|Trade names||Periactin, others|
|Protein binding||96 to 99%|
|Metabolism||Liver Mostly CYP3A4 mediated.|
|Elimination half-life||8.6 hours|
|Excretion||Faecal (2-20%; 34% of this as unchanged drug) and renal (40%; none as unchanged drug)|
|Chemical and physical data|
|Molar mass||287.406 g·mol−1|
|3D model (JSmol)|
Cyproheptadine, sold under the brand name Periactin among others, is a first-generation antihistamine primarily used to treat allergies. This may include itchiness, hay fever, and hives. It is taken by mouth.
Common side effects include sleepiness, dizziness, agitation, and poor coordination. Other side effects may include swelling, problems urinating, and increased weight. There is no evidence of harm with use during pregnancy, however such use has not been well studied. Care should be taken in those at risk of glaucoma.
Cyproheptadine was patented in 1959 and came into medical use in 1961. It is available as a generic medication. In the United Kingdom 30 tablets of 4 mg costs the NHS about 6 pounds in 2020. This amount in the United States costs about 10 USD.
Cyproheptadine is used to treat allergic reactions (specifically hay fever). While effective for this purpose, second generation antihistamines such as ketotifen and loratadine have shown equal results with fewer side effects.
It is also used to prevent migraines. A 2013 study found a reduced rate within 7 to 10 days. The average frequency before use was 8.7 times per month, this was decreased to 3.1 times per month at 3 months after the start of treatment. This use is on the label in the UK and some other countries.
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 effects of the drug is increased appetite and weight gain, which has led to its use (off-label in the USA) for this purpose in children who are wasting as well as people with cystic fibrosis.
It is also 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.
The typical dose is 4 mg three times per day in adults.
- Sedation and sleepiness (often transient)
- Disturbed coordination
- Allergic manifestation of rash and edema
- Acute labyrinthitis
- Diplopia (seeing double)
- Hypotension (low blood pressure)
- Anaphylactic shock
- Hemolytic anemia
- Blood dyscrasias such as leukopenia, agranulocytosis and thrombocytopenia
- Liver effects such as:
- - Blurred vision
- - Constipation
- - Xerostomia (dry mouth)
- - Tachycardia (high heart rate)
- - Urinary retention
- - Difficulty passing urine
- - Nasal congestion
- - Nasal or throat dryness
- Urinary frequency
- Early menses
- Thickening of bronchial secretions
- Tightness of chest and wheezing
- Increased appetite
- Weight gain
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.
|Values are Ki (nM). The smaller the value,|
the more strongly the drug binds to the site.
The ↓ and ↑ indicate antagonist and
agonist type actions respectively.
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 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. 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 SSRI and antipsychotic medications.
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.
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