Use of sublingual dexmedetomidine for the treatment of agitation
Inventors
Nandabalan, Krishnan • Yocca, Frank • Sharma, Sameer • NEGI, Harsh • Saini, Deepa
Assignees
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Publication Number
US-11786508-B2
Publication Date
2023-10-17
Expiration Date
Abstract
The present invention discloses a method of treating agitation or the signs of agitation in a subject comprising the sublingual administration of an effective amount of an alpha-2 adrenergic agonist, more particularly Dexmedetomidine, or a pharmaceutically acceptable salt thereof. The method is particularly suitable for the treatment of agitation associated with neurodegenerative and/or neuropsychiatric diseases. The present invention also discloses the sublingual administration of an alpha-2 adrenergic agonist, more particularly Dexmedetomidine or a pharmaceutically acceptable salt thereof at a dose that is effective to treat agitation or the signs of agitation in a subject, but does not cause significant sedation.
Core Innovation
The invention relates to treating agitation in an agitated subject by administering dexmedetomidine or a pharmaceutically acceptable salt of dexmedetomidine to the oral mucosa of the subject. The agitation is not perioperative agitation. The administration provides an anti-agitation effect in less than about 60 minutes after administration.
The method is configured to avoid also causing significant sedation after administration. The anti-agitation effect is associated with rapid onset while maintaining sedation control, including not exceeding Ramsay Sedation Scale Level 3 in the described context. Sublingual administration to the oral mucosa is emphasized, including embodiments in solid water-soluble dosage forms.
The described dosage-form approaches include administering dexmedetomidine in a solid water-soluble dosage form in the form of a film for oral mucosa delivery. Representative sublingual dosage-form types are described, including film and other oral mucosa delivery formats. The document additionally reports resident-intruder rat model observations showing dose-related reductions in aggressive or agitated behaviors and presents plasma concentration data over time windows aligned with behavioral response after sublingual versus IV dosing.
Claims Coverage
The document provides one independent claim defining a constrained method for treating agitation in a subject with schizophrenia using oral mucosa delivery of dexmedetomidine in a specific solid water-soluble film dosage form. The independent claim includes multiple key limitations: patient condition, route and dosage timing, dose, sedation constraint, onset constraint, agitation characterization, and dosage form identity. No other independent claims are provided in the provided partial content.
Rapid anti-agitation by oral mucosa dexmedetomidine without significant sedation
Administering to the oral mucosa of an agitated subject one or two single dosage administrations of 60 micrograms of dexmedetomidine (or a pharmaceutically acceptable salt thereof) without also causing significant sedation, wherein dexmedetomidine produces an anti-agitation effect in less than about 60 minutes after administration.
Treating non-perioperative agitation in a subject with schizophrenia
Treating agitation in an agitated subject having schizophrenia, wherein the agitation is not perioperative agitation.
Solid water-soluble film delivery for oral mucosa administration
Administering dexmedetomidine (or a pharmaceutically acceptable salt) in a solid, water-soluble dosage form and wherein the dosage form is a film.
Across the available claim set, the coverage centers on oral mucosa administration of 60 micrograms dexmedetomidine (or a pharmaceutically acceptable salt) that produces an anti-agitation effect in less than about 60 minutes while avoiding significant sedation, specifically for non-perioperative agitation in subjects with schizophrenia, using a solid water-soluble film dosage form.
Stated Advantages
Provides an anti-agitation effect in less than about 60 minutes after administration.
Does not also cause significant sedation after the administration.
Documented Applications
Treating agitation in an agitated subject having schizophrenia using oral mucosa administration of dexmedetomidine as a solid water-soluble film dosage form.
Non-perioperative agitation is specifically addressed.
Preclinical resident-intruder rat model use is documented for assessing reductions in aggressive or agitated behaviors and neutral behaviors after sublingual versus IV dosing.
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