The pharmacokinetics of heptacaine, N-(2-(2-heptyloxyphenylcarbamoyloxy)ethyl)-piperidinium chloride, a new long-acting potent carbanilate type local anaesthetic, proposed for local anaesthesia in complex treatment of hemorrhoids, was studied following its rectal administration to rats in the form of cocoa butter suppositories. The heptacaine plasma concentration, 0.0083% of dose/ml, peaked at 90 min post administration and the maximum rate of its bioavailability, 0.19% of dose/min, assessed by deconvolution, occurred 38 min post administration. The plasma elimination half-life of heptacaine was 133 min and its biological availability of 52% was comparable to other agents of the class.

• MeSH
• anestetika lokální krev   farmakokinetika   MeSH
• aplikace rektální MeSH
• biologická dostupnost MeSH
• intestinální absorpce MeSH
• koncentrace vodíkových iontů MeSH
• krysa rodu Rattus MeSH
• piperidiny krev   farmakokinetika   MeSH
• potkani Wistar MeSH
• rektum metabolismus   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• anestetika lokální MeSH
• heptacaine MeSH Prohlížeč
• piperidiny MeSH

The potential involvement of increased mucus secretion in the antiulcer activity of a cytoprotective agent, pentacaine, and of the H2-antagonist ranitidine was studied in stressed rats. Cold-restraint stress decreased the gastric mucus content and induced haemorrhagic erosions in the stomach. Pretreatment with pentacaine and ranitidine dose-dependently diminished the extent of stress-induced gastric damage. Pentacaine prevented the depletion of mucus after stress, while ranitidine failed to affect it. In non-stressed rats only pentacaine was able to enhance mucus secretion. The stimulating effect of pentacaine on gastric mucus secretion may account for some of its antiulcer properties.

• MeSH
• fyzické omezení MeSH
• fyziologický stres etiologie   patologie   MeSH
• inbrední kmeny potkanů MeSH
• karbamáty farmakologie   terapeutické užití   MeSH
• karbenoxolon farmakologie   MeSH
• krysa rodu Rattus MeSH
• nízká teplota MeSH
• ranitidin farmakologie   terapeutické užití   MeSH
• žaludeční sliznice účinky léků   metabolismus   patologie   MeSH
• žaludeční vředy etiologie   prevence a kontrola   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• ženské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• karbamáty MeSH
• karbenoxolon MeSH
• pentacaine MeSH Prohlížeč
• ranitidin MeSH

The passage of 6 model drugs; acetylsalicylic acid, chloramphenicol, ethimizol, carbisocaine, heptacaine, and diazepam, through the blood-brain barrier, was determined in unirradiated control rats and in animals 1, 3, and 7 days after irradiation of the head only with a dose of 25 Gy from a 60Co source. The brain uptake index (BUI), which compares the uptake of the test substance with that of 3H2O 5 s after their injection into the common carotid artery, was significantly increased in comparison with unirradiated controls 7 days after irradiation, for all substances tested except for ethimizol. For acetylsalicylic acid and chloramphenicol it was also significantly increased in the other time intervals. The less lipophilic substances showed a greater relative increase of BUI than the more lipophilic ones.

• MeSH
• Aspirin farmakokinetika   MeSH
• chloramfenikol farmakokinetika   MeSH
• diazepam farmakokinetika   MeSH
• etimizol farmakokinetika   MeSH
• hematoencefalická bariéra účinky záření   MeSH
• inbrední kmeny potkanů MeSH
• karbamáty farmakokinetika   MeSH
• kraniální ozáření * MeSH
• krysa rodu Rattus MeSH
• mozek metabolismus   MeSH
• piperidiny farmakokinetika   MeSH
• radioizotopy kobaltu MeSH
• regresní analýza MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• Aspirin MeSH
• carbizocaine MeSH Prohlížeč
• chloramfenikol MeSH
• diazepam MeSH
• etimizol MeSH
• heptacaine MeSH Prohlížeč
• karbamáty MeSH
• piperidiny MeSH
• radioizotopy kobaltu MeSH