It seems that typically clonazepam is distributed mostly into peripheral circulation with poor uptake by the brain.
My question is: assuming one has pills or drops, is there a way to improve distribution into the systemic cirtculation/the brain ?
Some references:
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2846487/
'The nasal route opens up an avenue of possibilities for a drug to reach the brain. Clonazepam is highly metabolized with a poor uptake by the blood brain barrier via the peripheral circulation[1]. Hence, the objective of this investigation was to prepare brain-targeted gelatin-chitosan mucoadhesive microspheres to obtain rapid onset of action'
http://www.priory.com/pharmacy/clonazepam.htm
'Clonazepam is a drug of choice for various Central Nervous System (CNS) disorders. Out of that, it is commonly used for the treatment of status epileptics. The drug however does not reach the CNS in an efficient manner. The nasal route could be a possible solution to the problem, as many evidences have been reported for nose to brain targeting'
'Clonazepam (CZ) is a benzodiazepine derivative and is widely used in disorders like status epileptics, myoclonus and associated abnormal movements, panic attacks, psychiatric disorders. Presently, CZ is marketed as tablets and injectables. Though CZ is well absorbed following oral administration, it is extensively metabolized in the liver. The principle metabolite being 7- aminoclonazepam; which probably has little or no antiepileptic activity (Parfitt K, 1999). In addition to this, the tablets and injectables release the drug in peripheral circulation, with subsequent limited uptake by the Blood Brain Barrier (BBB). Moreover, these routes may become inconvenient or impractical depending upon the patient condition.'
My question is: assuming one has pills or drops, is there a way to improve distribution into the systemic cirtculation/the brain ?
Some references:
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2846487/
'The nasal route opens up an avenue of possibilities for a drug to reach the brain. Clonazepam is highly metabolized with a poor uptake by the blood brain barrier via the peripheral circulation[1]. Hence, the objective of this investigation was to prepare brain-targeted gelatin-chitosan mucoadhesive microspheres to obtain rapid onset of action'
http://www.priory.com/pharmacy/clonazepam.htm
'Clonazepam is a drug of choice for various Central Nervous System (CNS) disorders. Out of that, it is commonly used for the treatment of status epileptics. The drug however does not reach the CNS in an efficient manner. The nasal route could be a possible solution to the problem, as many evidences have been reported for nose to brain targeting'
'Clonazepam (CZ) is a benzodiazepine derivative and is widely used in disorders like status epileptics, myoclonus and associated abnormal movements, panic attacks, psychiatric disorders. Presently, CZ is marketed as tablets and injectables. Though CZ is well absorbed following oral administration, it is extensively metabolized in the liver. The principle metabolite being 7- aminoclonazepam; which probably has little or no antiepileptic activity (Parfitt K, 1999). In addition to this, the tablets and injectables release the drug in peripheral circulation, with subsequent limited uptake by the Blood Brain Barrier (BBB). Moreover, these routes may become inconvenient or impractical depending upon the patient condition.'
