- Klíčová slova
- analgetická účinnost, kombinace analgetik,
- MeSH
- antiflogistika nesteroidní MeSH
- farmakoterapie statistika a číselné údaje MeSH
- financování organizované MeSH
- inhibitory cyklooxygenasy 2 MeSH
- klinické zkoušky jako téma MeSH
- kombinovaná terapie MeSH
- lidé MeSH
- neopioidní analgetika terapeutické užití MeSH
- preklinické hodnocení léčiv metody statistika a číselné údaje MeSH
- statistika jako téma MeSH
- výsledek terapie MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- Check Tag
- lidé MeSH
OBJECTIVES: There is good evidence that opioids can potentiate analgesic activity of some older non-opioid analgesics (such as paracetamol or ibuprofen) but it is not known whether this also holds true for newer non-opioid analgesics that selectively inhibit cyclooxygenase 2 (coxibs). This study was undertaken to determine the nature of the interaction between codeine and celecoxib or etoricoxib in peritoneal irritation-induced visceral pain in mice. For comparison, interactions of codeine with paracetamol and ibuprofen were also tested using the same method. MATERIAL AND METHODS: A small volume of a weak acetic acid (0.6%) was injected into the peritoneal cavity and the number of writhes (contractions of abdominal muscles) was counted. All drugs were given orally. Their interaction was characterized using isobolographic analysis. RESULTS: Codeine, etoricoxib, celecoxib, ibuprofen and paracetamol all independently produced dose-dependent suppression of writhing. The isobolographic analysis carried out using equipotent dose ratios showed that the interactions between codeine and etoricoxib or celecoxib were sub-additive or additive, respectively. This was in contrast to combinations of codeine with ibuprofen or paracetamol, which were supra-additive. Interaction indexes γ, determined as a ratio between experimental and theoretical ED50 values of the mixture, were as follows: 2.7 for codeine + etoricoxib, 0.62 for codeine + celecoxib, 0.43 for codeine + ibuprofen and 0.33 for codeine + paracetamol. CONCLUSIONS: These and other results suggest that opioids do not seem to potentiate analgesic effects of selective COX-2 inhibitors, in contrast to nonselective COX inhibitors or paracetamol.
- MeSH
- bolest chemicky indukované farmakoterapie MeSH
- ibuprofen terapeutické užití MeSH
- inbrední kmeny myší MeSH
- inhibitory cyklooxygenasy 2 terapeutické užití MeSH
- interpretace statistických dat MeSH
- kodein terapeutické užití MeSH
- kyselina octová škodlivé účinky MeSH
- lékové interakce MeSH
- modely u zvířat MeSH
- myši MeSH
- neopioidní analgetika terapeutické užití MeSH
- opioidní analgetika terapeutické užití MeSH
- paracetamol terapeutické užití MeSH
- pyrazoly terapeutické užití MeSH
- pyridiny terapeutické užití MeSH
- regresní analýza MeSH
- sulfonamidy terapeutické užití MeSH
- sulfony terapeutické užití MeSH
- synergismus léků MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- zvířata MeSH
- Check Tag
- mužské pohlaví MeSH
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- srovnávací studie MeSH
The aim of the present study was to evaluate and compare the analgesic activity and serum levels of meloxicam (CAS 71125-38-7) after administration of meloxicam associated with beta-cyclodextrin (BCD, CAS 7585-39-9) and unmodified meloxicam. The analgesic activity was measured using the plantar test (rats) and the writhing test (mice). In the plantar test, BCD-meloxicam (3 mg/kg and 10 mg/kg orally) showed higher analgesic activity than corresponding doses of meloxicam alone; in the writhing test BCD-meloxicam (7 mg/kg and 15 mg/kg orally) showed stronger analgesic activity than unmodified meloxicam. Serum levels of meloxicam were significantly higher, at 0.5 h and 1 h after administration of BCD-meloxicam orally than those of unmodified meloxicam (both dosed at 10 mg/kg). The present results suggest that association with beta-cyclodextrin increases the analgesic activity of meloxicam. This may be due to an icreased systemic bioavailability of meloxicam after oral administration of its complex with beta-cyclodextrin.
- MeSH
- analgetika farmakologie MeSH
- antiflogistika nesteroidní krev farmakologie MeSH
- beta-cyklodextriny krev MeSH
- bolest farmakoterapie MeSH
- hyperalgezie chemicky indukované MeSH
- karagenan MeSH
- krysa rodu rattus MeSH
- měření bolesti účinky léků MeSH
- myši MeSH
- potkani Wistar MeSH
- thiaziny krev farmakologie MeSH
- thiazoly krev farmakologie MeSH
- vény účinky léků fyziologie MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- mužské pohlaví MeSH
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
Methamphetamine is a commonly abused psychostimulant that causes addiction and is often abused by pregnant women. Acute or chronic administration of methamphetamine elevates the levels of the extracellular monoamine neurotransmitters, such as dopamine. The aim of the present study was to show whether prenatal exposure to methamphetamine (5mg/kg, entire gestation) or saline in Wistar rats induces changes in dopamine levels and its metabolites in the nucleus accumbens, and in behavior (locomotor activity, rearing, and immobility) after the administration of a challenge dose of methamphetamine (1mg/kg) or saline in male offspring. We found that adult offspring prenatally exposed to methamphetamine had higher basal levels of dopamine (about 288%), dihydroxyphenylacetic acid (about 67%) and homovanillic acid (about 74%) in nucleus accumbens. An increased basal level of dopamine corresponds to lower basal immobility in offspring prenatally exposed to methamphetamine. The acute injection of methamphetamine in adulthood increased the level of dopamine in the nucleus accumbens, which is related to an increase of locomotion and rearing (exploration). In addition, prenatally methamphetamine-exposed rats showed higher response to the challenge dose of methamphetamine, when compared to prenatally saline-exposed rats. In conclusion, rats exposed to methamphetamine in utero have shown changes in the mesolimbic dopaminergic system and were more sensitive to the administration of the acute dose of methamphetamine in adulthood.
- MeSH
- čas MeSH
- chování zvířat fyziologie účinky léků MeSH
- dopamin metabolismus MeSH
- inhibitory vychytávání adrenergních neurotransmiterů toxicita MeSH
- krysa rodu rattus MeSH
- kyselina 3,4-dihydroxyfenyloctová metabolismus MeSH
- kyselina homovanilová metabolismus MeSH
- methamfetamin toxicita MeSH
- modely nemocí na zvířatech MeSH
- nervové dráhy patofyziologie růst a vývoj účinky léků MeSH
- nucleus accumbens patofyziologie růst a vývoj účinky léků MeSH
- pátrací chování fyziologie účinky léků MeSH
- pohybová aktivita fyziologie účinky léků MeSH
- tegmentum mesencephali - area ventralis patofyziologie růst a vývoj účinky léků MeSH
- těhotenství MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- zpožděný efekt prenatální expozice metabolismus patofyziologie patologie MeSH
- zvířata MeSH
- Check Tag
- krysa rodu rattus MeSH
- mužské pohlaví MeSH
- těhotenství MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- práce podpořená grantem MeSH
- Publikační typ
- abstrakt z konference MeSH
