- Molecular NameTelmisartan
- SynonymBIBR 277; BIBR 277SE; telmisartan
- Weight516.645
- Drugbank_IDDB00966
- ACS_NO144701-48-4
- Show 3D model
- LogP (experiment)7.245
- LogP (predicted, AB/LogP v2.0)6.19
- pkaN/A
- LogD (pH=7, predicted)3.52
- Solubility (experiment)Insoluble
- LogS (predicted, ACD/Labs)(ph=7)-6.26
- LogSw (predicted, AB/LogsW2.0)0.0
- Sw (mg/ml) (predicted, ACD/Labs)0.0
- No.of HBond Donors1
- No.of HBond Acceptors6
- No.of Rotatable Bonds7
- TPSA70.72
- StatusFDA approved
- AdministrationN/A
- PharmacologyAn angiotensin II receptor antagonist (ARB) used in the management of hypertension.
- Absorption_value50.0
- Absorption (description)Absolute bioavailability depends on dosage. Food slightly decreases the bioavailability (a decrease of about 6% is seen when the 40-mg dose is administered with food).
- Caco_2-4.82
- Bioavailability43.0
- Protein binding99.5
- Volume of distribution (VD)7.14 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmMinimally metabolized by conjugation to form a pharmacologically inactive acylglucuronide; the glucuronide of the parent compound is the only metabolite that has been identified in human plasma and urine. The cytochrome P450 isoenzymes are not involved in the metabolism of telmisartan.
- Half life24 h
- ExcretionFaecal 97%
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityIntravenous LD50 in rats is 150-200 mg/kg in males and 200 to 250 mg/kg in females. Acute oral toxicity is low: no deaths and no changes occurred in rats or dogs at 2000 mg/kg, the highest dose tested. Limited data are available with regard to overdosage in humans. The most likely manifestations of overdosage with telmisartan would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation.
- LD50 (rat)N/A
- LD50 (mouse)N/A