Of the serotonin receptors, it is an especially potent antagonist of the 5-HT2 receptors. This is thought to underlie its effectiveness in the treatment of serotonin syndrome. However, it is possible that blockade of 5-HT1 receptors may also contribute to its effectiveness in serotonin syndrome. Cyproheptadine has been reported to block 85% of 5-HT2 receptors in the human brain at a dose of 4 mg three times per day (12 mg/day total) and to block 95% of 5-HT2 receptors in the human brain at a dose of 6 mg three times per day (18 mg/day total) as measured with positron emission tomography (PET). The dose of cyproheptadine recommended to ensure blockade of the 5-HT2 receptors for serotonin syndrome is 20 to 30 mg. Besides its activity at neurotransmitter targets, cyproheptadine has been reported to possess weak antiandrogenic activity. Pharmacokinetics
Cyproheptadine is well-absorbed following oral ingestion, with peak plasma levels occurring after 1 to 3 hours. Its terminal half-life when taken orally is approximately 8 hours. Chemistry
Cyproheptadine is a tricyclic benzocycloheptene and is closely related to pizotifen and ketotifen as well as to tricyclic antidepressants. Research
Cyproheptadine was studied in one small trial as an adjunct in people with schizophrenia whose condition was stable and were on other medication; while attention and verbal fluency appeared to be improved, the study was too small to draw generalizations from.
Familial nasal acilia is a rare congenital defect which is characterized by the complete absence of cilia on the epithelial cells of the respiratory tract. Symptoms are common within ones family and start as soon as one is born, with signs such as respiratory distress, dyspnea, lobar atelectasis, bronchiectasis and neo-natal pneumonia. Other symptoms that occur later in life include chronic moist coughing, chronic sinusitis, chronic otitis media, chronic rhinitis, and recurrence of upper and lower respiratory tract infections.Exact prevalence is unknown, OrphaNet estimates this condition to affect less than 1 out of every million people worldwide. R Soferman et al. described this disorder to be "autosomal recessive". == References ==