- Molecular NameBalsalazide
- SynonymBalsalazida [Spanish]; balsalazide; Balsalazide disodium; Balsalazido [Spanish]; Balsalazidum [Latin]
- Weight357.322
- Drugbank_IDDB01014
- ACS_NO80573-04-2
- Show 3D model
- LogP (experiment)2.417
- LogP (predicted, AB/LogP v2.0)0.84
- pkaN/A
- LogD (pH=7, predicted)-4.11
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)0.45
- LogSw (predicted, AB/LogsW2.0)2.13
- Sw (mg/ml) (predicted, ACD/Labs)3.4
- No.of HBond Donors4
- No.of HBond Acceptors9
- No.of Rotatable Bonds7
- TPSA145.16
- StatusFDA approved
- AdministrationN/A
- PharmacologyAn anti-inflammatory drug used in the treatment of inflammatory bowel disease.
- Absorption_valueN/A
- Absorption (description)N/A
- Caco_2N/A
- Bioavailability1.0
- Protein binding99.0
- Volume of distribution (VD)4.5 L/h
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmBalsalazide is metabolised in the colon, by bacterial azoreductases, to 5-aminosalicyclic acid (5-ASA) which is responsible for the anti-inflammatory action, and 4-aminobenzoyl-β-alanine (4-ABA), an inert carrier. 25% of the released 5-ASA is inactivated in the colonic mucosa and liver to the N-acetylated metabolite, NASA. Likewise, 4-ABA becomes converted to its N-acetylated metabolite, NABA.
- Half lifeElimination half-life of NASA is 6 to 9 h, and of 5-ASA is approx. 1 h
- ExcretionIt is only NASA and NABA which are detected in urine; the parent drug is excreted mainly in faeces.
- Urinary ExcretionN/A
- Clerance4.5 L/h.
- ToxicityHypersensitivity reaction: a 59-year-old woman was administered with 2.25 g balsalazide 3 times a day and after 8 days, was admitted into hospital with central chest pain, shortness of breath and back pain, which worsened over the next 3 days. Examination showed a pyrexial, splinter haemorrhages in her fingernails, raised jugular venous pressure, a loud pericardial rub and a soft, tender liver. Balsalazide treatment was stopped and all symptoms were resolved within a month. [V. Adhiyaman et al.,BMJ,2000, 320, 613].
- LD50 (rat)N/A
- LD50 (mouse)N/A