Dextrorphan (CAS 125-73-5) is the active metabolite of the antitussive agent dextromethorphan (CAS 125-71-3).The activity of dextrorphan, its specific pharmacol., acute toxicity and general pharmacol. in respect to the central nervous system were investigated in comparison to dextromethorphan.The studies showed that dextrorphan exerts an antitussive activity comparable to the one of dextromethorphan, but a better tolerability and a lower toxicity.These results suggest to use dextrorphan instead of its precursor dextromethorphan in therapy.

Arzneimittel-Forschung

Comparative pharmacokinetics of oral dextromethorphan and dextrorphan in the rabbit

Author: Caputo, R. ; Vimercati, M. G. ; Valenti, M. ; Ceriani, R. ; Citerio, L. ; Fossati, A.

The pharmacokinetics of dextromethorphan and its metabolite dextrorphan were compared.The drugs were administered orally at the same molar dose of 0.085 mmol/kg.Plasma levels of dextromethorphan, dextrorphan, and metabolites 3-hydroxymorphinan and 3-methoxymorphinan were determined by HPLC with fluorimetric detection.Dextromethorphan was rapidly and extensively metabolized and the plasma profiles of dextrorphan, administered directly or as metabolite of dextromethorphan, were similar.The concentrations of 3-hydroxymorphinan were higher after dextromethorphan than dextrorphan.3-Methoxymorphinan was detectable only 60 and 120 min after dextromethorphan.This work proposes the therapeutic use of the dextrorphan instead of its precursor dextromethorphan.

Acta Toxicologica et Therapeutica

Adrenergic effects of dopamine after nasal administration in the rat

Author: Bandi, G. ; Passarotti, C. ; Foschi, D. ; Fossati, A.

Intranasal administration of dopamine to anesthetized rats produced transient hypotension at low doses (2-50 mg/kg) due to a β-adrenergic effect and increases in blood pressure and heart rate at higher doses (100 mg/kg) due to stimulation of α-adrenergic and β-adrenergic systems, resp.Higher doses of dopamine are required to produce the cardiovascular effects on intranasal administration compared with i.v. administration.The use of promotors or carriers to modulate dopamine absorption by nasal mucosa is suggested.

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