Intranasal absorption of sumatriptan and naratriptan: No evidence of local transfer from the nasal cavities to the brain arterial blood in male rats
| Autor: | Elaine Starns, Niels Einer-Jensen, Sheila Schwartz, Stephanie Deprez, Lise Larsen |
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| Jazyk: | angličtina |
| Rok vydání: | 2001 |
| Předmět: |
Nasal cavity
Male Indoles Pharmaceutical Science Absorption Rats Sprague-Dawley Pharmacokinetics Piperidines medicine Animals Pharmacology (medical) Vein Pharmacology Naratriptan business.industry Sumatriptan General Medicine Cerebral Arteries Tryptamines Rats Serotonin Receptor Agonists medicine.anatomical_structure Anesthesia cardiovascular system Arterial blood Nasal administration Nasal Cavity business medicine.drug Artery |
| Zdroj: | Einer-Jensen, N, Larsen, L, Deprez, S, Starns, E & Schwartz, S 2001, ' Intranasal absorption of sumatriptan and naratriptan: No evidence of local transfer from the nasal cavities to the brain arterial blood in male rats ', J. Biopharmaceut. Drug Disposition, vol. 22, pp. 213-219 . https://doi.org/10.1002/bdd.281 |
| Popis: | Nasal administration to rats of small molecules (tritiated water, tyrosine, and propanol) results in a higher concentration in the brain arterial blood than in other arteries. The preferential distribution is based on a counter current transfer, which takes place between nasal vein blood and brain arterial blood in the cavernous sinus-carotid artery complex. This model was used to investigate whether the antimigraine 5HT1B/1D receptor agonists sumatriptan and naratriptan may also be transferred by the system. The ratio of ‘head’:‘heart’ plasma concentrations obtained from two carotid catheters after intranasal administration was not different from 1.00 for either compound, and thus, there was no experimental evidence of a preferential local transfer of drug from the nose to the carotid artery circulation. However, plasma concentrations increased from the first minute after intranasal dosing suggesting that sumatriptan and naratriptan are absorbed into the general systemic circulation from the nasal cavity in rats in a first-order fashion with no lag time. This is consistent with the clinical onset of efficacy of sumatriptan after an intranasal dose which occurs as early as 15 min post dose. Copyright © 2001 John Wiley & Sons, Ltd. |
| Databáze: | OpenAIRE |
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