Brand name Periactin.
A first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties.
US: B, no risk in non-human studies.
Protein bound 96 to 99%.
Metabolism is hepatic, and mostly CYP3A4 meditated.
Biological half-life is 8.6 hours.
Fecal excretion 2-20%, with 34% of this as unchanged drug.
Renal excretion, 40%.
Dose 4 mg tablets.
Used to treat allergic reactions, vasomotor mucosal edema, including vasomotor rhinitis and edema of the throat.
Effective 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, and serotonin-producing carcinoid tumor.
Used as a preventive measure against migraine in children and adolescents.
Can help in SSRI-induced sexual dysfunction, drug-induced hyperhidrosis, and in the treatment of cyclical vomiting syndrome.
Can stimulate the appetite and may lead to weight gain.
Can improve sleep, calmness, and mood and energy levels.
May improve akathisia in patients on antipsychotic medications, and can be used as an adjunct to antipsychotic treatment for patients with schizophrenia.
Adverse reactions include:
Sedation and sleepiness
Allergic manifestation of rash and edema
Blood dyscrasias such as leukopenia, agranulocytosis and thrombocytopenia
Hepatic side effects to get include:
– Hepatic failure
– Hepatic function abnormality
Anticholinergic side effects:
– Blurred vision
– Urinary retention
– Difficulty passing urine
– Nasal congestion
– Nasal or throat dryness
Thickening of bronchial secretions
Tightness of chest and wheezing
It suppresses growth hormone with doses of 8–12 mg per day taken for 5 days.
Gastric decontamination measures such as a
Activated charcoal are sometimes recommended in cases of overdose for gastric decontamination.
Overdose symptoms are usually indicative of CNS depression and excess anticholinergic side effects.
Well-absorbed following oral ingestion, with peak plasma levels occurring after 1–3 hours.
Its half-life when taken orally is approximately 8 hours.