Comparative Pharmacology
Head-to-head clinical analysis: CYPROHEPTADINE HYDROCHLORIDE versus PROMETHAZINE DM.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CYPROHEPTADINE HYDROCHLORIDE versus PROMETHAZINE DM.
CYPROHEPTADINE HYDROCHLORIDE vs PROMETHAZINE DM
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Cyproheptadine is a potent antihistamine (H1 receptor antagonist) and antiserotonergic agent (5-HT2 receptor antagonist). It also exhibits weak anticholinergic and sedative properties. It blocks histamine-mediated vasodilation, increased capillary permeability, and pruritus, as well as serotonin-mediated effects on appetite and mood.
Promethazine is a phenothiazine derivative that acts as a histamine H1 receptor antagonist, antiemetic via blockade of dopamine D2 receptors in the chemoreceptor trigger zone, and sedative via central anticholinergic effects. Dextromethorphan is an NMDA receptor antagonist and sigma-1 receptor agonist, suppressing cough by central action on the cough center.
4 mg orally three times daily; range 4-20 mg/day, not to exceed 0.5 mg/kg/day
2 teaspoonfuls (10 mL) orally every 4-6 hours, not to exceed 8 teaspoonfuls (40 mL) per 24 hours.
None Documented
None Documented
Terminal half-life approximately 8–16 hours in adults; may be prolonged in elderly or hepatic impairment.
16-19 hours (terminal); note: effect may last longer due to active metabolites and tissue binding
Primarily renal (appreciable unchanged drug and metabolites); biliary/fecal elimination minor (<5%).
Renal (70-80% as metabolites, <1% unchanged); biliary/fecal (20-30%)
Category A/B
Category A/B
Antihistamine
Antihistamine / Antiemetic