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

Basic Information

Drug ID DDPD00678 ...
Drug Name Losartan
Molecular Weight 422.911
Molecular Formula C22H23ClN6O
CAS Number 114798-26-4
SMILES CCCCC1=NC(Cl)=C(CO)N1CC1=CC=C(C=C1)C1=CC=CC=C1C1=NNN=N1
External Links
DRUGBANK DB00678
PubChem Compound 3961
PDR 24322
Drugs.com Drugs.com Drug Page

Experimental Physicochemical Property

Property Name Property Value Unit Raw Value Raw Unit Reference
Log P 1.19 - 1.19 - https://www.accessdata.fda.gov/drugsatfda_docs/nda/2004/20-386S019_Cozaar_EAFONSI.pdf
Boiling Point 682.0 ℃ 682 ℃ http://www.chemspider.com/Chemical-Structure.3824.html
Melting Point 181.0 ℃ 178-184 ℃ http://www.chemspider.com/Chemical-Structure.3824.html
Water Solubility 1000.0 mg/L <1 mg/ml http://www.chemspider.com/Chemical-Structure.3824.html
pKa 5.5 - 5.5 - MERCK INDEX (1996); approx.

Pharmacokinetic/ Toxicokinetic Property

Property Name Property Value Unit Raw Value Raw Unit Annotation Factor Reference
Bioavailability 33.0 % 33 % PO, oral; DRUGBANK
Bioavailability 35.8 % 35.8±15.5 % PO, oral; The Pharmacological Basis of Therapeutics
C Max 225.0 ng/ml 200-250 ng/ml PO, oral; DRUGBANK
C Max 296.0 ng/ml 296±217 ng/ml Male, men; normal,healthy; The Pharmacological Basis of Therapeutics
C Max 249.0 ng/ml 249±74 ng/ml Active metabolite; Male, men; normal,healthy; The Pharmacological Basis of Therapeutics
T Max 1.0 h 1 h PO, oral; DRUGBANK
T Max 3.5 h 3-4 h PO, oral; Active metabolite; DRUGBANK
T Max 1.0 h 1.0±0.5 h Male, men; normal,healthy; The Pharmacological Basis of Therapeutics
T Max 4.1 h 4.1±1.6 h Active metabolite; Male, men; normal,healthy; The Pharmacological Basis of Therapeutics
Clearance 36.0 L/h 600.0 ml/min Plasma clearance; DRUGBANK
Clearance 4.5 L/h 75.0 ml/min Plasma clearance; DRUGBANK
Clearance 3.0 L/h 50.0 ml/min Plasma clearance; DRUGBANK
Clearance 1.5 L/h 25.0 ml/min Renal clearance; DRUGBANK
Clearance 0.49 L/h/kg 8.1±1.8 ml/min/kg hydrolysis; normal,healthy; Male, men; mild hepatic impairment ↓ ;moderate hepatic impairment ↓ ;RD, renal impairment, Renal disease，including uremia ↓ ; The Pharmacological Basis of Therapeutics
Clearance 0.49 L/h/kg 8.2 ml/min/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Volume of Distribution 34.4 L 34.4±17.9 L DRUGBANK
Volume of Distribution 10.3 L 10.3±1.1 L DRUGBANK
Volume of Distribution 0.45 L/kg 0.45±0.24 L/kg hydrolysis; normal,healthy; Male, men; The Pharmacological Basis of Therapeutics
Volume of Distribution 0.37 L/kg 0.37 L/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Half-life 2.0 h 1.5-2.5 h elimination half-life; DRUGBANK
Half-life 7.5 h 6-9 h Active metabolite; DRUGBANK
Half-life 2.5 h 2.5±1.0 h normal,healthy; Male, men; The Pharmacological Basis of Therapeutics
Half-life 5.4 h 5.4±2.3 h normal,healthy; Male, men; Active metabolite; Metabolite; The Pharmacological Basis of Therapeutics
Half-life 1.8 h 1.8 h intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Toxicity TDLo 1000.0 mg/kg 1000.0 mg/kg PO, oral; mouse; DRUGBANK
Toxicity TDLo 2000.0 mg/kg 2000.0 mg/kg PO, oral; Rattus, Rat; DRUGBANK
Toxicity TDLo 0.71 mg/kg/day 10.0 mg/kg/2W human, homo sapiens; Male, men; DRUGBANK
Toxicity TDLo 1.0 mg/kg/day 1.0 mg/kg/1D human, homo sapiens;  Female, women; DRUGBANK
Eliminate Route 35.0 % 35 % Urinary excretion; PO, oral; DRUGBANK
Eliminate Route 60.0 % 60 % Faeces excretion; PO, oral; DRUGBANK
Eliminate Route 45.0 % 45 % Urinary excretion; intravenous injection, IV; DRUGBANK
Eliminate Route 50.0 % 50 % Faeces excretion; intravenous injection, IV; DRUGBANK
Eliminate Route 4.0 % 4 % Urinary excretion; Oral single dose; Unchanged drug; DRUGBANK
Eliminate Route 12.0 % 12±2.8 % Urinary excretion; Male, men; normal,healthy; human, homo sapiens; Unchanged drug; The Pharmacological Basis of Therapeutics
Protein Binding 98.7 % 98.6-98.8 % DRUGBANK
Protein Binding 98.7 % 98.7 % Male, men; normal,healthy; human, homo sapiens; The Pharmacological Basis of Therapeutics
Protein Binding 99.8 % 99.8 % Active metabolite; Male, men; normal,healthy; human, homo sapiens; 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 1.4 mg/kg/day 1.4 mg/kg/day PO, oral Losartan Potassium losartan potassium PDR
Max dose for children 100.0 mg/day 100 mg/day PO, oral Losartan Potassium losartan potassium PDR
Max dose for adolescents 100.0 mg/day 100 mg/day PO, oral Losartan Potassium losartan potassium PDR
Max dose for adults 100.0 mg/day 100 mg/day PO, oral Losartan Potassium losartan potassium PDR
Max dose for elderly 100.0 mg/day 100 mg/day PO, oral Losartan Potassium losartan potassium 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