Dimenhydrinate works by blocking histamine H1 receptors in the brain. Histamine is a chemical involved in the bodyâs response to allergens and also plays a role in regulating sleep and wakefulness. By inhibiting these receptors, dimenhydrinate reduces the activity in the inner ear that triggers nausea and vomiting. Additionally, its sedative effects can help calm the nervous system, making it effective in treating motion sickness.