- Molecular NameGuanethidine
- SynonymGuanethidine Monosulfate; Guanethidine Sulphae
- Weight198.314
- Drugbank_IDDB01170
- ACS_NO55-65-2
- Show 3D model
- LogP (experiment)0.693
- LogP (predicted, AB/LogP v2.0)0.81
- pka9, 12
- LogD (pH=7, predicted)-2.3
- Solubility (experiment)Soluble
- LogS (predicted, ACD/Labs)(ph=7)0.7
- LogSw (predicted, AB/LogsW2.0)3.7
- Sw (mg/ml) (predicted, ACD/Labs)6.72
- No.of HBond Donors4
- No.of HBond Acceptors4
- No.of Rotatable Bonds4
- TPSA65.14
- StatusFDA approved
- AdministrationN/A
- PharmacologyAn antihypertensive drug that reduces the release of catecholamines, such as noradrenaline. Its mechanism is inhibition of the Na+ATPase dependent pump.
- Absorption_valueN/A
- Absorption (description)Incompletely absorbed after oral administration.
- Caco_2N/A
- Bioavailability20.0
- Protein bindingN/A
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmGuanethidine is converted by the liver to three metabolites, which are excreted in the urine. The metabolites are pharmacologically less active than the parent compound.
- Half life4~8 days
- ExcretionUp to about 25% of an oral dose is excreted in the urine in 24 h as unchanged drug and two metabolites, guanethidine N-oxide and 2-(6-carboxyhexylamino)ethylguanidine; the proportion of metabolites to unchanged drug is variable. A total of about 40% of an oral dose is excreted in the urine in 9 days and about 40 to 47% is eliminated in the faeces as unchanged drug in 6 days.
- Urinary ExcretionN/A
- CleranceN/A
- ToxicitySide effects include drowsiness, dizziness, tiredness or confusion.
- LD50 (rat)N/A
- LD50 (mouse)LD 50=1000 mg/kg