- Molecular NameCilastatin
- SynonymNA
- Weight358.459
- Drugbank_IDDB01597
- ACS_NO82009-34-5
- Show 3D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)-1.02
- pkaN/A
- LogD (pH=7, predicted)-2.03
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-0.96
- LogSw (predicted, AB/LogsW2.0)0.21
- Sw (mg/ml) (predicted, ACD/Labs)0.09
- No.of HBond Donors5
- No.of HBond Acceptors7
- No.of Rotatable Bonds11
- TPSA155.02
- StatusFDA approved
- AdministrationN/A
- PharmacologyA chemical compound which inhibits the human enzyme dehydropeptidase.
- Absorption_valueN/A
- Absorption (description)When compared to intravenous administration of imipenem-cilastatin sodium, imipenem is approximately 75% bioavailable following intramuscular administration while cilastatin is approximately 95% bioavailable. The absorption of imipenem from the intramuscular injection site continues for 6 to 8 hours while that for cilastatin is essentially complete within 4 hour.
- Caco_2N/A
- BioavailabilityN/A
- Protein binding35.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmCilastatin is primarily excreted in urine as either parent compound (75%) or undergoes intrarenal acetylation to N-acetyl cilastatin (12%).
- Half lifeN/A
- ExcretionN/A
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityThe most frequently reported systemic adverse clinical reactions that were reported as possibly, probably, or definitely related to Primaxin (Imipenem - Cilastatin combination) were nausea (0.6%), diarrhea (0.6%), vomiting (0.3%) and rash (0.4%). The LD50 of imipenem:cilastatin in at 1:1 ratio in mice and rats is approximately 1 g/kg/day.
- LD50 (rat)N/A
- LD50 (mouse)N/A