A non sedating
A method of providing a neuroprotectant to a human comprising administering a therapeutically effective amount of a pharmaceutical composition of a salt of 5,5-diphenyl barbituric acid to the human, wherein the human is undergoing cardiac surgery or carotid endartectomy, or has experienced cerebral ischemia, a cerebral aneurysm, or head trauma, and is at risk for atrial fibrillation, transient ischemic attack (TIA), bacterial endocarditis, ischemic stroke, head trauma or subarachnoid hemorrhage. This invention differs from the prior art in the recognition of specific compounds, their modifications and dosages that are effective in neuroprotection but that were not previously recognized.
In summary, the invention involves non-sedating barbiturates such as for example 1,3-dimethoxymethyl 5,5-diphenyl-barbituric acid (DMMDPB), 1-monomethoxymethyl 5,5-diphenylbarbituic acid (MMMDPB) and diphenyl-barbituric acid (DPB) and their precursors, derivatives and analogs, and their administration over a range of dosages that result in a range of blood levels and brain levels of these drugs and their metabolites making them useful as neuroprotectants.
The pharmacist sends all these prescriptions to the Prescription Pricing Authority, which under conditions of full confidentiality, provides electronic copies of the exposure data to the Drug Safety Research Unit.
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Toxic Mechanism: They are less sedating due to the fact they are less lipophilic and do not cross the blood-brain-barrier as easily.
They selectively inhibit the peripheral H1 receptors and therefore have a lower affinity for the central H1, muscarinic, alpha adrenergic and serotingeric (5-HT) receptors that the sedating anti-histamines do.