Abstract | PURPOSE: METHODS: RESULTS: In both solutions, CBZ rapidly suppressed seizures after intravenous bolus injection. Potent anticonvulsant activity was obtained as early as 30 s after injection, and peak effects were observed at approximately 3 min. ED50 for blockade of GTCS throughout the 30-min period of repeated electrical stimulation was approximately 7 mg/kg, similar to the potency of DZP in this model. Whereas the HP beta CD/CBZ solutions were tolerated by the animals, with no pronounced behavioral or motor adverse effects, the glycofurol/CBZ solutions induced marked sedation and motor impairment, indicating interactions between drug and solvent. Determination of CBZ in plasma and brain demonstrated that the rapid onset of anticonvulsant action after intravenous bolus injection was related to rapid drug penetration into brain tissue. CONCLUSIONS: An intravenous formulation of CBZ achieved through complexing with HP beta CD might be suitable for parenteral use in acute clinical conditions such as SE, particularly because CBZ has the advantage of being almost free of respiratory or cardiovascular adverse effects.
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Authors | W Löscher, D Hönack |
Journal | Epilepsia
(Epilepsia)
Vol. 38
Issue 1
Pg. 106-13
(Jan 1997)
ISSN: 0013-9580 [Print] United States |
PMID | 9024191
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Cyclodextrins
- Pharmaceutical Vehicles
- Solutions
- Solvents
- beta-Cyclodextrins
- 2-Hydroxypropyl-beta-cyclodextrin
- Carbamazepine
- Polyethylene Glycols
- glycofurol
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Topics |
- 2-Hydroxypropyl-beta-cyclodextrin
- Animals
- Carbamazepine
(administration & dosage, pharmacokinetics, therapeutic use)
- Cyclodextrins
(administration & dosage)
- Disease Models, Animal
- Drug Administration Schedule
- Electroshock
- Humans
- Injections, Intravenous
- Male
- Mice
- Pharmaceutical Vehicles
(administration & dosage)
- Polyethylene Glycols
(administration & dosage)
- Rats
- Solutions
- Solvents
(administration & dosage)
- Status Epilepticus
(etiology, prevention & control)
- beta-Cyclodextrins
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