- Molecular NameButorphanol
- SynonymButorfanol; Butorfanol [INN-Spanish]; Butorphanol Tartrate; Butorphanolum [INN-Latin]
- Weight327.468
- Drugbank_IDDB00611
- ACS_NO42408-82-2
- Show 2D model
- LogP (experiment)4.176
- LogP (predicted, AB/LogP v2.0)3.29
- pka8.6
- LogD (pH=7, predicted)1.36
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-1.99
- LogSw (predicted, AB/LogsW2.0)0.34
- Sw (mg/ml) (predicted, ACD/Labs)0.31
- No.of HBond Donors2
- No.of HBond Acceptors3
- No.of Rotatable Bonds2
- TPSA43.7
- StatusFDA approved
- AdministrationIV, intranasal
- PharmacologyA morphinan-type synthetic opioid analgesic.
- Absorption_valueN/A
- Absorption (description)Well absorbed after oral or IM administration.
- Caco_2N/A
- Bioavailability17.0
- Protein binding81.5
- Volume of distribution (VD)12 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmIt undergoes extensive first-pass metabolism, mainly by hydroxylation, dealkylation, and conjugation. The major metabolite is 3′-hydroxybutorphanol.
- Half life18 h
- ExcretionAbout 70% of a dose is excreted in the urine and 13% eliminated in the faeces in 5 days. In 24 h, 5 to 10% of a dose is excreted in the urine as unchanged drug, 5 to 10% as free and conjugated norbutorphanol, and about 50% as 3′-hydroxybutorphanol.
- Urinary Excretion1.9
- Clerance40 ml/min/kg
- ToxicityThe clinical manifestations of butorphanol overdose are those of opioid drugs in general. The most serious symptoms are hypoventilation, cardiovascular insufficiency, coma, and death.
- LD50 (rat)N/A
- LD50 (mouse)N/A