After a single 4 mg oral dose of 14C-labeled cyproheptadine HCl in normal subjects, given as tablets or syrup, 2-20% of the radioactivity was excreted in the stools. Only about 34% of the stool radioactivity was unchanged drug, corresponding to less than 5.7% of the dose. At least 40% of the administered radioactivity was excreted in the urine. No significant difference in the mean urinary excretion exists between the tablet and syrup formulations. No detectable amounts of unchanged drug were present in the urine of patients on chronic 12-20 mg daily doses of cyproheptadine syrup. The principle metabolite found in human urine has been identified as a quaternary ammonium glucuronide conjugate of cyproheptadine. Elimination is diminished in renal insufficiency.
Cyproheptadine is used in serotonin syndrome, a complex of symptoms
associated with selective serotonin reuptake inhibitors, especially
when taken in excess dose, meperidine and in the disease carcinoid
in which serotonin is overproduced by tumor cells. Cyproheptadine
in an useful alternative to benzodiazepine hypnotics in the treatment
of insomnia. Cyproheptadine may be superior to benzodiazepines in
the treatment of insomnia because cyproheptadine enhances sleep
quality and quantity whereas benzodiazepines tend to decrease sleep
quality.
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While not specifically used as a sedative, cyproheptadine causes sedation, likely due to its anti-histamine effects.[citation needed]
Digestive system: epigastric distress (dysphagia), loss of appetite, nausea, vomiting, (it is noted that these side effects are much more common in people with neuromuscular disorders)
Antihistamine overdosage reactions may vary from central nervous system depression to stimulation especially in children. Also, atropine-like signs and symptoms (dry mouth; fixed, dilated pupils; flushing, etc.) as well as gastrointestinal symptoms may occur.
If vomiting has not occurred spontaneously, the patient should be induced to vomit with syrup of ipecac.
If patient is unable to vomit, perform gastric lavage followed by activated charcoal. Isotonic or ? isotonic saline is the lavage of choice. Precautions against aspiration must be taken especially in infants and children.
Antihistamines may diminish mental alertness; conversely, particularly, in the young child, they may occasionally produce excitation. Patients should be warned about engaging in activities requiring mental alertness and motor coordination, such as driving a car or operating machinery.