Cyproheptadine (), sold under the brand name Periactin or Peritol, 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). It is also used to treat vasomotor mucosal edema, including vasomotor rhinitis and edema of the throat.
- It has shown effectiveness in the treatment of nightmares, including those related to post-traumatic stress disorder.
- It has been used 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.
- It can also be used as a preventive measure against migraine in children and adolescents. In Australia this is the only indication for which cyproheptadine is subsidised by the PBS.
- It can relieve SSRI-induced sexual dysfunction and drug-induced hyperhidrosis (excessive sweating).
- It is also used in the treatment of cyclical vomiting syndrome
- Use of the drug can stimulate the appetite and may lead to weight gain, which is helpful for underweight people.
- According to a small study, cyproheptadine hydrochloride has been found to improve sleep, calmness, and mood and energy levels, and to improve both negative and (sometimes even) positive psychotic symptoms in a subgroup of chronic schizophrenics who did not respond (either completely or sufficiently) to other therapies.
- Cyproheptadine may improve akathisia in patients on antipsychotic medications.
- In clinical trials in which cyproheptadine was used as an adjunct to antipsychotic treatment for patients with schizophrenia, an improvement in negative symptoms was seen.
Adverse effects
Adverse effects include
Research has shown a suppression of growth hormone with doses of 8-12 mg per day taken for 5 days.
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.
Pharmacology
Cyproheptadine is known to be an antagonist (or inverse agonist depending on the site in question) of the receptors listed in the table below.
Acronyms used:
RC - Cloned rat receptor.
MN - Mouse NG108-15 receptor.
Pharmacokinetics
Cyproheptadine is well-absorbed following oral ingestion, with peak plasma levels occurring after 1-3 hours. Its half-life when taken orally is approximately 8 hours.
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 has been used successfully in treatment of pituitary pars intermedia dysfunction in horses.
Source of the article : Wikipedia
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