Každé rozšíření léčebných možností antidepresivních látek zvyšuje šanci na volbu antidepresiva, které je nejen účinné, ale i dobře tolerované. Nové antidepresivum vortioxetin se vyznačuje kombinovaným antidepresivním a anxiolytickým účinkem. Vortioxetin působí prostřednictvím antagonizace receptorů 5-HT3 a 5-HT7, agonizace receptorů 5-HT1A, částečné agonizace receptorů 5-HT1B a inhibice serotoninového transportéru. Klinické studie ukazují, že vortioxetin je účinný v léčbě deprese, i když neexistuje žádný náznak převahy nad aktivním komparátorem. Jeho použití může přinášet klinicky významné výhody z hlediska snášenlivosti.
Each extension of treatment options of antidepressant drugs increases the chance to choose an antidepressant that is not only effective but also well tolerated. The new antidepressant vortioxetine has combined antidepressant and anxiolytic effect on the serotonin neurotransmitter system; it antagonizes -5-HT3, and 5-HT7 receptors, agonizes the 5-HT1A receptors, partially agonizes 5-HT1B receptors and acts as an inhibitor of the serotonin transporter. Clinical studies indicate that vortioxetine is effective in the treatment of depression, though there is no suggestion of superiority over active comparators. There may be a clinically meaningful advantage in terms of tolerability.
- MeSH
- Serotonin 5-HT1 Receptor Agonists MeSH
- Serotonin 5-HT1 Receptor Antagonists MeSH
- Antidepressive Agents * therapeutic use MeSH
- Anti-Anxiety Agents therapeutic use MeSH
- Depression * drug therapy MeSH
- Diketopiperazines administration & dosage pharmacokinetics adverse effects therapeutic use MeSH
- Adult MeSH
- Drug Evaluation MeSH
- Clinical Trials as Topic MeSH
- Cognition MeSH
- Drug Interactions MeSH
- Humans MeSH
- Longitudinal Studies MeSH
- Meta-Analysis as Topic MeSH
- Prospective Studies MeSH
- Receptor, Serotonin, 5-HT1A MeSH
- Receptor, Serotonin, 5-HT1B MeSH
- Receptors, Serotonin, 5-HT3 MeSH
- Medication Reconciliation MeSH
- Aged MeSH
- Sulfides administration & dosage pharmacokinetics adverse effects therapeutic use MeSH
- Vortioxetine MeSH
- Check Tag
- Adult MeSH
- Humans MeSH
- Male MeSH
- Aged MeSH
- Female MeSH
Monoaminergic neurotransmitter 5-hydroxytryptamine (5-HT), also known as serotonin, plays important roles in modulating the function of the olfactory system. However, thus far, the knowledge about 5-HT and its receptors in olfactory receptor neurons (ORNs) and their physiological role have not been fully characterized. In the present study, reverse transcription-polymerase chain reaction (RT-PCR) analysis revealed the presence of 5-HT(1A) and 5-HT(1B) receptor subtypes in mouse olfactory epithelium at the mRNA level. With subtype selective antibodies and standard immunohistochemical techniques, both receptor subtypes were found to be positively labeled. To further elucidate the molecular mechanisms of 5-HT act on the peripheral olfactory transduction, the whole-cell patch clamp techniques were used on freshly isolated ORNs. We found that 5-HT decreased the magnitude of outward K(+) current in a dose-dependent manner and these inhibitory effects were markedly attenuated by the 5-HT(1A) receptor blocker WAY-100635 and the 5-HT(1B) receptor antagonist GR55562. These data suggested that 5-HT may play a role in the modulation of peripheral olfactory signals by regulating outward potassium currents, both 5-HT(1A) and 5-HT(1B) receptors were involved in this regulation.
- MeSH
- Serotonin 5-HT1 Receptor Antagonists pharmacology MeSH
- Olfactory Receptor Neurons drug effects metabolism MeSH
- Potassium Channels drug effects metabolism MeSH
- Membrane Potentials MeSH
- RNA, Messenger metabolism MeSH
- Mice MeSH
- Receptor, Serotonin, 5-HT1A drug effects genetics metabolism MeSH
- Receptor, Serotonin, 5-HT1B drug effects genetics metabolism MeSH
- Serotonin metabolism MeSH
- Signal Transduction MeSH
- Animals MeSH
- Check Tag
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
V otevřené klinické studii autoři srovnávali konvenční perorální sumatriptan 50?mg s rychlorozpustnou formou sumatriptanu 50?mg. Na souboru 70 pacientů (66 žen a 4 muži) hodnotili účinek obou léků ve 4 po sobě následujících záchvatech. Hodnotili rychlost nástupu úlevy od bolesti a významné zlepšení bolesti. Dále sledovali nežádoucí účinky a tzv. časnou intervenci. Sumatriptan s rychlou dezintegrací tablety měl rychlejší nástup úlevy od bolesti a byl rovněž účinnější než konvenční sumatriptan. Autoři doporučují novou rychlorozpustnou formu sumatriptanu pro léčbu migrenózních záchvatů, zejména v případě rychlého rozvoje bolesti nebo zvracení.
- Keywords
- Rosemig Sprintab,
- MeSH
- Administration, Oral MeSH
- Drug Therapy methods trends utilization MeSH
- Data Interpretation, Statistical MeSH
- Migraine Disorders drug therapy MeSH
- Receptor, Serotonin, 5-HT1B therapeutic use MeSH
- Receptor, Serotonin, 5-HT1D therapeutic use MeSH
- Sumatriptan MeSH
- Publication type
- Comparative Study MeSH
Zavedení triptanů, specifických selektivních agonistů 5-HT1B/1D receptorů, představuje výrazný pokrok v akutní léčbě migrény. Triptany našly široké uplatnění v léčbě záchvatů zejména střední a silné intenzity, významně zkrátily průměrnou délku záchvatu a v porovnání s nespecifickými antimigreniky znamenají i ekonomickou úsporu. Určité rozdíly v účinnosti a snášenlivosti mezi jednotlivými triptany umožňují léčbu přizpůsobit konkrétnímu pacientovi.
Introduction of triptans, specific selective agonists 5-HT1B/1D receptors, represent a significant progress in acute treatment of migraine. Triptans found a broad application in the treatment, especially for moderate and severe migraine attacks, significantly shortened average length of migraine attack. When compared to non-specific antimigraine drugs, triptans lead to the economical savings. Differences in efficacy and safety among the triptans make the individually tailored therapy possible.
- MeSH
- Pharmacologic Actions MeSH
- Research Support as Topic MeSH
- Conflict, Psychological MeSH
- Rats MeSH
- Methamphetamine pharmacology metabolism MeSH
- Receptor, Serotonin, 5-HT1B therapeutic use drug effects MeSH
- Social Behavior MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Animals MeSH
- Publication type
- Comparative Study MeSH
- MeSH
- Serotonin 5-HT1 Receptor Agonists MeSH
- Aggression psychology drug effects MeSH
- Research Support as Topic MeSH
- Methamphetamine pharmacokinetics metabolism MeSH
- Mice psychology MeSH
- Receptor, Serotonin, 5-HT1B MeSH
- Social Behavior MeSH
- Animals MeSH
- Check Tag
- Mice psychology MeSH
- Animals MeSH
- Publication type
- Comparative Study MeSH
Current medical research and opinion, ISSN 0300-7995 vol. 21, suppl. 3, 2005
24 s. : il., tab. ; 28 cm
- MeSH
- Serotonin 5-HT1 Receptor Agonists MeSH
- Acute Disease MeSH
- Clinical Medicine MeSH
- Drug Delivery Systems methods trends MeSH
- Migraine Disorders drug therapy MeSH
- Receptor, Serotonin, 5-HT1A administration & dosage therapeutic use MeSH
- Receptor, Serotonin, 5-HT1D administration & dosage therapeutic use MeSH
- Receptors, Serotonin, 5-HT1 therapeutic use MeSH
- Tryptamines administration & dosage pharmacokinetics therapeutic use MeSH
- Publication type
- Collected Work MeSH
- Conspectus
- Farmacie. Farmakologie
- NML Fields
- neurologie
- farmacie a farmakologie
- farmakoterapie
