Cyproheptadine

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Cyproheptadine, sold under the brand name Periactin among others, is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties.

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Medical uses

• Cyproheptadine is used to treat allergic reactions (specifically hay fever). The evidence for its use for this purpose in children is weak and ketotifen and loratadine showed equal or better results in the small trials in which they have been compared.
• It is sometimes used, especially in its liquid formulation, as a preventive measure against migraine in children and adolescents, but as of 2017 the evidence for this was weak. This use is on the label in the UK and some other countries. In Australia, this is the only indication for which cyproheptadine is subsidised by the PBS.
• It is also used off-label in the treatment of cyclical vomiting syndrome in infants; the only evidence for this use comes from retrospective studies.
• Cyproheptadine is sometimes used off-label to improve akathisia in people on antipsychotic medications.
• It used off-label to treat various dermatological conditions, including psychogenic itch drug-induced hyperhidrosis (excessive sweating), and prevention of blister formation for some people with epidermolysis bullosa simplex.
• One of the side effects of the drug is increased appetite and weight gain, which has led to its off-label use for this purpose in children who are wasting as well as people with cystic fibrosis. The evidence for the efficacy in light of other side effects is weak.
• It is sometimes used off-label in the management of moderate to severe cases of serotonin syndrome, a complex of symptoms associated with the use of serotonergic drugs, such as selective serotonin reuptake inhibitors and monoamine oxidase inhibitors), and in cases of high levels of serotonin in the blood resulting from a serotonin-producing carcinoid tumor.

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Adverse effects

Adverse effects include:

Overdose

Gastric decontamination measures such as activated charcoal are sometimes recommended in cases of overdose. The symptoms are usually indicative of CNS depression (or conversely CNS stimulation in some) and excess anticholinergic side effects. The LD₅₀ in mice is 123 mg/kg and 295 mg/kg in rats.

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Pharmacology

Cyproheptadine is a very potent antihistamine or antagonist of the H₁ receptor. At higher concentrations, it also has anticholinergic, antiserotonergic, and antidopaminergic activities. Of the serotonin receptors, it is an especially potent antagonist of the 5-HT₂ receptors, and this underlies its effectiveness in the treatment of serotonin syndrome.

Cyproheptadine is known to be an antagonist or inverse agonist of all of the receptors listed in the table to the right.

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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.

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Chemistry

Cyproheptadine is a tricyclic benzocycloheptene and is closely related to pizotifen and ketotifen as well as to tricyclic antidepressants.

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Research

Cyproheptadine was studied in one small (N=18) 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. It has also been studied as an adjuvant in two other trials in people with schizophrenia, around fifty people overall, and did not appear to have an effect.

There have been some trials to see if cyproheptadine could reduce sexual dysfunction caused by antipsychotics; it failed to show an effect.

As of 2012, descriptions of the use of cyproheptadine to reduce the number of nightmares in around 12 people with post-traumatic stress syndrome had been published; it appeared to be helpful in all of them.

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Veterinary use

Cyproheptadine is used in cats as an appetite stimulant and as an adjunct in the treatment of asthma. Possible adverse effects include excitement and aggressive behavior. The elimination half-life of cyproheptadine in cats is 12 hours.

Cyproheptadine is a second line treatment for pituitary pars intermedia dysfunction in horses.

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References

Source of the article : Wikipedia