ADME Research, USCD

Pharmacokinetic/ Toxicokinetic Property

Property Name Property Value Unit Raw Value Raw Unit Annotation Factor Reference
AUC 30000.0 ng.h/ml 30.0 mg.h/l Oral single dose; DRUGBANK
Bioavailability 63.0 % >63 % PO, oral; The Pharmacological Basis of Therapeutics
C Max 1000.0 ng/ml 1.0 ug/ml Oral single dose; DRUGBANK
C Max 2000.0 ng/ml 2.0 ug/ml Oral single dose; DRUGBANK
C Max 1200.0 ng/ml 1.2 mcg/ml Oral single dose; adults; normal,healthy; The Pharmacological Basis of Therapeutics
T Max 2.5 h 1-4 h Oral single dose; DRUGBANK
T Max 5.0 h 2-8 h Oral single dose; DRUGBANK
T Max 2.0 h 2.0 h Oral single dose; adults; normal,healthy; The Pharmacological Basis of Therapeutics
Tss 72.0 h 3.0 day Oral multiple dose; DRUGBANK
Metabolic 65.0 % 65 % DRUGBANK
Metabolic 25.0 % 25 % DRUGBANK
Clearance 4.3 L/h 51.7-91.3 ml/min DRUGBANK
Clearance 0.11 L/h/kg 1.9±0.3 ml/min/kg Children ↑ ;RD, renal impairment, Renal disease，including uremia ↓ ;Cystic fibrosis ↑ ; The Pharmacological Basis of Therapeutics
Clearance 0.13 L/h/kg 2.1 ml/min/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Volume of Distribution 1.6 L/kg 1.6±0.2 L/kg Neonates ↑ ;Children ↓ ;RD, renal impairment, Renal disease，including uremia → ;Cystic fibrosis → ; The Pharmacological Basis of Therapeutics
Volume of Distribution 1.5 L/kg 1.5 L/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Half-life 9.0 h 8-10 h RD, renal impairment, Renal disease，including uremia ↑ ; DRUGBANK
Half-life 10.0 h 10±2 h Children ↓ ;RD, renal impairment, Renal disease，including uremia ↑ ;Cystic fibrosis ↓ ;normal BMI → ; The Pharmacological Basis of Therapeutics
Half-life 9.6 h 9.6 h intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Toxicity LD50 2764.0 mg/kg 2764.0 mg/kg PO, oral; mouse; DRUGBANK
Toxicity LD50 5300.0 mg/kg >5300 mg/kg PO, oral; Rattus, Rat; DRUGBANK
Eliminate Route 55.0 % 50-60 % Urinary excretion; PO, oral; DRUGBANK
Eliminate Route 80.0 % ~80 % Urinary excretion; Unchanged drug; DRUGBANK
Eliminate Route 63.0 % 63±10 % Urinary excretion; Unchanged drug; Cystic fibrosis → ; The Pharmacological Basis of Therapeutics
Protein Binding 44.0 % 44 % plasma proteins; DRUGBANK
Protein Binding 37.0 % 37±5 % RD, renal impairment, Renal disease，including uremia → ;hypoalbuminemia Alb → ;Cystic fibrosis → ; The Pharmacological Basis of Therapeutics

Maximum Dosage

Property Name Property Value Unit Raw Value Raw Unit Annotation Brand Name Component Reference
Max dose for infants 10.0 mg/kg/day 10 mg/kg/day PO, oral Trimethoprim trimethoprim PDR
Max dose for infants 15.0 mg/kg/day 15 mg/kg/day PO, oral Trimethoprim trimethoprim PDR
Max dose for infants 15.0 mg/kg/day 15 mg/kg/day PO, oral Trimethoprim trimethoprim PDR
Max dose for children 10.0 mg/kg/day 10 mg/kg/day PO, oral Trimethoprim trimethoprim PDR
Max dose for children 400.0 mg/day 400 mg/day PO, oral Trimethoprim trimethoprim PDR
Max dose for children 15.0 mg/kg/day 15 mg/kg/day PO, oral Trimethoprim trimethoprim PDR
Max dose for adolescents 400.0 mg/day 400 mg/day PO, oral Trimethoprim trimethoprim PDR
Max dose for adolescents 15.0 mg/kg/day 15 mg/kg/day PO, oral Trimethoprim trimethoprim PDR
Max dose for adults 200.0 mg/day 200 mg/day PO, oral Trimethoprim trimethoprim PDR
Max dose for adults 15.0 mg/kg/day 15 mg/kg/day PO, oral Trimethoprim trimethoprim PDR
Max dose for geriatric 200.0 mg/day 200 mg/day PO, oral Trimethoprim trimethoprim PDR
Max dose for geriatric 15.0 mg/kg/day 15 mg/kg/day PO, oral Trimethoprim trimethoprim 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