- Molecular NameRizatriptan
- SynonymMK 462 Free Base; Risatriptan; Rizatriptan benzoat; Rizatriptan benzoate
- Weight269.352
- Drugbank_IDDB00953
- ACS_NO145202-66-0
- Show 3D model
- LogP (experiment)2.129
- LogP (predicted, AB/LogP v2.0)1.91
- pkaN/A
- LogD (pH=7, predicted)0.22
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)0.04
- LogSw (predicted, AB/LogsW2.0)0.87
- Sw (mg/ml) (predicted, ACD/Labs)1.62
- No.of HBond Donors1
- No.of HBond Acceptors5
- No.of Rotatable Bonds5
- TPSA49.74
- StatusFDA approved
- AdministrationN/A
- PharmacologyA 5-HT1 agonist triptan drug developed by Merck & Co. for the treatment of migraine headaches.
- Absorption_value90.0
- Absorption (description)Rapid following oral administration. Bioavailability is 45%. Food has no effect on the bioavailability of rizatriptan. However, administering rizatriptan with food will delay by 1 hour the time to reach peak plasma concentration. The rate of absorption is not affected by the presence of a migraine attack.
- Caco_2N/A
- Bioavailability47.0
- Protein binding14.0
- Volume of distribution (VD)1.5 L/kg (Female) or 2.2 L/kg (Male)
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmRizatriptan is metabolized by monoamine oxidase A isoenzyme (MAO-A) to an inactive indole acetic acid metabolite. In addition, several other inactive metabolites are formed. An active metabolite, N-monodesmethyl-rizatriptan, with pharmacological activity similar to that of the parent compound has been identified in small concentrations (14%) in the plasma.
- Half life2.2 h (Female) or 2.4 (Male)
- Excretion82% urine; 12% faeces
- Urinary Excretion28.5
- Clerance12.3 ml/min/kg (Female) or 18.9 ml/min/kg (Male)
- ToxicitySymptoms of overdose include dizziness, fainting, heart and blood vessel problems, high blood pressure, loss of bowel and bladder control, slow heartbeat, and vomiting.
- LD50 (rat)N/A
- LD50 (mouse)N/A