Korektivní dermatologie provádí různé výkony, které jsou přinejmenším nepříjemné, mnohdy bolestivé. Proto je namístě použití sedace a analgézie. Ze sedativ jsou používány nejčastěji benzodiazepiny a propofol, k analgézii používáme fentanyl a jeho deriváty – alfentanil, sufentanil, remifentanil. Vzácněji je používáno disociativní anestetikum ketamin. Výhodou použití benzodiazepinů a opioidů je přítomnost specifického antagonisty, který umožňuje výbornou řiditelnost účinku. K inha-lační analgosedaci lze použít oxid dusný nebo methoxyfluran. Z anesteziologických technik se používá perorální sedace, sedace při vědomí, inhalační analgosedace. Kromě tradičních způsobů aplikace anestetik perorálně nebo intravenózně můžeme použít netradiční způsoby aplikace nazálně nebo transbukálně, které jsou neinvazivní. Dermatolog nebo zdravotní sestra mohou použít perorální seda-ci nebo inhalační analgosedaci oxidem dusným. Ostatní techniky vyžadují přítomnost anesteziologa.
Various procedures in corrective dermatology are often unpleasant or even painful. From this reason, analgesia and sedation are indicated. The most commonly used drugs for sedation are benzo-diazepines and propofol, for analgesia fentanyl and derivatives of fentanyl like alfentanil, sufentanil, remi-fentanil. Dissociative anaesthetic agent ketamine is rarely used. The main advantage of benzodiazepines and opioids is the possibility to use a specific antagonist enabling excellent control of effect. Inhalational anaesthetics nitrous oxide and methoxyflurane can be used for inhalational analgesic sedation. Anaesthe-tic techniques used are oral sedation, conscious sedation and inhalational analgesic sedation. Except of standard ways of administration of anaesthetics orally or intravenously, non-traditional non-invasive ways of administration, e.g. nasal or buccal can be used. Dermatologists and/or nurses can use oral sedation or inhalation of nitrous oxide only. The use of other techniques requires the presence of an anaesthetist.
- Keywords
- sedace, antagonizace, kombinace analgetik,
- MeSH
- Conscious Sedation * methods MeSH
- Anesthesia and Analgesia methods MeSH
- Administration, Intranasal MeSH
- Administration, Topical MeSH
- Administration, Oral MeSH
- Benzodiazepines antagonists & inhibitors administration & dosage pharmacology classification MeSH
- Flumazenil administration & dosage pharmacology MeSH
- Ketamine administration & dosage pharmacology MeSH
- Cosmetic Techniques MeSH
- Humans MeSH
- Midazolam administration & dosage MeSH
- Analgesics, Opioid administration & dosage pharmacology classification MeSH
- Nitrous Oxide pharmacokinetics pharmacology MeSH
- Half-Life MeSH
- Propofol administration & dosage pharmacology MeSH
- Drug Administration Routes * MeSH
- Check Tag
- Humans MeSH
- Publication type
- Review MeSH
Benzodiazepines have been widely used in clinical praxis for many decades. They act as GABAA receptor agonists and possess muscle-relaxant, hypnotic-sedative, anticonvulsant, and anxiolytic properties. Flumazenil acts as a benzodiazepine receptor antagonist (subunits α1, α2, α3, and α5) or partial agonist (subunits α4 and α6). It competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex, thereby reversing the effects of benzodiazepines. In our experiments, administration of flumazenil in rabbits was surprisingly associated with anxiolytic effects similar to those of midazolam. Additionally, flumazenil significantly and dose-dependently decreased the total number of vocalizations in rats, i.e. it was anxiolytic. These observations seem to be in contrast to the effect of flumazenil in humans, where it is believed to produce mainly anxiogenic effects. It seems that in individuals, who exhibit anxiogenic behavior or in individuals with anticipation anxiety, flumazenil acts as an anxiolytic agent, while in individuals without any signs of anxiety, flumazenil can also act as anxiogenic agent. Thus, we hypothesize that flumazenil is associated with decreased intensity of anticipatory anxiety due to occupancy of benzodiazepine binding sites by an endogenous ligand with inverse agonistic properties.
- MeSH
- GABA-A Receptor Antagonists administration & dosage pharmacology MeSH
- Anti-Anxiety Agents administration & dosage pharmacology MeSH
- Benzodiazepines antagonists & inhibitors metabolism MeSH
- Models, Biological * MeSH
- Flumazenil administration & dosage pharmacology MeSH
- Rabbits MeSH
- Humans MeSH
- Ligands MeSH
- Anxiety drug therapy MeSH
- Binding Sites MeSH
- Animals MeSH
- Check Tag
- Rabbits MeSH
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
Panická porucha patří mezi časté psychické problémy. Její léčba je dnes dostupná a účinná. Pomoci mohou psychofarmaka ze skupiny antidepresiv nebo anxiolytik. Antidepresiva (citalopram, fluoxetin, fluvoxamin, paroxetin, escitalopram, sertralin, venlafaxin, imipramin a klomipramin) jsou léky první volby. Benzodiazepiny jsou méně vhodné pro riziko vzniku závislosti. První volbou je také psychoterapie. Řadě pacientů může pomoci podpůrná, psychodynamická nebo skupinová psychoterapie. Ovšem o reálné efektivitě těchto přístupů nemáme dostatek informací, protože kontrolované studie chybějí. Prokázanou dlouhodobou efektivitu má kognitivně behaviorální terapie.
Panic disorder is common psychiatric disorders. Effective treatments are available. Pharmacological interventions include the possible use of a variety of agents. Antidepressants (citalopram, fluoxetine, fluvoxamine, paroxetine, escitalopram, sertralin, venlafaxin, imipramine, clomipramine), have emerged as primary interventions for the treatment of panic disorder. Benzodiazepines can also effective, but there are less useful because of high risk of dependence. The psychotherapy is the treatment of choice for this disorder. Supportive, psychodynamic or group psychotherapy alone or in addition to medication might be helpful for some of these patients. But real efficacy of these approaches is unknown yet because lack of controlled studies. On the other side cognitive-behavioral therapy demonstrated long term efficacy in most of the patients with panic disorders in many research studies.
- MeSH
- Antidepressive Agents, Tricyclic administration & dosage MeSH
- Benzodiazepines antagonists & inhibitors adverse effects MeSH
- Diagnosis, Differential MeSH
- Monoamine Oxidase Inhibitors administration & dosage MeSH
- Adrenergic Uptake Inhibitors administration & dosage MeSH
- Drug Therapy, Combination MeSH
- Comorbidity MeSH
- Crisis Intervention methods MeSH
- Humans MeSH
- Panic Disorder diagnosis physiopathology therapy MeSH
- Pathological Conditions, Signs and Symptoms MeSH
- Psychotherapy methods MeSH
- Selective Serotonin Reuptake Inhibitors administration & dosage MeSH
- Check Tag
- Humans MeSH
Flumazenil byl vyvinut v roce 1979 behem hledání specifických agonistu benzodiazepinových receptoru popsaných v roce 1977. Registrován byl v roce 1987 ve Švýcarsku firmou Roche pod firemním názvem Anexate jako antagonista úcinku benzodiazepinu.Vzhledem k jeho krátkému efektu byly hledány další deriváty. Výsledkem byl preparát Sarmazol užívaný ve veterinární medicíne a další látky využívané pouze experimentálne. Flumazenil byl používán v anesteziologii a intenzivní péci intenzivne v 80. a zacátkem 90. let minulého století, pozdeji jeho obliba i díky vysoké cene klesá. V clánku jsou rozebrány jednotlivé indikace flumazenilu: odstranení paradoxní reakce na midazolam a antagonizace sedace pri vedomí navozené midazolamem pri použití ruzných dávek. Bežná nitrožilní dávka 0,5 mg urychlí psychomotorické zotavení ze sedace midazolamem do 60 minut po aplikaci. Flumazenil lze podat i intranazálne nebo rektálne, zejména u detí. Zajímavým úcinkem flumazenilu je antagonizace sedace navozené halotanem, potenciace hypnotického úcinku propofolu a antinociceptivního úcinku morfinu.
Flumazenil was developed in 1979 during a search for new agonists of the benzodiazepine receptor discovered 2 years earlier in 1977. Flumazenil was registered as a benzodiazepine antagonist by Roche (brand name Anexate) in Switzerland in 1987. Similar drugs with longer duration of effect were tested but only Sarmazol is used and that is in veterinary anaesthesia. Other derivates are used in experiments only.The main boom of flumazenil use was in the 80s and early 90s, later on its popularity decreased because of its high cost and short-lasting effect. The main indications for flumazenil are a reversal of the paradoxical reaction to midazolam and antagonism of conscious sedation induced by the benzodiazepines. A common intravenous dose of 0.5 mg of flumazenil accelerates psychomotoric recovery from midazolam for 60 minutes. Intranasal and rectal applications of flumazenil have also been described mainly in children. Interesting effects of flumazenil include the reversal of halothane-induced sedation and the potentiation of the hypnotic effects of propofol and of the antinociceptive effect of morphine.
Acta anaesthesiologica scandinavica, ISSN 0515-2720 Supplement Vol. 39. 108
42 s. : tab., grafy ; 26 cm
- MeSH
- Benzodiazepines antagonists & inhibitors MeSH
- Flumazenil pharmacology MeSH
- Publication type
- Congress MeSH
- Conspectus
- Patologie. Klinická medicína
- NML Fields
- anesteziologie a intenzivní lékařství
- MeSH
- Drug Antagonism physiology MeSH
- Benzodiazepines antagonists & inhibitors pharmacokinetics therapeutic use MeSH
- Dihydropyridines antagonists & inhibitors pharmacokinetics therapeutic use MeSH
- Drug Incompatibility MeSH
- Cardiovascular Diseases drug therapy MeSH
- Humans MeSH
- Calcium contraindications metabolism drug effects MeSH
- Verapamil antagonists & inhibitors pharmacokinetics therapeutic use MeSH
- Check Tag
- Humans MeSH
- Publication type
- Review MeSH
- Keywords
- ANEXATE (HOFFMANN-LA ROCHE, ŠVÝCARSKO),
- MeSH
- Antidotes MeSH
- Benzodiazepines antagonists & inhibitors pharmacology therapeutic use MeSH
- Publication type
- Review MeSH
- Keywords
- RO 154513,
- MeSH
- Benzodiazepines antagonists & inhibitors MeSH
- Flumazenil pharmacokinetics pharmacology therapeutic use MeSH
- Publication type
- Review MeSH
