• Molecular NameCyproheptadine
  • SynonymNA
  • Weight287.406
  • Drugbank_IDDB00434
  • ACS_NO129-03-3
  • Show 2D model
  • LogP (experiment)N/A
  • LogP (predicted, AB/LogP v2.0)4.66
  • pkaN/A
  • LogD (pH=7, predicted)3.07
  • Solubility (experiment)Soluble
  • LogS (predicted, ACD/Labs)(ph=7)-2.64
  • LogSw (predicted, AB/LogsW2.0)0.0
  • Sw (mg/ml) (predicted, ACD/Labs)0.01
  • No.of HBond Donors0
  • No.of HBond Acceptors1
  • No.of Rotatable Bonds0
  • TPSA3.24
  • StatusFDA approved
  • AdministrationN/A
  • PharmacologyAn antihistaminic/anticholinergic and antiserotonergic agent. It acts as a 5-HT2 receptor antagonist and also blocks calcium channels.
  • Absorption_value80.0
  • Absorption (description)Absorbed after oral administration and extensively distributed throughout the tissues.
  • Caco_2N/A
  • BioavailabilityN/A
  • Protein binding97.5
  • Volume of distribution (VD)N/A
  • Blood/Plasma Partitioning ratio (D_blood)N/A
  • MetabollsmMetabolised by aromatic ring hydroxylation, N-demethylation, heterocyclic ring oxidation, and glucuronic acid conjugation; the major metabolite in urine is a quaternary ammonium glucuronide conjugate.
  • Half life1~4 h
  • ExcretionAbout 67 to 77% of a dose is excreted in the urine in 6 days, the remainder being eliminated in the faeces. Of the excreted material, 58 to 65% is conjugated with glucuronic acid, 9 to 11% is conjugated with sulfate, 20 to 26% is excreted as polar material not hydrolysable by glucuronidase or sulfatase, and about 5% is unconjugated.
  • Urinary ExcretionN/A
  • CleranceN/A
  • ToxicityAs for all antihistamines, Cyproheptadine administration may result in the following adverse events. Central Nervous System: Sedation and sleepiness (often transient), dizziness, disturbed coordination, confusion, restlessness, excitation, nervousness, tremor, irritability, insomnia, paresthesias, neuritis, convulsions, euphoria, hallucinations, hysteria, faintness. Integumentary: Allergic manifestation of rash and edema, excessive perspiration, urticaria, photosensitivity. Special Senses: Acute labyrinthitis, blurred vision, diplopia, vertigo, tinnitus. Cardiovascular: Hypotension, palpitation, tachycardia, extrasystoles, anaphylactic shock. Hematologic: Hemolytic anemia, leukopenia, agranulocytosis, thrombocytopenia. Digestive System: Dryness of mouth, epigastric distress, anorexia, nausea, vomiting, diarrhea, constipation, jaundice. Genitourinary: Urinary frequency, difficult urination, urinary retention, early menses. Respiratory: Dryness of nose and throat, thickening of bronchial secretions, tightness of chest and wheezing, nasal stuffiness. Miscellaneous: Fatigue, chills, headache, increased appetite/weight gain.
  • LD50 (rat)N/A
  • LD50 (mouse)LD50=64 (ip); LD50=56.2 (intraperitoneal)