KeywordsReceptor Antagonist Immune Cell Sexual Behavior Social Work School Psychology
Antihistamines are a class of drugs that inhibit histamine, a neurotransmitter involved in mood and behavior regulation, by either (a) blocking the action of histamine at the receptor, (b) competing with histamine for binding to the receptor, or (c) displacing histamine from the receptor. In the field of ASD, the majority of interest surrounds mirtazapine and cyproheptadine, both nonselective H1 receptor (histamine receptor) inverse agonists (similar to antagonist). Mirtazapine specifically shows promise in treating inappropriate sexual behaviors associated with autism. However, the mechanism of action of both these drugs in the context of ASD is likely to be through antihistamines’ off-target highly potent antagonism of α-adrenergic receptors (fight-or-flight response) and/or serotonin (mood regulation) receptors as opposed to the H1 receptor. Antihistamines may be useful in the treatment of sleeping problems associated with autism; however, evidence suggests a greater effectiveness in this regard in typically developing children.
Histamine’s more prominent role is as an inflammation mediator, increasing permeability of blood vessels to immune cells. In concordance, antihistamines are normally used in the treatment of allergies by blocking histamine-induced vasodilation and swelling. Common side effects include dry mouth, drowsiness, dizziness, nausea, and vomiting.
References and Readings
- Akhondzadeh, S., Erfani, S., Mohammadi, M. R., Tehrani-Doost, M., Amini, H., Gudarzi, S. S., & Yasamy, M. T. (2004). Cyproheptadine in the treatment of autistic disorder: A double-blind placebo-controlled trial. Journal of Clinical Pharmacy and Therapeutics, 29(2), 145–150.PubMedCrossRefGoogle Scholar
- Stone, C. A., Wenger, H. C., Ludden, C. T., Stavorski, J. M., & Ross, C. A. (1961). Antiserotonin-antihistaminic properties of cyproheptadine. Journal of Pharmacology and Experimental Therapeutics, 131(1), 73–84.Google Scholar