- Molecular NameTimolol
- SynonymTimolol maleate; Timololum [INN-Latin]
- Weight316.426
- Drugbank_IDDB00373
- ACS_NO26839-75-8
- Show 3D model
- LogP (experiment)1.91
- LogP (predicted, AB/LogP v2.0)1.71
- pka3.9
- LogD (pH=7, predicted)-0.91
- Solubility (experiment)2.74 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-0.26
- LogSw (predicted, AB/LogsW2.0)98.53
- Sw (mg/ml) (predicted, ACD/Labs)1.08
- No.of HBond Donors2
- No.of HBond Acceptors7
- No.of Rotatable Bonds7
- TPSA107.98
- StatusFDA approved
- AdministrationOral, Ophthalmic
- PharmacologyA non-selective beta-adrenergic receptor blocker. In its oral form (Blocadren), it is used to treat high blood pressure and prevent heart attacks, and occasionally to prevent migraine headaches. In its ophthalmic form (brand names Timoptol in Italy; Timoptic), it is used to treat open-angle and occasionally secondary glaucoma by reducing aqueous humour production through blockage of the beta receptors on the ciliary epithelium.
- Absorption_value95.0
- Absorption (description)N/A
- Caco_2-4.85
- Bioavailability61.0
- Protein binding10.0
- Volume of distribution (VD)1.7 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmTimolol is metabolized primarily by the polymorphic enzyme CYP2D6.
- Half life2.7 h
- ExcretionRenal
- Urinary Excretion8
- Clerance7.7 ml/min/kg
- ToxicitySymptoms of overdose include drowsiness, vertigo, headache, and atriventricular block.
- LD50 (rat)LD50=900 mg/kg
- LD50 (mouse)LD50=1190 mg/kg