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Rotoxamine: Full Drug Profile

Medically reviewed by Min Clinic Staff | Updated: January 2026

Rotoxamine - General Information

Rotoxamine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. In addition to the usual allergic symptoms, the drug also treats irritant cough and nausea, vomiting, and vertigo associated with motion sickness. Rotoxamine's anticholinergic action appears to be due to a central antimuscarinic effect, which also may be responsible for its antiemetic effects, although the exact mechanism is unknown. It also is used commonly to treat drug-induced extrapyramidal symptoms as well as to treat mild cases of Parkinson's disease.

 

Pharmacology of Rotoxamine

Rotoxamine is an antihistamine of the ethanolamine class. Ethanolamine antihistamines have significant antimuscarinic activity and produce marked sedation in most patients. In addition to the usual allergic symptoms, the drug also treats irritant cough and nausea, vomiting, and vertigo associated with motion sickness. It also is used commonly to treat drug-induced extrapyramidal symptoms as well as to treat mild cases of Parkinson's disease. Rather than preventing the release of histamine, as do cromolyn and nedocromil, carbinoxamine competes with free histamine for binding at HA-receptor sites. Rotoxamine competitively antagonizes the effects of histamine on HA-receptors in the GI tract, uterus, large blood vessels, and bronchial muscle. Ethanolamine derivatives have greater anticholinergic activity than do other antihistamines, which probably accounts for the antidyskinetic action of carbinoxamine.

 

Rotoxamine for patients

Avoid alcohol and other CNS depressants while taking these products. Patients sensitive to antihistamines may experience moderate to severe drowsiness. Patients sensitive to sympathomimetic amines may note mild CNS stimulation. While taking these products, exercise care in driving or operating appliances, machinery, etc.

 

Rotoxamine Interactions

Antihistamines may enhance the effects of tricyclic antidepressants, barbiturates, alcohol, and other CNS depressants. MAO inhibitors prolong and intensify the anticholinergic effects of antihistamines. Sympathomimetic amines may reduce the antihypertensive effects of reserpine, veratrum alkaloids, methyldopa and mecamylamine. Effects of sympathomimetics are increased with MAO inhibitors and beta adrenergic blockers.

 

Rotoxamine Contraindications

Patients with hypersensitivity or idiosyncrasy to any of its ingredients. Sympathomimetic amines are contraindicated in patients with severe hypertension, severe coronary artery disease and patients on monoamine oxidase (MAO) inhibitor therapy. Antihistamines are contraindicated in patients with narrow-angle glaucoma, urinary retention, peptic ulcer and during an asthma attack.

 

Additional information about Rotoxamine

Rotoxamine Indication: For symptomatic relief of seasonal and perennial allergic rhinitis and vasomotor rhinitis. Mechanism Of Action: Rotoxamine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Rotoxamine's anticholinergic action appears to be due to a central antimuscarinic effect, which also may be responsible for its antiemetic effects, although the exact mechanism is unknown. Drug Interactions: Not Available Food Interactions: Not Available Generic Name: Carbinoxamine Synonyms: Carbinoxamine Maleate; Paracarbinoxamine; Paracarinoxamine Drug Category: Antihistamines Drug Type: Small Molecule; Approved Other Brand Names containing Carbinoxamine: Allergefon; Clistin; Rotoxamine; Twiston; Absorption: Not Available Toxicity (Overdose): Not Available Protein Binding: Not Available Biotransformation: Not Available Half Life: 10 to 20 hours Dosage Forms of Rotoxamine: Tablet OralSyrup OralSolution / drops OralTablet, extended release Oral Chemical IUPAC Name: 2-[(4-chlorophenyl)-pyridin-2-ylmethoxy]-N,N-dimethylethanamine Chemical Formula: C16H19ClN2O Carbinoxamine on Wikipedia: https://en.wikipedia.org/wiki/Carbinoxamine Organisms Affected: Humans and other mammals