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

Basic Information

Drug ID DDPD01018 ...
Drug Name Guanfacine
Molecular Weight 246.093
Molecular Formula C9H9Cl2N3O
CAS Number 29110-47-2
SMILES NC(=N)NC(=O)CC1=C(Cl)C=CC=C1Cl
External Links
DRUGBANK DB01018
PubChem Compound 3519
PDR 2662
Drugs.com Drugs.com Drug Page

Experimental Physicochemical Property

Property Name Property Value Unit Raw Value Raw Unit Reference
Log P 0.857 - 0.857 - ChemSpider
Melting Point 214.5 ℃ 213-216 ℃ U.S. Patent 3,632,645.
Water Solubility 1000.0 mg/L 1 mg/ml FDA Label

Pharmacokinetic/ Toxicokinetic Property

Property Name Property Value Unit Raw Value Raw Unit Annotation Factor Reference
AUC 56.0 ng.h/ml 56±15 ng.h/ml PO, oral; immediate release formulation; DRUGBANK
AUC 32.0 ng.h/ml 32±9 ng.h/ml PO, oral; extended release formulation; DRUGBANK
Bioavailability 80.0 % 80 % PO, oral; DRUGBANK
C Max 2.5 ng/ml 2.5±0.6 ng/ml PO, oral; immediate release formulation; DRUGBANK
C Max 1.0 ng/ml 1.0±0.3 ng/ml PO, oral; extended release formulation; DRUGBANK
C Max 3.6 ng/ml 3.58±1.39 ng/ml PO, oral; adults; extended release formulation; DRUGBANK
C Max 2.6 ng/ml 2.6±1.03 ng/ml PO, oral; Children; extended release formulation; DRUGBANK
C Max 1.7 ng/ml 1.7±0.43 ng/ml PO, oral; Adolescents; extended release formulation; DRUGBANK
T Max 3.0 h 3 h PO, oral; immediate release formulation; DRUGBANK
T Max 6.0 h 6 h PO, oral; extended release formulation; DRUGBANK
T Max 5.5 h 5.5 h PO, oral; adults; extended release formulation; DRUGBANK
T Max 5.0 h 4.98 h PO, oral; Children; extended release formulation; DRUGBANK
T Max 5.0 h 4.96 h PO, oral; Adolescents; extended release formulation; DRUGBANK
Clearance 21.6 L/h 360±262 ml/min Total clearance; normal renal function; patients; DRUGBANK
Clearance 14.0 L/h 233±245 ml/min Renal clearance; normal renal function; patients; DRUGBANK
Clearance 18.5 L/h 308±274 ml/min Total clearance; Chronic Kidney Disease; DRUGBANK
Clearance 2.0 L/h 34±22 ml/min Renal clearance; Chronic Kidney Disease; DRUGBANK
Clearance 15.4 L/h 257±187 ml/min Total clearance; renal insufficiency; DRUGBANK
Clearance 1.1 L/h 18±15 ml/min Renal clearance; renal insufficiency; DRUGBANK
Clearance 0.27 L/h/kg 4.5 ml/min/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Volume of Distribution 6.3 L/kg 6.3 L/kg DRUGBANK
Volume of Distribution 5.6 L/kg 5.6 L/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Half-life 17.0 h 17(10-30) h renal insufficiency → ; DRUGBANK
Half-life 15.0 h 15 h intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Toxicity LD50 142.0 mg/kg 142.0 mg/kg PO, oral; Rattus, Rat; DRUGBANK
Toxicity LD50 15.3 mg/kg 15.3 mg/kg PO, oral; mouse; DRUGBANK
Toxicity LD50 114.0 mg/kg 114.0 mg/kg subcutaneous injection, SC; Rattus, Rat; DRUGBANK
Toxicity LD50 46.0 mg/kg 46.0 mg/kg subcutaneous injection, SC; mouse; DRUGBANK
Eliminate Route 57.0 % 57±32 % Urinary excretion; normal renal function; patients; DRUGBANK
Protein Binding 70.0 % ~70 % DRUGBANK

Maximum Dosage

Property Name Property Value Unit Raw Value Raw Unit Annotation Brand Name Component Reference
Max dose for children 4.0 mg/day 4 mg/day Tablet,PO，oral Tenex guanfacine hydrochloride PDR
Max dose for children 4.0 mg/day 4 mg/day PO, oral Tenex guanfacine hydrochloride PDR
Max dose for adolescents 7.0 mg/day 7 mg/day Tablet,PO，oral Tenex guanfacine hydrochloride PDR
Max dose for adolescents 3.5 mg/day 3.5 mg/day PO, oral Tenex guanfacine hydrochloride PDR
Max dose for adults 3.5 mg/day 3.5 mg/day PO, oral Tenex guanfacine hydrochloride PDR
Max dose for geriatric 3.5 mg/day 3.5 mg/day PO, oral Tenex guanfacine 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